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2. 发明申请

WO1995003284A1 1,5-BENZODIAZEPINE DERIVATIVES USEFUL AS CCK OR GASTRIN ANTAGONISTS 审中-公开
标题翻译： 1,5-苯二酮衍生物作为CCK或GASTRIN ANTAGONISTS有用
公开(公告)号：WO1995003284A1
公开(公告)日：1995-02-02
申请号：PCT/EP1994002352
申请日：1994-07-18
申请人： GLAXO SPA , CUROTTO, Giovanni , PELLEGATTI, Mario , POLINELLI, Stefano
发明人： GLAXO SPA
IPC分类号： C07D243/12
CPC分类号： C07D243/12
摘要： Compounds of formula (I) wherein R represents a phenyl, C3-7cycloalkyl, C7-11 bridgedcycloalkyl or C1-6alkyl group which alkyl group may be substituted by a hydroxy, phenyl, C1-6alkoxycarbonyl, C3-7cycloalkyl, or C7-11 bridgedcycloalkyl group; R represents phenyl substituted by a group (CH2)nNR R , O(CH2)pR , or (CH2)nCO2R ; R represents phenyl optionally substituted by one or 2 halogen atoms; R represents hydrogen or C1-4alkyl; R represents acyl, or C2-4alkyl substituted by one or more hydroxy, carboxyl and/or amino groups or R and R together with the nitrogen atom to which they are attached form a 5-7 saturated heterocyclic ring which contain an additional heteroatom selected from oxygen, sulphur or nitrogen and/or may be substituted by 1 or 2 C1-4alkyl or hydroxy groups. R represents hydroxy, C1-4alkoxy, CO2R or NR R ; R represents hydrogen or C1-4alkyl or a metabolically labile ester group; R represents hydrogen, C1-4alkyl, acyl or C2-6alkyl substituted by one or more hydroxy, carboxyl and/or amino groups or R and R together with the nitrogen atom to which they are attached form a 5-7 saturated heterocyclic ring which contain an additional heteroatom selected from oxygen, sulphur or nitrogen and/or may be substituted by 1 or 2 C1-4alkyl or hydroxy groups; R represents hydrogen or a halogen atom; R represents a metabolically labile ester group; m is zero, 1 or 2; n is zero or 1; p is an integer from 1 to 4; X represents oxygen or NH and pharmaceutically acceptable salts thereof are antagonists of gastrin and CCK.
摘要翻译：式（I）的化合物，其中R 1表示苯基，C 3-7环烷基，C 7-11桥环的环烷基或C 1-6烷基，该烷基可被羟基，苯基，C 1-6烷氧基羰基，C 3-7环烷基或C 7 -11桥连环烷基; R 2表示被基团（CH 2）n NR 4 R 5，O（CH 2）p R 6或（CH 2）n CO 2 R 11取代的苯基; R 3表示任选被一个或两个卤素原子取代的苯基; R 4表示氢或C 1-4烷基; 或被一个或多个羟基，羧基和/或氨基取代的C 2-4烷基或R 4和R 5与它们所连接的氮原子一起形成5-7饱和的杂环，其含有选自氧，硫或氮的另外的杂原子和/或可以被1或2个C 1-4烷基或羟基取代。 R 6表示羟基，C 1-4烷氧基，CO 2 R 7或NR 8 R 9; R 7表示氢或C 1-4烷基或代谢不稳定的酯基; R 8表示氢，C 1-4烷基，酰基或被一个或多个羟基，羧基和/或氨基取代的C 2-6烷基或R 8和R 9与它们所连接的氮原子一起形成 5-7饱和杂环，其含有选自氧，硫或氮的另外的杂原子和/或可被1或2个C 1-4烷基或羟基取代; R 10表示氢或卤素原子; R 11表示代谢不稳定的酯基; m为零，1或2; n为零或1; p是1至4的整数; X表示氧或NH，其药学上可接受的盐是胃泌素和CCK的拮抗剂。

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