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).

    DERIVADO DE 1,5 BENZODIAZEPINA
    70.
    发明专利

    公开(公告)号:PE50994A1

    公开(公告)日:1995-01-06

    申请号:PE24002794

    申请日:1994-04-13

    Applicant: GLAXO INC

    Abstract: SE REFIERE A UN COMPUESTO DE FORMULA I DONDE: 1) NR1R2 ES UN ANILLO HETEROCICLICO SATURADO DE 5 A 7 MIEMBROS QUE PUEDE ESTAR SUSTITUIDO POR 1 o 2 METILOS, TAL COMO UN ANILLO PIRROLIDINO, PIPERIDINO; 2) R3 ES UN ALQUILO C1-C6, CICLOALQUILO C3-C6, FENILO, FENILO SUSTITUIDO CON 2 HALOGENOS; 3) R4 ES UN FENILO O FENILO SUSTITUIDO CON 1 o 2 HALOGENOS, ALQUILO C1-C4, TRIFLUOROMETILO, TRIFLUOROMETOXI, (CH2)nR5 DONDE n ES 0 o 1 Y R5 ES UN ALCOXI C1-C4, Y OTROS; 4) X ES H, ALQUILO C1-C4, HALOGENO; 5) m VARIA DE 0 A 2; ESTE COMPUESTO PUEDE SER ANTAGONISTA DE LA GASTRINA Y COLECISTOCININA (CCK) TENIENDO MAYOR AFINIDAD POR EL RECEPTOR CCK-B, SIENDO UTIL EN EL TRATAMIENTO DE TRANSTORNOS GASTROINTESTINALES YA QUE PUEDE DISMINUIR LA SECRECION GASTRICA, Y EN TRANSTORNOS DEL SISTEMA NERVIOSO CENTRAL TAL COMO ANSIEDAD, DEPRESION, DISQUINESIA TARDIA

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