SERINE, ASPARTIC ACID AND GLUTAMIC ACID DERIVATIVE HAVING ANTI-CCK ACTIVITY

PURPOSE: To obtain a serine, an aspartic acid and a glutamic acid derivatives having cck activity resistance having strong and selective competitive inhibition on cholecystokinin(CCK). CONSTITUTION: This compound is shown by formula I ((n) is 1-3; R1 is diphenylmethylpiperazinyl; R2 is carboxytriazo...

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Hauptverfasser: MATSUDA SEI, KIDOKORO SHINPEI, MORITA TADASHI, OGAWA MASASHI, IIBUCHI NORIHIRO
Format: Patent
Sprache:eng
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Zusammenfassung:PURPOSE: To obtain a serine, an aspartic acid and a glutamic acid derivatives having cck activity resistance having strong and selective competitive inhibition on cholecystokinin(CCK). CONSTITUTION: This compound is shown by formula I ((n) is 1-3; R1 is diphenylmethylpiperazinyl; R2 is carboxytriazolyl, carboxyoxazolyl or carboxypyridylthio; R3 is indolyl) such as (S)-1-[5-(4,5-dicarboxy-1,2,3-trrazol-1- yl)-2-(mndol-2-yl)carbonylamino]valeryl-4-diphenylmethylpiperazine. The compound of formula I (in the case of serine) is obtained by amidating a compound of formula II (Boc is t-butoxycarbonyl; R11 is tetrahydropyranyl; (n) is 1) as a starting compound, modifying the end hydroxyl group of serine and acylating. The compound is useful for preventing and treating pancreatic cancer, gastric ulcer, duodenal ulcer, peptic ulcer, colitis and cholecyst function ataxia, especially acute pancreatitis.