Cck or gastrin modulating 1,5 benzodiazepines derivatives

    公开(公告)号:AU2306295A

    公开(公告)日:1995-11-10

    申请号:AU2306295

    申请日:1995-04-13

    Applicant: GLAXO INC

    Abstract: PCT No. PCT/EP95/01336 Sec. 371 Date Nov. 14, 1996 Sec. 102(e) Date Nov. 14, 1996 PCT Filed Apr. 13, 1995 PCT Pub. No. WO95/28391 PCT Pub. Date Oct. 26, 1995 (I) Benzo[b][1,4]diazepine compounds of formula (I), where R1 is selected from C1C6alkyl, C3-C6cycloalkyl, phenyl, or substituted phenyl; R2 is selected from C3-C6alkyl, C3C6cycloalkyl, C3-C6alkenyl, benzyl, phenylC1-C3alkyl of substituted phenyl; or NR1R2 together form 1,2,3,4-tetrahydroquinoline or benzazepine, mono-, di-, or trisubstituted independently with C1-6alkyl C1-6alkoxy or halogen substituents; p is an integer 0 or 1; q is an integer 0 or 1; r is an integer 0 or 1; t is an integer 0 or 1, provided that when r is 0 then t is 0; R3, R5, and R6 are independently hydrogen or C1-6alkyl; R4 is C1-6alkyl or C1-6alkenyl; R7 is selected from the group consisting of hydrogen, C1-6alkyl, C1-6cycloalkyl, C1-6alkenyl, phenyl, substituted phenyl, napthyl, heteroaryl, substituted heteroaryl, bicycloheteroaryl or substituted bicycloheteroaryl; or NR6R7 together form a saturated 5,6, or 7 membered ring optionally interrupted by 1,2,3 or 4 N, S or O heteroatoms, with the proviso that any two O or S atoms are not bonded to each other, m is an integer selected from the group of 0, 1, 2, 3 or 4; R8 and R9 are selected from a variety of substituents; Z is hydrogen or halogen; novel intermediates, a pharmaceutical composition for treating obesity, gall bladder stasis, disorders of pancreatic secretion, methods for such treatment and processes for preparing compounds of formula (I).

    1,5 benzodiazepine derivatives
    10.
    发明专利

    公开(公告)号:ZA942570B

    公开(公告)日:1994-11-11

    申请号:ZA942570

    申请日:1994-04-14

    Applicant: GLAXO INC

    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.

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