发明授权
US4975438A Pentadieneamide compounds which have useful activity of treating a
disease characterized by an excess of platelet activating factor
失效
具有治疗以过量血小板活化因子为特征的疾病的有用活性的戊二酰胺化合物
- 专利标题: Pentadieneamide compounds which have useful activity of treating a disease characterized by an excess of platelet activating factor
- 专利标题(中): 具有治疗以过量血小板活化因子为特征的疾病的有用活性的戊二酰胺化合物
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申请号: US241174申请日: 1988-09-06
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公开(公告)号: US4975438A公开(公告)日: 1990-12-04
- 发明人: Robert W. Guthrie , Richard W. Kierstead , Jefferson W. Tilley
- 申请人: Robert W. Guthrie , Richard W. Kierstead , Jefferson W. Tilley
- 申请人地址: NJ Nutley
- 专利权人: Hoffmann-La Roche Inc.
- 当前专利权人: Hoffmann-La Roche Inc.
- 当前专利权人地址: NJ Nutley
- 主分类号: C07D213/56
- IPC分类号: C07D213/56 ; C07D217/02 ; C07D217/16 ; C07D409/12
摘要:
Compounds of the formula ##STR1## Y is O or S, *A is paraphenylene or *--(CH.sub.2).sub.n --(X).sub.m --(CH.sub.2).sub.r --, X is O, S or --CH.dbd.CH--, n or r, independently, are integers from 0 to 3, s is an integer from 0 to 1, m is an integer from 0 to 1, provided that when m is 1, n+s must be at least 2, R.sub.1 and R.sub.2, independently, are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, Het, Aryl, R.sub.3, R.sub.4 and R.sub.8, independently, are hydrogen, lower alkyl, aryl, R.sub.5 and R.sub.6, independently, are hydrogen or lower alkyl, R.sub.7 is hydrogen, lower alkyl, cycloalkyl, Het-lower alkyl or aryl, Het is a monocyclic 5- or 6-membered hetero aromatic or a bicyclic heteroaromatic radical containing one or two hetero atoms selected from nitrogen, oxygen and sulfur, which radical may be substituted by lower alkyl, halogen or aryl, and the asterisk denotes the point of attachment,and when R.sub.6 and R.sub.7 are different, their enantiomers and racemic mixtures thereof, when R.sub.1 and R.sub.2 are different, their geometric isomers, and pharmaceutically acceptable acid addition salts thereof, are described.The compounds of formula I exhibit activity as platelet activating factor (PAF) antagonists and are, therefore, useful in disease states characterized by excess platelet activating factor or for the prevention and treatment of cardiovascular diseases, pulmonary diseases, immunological disorders, inflammatory diseases, dermatological disorders, shock or transplant rejection.
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