基本信息:
- 专利标题: DIHYGROPYRIDINE DERIVATIVES AS BRADYKININ ANTAGONISTS
- 专利标题(中):二氢吡啶衍生物作为BRADYKININ ANTAGONISTS
- 申请号:PCT/IB1995000400 申请日:1995-05-26
- 公开(公告)号:WO1996006082A1 公开(公告)日:1996-02-29
- 发明人: PFIZER INC. , PFIZER PHARMACEUTICALS INC.
- 申请人: PFIZER INC. , PFIZER PHARMACEUTICALS INC. , ITO, Fumitaka , KONDO, Hiroshi , HAGEMAN, David, L. , LOWE, John, A., III , NAKANISHI, Susumu , VINICK, Fredric, J.
- 专利权人: PFIZER INC.,PFIZER PHARMACEUTICALS INC.,ITO, Fumitaka,KONDO, Hiroshi,HAGEMAN, David, L.,LOWE, John, A., III,NAKANISHI, Susumu,VINICK, Fredric, J.
- 当前专利权人: PFIZER INC.,PFIZER PHARMACEUTICALS INC.,ITO, Fumitaka,KONDO, Hiroshi,HAGEMAN, David, L.,LOWE, John, A., III,NAKANISHI, Susumu,VINICK, Fredric, J.
- 优先权: JPPCT/JP94/01398 19940824
- 主分类号: C07D211/90
- IPC分类号: C07D211/90
摘要:
A compound of formula (I) and its pharmaceutically acceptable salts, wherein A and A are each halo; X is direct bond, CH2, CO, O, S, S(O) or S(O)2; R is selected from a variety of groups such as hydrogen; substituted or unsubstituted C1-4 alkyl; substituted or unsubstituted piperidinyl; substituted or unsubstituted C5-14 cycloalkyl, bicycloalkyl or tricycloalkyl; substituted or unsubstituted C7-14 azacyclo-, azabicyclo- or azatricyclo-alkyl; bicyclo C7-10 alkenyl; benzocyclo C5-7 alkyl; and heterocyclic; R is hydrogen, C1-4 alkyl, substituted or unsubstituted phenyl or heterocyclic; and R and R are each C1-5 alkyl. The novel dihydropyridine compounds of this invention have excellent bradykinin antagonistic activity and are thus useful for the treatment of inflammation, cardiovascular disease, pain, common cold, allergies, asthma, pancreatitis, burns, virus infection, head injury, multiple trauma or the like in mammalian, especially humans.
摘要(中):
式(I)化合物及其药学上可接受的盐,其中A 1和A 2各自为卤素; X是直接键,CH2,CO,O,S,S(O)或S(O)2; R 1选自各种基团,例如氢; 取代或未取代的C 1-4烷基; 取代或未取代的哌啶基; 取代或未取代的C 5-14环烷基,双环烷基或三环烷基; 取代或未取代的C7-14氮杂环,氮杂双环或氮杂三环烷基; 双环C7-10烯基; 苯并环C5-7烷基; 和杂环; R 2是氢,C 1-4烷基,取代或未取代的苯基或杂环; R 3和R 4各自为C 1-5烷基。 本发明的新型二氢吡啶化合物具有优异的缓激肽拮抗活性,因此可用于治疗炎症,心血管疾病,疼痛,感冒,过敏,哮喘,胰腺炎,烧伤,病毒感染,头部损伤,多发性创伤等 哺乳动物,特别是人类。
IPC结构图谱:
C | 化学;冶金 |
--C07 | 有机化学 |
----C07D | 杂环化合物 |
------C07D211/00 | 杂环化合物,含氢化吡啶环,不与其他环稠合 |
--------C07D211/04 | .只有氢或碳原子直接连在环氮原子上 |
----------C07D211/06 | ..环原子间或环原子与非环原子间无双键 |
------------C07D211/84 | ...有杂原子或有以3个键连杂原子。其中最多以1个键连卤素的碳原子,直接连在环碳原子上 |
--------------C07D211/90 | ....以3个键连杂原子、其中最多以1个键连卤素的碳原子 |