公开(公告)号：US4808729A

公开(公告)日：1989-02-28

申请号：US100685

申请日：1987-09-24

申请人： James R. Deason ,  Michael A. Stealey ,  Richard M. Weier

发明人： James R. Deason ,  Michael A. Stealey ,  Richard M. Weier

IPC分类号： C07D327/04 ,  C07D339/06 ,  C07D339/02

CPC分类号： C07D339/06 ,  C07D327/04

摘要： The invention encompasses compounds of Formula I ##STR1## and the pharmaceutically acceptable salts and geometrical and optical isomers thereof wherein:X, Y, and Z are each independently O or S with S optionally oxidized to S.dbd.O;Alk is alkylene or hydroxyalkylene containing 1-6 carbon atoms;R.sub.1 is hydrogen or lower alkyl;n is 0 to 5;R.sub.2 is hydrogen, lower alkyl, cycloalkyl, --(CH.sub.2).sub.n --CO.sub.2 R.sub.1, phenyl, phenyl substituted with halo, lower alkyl or lower alkoxy; andAr is 5,6,7,8-tetrahydro-1-naphthalenyl, phenyl, or phenyl substituted with lower alkyl, hydroxy, lower alkoxy, or lower alkanoyl. The compounds are useful as anti-allergy agents and anti-inflammatory agents.

摘要翻译： 本发明包括式I的化合物及其药学上可接受的盐和几何和旋光异构体，其中：X，Y和Z各自独立地为O或S，S任选被氧化成S = O; Alk是含有1-6个碳原子的亚烷基或羟基亚烷基; R1是氢或低级烷基; n为0〜5; R 2是氢，低级烷基，环烷基， - （CH 2）n -CO 2 R 1，苯基，被卤素，低级烷基或低级烷氧基取代的苯基; 和Ar为5,6,7,8-四氢-1-萘基，苯基或被低级烷基，羟基，低级烷氧基或低级烷酰基取代的苯基。 该化合物可用作抗过敏剂和抗炎剂。

公开(公告)号：US4988707A

公开(公告)日：1991-01-29

申请号：US406638

申请日：1989-09-13

申请人： Michael A. Stealey ,  Richard M. Weier

发明人： Michael A. Stealey ,  Richard M. Weier

IPC分类号： A61K31/505 ,  A61P7/02 ,  A61P11/08 ,  A61P11/16 ,  A61P29/00 ,  A61P43/00 ,  C07D471/04

CPC分类号： C07D471/04

摘要： This invention relates to substituted imidazopyridine dervatives having the following formula ##STR1## and isomers thereof; or a pharmaceutically acceptable acid addition salt thereof: whereinR.sub.1 and R.sub.2 are each independently selected from hydrogen; straight or branched chain alkyl of 1 to 15 carbon atoms; cycloalkyl of 3 to 8 carbon atoms; cycloalkyl which can be substituted once or more by alkyl of 1 to 6 carbon atoms; phenyl; phenyl which can be substituted once or more by alkyl of 1 to 6 carbon atoms or halogen; straight or branched alkenyl having 3 to 15 carbon atoms.y is phenyl or phenyl substituted once or more by alkyl of 1 to 6 carbon atoms; alkoxy wherein the alkyl is 1 to 6 carbon atoms; and halogen selected from the group consisting of bromo, fluoro or chloro.m is an integer from 0 to 5.n is an integer from 1 to 5.R.sub.3 is a group substituted at one or more of the 4, 6 or 7 positions of the pyridine ring said groups being independently selected from hydrogen, alkyl of 1 to 6 carbon atoms; halogen wherein the halogen is selected from bromo, fluoro, or chloro; or alkoxy wherein the alkyl is 1 to 6 carbon atoms;R.sub.4 is hydrogen or alkyl of 1 to 4 carbon atoms.useful in the treatment of diseases or disorders mediated by platelet-activating factor. This invention also relates to pharmaceutical compositions of such substituted imidazopyridines.

公开(公告)号：US5223539A

公开(公告)日：1993-06-29

申请号：US796513

申请日：1991-11-21

申请人： Roger A. Nosal ,  Michael A. Stealey ,  Richard M. Weiser

发明人： Roger A. Nosal ,  Michael A. Stealey ,  Richard M. Weiser

IPC分类号： C07C233/65 ,  C07C235/42 ,  C07C235/54 ,  C07C235/84 ,  C07C237/38 ,  C07D317/60 ,  C07D317/64

CPC分类号： C07C235/54 ,  C07C233/65 ,  C07C235/42 ,  C07C235/84 ,  C07C237/38 ,  C07D317/60 ,  C07D317/64 ,  C07C2101/08 ,  C07C2101/14 ,  Y10S514/826 ,  Y10S514/886

摘要： The present invention relates to compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Z can be: ##STR2## wherein R.sup.3 is alkyl having 1 to 6 carbon atoms and, when n is greater than 1, each R.sup.3 can be the same or different; and n is an integer from 1 to 3;R.sup.1 and R.sup.2 can each independently be hydrogen, straight or branched chain alkyl, or cycloalkyl having 3 to 8 carbon atoms which can optionally be substituted at one or more positions by alkyl of 1 to 6 carbon atoms; X is oxygen, sulfur, NR.sup.4, wherein R.sup.4 is hydrogen or alkyl having 1 to 4 carbon atoms, C.dbd.O, CHOH, or CH.sub.2 ; Y is hydrogen, alkoxy, halogen, alkyl, or hydroxy; and m is an integer from 0 to 3. The compounds are antagonists of platlet-activating factor (PAF).

摘要翻译： 本发明涉及下式的化合物及其药学上可接受的盐，其中Z可以是：（a）其中R 3是具有1至6个碳原子的烷基，当n大于1时， 每个R3可以相同或不同; n为1〜3的整数， R 1和R 2可各自独立地为氢，直链或支链烷基或具有3至8个碳原子的环烷基，其可以任选地在一个或多个位置被1-6个碳原子的烷基取代; X是氧，硫，NR 4，其中R 4是氢或具有1至4个碳原子的烷基，C = O，CHOH或CH 2; Y是氢，烷氧基，卤素，烷基或羟基; m是0-3的整数。化合物是铂弹性因子（PAF）的拮抗剂。