首页> 外国专利> OX(ADI)AZOLYL-HYDROXAMIC ACIDS USEFUL AS PROCOLLAGEN C-PROTEINASE INHIBITORS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

OX(ADI)AZOLYL-HYDROXAMIC ACIDS USEFUL AS PROCOLLAGEN C-PROTEINASE INHIBITORS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

机译:用作胶原蛋白C蛋白酶抑制剂的OX(ADI)氮唑基羟基酸,其制备方法和包含它们的药物组合物

摘要

SUMMARY OF THE INVENTION The present invention relates to pharmaceutically acceptable salts and solvates of the compounds of formula (I), including hydrates thereof, and their prodrugs, wherein X is an optionally substituted C 1-6 alkylene or C 2-6 alkenylene, R is optionally substituted aryl or 3 -8 carbon atoms cycloalkyl, W is N or CZ, Y and Z are independently H, optionally substituted 1-4 carbon atoms, C 1-4 alkanoyl, C 1-4 alkoxycarbonyl, or CONR 1 R 2, R 1 and R 2 independently of one another two or two further heteroatoms selected from N, O, independently selected from H, C 3-8 cycloalkyl, optionally substituted C 1-4 alkyl, or R 1 and R 2 together with the nitrogen to which they are attached. and S atoms, which is a heterocyclic ring optionally having a benzo or pyrido group condensed or optionally substituted, R3 and R4 independently of one another are H, or optionally substituted 1-4 carbon atoms, or C1-4alkoxycarbonyl, or R3 and R4 taken together with the nitrogen atom to which they are attached form a single-morpholine, piperidine, azetidine- or piperazine ring optionally substituted with C 1-4 alkyl, R 5 is optionally substituted 1-4 carbon atoms, or may be aryl, R 6 is optionally substituted C 1-4 alkyl, or aryl, R 7 is H or R6, p is 0.1 or 2. The compounds of the invention have procollagen C proteinase (PCP) inhibitory activity. The invention also relates to the preparation of compounds and pharmaceutical compositions containing them. HE
机译:发明概述本发明涉及式(I)化合物的药学上可接受的盐和溶剂化物,包括其水合物,以及它们的前药,其中X是任选取代的C 1-6亚烷基或C 2-6亚烯基,R是任选取代的芳基或3 -8个碳原子的环烷基,W是N或CZ,Y和Z独立地是H,任选取代的1-4个碳原子,C 1-4烷酰基,C 1-4烷氧羰基或CONR 1 R 2 ,R 1和R 2彼此独立地选自N,O,独立地选自H,C 3-8环烷基,任选取代的C 1-4烷基或R 1和R 2的两个或两个其他杂原子以及氮它们所附着的。和S原子,其为任选具有稠合或任选取代的苯并或吡啶基的杂环,R 3和R 4彼此独立地为H,或任选取代的1-4个碳原子,或C 1-4烷氧羰基,或R 3和R 4 R 5与它们所连接的氮原子一起形成任选被C 1-4烷基取代的单吗啉,哌啶,氮杂环丁烷或哌嗪环,R 5是任选取代的1-4个碳原子,或可以是芳基,R 6 R 7是任选取代的C 1-4烷基或芳基,R 7是H或R6,p是0.1或2。本发明的化合物具有胶原蛋白C蛋白酶(PCP)抑制活性。本发明还涉及化合物的制备和包含它们的药物组合物。他

著录项

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号