发明授权
US4891381A Derivatives of 5-pentylamino-5-oxopentanoil and
4-pentlamino-4-oxobutanoic acids with antagonistic activity towards
cholecystokinin
失效
5-戊基氨基-5-氧代戊二醇和对胆囊收缩素具有拮抗作用的4-戊氨基-4-氧代丁酸的衍生物
- 专利标题: Derivatives of 5-pentylamino-5-oxopentanoil and 4-pentlamino-4-oxobutanoic acids with antagonistic activity towards cholecystokinin
- 专利标题(中): 5-戊基氨基-5-氧代戊二醇和对胆囊收缩素具有拮抗作用的4-戊氨基-4-氧代丁酸的衍生物
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申请号: US284002申请日: 1988-12-07
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公开(公告)号: US4891381A公开(公告)日: 1990-01-02
- 发明人: Francesco Makovec , Rolando Chiste' , Walter Peris , Luigi Rovati
- 申请人: Francesco Makovec , Rolando Chiste' , Walter Peris , Luigi Rovati
- 申请人地址: ITX Milano
- 专利权人: Rotta Research Laboratorium
- 当前专利权人: Rotta Research Laboratorium
- 当前专利权人地址: ITX Milano
- 优先权: ITX67937A/86 19861216
- 主分类号: A61K31/195
- IPC分类号: A61K31/195 ; A61K31/34 ; A61K31/343 ; A61K31/38 ; A61K31/381 ; A61K31/40 ; A61K31/403 ; A61K31/404 ; A61K31/47 ; A61P1/00 ; A61P25/00 ; A61P43/00 ; C07C231/00 ; C07C231/02 ; C07C237/06 ; C07C237/08 ; C07C237/22 ; C07D209/42 ; C07D215/48 ; C07D215/54 ; C07D307/84 ; C07D307/85 ; C07D333/68 ; C07D333/70
摘要:
New original derivatives are described of 5-pentylamino -5-oxopentanoic and 4-pentylamino-4-oxobutanoic acids having the formula: ##STR1## in which n is 1 or 2, R.sub.1 is selected from the groups 2-naphthyl, 2 (or 3)-quinolinyl, 2 (or 3)-indolyl, 2 (or 3)-benzofuranyl, 2 (or 3)-benzothiophenyl, and R.sub.2 is a pentyl group or an alkoxyalkyl group with 4 or 5 carbon atoms, preferably pentyl, 2-ethoxyethyl, 3-methoxypropyl or 3-ethoxypropyl.The compounds have a powerful antagonistic activity towards cholecystokinin and are particularly useful in the treatment of illnesses of the digestive system, such as colitis, biliary diskinesia, pancreatitis or in the treatment of disorders of the central nervous system imputable to deficiencies in the physiological neuron levels of cholecystokinin or other related bioactive polypeptides.
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