首页> 外国专利> Derivatives of 5-pentylamino-5-oxopentanoil and 4-pentlamino-4- oxobutanoic acids with antagonistic activity towards cholecystokinin

Derivatives of 5-pentylamino-5-oxopentanoil and 4-pentlamino-4- oxobutanoic acids with antagonistic activity towards cholecystokinin

机译:对胆囊收缩素有拮抗作用的5-戊基氨基-5-氧戊丹油和4-戊基氨基-4-氧丁酸的衍生物

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.PPThe 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.
机译:描述了具有以下通式的5-戊基氨基-5-氧代戊酸和4-戊基氨基-4-氧代丁酸的新原始衍生物:其中n为1或2,R.sub.1选自组2 -萘基,2(或3)-喹啉基,2(或3)-吲哚基,2(或3)-苯并呋喃基,2(或3)-苯并噻吩基和R 2是戊基或烷氧基烷基,其中4或5个碳原子,优选戊基,2-乙氧基乙基,3-甲氧基丙基或3-乙氧基丙基。该化合物对胆囊收缩素具有强大的拮抗活性,尤其可用于治疗消化系统疾病,例如结肠炎,胆道疾病,胰腺炎或中枢神经系统疾病的治疗,归因于胆囊收缩素或其他相关生物活性多肽的生理神经元水平缺乏。

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