Organic diamine compounds for use as oral hypoglycemic agents and pharmaceutical compositions thereof
申请人:PFIZER INC.
公开号:EP0010896A1
公开(公告)日:1980-05-14
The compounds for use as oral hypoglycemic agents are of the formulae:
wherein X is hydrogen, fluorine, chlorine, bromine, nitro, cyano, lower alkyl or lower alkoxy, X being other than hydrogen in formula (I);
Y and Y' are each amino, lower N-monoalkylamino, lower N,N-dialkylamino, pyridylamino, pyrrolidino, piperidino, homopiperidino, morpholino, thiomorpholino, 2,3-dihydroisoindolyl and 1,2,3,4-tetrahydroisoquinolyl; and
Z is oxygen or sulfur. Several methods for the preparation of these compounds are described; e.g. a,a'-dibromo-o-oxylene by reaction with piperidine gives 1,1'-[1,2--phenylene-bis-(methylene)]bispiperidine.
Novel compounds claimed are: those of formula (I) wherein X is other than hydrogen or methyl, or wherein Y is pyridylamino and Y' is other than pyridylamino; and the compounds of formulae (IV) and (VI). Compositions claimed comprise an effective blood sugar lowering amount of a compound of formulae (I) to (VI) and a carrier material.
用作口服降血糖剂的化合物属于以下式子:
其中 X 是氢、氟、氯、溴、硝基、氰基、低级烷基或低级烷氧基,在式(I)中 X 不是氢;
Y 和 Y'分别是氨基、低级 N-单烷基氨基、低级 N,N-二烷基氨基、吡啶基氨基、吡咯烷基、哌啶基、均哌啶基、吗啉基、硫代吗啉基、2,3-二氢异吲哚基和 1,2,3,4-四氢异喹啉基;以及
Z 是氧或硫。这些化合物的制备方法有多种,例如,a,a'-二溴邻二甲苯与哌啶反应生成 1,1'-[1,2-亚苯基-双(亚甲基)]双哌啶。
权利要求的新型化合物有:式(I)的化合物,其中X不是氢或甲基,或Y是吡啶氨基,Y'不是吡啶氨基;以及式(IV)和(VI)的化合物。权利要求的组合物包含有效降血糖量的式(I)至(VI)化合物和载体材料。