公开(公告)号：PH30897A

公开(公告)日：1997-12-23

申请号：PH48093

申请日：1994-04-14

Applicant: GLAXO INC

Inventor： SUGG ELIZABETH E ,  AQUINO CHRISTOPHER J ,  RYSZARD SZEWCZYK JERZY ,  HARRY FINCH ,  ELLIS CARR ROBIN ARTHUR

IPC: A61K31/551 ,  A61K38/02 ,  A61P3/00 ,  A61K38/00 ,  A61P5/00 ,  A61P43/00 ,  C07D243/12 ,  C07K5/02 ,  C07K5/06 ,  C07K5/078 ,  C07K5/08 ,  C07K5/097 ,  C07K4/08 ,  A61K37/02

Abstract: PCT No. PCT/EP94/01130 Sec. 371 Date Oct. 30, 1995 Sec. 102(e) Date Oct. 30, 1995 PCT Filed Apr. 13, 1994 PCT Pub. No. WO94/24151 PCT Pub. Date Oct. 27, 1994The present invention relates to compounds of general formula (I) (I) and physiologically acceptable salts thereof wherein the group NR1R2 represents a 5-7 membered saturated heterocyclic ring which may be substituted by one or two methyl groups; R3 is C1-6alkyl, C3-6cycloalkyl or phenyl optionally substituted by 1 or 2 halogen atoms; R4 is phenyl or phenyl substituted by one or two groups selected from the group consisting of halogen, C1-4alkyl, trifluoromethyl, trifluoromethoxy or (CH2)nR5 wherein n is zero or 1 and R5 represents C1-4alkoxy, hydroxy, nitro, cyano, CO2R6, S(O)pCH3, NR7R8, CONR7R8, SO2NR7CO(C1-4)alkyl, tetrazolyl, carboxamidotetrazolyl, or a 3-trifluoromethyl 1,2,4-triazolyl; R6 is hydrogen, C1-4alkyl or benzyl; R7 is hydrogen or C1-4alkyl, R8 is hydrogen, C1-4alkyl, SO2CH3 or SO2CF3, X represent hydrogen, C1-4alkyl or halogen; m is zero, 1 or 2, and p is zero, 1 or 2. The invention also relates to processes for preparation of these compounds and to their use in medicine as antagonists of gastrin and CCK.

公开(公告)号：MY112237A

公开(公告)日：2001-05-31

申请号：MYPI19940880

申请日：1994-04-12

Applicant: GLAXO INC

Inventor： CHRISTOPHER JOSEPH AQUINO ,  HARRY FINCH ,  ROBIN ARTHUR ELLIS CARR ,  ELIZABETH ELLEN SUGG ,  JERZY RYSZARD SZEWCZYK

IPC: A61K31/55 ,  A61K38/00 ,  A61K31/551 ,  C07D243/12 ,  A61K38/02 ,  A61P3/00 ,  A61P5/00 ,  A61P43/00 ,  C07K5/02 ,  C07K5/06 ,  C07K5/078 ,  C07K5/08 ,  C07K5/097

Abstract: NOVEL BENZODIAZEPINE COMPOUNDS OF FORMULAWHICH EXHIBIT AGONIST ACTIVITY FOR CCK-A RECEPTORS ENABLING THEM TO MODULATE THE HORMONES GASTRIN AND CHOLECYSTOKININ (CCK) IN MAMMALS FOR USE IN MEDICINE AS ANORECTIC AGENTS IN THE REGULATION OF APPETITE, THE TREATMENT OF OBESITY AND THE MAINTENANCE OF WEIGHT LOSS.