首页> 外国专利> Antidiabetic oxazolidinediones and thiazolidinediones as agonists or partial agonists of PPAR gamma

Antidiabetic oxazolidinediones and thiazolidinediones as agonists or partial agonists of PPAR gamma

机译:抗糖尿病的恶唑烷二酮和噻唑烷二酮作为PPARγ的激动剂或部分激动剂

摘要

Disclosed is a compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: A is O or S; X is a bond or CH2; R1 is selected from the group consisting of H and C1-C3 alkyl, wherein C1-C3 alkyl is optionally substituted with 1-3 F; Each R2 is independently selected from the group consisting of F, Cl, CH3, CF3, -OCH3, and -OCF3; Each R4 is independently selected from the group consisting of halogen, C1-C3 alkyl, -OC1-C3 alkyl, -OC(=O)C1-C3 alkyl, and -S(O)qC1-C3 alkyl, wherein C1-C3 alkyl, -OC1-C3 alkyl, -OC(=O)C1-C3 alkyl, and -S(O)qC1-C3 alkyl are optionally substituted with 1-3 F; Each R5 is independently selected from the group consisting of F, Cl, CH3, -OCH3, CF3, and -OCF3; R6 is selected from the group consisting of C2-C5 alkyl, -CH2Cyclopropyl, and -C(=O)C1-C3 alkyl, wherein said R6 substituent is optionally substituted with 1-3 F; m is 0 or 1; n is an integer from 1-3; P is an integer from 0-2; and q is an integer from 0-2. Also disclosed is a pharmaceutical composition comprising of the said compound, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, and additionally, the use of the said compound or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of Type 2 diabetes is also disclosed.
机译:公开了式I的化合物:或其药学上可接受的盐,其中:A为O或S; X是键或CH 2; R1选自H和C1-C3烷基,其中C1-C3烷基任选被1-3个F取代;每个R 2独立地选自F,Cl,CH 3,CF 3,-OCH 3和-OCF 3;每个R 4独立地选自卤素,C 1 -C 3烷基,-OC 1 -C 3烷基,-OC(= O)C 1 -C 3烷基和-S(O)q C 1 -C 3烷基,其中C 1 -C 3烷基,-OC1-C3烷基,-OC(= O)C1-C3烷基和-S(O)qC1-C3烷基任选被1-3个F取代;每个R 5独立地选自F,Cl,CH 3,-OCH 3,CF 3和-OCF 3; R6选自由C2-C5烷基,-CH2环丙基和-C(= O)C1-C3烷基组成的组,其中所述R6取代基任选被1-3个F取代; m为0或1; n是1-3的整数; P是0-2的整数; q是0到2的整数。还公开了包含所述化合物或其药学上可接受的盐和药学上可接受的载体的药物组合物,另外,所述化合物或其药学上可接受的盐在制备用于治疗糖尿病的药物中的用途。还公开了2型糖尿病。

著录项

  • 公开/公告号NZ548556A

    专利类型

  • 公开/公告日2009-03-31

    原文格式PDF

  • 申请/专利权人 MERCK & CO. INC.;

    申请/专利号NZ20050548556

  • 申请日2005-01-18

  • 分类号C07D263/44;C07D277/34;A61K31/421;A61K31/426;A61P3/10;

  • 国家 NZ

  • 入库时间 2022-08-21 19:26:05

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