发明授权
- 专利标题: Pyridyl and pyrimidinyl substituted tyrosyl dipeptide amides
- 专利标题(中): 吡啶基和嘧啶基取代的酪氨酰二肽酰胺
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申请号: US145953申请日: 1988-01-20
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公开(公告)号: US4933325A公开(公告)日: 1990-06-12
- 发明人: Donald W. Hansen, Jr. , Barnett S. Pitzele , Michael Clare , Robert W. Hamilton
- 申请人: Donald W. Hansen, Jr. , Barnett S. Pitzele , Michael Clare , Robert W. Hamilton
- 申请人地址: IL Chicago
- 专利权人: G. D. Searle & Co.
- 当前专利权人: G. D. Searle & Co.
- 当前专利权人地址: IL Chicago
- 主分类号: A61K38/00
- IPC分类号: A61K38/00 ; C07K5/065
摘要:
The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is hydrogen, lower alkyl, hydroxy, --OCO.sub.2 lower alkyl, lower alkoxy, --O(CH.sub.2).sub.n -phenyl with the phenyl optionally substituted by halogen, --NO.sub.2, --CN, --NH.sub.2 or lower alkyl wherein n is 1 to 4; R.sup.2 and R.sup.3 represent lower alkyl, halogen, or lower alkoxy, or either one of R.sup.2 or R.sup.3 is hydrogen and the other is lower alkyl, lower alkoxy or halogen; R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 may be the same or different and represent hydrogen or lower alkyl; R.sup.10 is selected from the gorup consisting of--(ALK)Xwhere ALK represents alkylene, thioalkylene, oxyalkylene, having 1 to 5 carbon atoms; alkenylene and alkynylene having 2 to 4 carbon atoms; and X represents pyridyl, pyrimidinyl, 9H-fluoren-9-yl, diphenylmethyl, thienyl, carboxy, lower alkoxy carbonyl, substituted phenyl wherein the phenyl substituent is amino, hydroxy, halogen, nitro, methylenedioxy, lower alkyl, carboxy, lower alkoxycarbonyl, lower alkoxy, carboxamide, diloweralkylamino or X represents phenyl when ALK is not alkylene; or R.sup.10 is ##STR2## where p and q are independently 1 to 4; or R.sup.9 and R.sup.10 together with N is ##STR3## where r and t are independently 1 to 4;v represents an asymmetric carbon that may be racemic or have the D or L configuration;w represents an asymmetric carbon when R.sup.7 and R.sup.8 are not the same that may be racemic or have the D or L configuration.These compounds are useful as analgesic and/or antihypertensive compounds.
公开/授权文献
- US5987223A Image processing device 公开/授权日:1999-11-16
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