专利号:US-2002156277-A1 优先权日:2001-04-20 标题 :Synthesis and methods of use of purine analogues and derivatives 发明人:FICK DAVID B; FOREMAN MARK M; GLASKY ALVIN J 摘要:A purine derivative or analogue comprises a 9-atom bicyclic moiety, moiety A, linked through a linker L to a moiety B, where B is a carboxylic acid, a carboxylic acid ester, or a moiety of the structure N(Y 1 )—D, where Y 1 can be one of a variety of substituents, including hydrogen or alkyl, and D is a moiety that enhances the pharmacological effects, promotes absorption or blood-brain barrier penetration of the derivative or analogue. The moiety A has a six-membered ring fused to a five-membered ring. The moiety A can have one, two, or three nitrogen atoms in the five membered ring and has two nitrogen atoms in the six-membered ring. The moiety A can be a purine moiety. The moiety B can be one of a variety of moieties, including moieties having nootropic activity or other biological or physiological activity.
专利号:US-6207836-B1 优先权日:1993-02-17 标 题 :Indolin-2-one derivatives 发明人:ESAKI TORU; EMURA TAKASHI; HOSHINO EIICHI 权利人:CHUGAI PHARMACEUTICAL CO LTD 摘要:A compound represented by formula (I):wherein R1 represents a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a nitro group, a trifluoromethyl group, a lower alkylthio group, an acyl group, a carboxyl group, a mercapto group or an amino group; R2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, an alkoxy group, an acyl group, an aryl group or a heterocyclic group; R3 represents a lower alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; R4 represents a hydrogen atom, a lower alkyl group, an aryl group, a heterocyclic group, -OR5, -SR5 or -NR6R7 (wherein R5, R6, and R7 each represent a lower alkyl group, etc.); X and Y each represent -CH2-, -NH- or -O-; and n represents an integer of from 0 to 4, and an intermediate for synthesis thereof are disclosed. The compound of the present invention exhibits selective antagonism against gastrin receptors without causing side effects attributed to CCK-A receptor antagonism and is useful for the treatment and prevention of peptic ulcers, gastritis, reflux esophagitis, and Zollinger-Ellison syndrome, and for the treatment of neoplasm originating in the gastrointestinal system.