Novel condensed pyrrole derivatives

IPC classes for russian patent Novel condensed pyrrole derivatives (RU 2434853):

C07D495/04 - Ortho-condensed systems

C07D493/04 - Ortho-condensed systems

C07D471/04 - Ortho-condensed systems

C07D413/06 - linked by a carbon chain containing only aliphatic carbon atoms

C07D409/06 - linked by a carbon chain containing only aliphatic carbon atoms

C07D407/06 - linked by a carbon chain containing only aliphatic carbon atoms

C07D403/06 - linked by a carbon chain containing only aliphatic carbon atoms

C07D401/06 - linked by a carbon chain containing only aliphatic carbon atoms

C07D209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

A61P29 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; Non-steroidal antiinflammatory drugs (NSAIDs)

A61K31/437 -

A61K31/407 -

A61K31/404 -

A61K31/4025 -

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FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (1) (lb) in which A denotes a benzene ring; Ar denotes naphthalenyl which optionally contains 1-3 substitutes independently selected from a group comprising C₁-C₆alkyl, C₃-C₇cycloalkyl, C₃-C₇cycloalkyl-C₁-C₆alkyl, C₂-C₆alkenyl, C₂-C₆alkynyl, hydroxy group, C₁-C₆alkoxy group, halogen, heteroalkyl, heteroalkoxy group, nitro group, cyano group, amino- and mono- or di- C₁-C₆alkyl-substuted amino group; R¹ denotes hydrogen, halogen, C₁-C₆alkyl, C₁-C₆alkoxy group, carboxy group, heteroalkyl, hydroxy group optionally substituted with heterocyclylcarbonyl-C₁-C₆alkyl or R¹ denotes N(R')(R")-C₁-C₆alkyl or N(R')(R")-carbonyl- C₁-C₆alkyl-, in which R' and R" are independently selected from a group comprising hydrogen, C₁-C₆alkyl, C₃-C₇cycloalkyl, C₃-C₇cycloalkyl-C₁-C₆alkyl, heteroalkyl, phenyl-C₁-C₆alkyl; or R¹ denotes R'-CO-N(R")-C₁-C₆alkyl, R'-O-CO-N(R^")- C₁-C₆alkyl- or R'-SO₂-N(R")- C₁-C₆alkyl-, in which R' and R" are independently selected from a group comprising hydrogen, C₁-C₆alkyl, C₃-C₇cyclalkyl, C₃-C₇cycloalkyl- C₁-C₆alkyl or optionally substituted phenyl; R², R^2' and R^2" independently denote hydrogen, halogen, cyano group, C₁-C₆alkyl, halogenated C₁-C₆alkyl or C₁-C₆alkoxy group; n equals 1; and pharmaceutically acceptable salts thereof. The invention also relates to use of compounds in any of claims 1-9, as well as to a pharmaceutical composition.

EFFECT: obtaining novel biologically active compounds with chymase inhibiting activity.

14 cl, 128 ex

The text descriptions are given in facsimile form.

1. The compounds of formula (I)

where And denotes a benzene ring;
AG indicates naphthalenyl, which optionally contains 1-3 substituent, independently selected from the group comprising C₁-C₆alkyl, C₃-C₇cycloalkyl,₃-C 7cycloalkyl-C₁-C₆alkyl, C₂-C₆alkenyl, C₂-C₆quinil, the hydroxy-group, C₁-C₆alkoxygroup, halogen, heteroalkyl, heteroalkyl, a nitrogroup, cyano, amino and mono - or di-C₁-C₆alkyl substituted an amino group;
R¹denotes hydrogen, halogen, C₁-C₆alkyl, C₁-C₆alkoxygroup, carboxypropyl, heteroalkyl, the hydroxy-group, optionally substituted heterocalixarenes-C₁-C₆alkyl, or
R¹denotes N(R')(R")-C₁-C₆alkyl - or N(R')(R")-carbonyl-C₁-C₆alkyl-, in which R' and R" are independently selected from the group comprising hydrogen, C₁-C₆alkyl, C₃-C₇cycloalkyl,₃-C₇cycloalkyl-C₁-C₆alkyl, heteroalkyl, phenyl-C₁-C₆alkyl; or
R¹denotes R'-CO-N(R")-C₁-C₆alkyl-, R'-O-CO-N(R")-C₁-C₆alkyl - or R'-SO₂-N(R")-C₁-C₆alkyl-, in which R' and R" are independently selected from the group comprising hydrogen, C₁-C₆alkyl, C₃-C₇cycloalkyl,₃-C₇cycloalkyl-C₁-C₆alkyl or optionally substituted phenyl;
R², R^2'and R^2"independently represent hydrogen, halogen, cyano, C₁-C₆alkyl, halogenated C₁-C₆alkiline C ₁-C₆alkoxygroup;
n = 1;
and their pharmaceutically acceptable salts;
in which, if not given a different definition,
the term "heteroalkyl" means C₁-C₆alkyl containing one or more substituents independently selected from the group comprising a hydroxy-group, halogen, C₁-C₆alkoxygroup, formyl, C₁-C₆alkylsulphonyl, carboxypropyl, carbarnoyl, amino and mono - or di-C₁-C₆alkyl substituted an amino group;
the term "heterocyclyl" means a non-aromatic monocyclic radicals containing from 3 to 8 atoms, in which 1 or 2 atoms of the ring are heteroatoms selected from the group comprising N, O and S(O)_n(where n is a whole number equal to from 0 to 2), the remaining ring atoms are atoms With;
the term "optionally substituted phenyl and optionally substituted heterocyclyl" means, respectively, phenyl and heterocyclyl, optionally containing one or more substituents independently selected from the group comprising halogen, C₁-C₆alkyl, hydroxy-group and C₁-C₆alkoxygroup.

2. Compounds according to claim 1,
in which R¹denotes hydrogen, halogen, C₁-C₆alkyl, C₁-C₆alkoxygroup, carboxypropyl, the hydroxy-group, optionally substituted heterocyclic ronil-C ₁-C₆alkyl, or
R¹denotes N(R')(R")-C₁-C₆alkyl - or N(R')(R")-carbonyl-C₁-C₆alkyl-, in which R' and R" are independently selected from the group comprising hydrogen, C₁-C₆alkyl, C₃-C₇cycloalkyl,₃-C₇cycloalkyl-C₁-C₆alkyl, heteroalkyl, phenyl-C₁-C₆alkyl; or
R¹denotes R'-O-CO-N(R")-C₁-C₆alkyl - or R'-SO₂-N(R")-C₁-C₆alkyl-, in which R' and R" are independently selected from the group comprising hydrogen, C₁-C₆alkyl, C₃-C₇cycloalkyl,₃-C₇cycloalkyl-C₁-C₆alkyl or optionally substituted phenyl.

3. Compounds according to claim 1 or 2, in which Ar denotes naphthalenyl, which optionally contains 1-3 substituent, independently selected from the group comprising C₁-C₆alkyl, C₁-C₆alkoxygroup and halogen.

4. Compounds according to claim 1 or 2, in which R' denotes hydrogen, halogen, C₁-C₆alkyl, C₁-C₆alkoxygroup, carboxypropyl, optionally substituted heterocalixarenes-C₁-C₆alkyl or heteroalkyl, or
R¹denotes N(R')(R")-(C₁-C₆alkylene)- or N(R')(R")-carbonyl-C₁-C₆alkyl-, in which R' and R" are independently selected from the group comprising hydrogen, C₁-C₆alkyl, heteroalkyl, obazatelno substituted phenyl-C ₁-C₆alkyl.

5. Compounds according to claim 1 or 2, in which R¹denotes hydrogen, C₁-C₆alkyl, carboxypropyl or N(R')(R")-carbonyl-C₁-C₆alkyl-, in which R' and R" are independently selected from the group comprising hydrogen and C₁-C₆alkyl.

6. Compounds according to claim 1 or 2, in which one of R², R^2'and R^2"denotes hydrogen and the other two independently represent hydrogen, halogen, C₁-C₆alkyl, halogenated₁-C₆alkyl or C₁-C₆alkoxygroup.

7. Compounds according to claim 1 or 2, in which two of R², R^2'and R^2"denote hydrogen, and the remainder represents a hydrogen or halogen.

8. The compound according to claim 1 or 2, which is
3-methyl-1-naphthalene-1-ylmethyl-1H-indole-2-carboxylic acid,
3-carboxymethyl-5-fluoro-1-naphthalene-1-ylmethyl-1H-indole-2-carboxylic acid,
3-dimethylcarbamoyl-5-fluoro-1-naphthalene-1-ylmethyl-1H-indole-2-carboxylic acid,
1-(7-fornatale-1-ylmethyl)-1H-indole-2-carboxylic acid,
1-(8-methylnaphthalene-2-ylmethyl)-1H-indole-2-carboxylic acid.

9. The compound according to claim 1 or 2, which is 5-fluoro-3-(methoxycarbonylaminophenyl)-1-naphthalene-1-ylmethyl-1H-indole-2-carboxylic acid,
5-fluoro-3-(methanesulfonylaminoethyl)-1-naphthalene-1-ylmethyl-1H-indole-2-carboxylic acid,
5-fluoro-3-[(methoxycarbonylmethylene)-methyl]-1-naphthalene-1-yl is ethyl-1H-indole-2-carboxylic acid,
3-[(ethoxycarbonylmethylene)-methyl]-5-fluoro-1-naphthalene-1-ylmethyl-1H-indole-2-carboxylic acid,
5-fluoro-3-[(methysulfonylmethane)-methyl]-1-naphthalene-1-ylmethyl-1H-indole-2-carboxylic acid,
3-[(telmatogetoninae)-methyl]-5-fluoro-1-naphthalene-1-ylmethyl-1H-indole-2-carboxylic acid,
3-ethoxymethyl-5-fluoro-1-naphthalene-1-ylmethyl-1H-indole-2-carboxylic acid,
3-dimethylcarbamoyl-5-fluoro-1-(7-fornatale-1-ylmethyl)-1H-indole-2-carboxylic acid,
5-chloro-1-(7-fornatale-1-ylmethyl)-1H-indole-2-carboxylic acid,
1-(7-fornatale-1-ylmethyl)-5-methyl-1H-indole-2-carboxylic acid,
1-(7-fornatale-1-ylmethyl)-4-methoxy-1H-indole-2-carboxylic acid,
3-dimethylcarbamoyl-1-(7-fornatale-1-ylmethyl)-1H-indole-2-carboxylic acid,
1-(7-fornatale-1-ylmethyl)-3-(methoxycarbonylaminophenyl)-1H-indole-2-carboxylic acid,
1-(7-fornatale-1-ylmethyl)-3-(methanesulfonylaminoethyl)-1H-indole-2-carboxylic acid,
1-(7-fornatale-1-ylmethyl)-3-[(methoxycarbonylmethylene)-methyl]-1H-indole-2-carboxylic acid,
3-[(ethoxycarbonylmethylene)-methyl]-1-(7-fornatale-1-ylmethyl)-1H-indole-2-carboxylic acid,
1-(7-fornatale-1-ylmethyl)-3-[(methysulfonylmethane)-methyl]-1H-indole-2-carboxylic acid,
5-fluoro-1-(7-fornatale-1-ylmethyl)-3-(methoxycarbonylaminophenyl)-1H-indole-2-carboxylic acid,
5-fluoro-1-(7-fornatale-1-ylmethyl)--(methanesulfonylaminoethyl)-1H-indole-2-carboxylic acid,
5-fluoro-1-(7-fornatale-1-ylmethyl)-3-[(methoxycarbonylmethylene)-methyl]-1H-indole-2-carboxylic acid,
3-[(ethoxycarbonylmethylene)-methyl]-5-fluoro-1-(7-fornatale-1-ylmethyl)-1H-indole-2-carboxylic acid,
5-fluoro-1-(7-fornatale-1-ylmethyl)-3-[(methysulfonylmethane)-methyl]-1H-indole-2-carboxylic acid.

10. Compounds according to claim 1 or 2, intended for use as therapeutically active substances, inhibiting himizu.

11. Compounds according to claim 1 or 2, intended for use as therapeutically active substances for the treatment and/or prevention of allergic, inflammatory or fibrotic diseases.

12. The use of compounds according to any one of claims 1 to 9 for the preparation of medicinal products intended for therapeutic and/or prophylactic treatment of allergic, inflammatory or fibrotic diseases.

13. The application indicated in paragraph 12, in which the disease is Allergy, asthma, occlusive peripheral artery disease, critical limb ischemia, unstable atherosclerotic plaque patients, unstable angina, congestive heart failure, left ventricular hypertrophy, ischemic reperfusion lesion, stroke, cardiomyopathy, restenosis, rheumatoid arthritis, diabetic nephropathy, touchy thick the second colon, Crohn's disease, atherothrombosis and/or burns/ulcers in diabetes/KICK (critical limb ischemia).

14. Pharmaceutical composition having activity inhibitors himas comprising the compound according to any one of claims 1 to 9 and a pharmaceutically acceptable excipient.