公开(公告)号：ECSP941065A

公开(公告)日：1994-12-15

申请号：ECSP941065

申请日：1994-04-12

Applicant: GLAXO INC

Inventor： SUGG ELIZABETH E ,  AQUINO CHRISTOPHER JOSEPH ,  DEZUBE MILANA ,  HENKE BRAD RICHARD ,  BRACKEEN MARCUS ,  JEFFS PETER WALTER ,  SUH EDWARD MARTIN ,  HIRST GAVIN CHARLES ,  WILLSON TIMOTHY MARK ,  MOMTAHEN TANYA

IPC: A61K20060101 ,  A61K38/00 ,  C07D20060101

Abstract: Novedosos como el proceso para su preparación, con las composiciones farmacéuticas que los contienen y con su uso en medicina, más particularmente, se relaciona con compuestos que exhiben actividad egonista para los receptores de CCK-A permitiéndoles por tanto modular las hormonas gastrina y colecistocinina en mamíferos.

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.