NEW INHIBITORS OF ALPHA AND BETA MEPRIN Russian patent published in 2021 - IPC C07C259/06 C07D207/16 C07D213/36 C07D317/58 C07D317/64 C07D319/18 A61K31/16 A61K31/36 A61P1/04 A61P11/00 A61P13/00 A61P17/02 A61P25/28 A61P29/00 A61P35/00 

Abstract RU 2746850 C2

FIELD: chemistry.

SUBSTANCE: invention relates to compounds following the formula I below or to pharmaceutically acceptable salts thereof which are inhibitors of beta and/or alpha meprin. In the formula I n = 1–3; R1 is selected from the group consisting of C6-8 arylmethyl and C6-8heteroarylmethyl, wherein each of them may optionally be substituted with 1-3 substituents independently selected from the group consisting of -OH, -C(O)-NH2, cyano, -COOH, -C(O)-O-C1-4alkyl), halogen, C1-6alkoxy, fluoro(C1-6alkoxy), wherein two adjacent alkoxy substituents can be connected to form a part of a 5-8-membered heterocycle, wherein 1, 2 or 3 ring atoms are substituted in said 5-8-membered heterocycle and said C6-8-heteroaryl by heteroatoms selected from N, S and O; R3 and R4 are H; R2 is selected from the group consisting of C6-8aryl, C6-8heteroaryl, wherein said C6-8aryl is additionally substituted with 1-3 substituents independently selected from the group consisting of -OH, -C(O)-NH2, cyano, -COOH, -C(O)-O-(C1-4alkyl), halogen, C1-6alkoxy, fluoro(C1-6alkoxy), C6-8aryl, wherein two adjacent alkoxy substituents can be connected to form a part of a 5-8-membered heterocycle and wherein 1, 2 or 3 ring atoms are substituted in said C6-8heteroaryle with heteroatoms selected from N, S and O; X is -CH2-. Invention also relates to a pharmaceutical composition and a method for treatment or prevention of a disease or a pathological condition mediated by inhibition of beta and/or alpha meprin using said compounds.

EFFECT: new inhibitors of alpha and beta meprin and use thereof in medical treatment.

11 cl, 3 tbl, 74 ex

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RU 2 746 850 C2

Authors

Wermann, Michael

Buchholz, Mirko

Demuth, Hans-Ulrich

Ramsbeck, Daniel

Schlenzig, Dagmar

Schilling, Stephan

Dates

2021-04-21Published

2017-04-18Filed