Pyrazolo[1,5-a]pyrimidines and pyrazolo[1,5-a]triazine and medicines

 

The invention relates to a new one with selective affinity to T6receptors, pyrazolo[1,5-a]pyrimidines and pyrazolo[1,5-a]triazines General formula I, where X denotes a =C(R4)- or =N-, R1denotes phenyl, optionally substituted by one or more radicals of lower alkyl, halogen, lower alkoxygroup, tolyl, pyridyl, naphthyl or thiophenyl, R2denotes hydrogen, (ness.)alkyl, (ness.)thioalkyl or hydroxy(ness.) alkoxygroup, R3denotes amino(ness.)alkylamino, di(ness.)alkylamino, piperazinil, optionally substituted by one or more radicals, lower alkyl, benzyl, phenyl or hydroxy(NISS. )alkyl, morpholinyl, imidazolyl, (CH3)2N(CH2)nNH-, (CH3)2N(CH2)nO - or morpholinyl(CH2)nO-, where n denotes 2 or 3, R4denotes hydrogen, (ness.) alkyl or hydroxy(ness.)alkyl, R5denotes hydrogen, halogen, (NISS. ) alkyl, C3-C6cycloalkyl, (ness.) alkyl(ness.)alkoxygroup, hydroxy(ness.)alkyl(ness.)alkoxygroup, (CH3)2N(CH2)nNH-, piperazinil, optionally substituted (ness.) the alkyl, piperazinylmethyl, optionally substituted (NISS 4 and R5together represent the group -(CH2)m- or-CH2-S-CH2-, m is 3 or 4, X denotes a =C(R4)- or =N-, R1denotes phenyl, optionally substituted by one or more radicals (ness.)of alkyl, halogen, (ness.)alkoxygroup, tolyl, pyridyl, naphthyl or thiophenyl, as well as their pharmaceutically acceptable salts. Preferred compounds of formula I, where R3denotes an amino group, piperazinil, methylpiperazine. The drug contains a compound of formula I and a therapeutically inert carrier. 2 S. and 9 C.p. f-crystals, 1 PL.

Description text in facsimile form (see graphic part).

Claims

1. Pyrazolo[1,5-a]pyrimidines and pyrazolo[1,5-a]triazine General formula

where X denotes a =C(R4)-or =N-;

R1denotes phenyl, optionally substituted by one or more radicals of lower alkyl, halogen, lower alkoxygroup, tolyl, pyridyl, naphthyl or thiophenyl;

R2denotes hydrogen, lower alkyl, lower thioalkyl or hydroxy-lower alkoxygroup;

R3denotes amino, lower alkylamines of alkyl, benzyl, phenyl or hydroxy-lower alkyl, morpholinyl, imidazolyl, (CH3)2N(CH2)nNH-, (CH3)2N(CH2)nO - or morpholinyl-(CH2)nO-, where n = 2 or 3;

R4denotes hydrogen, lower alkyl or hydroxy-lower alkyl;

R5denotes hydrogen, halogen, lower alkyl, C3-C6cycloalkyl, lower alkyl-lower alkoxygroup, hydroxy-lower alkyl-lower alkoxygroup, (CH3)2N(CH2)nNH-, piperazinil, optionally substituted lower alkyl, piperazinylmethyl, optionally substituted lower alkyl, morpholinyl, morpholinylmethyl, di-lower alkylamino or di-lower alkylamino-lower alkyl,

or R4and R5together represent the group -(CH2)m- or-CH2-S-CH2-, m = 3 or 4,

and their pharmaceutically acceptable salts.

2. Compounds of General formula I on p. 1, where R3denotes the amino group.

3. Connection on p. 2 of the group, including

3-benzazolyl-5-methyl-2-methylsulfonylbenzoyl[1,5-a]pyrimidine-7-ylamine,

3-(4-isopropylbenzenesulfonyl)-5-methyl-2-methylsulfonylbenzoyl [1,5-a]pyrimidine-7-ylamine,

5-methyl-2-methylsulfanyl-3-(naphthalene-2-sulfonyl)pyrazolo [1,5-a]pyrimidine-7-is of IMT-5-cyclopropyl-2-methylsulfonylbenzoyl[1,5-a]pyrimidine-7-ylamine,

3-benzazolyl-2-methylsulfanyl-6,7-dihydro-5H-cyclopent[d]pyrazolo[1,5-a]pyrimidine-8-ylamine,

3-benzazolyl-5-isopropyl-2-methylsulfonylbenzoyl[1,5-a]pyrimidine-7-ylamine,

5-methyl-2-methylsulfanyl-3-(toluene-2-sulfonyl)pyrazolo[1,5-a]pyrimidine-7-ylamine,

5-methyl-2-methylsulfanyl-3-(toluene-3-sulfonyl)pyrazolo[1,5-a]pyrimidine-7-ylamine,

3-benzazolyl-5-methoxymethyl-2-methylsulfonylbenzoyl[1,5-a]pyrimidine-6-ylamine,

3-benzazolyl-N5, N5-dimethyl-2-methylsulfonylbenzoyl[1,5-a]pyrimidine-5,7-diamine,

3-benzazolyl-N5-(2-dimethylaminoethyl)-2-methylsulfinylphenyl[1,5-a]pyrimidine-5,7-diamine,

3-benzazolyl-5-(4-methylpiperazin-1-yl)-2-methylsulfinylphenyl[1,5-a]pyrimidine-7-ylamine and

3-benzazolyl-5-dimethylaminomethyl-2-methylsulfonylbenzoyl [1,5-a]pyrimidine-7-ylamine.

4. Compounds of General formula I on p. 1, where R3means piperazinil.

5. Connection under item 4 of the group, including

3-benzazolyl-5-methyl-2-methylsulfanyl-7-piperazine-1-alprazola[1,5-a]pyrimidine,

3-(4-tert-butylbenzenesulfonyl)-5-methyl-2-methylsulfanyl-7-piperazine-1-alprazola[1,5-a]pyrimidine,

3-benzazolyl-5,6-dimethyl-2-methylsulfanyl-7-piperazine-1-alprazola[1,5-a]pyrimidine,

3-benzolsulfonate-7-piperazine-1-alprazola[1,5-a]pyrimidine,

3-benzazolyl-2-methylsulfanyl-8-piperazine-1-yl-6,7-dihydro-5H-cyclopent[d]pyrazolo[1,5-a]pyrimidine,

3-benzazolyl-2-methylsulfanyl-8-piperazine-1-yl-5H,7H-pyrazolo[1,5-a]thieno[3,4-d]pyrimidine,

5-methyl-2-methylsulfanyl-7-piperazine-1-yl-3-(thiophene-2-sulfonyl)pyrazolo[1,5-a]pyrimidine,

3-benzazolyl-2-ethyl-8-piperazine-1-yl-6,7-dihydro-5H-cyclopent[d]pyrazolo[1,5-a]pyrimidine and

5-methyl-2-methylsulfanyl-7-piperazine-1-yl-3-(toluene-2-sulfonyl)pyrazolo[1,5-a] pyrimidine.

6. Compounds of General formula I on p. 1, where R3denotes methylpiperazine.

7. Connection on p. 6 of the group, including

3-benzazolyl-5-cyclopropyl-2-methylsulfanyl-7-(4-methylpiperazin-1-yl)pyrazolo[1,5-a]pyrimidine,

3-benzazolyl-8-(4-methylpiperazin-1-yl)-2-methylsulfanyl-6,7-dihydro-5H-cyclopent[d]pyrazolo[1,5-a]pyrimidine,

3-benzazolyl-8-(4-methylpiperazin-1-yl)-2-methylsulfanyl-5H, 7H-pyrazolo[1,5-a]thieno[3,4-d]pyrimidine,

3-benzazolyl-5-isopropyl-7-(4-methylpiperazin-1-yl)-2-methylsulfinylphenyl[1,5-a]pyrimidine and

2-[3-benzazolyl-7-(4-methylpiperazin-1-yl)-2-methylsulfinylphenyl[1,5-a]pyrimidine-5-yloxy]ethanol.

8. Compounds of General formula I on p. 1, where R3denotes the amino group or methylpiperazine.<-ylamine and 8-benzazolyl-2-methyl-4-(4-methylpiperazin-1-yl)-7-methylsulfonylmethane[1,5-a][1,3,5]triazine.

10. Compounds of General formula I according to any one of paragraphs.1-9, with selective affinity to T6-receptors.

11. Drug with selective affinity to T6receptors containing the compound according to any one of paragraphs.1-9 and a therapeutically inert carrier.

 

Same patents:

The invention relates to tetrahydro-gamma carbolines formula (I), where R1, R2D, Alk and n are such as defined in the claims

-converting enzyme)" target="_blank">

The invention relates to novel ortho-sulfonamidophenylhydrazine heteroaryl hydroxamic acids of the formula

< / BR>
where W and X are both carbon, T is nitrogen, U represents CR1where R1represents hydrogen, or alkyl containing 1-8 carbon atoms, R represents-N(CH2R5)-SO2Z, Q represents -(C=O)-NHOH, with

< / BR>
is a benzene ring, or is a heteroaryl ring of 5 to 6 atoms in the cycle, which may contain 0-2 heteroatoms selected from nitrogen, oxygen and sulfur, in addition to the heteroatom of nitrogen, denoted as W, where benzene or heteroaryl ring may optionally contain one or two substituent R1where permissible; Z is phenyl, which is optionally substituted by phenyl, alkyl with 1-8 carbon atoms, or a group OR2; R1represents halogen, alkyl with 1-8 carbon atoms, alkenyl with 2-6 carbon atoms, perfluoroalkyl from 1 to 4 carbon atoms, phenyl, optionally substituted by 1-2 groups OR2group-NO2group -(CH2)nZ, where Z is a phenyl which allows an alkyl with 1-8 carbon atoms, phenyl, optionally substituted with halogen, or heteroaryl radical containing 5 to 6 atoms in the cycle, including 1-2 heteroatoms selected from nitrogen, oxygen and sulfur; R5represents hydrogen, alkyl with 1-8 carbon atoms, phenyl, or heteroaryl containing 5 to 6 atoms in the cycle, including 1-2 heteroatoms selected from nitrogen, oxygen and sulfur; or their pharmaceutically acceptable salts

The invention relates to new compounds having formula I or formula II:

< / BR>
< / BR>
where R1represents H, lower alkylthio or R1together with R2form a-CH2-; each of R2and R3independently represents H or lower alkyl; R4represents Oh or H2; R5is H, unsubstituted lower alkyl, cyclohexyl - lower alkyl; each of R6and R7independently represents hydrogen, phenyl, naphthyl, -C(O)-NHCHR13CO2R14or substituted phenyl, where the Deputy represents halogen, lower alkyl, lower alkoxy, hydroxy, or phenyl - lower alkoxy; R8represents H or lower alkyl; R9represents H or lower alkyl; R12is NR9or S; R13is lower alkylthio; R14represents H or lower alkyl; or their pharmaceutically acceptable salts, with the exception of 4,5-bis(4-methoxyphenyl)-2-(4-thiazolidinediones)thiazole and its hydrochloride

The invention relates to sulfonamidnuyu to the compound of formula I, where R1- alkyl, alkenyl, quinil; a represents optionally substituted heterocyclic group, excluding benzimidazolyl, indolyl, 4,7-dehydrobenzperidol and 2,3-dihydrobenzofuranyl; X - alkylene, oxa, oxa(lower) alkylene; R2- optional substituted aryl, substituted biphenyl, its salts and pharmaceutical compositions comprising this compound

The invention relates to new derivatives of 4-oxo-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-ndimethylacetamide formula I

< / BR>
where X= H, halogen, methyl, methoxy, phenylmethoxy-; Y Is H, 1 or 2 halogen atom, HE, CH3OH, NO2-, CH3; R1-H, C1-C4alkyl; R2and R3each, independently of one another, is H, C1-C4alkyl, phenylmethylene group, or R2and R3form together with the nitrogen atom which carries them, azetidinone, pyrrolidinyloxy, 3-ethoxypyrrolidine, piperidinyloxy, morpholinyl, 4-methylpiperidino or 1,3-thiazolidinedione group

The invention relates to a new pyrimido[5,4-d]pyrimidines of General formula I and medicines with the properties of an inhibitor of protein tyrosine kinase receptors of epidermal growth factor on the basis of their

The invention relates to the class of heterocyclic metallocenes and containing catalytic systems, as well as the method of polymerization joining the polymerized monomers using a given catalytic system, and these heterocyclic metallocene correspond to the formula (I), YjRiZjjMeQkP1,

where Y represents a coordinating group containing the Central radical with six-electrons, directly coordinating IU, which condensed one or more rings containing at least one atom that is not carbon atom and is selected from S; R" represents a divalent bridging communication between the groups Y and Z; Z is a coordinating group having the same meaning as Y; Me represents a transition metal of group 3, 4, 5, 6; Q is halogen or linear or branched C1-C6-alkyl; R represents a counterion; i=0 or 1; j=1-3; jj=0-2; k=1-3 and 1= 0-2

The invention relates to compounds of formula (I)

< / BR>
where R(2) and R(3) independently from each other denote hydrogen, Cl, Br, J, (C1-C8)-alkyl, (C3-C8-cycloalkyl or(5), R(5) - (C1-C8)-alkyl, and one of the two substituents R(2) and R(3) is always hydrogen, however, both Deputy R(2) and R(3) at the same time are not hydrogens, as well as their pharmaceutically acceptable salts

The invention relates to medicine, namely to create drugs with complex medical and preventive action, and for the composition for the prevention of atherosclerosis, cardiovascular disease and maintenance therapy of viral diseases

The invention relates to medicine, namely to create drugs with complex medical and preventive action, and for the composition for the prevention of atherosclerosis, cardiovascular disease and maintenance therapy of viral diseases

The invention relates to 5-[4-(6-methoxy-1-methyl-1H-benzimidazole-2-ylethoxy)benzyl] thiazolidin-2,4-dione hydrochloride

The invention relates to new orthotamine benzoylpyridine formula (1), where R(1) - H, alkyl with 1-8 C-atoms, Xand-(CH2)b-(CF2)c-CF3where a, b, C = 0; one of the two substituents R(2) and R(3) means-O-CO-R(27), respectively, and the other substituents R(2) and R(3) is R(1) where R(27) - alkyl with 1-8 C-atoms; R(4) is hydrogen, alkoxy with 1-4 C-atoms, F, Cl, Br, I; R(5) is hydrogen, and their pharmaceutically acceptable salts

The invention relates to medicine, namely to homeopathic, treatment and prevention tools for internal and external use, has tonic, anti-inflammatory, wound healing, detoxifying, anti-microbial, antianginal, anti-atherosclerotic, antioxidant, antihypoxic, neuroprotective, sedative, cardioprotective, anti-arrhythmic, angioprotective, stress-protective, immunotropic, antifungal, nephroprotective, hepatoprotective, gastroprotective, thermoprotector, lipoic, megaproducer, radioprotective, and retinoprotective anticoordination action

The invention relates to the field of medicine and relates to an infusion solution for improving cerebral circulation

The invention relates to novel ortho-substituted benzoylpyridine formula (1), where R(1) denotes H, halogen, Xand-(CH2)b-(CF2)with-CF3, a, b, C denote the zero, one of the two substituents R(2) and R(3) denotes hydroxyl, and the other of the substituents R(2) and R(3) is R(1), R(4) denotes a1-C4-alkyl, halogen, (CH2)n-(CF2)o-CF3n, mean zero, and their pharmaceutically acceptable salts
The invention relates to medicine, namely to intensive cardiology, and for the treatment of myocardial infarction
Up!