NEW DIHYDROINDOLONE DERIVATIVES, METHOD OF PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

    公开(公告)号:RS52701B

    公开(公告)日:2013-08-30

    申请号:RSP20130099

    申请日:2010-08-03

    Applicant: SERVIER LAB

    Abstract: Dihydroindolone derivatives (I) and their optical and geometric isomers, or addition salts with an acid or base are new. Dihydroindolone derivatives of formula (I) and their optical and geometric isomers, or addition salts with an acid or base are new. m : 1 or 2; n : 1 or 2; A : a pyrrolyl group optionally substituted by 1-3 groups of 1-6C alkyl; X : C(O), S(O) or SO 2; either R 1>, R 2> : 1-6C alkyl; or NR 1>R 2> : a heterocyclic group; R 3>R 4> : a heterocyclic group; R 5> : H or 1-6C alkyl; and R 6> : H or halo, where the heterocyclic group is a mono or bicyclic 5-8 membered group (optionally containing one to three heteroatoms of N, O or S, and one or more unsaturations, and optionally substituted by one or more 1-6C alkyl, 1-6C alkenyl, oxo, hydroxy, 1-6C alkoxy, aryl, arylalkyl or arylalkenyl), the aryl is phenyl group optionally substituted by one or more halo or 1-6C alkyl, and X represents the double bond, which is in configuration is Z or E. Independent claims are included for: (1) the preparations of (I); and (2) combination comprising (I) with an anticancer agent comprising genotoxic agents, mitotic poisons, antimetabolites, proteasome inhibitors or kinase inhibitors. [Image] ACTIVITY : Cytostatic. MECHANISM OF ACTION : None given.

    DERIVADOS DIHIDROINDOLONAS, SU PROCEDIMIENTO DE PREPARACION Y LAS COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN

    公开(公告)号:PE20110206A1

    公开(公告)日:2011-04-09

    申请号:PE2010000465

    申请日:2010-07-21

    Applicant: SERVIER LAB

    Abstract: REFERIDA A UN DERIVADO DE DIHIDROINDOLONA DE FORMULA (I), DONDE m Y n SON 1 O 2; A ES PIRROLILO NO SUSTITUIDO O SUSTITUIDO POR 1 A 3 ALQUILO C1-C6 LINEALES O RAMIFICADOS; X ES C(O), S(O) O SO2; R1 Y R2 SON ALQUILO C1-C6 O JUNTO CON EL NITROGENO AL QUE ESTAN UNIDOS FORMAN UN HETEROCICLO MONO O BICICLICO DE 5 A 8 ATOMOS CON HETEROATOMOS TALES COMO N, O Y S; R3 Y R4 FORMAN JUNTO CON LOS ATOMOS A LOS QUE ESTAN UNIDOS UN HETEROCICLO MONO O BICICLICO DE 5 A 8 ATOMOS CON HETEROATOMOS TALES COMO N, O Y S; R5 ES H O ALQUILO C1-C6 LINEAL O RAMIFICADO; R6 ES H O HALOGENO. SON COMPUESTOS PREFERIDOS: 3-[(3-{[4-(4-MORFOLINILMETIL)-1H-PIRROL-2-IL]METILEN}-2-OXO-2,3-DIHIDRO-1H-INDOL-5-IL)METIL]-1,3-TIAZOLIDIN-2,4-DIONA, 3-[((3Z)-3-{[4-(4-MORFOLINILMETIL)-1H-PIRROL-2-IL]METILEN}-2-OXO-2,3-DIHIDRO-1H-INDOL-5-IL)METIL]-1,3-TIAZOLIDIN-2,4-DIONA, 3-[3-(4-MORFOLIN-4-ILMETIL-1H-PIRROL-2-ILMETILEN)-2-OXO-2,3-DIHIDRO-1H-INDOL-5-ILMETIL]-OXAZOLIDIN-2,4-DIONA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA MIGRACION DE CELULAS CANCEROSAS Y SON UTILES EN EL TRATAMIENTO DEL CANCER, PRINCIPALMENTE, EN TUMORES SOLIDOS METASTASICOS

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