发明授权
- 专利标题: Substituted n-[(pyridyl)alkyl]aryl-carboxamide
- 专利标题(中): 取代的n - [(吡啶基)烷基]芳基 - 甲酰胺
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申请号: US072386申请日: 1987-07-10
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公开(公告)号: US4916145A公开(公告)日: 1990-04-10
- 发明人: Jefferson W. Tilley , Robert W. Guthrie , John W. Clader , Ronald A. LeMahieu
- 申请人: Jefferson W. Tilley , Robert W. Guthrie , John W. Clader , Ronald A. LeMahieu
- 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: C07D213/40
- IPC分类号: C07D213/40 ; C07D401/06
摘要:
The invention relates to compounds of the formula ##STR1## wherein *B is ##STR2## Y is O or S, *A is *--(CH.sub.2).sub.n --(X).sub.m --(CH.sub.2).sub.r --, n or r, independently, are integers from 0 to 3, m is an integer from 0 to 1, provided that when m is 1, then n must be at least 1, X is O or S, R.sub.1 and R.sub.4, independently, are hydrogen, lower alkyl, hydroxy or lower alkoxy, provided that when *B is other than ##STR3## at least one of R.sub.1 and R.sub.4, and one of R.sub.6 and R.sub.7 must be hydrogen, R.sub.2 and R.sub.3 are independently hydrogen, lower alkyl, cycloalkyl, halogen, nitro, lower alkoxy, lower alkenyl, lower alkynyl or aryl, R.sub.5 and R.sub.6, independently are hydrogen or lower alkyl, R.sub.7 is hydrogen, lower alkyl, cycloalkyl 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, and pharmaceutical acceptable acid addition salts thereof.The compounds of formula I exhibit activity as Platelet Activating Factor (PAF) antagonists and are, therefore, useful as agents for the prevention and treatment of vascular diseases, pulmonary diseases, dermatological disorders, transplant rejection, immunological disorders and inflammatory conditions.
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