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CYCLIC AMIDE DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE AND USES THEREOF
专利权人:
KONEKSHIS LAJF SAJENSIZ PVT. LTD.
发明人:
RAO Dzhagannat Madanakhalli Ranganat (IN),РАО Джаганнат Маданахалли Ранганат (IN),VENKATESHAM Uppala (IN),ВЕНКАТЕШАМ Уппала (IN),DZHORDZH Dzhenson (IN),ДЖОРДЖ Дженсон (IN),FERNAND Dzhordzh (IN),ФЕРНАН
申请号:
RU2014126646
公开号:
RU0002669695C2
申请日:
2012.12.21
申请国别(地区):
RU
年份:
2018
代理人:
摘要:
FIELD: chemistry.SUBSTANCE: invention relates to the field of organic chemistry, specifically to a heterocyclic compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein each R1 and R1a is independently selected from the group consisting of H, methyl, CONHC(CH3)3, OH, CO2H, CO2CH3, CO2CH2CH3, CH2OH, CN, OCH3 and phenyl; or R1 represents CH2CO2H; or any two R1 on the same carbon atom when taken together may form a group of the formula =O; Ar is a heteroaryl group selected from the group consisting of:,where each R7 is independently selected from the group consisting of halogen, OH, CN, C1-C3 alkyl, C1-C3 alkoxy, C3cycloalkyl, heterocycloalkyl selected from piperidine which may be substituted with one carboxyl group; C6aryl, which may be substituted by one halogen atom; heteroaryl, selected from the group consisting of thiophene, furan, which may be substituted with C1-C3alkyl, and pyridine; wherein R8 is selected from the group consisting of H, C1-C2alkyl, C1alkoxy, C3cycloalkyl and SO2R9; wherein R9 is C6aryl; e is an integer selected from a group consisting of 0, 1 and 2; f is an integer selected from a group consisting of 0 and 1; A is -CRaRb-; B is CH2; wherein each Ra and Rb is independently selected from the group consisting of H, OH, CN, CF3, C1-C3alkyl, C6aryl, heteroaryl selected from thiophene; and wherein Ra and Rb are different; W1 and W2 are selected such that one is N and the other is (CR12); bond from the carbonyl carbon is joined to W1 or W2, which is N; D is O or (CR12); a is an integer selected from a group consisting of 0, 1 and 2; b is an integer selected from a group consisting of 0 and 1; c is equal to 1. Invention also relates to the pharmaceutical composition based on compound with formula (I) and use of compound with formula (I). .EFFECT: novel heterocyclic compounds having the ability to inhibit 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1).12 cl, 1 tbl, 268 exИзобретение относится к области органической химии, а
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