DERIVADOS DE DIHIDROINDOLONAS, SU PROCEDIMIENTO DE PREPARACION Y LAS COM-POSICIONES FARMACEUTICAS QUE LOS CONTIENEN

    公开(公告)号:AR077510A1

    公开(公告)日:2011-08-31

    申请号:ARP100102775

    申请日:2010-07-30

    Applicant: SERVIER LAB

    Abstract: Su empleo en medicamentos para el tratamiento del cáncer. Reivindicacion 1: Compuestos de formula (1): en la que ò m representa 1 o 2, ò n representa 1 o 2, ò A representa un grupo pirrolilo no sustituido o sustituido con 1 a 3 grupos alquilo (C1-6) lineal o ramificado, ò X representa el grupo C(O), S(O) o SO2, ò R1 y R2, idénticos o diferentes, representan cada uno un grupo alquilo (C1-6) lineal o ramificado, o R1 y R2 forman junto con el átomo de nitrogeno al que están unidos un grupo heterocíclico, ò R3 y R4 forman junto con los átomos a los que están unidos un grupo heterocíclico, ò R5 representa un átomo de hidrogeno o un grupo alquilo (C1-6) lineal o ramificado, ò R6 representa un átomo de hidrogeno o un átomo de halogeno, entendiéndose que: - por ôgrupo heterocíclicoö, se entiende un grupo mono o bicíclico que puede contener de 5 a 8 vértices, que puede contener de uno a tres heteroátomos elegidos entre nitrogeno, oxigeno y azufre, y que puede contener una o varias insaturaciones, pudiendo estar el grupo heterociclico así definido no sustituido o sustituido con uno o varios grupos elegidos entre alquilo (C1-6) lineal o ramificado, alquenilo (C1-6) lineal o ramificado, oxo, hidroxi, alcoxi (C1-6) lineal o ramificado, arilo, arilalquilo, y arilalquenilo, - por ôariloö, se entiende el grupo fenilo no sustituido o sustituido con uno o varios grupos elegidos entre los átomos de halogeno y los grupos alquilo (C1-6) lineal o ramificado, - el siglo X significa que la doble enlace tiene configuracion Z o E, sus isomeros opticos y geométricos, así como sus sales de adicion a un ácido o a una base farmacéuticamente aceptable.

    DIHYDROINDOLONE COMPOUNDS,A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

    公开(公告)号:ZA201005424B

    公开(公告)日:2011-04-28

    申请号:ZA201005424

    申请日:2010-07-29

    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.

    New dihydroindolone compounds, a process for their preparation and pharmaceutical compositions containing them

    公开(公告)号:AU2010203305A1

    公开(公告)日:2011-02-24

    申请号:AU2010203305

    申请日:2010-07-23

    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.

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