公开(公告)号：EP1342719A1

公开(公告)日：2003-09-10

申请号：EP03010776.7

申请日：1993-02-26

申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. ,  FERRING RESEARCH LIMITED

发明人： Ryder, Hamish ,  Semple, Graeme ,  Kendrick, David Alan ,  Szelke, Michael ,  Satoh, Masato ,  Ohta, Mitsuaki ,  Miyata, Keiji ,  Nishida, Akito

IPC分类号： C07D243/24 ,  A61K31/5513 ,  A61P35/00

CPC分类号： C07D401/04 ,  C07D243/24 ,  C07D403/06

摘要： A benzodiazepine derivative of formula I, or a pharmaceutically acceptable salt thereof:
wherein

(a) R 1 is -CH 2 CHOH(CH 2 ) a R 4 or a ketone group -CH 2 CO(CH 2 ) a R 5 in which a is 0 or 1 and R 4 and R 5 are selected from alkyl groups of up to 8 carbon atoms;
(b) R 2 and R 3 are independently selected from optionally substituted monocyclic aromatic carbocylic and heterocyclic residues of 5 or 6 ring atoms of which one, two or three may be heteroatoms, the optional substituents being selected from halogen atoms and hydroxy, amino, nitro, carboxylic acid, carboxamido and cyano groups and alkyl, alkoxy, alkylamino and dialkylamino groups in which the or each alkyl group is of up to 8 carbon atoms; and
(c) W and X are selected independently from halogen and hydrogen atoms and C 1 -C 8 alkyl and C 1 -C 8 alkoxy groups.

These compounds are gastrin and/or CCK-B receptor antagonists.

摘要翻译： 式I的苯并二氮杂衍生物或其药学上可接受的盐：其中（a）R 1是-CH 2 CHOH（CH 2）aR 4或酮基-CH 2 CO（CH 2）a R 5，其中 a为0或1，R 4和R 5选自至多8个碳原子的烷基; （b）R 2和R 3独立地选自5或6个环原子的任选取代的单环芳族碳环和杂环残基，其中一个，两个或三个可以是杂原子，任选的取代基选自卤素原子和 羟基，氨基，硝基，羧酸，甲酰胺基和氰基以及烷基，烷氧基，烷基氨基和二烷基氨基，其中烷基或每个烷基具有多至8个碳原子; 和（c）W和X独立地选自卤素和氢原子和C 1 -C 8烷基和C 1 -C 8烷氧基。 这些化合物是胃泌素和/或CCK-B受体拮抗剂。