NEW BICYCLIC COMPOUNDS AS DUAL INHIBITORS OF ATX/CA Russian patent published in 2020 - IPC C07D471/04 C07D487/04 A61K31/407 A61K31/437 A61P27/02 

Abstract RU 2724899 C2

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to a compound of formula (I)

(I)

and pharmaceutically acceptable salts thereof. In formula (I): R1 represents substituted phenyl-C1-6-alkyl substituted by phenoxy-C1-6-alkyl, substituted phenyl-C2-6-alkenyl, substituted quinolinyl, substituted quinolinyl-C1-6-alkyl, substituted quinolinyl-C1-6-alkenyl, substituted quinolinyl-C1-6-alkynyl, substituted pyridinyl, substituted pyridinyl-C1-6-alkyl, where substituted phenyl-C1-6-alkyl, substituted phenoxy-C1-6-alkyl, substituted phenyl-C2-6-alkenyl, substituted quinolinyl, substituted quinolinyl-C1-6-alkyl, substituted quinolinyl-C1-6-alkenyl, substituted quinolinyl-C1-6-alkynyl, substituted pyridinyl, substituted pyridinyl-C1-6-alkyl, substituted by R3, R4 and R5; Y is -OC(O)- or -C(O)-; W is -C(O)-, -S(O)2-; R2 denotes substituted phenyl, substituted pyridinyl, where substituted phenyl, substituted pyridinyl is substituted by R6, R7 and R8; R3 represents halogen, cyano, C1-6-alkyl, halogen-C1-6-alkoxy, halogen-C1-6-alkyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl, C1-6-alkilkarbonilamino, C1-6-alkiltetrazolyl, C1-6-alkiltetrazolyl-C1-6-alkyl or (heterocycloalkyl, containing 1 heteroatom selected from N and O)-C1-6-alkoxy; R4 and R5 are independently selected from H, halogen, cyano, C1-6-alkyl, halogen-C1-6-alkoxy, halogen-C1-6-alkyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl, C1-6-alkylcarbonylamino, C1-6-alkiltetrazolyl, C1-6-alkiltetrazolyl-C1-6-alkyl and (heterocycloalkyl containing one heteroatom selected from N and O)-C1-6-alkoxy; R6 is aminosulphonyl; R7 and R8 are independently selected from H, halogen; m, n, p and q are independently selected from 1 or 2. Also disclosed are a pharmaceutical composition, use of the compound and a method of inhibiting autotaxin and carbonic anhydrase.

EFFECT: disclosed compounds have the effect of a double inhibitor of autotaxin (ATX) / carbonic anhydrase and can be used for treating or preventing diseases, disorders or conditions, which are associated with autotaxin activity and/or biological activity of lysophosphatidic acid (LPA).

31 cl, 7 ex

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RU 2 724 899 C2

Authors

Di Dzhordzho Patrik

Khert Zherom

Khuntsiker Daniel

Mattej Patritsio

Rudolf Markus

Shmits Petra

Ullmer Kristof

Dates

2020-06-26Published

2016-09-21Filed