Amide derivative and pharmaceutical composition containing said derivative. RU patent 2481343.
 Nitrogen-containing aromatic heterocyclic compound / 2481330Invention refers to compounds of general formula (I), wherein A represents a pyrrole group or a pyrazole group, and X represents a carbon atom or a nitrogen atom; R1 represents a carboxy group; R2 independently represents a group specified in a substitute group α; R3 independently represents phenyl(C1-C6alkyl)group substituted by, phenyl(C1-C6alkyl)group (wherein the substitute(s) represents (represent) 1-4 groups independently specified in the substitute group α); m is equal to 0, 1, 2 or 3, n is equal to 0 or 1; each of R4, R5, R6 and R7 independently represents a hydrogen atom, C1-C6alkyl group or a halogen atom; B represents a substituted naphthyl group (wherein the substitute(s) represents (represent) 1-4 groups independently specified in the substitute group α), or the group represented by formula (II), wherein B1, B2 and α are those as specified in the patent claim. Also, the invention refers to a pharmaceutical composition possessing lipolysis inhibiting activity, to the use of the compounds of formula (I) in preparing a drug preparation for treating hyperlipidemia, dislipidemia, abnormal lipid metabolism, arteriosclerosis or type II diabetes mellitus and to a method of treating or preventing the mentioned diseases. |
 5-ht2a- and d3-receptor double modulators / 2480466Invention refers to compounds of general formula |
 Phenylpyrazol derivatives / 2480456Invention refers to a phenylpyrazol derivative presented by formula (1) or to its pharmaceutically acceptable salt: wherein R1 and R2, which may be identical or different, each represents C1-C6 alkyl, or R1 and R2 are coupled together with an adjacent nitrogen atom to form a 5-6-merous saturated heterocylic ring (wherein the mentioned saturated heterocylic ring may be substituted by halogen or C1-C6 alkyl), n represents an integer 0 to 2, T represents a hydrogen atom, halogen or C1-C6 alkyl, and R has one of formulas (I)-(V), (VII) or (VIII): |
 Substituted n-phenyl-bipyrrolidine ureas and therapeutic use thereof / 2478094Invention relates to substituted N-phenyl-bipyrrolidine ureas of formula (I) , |
 Mdm2 and p53 interaction inhibitors / 2477724Invention refers to compounds of formula |
 Polycyclic indazole-derivatives and their application as erk inhibitors for cancer treatment / 2475484Invention relates to particular compounds, which demonstrate inhibiting activity with respect to ERK, whose structure formula is given in description, to their pharmaceutically acceptable salts, based on them pharmaceutical composition and their application for treatment of cancer, mediated by ERK activity. |
 Method of producing heterocycle-substituted pyridine derivatives / 2474581Invention relates to a method of producing heterocycle-substituted pyridine derivatives of general formula (I) by reacting a compound of general formula (III) with a compound of formula (II) in a solvent and in the presence of a catalyst based on palladium or a base, where R1, R2, X, Y, Q, A, Z, R, R3 and R4 are described in the claim. |
 Inhibitors of diacylglycerol o-acyltransferase type 1 enzyme / 2474576Invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, where Q is phenyl or pyridinyl; A is pyrazolyl or triazolyl, where each A is independently additionally unsubstituted or substituted with 1 or 2 substitutes represented by Ra, or A is formula (a); Va is C(R4), Vb is N or C(R5) and Vc is N; or Va is N, Vb is C(R5) and Vc is N or C(R6); R4 is hydrogen, R5 is hydrogen, C1-6alkyl, -ORb, -SRb, aryl, selected from phenyl, heteroaryl, selected from thienyl, or cycloalkyl, selected from cyclopropyl; R6 is hydrogen or aryl, selected from phenyl; R7 is hydrogen or C1-6alkyl; R3 is hydrogen, C1-3alkyl, -OH, -S(O)2R1, or heteroaryl, selected from tetrazolyl, where the heteroaryl is bonded to a nitrogen atom through a ring carbon atom; Rb, Rx, Ry, Rza, Rzb, Rw, Re, Rk, Rm, Rn, Rq and R1, in each case, are independently hydrogen, C1-3alkyl or C1-3haloalkyl; and Rf, in each case, is independently hydrogen, C1-3alkyl or -OH (the rest of the substitutes assume values given in the claim). The invention also relates to a pharmaceutical composition, having inhibiting action on DGAT-1, which contains a compound of formula (I), and a treatment method. |
 Pyrimidine compounds, compositions and methods of use / 2473549Invention refers to new pyrimidine derivatives and their pharmaceutically acceptable salts possessing the properties of a mTOR kinase inhibitor. In formula (I): A represents a 6-8-member mono- or bicyclic heterocyclic ring containing 1 to 2 heteroatoms optionally specified in N and O as apexes of the ring and having 0-2 double bonds; and wherein the ring A is additionally substituted by 0 to 2 substitutes RA specified in a group consisting of -ORa, -Rc and -(CH2)1-4-ORa wherein Ra is optionally specified in hydrogen and C1-6alkyl; Rc represents C1-6alkyl; G is specified in a group consisting of -C(O)-, -OC(O)-, -NHC(O)- and -S(O)0-2-; B is specified in a group consisting of phenylene and 5-6-member heteroarylene consisting 1-2 nitrogen heteroatom as apexes of the ring, and substituted by 0 to 1 substitutes RB specified in F, Cl, Br, I and Rp; wherein Rp represents C1-6 alkyl; D is specified in a group consisting of -NR3C(O)NR4R5, -NR4R5, C(O)NR4R5, -NR3C(=N-CN)NR4R5, -NR3C(O)R4, -NR3C(O)OR4 and -NR3S(O)2R4, and wherein the group D and a substitute placed on an adjoining atom in the ring B, optionally combined to form a 5-6-member heterocyclic or heteroaryl ring containing 1 to 3 heteroatoms specified in N, O and S, as apexes of the ring and substituted by the substitute 0-1 RD. The R1-R5 radical values are presented in the patent claim. |
 3-amino-6-(1-aminoethyl)tetrahydropyrane derivatives / 2471795Invention refers to new antibacterial compounds of formula I |
 Isoxazole derivatives as type 1 11-beta-hydroxysteroiddehydrogenase modulators / 2480467Invention refers to isoxazole derivatives of formula |
 7-substituted indole mcl-1 inhibitors / 2473542Invention refers to 7-substituted indoles of formula I: |
 Novel phenyl pyrrole derivative / 2470917Invention relates phenyl pyrrole derivatives formula (I) where: A denotes =NOR4, O; R4 denotes, C1-C6 alkyl; R1 denotes C1-C6 alkyl, C1-C6 alkoxy, halogen-C1-C6 alkyl, halogen-C1-C6 alkoxy, NH2, mono- C1-C6 alkylamino, halogen-mono-C1-C6 alkylamino, di(C1-C6 alkyl)amino, halogen-di-(C1-C6 alkyl)amino; or A and R1 together with the carbon atom with which they are bonded form a 5- or 6-member heterocyclic aromatic group or a heterocyclic group with partially or completely reduced saturation, which can be benzo-condensed, can contain 1-3 heteroatoms selected from N, O and S, which can be substituted and contain 1 or 2 α substitutes; R2 denotes phenyl which can be substituted with 1 or 2 α substitutes, or a 6-member heteroaryl group containing 1 or 2 N atoms, which can be substituted with 1 or 2 α substitutes; R3 denotes OH, C1-C6 alkoxy, values of α are given in claim 1, or a pharmaceutically acceptable salt thereof. |
 Synthesis of epothiliones, intermediate products thereof, analogues and use thereof / 2462463Invention relates to a compound of formula or a pharmaceutically acceptable salt thereof, in which R1 denotes hydrogen or C1-6alkyl; R2 denotes isooxazolyl group, substituted with C1-6alkyl; RB denotes -CF3, -CHF2, -CH2F, or C1-6alkyl. The invention also relates to pharmaceutical compositions for treating cancer which contain the disclosed compounds. |
 Carbamoyloxyaryl alkanoyl arylpiperazine compound, pharmaceutical compositions containing said compound and method of treating pain, anxiety and depression / 2460731In general formula 1 , a cyclic ring can be selectively formed; each of R1 and R2 is independently selected from a group consisting of hydrogen, with a straight or branched alkyl chain having 1-6 carbon atoms and phenetyl or R1 and R2 together form a 5- or 6-member heterocyclic ring or R1 and R2 together with Ar1 form a bicyclic ring; Ar1 is selected from a group consisting of furanyl, thionyl, methylene dioxyphenyl and phenyl, which can be substituted with at least one identical or different substitutes selected from a group consisting of hydrogen, with a straight or branched alkyl chain having 1-6 carbon atoms, a halogen such as F, O and Br, with a straight or branched alkoxy chain, having 1-6 carbon atoms, nitro and trifluoromethyl; Z is hydrogen or fluorine, or taken together with Ar1 forms a bicyclic ring; Ar2 is selected from a group consisting of phenyl, methylene dioxyphenyl, pyridine pyrimidine, naphthyl, bis(fluorophenyl)methyl and quinoxaline, which can be substituted with at least one identical or different substitutes selected from a group consisting of hydrogen, with a straight or branched alkyl chain, having 1-6 carbon atoms, hydroxy, halogen, with a straight or branched alkoxy chain having 1-6 carbon atoms, nitro, acetyl, tert-butyl acetate, trifluoromethyl, amino and acetate; n is equal to 1 or 2; m is an integer from 0 to 2. |
 Novel 2-aminooxazolines as taar1 ligands / 2460725Invention is a 6-10-member aryl selected from phenyl, naphthyl, tetrahydronaphthalenyl, indanyl or a 6-member heteroaryl containing 1-2 N atoms, selected from pyridyl or pyrimidinyl, where the aryl and heteroaryl groups can be unsubstituted or substituted with 1-3 substitutes selected from a group consisting of C3-6-cycloalkyl, phenyl, phenyloxy, benzyl, benzyloxy, halogen atom, C1-7-alkyl, C1-7-alkoxy, oxazolyl, piperidin-1-yl, or C1-7-alkyl, substituted with a halogen atom, or represents phenyl, where at least one hydrogen atom is substituted with deuterium or tritium; R2 is a hydrogen atom, C1-7-alkyl or is benzyl, unsubstituted or substituted C1-7-alkoxy or halogen atom; or R1 and R2 together with a N atom with which they are bonded form 2,3-dihydroindol-1-yl or 3,4-dihydro-1quinolin-1-yl. The invention also relates to a method of producing compounds of formula and to a pharmaceutical composition having high affinity for the TAAR1 receptor. |
 Substituted heteroaryl derivatives / 2459806Invention refers to new substituted heteroaryl derivatives of general formula I: , wherein: A means N, CR7-10, with A at the most twice meaning N; W means O, S or NR4, the values B, C, R7-10 are presented in clause 1 of the patent claim. The method for preparing the compound I is described. |
 Substituted 4-imidazoles, method for preparing and using them / 2456281Present invention refers to new imidazole derivatives of formula I wherein R1 represents a hydrogen atom or C1-7alkyl; R2 represents C1-7alkyl; R3 represents C1-7alkyl, C1-7alkoxy, phenyloxy, benzyloxy, a halogen atom or C1-7alkyl substituted by a halogen atom; R4 represents a hydrogen atom or C1-7alkyl; X represents -CH2-, -CHR2 - or -O; Y represents -CH2-, -CH2CH2- or a bond; provided X represents -O-, Y represents -CH2-; Z represents -CH2- or -CHR2-; provided R2 is found twice, simultaneously for X and Z which are CHR2 , then R2 can be identical alkyls or different; n has the value 0, 1 or 2; provided n has the value 2, R3 can be identical or different; and its pharmaceutically acceptable acid addition salts, except for the following compounds: 1-(1H-imidazol-4-ylmethyl)-1,2,3,4-tetrahydro-quinoline and 1-(3H-imidazol-4-ylmethyl)-2,3-dihydro-1H-indole. Also, the invention refers to a method for preparing the compounds of formula I, to a drug based on the compound of formula I and applying the compound of formula I in preparing the drug. |
 Nitrogen containing heterocyclic derivative showing type i 11β -hydroxysteroiddehydrogenase inhibitory activity / 2455285Invention refers to a compound of formula (II) |
![Clathrate complexes of beta-cyclodextrin with 1-{[6-bromo-1-methyl-5-methoxy-2-phenylthiomethyl-1-h-indol-3-yl]carbonyl}-4-benzylpiperazine, having antiviral activity, synthesis and use thereof](http://img.russianpatents.com/img_data/965/9657564-s.gif) Clathrate complexes of beta-cyclodextrin with 1-{[6-bromo-1-methyl-5-methoxy-2-phenylthiomethyl-1-h-indol-3-yl]carbonyl}-4-benzylpiperazine, having antiviral activity, synthesis and use thereof / 2448120Invention relates to a novel clathrate complex of β-cyclodextrin with 1-{[6-bromo-1-methyl-5-methoxy-2-phehylthiomethyl-1-H-indol-3-yl]carbonyl}-4-benzylpiperazine of formula : with molar ratio 1-{[6-bromo-1-methyl-5-methoxy-2-phehylthiomethyl-1-H-indol-3-yl]carbonyl}-4-benzylpiperazine: β-cyclodextrin from 1:1 to 1:10, synthesis method and use thereof as an antiviral agent for treating influenza. The disclosed method involves mixing solutions of β-cyclodextrin and 1-{[6-bromo-1-methyl-5-methoxy-2-phehylthiomethyl-1-H-indol-3-yl]carbonyl}-4-benzylpiperazine in molar ratio from 1:1 to 1:10 while stirring and heating to temperature not higher than 70°C and then maintaining said conditions until a homogeneous solution is obtained and extraction of the obtained complex. |
 Conjugated lipid derivatives / 2480447Invention refers to a new lipid compound of general formula , wherein n=0; R1 and R2 are identical or different, and may be specified in a group of substitutes consisting of a hydrogen atom, a C1-C7alkyl group, a halogen atom and a C1-C7alkoxy group; X represents COR3 or CH2OR4, wherein R3 is specified in a group consisting of hydrogen, hydroxy, C1-C7alkoxy and amino; and R4 is specified in a group consisting of hydrogen, C1-C7alkyl or C1-C7acyl, Y represents C9-C21 alkene with one or more double bonds in E- or Z-configurations with the chain Y being unsubstituted and containing a double bond in the ω-3 position; provided R1 and R2 cannot simultaneously represent a hydrogen atom. |
FIELD: chemistry.
SUBSTANCE: invention relates to a compound of formula (1), in which Ar is a group of formula
(Ar-1) or
(Ar-2), in which R1 is a halogen, R2 is hydrogen, R3 is hydrogen, R4 is hydrogen, alkyl or alkenyl, X is a nitrogen atom or CH, R5 and R6 are each hydrogen and h equals 1; 1 equals 1 or 2; m equals 1 or 2; n equals 0, 1 or 2; o equals an integer from 0 to 3, under the condition that n and o are equal to 0 at the same time. Values of group A are as given in claim 1 of the invention. Described also is a pharmaceutical composition having agonistic activity with respect to 7 serotonin (5-HT4-receptors), which contains a compound of formula (1) and an agent which stimulates enterokinesis or improves functioning of the alimentary canal, which contains a compound of formula (1) as an active ingredient.
EFFECT: novel compounds are obtained and described, which have strong affinity towards 4 serotonin receptors, which are useful as an agent which stimulates enterokinesis or an agent which improves functioning of the alimentary canal.
28 cl, 233 ex, 29 tbl
The text of the description is given in facsimile form.
1. The connection formula (1)
where Ar is a group of formula (Ar-1) or (Ar-2)
where R 1 represents halogen, R 2 represents hydrogen, R 3 represents hydrogen, R 4 is a hydrogen alkyl or , X represents the nitrogen atom or SN, R-5 and R 6 each represent a hydrogen and h is equal to 1; l is equal to 1 or 2; m is 1 or 2; n is 0, 1 or 2; integer from 0 to 3, provided that n and o are not equal simultaneously 0; Rather it represents a group, selected from the group consisting of groups of (1) to (6); (1) hydrogen, cyano or formyl; (2) optionally substituted alkyl; (3) -COR 7 , -COOR 7 , -SO 2 R 7 or CO-COR 7 , where R 7 represents an optionally substituted alkyl, optionally substituted , optionally substituted , optionally substituted cycloalkyl, optionally substituted , optionally substituted aryl, optionally substituted , optionally substituted or unsaturated where attached to any atom carbon heterocycle, or optionally substituted or rich where attached to any atom of carbon of heterocycle; (4) to CO-COOR 8 , where R 8 represents an alkyl; (5) -CONR 9-OR 10 , where R 9 and R 10 are the same or different, and each represent a hydrogen or alkyl; and (6) -CONR 12 R 13 , -CSNR 12 R 13 or SO 2 NR 12 R 13 , where R 12 is a hydrogen or any of the groups in R-7 , R 13 is a hydrogen alkyl or or R 12 and R 13 can connect to each other and together with the neighboring nitrogen atom form optional replacing saturated or unsaturated heterocycle containing 1-3 heteroatoms selected of 1-3 nitrogen atoms or 1 oxygen atom; provided that, if alkyl, or in A or R 7 is substituted, then they are replaced by the same or different 1-5 deputies selected from the group consisting of deputies (a) through (d): (a) halogen, cyano, hydroxy, carboxy, amino or carbarnoyl; (b) -OR 14 , -COR 14 , -COOR 14 , -O-COR 14 , -NR 15-COR 14 , -NR 15-COOR 14 , number 15 R 16 or CONR 15 R 16 , where R represents 14 alkyl, optionally substituted the same or different 1-5 deputies selected from the group consisting of the following deputies: (b') hydroxy, carboxy, -OR 17-and-COOR 17 , where R 17 represents an alkyl; R 15 is a hydrogen or alkyl; R 16 represents an alkyl, or both R 15 and R 16 can connect to each other and together with the neighboring nitrogen atom to form optional replacing saturated or unsaturated heterocycle containing 1-3 heteroatoms selected of 1-3 nitrogen atoms or 1 atom of oxygen; (c) -R-20 , where R is 20 an optionally substituted cycloalkyl, optionally substituted , optionally substituted or unsaturated , optionally substituted or rich ; and (d) -R 21 R 21 represents an optionally substituted aryl or optionally substituted ; provided that, if cycloalkyl or is substituted, then they are replaced by the same or different 1-5 deputies selected from the following groups (e): (e) alkyl, alkoxy or oxo; provided, what, if any atoms of carbon rings are substituted in or unsaturated , or saturated or saturated or unsaturated , the atoms of carbon replaced by the same or different 1-5 deputies selected from the above group (e), provided that, if any atoms of nitrogen rings are substituted, then they are replaced by deputies following groups (f): (f) alkyl, or ; provided that, if aryl or is substituted, then they are replaced by the same or different 1-5 deputies selected from the group consisting of groups of (g) to (i): (g) halogen, cyano, nitro, hydroxy, carboxy, amino, carbarnoyl or(CH 2 ) 2-O-; (h) -e 14 , -OR 14 , -COOR 14 , -O-COR 14 , -NR 15-COR 14 , -NR 15 -COOR 14 , NUMBER 15 R 16
or-CONR 15 R 16 , where R 14 , R 15 and R 16 have the same value as specified above; and (i) phenyl or phenoxy, or pharmaceutically acceptable salt.
2. The connection of claim 1, wherein R 1 represents chlorine, bromine or iodine, R 4 represents an alkyl -, R-5 and R 6 each represent a hydrogen or pharmaceutically acceptable salt.
3. The connection of claim 2, where R 4 is a methyl, ethyl, propyl or isopropyl, or pharmaceutically acceptable salt.
4. Compound according to claim 1, where l is equal to 1 or 2, m is 1 or 2, n is 1 or 2, is 1 or 2, or pharmaceutically acceptable salt.
5. The connection of claim 1, wherein R 1 is a chlorine or bromine, R2 and R3 are hydrogen, R 4 is a methyl or ethyl -, R-5 and R 6 represent hydrogen, h is equal to 1, l is equal to 1, and m is equal to 1, n = 2, about equal to 1, or pharmaceutically acceptable salt.
6. Connection on any one of claims 1 to 5, where a is a (1-1) hydrogen, cyano or formyl, or (2-1) alkyl or alkyl, where phenyl optional replaced by the same or different 1-5 deputies selected from the group consisting of halogen, hydroxy, alkyl, alkoxy, amino and carboxy, or pharmaceutically acceptable salt.
7. Connection on any one of claims 1 to 5, where a is a (3-1) -COR 7a , -COOR 7a , -SO 2 R 7a or CO-COR 7a , where R 7a represents an optionally substituted alkyl, optionally substituted , optionally substituted , optionally substituted cycloalkyl, optionally substituted , optionally substituted aryl, optionally substituted , optionally substituted or unsaturated or optional substituted or rich ; provided that, if alkyl, or in R 7a is substituted, then they are replaced by 1-5 deputies selected from the group consisting of groups of (1) $ (d-1): (1) halogen, cyano, hydroxy, carboxy, amino or carbarnoyl; (b-1) -R-14a , -COR 14a , -COOR 14a-O-COR 14a , -NR 15a-COR 14a , -NR 15a-COOR 14a , -NR 15a R 16a or-CONR 15a R 16a , where R 14a represents an alkyl, R 15a is a hydrogen or alkyl, R 16a represents an alkyl or both R 15a and R 16a can connect to each another and together with the neighboring nitrogen atom to form a rich heterocycle containing 1-3 heteroatoms selected of 1-3 nitrogen atoms, 1 oxygen atom or 1 atom of sulfur, and nitrogen atom nitrogen-containing heterocycle optional replaced , or ; (C-1) cycloalkyl, which is not necessarily replaced by the same or different 1-5 deputies selected from alkyl or alkoxy, or rich , whose carbon atom ring optional replaced by the same or different 1-5 deputies selected from alkyl or alkoxy, and the nitrogen atom ring optional replaced , or ; and (d-1) -R 21a , where R 21a is a aryl or , optionally substituted the same or different 1-5 deputies selected from halogen hydroxy, carboxy, amino, , cyano, -R 14a , -OR, 14a , -NR 15a-COR 14a or-NR 15a R 16a where-R 14a , -R 15a and-R 16a have the same values shown above; provided that if cycloalkyl or in R 7a is substituted, then they are replaced by the same or different 1-5 deputies selected from the following deputies (e-1): (e-1) alkyl or alkoxy; provided that, if any atoms of carbon rings are substituted in a substituted optional or unsaturated and not necessarily a substituted or saturated in R 7a , then they are replaced by the same or different 1-5 deputies selected from the above deputies (e-1), and if any of the nitrogen atoms rings are substituted, then they are replaced by the same or different 1-5 deputies, selected of the following Vice (f-1): (f-1) alkyl, or ; provided that, if aryl or in R 7a is substituted, then they are replaced by the same or different 1-5 deputies selected from the group consisting of the following groups: (g-1) halogen, nitro, hydroxy, carboxy, amino, carbarnoyl or cyano; (h-1) -R-14a , -OR, 14a , -COOR 14a-O-COR 14a , -NR 15a-COR 14a , -NR 15a-COOR 14a or-NR 15a R 16a where-R 14a , -R 15a and-R 16a have the same values specified above; and (i-1) phenyl or phenoxy, or pharmaceutically acceptable salt.
8. Connection in paragraph 7, in which a is a (3-2) -SO 2 R 7b , where R 7b represents an alkyl, alkyl, substituted optional substituted , or optionally substituted phenyl, provided that if phenyl is substituted, then it is substituted by an identical or different 1-5 deputies, chosen from the group consisting of halogen, hydroxy, carboxy, amino, , -R 14b , -OR, 14b , -COOR 14b and-O-COR 14b where-R 14b represents an alkyl, or pharmaceutically acceptable salt.
9. Connection to paragraph 8, in which R 7b is 1-3 alkyl, or pharmaceutically acceptable salt.
10. Connection in paragraph 7, in which a is a (3-3) -COR 7c or CO-COR 7c , where R 7c represents an optionally substituted alkyl or optionally substituted ; provided that, if alkyl or in R 7c is substituted, then they are replaced by 1-5 deputies selected from the group consisting of deputies from (a-2) to (d-2) (a-2) hydroxy, halogen, carbarnoyl or cyano; (b-2) -OR 14a , -COR 14 C-COOR 14c-O-COR 14c , -NR 15c-COR 14c , -NR 15c R or 14c-CONR 15c R 16c where-R 14c and-R 16c represent the same or different alkyls and R 15C is a hydrogen or alkyl; (2) cycloalkyl or or rich , where nitrogen atom or bicyclic busy optional replaced , or ; and (d-2) -R 21c , where R 21c is a aryl or and aryl and optional replaced by the same or different 1-5 deputies selected from the group consisting of halogen, hydroxy, carboxy, amino, , cyano, -R or 14c-OR 14c , where R 14c has the same values specified above; or its pharmaceutically acceptable salt.
11. Connection to 10, where R 7c is 1-3 alkyl, optionally substituted group, selected from the group consisting of the following groups (a-3) and (b-3): (3) hydroxy, carbarnoyl or cyano, and (b-3) -OR 14d-COR 14d , -COOR 14d-O-COR 14d , -NR 15d-COR 14d , -NR 15d R 16d or-CONR 15d R 16d , where R 14d and R 16d represent the same or different C 1-3 alkyls and R 15d is a hydrogen or C 1-3 alkyl; or 2-3 , optionally substituted group, selected from the group consisting of the above groups (a-3), and (b-3), or pharmaceutically acceptable salt.
12. Connection in paragraph 7, in which a is a (3-4) -COR 7d , where R 7d represents an optionally substituted cycloalkyl, optionally substituted , optionally substituted or unsaturated or optionally substituted rich ; provided that, if any atoms of carbon rings are substituted, then they are replaced by the same or different 1-5 deputies selected from alkyl or alkoxy, and, if the atoms of nitrogen rings are substituted, then they are replaced by , or , or pharmaceutically acceptable salt.
13. Connection in paragraph 7, in which a is a (3-5) -COR 7e , where R 7e represents an optionally substituted aryl or optionally substituted ; provided that if aryl or is substituted, then they are replaced by the same or different 1-5 deputies selected from the group consisting of the following deputies from (g-2) to (i-2): (g-2) halogen, amino, carbarnoyl or cyano; (h-2) -R 14e , -OR 14e-O-COR 14e , -NR 15e-COR 14e , -NR 15e-COOR 14e or-NR 15e R 16e , where R 14e and R 16e are the same or different, and each represents an alkyl, R 15e is a hydrogen or alkyl; and (i-2) phenyl or phenoxy, or pharmaceutically acceptable salt.
14. Connection in paragraph 7, in which a is a (3-6) -COOR 7f , where R 7f represents an alkyl, or optionally substituted phenyl; provided that, if phenyl is substituted, then it is substituted by an identical or different 1-5 deputies selected from the group consisting of halogen, nitro, hydroxy, -R, 14f and-OR 14f , where R 14f represents an alkyl, or its pharmaceutically acceptable salt.
15. Connection to paragraph 14, in which R 7f is 1-3 alkyl or 2-3 , or pharmaceutically acceptable salt.
16. Connection on any one of claims 1 to 5, where a is a (6-1) -CONR 12a R 13a , -CSNR 12a R 13a or-SO 2 NR 12a R 13a , where R 12a represents hydrogen, With 1-3 alkyl, With 2-3 , C 1-3 alkyl, substituted With 2-3 , With 1-3 alkyl, substituted optional substituted , or optionally substituted phenyl, provided that, if phenyl is substituted, then it is substituted by an identical or different 1-5 deputies selected from the group consisting of halogen, nitro, hydroxy, carboxy, amino, , -R 14a , -OR, 14a , -COOR and 14a-O-COR 14a , where R 14a represents an alkyl; R 13a is a hydrogen or alkyl or both R 12a and R 13a can connect to each other and together with neighbouring the nitrogen atom to form optional replacing saturated or unsaturated 4-6-membered heterocycle containing 1-3 heteroatoms selected from the group consisting of 1-3 atoms of nitrogen and 1 atom of oxygen, and nitrogen atom nitrogen-containing heterocycle optional replaced , or , or pharmaceutically acceptable salt.
17. Connection to article 16, in which R 12a and R 13a are the same or different, and each is a C 1-3 alkyl; R 12a represents an optionally substituted phenyl, where phenyl optional replaced by 1 or 2 atoms of halogen, hydroxy, carboxy, amino, , -R 14a , -OR, 14a , -COOR 14a or-O-COR 14a , where R 14a represents an alkyl, and R 13a is a hydrogen; or both R 12a and R 13a joined to each other and together with the neighboring atom of nitrogen form pyrrolidinyl, , or ; or pharmaceutically acceptable salt.