申请人:THE UPJOHN COMPANY
公开号:EP0162690A2
公开(公告)日:1985-11-27
A compound of the formula
wherein the stereochemistry at the spiro carbon atom is either of the two possible orientations;
each wavy line independently indicates cis or trans relationship of the respective nitrogen-containing substituent with respect to the cycloalkyl ring;
wherein p is 0, 1, 2, 3 or 4 and n is 0, 1, 2, 3 or 4, and the cycloalkyl ring containing them has 5, 6 or 7 carbon atoms;
m is 2 or 3;
A is a bond, -(CH3)q- wherein q is an integer of 1 to 4, or -CH(CH3)-;
X and Y are independently selected from H, F, Cl, Br, CF,, N02, OH, OCH3, azido, C1-3 alkyl, phenyl, methanesulfonyl, cyano, amino, (C1-3 alkoxy)carbonyl, C-3 alkanoyloxy and C1-3 carboxacylamino;
R is H or C1-3 alkyl;
either R, and R2 are independently selected from H, C1-3 alkyl and 2-propen-1-yl, or NR1R2 is 1-azetidinyl, 1-pyrrolidinyl or 1-piperidinyl; and
E is oxygen or sulfur;
or a pharmacologically-acceptable salt thereof. Such compounds can have therapeutic utility.
式中的化合物
其中螺碳原子上的立体化学为两种可能取向中的一种;
每条波浪线独立地表示各含氮取代基相对于环烷基环的顺式或反式关系;
其中 p 为 0、1、2、3 或 4,n 为 0、1、2、3 或 4,含有它们的环烷基环有 5、6 或 7 个碳原子;
m 是 2 或 3;
A 是键、-(CH3)q-(其中 q 是 1 至 4 的整数)或-CH(CH3)-;
X 和 Y 独立选自 H、F、Cl、Br、CF、N02、OH、OCH3、叠氮、C1-3 烷基、苯基、甲磺酰基、氰基、氨基、(C1-3 烷氧基)羰基、C-3 烷酰氧基和 C1-3 羧基氨基;
R 是 H 或 C1-3 烷基;
R 和 R2 要么独立选自 H、C1-3 烷基和 2-丙烯-1-基,要么 NR1R2 是 1-氮杂环丁基、1-吡咯烷基或 1-哌啶基;以及
E 是氧或硫;
或其药理上可接受的盐。此类化合物具有治疗作用。