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Novel condensed pyrrole derivatives

Novel condensed pyrrole derivatives
IPC classes for russian patent Novel condensed pyrrole derivatives (RU 2434853):
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Dibenzylidene sorbitol (dbs) based compounds, composition and method of using said compounds Dibenzylidene sorbitol (dbs) based compounds, composition and method of using said compounds / 2401271
Invention relates to novel dibenzylidene sorbitol (DBS) compounds of formula 1: , in which R1 and R2 are independently selected from a group consisting of CH3CH2CH2- and CH3CH2CH2O-; and in which R3 is independently selected from -CH2CH2CH3 and -CH2-CH=CH2 groups. According to one version, this invention pertains to a disubstituted DBS based compound having an allyl or propyl group as a substitute at the first carbon atom in the sorbitol chain. The present invention also relates to compositions containing such DBS based compounds and preparation methods thereof.
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Heterocyclic janus kinase 3 inhibitors Heterocyclic janus kinase 3 inhibitors / 2434013
Invention relates to a compound of formula (I), in which X denotes N or CR3, M denotes (CH2)m; m equals 0 or 1, R1 denotes H or lower alkyl which can be substituted with a group selected from a group consisting of mono- or di-lower alkylamino and -O-lower alkyl, R2 denotes H or lower alkyl, R3 denotes H or lower alkyl substituted with a group selected from a group consisting of halogen, mono- or di-lower alkylamino and cyclic amino, R41 denotes H or pyridine which can be substituted with a cyano group, R42 denotes a bridged polycyclic hydrocarbon or a bridged azacyclic hydrocarbon, each of which can be substituted, R5 denotes a group selected from a group consisting of halogen, cyano, lower alkyl-carbonyl, lower alkyl-oxycarbonyl, hydroxycarbonyl, formyl, amidinooxycarbonyl, guanidinooxycarbonyl, guanidino, carbamoyl, -C(=O)-5- or -6-member heterocycloalkyl, -C(=O)-5- or -6-member heteroaryl, lower alkyl, lower alkenyl, -O-lower alkyl, 5- or 6-member heterocycloalkyl and 5-member heteroaryl, each of which can be substituted, provided that when R5 denotes a 5-member heteroaryl, X denotes -CR3; or R41 and R15 can be bonded through a defined functional group to form divalent groups shown below: (I-A) (I-B) or (I-C), in which RA denotes H or acyl, which can be substituted, provided that the term "substituted" with respect to R4 and/or R5 denotes substitution with one or more substitutes selected from a group comprising the following substitutes: (a). halogen; (b) -OH, -O-R2, -O-phenyl, -OCO-RZ-OCONH-RZ oxo (=O); (c) -SH, -S-R2, -S-phenyl, -S-heteroaryl, -SO-R2, -SO-phenyl, -SO-heteroaryl, -SO3H, -SO2-RZ, -SO2-phenyl, - SO2-heteroaryl, sulphamoyl, which can be substituted with one or two RZ groups; (d) amino, which can be substituted with one or two RZ groups, -NHCO-RZ, -NHCO-phenyl, -NHCO2-RZ, -NHCONH2, -NHCONH-RZ, -NHSO2-R0, -NHSO2-phenyl, -NHSO2NH2, -NO2, =N-O-RZ; (e) -CHO, -CO-RZ, -CO2H, -CO2-RZ, carbamoyl, which can be substituted with one or two RZ groups, -CO-cyclic amino, -COCO-RZ, cyano; (f) RZ; (g) phenyl, which can be substituted with one or more groups selected from substitutes described above in paragraphs from (a) to (f), a 5- or 6-member heterocycloalkyl, a 5- or 6-member heteroaryl, a 5- or 6-member heterocycloaryl; or pharmaceutically acceptable salts thereof. The invention also relates to a method of producing compounds of formula II, a pharmaceutical composition based on said compounds which is a Janus kinase 3 inhibitor, a method of treating and/or preventing different immunopathological diseases, including autoimmune diseases, inflammatory diseases and allergic diseases.

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, R2' and R2" 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, R2'and R2"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, R2'and R2"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, R2'and R2"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.

 

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