发明名称 2,5-DISUBSTITUTED-4(3H)-PYTIMIDONES HAVING HISTAMINE H2-RECEPTOR ANTIGONIST ACTIVTY
摘要 The title compds. (I; m = 0-2; n = 2-5; Z = S, 0 or methylene; R1 = NO2 or NR2R3 (R2 and R3 = H or (lower) alkyl, or R2 = H and R3 = formyl, carbalkoxy, alkanoyl or benzoyl); and A = phenyl, furyl, thienyl, phridyl, thiazolyl, imidazolyl, oxazolyl or pyrimidinyl, provided that A is mono-or di-substd.), are prepd. 10 Compds. and salts are specifically claimed, including 5-carbethoxy amino-2-(3-(3- piperidino methyl phenoxy)-propylamino)-4(3)pyrimidone and salt. Prepn. may be done by the reaction of A-(CH2)mZ(CH2)n NH2 with compd. (II; R8 = nucleophile, e.g. F) in a non-reactive solvent to give compd. (Ia) which is reduced to give (I6)(Ia; R1 = NO2, I6; R1 = NH2) .
申请公布号 KR900001198(B1) 申请公布日期 1990.02.28
申请号 KR19840005791 申请日期 1984.09.21
申请人 SQUIBB-BRISTOL-MYERS CO 发明人 ALGIERI ALDO A.
分类号 C07D239/32;A61K31/505;A61P1/04;A61P43/00;C07D239/46;C07D239/48;C07D295/096;C07D333/00;C07D401/12;C07D403/12;C07D405/12;C07D409/12;C07D417/12;(IPC1-7):C07D239/32 主分类号 C07D239/32
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