申请人:PFIZER INC.
公开号:EP0899261A1
公开(公告)日:1999-03-03
This invention provides a compound of the formula (I):
and its pharmaceutically acceptable salts, wherein A1 and A2 are each halo; R1 and R2 are independently C1-4 alkyl; R3 is substituted or unsubstituted, phenyl or naphthyl; Y is heterocyclic group selected from C5-10 azacycloalkyl, C6-10 diazacycloalkyl, C7-10 azabicycloalkyl and the like; and R4 is selected from (a) substituted or unsubstituted C1-8 alkyll; (b) substituted or unsubstituted amino; (c) substituted or unsubstituted C2-6 alkanoyl; (d) substituted or unsubstituted C3-8 cycloalkyl or C7-14 bicycloalkyl; (e) substituted or unsubstituted C5-10 azacycloalkyl or C6-10 diazacycloalkyl, and (f) substituted or unsubstituted C7-14 mono- or di-azabicycloalkyl. These compounds are useful for the treatment of medical conditions caused by bradykinin such as inflammation, cardiovascular disease, pain, etc. This invention also provides a pharmaceutical composition comprising the above compound, and intermediates of the above compounds.
本发明提供了一种式(I)化合物:
及其药学上可接受的盐类,其中 A1 和 A2 各为卤代;R1 和 R2 独立地为 C1-4 烷基;R3 为取代或未取代的苯基或萘基;Y 为杂环基团,选自 C5-10 氮杂环烷基、C6-10 二氮杂环烷基、C7-10 氮杂双环烷基等;R4 选自 (a) 取代或未取代的 C1-8 烷基;(b) 取代或未取代的氨基; (c) 取代或未取代的 C2-6 烷酰基; (d) 取代或未取代的 C3-8 环烷基或 C7-14 双环烷基; (e) 取代或未取代的 C5-10 氮杂环烷基或 C6-10 二氮杂环烷基,以及 (f) 取代或未取代的 C7-14 单氮杂双环烷基或双氮杂双环烷基。这些化合物可用于治疗由缓激肽引起的病症,如炎症、心血管疾病、疼痛等。本发明还提供了一种药物组合物,其中包含上述化合物以及上述化合物的中间体。