3-ethylidenehydrazine-substituted heterocyclic compounds as thrombopoietin receptor activators

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (1), their tautomers and pharmaceutically acceptable salts. The disclosed compounds have thromobopoietin receptor agonist properties. In formula (1) , A is a nitrogen atom or CH, when A is a nitrogen atom, B is NR9 (where R9 is a C1-10 alkyl group), and when A is CH, B is a sulphur atom, R1 is a phenyl group (the phenyl group is substituted with one or more substitutes selected from a group consisting of halogen atoms, C1-10 alkyl groups and C1-10 alkoxy groups (C1-10 alkyl groups and C1-10 alkoxy groups are unsubstituted or substituted with one or more halogen atoms)), L1 is bond, X is OH, R2 is a C1-10 alkyl group, L2 is a bond, L3 is NH, L4 is a bond or NH, Y is a sulphur atom, and when L4 is a bond, R3 is a piperidinyl group, a piperazinyl group (the piperidinyl group and the piperazinyl group are substituted with substitutes selected from a group containing C1-10 alkoxycarbonyl groups, carboxyl group, hydroxyl groups, di-C1-10 alkylaminocarbonyl groups, C1-10 alkylaminocarbonyl groups and C1-10 alkyl groups (C1-10 alkylaminocarbonyl groups and C1-10 alkyl groups are substituted with a substitute selected from a group containing pyridyl groups, hydroxyl groups and carboxyl groups)), or when L4 is NH, R3 is a C1-10 alkyl group (C1-10 alkyl group is substituted with a substitute selected from a group containing C1-10 alkoxy groups, C1-10 alkoxycarbonyl groups or carboxyl groups).

EFFECT: obtaining a thrombopoietin receptor activator which is a formula (1) compound and a medicinal agent which contains the disclosed compound as an active ingredient.

10 cl, 3 tbl, 47 ex

 

BACKGROUND of INVENTION

The technical field

The present invention relates to preventive, therapeutic and improving agents having affinity and agonistic action on the receptor thrombopoetin, for diseases for which effective activation of the receptor thrombopoetin. In particular, it relates to pharmaceutical compositions containing compounds that increase the number of platelets by stimulating differentiation and proliferation of hematopoietic stem cells, megakaryocytic of progenitor cells and megakaryocytes or compounds for therapeutic angiogenesis or with antiarteriosclerotic action, which stimulate differentiation and proliferation of vascular endothelial cells and endothelial progenitor cells.

The level of technology

Thrombopoetin is a cytokine that consists of 332 amino acids, which increases the production of platelets by stimulating differentiation and proliferation of hematopoietic stem cells, megakaryocytic of progenitor cells and megakaryocytes, mediated by its receptors, and therefore is a promising interest as a drug for Hematology the breach is. Recent reports that it stimulates the differentiation and proliferation of vascular endothelial cells and endothelial progenitor cells, increased assumptions concerning therapeutic angiogenesis, protivoateroskleroticheskim actions and prevention of cardiovascular diseases (for example, non-patent document 1, non-patent document 2 and non-patent document 3).

Regulates the production of platelets by using receptor thrombopoetin biologically active compounds known to date include, in addition to thrombopoetin, low molecular weight peptides having affinity towards the receptor of thrombopoietin (for example, patent document 1, patent document 2, patent document 3 and patent document 4).

Search ones low molecular weight compounds that increase the production of platelet-mediated receptor thrombopoetin it was reported that low molecular weight compounds having affinity towards the receptor (for example, patent document 5, patent document 26).

1) Patent applications filed Hokuriku Seiyaku Co., Ltd., related to the derivatives of 1,4-benzodiazepine (patent documents 5 and 6).

2) International laid patent application Shionogi & Co., Ltd. (patent documents 7-10).

3) international is e lined a patent application, filed by SmithKline Beecham Corp (patent documents 11-19).

4) Posted patent Japan filed Torii Pharmaceutical Co., Ltd. (patent document 20).

5) international laid patent application filed by Roche Diagnostics GMBH (patent document 21).

6) international laid patent application Yamanouchi Pharmaceutical Co., Ltd. (patent document 22 and 23).

7) Posted patent Japan filed Japan Tabacco Inc. (patent document 24).

8) Posted a patent Japan filed by Nissan Chemical Industries, Ltd. (patent documents 25 and 26).

Patent document 1 JP-A-10-72492

Patent document 2 WO96/40750

Patent document 3 WO96/40189

Patent document 4 WO98/25965

Patent document 5 JP-A-11-1477

Patent document 6 JP-A-11-152276

Patent document 7 WO01/07423

Patent document 8 WO01/53267

Patent document 9 WO02/059099

Patent document 10 WO02/059100

Patent document 11 WO00/35446

Patent document 12 WO00/66112

Patent document 13 WO01/34585

Patent document 14 WO01/17349

Patent document 15 WO01/39773

Patent document 16 WO01/21180

Patent document 17 WO01/89457

Patent document 18 WO02/49413

Patent document 19 WO02/085343

Patent document 20 JP-A-2001-97948

Patent document 21 WO99/11262

Patent document 22 WO02/062775

Patent document 23 WO03/062233

Patent document 24 JP-A-2003-238565

Patent documents the UNT 25 WO04/033433

Patent document 26 WO04/108683

Non-patent document 1: Microvasc. Res., 1999: 58, p.108-113

Non-patent document 2: Circ. Res., 1999: 84, p.785-796

Non-patent document 3: Blood 2001:98, p.71a-72a

Description of the INVENTION

Thrombopoetin and low molecular weight peptides having affinity towards the receptor of thrombopoietin probably break down in the gastrointestinal tract, and they are usually difficult to be administered orally. As for thrombopoetin, reported on the appearance of antibodies against thrombopoetin.

In addition, although, in all likelihood, ones low molecular weight compounds can be administered orally, real drugs on the market are not presented.

Therefore, a low-molecular compound which has excellent affinity and agonistic action on the receptor thrombopoetin, which can be administered orally, as a preventive, therapeutic and improving agents for diseases where effective activation of the receptor thrombopoetin. In particular, there is a need for low molecular weight compounds, which can serve as agents that increase the number of platelets, or agents that increase the number of other blood cells, by stimulating the differentiation and proliferation of hematopoietic stem cells, megakaryocyte the precursor cells and megakaryocytes, or low molecular weight compounds that can be used for therapeutic angiogenesis or as prophylactic and therapeutic agents to atherosclerosis by stimulating endothelial cells and endothelial progenitor cells.

The authors of the present invention conducted a comprehensive survey to identify low molecular weight compounds having affinity and agonistic action on the receptor thrombopoetin, and as a result found that the compounds of the present invention have a high affinity and agonist activity, which allows them to be strong, increasing the number of platelets by stimulating differentiation and proliferation megakaryocytic of progenitor cells and megakaryocytes. The present invention is carried out on the basis of this discovery.

Namely, the present invention relates to:

1. The compound represented by formula (1)

where A represents a nitrogen atom or CR4(where R4represents a hydrogen atom, a hydroxyl group (the hydroxyl group may be substituted C2-6alkenylphenol group or a C2-6alkenylphenol group), Tilney group (Tolna group may be substituted C1-10alkyl group, 2-6alkenylphenol group, C2-6alkenylphenol group or a C1-10alkylcarboxylic group), amino group (the amino group may be substituted by one or two C2-6alkenylamine groups or one or two C2-6alkenylamine groups), a formyl group, a halogen atom, a nitro-group, a cyano, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkylcarboxylic, mono - or di-C1-10alkylamino, C1-10alkoxygroup (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkylcarboxylic, mono - or di-C1-10alkylamino and C1-10alkoxygroup optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkylene and groups (C 1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups and2-14aryloxy), C2-14alloctype (C2-14alloctype optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic g the SCP, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy), SO2R5, SOR5or COR5(where R5represents a hydroxyl group, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C2-9heterocyclic group, a C1-10alkoxygroup (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C2-9heterocyclic group, and C1-10alkoxygroup optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6Alki the performance communications group may be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy), C2-14alloctype (C2-14alloctype optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino, mo is about - or di-C 1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy) or NR6R7(where each of R6and R7independently represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6 alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy), or R6and R7together with each other, means -(CH2)m1-E-(CH2)m2- (where E represents an oxygen atom, a sulfur atom, CR26R27(where each of R26and R27independently represents a hydrogen atom, a C1-10alkyl group, a C2-14aryl group, a C1-10alkoxygroup, C2-14alloctype, a hydroxyl group or a protected hydroxyl group) or NR8(where R8is the battle hydrogen atom, hydroxyl group, a formyl group, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl gr is the PAP optionally may be substituted by one or more substituents, selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)), and each of m1 and m2 independently represents an integer from 0 to 5 provided that m1+m2 is 3, 4 or 5)))),

B represents an oxygen atom, a sulfur atom or NR9(where R9represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group is and may not necessarily be substituted by one or more substituents, selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, g is koksilah groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy) or C2-14alloctype (C2-14alloctype optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)) (provided that when a represents a nitrogen atom, B is not NH),

R1represents a C2-14aryl group (C2-14the aryl group may be substituted by one or more substituents selected from the group consisting of halogen atoms, carboxyl groups, nitro groups, formyl groups, cyano groups, hydroxyl groups, protected hydroxyl groups, C1-10alkyl groups, C2-6alkenyl groups, C2-6etkinlik groups, C1-10alkoxygroup is, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups (C1-10alkyl group, a C2-6alkeneamine group, C2-6alkyline group, C1-10alkoxygroup, C1-10acylcarnitine group, C1-10alkylcarboxylic and C1-10alkoxycarbonyl group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl groups (C2-14aryl group optionally can be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl gr is PPI can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy), tylnej groups and amino groups (tirinya group and an amino group optionally can be substituted by one or two substituents selected from the group consisting of formyl group, a C1-10alkyl groups, C2-6alkenyl groups, C2-6etkinlik groups and C1-10alkylcarboxylic groups (C1-10alkyl group, a C2-6alkeneamine group, C2-6alkyline group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroc the ilen groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)))),

L1represents a bond, CR10R11(where each of R10and R11independently represents a hydrogen atom or a C1-6alkyl group, (C1-6the alkyl group may be substituted by one or more halogen atoms)), an oxygen atom, a sulfur atom or NR12(where R12represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, the volumes of halogen, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or neskolkimi halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14and what of lexigram)),

X is a OR13, SR13or NR14R15(where R13represents a hydrogen atom, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group or a C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), and each of R14and R15independently represents a hydrogen atom, a formyl group, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino gr the PPU, C1-10alkoxygroup, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik g is PP, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)),

R2represents a hydrogen atom, a formyl group, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14aryloxy the group may be substituted by one or more C 1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy),

L2represents a bond, CR34R35(where each of R34and R35independently represents a hydrogen atom or a C1-6alkyl group, (C1-6the alkyl group may be substituted by one or more halogen atoms)), an oxygen atom, a sulfur atom or NR16(where R16represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents you the security of a group, consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)),

L3represents a bond, CR17R18(where each of R17and R18independently represents a hydrogen atom, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10aldoxycarb nalnyh groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)), an oxygen atom, a sulfur atom or NR19(where R19represents a hydrogen atom, hydroxyl group, formyl is the Rupp, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkoxygroup and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted od is them or more substituents, selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)),

Y represents an oxygen atom, a sulfur atom or NR23(where R23represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents, selected from the group status is the present of the carboxyl groups, of nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14the aryl group may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl is groups and C 2-14aryloxy)),

L4represents a bond, CR20R21(where each of R20and R21independently represents a hydrogen atom, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be for esena one or more substituents, selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms))), an oxygen atom, a sulfur atom or NR22(where R22represents a hydrogen atom, hydroxyl group, protected hydroxyl group, a formyl group, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group C 2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups,halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms))),

when L4represents a bond, R3represents a methyl group (methyl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic (C1-10alkyl group, a C2-10alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-10is alkoxygroup, C1-10thioalkyl group, C1-10acylcarnitine group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more C2-14aryl groups (C2-14aryl group optionally can be substituted by one or more substituents independently represents-W1(CW2W3)mW4(where W1represents (CR24R25)n(where each of R24and R25independently represents a hydrogen atom or a C1-6alkyl group, (C1-6the alkyl group may be substituted by one or more halogen atoms), or R24and R25in conjunction with one another denote O= or S= and n is 0, 1, 2 or 3), an oxygen atom, a sulfur atom or NR36(where R36represents a hydrogen atom, a C1-6alkyl group, formyl group or a C1-6alkylcarboxylic group), each of W2and W3independently represents a hydrogen atom or a C1-3alkyl group, (C1-3the alkyl group may be substituted by one or more halogen atoms), m is 0, 1, 2 or 3 and W4represents a hydroxyl group, a protected hydroxyl group, ciolino the group, the amino group, formyl group, a halogen atom, a nitro-group, a cyano, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkylcarboxylic, mono - or di-C1-10alkylamino (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkylcarboxylic and mono - or di-C1-10alkylamino optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more atoms is halogen or by one or more halogen atoms)), C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, tylnej groups, groups, phosphonic acid groups, sulfonic acid groups tetrazole, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), SO2R28, SOR28, COR28(where R28represents a hydroxyl group, a protected hydroxyl group, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C2-9heteros Klionsky group, C1-10alkoxygroup (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C2-9heterocyclic group, and C1-10alkoxygroup optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl group, a C2-14alloctype (C2-14aryl group, and C2-14alloctype optionally can be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6and kinilig groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or NR29R30(where each of R29and R30independently represents a hydrogen atom, hydroxyl group, protected hydroxyl group, a formyl group, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylsulfonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylsulfonyl is supplemented flax group and C 1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype optionally can be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, sulfanilic groups, sulfamoyl groups, sulfo, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup (C1-10alkoxygroup can be substituted by one or more halogen atoms), C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl what Rupp, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms))or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or ascoltami halogen atoms)), or R29and R30together with each other, means -(CH2)m3-G-(CH2)m4- (where G represents an oxygen atom, a sulfur atom, CR31R32(where each of R31and R32independently represents a hydrogen atom, a C1-10alkyl group, a C2-14aryl group, a C1-10alkoxygroup, C2-14alloctype, a hydroxyl group or a protected hydroxyl group) or NR33(where R33represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic is p, amino, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups could the t to be substituted by one or more halogen atoms) or one or more halogen atoms))), and each of m3 and m4 independently represents an integer from 0 to 5, provided that m3+m4 is 3, 4 or 5))), group tetrazole or a phosphonic acid group)), or by one or more substituents independently represents-W5(CW6W7)m10W8(where W5, W6, W7and m10 are the same as W1, W2, W3and m, respectively, W1, W2, W3and m are the same as defined above, and W8represents a hydroxyl group, a protected hydroxyl group, Tilney group, amino group, formyl group, a halogen atom, a nitro-group, a cyano, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkylcarboxylic, mono - or di-C1-10alkylamino (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkylcarboxylic and mono - or di-C1-10alkylamino optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyanoprop is, atoms of halogen, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), SO2R28a, SOR28a, COR28a(where R28ais the same as R28and R28is the same as defined above), a group of tetrazole or group phosphonic acid)) and substituents independently represented by-W9(CW10W11)m11W12(where W9, W10, W11, W12and m11 are the same as W1, W2, W3, W8and m, respectively, and W1, W2, W3, W8and m are the same as defined above)), C2-10alkyl group, a C2-10alkenylphenol group, C2-10alkylamino group or a C2-9heterocyclic group (C2-10alkyl group, a C2-10Alchemilla group, C2-10Alchemilla groups and C 2-9heterocyclic group optionally can be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylsulfonyl groups, C1-10alkylaminocarbonyl groups, C1-10alkylaminocarbonyl groups, C1-10dialkylaminoalkyl groups, C1-10alkylcarboxylic (C1-10alkyl group, a C2-10alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl group, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylsulfonyl group, C1-10alkylaminocarbonyl group, C1-10alkylaminocarbonyl group, C1-10dialkylaminoalkyl group and C1-10alkylcarboxylic optionally can be substituted by one or more C2-14aryl groups (C2-14aryl group optionally can be substituted by one or more substituents, independently represents-W1(CW2W3)mW4(where W1, W2, W3, W4and m are the same as defined above)) or by one or more substituents independently represents-W5(CW6W7)m10W8(where W5, W6, W7, W8and m10 are the same as defined above)), substituents independently represents W9(CW10W11)m11W12(where W9, W10, W11, W12and m11 are the same as defined above) and C2-14aryl groups (C2-14aryl group optionally can be substituted by one or more substituents independently represents-W13(CW14W15)m12W16(where W13, W14, W15, W16and m12 are the same as W1, W2, W3, W4and m, respectively, and W1, W2, W3, W4and m are the same as defined above))), or when L4represents CR20R21(where each of R20and R21independently represents a hydrogen atom, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla groups who, C2-6Alchemilla group, C1-10alkoxygroup and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic the Rupp, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms))), an oxygen atom, a sulfur atom or NR22(where R22represents a hydrogen atom, a hydroxyl group, a protected hydroxyl group, a formyl group, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, atoms is of alogena, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14ar is maxigrip (C 2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms))), R3represents a C1-10alkyl group, a C2-10alkenylphenol group, C2-10alkylamino group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl group, C1-10alkylcarboxylic group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group or a C1-10alkylcarboxylic (C1-10alkyl group, a C2-10Alchemilla group, C2-10Alchemilla group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10Tolkalina group, C1-10acylcarnitine group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10tioa killnig groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic (C1-10alkyl group, a C2-10alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl group, C1-10acylcarnitine group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more C2-14aryl groups (C2-14aryl group optionally can be substituted by one or more substituents independently represents-W1(CW2W3)mW4(where W1, W2, W3, W4and m are the same as defined above)) or by one or more substituents independently represents-W5(CW6W7)m10W8(where W5, W6, W7, W8and m10 are the same as defined above)), substituents independently represents-W9(CW10W11)m11W12(where W9, W10, W11, W12and m11 are the same as defined above), and C2-14 aryl groups (C 2-14aryl group optionally can be substituted by one or more substituents independently represents-W13(CW14W15)m12W16(where W13, W14, W15, W16and m12 are the same as defined above))), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

2. The connection point 1, where L4represents a bond, R3represents a methyl group (methyl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic (C1-10alkyl group, a C2-10alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl group, C1-10acylcarnitine group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10al is incorporating optionally can be substituted by one or more C 2-14aryl groups (C2-14aryl group optionally can be substituted by one or more substituents independently represents-W1(CW2W3)mW4(where W1represents (CR24R25)n(where each of R24and R25independently represents a hydrogen atom or a C1-6alkyl group, (C1-6the alkyl group may be substituted by one or more halogen atoms), or R24and R25in conjunction with one another denote O= or S= and n is 0, 1, 2 or 3), an oxygen atom, a sulfur atom or NR36(where R36represents a hydrogen atom, a C1-6alkyl group, formyl group or a C1-6alkylcarboxylic group), each of W2and W3independently represents a hydrogen atom or a C1-3alkyl group, (C1-3the alkyl group may be substituted by one or more halogen atoms), m is 0, 1, 2 or 3, and W4represents a hydroxyl group, a protected hydroxyl group, Tilney group, amino group, formyl group, a halogen atom, a nitro-group, a cyano, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10Ala is carbonylation, mono - or di-C1-10alkylamino (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkylcarboxylic and mono - or di-C1-10alkylamino optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted one is m or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, tylnej groups, groups, phosphonic acid groups, sulfonic acid groups tetrazole, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), SO2R28, SOR28, COR28(where R28represents a hydroxyl group, a protected hydroxyl group, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C2-9heterocyclic group, a C1-10alkoxygroup (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C2-9heterocyclic group, and C1-10alkoxygroup optionally can be substituted by one or more substituents, selected and from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl group, a C2-14alloctype (C2-14aryl group, and C2-14alloctype optionally can be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - Il is di-C 1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or NR29R30(where each of R29and R30independently represents a hydrogen atom, hydroxyl group, protected hydroxyl group, a formyl group, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylsulfonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylsulfonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10Alki the carbonyl groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype optionally can be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, sulfanilic groups, sulfamoyl groups, sulfo, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup (C1-10alkoxygroup can be substituted by one or more halogen atoms), C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be C medeni one or more halogen atoms) or one or more halogen atoms))or C 2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), or R29and R30together with each other, means -(CH2)m3-G-(CH2)m4- (where G represents an oxygen atom, a sulfur atom, CR31R32(where each of R31and R32independently represents a hydrogen atom, a C1-10alkyl group, a C2-14aryl group, a C1-10alkoxyl the PPU, C2-14alloctype, a hydroxyl group or a protected hydroxyl group) or NR33(where R33represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can bytesneeded one or more halogen atoms) or one or more halogen atoms)) or C 2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms))), and each of m3 and m4 independently represents an integer from 0 to 5, provided that m3+m4 is 3, 4 or 5))), group tetrazole illi group phosphonic acid)) or by one or more substituents independently represents-W5(CW6W7)m10W8(where W5, W6, W7and m10 are the same, as W1, W2, W3and m, respectively, W1, W2, W3and m are the same as defined above, and W8represents a hydroxyl group, a protected hydroxyl group, Tilney group, amino group, formyl group, a halogen atom, a nitro-group, a cyano, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkylcarboxylic, mono - or di-C1-10alkylamino (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkylcarboxylic and mono - or di-C1-10alkylamino optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C-14 aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), SO2R28a, SOR28a, COR28a(where R28ais the same as R28and R28is the same as defined above), a group of tetrazole or group phosphonic acid)) and substituents independently represented by-W9(CW10W11)m11W12(where W9, W10, W11, W12and m11 are the same as W1, W2, W3, W8and m, respectively, and W1, W2, W3, W8and m are the same as defined above)), C2-10alkyl group, a C2-10alkenylphenol group, C2-10alkylamino group or a C2-9heterocyclic group (C2-10alkyl group, a C2-10Alchemilla group, C2-10Alchemilla group and C2-9heterocyclic group optionally can be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl groups, C1-10/sub> alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylaminocarbonyl groups, C1-10dialkylaminoalkyl groups, C1-10alkylcarboxylic (C1-10alkyl group, a C2-10alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl group, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylaminocarbonyl group, C1-10dialkylaminoalkyl group and C1-10alkylcarboxylic optionally can be substituted by one or more C2-14aryl groups (C2-14aryl group optionally can be substituted by one or more substituents independently represented by-W1(CW2W3)mW4(where W1, W2, W3, W4and m are the same as defined above)) or by one or more substituents independently represented by-W5(CW6W7)m10W8(where W5, W6, W7, W8and m10 are the same as defined above)), substituents independently represented Wsup> 9(CW10W11)m11W12(where W9, W10, W11, W12and m11 are the same as defined above), and C2-14aryl groups (C2-14aryl group optionally can be substituted by one or more substituents independently represented by-W13(CW14W15)m12W16(where W13, W14, W15, W16and m12 are the same as W1, W2, W3, W4and m, respectively, and W1, W2, W3, W4and m are the same as defined above))), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

3. The compound according to paragraph 1, where L4represents CR20R21(where each of R20and R21independently represents a hydrogen atom, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylboron the selected groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14aryloxy uppy can be substituted by one or more C 1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms))), an oxygen atom, a sulfur atom or NR22(where R22represents a hydrogen atom, hydroxyl group, protected hydroxyl group, a formyl group, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C-14 alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms))), and R3represents a C1-10alkyl group, a C2-10alkenylphenol group, C2-0 alkylamino group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl group, C1-10alkylcarboxylic group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group or a C1-10alkylcarboxylic (C1-10alkyl group, a C2-10Alchemilla group, C2-10Alchemilla group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10Tolkalina group, C1-10acylcarnitine group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic (C1-10alkyl group, a C2-10alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-10alkoxygroup, C thioalkyl group, C1-10acylcarnitine group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more C2-14aryl groups (C2-14aryl group optionally can be substituted by one or more substituents independently represented by-W1(CW2W3)mW4(where W1represents (CR24R25)n(where each of R24and R25independently represents a hydrogen atom or a C1-6alkyl group, (C1-6the alkyl group may be substituted by one or more halogen atoms), or R24and R25in conjunction with one another denote O= or S= and n is 0, 1, 2 or 3), an oxygen atom, a sulfur atom or NR36(where R36represents a hydrogen atom, a C1-6alkyl group, formyl group or a C1-6alkylcarboxylic group), each of W2and W3independently represents a hydrogen atom or a C1-3alkyl group, (C1-3the alkyl group may be substituted by one or more halogen atoms), m is 0, 1, 2 or 3 and W4represents a hydroxyl group, a protected hydroxyl group, Tilney group, amino is the Rupp, formyl group, a halogen atom, a nitro-group, a cyano, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkylcarboxylic, mono - or di-C1-10alkylamino (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkylcarboxylic and mono - or di-C1-10alkylamino optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or is one or more halogen atoms)), C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, tylnej groups, groups, phosphonic acid groups, sulfonic acid groups tetrazole, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), SO2R28, SOR28, COR28(where R28represents a hydroxyl group, a protected hydroxyl group, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C2-9heteros Klionsky group, C1-10alkoxygroup (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C2-9heterocyclic group, and C1-10alkoxygroup optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl group, a C2-14alloctype (C2-14aryl group, and C2-14alloctype optionally can be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6and kinilig groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or NR29R30(where each of R29and R30independently represents a hydrogen atom, hydroxyl group, protected hydroxyl group, a formyl group, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylsulfonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylsulfonyl is supplemented flax group and C 1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14aryloxy can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxy monilinia groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), or R29and R30together with each other, means -(CH2)m3-G-(CH2)m4- (where G represents an oxygen atom, a sulfur atom, CR31R32(where each of R31and R32independently represents a hydrogen atom, a C1-10alkyl group, a C2-14aryl group, a C1-10alkoxygroup, C2-14alloctype, a hydroxyl group or a protected hydroxyl group) or NR33(where R33represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxyl the PAP, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms))), and each of m3 and m4 independently represents an integer from 0 to 5, provided that m3+m4 is 3, 4 or 5))), group tetrazole or a phosphonic acid group)) or by one or more substituents independently represented by-W5(CW6W7)m10W8(where W5, W6, W7and m10 are the same as W1, W2, W3and m, respectively, W1, W2, W3and m are the same as defined above, and W8represents a hydroxyl group, a protected hydroxyl group, Tilney group, amino group, formyl group, a halogen atom, a nitro-group, a cyano, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10is alkylcarboxylic, C1-10alkylcarboxylic, mono - or di-C1-10alkylamino (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkylcarboxylic and mono - or di-C1-10alkylamino optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), SO2R28a, SOR28a, COR28a(where R28ais the same as R28and R28is the same as defined above), a group of tetrazole or a phosphonic acid group)), deputies, who ezavisimo presents-W 9(CW10W11)m11W12(where W9, W10, W11, W12and m11 are the same as W1, W2, W3, W8and m, respectively, and W1, W2, W3, W8and m are the same as defined above) and C2-14aryl groups (C2-14aryl group optionally can be substituted by one or more substituents independently represented by-W13(CW14W15)m12W16(where W13, W14, W15, W16and m12 are the same as W1, W2, W3, W4and m, respectively, and W1, W2, W3, W4and m are the same as defined above))), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

4. The compound according to any one of items 1-3, where A represents a nitrogen atom and B represents a sulfur atom, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

5. The compound according to any one of items 1-3, where A represents a nitrogen atom and B represents an oxygen atom, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

6. The compound according to any one of items 1-3, where A represents a nitrogen atom and B represents NR9different from NH (where R9is the battle hydrogen atom, hydroxyl group, a formyl group, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl group (C2-14aryl groups which optionally may be substituted by one or more substituents, selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy) or C2-14alloctype (C2-14alloctype optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C214 aryloxy)), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

7. The compound according to any one of items 1-3, where A is a CR4(where R4represents a hydrogen atom, a hydroxyl group (the hydroxyl group may be substituted C2-6alkenylphenol group or a C2-6alkenylphenol group), Tilney group (Tolna group may be substituted C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkenylphenol group or a C1-10alkylcarboxylic group), amino group (the amino group may be substituted by one or two C2-6alkenylamine groups or one or two C2-6alkenylamine groups), a formyl group, a halogen atom, a nitro-group, a cyano, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkylcarboxylic, mono - or di-C1-10alkylamino, C1-10alkoxygroup (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkylcarboxylic, mono - or di-C1-10alkylamino and C1-10alkoxygroup optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms,C 1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups and2-14aryloxy the SCP), C2-14alloctype (C2-14alloctype optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy), SO2R5, SOR5or COR5(where R5represents a hydroxyl group, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C2-9heterocyclic group, a C1-10alkoxygroup (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C2-9heterocyclic group, and C1-10alkoxygroup optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10ALCO is a system of groups, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy), C2-14aryl is xygraph (C 2-14alloctype optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy) or NR6R7(where each of R6and R7independently represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more of the Deputy is mi, selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino is, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy), or R6and R7together with each other, means -(CH2)m1-E-(CH2)m2- (where E represents an oxygen atom, a sulfur atom, CR26R27(where each of R26and R27independently represents a hydrogen atom, a C1-10alkyl group, a C2-14aryl group, a C1-10alkoxygroup, C2-14alloctype, a hydroxyl group or a protected hydroxyl group) or NR8(where R8represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C 1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)), and each of m1 and m2 independently represents a the th number from 0 to 5, provided that m1+m2 is 3, 4 or 5)))) and B represents an oxygen atom, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

8. The compound according to any one of items 1-3, where A is a CR4(where R4represents a hydrogen atom, a hydroxyl group (the hydroxyl group may be substituted C2-6alkenylphenol group or a C2-6alkenylphenol group), Tilney group (Tolna group may be substituted C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkenylphenol group or a C1-10alkylcarboxylic group), amino group (the amino group may be substituted by one or two C2-6alkenylamine groups or one or two C2-6alkenylamine groups), a formyl group, a halogen atom, a nitro-group, a cyano, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkylcarboxylic, mono - or di-C1-10alkylamino, C1-10alkoxygroup (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkylcarboxylic, mono - or di-C1-10alkylamino and C1-10alkoxygroup optionally can be substituted by one or more substituents selected from the group consisting of carboxyl gr is PP, of nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14 aryl groups and2-14aryloxy), C2-14alloctype (C2-14alloctype optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy), SO2R5, SOR5or COR5(where R5represents a hydroxyl group, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C2-9heterocyclic group, a C1-10alkoxygroup (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C2-9heterocyclic group, and C1-10alkoxygroup optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups,cyano groups, atoms of halogen, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups and 2-14aryloxy), C2-14alloctype (C2-14alloctype optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy) or NR6R7(where each of R6and R7independently represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optional m which may be substituted by one or more substituents, selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino is, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy), or R6and R7together with each other, means -(CH2)m1-E-(CH2)m2- (where E represents an oxygen atom, a sulfur atom, CR26R27(where each of R26and R27independently represents a hydrogen atom, a C1-10alkyl group, a C2-14aryl group, a C1-10alkoxygroup, C2-14alloctype, a hydroxyl group or a protected hydroxyl group) or NR8(where R8represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C 1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)) and each of m1 and m2 independently represents a is a number from 0 to 5, provided that m1+m2 is 3, 4 or 5)))) and B represents a sulfur atom, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

9. The compound according to any one of items 1-3, where A is a CR4(where R4represents a hydrogen atom, a hydroxyl group (the hydroxyl group may be substituted C2-6alkenylphenol group or a C2-6alkenylphenol group), Tilney group (Tolna group may be substituted C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkenylphenol group or a C1-10alkylcarboxylic group), amino group (the amino group may be substituted by one or two C2-6alkenylamine groups or one or two C2-6alkenylamine groups), a formyl group, a halogen atom, a nitro-group, a cyano, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkylcarboxylic, mono - or di-C1-10alkylamino, C1-10alkoxygroup (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkylcarboxylic, mono - or di-C1-10alkylamino and C1-10alkoxygroup optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, n is regroup, of cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl is groups and 2-14aryloxy), C2-14alloctype (C2-14alloctype optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy), SO2R5, SOR5or COR5(where R5represents a hydroxyl group, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C2-9heterocyclic group, a C1-10alkoxygroup (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C2-9heterocyclic group, and C1-10alkoxygroup optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, atoms ha is ogena, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14alloc is igroup), C2-14alloctype (C2-14alloctype optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy) or NR6R7(where each of R6and R7independently represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted one is m or more substituents, selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino is, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy), or R6and R7together with each other, means -(CH2)m1-E-(CH2)m2- (where E represents an oxygen atom, a sulfur atom, CR26R27(where each of R26and R27independently represents a hydrogen atom, a C1-10alkyl group, a C2-14aryl group, a C1-10alkoxygroup, C2-14alloctype, a hydroxyl group or a protected hydroxyl group) or NR8(where R8represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C 1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)), and each of m1 and m2 independently represents a the th number from 0 to 5, provided that m1+m2 is 3, 4 or 5)))) and B represents NR9(where R9represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more atoms halog is on) or one or more halogen atoms)), C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy) or C2-14alloctype (C2-14alloctype optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino mono - or di-C 1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

10. The compound according to any one of items 1-9, where L1that is the link, tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

11. The compound according to any one of items 1-10, where L2that is the link, tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

12. The compound according to any one of items 1-11, where L3represents NR19(where R19represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkoxygroup and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxy is lnyh groups, of nitro groups, cyano groups, automob halogen, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, automob halogen, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl group is, C2-14aryl groups, and C2-14aryloxy)), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

13. The compound according to any one of items 1-11, where L3represents NH, tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

14. The compound according to any one of paragraphs 3-11, where L3is the same as defined in paragraph 12, and L4represents NR22(where R22represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10is alkylcarboxylic, amino, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

15. The compound according to any one of paragraphs 3-11, where L3is so is m, as defined in paragraph 13, and L4represents NR22(where R22represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more of at the Mami halogen or by one or more halogen atoms)) or C 2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

16. The connection point 14 or 15, where L4represents NH, tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

17. The compound according to any one of items 2 and 4-11, where L3is as defined in paragraph 12, and L4that is the link, tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

18. The compound according to any one of items 2 and 4-11, where L3is as defined in paragraph 13, and L4 that is the link, tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

19. The compound according to any one of paragraphs 14 to 18, where Y represents an oxygen atom, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

20. The compound according to any one of paragraphs 14 to 18, where Y represents a sulfur atom, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

21. The connection point 19 or 20, where X represents a hydroxyl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

22. The compound according to any one of paragraphs 19 to 21, where R3represents a C2-9heterocyclic group (C2-9heterocyclic group optionally may be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, sulfamoyl groups, groups tetrazole, C1-10alkoxycarbonyl groups, C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkylcarboxylic and mono - or di-C1-10alkylamino), a tautomer, PR is the drug or pharmaceutically acceptable salt of the compound or its MES.

23. The compound according to any one of paragraphs 19 to 21, where R3represents a C2-9heterocyclic group (C2-9heterocyclic group is substituted by the Deputy selected from the group consisting of hydroxyl groups, amino groups, carboxyl groups, phosphonic acid groups, sulfonic acid, carbamoyl group, sulfamoyl group, group tetrazole and C1-10alkoxycarbonyl group, and Deputy selected from the group consisting of hydroxyl groups, amino groups, carboxyl groups, phosphonic acid groups, sulfonic acid, carbamoyl group, sulfamoyl group, group tetrazole, C1-10alkoxycarbonyl group, nitro group, ceanography, halogen atom, a C1-10alkyl group, a C1-10alkyl groups substituted by one or more fluorine atoms, sulfamoyl group, substituted C1-10alkyl group, carbamoyl group, substituted C1-10alkyl group, and C1-10alkylcarboxylic), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

24. The compound according to any one of paragraphs 19 to 21, where R3represents a C1-10alkyl group or a C2-10alkenylphenol group (C1-10alkyl group, and C2-10Alchemilla group long the flax can be substituted by one or more substituents, selected from the group consisting of C1-10alkyl groups, C2-10alkenyl groups, C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic (C1-10alkyl group, a C2-10alkeneamine group, C1-10alkoxygroup, C1-10thioalkyl group, C1-10acylcarnitine group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, sulfamoyl groups, groups tetrazole, C1-10alkoxycarbonyl groups, C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkylcarboxylic and mono - or di-C1-10alkylamino), nitro, halogen atoms, hydroxyl groups, amino groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl g the SCP, sulfamoyl groups of tetrazole), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

25. The compound according to any one of paragraphs 19 to 21, where R3represents a C1-10alkyl group or a C2-10alkenylphenol group (C1-10alkyl group, and C2-10Alchemilla group optionally can be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups, C2-6alkenyl groups, C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic (C1-10alkyl group, a C2-6alkeneamine group, C1-10alkoxygroup, C1-10thioalkyl group, C1-10acylcarnitine group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, sulfamoyl groups Tetra is Ola), of halogen atoms, nitro groups, hydroxyl groups, amino groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, sulfamoyl groups of tetrazole), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

26. The compound according to any one of paragraphs 19 to 21, where R3represents a C2-9heterocyclic group (C2-9heterocyclic group is substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, halogen atoms, carboxyl groups, groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, thiocarbamoyl groups, -CH2COOH, -OCH2COOH, -NHCH2COOH, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, -(C=O)COOH, -CH2(C=O)COOH, -NH(C=O)COOH, -NHSO2NH2C1-10alkyl groups, C1-10alkylsulfonyl groups, C1-10alkylaminocarbonyl groups, C1-10alkylcarboxylic groups, C1-10alkylaminocarbonyl groups and C1-10dialkylaminoalkyl groups (C1-10alkyl group, a C1-10alkylsulfonyl group, C1-10alkylaminocarbonyl group, C1-10alkyl is ebonyline group, C1-10alkylaminocarbonyl group and C1-10dialkylaminoalkyl group may be substituted by one or more substituents selected from the group consisting of phenyl groups, thienyl groups, fueling groups, peredelnyh groups, nitro groups, cyano groups, hydroxyl groups, amino groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, sulfamoyl groups of tetrazole)), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or its MES.

27. The activator receptor thrombopoetin according to any one of paragraphs 1-26.

28. Preventive, therapeutic or improving agent for diseases in which the effective activation of the receptor thrombopoetin, which contains the activator of the receptor thrombopoetin on paragraph 27, tautomer, prodrug or pharmaceutically acceptable salt of the activator or MES as an active ingredient.

29. The agent that increases the number of platelets containing activator receptor thrombopoetin on paragraph 27, tautomer, prodrug or pharmaceutically acceptable salt of the activator or MES as an active ingredient.

30. Medicinal product containing the compound according to any one of paragraphs 1-26, tautomer, prodrug or pharmaceutically priemel the needful salt of the compound or its MES as an active ingredient.

The present invention relates to pharmaceutical compositions comprising compounds that increase the number of platelets by stimulating the differentiation and proliferation of hematopoietic stem cells, megakaryocytic of progenitor cells and megakaryocytes or compounds for therapeutic angiogenesis or with antiarteriosclerotic action, which stimulate differentiation and proliferation of vascular endothelial cells and endothelial progenitor cells.

BRIEF DESCRIPTION of DRAWINGS

Figure 1 shows the proliferation of cells, UT7/EPO-mpl promote the connection of the present invention (example of synthesis 4).

Figure 2 shows cell proliferation UT7/EPO when the stimulation compound of the present invention (example of synthesis 4).

The BEST WAY of carrying out the INVENTION

Hereinafter the present invention will be described in detail.

In the present invention, “n” means normal radical (radical normal structure), “ISO” means isoradial (the radical isostructure), “sec” means the secondary radical, “t” means tertiary radical, “C” means cyclo, “o” means ortho, “m” means meta, “p” oznachaet pair, “Ph” means phenyl, “Py” means pyridyl, naphthyl” refers naphthyl, “Me” means methyl, “Et” oz ACHAT ethyl, “Pr” means propyl, “Bu” means butyl and “Ac” means acetyl.

Initially will be explained the terms in the respective substituents R1-R36.

As the halogen atom can be mentioned a fluorine atom, chlorine atom, bromine atom or iodine atom.

C1-3the alkyl group may be linear, branched, or a C3cycloalkyl group, and can be mentioned methyl, ethyl, n-propyl, isopropyl, and t-propyl and the like.

C1-6the alkyl group may be linear, branched, or a C3-6cycloalkyl group, and in addition to the above can be mentioned n-butyl, isobutyl, sec-butyl, tert-butyl, C-butyl, 1-methyl-C-propyl, 2-methyl-C-propyl, n-pentyl, 1-methyl-n-butyl, 2-methyl-n-butyl, 3-methyl-n-butyl, 1,1-dimethyl-n-propyl, 1,2-dimethyl-n-propyl, 2,2-dimethyl-n-propyl, 1-ethyl-n-propyl, t-pentyl, 1-methyl-C-butyl, 2-methyl-C-butyl, 3-methyl-C-butyl, 1,2-dimethyl-C-propyl, 2,3-dimethyl-C-propyl, 1-ethyl-C-propyl, 2-ethyl-C-propyl, n-hexyl, 1-methyl-n-pentyl, 2-methyl-n-pentyl, 3-methyl-n-pentyl, 4-methyl-n-pentyl, 1,1-dimethyl-n-butyl, 1,2-dimethyl-n-butyl, 1,3-dimethyl-n-butyl, 2,2-dimethyl-n-butyl, 2,3-dimethyl-n-butyl, 3,3-dimethyl-n-butyl, 1-ethyl-n-butyl, 2-ethyl-n-butyl, 1,1,2-trimethyl-n-propyl, 1,2,2-trimethyl-n-propyl, 1-ethyl-1-methyl-n-propyl, 1-ethyl-2-methyl-n-propyl, t-hexyl, 1-methyl-C-pentyl, 2-methyl-C-pentyl, 3-metals-pentyl, 1-ethyl-t-butyl, 2-ethyl-t-butyl, 3-ethyl-t-butyl, 1,2-dimethyl-C-butyl, 1,3-dimethyl-C-butyl, 2,2-dimethyl-C-butyl, 2,3-dimethyl-C-butyl, 2,4-dimethyl-C-butyl, 3,3-dimethyl-C-butyl, 1-n-propyl-C-propyl, 2-n-propyl-C-propyl, 1-isopropyl-C-propyl, 2-isopropyl-C-propyl, 1,2,2-trimethyl-C-propyl, 1,2,3-trimethyl-C-propyl, 2,2,3-trimethyl-C-propyl, 1-ethyl-2-methyl-C-propyl, 2-ethyl-1-methyl-C-propyl, 2-ethyl-2-methyl-C-propyl, 2-ethyl-3-methyl-C-propyl, and the like.

C1-10the alkyl group may be linear, branched, or a C3-10cycloalkyl group, and in addition to the above can be mentioned 1-methyl-1-ethyl-n-pentyl, 1-heptyl, 2-heptyl, 1-ethyl-1,2-dimethyl-n-propyl, 1-ethyl-2,2-dimethyl-n-propyl, 1-octyl, 3-octyl, 4-methyl-3-n-heptyl, 6-methyl-2-n-heptyl, 2-propyl-1-n-heptyl, 2,4,4-trimethyl-1-n-pentyl, 1 nonyl, 2-nonyl, 2,6-dimethyl-4-n-heptyl, 3-ethyl-2,2-dimethyl-3-n-pentyl, 3,5,5-trimethyl-1-n-hexyl, 1-decyl, 2-decyl, 4-decyl, 3,7-dimethyl-1-n-octyl, 3,7-dimethyl-3-n-octyl, t-heptyl, t-octyl, 1-methyl-C-hexyl, 2-methyl-C-hexyl, 3-methyl-C-hexyl, 1,2-dimethyl-C-hexyl, 1-ethyl-C-hexyl, 1-methyl-C-pentyl, 2-methyl-C-pentyl, 3-methyl-C-pentyl and the like.

C2-10the alkyl group may be linear, branched, or a C3-10cycloalkyl group, and here we can mention those bands mentioned above as C1-10alkyl groups, with the exception of etileno group.

As C2-6alkenylphenol group can be mentioned ethinyl, 1-PROPYNYL, 2-PROPYNYL, 1-butynyl, 2-butynyl, 3-butynyl, 1-methyl-2-PROPYNYL, 1-pentenyl, 2-pentenyl, 3-pentenyl, 4-pentenyl, 1-methyl-2-butenyl, 1-methyl-3-butynyl, 2-methyl-3-butenyl, 3-methyl-1-butynyl, 1,1-dimethyl-2-PROPYNYL, 2-ethyl-2-PROPYNYL, 1-hexenyl, 2-hexenyl, 3-hexenyl, 4-hexenyl, 5-hexenyl, 1-methyl-2-pentenyl, 1-methyl-3-pentenyl, 1-methyl-4-pentenyl, 2-methyl-3-pentenyl, 2-methyl-4-pentenyl, 3-methyl-1-pentenyl, 3-methyl-4-pentenyl, 4-methyl-1-pentenyl, 4-methyl-2-pentenyl, 1,1-dimethyl-2-butynyl, 1,1-dimethyl-3-butynyl, 1,2-dimethyl-3-butynyl, 2,2-dimethyl-3-butynyl, 3,3-dimethyl-1-butynyl, 1-ethyl-2-butinyl, 1-ethyl-3-butynyl, 1-n-propyl-2-PROPYNYL, 2-ethyl-3-butynyl, 1-methyl-1-ethyl-2-PROPYNYL, 1-isopropyl-2-PROPYNYL and the like.

C2-10Alchemilla group can be linear or branched, and in addition to the above can be mentioned 1-methyl-n-hexenyl, 1,2-dimethyl-n-hexenyl, 1-ethyl-n-hexenyl, 1-n-heptenyl, 2-n-heptenyl, 3-n-heptenyl, 4-n-heptenyl, 1-n-octenyl, 2-n-octenyl, 3-n-octenyl and the like.

C2-6Alchemilla group can be linear, branched, or a C3-6cycloalkenyl group, and there may be mentioned ethynyl, 1-propenyl, 2-propenyl, 1-methyl-1-ethynyl, 1-butenyl, 2-butenyl, 3-butenyl, 2-methyl-1-propenyl, 2-methyl-2-propenyl, 1-tilateral, 1-methyl-1-propenyl, 1-m is l-2-propenyl, 1-pentenyl, 2-pentenyl, 3-pentenyl, 4-pentenyl, 1-n-propylidene, 1-methyl-1-butenyl, 1-methyl-2-butenyl, 1-methyl-3-butenyl, 2-ethyl-2-propenyl, 2-methyl-1-butenyl, 2-methyl-2-butenyl, 2-methyl-3-butenyl, 3-methyl-1-butenyl, 3-methyl-2-butenyl, 3-methyl-3-butenyl, 1,1-dimethyl-2-propenyl, 1-isopropylidene, 1,2-dimethyl-1-propenyl, 1,2-dimethyl-2-propenyl, 1-C-pentenyl, 2-C-pentenyl, 3-C-pentenyl, 1-hexenyl, 2-hexenyl, 3-hexenyl, 4-hexenyl, 5-hexenyl, 1-methyl-1-pentenyl, 1-methyl-2-pentenyl, 1-methyl-3-pentenyl, 1-methyl-4-pentenyl, 1-n-butylidene, 2-methyl-1-pentenyl, 2-methyl-2-pentenyl, 2-methyl-3-pentenyl, 2-methyl-4-pentenyl, 2-n-propyl-2-propenyl, 3-methyl-1-pentenyl, 3-methyl-2-pentenyl, 3-methyl-3-pentenyl, 3-methyl-4-pentenyl, 3-ethyl-3-butenyl, 4-methyl-1-pentenyl, 4-methyl-2-pentenyl, 4-methyl-3-pentenyl, 4-methyl-4-pentenyl, 1,1-dimethyl-2-butenyl, 1,1-dimethyl-3-butenyl, 1,2-dimethyl-1-butenyl, 1,2-dimethyl-2-butenyl, 1,2-dimethyl-3-butenyl, 1-methyl-2-ethyl-2-propenyl, 1-second-butylether, 1,3-dimethyl-1-butenyl, 1,3-dimethyl-2-butenyl, 1,3-dimethyl-3-butenyl, 1-isobutylene, 2,2-dimethyl-3-butenyl, 2,3-dimethyl-1-butenyl, 2,3-dimethyl-2-butenyl, 2,3-dimethyl-3-butenyl, 2-isopropyl-2-propenyl, 3,3-dimethyl-1-butenyl, 1-ethyl-1-butenyl, 1-ethyl-2-butenyl, 1-ethyl-3-butenyl, 1-n-propyl-1-propenyl, 1-n-propyl-2-propenyl, 2-ethyl-1-butenyl, 2-ethyl-2-butenyl, 2-ethyl-3-butenyl, 1,1,2-trimethyl-2-propenyl, 1-tert-butylether, 1-methyl-1-ethyl-2-propenyl, 1-ethyl-2-methyl-1-ol which was penal, 1-ethyl-2-methyl-2-propenyl, 1-isopropyl-1-propenyl, 1-isopropyl-2-propenyl, 1-methyl-2-C-pentenyl, 1-methyl-3-C-pentenyl, 2-methyl-1-C-pentenyl, 2-methyl-2-C-pentenyl, 2-methyl-3-C-pentenyl, 2-methyl-4-C-pentenyl, 2-methyl-5-C-pentenyl, 2-the methylene-C-pentyl, 3-methyl-1-C-pentenyl, 3-methyl-2-C-pentenyl, 3-methyl-3-C-pentenyl, 3-methyl-4-C-pentenyl, 3-methyl-5-C-pentenyl, 3-methylene-C-pentyl, 1-C-hexenyl, 2-C-hexenyl, 3-C-hexenyl and the like.

C2-10Alchemilla group can be linear, branched, or a C3-10cycloalkenyl group, and in addition to the above there may be mentioned 1-methyl-n-hexanol, 1,2-dimethyl-n-hexenyl, 1-ethyl-n-hexenyl, 1-n-heptenyl, 2-n-heptenyl, 3-n-heptenyl, 4-n-heptenyl, 1-n-octenyl, 2-n-octenyl, 3-n-octenyl, 1-methyl-C-hexenyl, 1,2-dimethyl-C-hexenyl, 1-ethyl-C-hexenyl, 1-C-heptenyl, 2-C-heptenyl, 3-C-heptenyl, 4-C-heptenyl, 1-C-octenyl, 2-C-octenyl, 3-C-octenyl, 4-C-octenyl and the like.

C2-9heterocyclic group may be heterogenities or condensed heterobicyclic the group consisting of at least one atom arbitrarily selected from nitrogen atoms, oxygen atoms and sulfur atoms and from 2 to 9 carbon atoms, and specifically include the following patterns:

C2-14aryl group may be a C 6-14aryl group containing no heteroatoms as part of the ring atoms, or C2-9aromatic heterocyclic group, with C2-9aromatic heterocyclic group may be a 5-7-membered C2-6heterogenities group or an 8-10-membered C5-9condensed heterobicyclic group containing from 1 to 3 oxygen atoms, nitrogen atoms or sulfur atoms singly or in combination.

As C6-14aryl group, not containing heteroatoms, can be mentioned phenyl group, 1-indenolol group, 2-indenolol group, 3-indenolol group, 4-indenolol group, 5-indenolol group, 6-indenolol group, 7-indenolol group, α-naftalina group, β-naftalina group, 1-tetrahydronaphthyl group, 2-tetrahydronaphthalene group, 5-tetrahydronaphthyl group, 6-tetrahydronaphthyl group, o-biphenylyl group, m-biphenylyl group, p-biphenylyl group, 1-untilnow group, 2-untilnow group, 9-untilnow group, 1-phenanthroline group, 2-phenanthroline group, 3-phenanthroline group, 4-phenanthroline group, 9-phenanthroline group or the like.

5-7-membered C2-6heterophilically group can be a 2-thienyl group, 3-thienyl group, 2-follow group, 3-follow group, 2-perniciously, 3-pyranyloxy group, 4-pyranyloxy group, 1-pyrrolidinyl group, 2-pyrrolidinyl group, 3-pyrrolidinyl group, 1-imidazolidinyl group, 2-imidazolidinyl group, 4-imidazolidinyl group, 1-pyrazolidine group, 3-pyrazolidine group, 4-pyrazolidine group, 2-thiazolidine group, 4-thiazolidine group, 5-thiazolidine group, 3-isothiazolinone group, 4-isothiazoline group, 5-isothiazolinone group, 2-oxazolidinyl group, 4-oxazolidinyl group, 5-oxazolidinyl group, 3-isoxazolyl group, 4-isoxazolyl group, 5-isoxazolyl group, 2-pyridyloxy group, 3-pyridyloxy group, 4-pyridyloxy group, 2-personilnya group, 2-pyrimidinyl group, 4-pyrimidinyl group, 5-pyrimidinyl group, 3-pyridazinyl group, 4-pyridazinyl group, 2-1,3,4-oxadiazolyl group, 2-1,3,4-thiadiazolyl group, 3-1,2,4-oxadiazolyl group, 5-1,2,4-oxadiazolyl group, 3-1,2,4-thiadiazolyl group, 5-1,2,4-thiadiazolyl group, a 3-1,2,5-oxadiazolyl group, a 3-1,2,5-thiadiazolyl group or the like.

8-10-membered C5-9the condensed heterocyclic group may be a 2-benzofuranyl group, 3-benzofuranyl group, 4-benzofuranyl group, 5-benzofuranyl group, 6-benzofuranyl group, 7-benzofuranyl group, 1-isobenzofuranyl group, 4-isobenzo the uranyl group, 5-isobenzofuranyl group, 2-benzothiazoline group, 3-benzothiazoline group, 4-benzothiazoline group, 5-benzothiazoline group, 6-benzothiazoline group, 7-benzothiazoline group, 1-isobenzofuranyl group, 4-isobenzofuranyl group, 5-isobenzofuranyl group, 2-romanello group, 3-romanello group, 4-romanello group, 5-romanello group, 6-romanello group, 7-romanello group, 8-romanello group, 1-indolizinyl group, 2-indolizinyl group, 3-indolizinyl group, 5-indolizinyl group, 6-indolizinyl group, 7-indolizinyl group, 8-indolizinyl group, 1-isoindolyl group, 2-isoindolyl group, 4-isoindolyl group, 5-isoindolyl group, 1-indolering group, 2-indolering group, 3-indolering group, 4-indolering group, 5-indolering group, 6-indolering group, 7-indolering group, 1-indazolinone group, 2-indazolinone group, 3-indazolinone group, 4-indazolinone group, 5-indazolinone group, 6-indazolinone group, 7-indazolinone group, 1-parinello group, 2-parinello group, 3-parinello group, 6-parinello group, 7-parinello group, 8-parinello group, 2-pinolillo group, 3-pinolillo group, 4-pinolillo group, 5-pinolillo group, 6-pinolillo group, 7-pinolillo group, 8-pinolillo group, 1-ethanallen the th group, 3-izohinolinove group, 4-izohinolinove group, 5-izohinolinove group, 6-izohinolinove group, 7-izohinolinove group, 8-izohinolinove group, 1-phthalazinone group, 5-talinolol group, 6-talinolol group, 1-2,7-naphthyridinone group, 3-2,7-naphthyridinone group, 4-2,7-naphthyridinone group, 1-2,6-naphthyridinone group, 3-2,6-naphthyridinone group, 4-2,6-naphthyridinone group, 2-1,8-naphthyridines group, 3-1,8-naphthyridines group, 4-1,8-naphthyridines group, 2-1,7-naphthyridinone group, 3-1,7-naphthyridinone group, 4-1,7-naphthyridinone group, 5-1,7-naphthyridinone group, 6-1,7-naphthyridinone group, 8-1,7-naphthyridinone group, 2-1,6-naphthyridinone group, 3-1,6-naphthyridinone group, 4-1,6-naphthyridinone group, 5-1,6-naphthyridinone group, 7-1,6-naphthyridinone group, 8-1,6-naphthyridinone group, 2-1,5-naphthyridines group, 3-1 A 5-naphthyridines group, 4-1,5-naphthyridines group, 6-1,5-naphthyridines group, 7-1,5-naphthyridines group, 8-1,5-naphthyridines group, 2-khinoksalinona group, 5-khinoksalinona group, 6-khinoksalinona group, 2-chinazolinei group, 4-chinazolinei group, 5-chinazolinei group, 6-chinazolinei group, 7-chinazolinei group, 8-chinazolinei group, 3-indolinyl group, 4-indolinyl group, 5-indolinyl group-indolinyl group, 7-indolinyl group, 8-indolinyl group, 2-pteridinyl group, 4-pteridinyl group, 6-pteridinyl group, 7-pteridinyl group or the like.

C2-14alloctype can be a C6-14alloctype that do not contain heteroatoms as part of the ring atoms, or C2-9aromatic heterocyclic oxygraph, with C2-9aromatic heterocyclic oxygraph can be a 5-7-membered C2-6heterogenities oxygraph or 8-10-membered C5-9condensed heterobicyclic oxygraph containing from 1 to 3 oxygen atoms, nitrogen atoms or sulfur atoms singly or in combination.

As C6-14alloctype, not containing heteroatoms, may be noted fenoxaprop, 1-ingenjorsfirma, 2-ingenjorsfirma, 3-ingenjorsfirma, 4-ingenjorsfirma, 5-ingenjorsfirma, 6-ingenjorsfirma, 7 ingenjorsfirma, α-naphthyloxy, β-naphthyloxy, 1-tetrahydronaphthalene, 2-tetrahydronaphthalene, 5-tetrahydronaphthalene, 6-tetrahydronaphthalene, o-biphenyloxy, m-biphenyloxy, p-biphenyloxy, 1-antioxycaps, 2-antioxycaps, 9-antioxycaps, 1-frontreleaseswrap, 2-frontreleaseswrap, 3-frontreleaseswrap, 4-tenant is lexigraphy, 9-frontreleaseswrap or the like.

5-7-membered C2-6heterophilically oxygraph can be a 2-taylortype, 3-taylortype, 2-ferrochrome, 3-ferrochrome, 2-pyranyloxy, 3-pyranyloxy, 4-pyranyloxy, 1-errollaceaply, 2-errollaceaply, 3-errollaceaply, 1-imidazolylalkyl, 2-imidazolinium, 4-imidazolylalkyl, 1-pyrazolylborate, 3-pyrazolinone, 4-pyrazolylborate, 2-thiazoleacetate, 4-thiazoleacetate, 5-thiazoleacetate, 3-isothiazolones, 4-isothiazolone, 5-isothiazolone, 2-oxazolidones, 4-oxazolidones A 5-oxazolinone, 3-isoxazolone, 4-isoxazolone, 5-isoxazolone, 2-pyridyloxy, 3-pyridyloxy, 4-pyridyloxy, 2-personalantispy, 2-pyrimidinamine, 4-pyrimidinamine, 5-pyrimidinamine, 3-pyridazinone, 4-pyridinylamino, 2-1,3,4-oxadiazoline, 2-1,3,4-thiadiazolidine, 3-1,2,4-oxadiazolyl, 5-1,2,4-oxadiazolyl, 3-1,2,4-thiadiazolidine, 5-1,2,4-thiadiazolidine, 3-1,2,5-oxadiazolyl, 3-1,2,5-thiadiazolidine or something.

8-10-membered C5-9condensed heterobicyclic oxygraph can present is a 2-benzoperoxide, 3-benzoperoxide, 4-benzoperoxide, 5-benzoperoxide, 6-benzoperoxide, 7 benzoperoxide, 1-isobenzofuranone, 4-isobenzofurandione, 5-isobenzofurandione, 2-benzothiadiazine, 3-benzothiadiazin, 4-benzothiadiazine, 5-benzothiadiazine, 6-benzothiadiazine, 7 benzothiadiazine, 1-isobenzofuranyl, 4-isobenzofurandione, 5-isobenzofuranyl, 2-promediacorp, 3-promediacorp, 4-promediacorp, 5-promediacorp, 6-promediacorp, 7 promediacorp, 8-promediacorp, 1-indolizinium, 2-indolizinium, 3-indolizinium, 5-indolizinium, 6-indolizinium, 7 indolizinium, 8-indolizinium, 1-isoindoline, 2-isoindoline, 4-isoindoline, 5-isoindoline, 1-indoleacetate, 2-indoleacetate, 3-indoleacetate, 4-indoleacetate, 5-indoleacetate, 6-indoleacetate, 7 indoleacetate, 1-indazolinone, 2-indazolinone, 3-indazolinone, 4-indazolinone, 5-indazolinone, 6-indazolinone, 7 indazolinone, 1-purinacare, 2-purinacare, 3-purinacare, 6-purinacare, 7 purinacare, 8-purinacare-henrylacevedo, 3-henrylacevedo, 4-henrylacevedo, 5-henrylacevedo, 6-henrylacevedo, 7 henrylacevedo, 8-henrylacevedo, 1-ethenolysis, 3-ethenolysis, 4-ethenolysis, 5-ethenolysis, 6-ethenolysis, 7 ethenolysis, 8-ethenolysis, 1-phthalazinone, 5-phthalazinone, 6-phthalazinone, 1-2,7-naphthyridinone, 3-2,7-naphthyridinone, 4-2,7-naphthyridinone, 1-2,6-naphthyridinone, 3-2,6-naphthyridinone, 4-2,6-naphthyridinone, 2-1,8-naphthyridinone, 3-1,8-naphthyridinone, 4-1,8-naphthyridinone, 2-1,7-naphthyridinone, 3-1,7-naphthyridinone, 4-1,7-naphthyridinone, 5-1,7-naphthyridinone, 6-1,7-naphthyridinone, 8-1,7-naphthyridinone, 2-1,6-naphthyridinone, 3-1,6-naphthyridinone, 4-1,6-naphthyridinone, 5-1,6-naphthyridinone, 7-1,6-naphthyridinone, 8-1,6-naphthyridinone, 2-1,5-naphthyridinone, 3-1,5-naphthyridinone, 4-1,5-naphthyridinone, 6-1,5-naphthyridinone, 7-1,5-naphthyridinone, 8-1,5-naphthyridinone, 2-hinoksalinovym, 5-hinoksalinovym, 6-hinoksalinovym, 2-ginasolinspu, 4-ginasolinspu, 5-ginasolinspu, 6-ginasolinspu-ginasolinspu, 8 ginasolinspu, 3-linolenicacid, 4-linolenicacid, 5-linolenicacid, 6-linolenicacid, 7 linolenicacid, 8-linolenicacid, 2-peridiniaceae, 4-peridiniaceae, 6-peridiniaceae, 7 peridiniaceae or the like.

C1-6acylcarnitine group can be linear, branched, or a C3-6cycloalkylcarbonyl group, and here we can mention methylcarbamyl, ethylcarbazole, n-propylboronic, isopropylcarbonate, C-propylboronic, n-butylcarbamoyl, isobutylketone, second-butylcarbamoyl, tert-butylcarbamoyl, C-butylcarbamoyl, 1-methyl-C-propylboronic, 2-methyl-C-propylboronic, n-internabonal, 1-methyl-n-butylcarbamoyl, 2-methyl-n-butylcarbamoyl, 3-methyl-n-butylcarbamoyl, 1,1-dimethyl-n-propylboronic, 1,2-dimethyl-n-propylboronic, 2,2-dimethyl-n-propylboronic, 1-ethyl-n-propylboronic, C-internabonal, 1-methyl-C-butylcarbamoyl, 2-methyl-C-butylcarbamoyl, 3-methyl-C-butylcarbamoyl, 1,2-dimethyl-C-propylboronic, 2,3-dimethyl-C-propylboronic, 1-ethyl-C-propylboronic, 2-ethyl-C-propylboronic, n-hexylcaine, 1-methyl-n-internabonal, 2-methyl-n-internabonal, 3-methyl-n-internabonal, 4-methyl-n-internabonal, 1,1-dimethyl-n-butylcarbamoyl, 1,2-dimethyl-n-butylcarbamoyl, 1,3-dimethyl-n-butylcarbamoyl, 2,2-dimethyl-n-butylcarbamoyl, 2,3-dimethyl-butylcarbamoyl, 3,3-dimethyl-n-butylcarbamoyl, 1-ethyl-n-butylcarbamoyl, 2-ethyl-n-butylcarbamoyl, 1,1,2-trimethyl-n-propylboronic, 1,2,2-trimethyl-n-propylboronic, 1-ethyl-1-methyl-n-propylboronic, 1-ethyl-2-methyl-n-propylboronic, C-hexylcaine, 1-methyl-C-internabonal, 2-methyl-C-internabonal, 3-methyl-C-internabonal, 1-ethyl-C-butylcarbamoyl, 2-ethyl-C-butylcarbamoyl, 3-ethyl-C-butylcarbamoyl, 1,2-dimethyl-C-butylcarbamoyl, 1,3-dimethyl-C-butylcarbamoyl, 2,2-dimethyl-C-butylcarbamoyl, 2,3-dimethyl-C-butylcarbamoyl, 2,4-dimethyl-C-butylcarbamoyl, 3,3-dimethyl-C-butylcarbamoyl, 1-n-propyl-C-propylboronic, 2-n-propyl-C-propylboronic, 1-isopropyl-C-propylboronic, 2-isopropyl-C-propylboronic, 1,2,2-trimethyl-C-propylboronic, 1,2,3-trimethyl-C-propylboronic, 2,2,3-trimethyl-C-propylboronic, 1-ethyl-2-methyl-C-propylboronic, 2-ethyl-1-methyl-C-propylboronic, 2-ethyl-2-methyl-C-propylboronic, 2-ethyl-3-methyl-C-propylboronic or the like.

C1-10alkylsulphonyl can be linear, branched, or a C3-10cycloalkylcarbonyl group, and in addition to the above can be mentioned 1-methyl-1-ethyl-n-internabonal, 1-heptylammonium, 2-heptylammonium, 1-ethyl-1,2-dimethyl-n-propylboronic, 1-ethyl-2,2-dimethyl-n-propylboronic, 1-octigabay, 3-octigabay, 4-methyl-3-n-heptylammonium, 6-methyl-2-n-heptylammonium, 2-propyl-1-n-heptylammonium, 2,4,4-trimethyl-1-the-internabonal, 1-noninterbank, 2-noninterbank, 2,6-dimethyl-4-n-heptylammonium, 3-ethyl-2,2-dimethyl-3-n-internabonal, 3,5,5-trimethyl-1-n-hexylcaine, 1-deceleron, 2-deceleron, 4-deceleron, 3,7-dimethyl-1-n-octigabay, 3,7-dimethyl-3-n-octigabay or the like.

C1-6alkylaminocarbonyl group can be linear, branched, or a C3-6cycloalkylcarbonyl group, and among them methylaminomethyl, ethylaminomethyl, n-propylaminosulfonyl, isopropylaminocarbonyl, C-propylaminosulfonyl, n-butylaminoethyl, sibutraminesolution, second-butylaminoethyl, tert-butylaminoethyl, C-butylaminoethyl, 1-methyl-C-propylaminosulfonyl, 2-methyl-C-propylaminosulfonyl, n-intramyocellular, 1-methyl-n-butylaminoethyl, 2-methyl-n-butylaminoethyl, 3-methyl-n-butylaminoethyl, 1,1-dimethyl-n-propylaminosulfonyl, 1,2-dimethyl-n-propylaminosulfonyl, 2,2-dimethyl-n-propylaminosulfonyl, 1-ethyl-n-propylaminosulfonyl, C-intramyocellular, 1-methyl-C-butylaminoethyl, 2-methyl-C-butylaminoethyl, 3-methyl-C-butylaminoethyl, 1,2-dimethyl-C-propylaminosulfonyl, 2,3-dimethyl-C-propylaminosulfonyl, 1-ethyl-C-propylaminosulfonyl, 2-ethyl-C-propylaminosulfonyl, n-exelonexelon, 1-methyl-n-intramyocellular, 2-methyl-n-Penta is aminosulfonyl, 3-methyl-n-intramyocellular, 4-methyl-n-intramyocellular, 1,1-dimethyl-n-butylaminoethyl, 1,2-dimethyl-n-butylaminoethyl, 1,3-dimethyl-n-butylaminoethyl, 2,2-dimethyl-n-butylaminoethyl, 2,3-dimethyl-n-butylaminoethyl, 3,3-dimethyl-n-butylaminoethyl, 1-ethyl-n-butylaminoethyl, 2-ethyl-n-butylaminoethyl, 1,1,2-trimethyl-n-propylaminosulfonyl, 1,2,2-trimethyl-n-propylaminosulfonyl, 1-ethyl-1-methyl-n-propylaminosulfonyl, 1-ethyl-2-methyl-n-propylaminosulfonyl, C-exelonexelon, 1-methyl-C-intramyocellular, 2-methyl-C-intramyocellular, 3-methyl-C-intramyocellular, 1-ethyl-C-butylaminoethyl, 2-ethyl-C-butylaminoethyl, 3-ethyl-C-butylaminoethyl, 1,2-dimethyl-C-butylaminoethyl, 1,3-dimethyl-C-butylaminoethyl, 2,2-dimethyl-C-butylaminoethyl, 2,3-dimethyl-C-butylaminoethyl, 2,4-dimethyl-C-butylaminoethyl, 3,3-dimethyl-C-butylaminoethyl, 1-n-propyl-C-propylaminosulfonyl, 2-n-propyl-C-propylaminosulfonyl, 1-isopropyl-C-propylaminosulfonyl, 2-isopropyl-C-propylaminosulfonyl, 1,2,2-trimethyl-C-propylaminosulfonyl, 1,2,3-trimethyl-C-propylaminosulfonyl, 2,2,3-trimethyl-C-propylaminosulfonyl, 1-ethyl-2-methyl-C-propylaminosulfonyl, 2-ethyl-1-methyl-C-propylaminosulfonyl, 2-ethyl-2-methyl-C-propylaminosulfonyl, 2-ethyl-3-methyl-C-propylaminosulfonyl or the like.

1-10alkylaminocarbonyl group can be linear, branched, or a C3-10cycloalkylcarbonyl, and in addition to the above can be mentioned 1-methyl-1-ethyl-n-intramyocellular, 1-reptilescolleen, 2-reptilescolleen, 1-ethyl-1,2-dimethyl-n-propylaminosulfonyl, 1-ethyl-2,2-dimethyl-n-propylaminosulfonyl, 1-octylimidazolium, 3-octylimidazolium, 4-methyl-3-n-reptilescolleen, 6-methyl-2-n-reptilescolleen, 2-propyl-1-n-reptilescolleen, 2,4,4-trimethyl-1-n-intramyocellular, 1-nonelimination, 2-nonelimination, 2,6-dimethyl-4-n-reptilescolleen, 3-ethyl-2,2-dimethyl-3-n-intramyocellular, 3,5,5-trimethyl-1-n-exelonexelon, 1-decriminalises, 2-decriminalises, 4-decriminalises, 3,7-dimethyl-1-n-octylimidazolium, 3,7-dimethyl-3-n-octylimidazolium, C-reptilescolleen, C-octylimidazolium, 1-methyl-C-exelonexelon, 2-methyl-C-exelonexelon, 3-methyl-C-exelonexelon, 1,2-dimethyl-C-exelonexelon, 1-ethyl-C-exelonexelon, 1-methyl-C-intramyocellular, 2-methyl-C-intramyocellular, 3-methyl-C-intramyocellular or the like.

C1-6alkylsulfonyl group can be linear, branched, or a C3-6cycloalkylcarbonyl group, and ZV is camping you can mention methylsulphonyl, ethylsulfonyl, n-propylsulfonyl, isopropylphenyl, C-propylsulfonyl, n-butylsulfonyl, isobutylphenyl, second-butylsulfonyl, tert-butylsulfonyl, C-butylsulfonyl, 1-methyl-C-propylsulfonyl, 2-methyl-C-propylsulfonyl, n-peterculter, 1-methyl-n-butylsulfonyl, 2-methyl-n-butylsulfonyl, 3-methyl-n-butylsulfonyl, 1,1-dimethyl-n-propylsulfonyl, 1,2-dimethyl-n-propylsulfonyl, 2,2-dimethyl-n-propylsulfonyl, 1-ethyl-n-propylsulfonyl, C-peterculter, 1-methyl-C-butylsulfonyl, 2-methyl-C-butylsulfonyl, 3-methyl-C-butylsulfonyl, 1,2-dimethyl-C-propylsulfonyl, 2,3-dimethyl-C-propylsulfonyl, 1-ethyl-C-propylsulfonyl, 2-ethyl-C-propylsulfonyl, n-hexylsilane, 1-methyl-n-peterculter, 2-methyl-n-peterculter, 3-methyl-n-peterculter, 4-methyl-n-peterculter, 1,1-dimethyl-n-butylsulfonyl, 1,2-dimethyl-n-butylsulfonyl, 1,3-dimethyl-n-butylsulfonyl, 2,2-dimethyl-n-butylsulfonyl, 2,3-dimethyl-n-butylsulfonyl, 3,3-dimethyl-n-butylsulfonyl, 1-ethyl-n-butylsulfonyl, 2-ethyl-n-butylsulfonyl, 1,1,2-trimethyl-n-propylsulfonyl, 1,2,2-trimethyl-n-propylsulfonyl, 1-ethyl-1-methyl-n-propylsulfonyl, 1-ethyl-2-methyl-n-propylsulfonyl, C-hexylsilane, 1-methyl-C-peterculter, 2-methyl-C-peterculter, 3-methyl-C-peterculter, 1-ethyl-C-butylsulfonyl, 2-ethyl-C-butylsulfonyl, 3-ethyl-C-butylsulfonyl, 1,2-dimethyl-C-butylsulfonyl, 1,3-dim the Teal-C-butylsulfonyl, 2,2-dimethyl-C-butylsulfonyl, 2,3-dimethyl-C-butylsulfonyl, 2,4-dimethyl-C-butylsulfonyl, 3,3-dimethyl-C-butylsulfonyl, 1-n-propyl-C-propylsulfonyl, 2-n-propyl-C-propylsulfonyl, 1-isopropyl-C-propylsulfonyl, 2-isopropyl-C-propylsulfonyl, 1,2,2-trimethyl-C-propylsulfonyl, 1,2,3-trimethyl-C-propylsulfonyl, 2,2,3-trimethyl-C-propylsulfonyl, 1-ethyl-2-methyl-C-propylsulfonyl, 2-ethyl-1-methyl-C-propylsulfonyl, 2-ethyl-2-methyl-C-propylsulfonyl, 2-ethyl-3-methyl-C-propylsulfonyl or the like.

C1-10alkylsulfonyl group can be linear, branched, or a C3-10cycloalkylcarbonyl group, and in addition to the above there may be mentioned 1-methyl-1-ethyl-n-peterculter, 1-heptylaniline, 2-heptylaniline, 1-ethyl-1,2-dimethyl-n-propylsulfonyl, 1-ethyl-2,2-dimethyl-n-propylsulfonyl, 1-octylsilane, 3-octylsilane, 4-methyl-3-n-heptylaniline, 6-methyl-2-n-heptylaniline, 2-propyl-1-n-heptylaniline, 2,4,4-trimethyl-1-n-peterculter, 1-nonalcoholic, 2-nonalcoholic, 2,6-dimethyl-4-n-heptylaniline, 3-ethyl-2,2-dimethyl-3-n-peterculter, 3,5,5-trimethyl-1-n-hexylsilane, 1-decimalpoint, 2-decimalpoint, 4-decimalpoint, 3,7-dimethyl-1-n-octylsilane, 3,7-dimethyl-3-n-octylsilane, C-heptylaniline, C-octylsilane, 1-methyl-C-hexylsilane, 2-methyl-C-hexylsilane, 3-methyl-C-GE is calcultor, 1,2-dimethyl-C-hexylsilane, 1-ethyl-C-hexylsilane, 1-methyl-C-peterculter, 2-methyl-C-peterculter, 3-methyl-C-peterculter or the like.

C1-10alkoxygroup can be linear, branched, or a C3-10cycloalkanes, and there may be mentioned methoxy, ethoxy, n-propoxy, isopropoxy, C-propoxy, n-butoxy, isobutoxy, sec-butoxy, tert-butoxy, C-butoxy, 1-methyl-C-propoxy, 2-methyl-C-propoxy, n-pentyloxy, 1-methyl-n-butoxy, 2-methyl-n-butoxy, 3-methyl-n-butoxy, 1,1-dimethyl-n-propoxy, 1,2-dimethyl-n-propoxy, 2,2-dimethyl-n-propoxy, 1-ethyl-n-propoxy, t-pentyloxy, 1-methyl-C-butoxy, 2-methyl-C-butoxy, 3-methyl-C-butoxy, 1,2-dimethyl-C-propoxy, 2,3-dimethyl-C-propoxy, 1-ethyl-C-propoxy, 2-ethyl-C-propoxy, n-hexyloxy, 1-methyl-n-pentyloxy, 2-methyl-n-pentyloxy, 3-methyl-n-pentyloxy, 4-methyl-n-pentyloxy, 1,1-dimethyl-n-butoxy, 1,2-dimethyl-n-butoxy, 1,3-dimethyl-n-butoxy, 2,2-dimethyl-n-butoxy, 2,3-dimethyl-n-butoxy, 3,3-dimethyl-n-butoxy, 1-ethyl-n-butoxy, 2-ethyl-n-butoxy, 1,1,2-trimethyl-n-propoxy, 1,2,2-trimethyl-n-propoxy, 1-ethyl-1-methyl-n-propoxy, 1-ethyl-2-methyl-n-propoxy, t-hexyloxy, 1-methyl-C-pentyloxy, 2-methyl-C-pentyloxy, 3-methyl-C-pentyloxy, 1-ethyl-C-butoxy, 2-ethyl-C-butoxy, 3-ethyl-C-butoxy, 1,2-dimethyl-C-butoxy, 1,3-dimethyl-C-butoxy, 2,2-dimethyl-C-butoxy, 2,3-dimethyl-C-butoxy, 2,4-dimethyl-t-b is toxi, 3,3-dimethyl-C-butoxy, 1-n-propyl-C-propoxy, 2-n-propyl-C-propoxy, 1-isopropyl-C-propoxy, 2-isopropyl-C-propoxy, 1,2,2-trimethyl-C-propoxy, 1,2,3-trimethyl-C-propoxy, 2,2,3-trimethyl-C-propoxy, 1-ethyl-2-methyl-C-propoxy, 2-ethyl-1-methyl-C-propoxy, 2-ethyl-2-methyl-C-propoxy, 2-ethyl-3-methyl-C-propoxy, 1-methyl-1-ethyl-n-pentyloxy, 1-heptyloxy, 2-heptyloxy, 1-ethyl-1,2-dimethyl-n-propyloxy, 1-ethyl-2,2-dimethyl-n-propyloxy, 1-octyloxy, 3-octyloxy, 4-methyl-3-n-heptyloxy, 6-methyl-2-n-heptyloxy, 2-propyl-1-n-heptyloxy, 2,4,4-trimethyl-1-n-pentyloxy, 1-nonyloxy, 2-nonyloxy, 2,6-dimethyl-4-n-heptyloxy, 3-ethyl-2,2-dimethyl-3-n-pentyloxy, 3,5,5-trimethyl-1-n-hexyloxy, 1 decyloxy, 2-decyloxy, 4-decyloxy, 3,7-dimethyl-1-n-octyloxy, 3,7-dimethyl-3-n-octyloxy or the like.

C1-10Tolkalina group can be linear, branched, or a C3-10cicatiello group, and there may be mentioned methylthio, ethylthio, n-propylthio, isopropylthio, C-propylthio, n-butylthio, isobutyric, sec-butylthio, tert-butylthio, C-butylthio, 1-methyl-C-propylthio, 2-methyl-C-propylthio, n-pentylthio, 1-methyl-n-butylthio, 2-methyl-n-butylthio, 3-methyl-n-butylthio, 1,1-dimethyl-n-propylthio, 1,2-dimethyl-n-propylthio, 2,2-dimethyl-n-propylthio, 1-ethyl-n-propylthio, C-pentylthio, 1-methyl-C-butylthio, 2-methyl-C-butylthio, 3-methyl-C-butylthio, 1,2-dimethyl-C-propylthio, 2,3-dimethyl-C-property is, 1-ethyl-C-propylthio, 2-ethyl-C-propylthio, n-hexylthio, 1-methyl-n-pentylthio, 2-methyl-n-pentylthio, 3-methyl-n-pentylthio, 4-methyl-n-pentylthio, 1,1-dimethyl-n-butylthio, 1,2-dimethyl-n-butylthio, 1,3-dimethyl-n-butylthio, 2,2-dimethyl-n-butylthio, 2,3-dimethyl-n-butylthio, 3,3-dimethyl-n-butylthio, 1-ethyl-n-butylthio, 2-ethyl-n-butylthio, 1,1,2-trimethyl-n-propylthio, 1,2,2-trimethyl-n-propylthio, 1-ethyl-1-methyl-n-propylthio, 1-ethyl-2-methyl-n-propylthio, C-hexylthio, 1-methyl-C-pentylthio, 2-methyl-C-pentylthio, 3-methyl-C-pentylthio, 1-ethyl-C-butylthio, 2-ethyl-C-butylthio, 3-ethyl-C-butylthio, 1,2-dimethyl-C-butylthio, 1,3-dimethyl-C-butylthio, 2,2-dimethyl-C-butylthio, 2,3-dimethyl-C-butylthio, 2,4-dimethyl-C-butylthio, 3,3-dimethyl-C-butylthio, 1-n-propyl-C-propylthio, 2-n-propyl-C-propylthio, 1-isopropyl-C-propylthio, 2-isopropyl-C-propylthio, 1,2,2-trimethyl-C-propylthio, 1,2,3-trimethyl-C-propylthio, 2,2,3-trimethyl-C-propylthio, 1-ethyl-2-methyl-C-propylthio, 2-ethyl-1-methyl-C-propylthio, 2-ethyl-2-methyl-C-propylthio, 2-ethyl-3-methyl-C-propylthio, 1-methyl-1-ethyl-n-pentylthio, 1 Reptilia, 2-reptilio, 1-ethyl-1,2-dimethyl-n-propylthio, 1-ethyl-2,2-dimethyl-n-propylthio, 1 octylthio, 3 octylthio, 4-methyl-3-n-Reptilia, 6-methyl-2-n-Reptilia, 2-propyl-1-n-Reptilia, 2,4,4-trimethyl-1-n-pentylthio, 1 nonillion, 2-Nonito, 2,6-dimethyl-4-n-Reptilia, 3-ethyl-2,2-dimethyl-3-n-pentylthio, 3,5,5-trimethyl-1-n-hexylthio, 1-decillia, 2-decillia, 4-decillia, 3,7-dimethyl-1-n-octylthio, 3,7-dimethyl-3-the-octylthio or the like.

C1-6alkoxycarbonyl group can be linear, branched, or a C3-6cycloalkylcarbonyl group, and here we can mention methoxycarbonyl, etoxycarbonyl, n-propoxycarbonyl, isopropoxycarbonyl, C-propoxycarbonyl, n-butoxycarbonyl, isobutoxide, second-butoxycarbonyl, tert-butoxycarbonyl, C-butoxycarbonyl, 1-methyl-C-propoxycarbonyl, 2-methyl-C-propoxycarbonyl, n-pentyloxybenzoyl, 1-methyl-n-butoxycarbonyl, 2-methyl-n-butoxycarbonyl, 3-methyl-n-butoxycarbonyl, 1,1-dimethyl-n-propoxycarbonyl, 1,2-dimethyl-n-propoxycarbonyl, 2,2-dimethyl-n-propoxycarbonyl, 1-ethyl-n-propoxycarbonyl, C-pentyloxybenzoyl, 1-methyl-C-butoxycarbonyl, 2-methyl-C-butoxycarbonyl, 3-methyl-C-butoxycarbonyl, 1,2-dimethyl-C-propoxycarbonyl, 2,3-dimethyl-C-propoxycarbonyl, 1-ethyl-C-propoxycarbonyl, 2-ethyl-C-propoxycarbonyl, n-hexyloxymethyl, 1-methyl-n-pentyloxybenzoyl, 2-methyl-n-pentyloxybenzoyl, 3-methyl-n-pentyloxybenzoyl, 4-methyl-n-pentyloxybenzoyl, 1,1-dimethyl-n-butoxycarbonyl, 1,2-dimethyl-n-butoxycarbonyl, 1,3-dimethyl-n-butoxycarbonyl, 2,2-dimethyl-n-butoxycarbonyl, 2,3-dimethyl-n-butoxycarbonyl, 3,3-dimethyl-n-butoxycarbonyl, 1-ethyl-n-butoxycarbonyl, 2-ethyl-n-butoxycarbonyl, 1,1,2-trimethyl-n-propoxycarbonyl, 1,2,2-trimethyl-n-propoxycarbonyl, 1-ethyl-1-methyl-n ProPak carbonyl, 1-ethyl-2-methyl-n-propoxycarbonyl, C-hexyloxybenzoyl, 1-methyl-C-pentyloxybenzoyl, 2-methyl-C-pentyloxybenzoyl, 3-methyl-C-pentyloxybenzoyl, 1-ethyl-C-butoxycarbonyl, 2-ethyl-C-butoxycarbonyl, 3-ethyl-C-butoxycarbonyl, 1,2-dimethyl-C-butoxycarbonyl, 1,3-dimethyl-C-butoxycarbonyl, 2,2-dimethyl-C-butoxycarbonyl, 2,3-dimethyl-C-butoxycarbonyl, 2,4-dimethyl-C-butoxycarbonyl, 3,3-dimethyl-C-butoxycarbonyl, 1-n-propyl-C-propoxycarbonyl, 2-n-propyl-C-propoxycarbonyl, 1-isopropyl-C-propoxycarbonyl, 2-isopropyl-C-propoxycarbonyl, 1,2,2-trimethyl-C-propoxycarbonyl, 1,2,3-trimethyl-C-propoxycarbonyl, 2,2,3-trimethyl-C-propoxycarbonyl, 1-ethyl-2-methyl-C-propoxycarbonyl, 2-ethyl-1-methyl-C-propoxycarbonyl, 2-ethyl-2-methyl-C-propoxycarbonyl, 2-ethyl-3-methyl-C-propoxycarbonyl or the like.

C1-10alkoxycarbonyl group can be linear, branched, or a C3-10cycloalkylcarbonyl group, and in addition to the above can be mentioned 1-methyl-1-ethyl-n-pentyloxybenzoyl, 1-heptyloxybiphenyl, 2-heptyloxybiphenyl, 1-ethyl-1,2-dimethyl-n-propylenecarbonate, 1-ethyl-2,2-dimethyl-n-propylenecarbonate, 1-octyloxybiphenyl, 3-octyloxyphenyl, 4-methyl-3-n-heptyloxybiphenyl, 6-methyl-2-n-heptyloxybiphenyl, 2-propyl-1-n-heptyloxybiphenyl, 2,4,4-trimethyl-1-n-pentyloxybenzoyl, 1-nonintoxicating-nonlexically, 2,6-dimethyl-4-n-heptyloxybenzoic, 3-ethyl-2,2-dimethyl-3-n-pentyloxybenzoyl, 3,5,5-trimethyl-1-n-hexyloxybenzoyl, 1-decyloxybenzoic, 2-decyloxybenzoic, 4-decyloxybenzoic, 3,7-dimethyl-1-n-octyloxybiphenyl, 3,7-dimethyl-3-n-octyloxybiphenyl or the like.

C1-10alkylcarboxylic can be linear, branched, or a C3-10cycloalkylcarbonyl, and here we can mention methylcarbonate, ethylcarbonate, n-propylmalonate, isopropylcarbonate, C-propylmalonate, n-BUTYLCARBAMATE, isobutyryloxy, sec-butylcarbamoyl, tert-BUTYLCARBAMATE, C-BUTYLCARBAMATE, 1-methyl-C-propylmalonate, 2-methyl-C-propylmalonate, n-intercorporate, 1-methyl-n-BUTYLCARBAMATE, 2-methyl-n-BUTYLCARBAMATE, 3-methyl-n-BUTYLCARBAMATE, 1,1-dimethyl-n-propylmalonate, 1,2-dimethyl-n-propylmalonate, 2,2-dimethyl-n-propylmalonate, 1-ethyl-n-propylmalonate, C-intercorporate, 1-methyl-C-BUTYLCARBAMATE, 2-methyl-C-BUTYLCARBAMATE, 3-methyl-C-BUTYLCARBAMATE, 1,2-dimethyl-C-propylmalonate, 2,3-dimethyl-C-propylmalonate, 1-ethyl-C-propylmalonate, 2-ethyl-C-propylmalonate, n-hexylcaine, 1-methyl-n-intercorporate, 2-methyl-n-intercorporate, 3-methyl-n-intercorporate, 4-methyl-n-intercorporate, 1,1-di is ethyl-n-BUTYLCARBAMATE, 1,2-dimethyl-n-BUTYLCARBAMATE, 1,3-dimethyl-n-BUTYLCARBAMATE, 2,2-dimethyl-n-BUTYLCARBAMATE, 2,3-dimethyl-n-BUTYLCARBAMATE, 3,3-dimethyl-n-BUTYLCARBAMATE, 1-ethyl-n-BUTYLCARBAMATE, 2-ethyl-n-BUTYLCARBAMATE, 1,1,2-trimethyl-n-propylmalonate, 1,2,2-trimethyl-n-propylmalonate, 1-ethyl-1-methyl-n-propylmalonate, 1-ethyl-2-methyl-n-propylmalonate, C-hexylcaine, 1-methyl-C-intercorporate, 2-methyl-C-intercorporate, 3-methyl-C-intercorporate, 1-ethyl-C-BUTYLCARBAMATE, 2-ethyl-C-BUTYLCARBAMATE, 3-ethyl-C-BUTYLCARBAMATE, 1,2-dimethyl-C-BUTYLCARBAMATE, 1,3-dimethyl-C-BUTYLCARBAMATE, 2,2-dimethyl-C-BUTYLCARBAMATE, 2,3-dimethyl-C-BUTYLCARBAMATE, 2,4-dimethyl-C-BUTYLCARBAMATE, 3,3-dimethyl-C-BUTYLCARBAMATE, 1-n-propyl-C-propylmalonate, 2-n-propyl-C-propylmalonate, 1-isopropyl-C-propylmalonate, 2-isopropyl-C-propylmalonate, 1,2,2-trimethyl-C-propylmalonate, 1,2,3-trimethyl-C-propylmalonate, 2,2,3-trimethyl-C-propylmalonate, 1-ethyl-2-methyl-C-propylmalonate, 2-ethyl-1-methyl-C-propylmalonate, 2-ethyl-2-methyl-C-propylmalonate, 2-ethyl-3-methyl-C-propylmalonate, 1-methyl-1-ethyl-n-intercorporate, 1 latikambourke, 2-heptylammonium, 1-ethyl-1,2-dimethyl-n-propylmalonate, 1-ethyl-2,2-dimethyl-n-propylmalonate, 1 octylcarbinol, 3-octigabay and, 4-methyl-3-n-heptylammonium, 6-methyl-2-n-heptylammonium, 2-propyl-1-n-heptylammonium, 2,4,4-trimethyl-1-n-intercorporate, 1 monicabellucci, 2-monicabellucci, 2,6-dimethyl-4-n-heptylammonium, 3-ethyl-2,2-dimethyl-3-n-intercorporate, 3,5,5-trimethyl-1-n-hexylcaine, 1 dellcorporate, 2-dellcorporate, 4-dellcorporate, 3,7-dimethyl-1-n-octylcarbinol, 3,7-dimethyl-3-n-octylcarbinol or the like.

C1-10alkylcarboxylic can be linear, branched, or a C3-10cycloalkylcarbonyl, and here we can mention methylcobalamine, ethylcarbodiimide, n-propylnitrosamine, isopropylcarbodiimide, C-propylnitrosamine, n-BUTYLCARBAMATE, isobutylamino, sec-butylcarbamoyl, tert-butylcarbamoyl, C-BUTYLCARBAMATE, 1-methyl-C-propylnitrosamine, 2-methyl-C-propylnitrosamine, n-intelcorporation, 1-methyl-n-BUTYLCARBAMATE, 2-methyl-n-BUTYLCARBAMATE, 3-methyl-n-BUTYLCARBAMATE, 1,1-dimethyl-n-propylnitrosamine, 1,2-dimethyl-n-propylnitrosamine, 2,2-dimethyl-n-propylnitrosamine, 1-ethyl-n-propylnitrosamine, C-intelcorporation, 1-methyl-C-BUTYLCARBAMATE, 2-methyl-C-BUTYLCARBAMATE, 3-methyl-C-BUTYLCARBAMATE, 1,2-dimethyl-C-propylnitrosamine, 2,3-dimethyl-C-propylnitrosamine, Atil-C-propylnitrosamine, 2-ethyl-C-propylnitrosamine, n-paxilonline, 1-methyl-n-intelcorporation, 2-methyl-n-intelcorporation, 3-methyl-n-intelcorporation, 4-methyl-n-intelcorporation, 1,1-dimethyl-n-BUTYLCARBAMATE, 1,2-dimethyl-n-BUTYLCARBAMATE, 1,3-dimethyl-n-BUTYLCARBAMATE, 2,2-dimethyl-n-BUTYLCARBAMATE, 2,3-dimethyl-n-BUTYLCARBAMATE, 3,3-dimethyl-n-BUTYLCARBAMATE, 1-ethyl-n-BUTYLCARBAMATE, 2-ethyl-n-BUTYLCARBAMATE, 1,1,2-trimethyl-n-propylnitrosamine, 1,2,2-trimethyl-n-propylnitrosamine, 1-ethyl-1-methyl-n-propylnitrosamine, 1-ethyl-2-methyl-n-propylnitrosamine, C-paxilonline, 1-methyl-C-intelcorporation, 2-methyl-C-intelcorporation, 3-methyl-C-intelcorporation, 1-ethyl-C-BUTYLCARBAMATE, 2-ethyl-C-BUTYLCARBAMATE, 3-ethyl-C-BUTYLCARBAMATE, 1,2-dimethyl-C-BUTYLCARBAMATE, 1,3-dimethyl-C-BUTYLCARBAMATE, 2,2-dimethyl-C-BUTYLCARBAMATE, 2,3-dimethyl-C-BUTYLCARBAMATE, 2,4-dimethyl-C-BUTYLCARBAMATE, 3,3-dimethyl-C-BUTYLCARBAMATE, 1-n-propyl-C-propylnitrosamine, 2-n-propyl-C-propylnitrosamine, 1-isopropyl-C-propylnitrosamine, 2-isopropyl-C-propylnitrosamine, 1,2,2-trimethyl-C-propylnitrosamine, 1,2,3-trimethyl-C-propylnitrosamine, 2,2,3-trimethyl-C-propylnitrosamine, 1-ethyl-2-methyl-C-propylnitrosamine, 2-ethyl-1-methyl-C-propylnitrosamine, 2-ethyl-2-methyl-C-propyl what arbolino, 2-ethyl-3-methyl-C-propylnitrosamine, 1-methyl-1-ethyl-n-intelcorporation, 1 heptylammonium, 2-heptylcyclopentanone, 1-ethyl-1,2-dimethyl-n-propylnitrosamine, 1-ethyl-2,2-dimethyl-n-propylnitrosamine, 1 octylcarbinol, 3 octylcarbinol, 4-methyl-3-n-heptylammonium, 6-methyl-2-n-heptylcyclopentanone, 2-propyl-1-n-heptylammonium, 2,4,4-trimethyl-1-n-intelcorporation, 1 nonincorporation, 2-nonincorporation, 2,6-dimethyl-4-n-heptylammonium, 3-ethyl-2,2-dimethyl-3-n-intelcorporation, 3,5,5-trimethyl-1-n-paxilonline, 1 metilcarbonievy, 2-metilcarbonievy, 4-metilcarbonievy, 3,7-dimethyl-1-n-octylcarbinol, 3,7-dimethyl-3-n-octylcarbinol or the like.

C1-10alkylaminocarbonyl group can be a C1-10monoacylglycerols group or a C1-10dialkylaminoalkyl group. C1-10monoacylglycerols group can be linear, branched, or a C3-10cycloalkylcarbonyl group, and here we can mention methylaminomethyl, ethylaminomethyl, n-propylaminosulfonyl, isopropylaminocarbonyl, C-propylaminosulfonyl, n-butylaminoethyl, isobutylparaben, second-butylaminoethyl, tert-butylaminoethyl, C-butylaminoethyl, 1-methyl-C-propylaminosulfonyl, 2-methyl-C-cuts carbonyl, n-intramyocardial, 1-methyl-n-butylaminoethyl, 2-methyl-n-butylaminoethyl, 3-methyl-n-butylaminoethyl, 1,1-dimethyl-n-propylaminoethyl, 1,2-dimethyl-n-propylaminoethyl, 2,2-dimethyl-n-propylaminoethyl, 1-ethyl-n-propylaminoethyl, C-intramyocardial, 1-methyl-C-butylaminoethyl, 2-methyl-C-butylaminoethyl, 3-methyl-C-butylaminoethyl, 1,2-dimethyl-C-propylaminosulfonyl, 2,3-dimethyl-C-propylaminosulfonyl, 1-ethyl-C-propylaminosulfonyl, 2-ethyl-C-propylaminosulfonyl, n-mexiletineciclovir, 1-methyl-n-intramyocardial, 2-methyl-n-intramyocardial, 3-methyl-n-intramyocardial, 4-methyl-n-intramyocardial, 1,1-dimethyl-n-butylaminoethyl, 1,2-dimethyl-n-butylaminoethyl, 1,3-dimethyl-n-butylaminoethyl, 2,2-dimethyl-n-butylaminoethyl, 2,3-dimethyl-n-butylaminoethyl, 3,3-dimethyl-n-butylaminoethyl, 1-ethyl-n-butylaminoethyl, 2-ethyl-n-butylaminoethyl, 1,1,2-trimethyl-n-propylaminoethyl, 1,2,2-trimethyl-n-propylaminoethyl, 1-ethyl-1-methyl-n-propylaminoethyl, 1-ethyl-2-methyl-n-propylaminoethyl, C-mexiletineciclovir, 1-methyl-C-intramyocardial, 2-methyl-C-intramyocardial, 3-methyl-C-intramyocardial, 1-ethyl-C-butylaminoethyl, 2-ethyl-C-butylaminoethyl, 3-ethyl-C-butylaminoethyl, 1,2-dimethyl-C-butylaminoethyl, 1,3-dimethyl-C-butylaminoethyl, 2,2-dimethyl-C-butyl is enacarbil, 2,3-dimethyl-C-butylaminoethyl, 2,4-dimethyl-C-butylaminoethyl, 3,3-dimethyl-C-butylaminoethyl, 1-n-propyl-C-propylaminosulfonyl, 2-n-propyl-C-propylaminosulfonyl, 1-isopropyl-C-propylaminosulfonyl, 2-isopropyl-C-propylaminosulfonyl, 1,2,2-trimethyl-C-propylaminosulfonyl, 1,2,3-trimethyl-C-propylaminosulfonyl, 2,2,3-trimethyl-C-propylaminosulfonyl, 1-ethyl-2-methyl-C-propylaminosulfonyl, 2-ethyl-1-methyl-C-propylaminosulfonyl, 2-ethyl-2-methyl-C-propylaminosulfonyl, 2-ethyl-3-methyl-C-propylaminosulfonyl, 1-methyl-1-ethyl-n-intramyocardial, 1-getelementkey, 2-getelementkey, 1-ethyl-1,2-dimethyl-n-propylaminoethyl, 1-ethyl-2,2-dimethyl-n-propylaminoethyl, 1-octilinear, 3-octilinear, 4-methyl-3-n-getelementkey, 6-methyl-2-n-getelementkey, 2-propyl-1-n-getelementkey, 2,4,4-trimethyl-1-n-intramyocardial, 1-nonelimination, 2-nonelimination, 2,6-dimethyl-4-n-getelementkey, 3-ethyl-2,2-dimethyl-3-n-intramyocardial, 3,5,5-trimethyl-1-n-mexiletineciclovir, 1-decrimination, 2-decrimination, 4-decrimination, 3,7-dimethyl-1-n-octilinear, 3,7-dimethyl-3-n-octilinear or the like.

C1-10dialkylaminoalkyl group can be symmetrical or asymmetrical. Symmetric C1-10dialkylaminoalkyl group can be linear, PA is extensive, or a C 3-10cycloalkylcarbonyl group, and here we can mention dimethylaminoethyl, diethylaminoethyl, di-n-propylaminoethyl, diisopropylaminoethanol, di-t-propylaminoethyl, di-n-butylaminoethyl, diisobutylamine, di-sec-butylaminoethyl, di-tert-butylaminoethyl, di-t-butylaminoethyl, di(1-methyl-C-propyl)aminocarbonyl, di(2-methyl-C-propyl)aminocarbonyl, di-n-intramyocardial, di(1-methyl-n-butyl)aminocarbonyl, di(2-methyl-n-butyl)aminocarbonyl, di(3-methyl-n-butyl)aminocarbonyl, di(1,1-dimethyl-n-propyl)aminocarbonyl, di(1,2-dimethyl-n-propyl)aminocarbonyl, di(2,2-dimethyl-n-propyl)aminocarbonyl, di(1-ethyl-n-propyl)aminocarbonyl, di-t-intramyocardial, di(1-methyl-C-butyl)aminocarbonyl, di(2-methyl-C-butyl)aminocarbonyl, di(3-methyl-t-butyl)aminocarbonyl, di(1,2-dimethyl-C-propyl)aminocarbonyl, di(2,3-dimethyl-C-propyl)aminocarbonyl, di(1-ethyl-C-propyl)aminocarbonyl, di(2-ethyl-C-propyl)aminocarbonyl, di-n-mexiletineciclovir, di(1-methyl-n-pentyl)aminocarbonyl, di(2-methyl-n-pentyl)aminocarbonyl, di(3-methyl-n-pentyl)aminocarbonyl, di(4-methyl-n-pentyl)aminocarbonyl, di(1,1-dimethyl-n-butyl)aminocarbonyl, di(1,2-dimethyl-n-butyl)aminocarbonyl, di(1,3-dimethyl-n-butyl)aminocarbonyl, di(2,2-dimethyl-n-butyl)aminocarbonyl, di(2,3-dimethyl-n-butyl)aminocarbonyl, di(3,3-dimethyl-n-butyl)aminocarbonyl, di(1-FL is the l-n-butyl)aminocarbonyl, di(2-ethyl-n-butyl)aminocarbonyl, di(1,1,2-trimethyl-n-propyl)aminocarbonyl, di(1,2,2-trimethyl-n-propyl)aminocarbonyl, di(1-ethyl-1-methyl-n-propyl)aminocarbonyl, di(1-ethyl-2-methyl-n-propyl)aminocarbonyl, di-t-mexiletineciclovir, di(1-methyl-C-pentyl)aminocarbonyl, di(2-methyl-C-pentyl)aminocarbonyl, di(3-methyl-C-pentyl)aminocarbonyl, di(1-ethyl-t-butyl)aminocarbonyl, di(2-ethyl-t-butyl)aminocarbonyl, di(3-ethyl-t-butyl)aminocarbonyl, di(1,2-dimethyl-C-butyl)aminocarbonyl, di(1,3-dimethyl-C-butyl)aminocarbonyl, di(2,2-dimethyl-C-butyl)aminocarbonyl, di(2,3-dimethyl-C-butyl)aminocarbonyl, di(2,4-dimethyl-t-butyl)aminocarbonyl, di(3,3-dimethyl-C-butyl)aminocarbonyl, di(1-n-propyl-C-propyl)aminocarbonyl, di(2-n-propyl-C-propyl)aminocarbonyl, di(1-isopropyl-C-propyl)aminocarbonyl, di(2-isopropyl-C-propyl)aminocarbonyl, di(1,2,2-trimethyl-C-propyl)aminocarbonyl, di(1,2,3-trimethyl-C-propyl)aminocarbonyl, di(2,2,3-trimethyl-C-propyl)aminocarbonyl, di(1-ethyl-2-methyl-C-propyl)aminocarbonyl, di(2-ethyl-1-methyl-C-propyl)aminocarbonyl, di(2-ethyl-2-methyl-C-propyl)aminocarbonyl, di(2-ethyl-3-methyl-C-propyl)aminocarbonyl, di(1-methyl-1-ethyl-n-pentyl)aminocarbonyl, di(1-heptyl)aminocarbonyl, di(2-heptyl)aminocarbonyl, di(1-ethyl-1,2-dimethyl-n-propyl)aminocarbonyl, di(1-ethyl-2,2-dimethyl-n-propyl)aminocarbonyl, di(1-octyl)aminocarbonyl, di(3-octyl)aminocarbonyl, di(4-methyl-3-n-heptyl)amino shall arbonyl, di(6-methyl-2-n-heptyl)aminocarbonyl, di(2-propyl-1-n-heptyl)aminocarbonyl, di(2,4,4-trimethyl-1-n-pentyl)aminocarbonyl, di(1-nonyl)aminocarbonyl, di(2-nonyl)aminocarbonyl, di(2,6-dimethyl-4-n-heptyl)aminocarbonyl, di(3-ethyl-2,2-dimethyl-3-n-pentyl)aminocarbonyl, di(3,5,5-trimethyl-1-n-hexyl)aminocarbonyl, di(1-decyl)aminocarbonyl, di(2-decyl)aminocarbonyl, di(4-decyl)aminocarbonyl, di(3,7-dimethyl-1-n-octyl)aminocarbonyl, di(3,7-dimethyl-3-n-octyl)aminocarbonyl or the like.

Asymmetric C1-10dialkylaminoalkyl group can be linear, branched, or a C3-10cycloalkylcarbonyl group, and there can be mentioned methyl, ethyl)aminocarbonyl, (methyl, n-propyl)aminocarbonyl, (methyl, isopropyl)aminocarbonyl, (methyl, C-propyl)aminocarbonyl, (methyl, n-butyl)aminocarbonyl, (methyl, isobutyl)aminocarbonyl, (methyl, sec-butyl)aminocarbonyl, (methyl, tert-butyl)aminocarbonyl, (methyl, n-pentyl)aminocarbonyl, (methyl, C-pentyl)aminocarbonyl, (methyl, n-hexyl)aminocarbonyl, (methyl, C-hexyl)aminocarbonyl, (ethyl, n-propyl)aminocarbonyl, (ethyl, isopropyl)aminocarbonyl, (ethyl, s-propyl)aminocarbonyl, (ethyl, n-butyl)aminocarbonyl, (ethyl, isobutyl)aminocarbonyl, (ethyl, sec-butyl)aminocarbonyl, (ethyl, tert-butyl)aminocarbonyl, (ethyl, n-pentyl)aminocarbonyl, (ethyl, t-pentyl)aminocarbonyl, (ethyl, n-Gex is l)aminocarbonyl, (ethyl, t-hexyl)aminocarbonyl, n-propyl, isopropyl)aminocarbonyl, n-propyl, C-propyl)aminocarbonyl, n-propyl, n-butyl)aminocarbonyl, n-propyl, isobutyl)aminocarbonyl, n-propyl, sec-butyl)aminocarbonyl, n-propyl, tert-butyl)aminocarbonyl, n-propyl, n-pentyl)aminocarbonyl, n-propyl, t-pentyl)aminocarbonyl, n-propyl, n-hexyl)aminocarbonyl, n-propyl, t-hexyl)aminocarbonyl, isopropyl, t-propyl)aminocarbonyl, isopropyl, n-butyl)aminocarbonyl, (isopropyl, isobutyl)aminocarbonyl, isopropyl, sec-butyl)aminocarbonyl, (isopropyl, tert-butyl)aminocarbonyl, isopropyl, n-pentyl)aminocarbonyl, isopropyl, t-pentyl)aminocarbonyl, isopropyl, n-hexyl)aminocarbonyl, isopropyl, t-hexyl)aminocarbonyl, (C-propyl, n-butyl)aminocarbonyl, (C-propyl, isobutyl)aminocarbonyl, (C-propyl, sec-butyl)aminocarbonyl, (C-propyl, tert-butyl)aminocarbonyl, (C-propyl, n-pentyl)aminocarbonyl, (C-propyl, C-pentyl)aminocarbonyl, (C-propyl, n-hexyl)aminocarbonyl, (C-propyl, C-hexyl)aminocarbonyl, n-butyl, isobutyl)aminocarbonyl, n-butyl, sec-butyl)aminocarbonyl, (n-butyl, tert-butyl)aminocarbonyl, n-butyl, n-pentyl)aminocarbonyl, n-butyl, t-pentyl)aminocarbonyl, n-butyl, n-hexyl)aminocarbonyl, n-butyl, t-hexyl)aminocarbonyl, isobutyl, sec-butyl)aminocarbonyl, isobutyl, tert-butyl)aminocarbonyl, isobutyl, n-pentyl)aminocarbonyl is l, (isobutyl, t-pentyl)aminocarbonyl, isobutyl, n-hexyl)aminocarbonyl, isobutyl, t-hexyl)aminocarbonyl, (sec-butyl, tert-butyl)aminocarbonyl, (sec-butyl, n-pentyl)aminocarbonyl, (sec-butyl, t-pentyl)aminocarbonyl, (sec-butyl, n-hexyl)aminocarbonyl, (sec-butyl, t-hexyl)aminocarbonyl, (tert-butyl, n-pentyl)aminocarbonyl, (tert-butyl, t-pentyl)aminocarbonyl, (tert-butyl, n-hexyl)aminocarbonyl, (tert-butyl, C-hexyl)aminocarbonyl, (n-pentyl, C-pentyl)aminocarbonyl, (n-pentyl, n-hexyl)aminocarbonyl, (n-pentyl, C-hexyl)aminocarbonyl, (C-pentyl, n-hexyl)aminocarbonyl, (C-pentyl, C-hexyl)aminocarbonyl, n-hexyl, t-hexyl)aminocarbonyl, (methyl, n-heptyl)aminocarbonyl, (methyl, n-octyl)aminocarbonyl, (methyl, n-nonyl)aminocarbonyl, (methyl, n-decyl)aminocarbonyl, (methyl, n-heptyl)aminocarbonyl, (ethyl, n-octyl)aminocarbonyl, (ethyl, n-nonyl)aminocarbonyl, (ethyl, n-decyl)aminocarbonyl or the like.

C1-10monoalkylamines can be linear, branched, or a C3-10cycloalkylation, and here we can mention methylamino, ethylamino, n-propylamino, isopropylamino, C-propylamino, n-butylamino, isobutylamino, sec-butylamino, tert-butylamino, C-butylamino, 1-methyl-C-propylamino, 2-methyl-C-propylamino, n-pentylamine, 1-methyl-n-butylamino, 2-methyl-n-butylamine, 3-methyl-n-butylamino, ,1-dimethyl-n-propylamino, 1,2-dimethyl-n-propylamino, 2,2-dimethyl-n-propylamino, 1-ethyl-n-propylamino, C-pentylamine, 1-methyl-C-butylamino, 2-methyl-C-butylamine, 3-methyl-C-butylamine, 1,2-dimethyl-C-propylamino, 2,3-dimethyl-C-propylamino, 1-ethyl-C-propylamino, 2-ethyl-C-propylamino, n-hexylamine, 1-methyl-n-pentylamine, 2-methyl-n-pentylamine, 3-methyl-n-pentylamine, 4-methyl-n-pentylamine, 1,1-dimethyl-n-butylamine, 1,2-dimethyl-n-butylamino, 1,3-dimethyl-n-butylamino, 2,2-dimethyl-n-butylamino, 2,3-dimethyl-n-butylamino, 3,3-dimethyl-n-butylamino, 1-ethyl-n-butylamino, 2-ethyl-n-butylamino, 1,1,2-trimethyl-n-propylamino, 1,2,2-trimethyl-n-propylamino, 1-ethyl-1-methyl-n-propylamino, 1-ethyl-2-methyl-n-propylamino, C-hexylamine, 1-methyl-C-pentylamine, 2-methyl-C-pentylamine, 3-methyl-C-pentylamine, 1-ethyl-C-butylamino, 2-ethyl-C-butylamine, 3-ethyl-C-butylamine, 1,2-dimethyl-C-butylamino, 1,3-dimethyl-C-butylamino, 2,2-dimethyl-C-butylamino, 2,3-dimethyl-C-butylamino, 2,4-dimethyl-C-butylamino, 3,3-dimethyl-C-butylamino, 1-n-propyl-C-propylamino, 2-n-propyl-C-propylamino, 1-isopropyl-C-propylamino, 2-isopropyl-C-propylamino, 1,2,2-trimethyl-C-propylamino, 1,2,3-trimethyl-C-propylamino, 2,2,3-trimethyl-C-propylamino, 1-ethyl-2-methyl-C-propylamino, 2-ethyl-1-methyl-C-propylamino, 2-ethyl-2-methyl-C-propylamino, 2-ethyl-3-methyl-C-propylamino, 1-methyl-1-ethyl-n-pentylamine, 1 heptylamine, 2-heptylamine, 1-ethyl-1,2-dimethyl-n-propylamino, 1-ethyl-2,2-d is methyl-n-propylamino, 1 octylamine, 3 octylamine, 4-methyl-3-n-heptylamine, 6-methyl-2-n-heptylamine, 2-propyl-1-n-heptylamine, 2,4,4-trimethyl-1-n-pentylamine, 1 nonylamine, 2-nonylamine, 2,6-dimethyl-4-n-heptylamine, 3-ethyl-2,2-dimethyl-3-n-pentylamine, 3,5,5-trimethyl-1-n-hexylamino, 1 decylamine, 2-decylamine, 4-decylamine, 3,7-dimethyl-1-n-octylamine, 3,7-dimethyl-3-n-octylamine or the like.

C1-10dialkylamino may be symmetrical or asymmetrical. Symmetric C1-10dialkylamino can be linear, branched, or a C3-10cycloalkylation, and here we can mention dimethylamino, diethylamino, di-n-propylamino, diisopropylamino, di-t-propylamino, di-n-butylamino, diisobutylamine, di-sec-butylamino, di-tert-butylamino, di-t-butylamino, di(1-methyl-C-propyl)amino, di(2-methyl-C-propyl)amino, di-n-pentylamine, di(1-methyl-n-butyl)amino, di(2-methyl-n-butyl)amino, di(3-methyl-n-butyl)amino, di(1,1-dimethyl-n-propyl)amino, di(1,2-dimethyl-n-propyl)amino, di(2,2-dimethyl-n-propyl)amino, di(1-ethyl-n-propyl)amino, di-t-pentylamine, di(1-methyl-C-butyl)amino, di(2-methyl-C-butyl)amino, di(3-methyl-C-butyl)amino, di(1,2-dimethyl-C-propyl)amino, di(2,3-dimethyl-C-propyl)amino, di(1-ethyl-C-propyl)amino, di(2-ethyl-C-propyl)amino, di-n-hexylamino, di(1-methyl-n-pentyl)amino, di(2-methyl-n-pentyl)amino, di(3-methyl-n-pentyl)amino, di(4-methyl-n-Pentti is)amino, di(1,1-dimethyl-n-butyl)amino, di(1,2-dimethyl-n-butyl)amino, di(1,3-dimethyl-n-butyl)amino, di(2,2-dimethyl-n-butyl)amino, di(2,3-dimethyl-n-butyl)amino, di(3,3-dimethyl-n-butyl)amino, di(1-ethyl-n-butyl)amino, di(2-ethyl-n-butyl)amino, di(1,1,2-trimethyl-n-propyl)amino, di(1,2,2-trimethyl-n-propyl)amino, di(1-ethyl-1-methyl-n-propyl)amino, di(1-ethyl-2-methyl-n-propyl)amino, di-t-hexylamino, di(1-methyl-C-pentyl)amino, di(2-methyl-C-pentyl)amino, di(3-methyl-C-pentyl)amino, di(1-ethyl-C-butyl)amino, di(2-ethyl-t-butyl)amino, di(3-ethyl-t-butyl)amino, di(1,2-dimethyl-C-butyl)amino, di(1,3-dimethyl-C-butyl)amino, di(2,2-dimethyl-C-butyl)amino, di(2,3-dimethyl-C-butyl)amino, di(2,4-dimethyl-C-butyl)amino, di(3,3-dimethyl-C-butyl)amino, di(1-n-propyl-C-propyl)amino, di(2-n-propyl-C-propyl)amino, di(1-isopropyl-C-propyl)amino, di(2-isopropyl-C-propyl)amino, di(1,2,2-trimethyl-C-propyl)amino, di(1,2,3-trimethyl-C-propyl)amino, di(2,2,3-trimethyl-C-propyl)amino, di(1-ethyl-2-methyl-C-propyl)amino, di(2-ethyl-1-methyl-C-propyl)amino, di(2-ethyl-2-methyl-C-propyl)amino, di(2-ethyl-3-methyl-C-propyl)amino, di(1-methyl-1-ethyl-n-pentyl)amino, di(1-heptyl)amino, di(2-heptyl)amino, di(1-ethyl-1,2-dimethyl-n-propyl)amino, di(1-ethyl-2,2-dimethyl-n-propyl)amino, di(1-octyl)amino, di(3-octyl)amino, di(4-methyl-3-n-heptyl)amino, di(6-methyl-2-n-heptyl)amino, di(2-propyl-1-n-heptyl)amino, di(2,4,4-trimethyl-1-n-pentyl)amino, di(1-nonyl)amino, di(2 nonyl)amino, di(2,6-dime the Il-4-n-heptyl)amino, di(3-ethyl-2,2-dimethyl-3-n-pentyl)amino, di(3,5,5-trimethyl-1-n-hexyl)amino, di(1-decyl)amino, di(2-decyl)amino, di(4-decyl)amino, di(3,7-dimethyl-1-n-octyl)amino, di(3,7-dimethyl-3-n-octyl)amino or the like.

Asymmetric C1-10dialkylamino can be linear, branched, or a C3-10cycloalkylation, and there can be mentioned methyl, ethyl)amino, (methyl, n-propyl)amino, (methyl, isopropyl)amino, (methyl, C-propyl)amino, (methyl, n-butyl)amino, (methyl, isobutyl)amino, (methyl, sec-butyl)amino, (methyl, tert-butyl)amino, (methyl, n-pentyl)amino, (methyl, C-pentyl)amino, (methyl, n-hexyl)amino, (methyl, t-hexyl)amino, (ethyl, n-propyl)amino, (ethyl, isopropyl)amino, (ethyl, C-propyl)amino, (ethyl, n-butyl)amino, (ethyl, isobutyl)amino, (ethyl, sec-butyl)amino, (ethyl, tert-butyl)amino, (ethyl, n-pentyl)amino, (ethyl, t-pentyl)amino, (ethyl, n-hexyl)amino, (ethyl, t-hexyl)amino, n-propyl, isopropyl)amino, n-propyl, C-propyl)amino, n-propyl, n-butyl)amino, n-propyl, isobutyl)amino, n-propyl, sec-butyl)amino, n-propyl, tert-butyl)amino, n-propyl, n-pentyl)amino, n-propyl, t-pentyl)amino, n-propyl, n-hexyl)amino, (n-propyl, t-hexyl)amino, (isopropyl, C-propyl)amino, (isopropyl, n-butyl)amino, (isopropyl, isobutyl)amino, (isopropyl, sec-butyl)amino, (isopropyl, tert-butyl)amino, (isopropyl, n-pentyl)amino, (isopropyl, t-pentyl)the Mino, (isopropyl, n-hexyl)amino, (isopropyl, t-hexyl)amino, (C-propyl, n-butyl)amino, (C-propyl, isobutyl)amino, (C-propyl, sec-butyl)amino, (C-propyl, tert-butyl)amino, (C-propyl, n-pentyl)amino, (C-propyl, C-pentyl)amino, (C-propyl, n-hexyl)amino, (C-propyl, C-hexyl)amino, n-butyl, isobutyl)amino, n-butyl, sec-butyl)amino, n-butyl, tert-butyl)amino, n-butyl, n-pentyl)amino, n-butyl, t-pentyl)amino, n-butyl, n-hexyl)amino, n-butyl, t-hexyl)amino, (isobutyl, sec-butyl)amino, (isobutyl, tert-butyl)amino, (isobutyl, n-pentyl)amino, (isobutyl, t-pentyl)amino, (isobutyl, n-hexyl)amino, (isobutyl, t-hexyl)amino, (sec-butyl, tert-butyl)amino, (sec-butyl, n-pentyl)amino, (sec-butyl, t-pentyl)amino, (sec-butyl, n-hexyl)amino, (sec-butyl, t-hexyl)amino, (tert-butyl, n-pentyl)amino, (tert-butyl, C-pentyl)amino, (tert-butyl, n-hexyl)amino, (tert-butyl, C-hexyl)amino, (n-pentyl, C-pentyl)amino, (n-pentyl, n-hexyl)amino, (n-pentyl, C-hexyl)amino, (C-pentyl, n-hexyl)amino, (C-pentyl, C-hexyl)amino, n-hexyl, t-hexyl)amino, (methyl n-heptyl)amino, (methyl, n-octyl)amino, (methyl, n-nonyl)amino, (methyl, n-decyl)amino, (methyl, n-heptyl)amino, (ethyl, n-octyl)amino, (ethyl, n-nonyl)amino, (ethyl, n-decyl)amino or the like.

The protective group in the protected hydroxyl group may be a C1-4alkoxymethyl group (such as MOM: labels shall Ketil, MEM: 2-methoxyethoxymethyl, ethoxyethyl, n-propoxymethyl, isopropoxide, n-butoxymethyl, iBM: isobutylacetate, BUM: tert-butoxymethyl, POM: pivaloyloxymethyl, SEM: trimethylsilylethynyl and the like, preferably C1-2alkoxymethyl or the like), aryloxyalkyl (such as BOM: benzyloxyethyl, PMBM: p-methoxyethoxymethyl, p-AOM: the p-antilocality and the like), C1-4acylaminoalkyl group (such as dimethylaminomethyl), substituted acetamidomethyl group (such as Acm: atsetamidometil, Tacm: trimethylacetamido and the like), substituted thiomethyl group (such as MTM: methylthiomethyl, PTM: phenylthiomethyl, Btm: benzyldimethyl and the like), a carboxyl group, a C1-7acyl group (such as formyl, acetyl, peracetyl, divercity, TRIFLUOROACETYL, chloroacetyl, dichloroacetyl, trichloroacetyl, propionyl, Pv: pivaloyl, tignol and the like), arylcarbamoyl group (such as benzoyl, benzoylformate, benzoylpropionic, phenylpropionyl and the like), C1-4alkoxycarbonyl group (such as methoxycarbonyl, etoxycarbonyl, n-propoxycarbonyl, isopropoxycarbonyl, n-butoxycarbonyl, isobutoxide, BOC: tert-butoxycarbonyl, AOC: tert-aryloxyalkyl, VOC: vinyloxycarbonyl, AOC: allyloxycarbonyl, Teoc: 2-(trimethylsilyl)etoxycarbonyl, Troc: 2,2,2-trichlorethene the Nile, and the like, preferably BOC, and the like), aryloxyalkyl group (such as Z: benzyloxycarbonyl, p-nitrobenzenesulfonyl, MOZ: p-methoxybenzenesulfonyl and the like), C1-4alkylaminocarbonyl group (such as methylcarbamoyl, Ec: ethylcarbitol, n-propellerblades and the like), arylaminomethylene group (such as phenylcarbamoyl and the like), trialkylsilyl group (such as TMS: trimethylsilyl, TES: triethylsilyl, TIPS: triisopropylsilyl, DEIPS: diethylenediamine, DMIPS: dimethylazobenzene, DTBMS: di-tert-butylmethylether, IPDMS: isopropylimidazole, TBDMS: tert-butyldimethylsilyl, TDS: existimatio and the like, preferably tert-butyldimethylsilyl and the like), trialkylsilyl group (such as DPMS: diphenylmethylsilane, TBDPS: tert-butyldiphenylsilyl, TBMPS: tert-butyldimethylsilyl, TPS: triphenylsilanol and the like), alkylsulfonyl group (such as Ms: methanesulfonyl, econsultancy and the like) or arylsulfonyl group (such as benzazolyl, Ts: p-toluensulfonyl, p-chlorobenzenesulfonyl, MBS: p-methoxybenzenesulfonyl, m-nitrobenzenesulfonyl, iMds: 2,6-dimethoxy-4-methylbenzenesulfonyl, Mds: 2,6-dimethyl-4-methoxybenzenesulfonyl, Mtb: 2,4,6-trimethoxybenzylamine, Mte: 2,3,5,6-tetramethyl-4-methoxybenzenesulfonyl, Mtr: 2,3,6-trimethyl-4-methoxybenzenesulfonyl, Mts:2,4,6-trimethylbenzenesulfonyl, Pme: pentamethylbenzene and the like).

Specific preferred examples of the substituent R1is phenyl group, thienyl group (2-thienyl group and 3-thienyl group), furilla group (2-furilla group and 3-furilla group), pyridazinyl group (3-pyridazinyl group and 4-pyridazinyl group), Peregrina group (2-Peregrina group, 3-Peregrina group and 4-Peregrina group), kinolinna group (2-kinolinna group, 3-kinolinna group, 4-kinolinna group, 5-kinolinna group, 6-kinolinna group, 7-kinolinna group and 8 kinolinna group) and izochinolina group (1-izochinolina group, 3-izochinolina group, 4-izochinolina group, 5-izochinolina group, 6-izochinolina group, 7-izochinolina group and 8-izochinolina group), optionally substituted by one or more of the following substituents.

Deputies: C1-10alkyl group, a halogen atom, a C1-10alkyl group substituted by one or more halogen atoms, C1-10alkoxygroup substituted by one or more halogen atoms, the nitro-group, amino group, amino group, substituted by one or two C1-10alkyl group, amino group, substituted C1-10alkylcarboxylic group, Tolna group, substituted C1-10alkyl group, thio the other group, substituted C1-10alkylcarboxylic group, a hydroxyl group, a C1-6alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group.

Particularly preferred examples of the substituent R1is phenyl group, thienyl groups (a 2-thienyl group and 3-thienyl group), furilla group (2-furilla group and 3-furilla group), pyridazinyl group (3-pyridazinyl group and 4-pyridazinyl group), Peregrina group (2-Peregrina group, 3-Peregrina group and 4-Peregrina group), kinolinna group (2-kinolinna group, 3-kinolinna group, 4-kinolinna group, 5-kinolinna group, 6-kinolinna group, 7-kinolinna group and 8 kinolinna group) and izochinolina group (1-izochinolina group, 3-izochinolina group, 4-izochinolina group, 5-izochinolina group, 6-izochinolina group, 7-izochinolina group and 8-izochinolina group), optionally substituted by one or more of the following substituents.

Substituents: methyl group, tert-bucilina group, triptorelin group, tripterocarpa, a chlorine atom, a bromine atom, a fluorine atom, a methoxy group, methylaminopropyl, dimethylaminopropyl, tert-butylacrylate and tert-butylamino.

Even more preferred Conques is to maintain examples of the substituents include 3-methylphenylene group, 4-methylphenylene group, 3,4-dimethylaniline group, 3-tert-butylphenyl group, 4-tert-butylphenyl group, 3-triftormetilfullerenov group, 4-triphtalocyaninine group, 4-triftormetilfullerenov group, 3,4-dateformatstring group, 3-chloraniline group, 4-chloraniline group, 4-bratinella group, 3-Fortunella group, 4-Fortunella group, 3,4-dichloraniline group, 4-metoksifenilny group, 4-methylaminophenol group, 3-methylcytidine group, 4-methylcytidine group, 3,4-dimethylaniline group 3-tert-butylaniline group, 4-tert-butylaniline group, 3-triphtalocyaninine group, 4-triphtalocyaninine group, 3,4-dateformatpattern group, 3-chloraniline group, 4-chloraniline group, 3-forceinline group, 4-forceinline group, 3,4-dichloraniline group, 4-methoxytyramine group, 4-methylenedianiline group, 3-methylphenylene group, 4-methylphenylene group, 3,4-dimethylpyridine group, 3-tert-butifully group, 4-tert-butifully group, 3-triftormetilfullerenov group, 4-triftormetilfullerenov group, 3,4-dateformat.full group, 3-clorfenamina group, 4-clorfenamina group, 3-Tortorella group, 4-Tortorella group, 3,4-dichloropyridine group, 4-methoxypyridine group, 4-methylphenylene group, 5-chloropyridinyl GRU is PA, 5-metilprednisolona group, 5-methoxypyridazine group, 4-chloropyridinyl group, 4-metilprednisolona group, 4-methoxypyridazine group, 4-tert-butoxypyridine group and the like.

Specific preferred examples of L1are communications, CH2, an oxygen atom, a sulfur atom, NH, N-Me, N-CHO, CHMe, CMe2N-CH2Ph and the like, and particularly preferred examples are communication, CH2, an oxygen atom, a sulfur atom, NH, NMe and the like.

Specific preferred examples of the substituent R2are a hydrogen atom, methyl group, ethyl group, n-sawn group, isopropyl group, tert-bucilina group and phenyl group (methyl group, ethyl group, n-sawn group, isopropyl group, tert-bucilina group and the phenyl group optionally may be substituted amino group, monomethylamine, dimethylaminopropoxy, monoethyleneglycol, diethylaminopropyl, a methoxy group, ethoxypropane, methoxycarbonyl group, ethoxycarbonyl group, methylcarbonate, ethylcarboxylate, methylcarbaniloyloxy or ethylcarbodiimide and the like), and particularly preferred examples include a hydrogen atom, methyl group, ethyl group, n-sawn group, ISO-propyl, y is the SCP, tert-bucilina group, phenyl group and the like.

Specific preferred examples of L2are communications, CH2, an oxygen atom, a sulfur atom, NH, N-Me, N-CHO, CHMe, CMe2N-CH2Ph and the like, and particularly preferred examples are communication, CH2, an oxygen atom, a sulfur atom, NH, NMe and the like.

Specific preferred examples of L3are communications, CH2, an oxygen atom, a sulfur atom, NH, NH-OH, N-Me, N-CHO, CHMe, CMe2N-CH2PH and the like, and particularly preferred examples are communication, CH2, an oxygen atom, a sulfur atom, NH, NMe and the like.

Specific preferred examples of X are OH, SH, NH2, OMe, SMe, NHMe, NHEt, NH-CHO, NH-CH2Ph-OCH2Ph, SCH2Ph, OC(=O)CH3SC(=O)CH3, NHC(=O)CH3and the like, and particularly preferred examples are OH, SH, NH2and the like.

Specific preferred examples of Y are an oxygen atom, a sulfur atom, NH, N-OH, N-CHO, N-Me, N-CH2Ph, N-OMe, N-OCH2Ph and the like, and particularly preferable examples include an oxygen atom, a sulfur atom, NH, N-OH and the like.

Specific preferred examples of L4are communications, CH2, an oxygen atom, a sulfur atom, NH, N-Me, N-CHO, CHMe, CMe2N-CH2Ph and the like, and particularly preferred examples are tie is, CH2, an oxygen atom, a sulfur atom, NH, NMe and the like.

Specific preferred examples of the substituent R3are methyl group, ethyl group, n-sawn group, isopropyl group, n-bucilina group, sec-bucilina group, tert-bucilina group, t-through group, C-bucilina group, C-pencilina group, C-exilda group, etinilnoy group, 1-proponila group, 2-proponila group, 1-Butyrina group, 2-Butyrina group, 3-Butyrina group, 1-penicilina group, 2-penicilina group, 4-penicilina group, 1-methyl-2-Butyrina group, 1-methyl-3-Butyrina group, 2-methyl-3-Butyrina group, 3-methyl-1-Butyrina group and the following heterocyclic group, optionally substituted by one or more of the following substituents.

Heterocyclic group

Substituents: hydrogen atom, hydroxyl group, amino group, halogen atom, the nitro-group, Tolna group, carboxyl group, phosphonic acid group, a sulfonic acid group, carnemolla group, hydroxycarbamoyl group, cyanocarbonimidate group, alfamarine group, hydroxysultaine group, cyanomethylene group, tetryzoline group, phenyl group, thienyl group, Peregrina group, furilla group, -CH2CO 2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, -(C=O)CO2H, -CH2(C=O)CO2H, -NH(C=O)CO2H, -NHS(=O)2NH2C1-10alkyl group, (C1-10the alkyl group may be substituted by one or more substituents selected from the group consisting of hydroxyl groups, carboxyl groups, the following aryl groups, the following heterocyclic groups, and C1-10alkylamino (C1-10alkylamino can be substituted by one or more of the following aryl groups or one or more of the heterocyclic group)), C2-10Alchemilla group, C2-10Alchemilla group, C2-9heterocyclic group, a C1-10Tolkalina group, C1-10alkoxygroup, C1-10acylcarnitine group, C1-10alkylaminocarbonyl group, C1-10dialkylaminoalkyl group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, aminocarbonyl group, C1-10alkylcarboxylic (C1-10alkoxygroup, C1-10acylcarnitine group, C1-10alkylaminocarbonyl group, C1-10dialkylaminoalkyl group, mono - or di-C1-10alkylamino, C1-10Alki carbonyloxy, C1-10alkoxycarbonyl group, aminocarbonyl group and C1-10alkylcarboxylic can be substituted by one or more substituents selected from the group consisting of carboxyl groups, carbamoyl groups, sulfamoyl groups, sulfo, amino groups, the following aryl groups and the following heterocyclic groups), the following aryl group, and these heterocyclic groups.

Aryl group: phenyl group, thienyl groups (a 2-thienyl group and 3-thienyl group), furilla group (2-furilla group and 3-furilla group), pyridazinyl group (3-pyridazinyl group and 4-pyridazinyl group), perederina groups (2-Peregrina group, 3-Peregrina group and 4-Peregrina group), pyrimidinyl group (2-pyrimidinyl group, 4-pyrimidinyl group and 5-pyrimidinyl group), kinolinna group (2-kinolinna group, 3-kinolinna group 4-kinolinna group, 5-kinolinna group, 6-kinolinna group, 7-kinolinna group and 8-kinolinna group) and izochinolina group (1-izochinolina group, 3-izochinolina group, 4-izochinolina group, 5-izochinolina group, 6-izochinolina group, 7-izochinolina group and 8-izochinolina group).

Heterocyclic groups: group 1,3,4-oxadiazole, group, 1,3,4-thiadiazole, group, 1,2,4-oxadiazole, g is the SCP 1,2,4-thiadiazole, group 1,2,5-oxadiazole, group, 1,2,5-thiadiazole, group, 1,2-oxazole and the group of 1,2-thiazole.

In addition, specific preferred examples of the substituent R3are methyl group, ethyl group, n-sawn group, isopropyl group, n-bucilina group, sec-bucilina group, tert-bucilina group, t-through group, C-bucilina group, C-pencilina group, C-exilda group, etinilnoy group, 1-proponila group, 2-proponila group, 1-Butyrina group, 2-Butyrina group, 3-Butyrina group, 1-penicilina group, 2-penicilina group, 4-penicilina group, 1-methyl-2-Butyrina group, 1-methyl-3-Butyrina group, 2-methyl-3-Butyrina group, 3-methyl-1-Butyrina group and the following heterocyclic group, optionally substituted by one or more substituents arbitrarily selected from a set of substituents, and one or more substituents arbitrarily selected from a set of substituents Century

Heterocyclic group

The set of substituents A: hydroxyl group, amino group, carboxyl group, phosphonic acid group, a sulfonic acid group, carnemolla group, hydroxycarbamoyl group, cyanocarbonimidate group, alfamarine group, hydroxysultaine group, cyanomethylene gr is the PAP group tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H and alkoxycarbonyl group.

The set of substituents B: a hydroxyl group, amino group, carboxyl group, phosphonic acid group, a sulfonic acid group, carnemolla group, hydroxycarbamoyl group, cyanocarbonimidate group, alfamarine group, a nitrogroup, cyano, a halogen atom, a C1-10alkyl group, a C1-10alkyl group substituted by one or more fluorine atoms, alfamarine group, substituted C1-10alkyl group, carnemolla group, substituted C1-10alkyl group, a C1-10alkylcarboxylic and C1-10alkylaminocarbonyl group (C1-10alkylcarboxylic and C1-10alkylaminocarbonyl group may be substituted by one or more substituents selected from the group consisting of phenyl groups, peredelnyh groups, thienyl groups, and fueling groups).

The preferred compounds as an activator receptor thrombopoetin, preventive, therapeutic or improving agent for diseases in which the effective activation of the receptor thrombopoetin, and the agent that increases the number of platelets, according to the present invention are as follows.

1)Connection represented by formula (1), where A represents a nitrogen atom and B represents a sulfur atom, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

2) Compounds represented by the formula (1), where A represents a nitrogen atom and B represents an oxygen atom, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

3) Compounds represented by the formula (1), where A represents a nitrogen atom and B represents NR9different from NH (where R9represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic the SCP, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy) or C2-14alloctype (C2-14alloctype may not necessarily replace the s with one or more substituents, selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

4) Compounds represented by the formula (1), where A is a CR4(where R4represents a hydrogen atom, a hydroxyl group (the hydroxyl group may be substituted C2-6alkenylphenol group or a C2-6alkenylphenol group), Tilney group (Tolna group may be substituted C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkenylphenol group or a C1-10alkylcarboxylic group), amino group (the amino group may be substituted by one or two C2-6alkenylamine groups or one or two C2-6alkenylamine groups), a formyl group, an atom g is lagena, the nitrogroup, cyano, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkylcarboxylic, mono - or di-C1-10alkylamino, C1-10alkoxygroup (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkylcarboxylic, mono - or di-C1-10alkylamino and C1-10alkoxygroup optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected is from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups and2-14aryloxy), C2-14alloctype (C2-14alloctype optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy), SO 2R5, SOR5or COR5(where R5represents a hydroxyl group, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group and C1-10alkoxygroup optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be Emesene one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy), C2-14alloctype (C2-14alloctype optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy) or NR6R7(where each of R6and R7independently represents a hydrogen atom, hydroxyl group, farmilo the group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from g is uppy, consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy), or R6and R7together with each other, means -(CH2)m1-E-(CH2)m2- (where E represents an oxygen atom, a sulfur atom, CR26R27(where each of R26and R27independently represents a hydrogen atom, a C1-10alkyl group, a C2-14aryl group, a C1-10alkoxygroup, C2-14alloctype, a hydroxyl group or a protected hydroxyl group) or NR8(where R8represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylsulphonyl the ing group (C 1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6alkyne is selected groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)), and each of m1 and m2 independently represents an integer from 0 to 5 provided that m1+m2 is 3, 4 or 5)))) and B represents an oxygen atom, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

5) Compounds represented by the formula (1), where a is a CR4(where R4represents a hydrogen atom, a hydroxyl group (the hydroxyl group may be substituted C2-6alkenylphenol group or a C2-6alkenylphenol group), Tilney group (Tolna group may be substituted C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkenylphenol group or a C1-10alkylcarboxylic group), amino group (the amino group may be substituted by one or two C2-6alkenylamine groups or one or two C2-6alkenylamine groups), a formyl group, a halogen atom, a nitro-group, a cyano, C1-10alkyl group, a C2- alkenylphenol group, C2-6alkylamino group, C1-10alkylcarboxylic, mono - or di-C1-10alkylamino, C1-10alkoxygroup (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkylcarboxylic, mono - or di-C1-10alkylamino and C1-10alkoxygroup optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10and kilenyi group may be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups and2-14aryloxy), C2-14alloctype (C2-14alloctype optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy), SO2R5, SOR5or COR5(where R5represents a hydroxyl group, a C1-10alkyl group, a C2-6 alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group and C1-10alkoxygroup optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, n is regroup, of cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy), C2-14alloctype (C2-14alloctype optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy) or NR6R7(where each of R6and R7independently represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino g is the SCP, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be Zam is prevented by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy), or R6and R7together with each other, means -(CH2)m1-E-(CH2)m2- (where E represents an oxygen atom, a sulfur atom, CR26R27(where each of R26and R27independently represents a hydrogen atom, a C1-10alkyl group, a C2-14aryl group, a C1-10alkoxygroup, C2-14alloctype, a hydroxyl group or a protected hydroxyl group) or NR8(where R8represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10 alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alquiler onilne groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)), and each of m1 and m2 independently represents an integer from 0 to 5 provided that m1+m2 is 3, 4 or 5)))) and B represents a sulfur atom, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

6) Compounds represented by the formula (1), where a is a CR4(where R4represents a hydrogen atom, a hydroxyl group (the hydroxyl group may be substituted C2-6alkenylphenol group or a C2-6alkenylphenol group), Tilney group (Tolna group may be substituted C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkenylphenol group or a C1-10alkylcarboxylic group), amino group (the amino group may be substituted by one or two C2-6alkenylamine groups or one or two C2-6alkenylamine groups), a formyl group, a halogen atom, a nitro-group, a cyano, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkylcarboxylic, mono - or di-C1-10alkylamino the PPU, C1-10alkoxygroup (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkylcarboxylic, mono - or di-C1-10alkylamino and C1-10alkoxygroup optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik g the SCP, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups and2-14aryloxy), C2-14alloctype (C2-14alloctype optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy), SO2R5, SOR5or COR5(where R5represents a hydroxyl group, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-0 alkoxygroup (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group and C1-10alkoxygroup optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxy is PP, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy), C2-14alloctype (C2-14alloctype optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy) or NR6R7(where each of R6and R7independently represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups 2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy), or R6and R7together with each other, means -(CH2)m1-E-(CH2)m2- (where E represents an oxygen atom, a sulfur atom, CR26R27(where each of R26and R27independently represents a hydrogen atom, a C1-10alkyl group, a C2-14aryl group, a C1-10alkoxygroup, C2-14alloctype, a hydroxyl group or a protected hydroxyl group) or NR8(where R8represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic,C 1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10Ala is carbonyloxy, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)), and each of m1 and m2 independently represents an integer from 0 to 5 provided that m1+m2 is 3, 4 or 5)))) and B represents NR9(where R9represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected the military hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy) or C2-14alloctype (C2-14alloctype optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more atoms and halogen), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

7) Compounds represented by the formula (1), paragraph (4), 5) or 6), where A is a CR37(where R37represents a hydrogen atom, a hydroxyl group (the hydroxyl group may be substituted C2-6alkenylphenol group or a C2-6alkenylphenol group), Tilney group (Tolna group may be substituted C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkenylphenol group or a C1-10alkylcarboxylic group), amino group (the amino group may be substituted by one or two C2-6alkenylamine groups or one or two C2-6alkenylamine groups), a formyl group, a halogen atom, a nitro-group, a cyano, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10 alkoxygroup, C1-10alkylcarboxylic, mono - or di-C1-10alkylamino (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic and mono - or di-C1-10alkylamino can be substituted by one or more substituents selected from the group consisting of halogen atoms, carboxyl groups, nitro groups and cyano groups), SO2R38, SOR38or COR38(where R38represents a hydroxyl group, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group and C1-10alkoxygroup optionally can be substituted by one or more substituents selected from the group consisting of halogen atoms, carboxyl groups, nitro groups and cyano groups), C2-14aryl group or a C2-14alloctype (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups may be substituted by one or more halogen atoms) or one or more halogen atoms))), tautomers, prodrugs or pharmaceutically when mimie salts of the compounds or their solvate. The terms used in the application to the respective substituents R37and R38are the same as used to refer to the respective substituents R1-R36.

8) Compounds represented by the formula (1), paragraph (3) or 6), where B represents NR39(where R39represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group may be substituted by one or more substituents selected from the group consisting of carboxyl groups, halogen atoms, nitro groups and cyano groups), C2-14aryl group or a C2-14alloctype (C2-14aryl group, and C2-14alloctype can be substituted by one or more substituents selected from the group consisting of C1-6alkyl groups (C1-6alkyl groups may be substituted by one or more atoms halog is on), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups and halogen atoms)), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate. The terms used in the application to the appropriate Deputy R39are the same as used to refer to the respective substituents R1-R36.

9) Compounds represented by the formula (1), under item 1), 2), 3), 4), 5), 6), 7) or 8), where L1represents a bond, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

10) Compounds represented by the formula (1), under item 1), 2), 3), 4), 5), 6), 7), 8) or 9), where L2represents a bond, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

11) Compounds represented by the formula (1), under item 1), 2), 3), 4), 5), 6), 7), 8), 9) or 10), where L3represents NR19(where R19represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C 2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, automob halogen, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6the alkyl group may be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyanoprop is, automob halogen, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

12) Compounds according to paragraph 1), 2), 3), 4), 5), 6), 7), 8), 9) or 10), where L3represents NH, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

13) Connection point 1), 2), 3), 4), 5), 6), 7), 8), 9) or 10), where L3represents CH2, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

14) Compounds according to paragraph 11), 12) or (13), where R2represents a hydrogen atom, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group and C1-10alkoxygroup optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, 1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl group or a C2-14alloctype (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

15) the Compound according to item 11), 12) or (13), where R2represents a hydrogen atom, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-3alkoxygroup (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group and C1-3alkoxygroup not necessarily bytesneeded one or more substituents, selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, phenyl groups and fenoxaprop (phenyl groups and fenoxaprop can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), a phenyl group, or fenoxaprop (phenyl group and fenoxaprop can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

16) Compounds according to paragraph 11), 12) or (13), where R2represents a hydrogen atom, a C1-10alkyl group, a C2-6alkenylphenol group or a C2-6alkylamino group (C1-10alkyl group, a C2-6Alchemilla group and C2-6Alchemilla group is not necessarily the be substituted by one or more substituents, selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, a hydroxyl group and a protected hydroxyl groups), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

17) the Compound according to item 11), 12) or (13), where R2represents a hydrogen atom or a C1-6alkyl group, (C1-6alkyl group optionally may be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, a hydroxyl group and a protected hydroxyl groups), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

18) the Compound according to item 11), 12) or (13), where R2represents a hydrogen atom or a C1-3alkyl group, (C1-3alkyl group optionally mo is et to be substituted by one or more substituents, selected from the group consisting of halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, a hydroxyl group and a protected hydroxyl groups), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

19) of the Connection point 14), 15), 16), 17) or 18), where R1represents a C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of halogen atoms, carboxyl groups, nitro groups, formyl groups, cyano groups, hydroxyl groups, protected hydroxyl groups, C1-10alkyl groups, C2-6alkenyl groups, C2-6etkinlik groups, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic (C1-10alkyl group, a C2-6alkeneamine group, C2-6alkyline groups and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), C2-14aryl group, a C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms), tylnej groups and amino groups (tirinya group and an amino group optionally can be substituted by one or more substituents selected from the group consisting of formyl group, a C1-10alkyl groups, C2-6alkenyl groups, C2-6etkinlik groups and C1-10alkylcarboxylic groups (C1-10alkyl group, a C2-6alkeneamine group, C2-6alkyline group and C1-10alkali monilinia group optionally can be substituted by one or more substituents, selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)))), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

20) of the Connection point 14), 15), 16), 17) or 18), where R1represents a phenyl group, thienyl group, follow group, pyridazinyl group, pyridyloxy group, pinolillo group or izohinolinove group (phenyl group, thienyl group, furilla group, pyridazinyl group, Peregrina group, kinolinna group and izochinolina group optionally can be substituted by one or more substituents selected from the group consisting of halogen atoms, carboxyl groups, nitro groups, forms the selected groups, of cyano groups, hydroxyl groups, protected hydroxyl groups, C1-10alkyl groups, C2-6alkenyl groups, C2-6etkinlik groups, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic (C1-10alkyl group, a C2-6alkeneamine group, C2-6alkyline group, C1-10alkoxygroup, C1-10acylcarnitine group, C1-10alkylcarboxylic and C1-10alkoxycarbonyl group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), tylnej groups and amino groups (TiAlN the e group and an amino group optionally can be substituted by one or more substituents, selected from the group consisting of formyl group, a C1-10alkyl groups, C2-6alkenyl groups, C2-6etkinlik groups C1-10alkylcarboxylic groups (C1-10alkyl group, a C2-6alkeneamine group, C2-6alkyline group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)))), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

21) of the Connection point 14), 15), 16), 17) or 18), where R1represents a phenyl group, thienyl group, follow group, pyridazinyl group, p is rigelnuyu group, pinolillo group or izohinolinove group (phenyl group, thienyl group, furilla group, pyridazinyl group, Peregrina group, kinolinna group and izochinolina group optionally can be substituted by one or more substituents selected from the group consisting of halogen atoms, carboxyl groups, nitro groups, formyl groups, cyano groups, hydroxyl groups, protected hydroxyl groups, C1-10alkyl groups, C2-6alkenyl groups, C2-6etkinlik groups, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic (C1-10alkyl group, a C2-6alkeneamine group, C2-6alkyline group, C1-10alkoxygroup, C1-10acylcarnitine group, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more substituents selected from the group consisting of halogen atoms, carboxyl groups, nitro groups and cyano groups), C2-14aryl group, a C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more atoms is of alogena) or one or more halogen atoms), tylnej groups and amino groups (tirinya group and an amino group optionally can be substituted by one or more substituents selected from the group consisting of formyl group, a C1-10alkyl groups, C2-6alkenyl groups, C2-6etkinlik groups and C1-10alkylcarboxylic groups (C1-10alkyl group, a C2-6alkeneamine groups, C2-6alkyline group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of halogen atoms, carboxyl groups, nitro groups, cyano groups, hydroxyl groups and protected gidroksilnyh groups)), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

22) of the Connection point 14), 15), 16), 17) or 18), where R1represents a phenyl group (the phenyl group optionally may be substituted by one or more substituents selected from the group consisting of halogen atoms, carboxyl groups, nitro groups, formyl groups, cyano groups, hydroxyl groups, protected hydroxyl groups, C1-10alkyl groups, C2-6alkenyl groups, C2-6etkinlik groups, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkoxycarbonyl groups, C1-10alkylboron is maxigrip (C 1-10alkyl group, a C2-6alkeneamine group, C2-6alkyline group, C1-10alkoxygroup, C1-10acylcarnitine group, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)), tylnej groups and amino groups (tirinya group and an amino group optionally can be substituted by one or more substituents selected from the group consisting of formyl group, a C1-10alkyl groups, C2-6alkenyl groups, C2-6etkinlik groups and C1-10alkylcarboxylic groups (C1-10alkyl the s group, C2-6alkeneamine group, C2-6alkyline group and C1-10alkylcarboxylic groups optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl, Groupama (C1-6the alkyl group may be substituted by one or more halogen atoms) or one or more halogen atoms)))), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

23) of the Connection point 14), 15), 16), 17) or 18), where R1represents a phenyl group (the phenyl group optionally may be substituted by one or more substituents selected from the group consisting of halogen atoms, carboxyl groups, nitro groups, formyl groups, cyano groups, hydroxyl groups, protected hydroxyl groups, C1-10/sub> alkyl groups, C2-6alkenyl groups, C2-6etkinlik groups, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic (C1-10alkyl group, a C2-6alkeneamine group, C2-6alkyline group, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more substituents selected from the group consisting of halogen atoms, carboxyl groups, nitro groups and cyano groups), C2-14aryl group, a C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms), tylnej groups and amino groups (tirinya group and an amino group optionally can be substituted by one or more substituents selected from the group consisting of formyl group, a C1-10alkyl groups, C2-6alkenyl groups, C2-6etkinlik groups and C1-10alkylcarboxylic groups (C1-10alkyl group, a C2-6alkeneamine group, C2-6alkyline g is uppy and C 1-10alkylcarboxylic groups optionally can be substituted by one or more substituents selected from the group consisting of halogen atoms, carboxyl groups, nitro groups, cyano groups, hydroxyl groups and protected hydroxyl groups)), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

24) of the Connection point 19), 20), 21), 22) or 23), where Y represents an oxygen atom, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

25) Connection point 19), 20), 21), 22) or 23), where Y represents a sulfur atom, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

26) the Compound according to item 24 or 25), where X represents a hydroxyl group, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

27) the Compound according to item 24), 25) or 26), where L4is a bond and R3represents ethyl group, n-sawn group, isopropyl group, n-boutelou group, sec-boutelou group, tert-boutelou group, t-through group, C-boutelou group, C-pentelow group, C-hexoloy group, etinilnoy group, 1-propenyloxy group, 2-propenyloxy group, 1-butenyloxy group, 2-butenyloxy group, 3-butenyloxy group, 1-p is tonilou group, 2-pantanillo group, 4-pantanillo group, 1-methyl-2-butenyloxy group, 1-methyl-3-butenyloxy group, 2-methyl-3-butenyloxy group, 3-methyl-1-butenyloxy group or any of the following heterocyclic groups:

(ethyl group, n-sawn group, isopropyl group, n-bucilina group, sec-bucilina group, tert-bucilina group, t-through group, C-bucilina group, C-pencilina group, C-exilda group, etinilnoy group, 1-proponila group, 2-proponila group, 1-Butyrina group, 2-Butyrina group, 3-Butyrina group, 1-penicilina group, 2-penicilina group, 4-penicilina group, 1-methyl-2-Butyrina group 1-methyl-3-Butyrina group, 2-methyl-3-Butyrina group, 3-methyl-1-Butyrina group and the above-mentioned heterocyclic group optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH-OH 2OH, -NHCH2OH, -CH2CH2OH, C1-10alkoxycarbonyl groups, C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups and C1-10alkylcarboxylic and the following aryl groups and heterocyclic groups, (C1-10alkyl group, a C2-10alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl group, C1-10acylcarnitine group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic and these aryl groups and heterocyclic groups optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, carboxyl groups, carbamoyl groups, groups, sulfonic acids and sulfamoyl groups):

aryl group: phenyl group, thienyl groups (a 2-thienyl group and 3-thienyl group), foreline group (2-furilla group and 3-furilla group), the feast of casinolinea group (3-pyridazinyl group and 4-pyridazinyl group), peredelnye group (2-Peregrina group, 3-Peregrina group and 4-Peregrina group), piratininga group, pyrimidinyl group (2-pyrimidinyl group, 4-pyrimidinyl group and 5-pyrimidinyl group), chinoline group (2-kinolinna group, 3-kinolinna group, 4-kinolinna group, 5-kinolinna group, 6-kinolinna group, 7-kinolinna group and 8-kinolinna group) and ethanolamine group (1-izochinolina group, 3-izochinolina group, 4-izochinolina group, 5-izochinolina group, 6-izochinolina group, 7-izochinolina group and 8-izochinolina group);

heterocyclic groups: group 1,3,4-oxadiazole, group, 1,3,4-thiadiazole, group, 1,2,4-oxadiazole, group, 1,2,4-thiadiazole, group, 1,2,5-oxadiazole, group, 1,2,5-thiadiazole, group, 1,2-oxazole, group, 1,2-thiazole, the group of 1,3-oxazole, group, 1,3-thiazole group, a pyrrole group, imidazole and a group of pyrazole), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

28) the Compound according to item 24), 25) or 26), where L4is a bond and R3represents a methyl group, ethyl group, n-sawn group, isopropyl group, n-boutelou group, sec-boutelou group, tert-boutelou group, t-through group, C-boutelou group, C-pentelow group, C-hexoloy group, atenolop, 1-propenyloxy group, 2-propenyloxy group, 1-butenyloxy group, 2-butenyloxy group, 3-butenyloxy group, 1-pantanillo group, 2-pantanillo group, 4-pantanillo group, 1-methyl-2-butenyloxy group, 1-methyl-3-butenyloxy group, 2-methyl-3-butenyloxy group, 3-methyl-1-butenyloxy group or any of the following heterocyclic groups:

(methyl group, ethyl group, n-sawn group, isopropyl group, n-bucilina group, sec-bucilina group, tert-bucilina group, t-through group, C-bucilina group, C-pencilina group, C-exilda group, etinilnoy group, 1-proponila group, 2-proponila group, 1-Butyrina group, 2-Butyrina group, 3-Butyrina group, 1-penicilina group, 2-penicilina group, 4-penicilina group, 1-methyl-2-Butyrina group, 1-methyl-3-Butyrina group, 2-methyl-3-Butyrina group, 3-methyl-1-Butyrina group and the above-mentioned heterocyclic group optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxysulfonic GRU is p, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, C1-10alkoxycarbonyl groups, C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylaminocarbonyl groups and C1-10alkylcarboxylic (C1-10alkyl group, a C2-10alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl group, C1-10acylcarnitine group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylaminocarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more substituents selected from the group consisting of C2-14aryl groups, hydroxyl groups, carboxyl groups, carbamoyl groups, groups, sulfonic acids and sulfamoyl groups), tautomers,prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

29) the Compound according to item 24), 25) or 26), where L4is a bond and R3represents a methyl group, ethyl group, n-sawn group, isopropyl group, n-boutelou group, t-through group, C-hexoloy group, etinilnoy group, 1-propenyloxy group, 2-propenyloxy group or 1-butenyloxy group (methyl group, ethyl group, n-sawn group, isopropyl group, n-bucilina group, t-through group, C-exilda group, etinilnoy group, 1-proponila group, 2-proponila group and 1-Butyrina group optionally can be substituted one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, C1-10alkoxycarbonyl groups, C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10tioal the ilen groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups and C1-10alkylcarboxylic (C1-10alkyl group, a C2-10alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl group, C1-10acylcarnitine group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, carboxyl groups, carbamoyl groups, groups, sulfonic acids and sulfamoyl groups)), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

30) the Compound according to item 24), 25) or 26), where L4is a bond and R3represents a methyl group, ethyl group, n-sawn group, isopropyl group, n-boutelou group, t-through group, C-hexoloy group, etinilnoy group, 1-propenyloxy group, 2-propenyloxy group or 1-butenyloxy group (methyl group, ethyl group, n-sawn group, isopropyl group, n-bucilina group, t-p is opalina group, C-exilda group, etinilnoy group, 1-proponila group, 2-proponila group and 1-Butyrina group optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH and C1-10alkoxycarbonyl groups), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

31) of the Connection point 24), 25) or 26), where L4is a bond and R3is any of the following heterocyclic groups:

(the above heterocyclic group optionally can be substituted by one or more substituents selected from the group consisting of hydrogen atoms, hydroxyl groups, amino groups, halogen atoms, nitro groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl g the SCP, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, phenyl group, thienyl groups, peredelnyh groups, fueling groups, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, -(C=O)CO2H, -CH2(C=O)CO2H, -NH(C=O)CO2H, -NHS(=O)2NH2C1-10alkoxycarbonyl groups, C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more substituents, wybranymi from the group consisting of hydroxyl groups, carboxyl groups, phenyl groups, 2-thienyl group, 3-thienyl group, 2-fueling groups, 3-fueling groups, 3-pyridazinyl groups, 4-pyridazinyl groups, 2-peredelnyh groups, 3-peredelnyh groups, 4-peredelnyh groups, personilnya groups, 2-pyrimidinyl groups, 4-pyrimidinyl groups, 5-pyrimidinyl groups, groups, 1,3-oxazolyl, groups, 1,3-thiazolyl, pyrrolidine groups, imidazolinium groups, parasailing groups, 2-finalising groups, 3-finalising groups, 4-finalising groups, 5-finalising groups, 6-finalising groups, 7-finalising groups, 8-finalising groups, 1-sochinyennykh groups, 3-sochinyennykh groups, 4-sochinyennykh groups, 5-sochinyennykh groups, 6 and kinally groups, 7-sochinyennykh groups, 8-sochinyennykh groups, groups, 1,3,4-oxadiazole, groups, 1,3,4-thiadiazole, groups, 1,2,4-oxadiazole, groups, 1,2,4-thiadiazole, groups 1,2,5-oxadiazole, groups 1,2,5-thiadiazole, groups, 1,2-oxazole, groups, 1,2-thiazole, and C1-10alkylaminocarbonyl groups (C1-10alkylaminocarbonyl group may be substituted by one or more substituents selected from the group consisting of phenyl groups, 2-thienyl group, 3-thienyl group, 2-fueling groups, 3-fueling groups, 3-pyridazinyl groups, 4-pyridazinyl groups, 2-peredelnyh groups, 3-peredelnyh groups, 4-peredelnyh groups, 2-finalising groups, 3-finalising groups, 4-finalising groups, 5-finalising groups, 6-finalising groups, 7-finalising groups, 8-finalising groups, 1-sochinyennykh groups, 3-sochinyennykh groups, 4-sochinyennykh groups, 5-sochinyennykh groups, 6-sochinyennykh groups, 7-sochinyennykh groups, 8-sochinyennykh groups, groups, 1,3,4-oxadiazole, groups, 1,3,4-thiadiazole, groups, 1,2,4-oxadiazole, groups, 1,2,4-thiadiazole, groups 1,2,5-oxadiazole, groups 1,2,5-thiadiazole, groups, 1,2-oxazole, groups, 1,2-thiazole, groups of 1,3-oxazole, groups, 1,3-thiazole, pyrrole groups, imidazole groups and pyrazol groups)), C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10thioalkyl groups, C1-10alkoxygroup, C1-10 alkylcarboxylic groups, C1-10alkylaminocarbonyl groups, C1-10dialkylaminoalkyl groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic (C1-10alkoxygroup, C1-10acylcarnitine group, C1-10alkylaminocarbonyl group, C1-10dialkylaminoalkyl group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic can be substituted by one or more substituents selected from the group consisting of carboxyl groups, carbamoyl groups, sulfamoyl groups, sulfo, phenyl group, 2-thienyl group, 3-thienyl group, 2-fueling groups, 3-fueling groups, 3-pyridazinyl groups, 4-pyridazinyl groups, 2-peredelnyh groups, 3-peredelnyh groups, 4-peredelnyh groups, 2-finalising groups, 3-finalising groups, 4-finalising groups, 5-finalising groups, 6-finalising groups, 7-finalising groups, 8-finalising groups, 1-sochinyennykh groups, 3-sochinyennykh groups, 4-sochinyennykh groups, 5-sochinyennykh groups, 6-sochinyennykh groups, 7-sochinyennykh groups, 8-sochinyennykh groups, groups, 1,3,4-oxadiazole, groups, 1,3,4-thiadiazole, groups, 1,2,4-oxadiazole groups 1,2,4-thiadiazole, groups 1,2,5-oxadiazole, groups 1,2,5-thiadiazole, groups, 1,2-oxazole, groups, 1,2-thiazole, groups of 1,3-oxazole, groups, 1,3-thiazole, pyrrole groups, imidazole groups and pyrazol groups), pyridylmethylene groups, phenyl groups, 2-thienyl group, 3-thienyl group, 2-fueling groups, 3-fueling groups, 3-pyridazinyl groups, 4-pyridazinyl groups, 2-peredelnyh groups, 3-peredelnyh groups, 4-peredelnyh groups, 2-finalising groups, 3-finalising groups, 4-finalising groups, 5-finalising groups, 6-finalising groups, 7-finalising groups, 8-finalising groups, 1-sochinyennykh groups, 3-sochinyennykh groups, 4-sochinyennykh groups, 5-sochinyennykh groups, 6-sochinyennykh groups, 7-sochinyennykh groups, 8-sochinyennykh groups, groups, 1,3,4-oxadiazole, groups, 1,3,4-thiadiazole, groups, 1,2,4-oxadiazole, groups, 1,2,4-thiadiazole, groups 1,2,5-oxadiazole, groups 1,2,5-thiadiazole, groups, 1,2-oxazole, groups, 1,2-thiazole groups of 1,3-oxazole, groups, 1,3-thiazole, pyrrole groups, imidazole groups and pyrazol groups), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

32) the Compound according to item 24), 25) or 26), where L4is a bond and R3is any of the following heterocyclic groups:

(the above heterocyclic group optionally mo the ut to be substituted by one or more substituents, selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, C1-10alkoxycarbonyl groups, C1-10alkyl groups, C1-10alkylcarboxylic groups, C1-10alkylsulfonyl groups, C1-10alkylaminocarbonyl groups, C1-10alkylaminocarbonyl groups and C1-10dialkylaminoalkyl groups (C1-10alkyl group, a C1-10acylcarnitine group, C1-10alkylsulfonyl group, C1-10alkylaminocarbonyl group, C1-10alkylaminocarbonyl group and C1-10dialkylaminoalkyl group may be substituted by one or more substituents selected from the group consisting of phenyl groups, thienyl groups, fueling groups, peredelnyh groups, nitro groups, cyano groups, hydroxyl groups, amino groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, sulfamoyl the x groups of tetrazole)), the tautomers, prodrugs or farmatsevticeski acceptable salts of the compounds or their solvate.

33) the Compound according to item 24), 25) or 26), where L4is a bond and R3is any of the following heterocyclic groups:

(the above heterocyclic group optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, C1-10alkoxycarbonyl groups, C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups and C1-10alkylcarboxylic (C1-10alkyl group, a C2-10 alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl group, C1-10acylcarnitine group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, carboxyl groups, carbamoyl groups, groups, sulfonic acids and sulfamoyl groups)), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

34) the Compound according to item 24), 25) or 26), where L4is a bond and R3is any of the following heterocyclic groups:

(the above heterocyclic groups optionally are substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H-OCHsub> 2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, C1-10alkoxycarbonyl groups, methyl groups, ethyl groups, n-sawn groups, isopropyl groups, methylcarbamyl groups, ethylcarbodiimide groups, n-propylboronic groups, methylsulfonyl groups, ethylsulfonyl groups, n-propylsulfonyl groups, isopropylacetanilide groups, methylaminomethyl groups, acylaminoalkyl groups, n-propylaminosulfonyl groups, isopropylaminocarbonyl groups, methylaminomethyl groups, acylaminoalkyl groups, n-propylaminoethyl groups, isopropylaminocarbonyl groups, C-propylaminosulfonyl groups and n-butylaminoethyl groups (methyl group, ethyl group, n-sawn group, isopropyl group, methylcarbazole group, ethylcarbodiimide group, n-propelleronline group, methylsulfonyl group, ethylsulfonyl group, n-propylsulfonyl group, isopropylacetanilide group, methylaminomethyl group, ethylaminomethyl group, n-propylaminosulfonyl group, isopropylaminocarbonyl group, methylaminomethyl group, ethylaminomethyl group, n-propylaminosulfonyl group, isopropylaminocarbonyl group, t-p is openingceremony group and n-butylaminoethyl group may be substituted by one or more substituents, selected from the group consisting of phenyl groups, thienyl groups, peredelnyh groups and fueling groups)), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

35) the Compound according to item 24), 25) or 26), where L4represents NR22(where R22represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14ar is maxigrip (C 2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)) and R3represents ethyl group, n-sawn group, isopropyl group, n-boutelou group, sec-boutelou group, tert-boutelou group, t-through group, C-boutelou group, C-pentelow group, C-hexoloy group, etinilnoy group, 1-propenyloxy group, 2-propenyloxy group, 1-butenyloxy groups who, 2-butenyloxy group, 3-butenyloxy group, 1-pantanillo group, 2-pantanillo group, 4-pantanillo group, 1-methyl-2-butenyloxy group, 1-methyl-3-butenyloxy group, 2-methyl-3-butenyloxy group, 3-methyl-1-butenyloxy group or any of the following heterocyclic groups:

(ethyl group, n-sawn group, isopropyl group, n-bucilina group, sec-bucilina group, tert-bucilina group, t-through group, C-bucilina group, C-pencilina group, C-exilda group, etinilnoy group, 1-proponila group, 2-proponila group, 1-Butyrina group, 2-Butyrina group, 3-Butyrina group, 1-penicilina group, 2-penicilina group, 4-penicilina group, 1-methyl-2-Butyrina group 1-methyl-3-Butyrina group, 2-methyl-3-Butyrina group, 3-methyl-1-Butyrina group and the above-mentioned heterocyclic group optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2 H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, C1-10alkoxycarbonyl groups, C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups and C1-10alkylcarboxylic (C1-10alkyl group, a C2-10alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl group, C1-10acylcarnitine group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, carboxyl groups, carbamoyl groups, groups, sulfonic acids and sulfamoyl groups):

aryl group: phenyl group, thienyl groups (a 2-thienyl group and 3-thienyl group), fueling groups (2-furilla group and 3-furilla group), pyridazinyl groups (3-pyridazinyl group is 4-pyridazinyl group), peredelnyh groups (2-Peregrina group, 3-Peregrina group and 4-Peregrina group), finalising groups (2-kinolinna group, 3-kinolinna group, 4-kinolinna group, 5-kinolinna group, 6-kinolinna group, 7-kinolinna group and 8-kinolinna group) and sochinyennykh groups (1-izochinolina group, 3-izochinolina group, 4-izochinolina group, 5-izochinolina group, 6-izochinolina group, 7-izochinolina group and 8-izochinolina group);

heterocyclic groups: group 1,3,4-oxadiazole, group, 1,3,4-thiadiazole, group, 1,2,4-oxadiazole, group, 1,2,4-thiadiazole, group, 1,2,5-oxadiazole, group, 1,2,5-thiadiazole, group, 1,2-oxazole and the group of 1,2-thiazole), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

36) the Compound according to item 24), 25) or 26), where L4represents NR22(where R22represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10Ala is xixabangma group and C 1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxy monilinia groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)) and R3represents a methyl group, ethyl group, n-sawn group, isopropyl group, n-boutelou group, sec-boutelou group, tert-boutelou group, t-through group, C-boutelou group, C-pentelow group, C-hexoloy group, etinilnoy group, 1-propenyloxy group, 2-propenyloxy group, 1-butenyloxy group, 2-butenyloxy group, 3-butenyloxy group, 1-pantanillo group, 2-pantanillo group, 4-pantanillo group, 1-methyl-2-butenyloxy group, 1-methyl-3-butenyloxy group, 2-methyl-3-butenyloxy group, 3-methyl-1-butenyloxy group or any of the following heterocyclic groups:

(methyl group, ethyl group, n-sawn group, isopropyl group, n-bucilina group, sec-bucilina group, tert-bucilina group, t-through group, C-bucilina group, C-pencilina group, C-exilda group, etinilnoy group, 1-proponila group, 2-proponila group, 1-Butyrina group, 2-Butyrina group, 3-Butyrina group, 1-penicilina group, 2-penicilina group, 4-penicilina group, 1-methyl-2-Butyrina group, 1-methyl-3-butenyl the Naya group, 2-methyl-3-Butyrina group, 3-methyl-1-Butyrina group and the above-mentioned heterocyclic group optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, C1-10alkoxycarbonyl groups, C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups and C1-10alkylcarboxylic (C1-10alkyl group, a C2-10alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl group, C1-10acylcarnitine group, mono - or di-C1-10alkylamino the dust, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, carboxyl groups, carbamoyl groups, groups, sulfonic acids and sulfamoyl groups)), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

37) Connection point 24), 25) or 26), where L4represents NR22(where R22represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic the groups, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)) and R3represents a methyl group, ethyl group, n-sawn groups who, ISO-propyl group, n-boutelou group, t-through group, C-hexoloy group, etinilnoy group, 1-propenyloxy group, 2-propenyloxy group or 1-butenyloxy group (methyl group, ethyl group, n-sawn group, isopropyl group, n-bucilina group, t-through group, C-exilda group, etinilnoy group, 1-proponila group, 2-proponila group and 1-Butyrina group optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, C1-10alkoxycarbonyl groups, C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C 1-10alkylcarboxylic (C1-10alkyl group, a C2-10alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl group, C1-10acylcarnitine group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, carboxyl groups, carbamoyl groups, groups, sulfonic acids and sulfamoyl groups)), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

38) the Compound according to item 24), 25) or 26), where L4represents NR22(where R22represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C 1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxy monilinia groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)) and R3represents a methyl group, ethyl group, n-sawn group, isopropyl group, n-boutelou group, t-through group, C-hexoloy group, etinilnoy group, 1-propenyloxy group, 2-propenyloxy group or 1-butenyloxy group (methyl group, ethyl group, n-sawn group, isopropyl group, n-bucilina group, t-through group, C-exilda group, etinilnoy group, 1-proponila group, 2-proponila group and 1-Butyrina group optionally can be substituted one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH and C1-10alkoxycarbonyl groups), tautomers, prodrugs or supplied with the ski acceptable salts of the compounds or their solvate.

39) the Compound according to item 24), 25) or 26), where L4represents NR22(where R22represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or n is the number of halogen atoms) or one or more halogen atoms)) or C 2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)) and R3is any of the following heterocyclic groups:

(the above heterocyclic group optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2/sub> CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, C1-10alkoxycarbonyl groups, C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups and C1-10alkylcarboxylic (C1-10alkyl group, a C2-10alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl group, C1-10acylcarnitine group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, carboxyl groups, carbamoyl groups, groups, sulfonic acids and sulfamoyl groups)), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

40) of the Connection point 24), 25) or 26), where L4represents NR22(where R22not only is em a hydrogen atom, hydroxyl group, a formyl group, a C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl gr is the PAP optionally may be substituted by one or more substituents, selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)) and R3is any of the following heterocyclic groups:

(the above heterocyclic group optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, C1-10 alkoxycarbonyl groups), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

41) the Compound according to item 24), 25) or 26), where L4represents NR22(where R22represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be C medeni one or more C 1-6alkyl groups (C1-6alkyl groups can be substituted by one or more halogen atoms) or one or more halogen atoms)) or C2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)) and R3is any of the following heterocyclic groups:

(the above heterocyclic group optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycut mobilnyh groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, C1-10alkoxycarbonyl groups, C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups and C1-10alkylcarboxylic (C1-10alkyl group, a C2-10alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl group, C1-10acylcarnitine group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, carboxyl groups, carbamoyl groups, groups, sulfonic acids and sulfamoyl groups)), tautomers, prodrugs or pharmaceutical is Eski acceptable salts of the compounds or their solvate.

42) of the Connection point 24), 25) or 26), where L4represents NR22(where R22represents a hydrogen atom, hydroxyl group, formyl group, C1-10alkyl group, a C2-6alkenylphenol group, C2-6alkylamino group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic group (C1-10alkyl group, a C2-6Alchemilla group, C2-6Alchemilla group, C1-10alkoxygroup, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10acylcarnitine group optionally can be substituted by one or more substituents selected from the group consisting of carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy (C2-14aryl group, and C2-14alloctype can be substituted by one or more C1-6alkyl groups (C1-6alkyl groups can be substituted by one or n is the number of halogen atoms) or one or more halogen atoms)) or C 2-14aryl group (C2-14aryl group optionally may be substituted by one or more substituents selected from the group consisting of C1-10alkyl groups (C1-10alkyl groups can be substituted by one or more halogen atoms), C2-6alkenyl groups, C2-6etkinlik groups, carboxyl groups, nitro groups, cyano groups, halogen atoms, C1-10alkoxygroup, C1-10alkylcarboxylic groups, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic, amino groups, mono - or di-C1-10alkylamino, hydroxyl groups, protected hydroxyl groups, C2-14aryl groups, and C2-14aryloxy)) and R3is any of the following heterocyclic groups:

(the above heterocyclic group optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2/sub> CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, C1-10alkoxycarbonyl groups), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

43) the Compound according to item 24), 25) or 26), where L4represents NH and R3represents ethyl group, n-sawn group, isopropyl group, n-boutelou group, sec-boutelou group, tert-boutelou group, t-through group, C-boutelou group, C-pentelow group, C-hexoloy group, etinilnoy group, 1-propenyloxy group, 2-propenyloxy group, 1-butenyloxy group, 2-butenyloxy group, 3-butenyloxy group, 1-pantanillo group, 2-pantanillo group, 4-pantanillo group, 1-methyl-2-butenyloxy group, 1-methyl-3-butenyloxy group, 2-methyl-3-butenyloxy group, 3-methyl-1-butenyloxy group or any of the following heterocyclic groups:

(ethyl group, n-sawn group, isopropyl group, n-bucilina group, sec-bucilina group, tert-bucilina group, t-through group, C-bucilina group, C-pencilina group, C-exilda group, etinilnoy group, 1-proponila group, 2-proponila group, 1-Butyrina group, 2-Butyrina group, 3-Butyrina group, 1-penicilina group, 2-PE is Tinella group, 4-penicilina group, 1-methyl-2-Butyrina group, 1-methyl-3-Butyrina group, 2-methyl-3-Butyrina group, 3-methyl-1-Butyrina group and the above-mentioned heterocyclic group optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, C1-10alkoxycarbonyl groups, C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic and the following aryl and heterocyclic groups, (C1-10alkyl group, a C2-10alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-0 alkoxygroup, C1-10thioalkyl group, C1-10acylcarnitine group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic and these aryl groups and geterotsiklicheskikh group optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, carboxyl groups, carbamoyl groups, groups, sulfonic acids and sulfamoyl groups):

aryl group: phenyl group, thienyl group (2-thienyl group and 3-thienyl group), foreline group (2-furilla group and 3-furilla group), pyridazinyl group (3-pyridazinyl group and 4-pyridazinyl group), peredelnye group (2-Peregrina group, 3-Peregrina group and 4-Peregrina group), chinoline group (2-kinolinna group, 3-kinolinna group, 4-kinolinna group, 5-kinolinna group, 6-kinolinna group, 7-kinolinna group and 8-kinolinna group) and ethanolamine group (1-izochinolina group, 3-izochinolina group, 4-izochinolina group, 5-izochinolina group, 6-izochinolina group, 7-izochinolina group and 8-izochinolina group);

heterocyclic groups: group 1,3,4-oxadiazole, group, 1,3,4-thiadiazole, group, 1,2,4-oxadiazole, gr is the PAP 1,2,4-thiadiazole, group 1,2,5-oxadiazole, group, 1,2,5-thiadiazole, group, 1,2-oxazole and the group of 1,2-thiazole),

the tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

44) Connection point 24), 25) or 26), where L4represents NH and R3represents a methyl group, ethyl group, n-sawn group, isopropyl group, n-boutelou group, sec-boutelou group, tert-boutelou group, t-through group, C-boutelou group, C-pentelow group, C-hexoloy group, etinilnoy group, 1-propenyloxy group, 2-propenyloxy group, 1-butenyloxy group, 2-butenyloxy group, 3-butenyloxy group, 1-pantanillo group, 2-pantanillo group, 4-pantanillo group, 1-methyl-2-butenyloxy group, 1-methyl-3-butenyloxy group, 2-methyl-3-butenyloxy group, 3-methyl-1-butenyloxy group or any of the following heterocyclic groups:

(methyl group, ethyl group, n-sawn group, isopropyl group, n-bucilina group, sec-bucilina group, tert-bucilina group, t-through group, C-bucilina group, C-pencilina group, C-exilda group, etinilnoy group, 1-proponila group, 2-proponila group, 1-Butyrina group, 2-Butyrina group, 3-Butyrina group, 1-penicilina group, 2-penicilina group, 4-pentenyl the th group, 1-methyl-2-Butyrina group, 1-methyl-3-Butyrina group, 2-methyl-3-Butyrina group, 3-methyl-1-Butyrina group and the above-mentioned heterocyclic group optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, C1-10alkoxycarbonyl groups, C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups and C1-10alkylcarboxylic (C1-10alkyl group, a C2-10alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl group, C1-10alkyls monilinia group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, carboxyl groups, carbamoyl groups, groups, sulfonic acids and sulfamoyl groups)), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

45) Connection point 24), 25) or 26), where L4represents NH and R3represents a methyl group, ethyl group, n-sawn group, isopropyl group, n-boutelou group, t-through group, C-hexoloy group, etinilnoy group, 1-propenyloxy group, 2-propenyloxy group or 1-butenyloxy group (methyl group, ethyl group, n-sawn group, isopropyl group, n-bucilina group, t-through group, C-exilda group, etinilnoy group, 1-proponila group, 2-proponila group and 1-Butyrina group optionally can be substituted one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, sianok remailing groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, C1-10alkoxycarbonyl groups, C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups and C1-10alkylcarboxylic (C1-10alkyl group, a C2-10alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl group, C1-10acylcarnitine group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, carboxyl groups, carbamoyl groups, groups, sulfonic acids and sulfamoyl groups)), tautomers, prodrugs or pharmaceutically acceptable salts connect the changes or their solvate.

46) Connection point 24), 25) or 26), where L4represents NH and R3represents a methyl group, ethyl group, n-sawn group, isopropyl group, n-boutelou group, t-through group, C-hexoloy group, etinilnoy group, 1-propenyloxy group, 2-propenyloxy group or 1-butenyloxy group (methyl group, ethyl group, n-sawn group, isopropyl group, n-bucilina group, t-through group, C-exilda group, etinilnoy group, 1-proponila group, 2-proponila group and 1-Butyrina group optionally can be substituted one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH and C1-10alkoxycarbonyl groups), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

47) Connection point 24), 25) or 26), where L4represents NH and R 3is any of the following heterocyclic groups:

(the above heterocyclic group optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, C1-10alkoxycarbonyl groups, C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups and C1-10alkylcarboxylic (C1-10alkyl group, a C2-10alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl group, C1-10alkylsulphonyl the groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, carboxyl groups, carbamoyl groups, groups, sulfonic acids and sulfamoyl groups)), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

48) Connection point 24), 25) or 26), where L4represents NH and R3is any of the following heterocyclic groups:

(the above heterocyclic group optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH and C1-10alkoxycarbonyl groups), tautomers, prodrugs is whether the pharmaceutically acceptable salts of the compounds or their solvate.

49) the Compound according to item 24), 25) or 26), where L4represents NH and R3is any of the following heterocyclic groups:

(the above heterocyclic group optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, C1-10alkoxycarbonyl groups, C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups and C1-10alkylcarboxylic (C1-10alkyl group, a C2-10alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-0 alkoxygroup, C1-10thioalkyl group, C1-10acylcarnitine group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, carboxyl groups, carbamoyl groups, groups, sulfonic acids and sulfamoyl groups)), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

50) Connection point 24), 25) or 26), where L4represents NH and R3is any of the following heterocyclic groups:

(the above heterocyclic group optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -H 2CH2OH and C1-10alkoxycarbonyl groups), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

51) Connection point 24), 25) or 26), where L4represents an oxygen atom or a sulfur atom, and R3represents ethyl group, n-sawn group, isopropyl group, n-boutelou group, sec-boutelou group, tert-boutelou group, t-through group, C-boutelou group, C-pentelow group, C-hexoloy group, etinilnoy group, 1-propenyloxy group, 2-propenyloxy group, 1-butenyloxy group, 2-butenyloxy group, 3-butenyloxy group, 1-pantanillo group, 2-pantanillo group, 4-pantanillo group, 1-methyl-2-butenyloxy group, 1-methyl-3-butenyloxy group, 2-methyl-3-butenyloxy group, 3-methyl-1-butenyloxy group or any of the following heterocyclic groups:

(ethyl group, n-sawn group, isopropyl group, n-bucilina group, sec-bucilina group, tert-bucilina group, t-through group, C-bucilina group, C-pencilina group, C-exilda group, etinilnoy group, 1-proponila group, 2-proponila group, 1-Butyrina group, 2-Butyrina group, 3-Butyrina group, 1-penicilina group, 2-penicilina group, 4-penicilina group, 1-methyl-2-Butyrina group 1-m is Tyl-3-Butyrina group, 2-methyl-3-Butyrina group, 3-methyl-1-Butyrina group and the above-mentioned heterocyclic group optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, C1-10alkoxycarbonyl groups, C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups, C1-10alkylcarboxylic and the following aryl and heterocyclic groups, (C1-10alkyl group, a C2-10alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl group, C1-10alkylcarboxylic the e group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group, C1-10alkylcarboxylic and these aryl groups and heterocyclic groups optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, carboxyl groups, carbamoyl groups, groups, sulfonic acids and sulfamoyl groups):

aryl group: phenyl group, thienyl group (2-thienyl group and 3-thienyl group), foreline group (2-furilla group and 3-furilla group), pyridazinyl group (3-pyridazinyl group and 4-pyridazinyl group), peredelnye group (2-Peregrina group, 3-Peregrina group and 4-Peregrina group), chinoline group (2-kinolinna group, 3-kinolinna group, 4-kinolinna group, 5-kinolinna group, 6-kinolinna group, 7-kinolinna group and 8-kinolinna group) and ethanolamine group (1-izochinolina group, 3-izochinolina group, 4-izochinolina group, 5-izochinolina group, 6-izochinolina group, 7-izochinolina group and 8-izochinolina group);

heterocyclic groups: group 1,3,4-oxadiazole, group, 1,3,4-thiadiazole, group, 1,2,4-oxadiazole, group, 1,2,4-thiadiazole, group, 1,2,5-oxadiazole, group, 1,2,5-thiadiazole, group, 1,2-oxazol the group 1,2-thiazole), the tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

52) Connection point 24), 25) or 26), where L4represents an oxygen atom or a sulfur atom, and R3represents a methyl group, ethyl group, n-sawn group, isopropyl group, n-boutelou group, sec-boutelou group, tert-boutelou group, t-through group, C-boutelou group, C-pentelow group, C-hexoloy group, etinilnoy group, 1-propenyloxy group, 2-propenyloxy group, 1-butenyloxy group, 2-butenyloxy group, 3-butenyloxy group, 1-pantanillo group, 2-pantanillo group, 4-pantanillo group, 1-methyl-2-butenyloxy group, 1-methyl-3-butenyloxy group, 2-methyl-3-butenyloxy group, 3-methyl-1-butenyloxy group or any of the following heterocyclic groups:

(methyl group, ethyl group, n-sawn group, isopropyl group, n-bucilina group, sec-bucilina group, tert-bucilina group, t-through group, C-bucilina group, C-pencilina group, C-exilda group, etinilnoy group, 1-proponila group, 2-proponila group, 1-Butyrina group, 2-Butyrina group, 3-Butyrina group, 1-penicilina group, 2-penicilina group, 4-penicilina group, 1-methyl-2-Butyrina group, 1-methyl-3-Butyrina g is the SCP, 2-methyl-3-Butyrina group, 3-methyl-1-Butyrina group and the above-mentioned heterocyclic group optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, C1-10alkoxycarbonyl groups, C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups and C1-10alkylcarboxylic (C1-10alkyl group, a C2-10alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl group, C1-10acylcarnitine group, mono - or di-C1-10alkylamino the dust, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, carboxyl groups, carbamoyl groups, groups, sulfonic acids and sulfamoyl groups)), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

53) Connection point 24), 25) or 26), where L4represents an oxygen atom or a sulfur atom, and R3represents a methyl group, ethyl group, n-sawn group, isopropyl group, n-boutelou group, t-through group, C-hexoloy group, etinilnoy group, 1-propenyloxy group, 2-propenyloxy group or 1-butenyloxy group (methyl group, ethyl group, n-sawn group, isopropyl group, n-bucilina group, t-through group, C-exilda group, etinilnoy group, 1-proponila group, 2-proponila group and 1-Butyrina group optionally can be substituted one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine the Rupp, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, C1-10alkoxycarbonyl groups, C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups and C1-10alkylcarboxylic (C1-10alkyl group, a C2-10alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl group, C1-10acylcarnitine group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, carboxyl groups, carbamoyl groups, groups, sulfonic acids and sulfamoyl groups)), tautomers, prodrugs or pharmaceutically acceptable salts connect the changes or their solvate.

54) Connection point 24), 25) or 26), where L4represents an oxygen atom or a sulfur atom, and R3represents a methyl group, ethyl group, n-sawn group, isopropyl group, n-boutelou group, t-through group, C-hexoloy group, etinilnoy group, 1-propenyloxy group, 2-propenyloxy group or 1-butenyloxy group (methyl group, ethyl group, n-sawn group, isopropyl group, n-bucilina group, t-through group, C-exilda group, etinilnoy group, 1-proponila group, 2-proponila group and 1-Butyrina group optionally can be substituted one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH and C1-10alkoxycarbonyl groups), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

55) Connection point 24), 25) or 26), where L4 represents an oxygen atom or a sulfur atom, and R3is any of the following heterocyclic groups:

(the above heterocyclic group optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, C1-10alkoxycarbonyl groups, C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl groups and C1-10alkylcarboxylic (C1-10alkyl group, a C2-10alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-10alkoxygroup, C 1-10thioalkyl group, C1-10acylcarnitine group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, carboxyl groups, carbamoyl groups, groups, sulfonic acids and sulfamoyl groups)), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

56) Connection point 24), 25) or 26), where L4represents an oxygen atom or a sulfur atom, and R3is any of the following heterocyclic groups:

(the above heterocyclic group optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2 OH, -CH2CH2OH and C1-10alkoxycarbonyl groups), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

57) the Compound according to item 24), 25) or 26), where L4represents an oxygen atom or a sulfur atom, and R3is any of the following heterocyclic groups:

(the above heterocyclic group optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydroxycarbamoyl groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH, C1-10alkoxycarbonyl groups, C1-10alkyl groups, C2-10alkenyl groups, C2-10etkinlik groups, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl groups, C1-10alkylcarboxylic groups, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl is lnyh groups and C 1-10alkylcarboxylic (C1-10alkyl group, a C2-10alkeneamine group, C2-10alkyline group, C2-9heterocyclic group, a C1-10alkoxygroup, C1-10thioalkyl group, C1-10acylcarnitine group, mono - or di-C1-10alkylamino, C1-10alkylcarboxylic, C1-10alkoxycarbonyl group and C1-10alkylcarboxylic optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, carboxyl groups, carbamoyl groups, groups, sulfonic acids and sulfamoyl groups)), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

58) Connection point 24), 25) or 26), where L4represents an oxygen atom or a sulfur atom, and R3is any of the following heterocyclic groups:

(the above heterocyclic group optionally can be substituted by one or more substituents selected from the group consisting of hydroxyl groups, amino groups, tylnej groups, carboxyl groups, groups, phosphonic acid groups, sulfonic acid, carbamoyl groups, hydroxycarbamoyl groups, cyanocobalamine groups, sulfamoyl groups, hydro is selfamily groups, cyanomethylene groups, groups tetrazole, -CH2CO2H, -OCH2CO2H, -NHCH2CO2H, -CH2CH2CO2H, -CH2OH, -OCH2OH, -NHCH2OH, -CH2CH2OH and C1-10alkoxycarbonyl groups), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

59) Compounds, where A, B, R1L1, R2L2L3, Y, L4, R3and X are any of the following combinations shown in table 1, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate. The symbols in table 1 mean the following placeholders.

60) Connection, where A, B, R1L1, R2L2L3, Y, L4, R3and X are any of the following combinations shown in table 2, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate. The symbols in table 2 indicate the following placeholders.

61) Connection, where A, B, R1L1, R2L2L3, Y, L4, R3and X are any of the following combinations in table 2, the tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate (provided that in the case of 61) Q1a, Q1b, Q1c, Q1i, Q1j, T3a, T3b, T3c, T3d, T3e, Q3e, T3f, T3g T3h, T3i and T3j in table 2 indicate the following placeholders).

62) Compounds, where A, B, R1L1, R2L2L3, Y, L4, R3and X are any of the following combinations shown in table 3, the tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate. The symbols in table 3 indicate the following placeholders.

63) Connection, where A, B, R1L1, R2L2L3, Y, L4, R3and X are any of the following combinations in table 3, the tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate (provided that in the case of 63) Q1a, Q1b and Q3a in table 3 indicate the following placeholders).

64) Connection, where A, B, R1L1, R2L2L3, Y, L4, R3and X are any of the following combinations in table 2, the tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate (provided that in the case of 64) Q1a, Q1b, Q1c, Q1i, Q1j, T3a, T3b, T3c, T3d, T3e, Q3e, T3f, T3g, T3h, T3i and T3j in table 2 indicate the following placeholders).

65) Compounds, where A, B, R1L1, R2L2L3, Y, L4, R3and X represent any of clubusacasino in table 1, the tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate (provided that in the case of 65) Q1a, Q1b, Q1c, Q1d, Q1e, Q1f, Q1g, Q1h, Q1i, Q1j, Q1k, Q1l, Q1m, Q1n, Q1k', Q1l', Q1m', Q1n', Q3a, Q3b, Q3c, Q3d, Q3e, Q3f, Q3g and Q3h in table 1 mean the following placeholders).

66) Connection, where A, B, R1L1, R2L2L3, Y, L4, R3and X are any of the following combinations in table 1, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate (provided that in the case of 66) Q1a, Q1b, Q1c, Q1d, Q1e, Q1f, Q1g, Q1h, Q1i, Q1j, Q1k, Q1l, Q1m, Q1n, Q1k', Q1l', Q1m', Q1n', Q3a, Q3b, Q3c, Q3d, Q3e, Q3f, Q3g and Q3h in table 1 mean the following placeholders).

67) Connection, where A, B, R1L1, R2L2L3, Y, L4, R3and X are any of the following combinations in table 1, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate (provided that in the case of 67) Q1a, Q1b, Q1c, Q1d, Q1e, Q1f, Q1g, Q1h, Q1i, Q1j, Q1k, Q1l, Q1m, Q1n, Q1k', Q1l', Q1m', Q1n', Q3a, Q3b, Q3c, Q3d, Q3e, Q3f, Q3g and Q3h in table 1 mean the following placeholders).

68) Connection, where A, B, R1L1, R2L2L3, Y, L4, R3and X are any of the following combinations in table 1, tautomers, prodrugs or in pharmaceutical preparations is automatic acceptable salts of the compounds or their solvate (provided in the case 68) Q1a, Q1b, Q1c, Q1d, Q1e, Q1f, Q1g, Q1h, Q1i, Q1j, Q1k, Q1l, Q1m, Q1n, Q1k', Q1l', Q1m', Q1n', Q3a, Q3b, Q3c, Q3d, Q3e, Q3f, Q3g and Q3h in table 1 mean the following placeholders).

69) Connection, where A, B, R1L1, R2L2L3, Y, L4, R3and X are any of the following combinations in table 1, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate (provided that in the case of 69) Q1a, Q1b, Q1c, Q1d, Q1e, Q1f, Q1g, Q1h, Q1i, Q1j, Q1k, Q1l, Q1m, Q1n, Q1k', Q1l', Q1m', Q1n', Q3a, Q3b, Q3c, Q3d, Q3e, Q3f, Q3g and Q3h in table 1 mean the following placeholders).

70) Connection, where A, B, R1L1, R2L2L3, Y, L4, R3and X are any of the following combinations in table 1, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate (provided that in the case of 70) Q1a, Q1b, Q1c, Q1d, Q1e, Q1f, Q1g, Q1h, Q1i, Q1j, Q1k, Q1l, Q1m, Q1n, Q1k', Q1l', Q1m', Q1n', Q3a, Q3b, Q3c, Q3d, Q3e, Q3f, Q3g and Q3h in table 1 mean the following placeholders).

71) Connection, where A, B, R1L1, R2L2L3, Y, L4, R3and X are any of the following combinations in table 1, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate (provided that in the case of 71) Q1a, Q1b, Q1c, Q1d, Q1e, Q1f, Q1g, Q1h, Q1, Q1j, Q1k, Q1l, Q1m, Q1n, Q1k', Q1l', Q1m', Q1n', Q3a, Q3b, Q3c, Q3d, Q3e, Q3f, Q3g and Q3h in table 1 mean the following placeholders).

72) Connection, where A, B, R1L1, R2L2L3, Y, L4, R3and X are any of the following combinations in table 1, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate (provided that in the case of 72) Q1a, Q1b, Q1c, Q1d, Q1e, Q1f, Q1g, Q1h, Q1i, Q1j, Q1k, Q1l, Q1m, Q1n, Q1k', Q1l', Q1m', Q1n', Q3a, Q3b, Q3c, Q3d, Q3e, Q3f, Q3g and Q3h in table 1 mean the following placeholders).

73) Connection, where A, B, R1L1, R2L2L3, Y, L4, R3and X are any of the following combinations in table 1, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate (provided that in the case of 73) Q1a, Q1b, Q1c, Q1d, Q1e, Q1f, Q1g, Q1h, Q1i, Q1j, Q1k, Q1l, Q1m, Q1n, Q1k', Q1l', Q1m', Q1n', Q3a, Q3b, Q3c, Q3d, Q3e, Q3f, Q3g and Q3h in table 1 mean the following placeholders).

74) Connection, where A, B, R1L1, R2L2L3, Y, L4, R3and X are any of the following combinations in table 1, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate (provided that in the case of 74) Q1a, Q1b, Q1c, Q1d, Q1e, Q1f, Q1g, Q1h, Q1i, Q1j, Q1k, Q1l, Q1m, Q1n, Q1k', Q1l', Q1m', Q1n', Q3a, Q3b, Q3c, Q3d, 3e, Q3f, Q3g and Q3h in table 1 mean the following placeholders).

75) Compounds, where A, B, R1L1, R2L2L3, Y, L4, R3and X are any of the following combinations in table 1, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate (provided that in the case of 75) Q1a, Q1b, Q1c, Q1d, Q1e, Q1f, Q1g, Q1h, Q1i, Q1j, Q1k, Q1l, Q1m, Q1n, Q1k', Q1l', Q1m', Q1n', Q3a, Q3b, Q3c, Q3d, Q3e, Q3f, Q3g and Q3h in table 1 mean the following placeholders).

76) Connection, where A, B, R1L1, R2L2L3, Y, L4, R3and X are any of the following combinations in table 1, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate (provided that in the case of 76) Q1a, Q1b, Q1c, Q1d, Q1e, Q1f, Q1g, Q1h, Q1i, Q1j, Q1k, Q1l, Q1m, Q1n, Q1k', Q1l', Q1m', Q1n', Q3a, Q3b, Q3c, Q3d, Q3e, Q3f, Q3g and Q3h in table 1 mean the following placeholders).

77) Connection, where A, B, R1L1, R2L2L3, Y, L4, R3and X are any of the following combinations in table 1, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate (provided that in the case of 77) Q1a, Q1b, Q1c, Q1d, Q1e, Q1f, Q1g, Q1h, Q1i, Q1j, Q1k, Q1l, Q1m, Q1n, Q1k', Q1l', Q1m', Q1n', Q3a, Q3b, Q3c, Q3d, Q3e, Q3f, Q3g and Q3h in table 1 mean the following is Deputy).

78) Connection, where A, B, R1L1, R2L2L3, Y, L4, R3and X are any of the following combinations in table 1, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate (provided that in the case of 78) Q1a, Q1b, Q1c, Q1d, Q1e, Q1f, Q1g, Q1h, Q1i, Q1j, Q1k, Q1l, Q1m, Q1n, Q1k', Q1l', Q1m', Q1n', Q3a, Q3b, Q3c, Q3d, Q3e, Q3f, Q3g and Q3h in table 1 mean the following placeholders).

79) Connection, where A, B, R1L1, R2L2L3, Y, L4, R3and X are any of the following combinations in table 1, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate (provided that in the case of 79) Q1a, Q1b, Q1c, Q1d, Q1e, Q1f, Q1g, Q1h, Q1i, Q1j, Q1k, Q1l, Q1m, Q1n, Q1k', Q1l', Q1m', Q1n', Q3a, Q3b, Q3c, Q3d, Q3e, Q3f, Q3g and Q3h in table 1 mean the following placeholders).

80) Connections, where A, B, R1L1, R2L2L3, Y, L4, R3and X are any of the following combinations in table 1, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate (provided that in the case of 80) Q1a, Q1b, Q1c, Q1d, Q1e, Q1f, Q1g, Q1h, Q1i, Q1j, Q1k, Q1l, Q1m, Q1n, Q1k', Q1l', Q1m', Q1n', Q3a, Q3b, Q3c, Q3d, Q3e, Q3f, Q3g and Q3h in table 1 mean the following placeholders).

81)Connection, where A, B, R1L1, R2L2L3, Y, L4, R3and X are any of the following combinations in table 1, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate (provided that in the case of 81) Q1a, Q1b, Q1c, Q1d, Q1e, Q1f, Q1g, Q1h, Q1i, Q1j, Q1k, Q1l, Q1m, Q1n, Q1k', Q1l', Q1m', Q1n', Q3a, Q3b, Q3c, Q3d, Q3e, Q3f, Q3g and Q3h in table 1 mean the following placeholders).

82) Compounds represented by any one of paragraphs 59)-81), where X is transformed into SH, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

83) Compounds represented by any one of paragraphs 59)-81), where X is transformed into NH2, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

84) the Compound represented by any one of paragraphs 59)-81), where X is transformed into OAc, tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate.

85) Activators of receptor thrombopoetin presented in any of paragraphs (1)-84).

86) Preventive, therapeutic and improving agents for diseases in which the effective activation of the receptor thrombopoetin that contain activators of receptor thrombopoetin provided in paragraph 85) or having the formula (1), tautomers, prodrugs or pharmaceutically acceptable the salt activators or their solvate as an active ingredient.

87) Agents that increase the number of platelets containing activators of receptor thrombopoetin provided in paragraph 85) or having the formula (1), tautomers, prodrugs or pharmaceutically acceptable salts, activators or their solvate as an active ingredient.

88) Medicines containing compounds presented in any of paragraphs (1)-84) or having the formula (1), tautomers, prodrugs or pharmaceutically acceptable salts of the compounds or their solvate as an active ingredient.

In the present invention the compounds of the present invention, represented by formula (1)may exist as tautomers or geometrical isomers, which are industriously or ekzoticheskoy isomerization, mixtures of the tautomers or geometrical isomers or their mixtures. When the compounds of the present invention have a center of asymmetry, arising or not arising from isomerization of the compounds of the present invention can be in the form of separated optical isomers or as mixtures containing them in certain proportions.

For example, the compounds of furan, thiophene compounds or compounds of the pyrrole according to the present invention can exist in the form of (4-hydroxy-2(5H)-furninova) analogues of tetronic acid, (4-hydroxy-2(5H)-thiophene analogs is iotechnology acid and (4-hydroxy-3-pyrrolin-2-novyh) analogues terminoloy acid, as shown below using the formulas (2), (3) and (4), mixtures thereof or mixtures of their isomers.

Compounds of the present invention, represented by formula (1)or their pharmaceutically acceptable salts can exist as free crystals or arbitrary hydrates depending on conditions obtain. The present invention covers these crystals, hydrates and mixtures. They can be in the form of a solvate with an organic solvent, such as acetone, ethanol, and tetrahydrofuran, and the present invention encompasses any of the form data.

Compounds of the present invention, represented by formula (1)can be converted into a pharmaceutically acceptable salt and can be released from the resulting salt if necessary. Pharmaceutically acceptable salts of the present invention may constitute, for example, alkali metal salts (such as lithium, sodium and potassium), alkaline earth metals (such as magnesium and calcium), ammonium, organic bases and amino acids. They may be a salt with inorganic acids (such as hydrochloric acid, bromatologia acid, phosphoric acid and sulfuric acid) and organic acids (such as acetic acid, citric acid, maleic acid, fumaric sour is a, benzolsulfonat acid and p-toluensulfonate acid).

Compounds that serve as prodrugs, are derivatives of the present invention, which has a chemically or metabolically degradable group, which lead to the pharmacologically active compounds of the present invention when the solvolysis or under physiological conditions in vivo. Methods for selecting or obtaining the appropriate prodrugs are described, for example, in Design of Prodrugs (Elsevier, Amsterdam 1985). In the present invention, when the compound contains a hydroxyl group as prodrugs, can be mentioned, for example, allocryptopine, produced by the interaction of the compounds with suitable acylhomoserine or suitable anhydrides of the acids. Alloctype especially suitable as prodrugs include-OCOC2H5, -OCO(tert-Bu), -OCOC15H31, -OCO(m-CO2Na-Ph), -OCOCH2CH2CO2Na, -OCOCH(NH2)CH3, -OCOCH2N(CH3)2and things like that. When the compound of the present invention has an amino group as prodrugs can be mentioned, for example, amide derivatives obtained by reacting compounds having the amino group, with suitable halides of acids or suitable mixed anhydrides of the acids. Amides, particularly preferred as prodrugs, including the ut-NHCO(CH 2)20OCH3, -NHCOCH(NH2)CH3and things like that. When the compound of the present invention contains a carboxyl group as prodrugs can be mentioned esters of carboxylic acids with aliphatic alcohols or esters of carboxylic acids, obtained by the interaction with the hydroxyl groups of the 1,2 - or 1,3-diglycerides, does not contain alcohol. Particularly preferred prodrugs are methyl esters and ethyl esters.

Preventive, therapeutic and improving agents for diseases in which the effective activation of the receptor thrombopoetin and increase the number of platelets agents that contain activators of receptor thrombopoetin of the present invention, the tautomers, prodrugs or pharmaceutically acceptable salts, activators or their solvate as an active ingredient, usually you can enter as oral medicines, such as tablets, capsules, powders, granules, pills and syrup, in the form of rectal medicines, transcutaneous medicines and injections. The agents according to the present invention can be entered as a single therapeutic agent or as mixtures with other therapeutic agents. Although you can enter them by themselves, they are usually administered in the form of drug the compositions. Such pharmaceutical preparations can be obtained in the usual way by adding pharmacologically and pharmaceutically acceptable auxiliary additives. That is, for oral medicines, you can use the usual excipients, lubricants, binders, dezintegriruetsja agents, humectants, plasticizers and agents to obtain membranes. Oral liquid preparations may be in the form of aqueous or oily suspensions, solutions, emulsions, syrups or elixirs, or may be supplied as dry syrups for mixing with water or other suitable solvents before use. Such liquid preparations may contain conventional adjuvants, such as suspendresume agents, fragrances, solvents and emulsifiers. In the case of rectal introduction you can enter them in the form of suppositories. As the basis for suppositories may use a suitable substance, such as cocoa butter, lauric tallow, macrogol, glycoregulation, Witepsol, sodium stearate, and mixtures thereof, and they may optionally contain an emulsifier, suspendisse agent, preservative and the like. For injection to obtain water dosage forms and dosage forms that require dilution prior to application, you can use such pharmaceutical ingredients, as dis is allrounda water for injection, saline, 5%glucose, propylene glycol or other solvents or solubilizing agents, pH regulator, an isotonic agent and stabilizer.

The dosage of the agents according to the present invention for administration to man is usually from about 0.1 to 1000 mg/person/day in the case of oral medicines, or with the introduction of rectal and from about 0.05 mg to 500 mg/person/day in the case of injection, although it depends on the age and condition of the patient. The above ranges are only examples, and the dose should be determined based on the patient's condition.

The present invention finds application when it is expected that the use of compounds which have affinity towards the receptor of thrombopoietin and act as agonists of the receptor thrombopoetin, improve pathological condition. For example, it can be noted hematologic disorders involving abnormal platelet count. Specifically, it is effective in the treatment and prevention of diseases of humans and mammals caused by an abnormal megakaryopoiesis, especially accompanied by thrombocytopenia. Examples of such diseases include thrombocytopenia following chemotherapy and radiation therapy in cancer, thrombocytopenia accompanying antiviral therapy of diseases, that is as hepatitis C, thrombocytopenia caused by bone marrow transplantation, surgery, and severe infections or gastrointestinal bleeding, but such diseases are not limited to these. Typical thrombocytopenia, such as aplastic anemia, idiopathic thrombocytopenic purpura, myelodysplastic syndrome, liver disease, HIV infection and the lack of thrombopoetin are also targets for the agents of the present invention. The present invention can be used as a mobilizing agent for peripheral stem cell inducer of differentiation megakaryoblastic or megakaryocytic leukemia cells and an agent that increases the number of platelets for platelet donors. In addition, potential applications include therapeutic angiogenesis, based on differentiation and proliferation of vascular endothelial cells and endothelial progenitor cells, prevention and therapy of arteriosclerosis, myocardial infarction, unstable angina, occlusal peripheral artery disease, but there are no restrictions.

Compounds represented by formula (1), obtained by the method presented is illustrated by the following formula (5)

The interaction of the compound (I) containing a-NH2the group link is m (II) in a solvent, optionally, in the presence of a catalyst, by heating and stirring leads to the target compound or its predecessor. Predecessor, if necessary, may be subjected to hydrolysis, removal of protective groups, recovery or oxidation with the formation of the target compounds. Compounds of the present invention can usually be cleaned by column chromatography, thin-layer chromatography, high performance liquid chromatography (HPLC) or by high performance liquid chromatography-mass spectrometry (LC/MS), and, if necessary, they can be obtained with a high degree of purity by recrystallization or washing with solvents.

For the synthesis of intermediate compounds can be referenced by the following synthesis of heterocyclic compounds.

1) Pyrazole (formula (6))

J. Chem. Soc. Perkin. Trans.1, p.81, (1985)

2) Isothiazol (formula (7))

Liebigs. Annalen. der. Chemie., 10, 1534-1546 (1979)

3) Isoxazol (formula (8))

Synthesis, 10, 664-665 (1975)

4) Thiophene (formula (9))

JP-A-48-026755

5) Furan (formula (10))

J. Org. Chem., 21, 1492-1509 (1956) and EP1253146

6) Pyrrole (formula (11))

J. Heterocyclic Chem., 30, 1253 (1993) and Tetrahedron, 50(26), 7849-56 (1994)

7) (4-hydroxy-2(5H)furanone), analogue of tetronic acid (formula (12))

Synthesis, 7, 564-566 (1988) and Yakugaku Zasshi, 96(4), 536-543 (1976)

8) (4-hydroxy-3-pyrrolin-2-one), similar terminoloy acid (formula (13))

p> Synthesis, 2, 190-192 (1987) and Agric. Biol. Chem., 43(8), 1641-1646 (1979)

For the synthesis containing the group-NH2compounds (II), for example, when L3= NH, you can refer to the following publications.

1) L4= bond, Y = O

Synthetic Commun., 28(7), 1223-1231 (1998), J. Chem. Soc., 1225 (1948) and J. Chem. Soc., 2831 (1952)

2) L4= NH, Y = O

J. Am. Chem. Soc., 46, 2813 (1924) and J. Chem. Soc., 2654 (1952)

3) L4= NH, Y = S

Can. J. Chem., 35, 834 (1957)

4) L4= NR22or N-(heterocyclic group formed by R22and R3)

J. Org. Chem., 53, 2263 (1988)

5) L4= CH2Y = O

J. Org. Chem., 30, 2487 (1965)

6) L4= O, Y = O

Bull. Soc. Chim. Belg., 68, 409, (1959)

7) L4= S, Y = S

J. Med. Chem., 22, 853 (1979)

Compounds represented by formula (1), where L3represents NR19L4represents NH and Y represents O or S, get the method presented is illustrated by the following formula (14)

Compounds represented by formula (1), where L3represents NR19L4is a bond and Y represents O or S, get the method presented is illustrated by the following formula (15)

The interaction of the compound (I) containing a group NH2compound (IV) in a solvent, if necessary in prisutstvie the catalyst, while heating and stirring leads to the compound (III) as the target product.

Compounds represented by formula (1), where L3represents NR19L4represents NR22or form a heterocyclic group together with R3get the method presented is illustrated by the following formula (16)

EXAMPLES

Hereinafter the present invention will be described in more detail with reference to the reference synthetic examples synthetic examples, examples of analysis and sample compositions. However, it should be understood that the present invention is in no way limited to these specific examples.

1H-NMR analysis was performed at 300 MHz, and LC/MS (mass spectra) were recorded under the following conditions.

LC/MS conditions 1

Column: Waters SunFire C18 (3.5 µm, a 4.6×30 mm)

Eluent: acetonitrile/0.1% aqueous formic acid (10/90 → 60/40)

LC/MS conditions 2

Column: Waters SunFire C18 (3.5 µm, a 4.6×30 mm)

Eluent: acetonitrile/0.1% aqueous formic acid (10/90 → 85/15)

LC/MS conditions 3

Column: Waters SunFire C18 (3.5 µm, a 4.6×30 mm)

Eluent: acetonitrile/0.1% aqueous formic acid (20/80 → 100/0)

LC/MS conditions 4

Column: Waters Xterra MSC18 (5 μm, a 4.6×50 mm)

Eluent: acetonitrile/0.1% aqueous formic acid (10/90 → 60/40)

Column: Waters Xterra MSC18 (3.5 µm and 2.1×20 mm)

Eluent: acetonitrile/0.2% aqueous formic acid (20/80 → 90/10)

REFERENCE SYNTHETIC EXAMPLE 1

Synthesis of 2-(3,4-dichlorophenyl)-4-(1-hidradenitis)thiophene-3-ol

To a suspension of 2-(3,4-dichlorophenyl)-3-hydroxy-4-methylcarbonate (300 mg, 1.05 mmol) (obtained by the method described in WO2004/108683) in isopropanol (20 ml) was added hydrazine monohydrate (61 μl, 1.25 mmol). The reaction mixture was heated at the boil under reflux for 1.5 hours, stirred at room temperature for 0.5 hour and at 0°C for 1 hour. Precipitated precipitated solid substance was collected by filtration and dried using a vacuum pump, obtaining the target product (yield 100%).

Morphology: pale yellow solid

1H-NMR (DMSO-d6) δ (ppm): 2,10 (s, 3H), 6,63 (users, 2H), 7,58 (s, 2H), to 7.61 (s, 1H), 7,98 (s, 1H), 12,88 (s, 1H).

LC/MS: condition 4, the retention time of 4.95 (min)

LC/MS (ESI+) m/z 301, 303 [M+1]+

LC/MS (ESI-) m/z 299, 301 [M-1]-

REFERENCE SYNTHETIC EXAMPLE 2

Synthesis of methyl-1-hydrazinecarbothioamide-4-carboxylate

To a solution of metaliconfactory (1.0 g, 7.0 mmol) in tetrahydrofuran was added thiocarbonyldiimidazole (1.24 g, 6,98 mmol) at room temperature and the reaction solution was stirred at room temperature techenie,5 hours, and then was stirred with hydrazine monohydrate (700 mg, 14.0 mmol) for 4 hours. After adding a saturated aqueous solution of sodium chloride, the reaction solution was extracted with ethyl acetate and chloroform, the extract was dried over anhydrous magnesium sulfate and concentrated, obtaining the target product (yield 114%).

Morphology: pale yellow solid

LC/MS: condition 5, the retention time of 0.52 (min)

LC/MS (ESI+) m/z 218, [M+1]+

REFERENCE SYNTHETIC EXAMPLE 3

Synthesis of ethyl-1-hydrazinecarbothioamide-3-carboxylate

The synthesis was performed in the same manner as described in reference synthetic example 2, using telnperature.

REFERENCE SYNTHETIC EXAMPLE 4

Synthesis of diethylamide 1-hydrazinecarbothioamide-4-carboxylic acid

The synthesis was performed in the same manner as described in reference synthetic example 2, using diethylamide isonipecotic acid.

REFERENCE SYNTHETIC EXAMPLE 5

Synthesis of 1-hydrazinecarbothioamide-4-ol

The solution methylhydrocinnamic (1.0 g, 8.2 mmol) and piperidine-4-ol (1.24 g, 12.3 mmol) in ethanol (7 ml) was heated at boiling under reflux at a temperature of 90ºC for 2 days. After adding ethyl acetate to the reaction solution was washed with saturated aqueous Rast is the PR of sodium chloride, was dried over anhydrous magnesium sulfate and concentrated, obtaining the crude target product. The crude product is directly used in the next reaction.

REFERENCE SYNTHETIC EXAMPLE 6

Synthesis of 1-hydrazinecarbothioamide-3-ol

The synthesis was performed in the same manner as described in reference synthetic example 5, using piperidine-3-ol.

REFERENCE SYNTHETIC EXAMPLE 7

Synthesis of 1-hydrazinecarbothioamide-4-methanol

The synthesis was performed in the same manner as described in reference synthetic example 5, using 4-piperidinemethanol.

REFERENCE SYNTHETIC EXAMPLE 8

Synthesis of methyl 2-[4-(tert-butoxycarbonyl)piperazine-1-yl]acetate

A solution of 1-(tert-butoxycarbonyl)piperazine (1,38 g, 7.41 mmol) in acetonitrile (10 ml) was stirred with triethylamine (2,07 ml of 14.8 mmol) and methyl-2-bromoacetate (of 1.02 ml, 11.1 mmol) at room temperature for 4 hours and then filtered. The filtrate was concentrated and, after addition of a saturated aqueous solution of ammonium chloride was extracted with ethyl acetate. The organic phase is washed with saturated aqueous ammonium chloride and saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated, obtaining the target product (yield 83%).

Morph is logy: pale yellow liquid

1H-NMR (CDCl3) δ: of 1.46 (s, 9H), of 2.53 (t, J=5.1 Hz, 4H), 3,24 (s, 2H), 3,49 (t, J=5.1 Hz, 4H), to 3.73 (s, 3H).

REFERENCE SYNTHETIC EXAMPLE 9

Synthesis of ethyl-3-[4-(tert-butoxycarbonyl)piperazine-1-yl]propionate

The synthesis was performed in the same manner as described in reference synthetic example 8 using ethyl-3-bromopropionate.

Morphology: colorless mixture of solid and liquid substances

1H-NMR (CDCl3) δ: 1.26 in (t, J=7.2 Hz, 3H), of 1.46 (s, 9H), is 2.41 (t, J=4.8 Hz, 4H), 2.50 each (t, J=7.2 Hz, 2H), 2,71 (t, J=7.2 Hz, 2H), 3,42 (t, J=4.8 Hz, 4H), 4,14 (sq, J=7.2 Hz, 2H).

REFERENCE SYNTHETIC EXAMPLE 10

Synthesis of methyl 2-[4-hydrazinecarbothioamide-1-yl]acetate

A solution of methyl 2-[4-(tert-butoxycarbonyl)piperazine-1-yl]acetate obtained in reference synthetic example 8, in dioxane (9 ml) was stirred with 4 N. a solution of hydrogen chloride in dioxane (3,91 ml, 15.7 mmol) at 80°C for 1.5 hours. The solution was left to cool and was filtered. To the precipitate on the filter was added tetrahydrofuran and triethylamine (from 0.88 ml, 6.3 mmol) and the resulting solution was treated in accordance with the method described in reference synthetic example 2. The crude product is directly used in the next reaction.

Morphology: pale yellow solid

REFERENCE SYNTHETIC EXAMPLE 11

Synthesis of ethyl-3-[4-hydrosilation Boniperti-1-yl]propionate

The synthesis was performed in the same manner as described in reference synthetic example 10, using ethyl-3-[4-(tert-butoxycarbonyl)piperazine-1-yl]propionate obtained in reference synthetic example 9.

Morphology: pale yellow solid

SYNTHETIC EXAMPLE 1

Synthesis of methyl-1-[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylate

To a solution in dimethylformamide (600 ml) of 2-(3,4-dichlorophenyl)-3-hydroxy-4-methylcarbonate (30 mg, 0.10 mmol) and methyl-1-hydrazinecarbothioamide-4-carboxylate (46 mg, 0.20 mmol)obtained in reference synthetic example 2 was added at room temperature, concentrated hydrochloric acid (9 μl, 0.1 mmol) and the resulting solution was stirred at room temperature for 8 hours, then mixed with water and was extracted with ethyl acetate. The extract was washed with 1 M hydrochloric acid and saturated aqueous sodium chloride, dried over anhydrous magnesium sulfate and concentrated. The obtained residue was purified column chromatography on silica gel (hexane/ethyl acetate = 1/1) and recrystallized from chloroform, obtaining the target product (yield 55%).

Morphology: white solid

1H-NMR (DMSO-d6) δ: 1,55-1,75 (m, 2H), 1.85 to 1,95 (m, 2H), of 2.38 (s, 3H), 2,7-2,8 (m, 1H, 3,15-3,30 (m, 2H), 3,48 (s, 3H), 4,58 (d, J=13.5 Hz, 2H), to 7.64 (d, J=8,4 Hz, 1H), 7,71 (d, J=8,4, and 2.1 Hz, 1H), 8,00 (s, 1H), 8,03 (d, J=2.1 Hz, 1H), and 12.4 (s, 1H).

LC/MS: conditions 5, retention time 5,19 (min)

LC/MS (ESI+) m/z 486, 488 [M+1]+

LC/MS (ESI-) m/z 484, 486 [M-l]-

SYNTHETIC EXAMPLE 2

Synthesis of 1-[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylic acid

To a suspension of methyl 1-[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)carbonyl}piperidine-4-carboxylate (10 mg, 0,021 mmol) in methanol (300 ml) was added at room temperature a 1 M aqueous sodium hydroxide solution (250 μl) and the suspension was stirred at room temperature for 7 hours. After the interaction was added 1 M hydrochloric acid solution (250 μl) and the resulting crystals were collected by filtration as a target product (yield 71%).

Morphology: gray solid

LC/MS: conditions 5, retention time 4,87 (min)

LC/MS (ESI+) m/z 472, 474 [M+1]+

LC/MS (ESI-) m/z 470, 472 [M-1]-

SYNTHETIC EXAMPLE 3

Synthesis of methyl 2-{[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)carbonothioyl]amino}acetate

A solution of 2-(3,4-dichlorophenyl)-4-(1-hidradenitis)thiophene-3-ol (30 mg, 0.10 mmol)obtained in reference synthetic example 1 and methyl-2-isothiocyanatobenzene (20 mg, 0.15 mmol)in dimethylformamide (300 μl) was stirred at room temperature 40°C and 50°C for 2 hours, respectively. After adding a mixture of methanol-water solution was stirred at room temperature for 0.5 hours and the resulting crystals were collected by filtration as a target product (yield 72%).

Morphology: white solid

LC/MS: condition 5, the retention time of 4.95 (min)

LC/MS (ESI+) m/z 432, 434 [M+1]+

LC/MS (ESI-) m/z 430, 432 [M-1]-

SYNTHETIC EXAMPLE 4

Synthesis of 2-{[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)carbonothioyl]amino}acetic acid

The synthesis was performed in the same manner as described in synthetic example 2, using methyl 2-{[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)carbonothioyl]amino}acetate obtained in synthetic example 3 (yield 39%).

Morphology: white solid

LC/MS: condition 5, the retention time of the 4.65 (min)

LC/MS (ESI+) m/z 418, 420 [M+1]+

LC/MS (ESI-) m/z 416, 418 [M-1]-

SYNTHETIC EXAMPLE 5

Synthesis of methyl 3-{[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)carbonothioyl]amino}propionate

The synthesis was performed in the same manner as described in synthetic example 3, using methyl-3-isothiocyanatobenzene (yield 78%).

Morphology: white solid

LC/MS: condition 5, the retention time of 5.03 (min)

LC/MS (ESI +) m/z 446 [M+1]+

LC/MS (ESG-) m/z 444, 446 [M-1]-

SYNTHETIC EXAMPLE 6

Synthesis of 3-{[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)carbonothioyl]amino}propionic acid

The synthesis was performed in the same manner as described in synthetic example 2, using methyl-{3-[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)carbonothioyl]amino}propionate obtained in synthetic example 5 (yield 41%).

Morphology: white solid

LC/MS: conditions 5, retention time 4,74 (min)

LC/MS (ESI+) m/z 432, 434 [M+1]+

LC/MS (ESI-) m/z 430, 432 [M-1]-

SYNTHETIC EXAMPLE 7

Synthesis of 1-[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)carbonothioyl]amino-2-methoxyethane

The synthesis was performed in the same manner as described in synthetic example 3, using 2-methoxyethylamine (yield 43%).

Morphology: pale yellow solid

LC/MS: condition 5, the retention time of 5.05 (min)

LC/MS (ESI+) m/z 418, 420 [M+1]+

LC/MS (ESI-) m/z 416, 418 [M-1]-

SYNTHETIC EXAMPLE 8

Synthesis of methyl-1-[(2-{1-[5-(4-bromophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylate

The synthesis was performed in the same manner as described in synthetic example 1, using 1-[5-(4-bromophenyl)-4-g is proxytype-3-yl]ethanone (obtained by the method described in WO 2004/108683) and methyl-1-hydrazinecarbothioamide-4-carboxylate obtained in reference synthetic example 2 (yield 64%).

Morphology: pale yellow solid

LC/MS: conditions 2, retention time 3,74 (min)

LC/MS (ESI+) m/z 496, 498 [M+1]+

LC/MS (ESI-) m/z 494, 496 [M-l]-

SYNTHETIC EXAMPLE 9

Synthesis of 1-[(2-{1-[5-(4-bromophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylic acid

The synthesis was performed in the same manner as described in synthetic example 2, using methyl-1-{1-[5-(4-bromophenyl)-4-hydroxythiophene-3-yl]ethylidenenorbornene}piperidine-4-carboxylate, obtained in synthetic example 8 (yield 87%).

Morphology: pale yellow solid

LC/MS: conditions 2, retention time of 3.45 (min)

LC/MS (ESI+) m/z 482, 484 [M+1]+

LC/MS (ESI-) m/z; 480, 482 [M-1]-

SYNTHETIC EXAMPLE 10

Synthesis of 1-[(2-{1-[4-hydroxy-5-(4-triptoreline)thiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylic acid

Methyl-1-[(2-{1-[4-hydroxy-5-(4-triptoreline)thiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylate

The synthesis was performed in the same manner as described in synthetic example 1, using 1-[4-hydroxy-5-(4-triptoreline)thiophene-3-yl]ethanone (obtained by the method described is in WO 2004/108683) and methyl-1-hydrazinecarbothioamide-4-carboxylate, obtained in reference synthetic example 2 (yield 36%).

Morphology: pale yellow solid

LC/MS: conditions 1, retention time of 4.54 (min)

LC/MS (ESI+) m/z 486 [M+1]+

LC/MS (ESI-) m/z 484 [M-1]-

1-[(2-{1-[4-Hydroxy-5-(4-triptoreline)thiophene-3-yl] ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylic acid

The synthesis was performed in the same manner as described in synthetic example 2, using the previously obtained methyl-1-[(2-{1-[4-hydroxy-5-(4-triptoreline)thiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylate (yield 58%).

Morphology: white solid

LC/MS: conditions 5, retention time 4,88 (min)

LC/MS (ESI+) m/z 472 [M+1]+

LC/MS (ESI-) m/z 470 [M-1]-

SYNTHETIC EXAMPLE 11

Synthesis of 1-[(2-{1-[5-(4-trifloromethyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylic acid

Methyl-1-[(2-{1-[5-(4-trifloromethyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylate

The synthesis was performed in the same manner as described in synthetic example 1, using 1-[5-(4-trifloromethyl) -4-hydroxythiophene-3-yl]ethanone (obtained by the method described in WO 2004/108683) and methyl-1-hydrazinecarbothioamide-4-carboxylate obtained in reference synthetic example 2 (yield 53%).

Morph is logy: pale yellow solid

LC/MS: conditions 2, retention time of 3.75 (min)

LC/MS (ESI+) m/z : 502 [M+1]+

LC/MS (ESI-) m/z 500 [M-1]-

1-[(2-{1-[5-(4-Trifloromethyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylic acid

The synthesis was performed in the same manner as described in synthetic example 2, using the result of the above methyl-1-[(2-{1-[5-(4-trifloromethyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylate (yield 52%).

Morphology: pale yellow solid

LC/MS: conditions 2, retention time 3,49 (min)

LC/MS (ESI+) m/z 488 [M+1]+

LC/MS (ESI-) m/z 486 [M-1]-

SYNTHETIC EXAMPLE 12

Synthesis of 1-[(2-{1-[5-(4-chlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylic acid

Methyl-1-[(2-{1-[5-(4-chlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylate

The synthesis was performed in the same manner as described in synthetic example 1, using 1-[5-(4-chlorophenyl)-4-hydroxythiophene-3-yl]ethanone (obtained by the method described in WO 2004/108683) and methyl-1-hydrazinecarbothioamide-4-carboxylate obtained in reference synthetic example 2 (yield 41%).

Morphology: pale yellow solid

LC/MS: conditions 1, retention time 4,50 (min)

LC/MS (ESI+) m/z 452, 454 [M+1 ]+

LC/MS (ESI-) m/z 450, 452 [M1]-

1-[(2-{1-[5-(4-Chlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylic acid

The synthesis was performed in the same manner as described in synthetic example 2, using the result of the above methyl-1-[(2-{1-[5-(4-chlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylate (yield 92%).

Morphology: yellow solid

LC/MS: conditions 1, retention time 4,14 (min)

LC/MS (ESI+) m/z 438, 440 [M+1]+

LC/MS (ESI-) m/z 436, 438 [M-1]-

SYNTHETIC EXAMPLE 13

Synthesis of 1-[(2-{1-[5-(3,4-dimetilfenil)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylic acid

Methyl-1-[(2-{1-[5-(3,4-dimetilfenil)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylate

The synthesis was performed in the same manner as described in synthetic example 1, using 1-[5-(3,4-dimetilfenil)-4-hydroxythiophene-3-yl]ethanone (obtained by the method described in WO 2004/108683) and methyl-1-hydrazinecarbothioamide-4-carboxylate obtained in reference synthetic example 2 (yield 28%).

Morphology: pale yellow solid

LC/MS: conditions 2, retention time of 3.69 (min)

LC/MS (ESI+) m/z 446 [M+1]+

LC/MS (ESI-) m/z 444 [M-1]-

1-[(2-{1-[5-(3,4-Dimetilfenil)-4-HYDR shall xiaofen-3-yl] ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylic acid

The synthesis was performed in the same manner as described in synthetic example 2, using the result of the above methyl-1-[(2-{1-[5-(3,4-dimetilfenil)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylate (yield 100%).

Morphology: a pale-brown solid

LC/MS: conditions 2, retention time 3,38 (min)

LC/MS (ESI+) m/z; 431,78 [M+1]+

LC/MS (ESI-) m/z; 429,89 [M-1]-

SYNTHETIC EXAMPLE 14

Synthesis of 1-[(2-{1-[5-(4-tert-butylphenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylic acid

Methyl-1-[(2-{1-[5-(4-tert-butylphenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylate

The synthesis was performed in the same manner as described in synthetic example 1, using 2-(4-tert-butylphenyl)-3-hydroxy-4-methylcarbonate and methyl-1-hydrazinecarbothioamide-4-carboxylate obtained in reference synthetic example 2 (yield 57%).

Morphology: a pale-brown solid

LC/MS: condition 2, the retention time of a 3.87 (min)

LC/MS (ESI+) m/z 474 [M+1]+

LC/MS (ESI-) m/z 472 [M-1]-

1-[(2-{1-[5-(4-tert-Butylphenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylic acid

The synthesis was performed in the same manner as described in synthetic example 2, using the received above-methyl-1-[(2-{1-[5-(4-tert-butylphenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylate (yield 89%).

Morphology: dark brown solid

1H-NMR (ppm, in DMSO-d6) δ: 1,22 (s, N), 1,57-to 1.61 (m, 2H), 1,88-of 1.92 (m, 2H), a 2.36 (s, 3H), 4.53-in-4,58 (m, 2H), 7,41 (d, 2H, J=8.5 Hz), to 7.67 (d, 2H, J=8.5 Hz), the 7.85 (s, 1H), of 10.25 (users, 1H), 11,98 (users, 1H).

SYNTHETIC EXAMPLE 15

Synthesis of 1-[(2-{1-[5-(3-chlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylic acid

Methyl-1-[(2-{1-[5-(3-chlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylate

The synthesis was performed in the same manner as described in synthetic example 1, using 1-[5-(3-chlorophenyl)-4-hydroxythiophene-3-yl]ethanone (obtained by the method described in WO 2004/108683) and methyl-1-hydrazinecarbothioamide-4-carboxylate obtained in reference synthetic example 2 (yield 63%).

Morphology: pale yellow solid

LC/MS: conditions 2, retention time to 3.67 (min)

LC/MS (ESI+) m/z 452, 454 [M+l]+

LC/MS (ESI-) m/z 450, 452 [M-l]-

1-[(2-{1-[5-(3-Chlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylic acid

The synthesis was performed in the same manner as described in synthetic example 2, using the result of the above methyl-1-[(2-{1-[5-(3-chlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylate (yield 71%).

Morphology: pale yellow solid

W is/MS: conditions 2, retention time 3,38 (min)

LC/MS (ESI+) m/z 438, 440 [M+1]+

LC/MS (ESI-) m/z 436, 438 [M-1]-

SYNTHETIC EXAMPLE 16

Synthesis of 1-[(2-{1-[4-hydroxy-1-methyl-5-(4-triptoreline)-1H-pyrazole-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylic acid

Methyl-1-[(2-{1-[4-hydroxy-1-methyl-5-(4-triptoreline)-1H-pyrazole-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylate

The synthesis was performed in the same manner as described in synthetic example 1, using 1-[4-hydroxy-1-methyl-5-(4-triptoreline)-1H-pyrazole-3-yl]ethanone (obtained by the method described in WO 2004/108683) and methyl-1-hydrazinecarbothioamide-4-carboxylate obtained in reference synthetic example 2 (yield 70%).

Morphology: yellow solid

LC/MS: conditions 1, retention time of 4.12 (min)

LC/MS (ESI+) m/z 484 [M+1]+

LC/MS (ESI-) m/z 482 [M-1]-

1-[(2-{1-[4-Hydroxy-1-methyl-5-(4-triptoreline)-1H-pyrazole-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylic acid

The synthesis was performed in the same manner as described in synthetic example 2, using the result of the above methyl-1-[(2-{1-[4-hydroxy-1-methyl-5-(4-triptoreline)-1H-pyrazole-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylate (yield 85%).

Morphology: pale yellow solid

LC/MS: conditions 1, lie the retention of 3.69 (min)

LC/MS (ESI+) m/z 470 [M+1]+

LC/MS (ESI-) m/z 468 [M-1]-

SYNTHETIC EXAMPLE 17

Synthesis of 1-[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxy-1-methyl-1H-pyrazole-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylic acid

Methyl-1-[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxy-1-methyl-1H-pyrazole-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylate

The synthesis was performed in the same manner as described in synthetic example 1, using 1-[5-(3,4-dichlorophenyl) -4-hydroxy-1-methyl-1H-pyrazole-3-yl]ethanone (obtained by the method described in WO 2004/108683) and methyl-1-hydrazinecarbothioamide-4-carboxylate obtained in reference synthetic example 2 (yield 61%).

Morphology: pale pink solid

LC/MS: conditions 1, retention time 4,30 (min)

LC/MS (ESI+) m/z 484, 486 [M+1]+

LC/MS (ESI-) m/z 482, 484 [M-1]-

1-[(2-{1-[5-(3,4-Dichlorophenyl)-4-hydroxy-1-methyl-1H-pyrazole-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylic acid

The synthesis was performed in the same manner as described in synthetic example 2, using the result of the above methyl-1-[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxy-1-methyl-1H-pyrazole-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylate (yield 89%).

Morphology: pale yellow solid

LC/MS: conditions 1, retention time 3,79 (min)

LC/MS (ESI+) m/z 470, 472 [M+1]+

LC/MS (ESI-) m/z 468, 470 [M-1]-

SYNTHETIC EXAMPLE 18

Synthesis of 1-[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-3-carboxylic acid

Ethyl-1-[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-3-carboxylate

The synthesis was performed in the same manner as described in synthetic example 1 using ethyl-1-hydrazinecarbothioamide-3-carboxylate obtained in reference synthetic example 3 (yield 52%).

Morphology: white solid

1-[(2-{1-[5-(3,4-Dichlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-3-carboxylic acid

The synthesis was performed in the same manner as described in synthetic example 2, using the above ethyl-1-[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-3-carboxylate (yield 67%).

Morphology: white solid

LC/MS: condition 5, the retention time to 4.98 (min)

LC/MS (ESI+) m/z 472 [M+1]+

LC/MS (ESI-) m/z 470 [M-1]-

SYNTHETIC EXAMPLE 19

Synthesis of diethylamide 1-[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylic acid

The synthesis was performed in the same manner as described in synthetic example 1, using the IER is ylamide 1-hydrazinecarbothioamide-4-carboxylic acid, obtained in reference synthetic example 4 (yield 23%).

Morphology: white solid

LC/MS: condition 5, the retention time of 3.80 (min)

LC/MS (ESI+) m/z 527 [M+1]+

SYNTHETIC EXAMPLE 20

Synthesis of 1-[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-ol

The synthesis was performed in the same manner as described in synthetic example 1, using 1-hydrazinecarbothioamide-4-ol obtained in reference synthetic example 5 (yield 21%).

Morphology: white solid

LC/MS: conditions 5, retention time 4,88 (min)

LC/MS (ESI+) m/z 444 [M+1]+

LC/MS (ESI-) m/z 442 [M-1]-

SYNTHETIC EXAMPLE 21

Synthesis of 1-[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-3-ol

The synthesis was performed in the same manner as described in synthetic example 1 using crude 1-hydrazinecarbothioamide-3-ol obtained in reference synthetic example 6 (yield 53%).

Morphology: pale yellow solid

LC/MS: conditions 5, retention time 4,92 (min)

LC/MS (ESI+) m/z 444 [M+1]+

LC/MS (ESI-) m/z 442 [M-1]-

SYNTHETIC EXAMPLE 22

Synthesis of 1-[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-methanol

Sin is ez conducted in the same manner as described in synthetic example 1 using crude 1-hydrazinecarbothioamide-4-methanol obtained in reference synthetic example 7 (yield 22%).

Morphology: white solid

LC/MS: condition 5, the retention time to 4.98 (min)

LC/MS (ESI+) m/z 458 [M+1]+

LC/MS (ESI-) m/z 456 [M-1]-

SYNTHETIC EXAMPLE 23

Synthesis of 1-[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)carbonothioyl]amino-3-methoxypropane

The synthesis was performed in the same manner as described in synthetic example 3, using 3-methoxypropylamine (yield 19%).

Morphology: pale yellow solid

LC/MS: conditions 5, retention time 5,22 (min)

LC/MS (ESI+) m/z 432 [M+1]+

LC/MS (ESI-) m/z 430 [M-1]-

SYNTHETIC EXAMPLE 24

Synthesis of 4-picolylamine 1-[(2-{1-[5-(4-bromophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylic acid

To 1-[(2-{1-[5-(4-bromophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylic acid (84 mg, 0,17 mmol)obtained in synthetic example 9, was added dimethylformamide (2 ml), the hydrochloride of 1-[3-(dimethylamino)propyl]-3-ethylcarbodiimide (66 mg, 0.25 mmol) and HOBt (47 mg, 0.25 mmol)and then was added dimethylformamide (2.5 ml) and diisopropylethylamine (91 μl, 0.52 mmol). The resulting solution p is remedial at room temperature for 1 hour, and then mixed with a solution of 4-picolylamine (47 mg, 0.43 mmol) in dimethylformamide (1.5 ml) for 24 hours. After adding water, the reaction mixture was filtered and the filter cake was dried and washed several times with isopropyl alcohol, obtaining the target product (yield 34%).

Morphology: pale yellow solid

LC/MS: conditions 1, retention time 3,05 (min)

LC/MS (ESI+) m/z 572, 574 [M+1]+

LC/MS (ESI-) m/z 570, 572 [M-l]-

SYNTHETIC EXAMPLE 25

Synthesis of 2-picolylamine 1-[(2-{1-[5-(4-bromophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylic acid

The synthesis was performed in the same manner as described in synthetic example 24 using 2-picolylamine (yield 22%).

Morphology: pale yellow solid

LC/MS: conditions 1, retention time 3,62 (min)

LC/MS (ESI+) m/z 572, 574 [M+1]+

LC/MS (ESI-) m/z 570, 572 [M-1]-

SYNTHETIC EXAMPLE 26

Synthesis of 3-picolylamine 1-[(2-{1-[5-(4-bromophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperidine-4-carboxylic acid

The synthesis was performed in the same manner as described in synthetic example 24 using 3-picolylamine (yield 4%).

Morphology: yellow solid

LC/MS: conditions 1, retention time of 3.25 (min)

LC/MS (ESI+) m/z 572, 574 [M+1]+

LC/M is (ESI -) m/z 570, 572 [M-1]-

SYNTHETIC EXAMPLE 27

Synthesis of 2-{4-[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]}piperazine-1-yl}acetic acid

Methyl-2-{4-[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperazine-1-yl}acetate

Methyl-2-[4-hydrazinecarbothioamide-1-yl]acetate (356 mg, of 1.52 mmol)obtained in reference synthetic example 10 and 2-(3,4-dichlorophenyl)-3-hydroxy-4-methylcarbonate (147 mg, 0,512 mmol) was stirred with dimethylformamide (4 ml) and concentrated hydrochloric acid (42,6 μl, of 1.52 mmol) at a temperature of from room temperature up to 60°C for 5 days. After adding water, the reaction mixture was filtered and the filter cake was dried. The filter cake was mixed with chloroform and filtered, the filtrate was concentrated and then mixed with chloroform, isopropyl alcohol and n-hexane and filtered. The filter cake was dried, obtaining the target product (yield 18%). The crude product was used directly in the next reaction.

LC/MS: conditions 1, retention time of 3.97 (min)

LC/MS (ESI+) m/z 501, 503 [M+1]+

LC/MS (ESI-) m/z 499, 501 [M-1]-

Synthesis of 2-{4-[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperazine-1-yl}acetic acid

The synthesis was carried out in accordance with methods is Oh, described in synthetic example 2, using methyl-2-{4-[(2-{1-[5-(3,4-dichlorophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperazine-1-yl}acetate, receiving crude target product. The crude product was washed with chloroform, obtaining the target product (yield 11%).

Morphology: pale yellow solid

LC/MS: conditions 1, retention time of 3.60 (min)

LC/MS (ESI+) m/z 487, 489 [M+1]+

LC/MS (ESI-) m/z 485, 487 [M-1]-

SYNTHETIC EXAMPLE 28

Synthesis of 2-{4-[(2-{1-[5-(4-bromophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperazine-1-yl}]acetic acid

Methyl-2-{4-[(2-{1-[5-(4-bromophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]}piperazine-1-yl}acetate

The synthesis was carried out in accordance with the method of condensation described in synthetic example 27 using 2-(4-bromophenyl)-3-hydroxy-4-methylcarbonate, receiving crude target product (yield 57%). The crude product was used directly for the next reaction.

Morphology: pale yellow solid

2-{4-[(2-{1-[5-(4-Bromophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperazine-1-yl}]acetic acid

The synthesis was carried out according to the method of hydrolysis described in synthetic example 27 using methyl-2-{4-[(2-{1-[5-(4-bromophenyl)-4-hydroxamate the-3-yl]ethylidene}hydrazino)thiocarbonyl]piperazine-1-yl}acetate, receiving target product (yield 43%).

Morphology: pale yellow solid

LC/MS: conditions 1, retention time of 3.45 (min)

LC/MS (ESI+) m/z 497, 499 [M+1]+

LC/MS (ESI-) m/z 495, 497 [M-1]-

SYNTHETIC EXAMPLE 29

Synthesis of 3-{4-[(2-{1-[5-(4-bromophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperazine-1-yl}propionic acid

Methyl-3-{4-[(2-{1-[5-(4-bromophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperazine-1-yl}propionate

The synthesis was carried out in accordance with the method of condensation described in synthetic example 27, using ethyl-3-[4-hydrazinecarbothioamide-1-yl]propionate obtained in reference synthetic example 11, receiving the crude target product (yield 13%). The crude product was used directly for the next reaction.

LC/MS: conditions 1, retention time 3,05 (min)

LC/MS (ESI+) m/z 539, 541 [M+1]+

LC/MS (ESI-) m/z 537, 539 [M-1]-

3-{4-[(2-{1-[5-(4-Bromophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperazine-1-yl}propionic acid

The synthesis was carried out according to the method of hydrolysis described in synthetic example 2, using methyl 3-{4-[(2-{1-[5-(4-bromophenyl)-4-hydroxythiophene-3-yl]ethylidene}hydrazino)thiocarbonyl]piperazine-1-yl}propionate and ethanol as solvent, recip what I target product (yield 55%).

Morphology: pale yellow solid

LC/MS: conditions 1, retention time of 3.07 (min)

LC/MS (ESI+) m/z 511, 513 [M+1]+

LC/MS (ESI-) m/z 509, 511 [M-1]-

Structural formulas of the compounds obtained in synthetic examples below.

REFERENCE SYNTHETIC EXAMPLE 1REFERENCE SYNTHETIC EXAMPLE 2REFERENCE SYNTHETIC EXAMPLE 3REFERENCE SYNTHETIC EXAMPLE 4
REFERENCE SYNTHETIC EXAMPLE 5REFERENCE SYNTHETIC EXAMPLE 6REFERENCE SYNTHETIC EXAMPLE 7REFERENCE SYNTHETIC EXAMPLE 8
REFERENCE SYNTHETIC EXAMPLE 9REFERENCE SYNTHETIC EXAMPLE 10REFERENCE SYNTHETIC EXAMPLE 11SYNTHETIC EXAMPLE 1
SYNTHETIC EXAMPLE 2SYNTHETIC EXAMPLE 3SYNTHETIC EXAMPLE 4SYNTHETIC EXAMPLE 5
SINTET THE ICAL EXAMPLE 6 SYNTHETIC EXAMPLE 7SYNTHETIC EXAMPLE 8SYNTHETIC EXAMPLE 9
SYNTHETIC EXAMPLE 10SYNTHETIC EXAMPLE 11SYNTHETIC EXAMPLE 12SYNTHETIC EXAMPLE 13
SYNTHETIC EXAMPLE 14SYNTHETIC EXAMPLE 15SYNTHETIC EXAMPLE 16SYNTHETIC EXAMPLE 17
SYNTHETIC EXAMPLE 18SYNTHETIC EXAMPLE 19SYNTHETIC EXAMPLE 20SYNTHETIC EXAMPLE 21
SYNTHETIC EXAMPLE 22SYNTHETIC EXAMPLE 23SYNTHETIC EXAMPLE 24SYNTHETIC EXAMPLE 25
SYNTHETIC EXAMPLE 26SYNTHETIC EXAMPLE 27SYNTHETIC EXAMPLE 28SYNTHETIC EXAMPLE 29

SAMPLE ANALYSIS 1

Stimulation of proliferation of thrombopoetin (TPO)-dependent cell line

The reactivity of the compound of synthetic example 4 of the present invention in relation to receptor thrombopoetin (TPO) was analyzed using leukemic cell lines human UT7/EPO-mpl.

(1) Cells and cell culture

UT7/EPO-mpl is a stable transformed cell line, obtained by introducing in the leukaemic cell line human UT7/EPO vector, which induces the expression of the receptor for TPO person (C-mp1under the direct control of the early promoter of cytomegalovirus method Takatoku et al. (J. Biol. Chem., 272:7259-7263 (1997)). The proliferation of this cell line stimulated with TPO, while the parent cell line UT7/EPO does not show a response to the TA is. These two cell lines have subculturally in modified according to the method Iscove environment Dulbecco (IMDM; GIBCO)containing 10% fetal calf serum (FBS; Thermo Electron or BioWest) using CO2incubator (5% CO2, 37°C).

(2) Analysis of cell proliferation

The above subculturally cells were washed twice in phosphate buffered saline and suspended in IMDM medium containing 10% FBS at a density of cells 6×104cells/ml cell Suspension was transferred into 96-well plates to tissue culture (CORNING) in a 100-µl aliquot. Then or TPO (Pepro Tech EC), or the compound of synthetic example 4, dissolved in dimethyl sulfoxide (DMSO), diluted 83-fold using IMDM medium containing 10% FBS and added to the above cell suspensions in the form of a 20-µl aliquot. Cell suspension was incubated in CO2-incubator (5% CO2, 37 ░ C for 4 days. Cell proliferation was analyzed using the reagent WS-8 (Kishida Chemical Co., Ltd.) in accordance with the manufacturer's instructions. 10-ál aliquot of 5 mm solution of the reagent WS-8 was added to each well of the tablet for tissue cultures and the plate is incubated at 37°C for 4 hours. Educated formosanus pigment were detected by measuring the absorption at 450 nm using a reader for 96-well plates (Nihon Molecular Devices, Spectramax 190). In Fig. shows the results for cells, UT7/EPO-mpl, while figure 2 shows the data obtained for cells, UT7/EPO, not expressing the receptor for TPO.

Figure 1 shows that cell proliferation UT7/EPO-mpl, giving the response to TPO, was stimulated with compound of synthetic example 4 concentration-dependent manner, whereas for UT7/EPO parent cell line effect of this compound on the proliferation was not observed, as shown in figure 2. These results indicate that the compound of synthetic example 4 of the present invention selectively affects the TPO receptor as an activator.

EXAMPLE ANALYSIS 2

Connections the following synthetic examples were tested in accordance with the method of analysis example 1 to determine the concentration of each compound, which increases the speed corresponding to 50%GE growth leukemia cell line human IT-7/EPO-mpl observed in the presence of 10 ng/ml TPO (EC50). The results are summarized in table 4.

Table 4
Synthetic example No.EC50(ng/ml)
131
23,2
3 24
45,6
530
614
728
825
92,3
102,7
112,9
122,1
132,6
142,6
152,6
16the 3.8
177,8
1822
1926
203,1
2123
2221
2333

EXAMPLE 1 DRUG

Received the t of the granulated product, containing the following ingredients.

Ingredients
The compound represented by formula (1)10 mg
Lactose700 mg
Corn starch274 mg
GOC-L16 mg
1000 mg

The compound represented by formula (1), and lactose sieved through a sieve of 60 mesh. Corn starch is sifted through a sieve of 120 mesh. All this is mixed with magnesium stearate in the mixer, V-type. A powder mixture is ground with an aqueous solution of hydroxypropylcellulose (GOC-L) low viscosity, granularit (extrusion granulation, the die size of 0.5-1 mm) and dried. The obtained dried granules are sieved through a vibration sieve (12/60 mesh), receiving the granulated product.

EXAMPLE 2 DRUG

Get the powdered drug in the form of granules for encapsulation containing the following ingredients.

Ingredients
The compound represented by formula (1) 10 mg
Lactose79 mg
Corn starch10 mg
Magnesium stearate1 mg
100 mg

The compound represented by formula (1), and lactose sieved through a sieve of 60 mesh. Corn starch is sifted through a sieve of 120 mesh. All this is mixed with magnesium stearate in the mixer, V-type. In hard gelatin capsules No. 5 put 10%powder 100 mg in each.

EXAMPLE 3 DRUG

Receive the granulated product to encapsulate containing the following ingredients.

Ingredients
The compound represented by formula (1)15 mg
Lactose90 mg
Corn starch42 mg
GOC-L3 mg
150 mg

The compound represented by formula (1), and lactose perceivethat a sieve of 60 mesh. Corn starch is sifted through a sieve of 120 mesh. All this is mixed with magnesium stearate in the mixer, V-type. A powder mixture is ground with an aqueous solution of hydroxypropylcellulose (GOC-L) low viscosity, granularit and dried. The obtained dried granules are sieved through a vibration sieve (12/60 mesh). The pellets are placed in a hard capsule No. 4, 150 mg each.

EXAMPLE 4 DRUG

Get the product in the form of tablets containing the following ingredients.

Ingredients
The compound represented by formula (1)10 mg
Lactose90 mg
Microcrystalline cellulose30 mg
Magnesium stearate5 mg
SMC-Na15 mg
150 mg

The compound represented by formula (1), lactose, microcrystalline cellulose and CMC-Na (sodium carboxymethyl cellulose) sieved through a sieve of 60 mesh and mixed. A powder mixture is mixed with magnesium stearate, getting surround poroshkoobraznuju mixture. A powder mixture is pressed directly into the 150-mg tablet.

SAMPLE PREPARATION 5

Preparation for intravenous obtained as follows.

The compound represented by formula (1)100 mg
The glycerides of saturated fatty acids1000 ml

The solution having the above composition is typically administered to the patient intravenously at a rate of 1 ml in 1 minute.

INDUSTRIAL APPLICABILITY

Compounds of the present invention, which have an affinity towards the receptor of thrombopoietin and act as agonists of the receptor thrombopoetin, can be used as a therapeutic and improving agents for diseases in which the effective activation of the receptor thrombopoetin, particularly in the quality of medicines in hematological disorders, accompanied by abnormal platelet counts and in the quality of medicines in diseases, treatment and prevention which involve stimulating the differentiation and proliferation of endothelial cells of blood vessels and endothelial progenitor cells and can be used as medicines.

1. The compound represented by formula (1)

where A represents a nitrogen atom or CH,
when A represents a nitrogen atom, represents NR9(where R9represents a C1-10alkyl group), and when A represents CH, A represents a sulfur atom,
R1represents a phenyl group (the phenyl group substituted by one or more substituents selected from the group consisting of halogen atoms, C1-0 alkyl groups and C1-10alkoxygroup (C1-10alkyl groups and C1-10alkoxygroup are unsubstituted or substituted by one or more halogen atoms)),
L1is a relationship
X is a HE,
R2represents a C1-10alkyl group,
L2is a relationship
L3represents NH,
L4represents a bond or NH,
Y represents a sulfur atom, and
when L4represents a bond, R3represents piperidinyloxy group, piperazinilnom group (piperidinyl group and piperazinilnom group substituted by a Deputy selected from the group comprising C1-10alkoxycarbonyl group, carboxyl group, hydroxyl group, di-C1-10alkylaminocarbonyl group, C1-10alkylaminocarbonyl group and C1-10alkyl group, (C1-10alkylaminocarbonyl group and C1-10alkyl group substituted by a Deputy selected from the group comprising peredelnye group, hydroxyl group and carboxyl group)), or when L4represents NH, R3represents a C1-10alkyl group, (C1-10alkyl group substituted by a Deputy selected from the group comprising C1-10alkoxygroup, C1-10alkoxycarbonylmethyl or carboxyl group), tautomer, or pharmaceutically acceptable salt of the compound.

2. The compound according to claim 1, where R2represents a methyl group and
when L4represents a bond, R3represents piperidinyloxy group, piperazinilnom group (piperidinyl group and piperazinilnom group substituted by a Deputy selected from the group comprising methoxycarbonyl group, carboxyl group, hydroxyl group, diethylaminocarbonylmethyl group, paradimethylaminobenzaldehyde group, methyl group and ethyl group (methyl group and ethyl group substituted by a Deputy selected from the group comprising hydroxyl groups and carboxyl groups)), or when L4represents NH, R3represents a methyl group, ethyl group or n-sawn group (methyl group, ethyl group or n-sawn group substituted by a Deputy selected from the group comprising metoxygroup, methoxycarbonyl group or carboxyl group), tautomer, or pharmaceutically acceptable salt of the compound.

3. The compound according to claim 2, where L is a bond, R3represents piperidinyloxy group (piperideine group substituted by a carboxyl group), tautomer or pharmaceutically acceptable salt of the compound.

4. The compound according to any one of claims 1 to 3, g is e a represents CH, In represents a sulfur atom, tautomer or pharmaceutically acceptable salt of the compound.

5. The compound according to claim 4, where R1represents 3,4-dichlorophenyl, 4-tert-butylphenyl, 3,4-dimetilfenil, 4-triptoreline, 4-chlorophenyl, 4-bromophenyl, 4-trifloromethyl or 3-chlorophenyl, tautomer or pharmaceutically acceptable salt of the compound.

6. The compound according to claim 3, where a represents a nitrogen atom, represents NR9where R9represents a methyl group and R2represents a methyl group, tautomer or pharmaceutically acceptable salt of the compound.

7. The connection according to claim 6, where R1represents 3,4-dichlorophenyl or 4-triptoreline, tautomer or pharmaceutically acceptable salt of the compound.

8. Activator receptor thrombopoetin, representing a compound of formula (1) according to claim 1.

9. The compound according to claim 1 as an active ingredient for the preparation of a medicinal product having the properties of agonist receptor thrombopoetin.

10. Medicinal product which has the properties of the agonist receptor thrombopoetin containing as active ingredient a compound according to claim 1 or its pharmaceutically acceptable salt.



 

Same patents:

FIELD: chemistry.

SUBSTANCE: present invention relates to organic chemistry and specifically to compounds of formula I or to pharmaceutically acceptable salts thereof, where Ar is imidazole or pyrazole, where the said Ar can be substituted with substitute(s) selected from a group consisting of a C1-C6 alkyl group, a phenyl group and a halogen atom, each of Y1, Y2 and Y3 is a carbon ot nitrogen atom, A is an oxygen atom, a sulphur atom or a group of formula -SO2-, R1 is a hydrogen atom, a C1-C6 alkyl group which can be substituted with one phenyl group (where the said phenyl group can be substituted with one substitute selected from a group consisting of a halogen atom and a C1-C6 alkyl group), or a phenyl group, R2 is a C1-C6 alkyl group, R3 is (i) a C1-C18 alkyl group, (ii) C2-C8 alkenyl group, (iii) C2-C8 alkynyl group, (iv) C3-C8 cycloalkyl group, (v) C1-C6 alkyl group substituted with 1-3 substitutes selected from a group given in paragraph 1 of the formula of invention, or (vi) a phenyl group, a naphthyl group, a pyrazolyl group, a pyridyl group, an indolyl group, a quinolinyl group or an isoquinolinyl group, where each of the said groups can be substituted with 1-3 substitutes selected from a group given in paragraph 1, R4 is a hydrogen atom or a C1-C6 alkyl group, and R5 is (i) C1-C10 alkyl group, (ii) C1-C10 alkyl group which is substituted with one or two substitutes selected from a group given in paragraph 1, (iii) C2-C8 alkenyl group which can be substituted with a phenyl group, or (iv) phenyl group, naphthyl group, thienyl group, pyrrolyl group, pyrazolyl group, pyridyl group, furanyl group, benzothienyl group, isoquinolinyl group, isoxazolyl group, thiazolyl group, benzothiadiazolyl group, benzoxadiazolyl group, phenyl group, condensed with a 5-7-member saturated hydrocarbon ring which can contain one or two oxygen atoms as ring members, uracyl group or tetrahydroisoquinolinyl group, where each of the said groups can be substituted with 1-5 substitutes selected from a group given in paragraph 1, provided that when Ar is a group of formula 5, which can be substituted with a C1-C6 alkyl group, R5 is not a C1-C10 alkyl group, and the formula (I) compound is not 5-(3,5-dichlorophenylthio)-4-isopropyl-2-methane-sulfonylaminomethyl-1-methyl-1H-imidazole or 5-(3,5-dichlorophenylthio)-4-isopropyl-1-methyl-2-p-toluene-sulfonylaminomethyl-1H-imidazole. The invention also relates to a pharmaceutical composition based on the formula I compound and to formula II compounds, radicals of which are defined in the formula of invention.

EFFECT: obtaining novel compounds with inhibitory effect on the bond between S1P and its Edg-1 (SIP1) receptor.

32 cl, 43 tbl, 18 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel benzene derivatives of general formula (I) or salts thereof: [Chem. 12]

(Symbols in the given formula have the following values X1:-NR12-C(=O)- or -C(=O)-NR12-, X2 : -NR13 -C(=O)-, Ring A is a 6-member ring, if necessary having 1 or 2 double bonds and if necessary having 1-3 heteroatoms selected from N, O, Ring B is a benzene ring or a 6-member heteroaryl ring having 1-3 heteroatoms selected from N, R is a hydrogen atom or a residue of β-D- glucopyranoside uronic acid; R1-R8 are identical or different and each denotes a hydrogen atom, a halogen atom, -O-(lower alkyl), R9-R11 are identical or different and each denotes a hydrogen atom, lower alkyl, -O-(lower alkyl), -(CH2)n-N(lower alkyl)2, -(CH2)n-NH(lower alkyl), -(CH2)n-N(lower alkyl) (if necessary substituted with -C=O; a 6-member heterocycle having 1-3 heteroatoms selected from N, S, O) -(CH2)n-(C=O)-N(lower alkyl)2, -(CH2)n-(C-O)-N(lower alkyl) (if necessary substituted with -C=O, alkyl, a 6-member heterocycle having 1-3 heteroatoms selected from N) -(CH2)n- if necessary substituted with alkyl, -COCH3, -SO2CH3, -COOCH3, -C=O, CF3, -OCH3, OH, halogen; 5-7-member heterocycle having 1-3 heteroatoms selected from N, S, O), -(CH2)n-O- (if necessary substituted with alkyl; 6-member heterocycle having 1-3 heteroatoms selected from N), n is an integer from 0 to 3, R12 and R13 denote a hydrogen atom, provided that in R1-R11, when two lower alkyls are bonded to a nitrogen atom, they can together form a 3-8-member nitrogen-containing heterocycle.) The invention also relates to benzene derivatives of general formula (II), to a pharmaceutical composition, as well as to use of the said compounds.

EFFECT: obtaining novel biologically active compounds which are active as inhibitors of activated blood-coagulation factor X.

16 cl, 365 ex, 42 tbl

FIELD: chemistry.

SUBSTANCE: present invention relates to benzazepin derivatives of formula (I), where R1 is unsubstituted cyclobutyl, R2 is 3-pyrazinyl, substituted CON(H)(Me) or 2-pyridinyl-M-pyrrolidinyl, where the said pyrrolidinyl group is substituted with a =O group; which is: methylamide 5-(3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yloxy) pyrazine-2-carboxylic acid

or 1-{6-[(3-cyclbutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-3-pyridinyl}-2-pyrrolidinone

EFFECT: obtaining compounds which have affinity to histamine H3 receptor and pharmaceutical compositons containing said compounds.

11 cl, 288 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula

,

where the carbon atom denoted * is in R- or S-configuration; X is a concentrated bicyclic carbocycle or heterocycle selected from a group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, indazolyl, indolyl, benzooxazolyl, benzothiazolyl, indenyl, indanyl, dihydrobenzocycloheptenyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, quinoxalinyl, 2H-chromenyl, imidazo[1.2-a]pyridinyl, pyrazolo[1.5-a]pyridinyl, and condensed bicyclic carbocycle or condensed bicyclic heterocycle, optionally substituted with substitutes (1 to 4) which are defined below for R14; R1 is H, C1-C6-alkyl, C3-C6-cyclalkyl, C1-C3-alkyl, substituted OR11, -NR9R10 or -CN; R2 is H, C1-C6-alkyl, or gem-dimethyl; R3 is H, -OR11, C1-C6-alkyl or halogen; R4 is H, halogen, -OR11, -CN, C1-C6-alkyl, C1-C6-alkyl, substituted -NR9R10, C3-C6-cycloalkyl, substituted -NR9R10, C(O)R12; or R4 is morpholinyl, piperidinyl, pyrimidinyl, pyridazinyl, pyrazinyl, pyrrolyl, isoxazolyl, pyrrolidinyl, piperazinyl, 2-oxo-2H-pyridinyl, [1.2.4]triazolo[4.3-a]pyridinyl, 3-oxo-[1.2.4]triazolo[4.3-a]pyridinyl, quinoxalinyl, which are optionally substituted with substitutes (1 to 4) which are defined below for R14; R5 is H or C1-C6-alkyl; R6 is H, C1-C6-alkyl, or -OR11; R7 is H; R8 is H, -OR9, C1-C6-alkyl, -CN; R9 is H or C1-C4-alkyl; R10 is H or C1-C4-alkyl; or R9 and R10 taken together with the nitrogen atom to which they are bonded form morpholine; R11 is H, C1-C4-alkyl; R12 is C1-C6-alkyl; R14 in each case is independently selected from a substitute selected from a group consisting of halogen, -OR11, -NR11R12, C1-C6-alkyl, which is optionally substituted with 1-3 substitutes, in each case independently selected from a group consisting of C1-C3-alkyl, aryl; or to pharmaceutically acceptable salts thereof. The invention also relates to a pharmaceutical composition, to a method of obtaining formula (I) compounds, as well as to a method of treating disorders.

EFFECT: obtaining new biological active compounds having norepinephrine, dopamine and serotonin reuptake selective inhibitory activity.

90 cl, 162 ex, 2 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel 1-thio-D-glucitol compounds of formula I or to pharmaceutically acceptable salts thereof or hydrates of the compound or salts: , [where R1, R2, R3 and R4 are identical or different, and each is a hydrogen atom, C1-C6-alkyl group), A is -(CH2)n-, -CONH(CH2)n-, -O- or -(CH2)nCH=CH- (where n is an integer from 0 to 3, Ar1 is an arylene group, heteroarylene group, which is an unsaturated 5-9-member mono- or bicyclic group, containing 1-2 heteroatoms, selected from S and N, Ar2 is an aryl group or heteroaryl group which is an unsaturated 5-9-member mono- or bicyclic group containing 1-2 heteroatoms selected from O, S and N, and R5, R6, R7, R8, R9 and R10 are identical or different, and each is (i) a hydrogen atom, (ii) a halogen atom, (iii) a hydroxyl group, (iv) C1-8-alkyl group, optionally substituted with hydroxyl group(s), (v) -(CH2)m-Q {where m is an integer from 0 to 4, and Q is -CO2H, -ORc1, -CO2Ra3, -SRe1, -NHRa6 or -NRa7Ra7 (where each of Ra3, Ra6 and Ra7 is a C1-6-alkyl group, Rc1 is a C1-6-alkyl group, and Rc1 is a C1-6-alkyl group)}, (vi) -O-(CH2)m'-Q' {where m' is an integer from 1 to 4, and Q' is a hydroxyl group,-CO2H, -CO2Ra8, -CONRa10Ra10, -NRa12Ra12 (where each of Ra8, Ra10 and Ra12 is a C1-6-alkyl group)}, (vii) -ORf {where Rf is C3-7-cycloalkyl group or tetrahydropyranyl group)}, (viii) morpholine group, (ix) phenyl group, (x) pyridyl group]. The invention also relates to 1-thio-D-glucitol compounds of formulae IA, II, III, IV, to a pharmaceutical agent, to methods of obtaining 1-thio-D-glucitol compounds, as well as to compounds of formulae XIII, XIV.

EFFECT: obtaining novel biologically active compounds which are inhibitors of sodium-dependent co-transporter-2-glucose.

25 cl, 140 ex, 3 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula Ia: and its pharmaceutically acceptable salt, where: p equals 0 or 1; n assumes values from 1 to 3, q equals 1; R5 is selected from hydrogen, -XNR7R8, pyrimidine-C0-4alkyl, pyridine-C0-4alkyl, phenyl, C3-10cycloalkyl-C0-4alkyl and C3-6heterocycloalkyl-C0-4alkyl, where C3-6heterocycloalkyl is a saturated monocyclic ring system containing the said number of atoms, provided that one or more of the said carbon atoms is substituted with O or NR, where R is hydrogen or C1-4alkyl; R7 and R8 represent C1-4alkyl; R6 denotes hydrogen; or R5 and R6 together with a nitrogen atom to which they are both bonded form morpholine or piperidine; where any piperdine-C0-4alkyl, piperidine-C0-4alkyl or C3-10cycloalkyl-C0-4alkyl of substitute R5 or a combination of radicals R5 and R6 can be optionally substituted with 1-2 radicals which are independently selected from -XNR7R8 and -XOR7, the said phenyl of substitute R5 is substituted with a -XR9 group, the said C3-6heterocycloalkyl-C0-4alkyl of substitute R5 is optionally substituted with a -XOR7 group, where X is a single bond or C1-4alkylene; R7 and R8 are independently selected from hydrogen and C1-4alkyl; R9 is selected from C3-10heterocycloalkyl which is a saturated monocyclic ring system containing the said number of atoms, provided that one or more of the said carbon atoms is substituted with O or NR, where R is as given above; R10 denotes hydrogen; R15 is selected from halogen, C1-6alkyl and C1-6alkoxy; and R16 is selected from halogen, methoxy, nitro, -NR12C(O)R13, -C(O)NR12R12, -NR12R12, -C(O)OR12 and -C(O)NR12R13; each R12 is selected from hydrogen and C1-6alkyl; R13 is selected from phenyl, thienyl, pyrazolyl, pyridinyl or isoxazolyl, where any phenyl, thienyl, pyrazolyl, pyridinyl or isoxazolyl of substitute R13 can be optionally substituted with 1-2 radicals which are independently selected from halogen, C1-6alkyl, halogen-substituted C1-6alkyl, imidazole-C0-4alkyl, C3-10cycloalkyl, C3-10heterocycloalkyl-C0-4alkoxy and C3-10heterocycloalkyl-C0-4alkyl; where the said C3-10heterocycloalkyl-C0-4alkoxy and C3-10heterocycloalkyl-C0-4alkyl each represent a saturated monocyclic ring system containing the said number of atoms, provided that one or more of the said carbon atoms is substituted with O or NR, where R assumes values given above; and the said C3-10heterocycloalkyl-C0-4alkoxy and C3-10heterocycloalkyl-C0-4alkyl can each be optionally substituted with 1 radical independently selected from C1-6alkyl, hydroxyl-substituted C1-6alkyl and NR7R8, where R7 and R8 assume values given above. The invention also relates to pharmaceutical compositions containing the said compounds.

EFFECT: obtaining novel compounds and compositions based on the said compounds which can be used in medicine for treating and preventing diseases or disorders associated with abnormal or uncontrolled kinase activity, particularly diseases or disorders associated with abnormal activity of kinase c-Src, FGFR3, KDR and/or Lck.

12 cl, 1 tbl, 2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel therapeutically suitable derivatives of pyridazin-3(2H)-one of formula and pharmaceutical compositions containing the said derivatives. These compounds are used for treating, preventing or inhibiting corresponding pathological conditions, diseases or disorders, mainly asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, atopic dermatitis, psoriasis or irritable colon syndrome.

EFFECT: obtaining compounds which are active and selective phosphodiesterase 4 (PDE4) inhibitors.

11 cl, 1 tbl, 182 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method for synthesis of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophenecarboxamide by reacting 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]-phenyl}-morpholin-3-one-hydrochloride with 5-chlorothiophene-2-carbonyl chloride, distinguished by that the reaction is carried out in a solvent selected from ether, alcohol, ketone and water or a mixture thereof using an inorganic base.

EFFECT: design of a simple method for synthesis of said thiophenecarboxamide without use of toxic solvents.

13 cl, 1 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula

or

or to their pharmaceutically acceptable salts, where ring A, R2, R3, R4 and X are as defined in the description. The disclosed compounds are useful as 11βHSD1 inhibitor. The invention also relates to a pharmaceutical composition, an agent for treating or preventing pathology related to glucocorticoids, a 11βHSD1 inhibitor containing the disclosed compound or its pharmaceutically acceptable salt, and use of the disclosed compounds.

EFFECT: compounds are highly effective.

40 cl, 48 tbl, 191 ex

FIELD: chemistry.

SUBSTANCE: described are compounds of formula , where X, R1, R2, R3, R4 and R5 assume values given in the description and paragraphs of the formula of invention, and their pharmaceutically acceptable salts.

EFFECT: compounds have antagonistic activity on histamine receptor 3 (H3).

25 cl, 3 tbl, 215 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to organic chemistry and specifically to compounds of formula I or to pharmaceutically acceptable salts thereof, where Ar is imidazole or pyrazole, where the said Ar can be substituted with substitute(s) selected from a group consisting of a C1-C6 alkyl group, a phenyl group and a halogen atom, each of Y1, Y2 and Y3 is a carbon ot nitrogen atom, A is an oxygen atom, a sulphur atom or a group of formula -SO2-, R1 is a hydrogen atom, a C1-C6 alkyl group which can be substituted with one phenyl group (where the said phenyl group can be substituted with one substitute selected from a group consisting of a halogen atom and a C1-C6 alkyl group), or a phenyl group, R2 is a C1-C6 alkyl group, R3 is (i) a C1-C18 alkyl group, (ii) C2-C8 alkenyl group, (iii) C2-C8 alkynyl group, (iv) C3-C8 cycloalkyl group, (v) C1-C6 alkyl group substituted with 1-3 substitutes selected from a group given in paragraph 1 of the formula of invention, or (vi) a phenyl group, a naphthyl group, a pyrazolyl group, a pyridyl group, an indolyl group, a quinolinyl group or an isoquinolinyl group, where each of the said groups can be substituted with 1-3 substitutes selected from a group given in paragraph 1, R4 is a hydrogen atom or a C1-C6 alkyl group, and R5 is (i) C1-C10 alkyl group, (ii) C1-C10 alkyl group which is substituted with one or two substitutes selected from a group given in paragraph 1, (iii) C2-C8 alkenyl group which can be substituted with a phenyl group, or (iv) phenyl group, naphthyl group, thienyl group, pyrrolyl group, pyrazolyl group, pyridyl group, furanyl group, benzothienyl group, isoquinolinyl group, isoxazolyl group, thiazolyl group, benzothiadiazolyl group, benzoxadiazolyl group, phenyl group, condensed with a 5-7-member saturated hydrocarbon ring which can contain one or two oxygen atoms as ring members, uracyl group or tetrahydroisoquinolinyl group, where each of the said groups can be substituted with 1-5 substitutes selected from a group given in paragraph 1, provided that when Ar is a group of formula 5, which can be substituted with a C1-C6 alkyl group, R5 is not a C1-C10 alkyl group, and the formula (I) compound is not 5-(3,5-dichlorophenylthio)-4-isopropyl-2-methane-sulfonylaminomethyl-1-methyl-1H-imidazole or 5-(3,5-dichlorophenylthio)-4-isopropyl-1-methyl-2-p-toluene-sulfonylaminomethyl-1H-imidazole. The invention also relates to a pharmaceutical composition based on the formula I compound and to formula II compounds, radicals of which are defined in the formula of invention.

EFFECT: obtaining novel compounds with inhibitory effect on the bond between S1P and its Edg-1 (SIP1) receptor.

32 cl, 43 tbl, 18 ex

FIELD: chemistry.

SUBSTANCE: invention refers to compounds of the formula (I): , where R1 is C1-C8alkyl optionally substituted with one to three substitutes selected out of substitute group A; R2 is C1-C6alkyl or C1-C6alkoxyC1-C6alkyl; R3 is C1-C6alkyl or C1-C6alkoxy; or R2 and R3 together with adjoining carbon atoms form optionally substituted non-aromatic 5-10-member carbon ring; R4 is hydrogen; G is group represented by the formula: or the rest as provided in the invention claim; and to pharmaceutical composition, application of claimed compounds, and method of atopic dermatitis prevention or treatment.

EFFECT: novel compounds useful as atopic dermatitis treatment medication and antipruritic medicines.

24 cl, 75 ex, 290 tbl

FIELD: chemistry.

SUBSTANCE: present invention relates to cyclic derivatives of aminobenzoic acid and to their pharmaceutically acceptable salts of general formula , in which ring Ar is a phenyl group, a 5-member aromatic heterocyclic group containing 1-2 heteroatoms selected from nitrogen, sulphur and oxygen, or a benzothiazolyl group; where the said groups can have 1-2 substitutes selected from a group comprising lower alkyl; a phenyl group; a phenyl group substituted with 1-2 halogens; a phenyl group substituted with a lower alkoxy group; a phenyl group substituted with a halogen-substituted lower alkyl group; a phenoxy group substituted with a halogen; a halogen; Z is an oxygen atom or -(CH2)-n (where n equals 0, 1 or 2); Y is C1-C4 alkylene, C2-C4 alkenylene or general formula (2) -T-A-U- (2) in which T is a single bond, C1-C4 alkylene or C2-C4 alkenylene; U is single bond, C1-C4 alkylene; values of the rest of radicals are given in the formula of invention.

EFFECT: obtaining a PPARα, agonist which contains an active ingredient in form of at least one cyclic derivative of aminobenzoic acid, and an agent which reduces the level of lipids which contains an active ingredient in form of at least one cyclic derivative of aminobenzoic acid.

12 cl, 16 tbl, 184 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to new imidazole derivatives of general formula I , where R1 is C1-C10alkyl or C3-C10cycloalkyl, each possibly and independently substituted with 1 substitute selected from C3-C10cycloalkyl or aryl or a heteroaryl group, possibly substituted with one or two halogens; aryl or heteroaryl; R2 is C1-C10alkoxy or C1-C10thioalkyl; R3 is C1-C10alkoxy, possibly substituted with one C1-C10alkoxy or nitrile, where the said alkoxy group can be cyclic or can contain one O heteroatom; R4 is C1-C10alkyl; C2-C10alkenyl; C1-C10alkoxy or C3-C10cycloalkyl, each possibly and independently substituted with 1 or 2 substitutes selected from C1-C10alkoxy, C3-C10cycloalkyl, carboxylic ester, or with one or two aryl or heteroaryl groups, possibly substituted with one substitute selected from C1-C10alkyl, C3-C10cycloalkyl, nitro or halogen; aryl or heteroaryl, each possibly and independently substituted with 1-3 substitutes selected from C1-C10alkyl, C3-C10cycloalkyl, C1-C10alkoxy, phenoxy, thiophenyl, halogen, nitro, nitrile or aryl group, possibly substituted with one halogen; where up to three hydrogen atoms of the alkyl group can be substituted with fluorine atoms; where the said cycloalkyl can independently have one or two carbon atoms substituted with O or N; where the said aryl denotes an aromatic ring having 6 to 10 carbon atoms, including mono- and bicyclic compounds; and where the said heteroaryl denotes an aromatic ring having 3 to 10 carbon atoms, including mono- and bicyclic compounds in which one to three ring atoms are oxygen, nitrogen or sulphur atoms; except compounds given in paragraph 1. The invention also pertains to use of the said compounds for making a medicinal agent, a treatment and prevention method, a compound of formula II (values of radicals are given in the formula of invention).

EFFECT: new imidazole derivatives having positive allosteric modulator effect on GABAB receptor are obtained.

30 cl, 6 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel 1-thio-D-glucitol compounds of formula I or to pharmaceutically acceptable salts thereof or hydrates of the compound or salts: , [where R1, R2, R3 and R4 are identical or different, and each is a hydrogen atom, C1-C6-alkyl group), A is -(CH2)n-, -CONH(CH2)n-, -O- or -(CH2)nCH=CH- (where n is an integer from 0 to 3, Ar1 is an arylene group, heteroarylene group, which is an unsaturated 5-9-member mono- or bicyclic group, containing 1-2 heteroatoms, selected from S and N, Ar2 is an aryl group or heteroaryl group which is an unsaturated 5-9-member mono- or bicyclic group containing 1-2 heteroatoms selected from O, S and N, and R5, R6, R7, R8, R9 and R10 are identical or different, and each is (i) a hydrogen atom, (ii) a halogen atom, (iii) a hydroxyl group, (iv) C1-8-alkyl group, optionally substituted with hydroxyl group(s), (v) -(CH2)m-Q {where m is an integer from 0 to 4, and Q is -CO2H, -ORc1, -CO2Ra3, -SRe1, -NHRa6 or -NRa7Ra7 (where each of Ra3, Ra6 and Ra7 is a C1-6-alkyl group, Rc1 is a C1-6-alkyl group, and Rc1 is a C1-6-alkyl group)}, (vi) -O-(CH2)m'-Q' {where m' is an integer from 1 to 4, and Q' is a hydroxyl group,-CO2H, -CO2Ra8, -CONRa10Ra10, -NRa12Ra12 (where each of Ra8, Ra10 and Ra12 is a C1-6-alkyl group)}, (vii) -ORf {where Rf is C3-7-cycloalkyl group or tetrahydropyranyl group)}, (viii) morpholine group, (ix) phenyl group, (x) pyridyl group]. The invention also relates to 1-thio-D-glucitol compounds of formulae IA, II, III, IV, to a pharmaceutical agent, to methods of obtaining 1-thio-D-glucitol compounds, as well as to compounds of formulae XIII, XIV.

EFFECT: obtaining novel biologically active compounds which are inhibitors of sodium-dependent co-transporter-2-glucose.

25 cl, 140 ex, 3 tbl

FIELD: chemistry.

SUBSTANCE: described are novel thiophene derivatives of formula (1) and pharmaceutically acceptable salts thereof, where A is -CH2CH2-, -NH-CH2-, -CH2-O or -CH2NH-, R1 is hydrogen or alkyl, when X is C-R4, R1 additionally represents halogen, and when A is -CH2-CH2- or -CH2NH, R1 additionally represents alkoxy, R2 is hydrogen, alkoxy, fluoralkoxy, hydroxyalkoxy, hydroxyalkyl, di-(hydroxy)alkoxy, pyridinyl-3-methoxy, pyridinyl-4-methoxy, R3 is hydrogen, alkyl, trifluoromethyl, and when X is C-R4, R3 additionally represents halogen, and when A is -CH2-CH2-, R3 additionally represents alkoxy, X is N or C-R4, R4 is hydrogen, alkyl, alkoxy or halogen, R5 is methyl or ethyl. Also described are isomers of the said compounds, an initial compound for synthesis of formula (1) compound, which has agonistic effect on S1P1/EDG1 receptors, as well as a pharmaceutical composition based on formula (1) compound and use of formula (1) compound.

EFFECT: obtaining a pharmaceutical composition for preventing or treating diseases or disorders associated with activated immune system.

19 cl, 2 tbl, 167 ex

FIELD: chemistry.

SUBSTANCE: described is a compound selected from a group consisting of formula II formula III and formula IV , or its salt or ester, where G1 is selected from a group which includes - (CR1R2)n-, n equals 0 or 1; R1 and R2 are independently selected from a group which includes hydrogen; X1, X2 and X3 are independently selected from a group consisting of hydrogen, optionally substituted lower alkyl, halogen, optionally substituted lower alkoxy, G2 is a heterocycloalkyl linker optionally substituted with X4 and X5, where the heterocycloalkyl linker is selected from a group consisting of piperazinyl, 3,6-dihydro-2N-pyridinyl, [1,4]diazepanyl, 3,9-diazabicyclo[3,3,1]nonyl; X4 and X5 are independently selected from a group consisting of hydrogen and optionally substituted lower alkyl; CO2R; R is selected from a group consisting of optionally substituted lower alkyl and hydrogen; G3 is a bond; G4 is selected from a group consisting of hydrogen, aryl, selected from phenyl which is optionally substituted with a lower alkyl, halogen, lower haloalkyl or lower haloalkoxy; heteroaryl selected from pyridinyl which is optionally substituted with a halogen or lower haloalkyl; and optionally substituted cycloheteroalkyl selected from 1,3-benzodioxolyl. Described also are specific compounds and a pharmaceutical composition.

EFFECT: disclosed compounds are used as modulators of receptors activated by a peroxisomal proliferator.

5 cl, 2 tbl, 117 ex

FIELD: chemistry.

SUBSTANCE: novel compound is N-(5-hydroxy-2,4-di-tert-butylphenyl)-4-oxo-1H-quinoline-3-carboxamide or its pharmaceutically acceptable salts. The invention also relates to a pharmaceutical composition.

EFFECT: obtaining a novel biologically active compound with CFTR activity modulation properties.

2 cl, 485 ex, 3 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to compounds with general formula (I) and its isomers, where R1 is a hydrogen atom of an alkyl C1-4 group with a straight or branched chain, or a phenyl group, thienyl group or furyl group, optionally substituted with one or more alkyl C1-4 groups with a straight or branched chain, C1-4 alkoxy groups with a straight or branched chain, or halogen atoms; R2 is a hydrogen atom or an alkyl C1-4 group with a straight or branched chain, or a phenyl, benzyl, thienyl or furyl group, optionally substituted with a methylenedioxy group, or one or more alkyl C1-4 groups with a straight or branched chain, or C1-4 alkoxy-, hydroxyl-, trifluoromethyl- or cyano-group with a straight or branched chain, or halogen atoms, as well as to a method of producing said compound. The invention also relates to new intermediates with general formula (II) and their production.

EFFECT: radioligands A3 with antagonistic action are obtained and described, labeled with iodine isotopes with mass number 125, which have high specific activity.

16 cl, 3 ex, 2 tbl, 1 dwg

FIELD: chemistry.

SUBSTANCE: present invention relates to a quinazoline compound of formula or its pharmaceutically acceptable salts, used as inhibitors of potential-dependant sodium and calcium channels, where R1, R2, R3, R5a, R5, y and x are defined in the formula of invention. The invention also relates to a pharmaceutical composition containing the disclosed compound and to methods of inhibiting one or more of NaV1.2, NaV1.3, NaV1.8, or CaV2.2.

EFFECT: 4-aminoquinazoline antagonists of selective sodium and calcium ion channels.

17 cl, 3 tbl, 1 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of general formula (I') which have inhibitory effect on ALK kinase: , where n' is selected from 1 and 2; R'2 is selected from halogen; R'3 is selected from -S(O)2NR'5R'6, -S(O)2R'6 and -C(O)NR'5R'6, where R'5 is selected from hydrogen and C1-6alkyl, and R'1 is selected from C1-6alkyl; and R'1 is selected from phenyl which is substituted with 3 radicals independently selected from C2-6alkoxy group, C1-6alkyl, -X'R'4 and -OXR'4, where X' denotes a bond, and R'4 is selected from piperazinyl, piperidinyl, pyrrolidinyl, morpholino, where R'4 can be optionally substituted with 1-3 radicals independently selected from C1-6 alkyl, provided that the following compound is excluded .

EFFECT: design of a method of inhibiting and using compounds for making a medicinal agent for treating diseases which respond to ALK kinase inhibition.

7 cl, 61 ex

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