DERIVES D'AZACARBOLINES 9H-PYRROLO[2,3-b:5,4-c']DIPYRIDINE, LEUR PREPARATION ET LEUR UTILISATION THERAPEUTIQUE
    1.
    发明申请
    DERIVES D'AZACARBOLINES 9H-PYRROLO[2,3-b:5,4-c']DIPYRIDINE, LEUR PREPARATION ET LEUR UTILISATION THERAPEUTIQUE 审中-公开
    9H-吡咯并[2,3-B:5,4-C']二吡啶基咪唑啉衍生物,其制备方法及其治疗用途

    公开(公告)号:WO2010109084A2

    公开(公告)日:2010-09-30

    申请号:PCT/FR2009/052330

    申请日:2009-11-30

    IPC分类号: C07D471/14

    摘要: Nouvelles azacarbolines 9H-pyrrolo [2,3-b:5,4-c']dipyridine de formule (I) : avec Z2, Z3, Z4 représentent CH, CRa, CRs ou N; R3 représente H, HaI; CF3, CHF2;0H, alkoxy;NH2, NH(alkyle), N(alkyle)2; C(O)Oalkyle; C0NH(alkyle),C0N(alkyle)2; C1 -C10 alkyle; aryle; hétéroaryle; R6 représente hétéroaryle; Ra représente CONH2, CONHalkyle,CONHcycloalkyle; CONHhétérocycloalkyle; CON(alkyle)2; CON(alkyle)(hétérocycloalkyle); CONHN(alkyle)2; C(O)hétérocycloalkyle; Rs représente H;Hal, OH; 0-alkyle(C1 - C10); NH2; N(alkyle(C1 -C10) ou cycloalkyle(C3-C7))2; NHC(O)R3a; N(alkyle(C1 - C10)C(O)R3a; NHS(O2)R3a; N(alkyle(C1 -C10)S(O2)R3a; CO2R3a; SR3a; S(O)R3a;S(O2)R3a; Ra et Rs forment éventuellement un cycle; ??R3a étant choisi parmi HaI, CF3, C1 -C10 alkyle; C3-C7 cycloalkyle; C2-C6 alkenyle; C2-C6 alkynyle; OH; O-alkyle(C1 -C10); (C3-C7); hétérocycloalkyle (C3-C7); NH2; NH- (alkyle(C1 -C10) ou cycloalkyle(C3-C7)); N(alkyle(C1 -C10) ou cycloalkyle(C3-C7))2; NH-(alkyle(C1 -C10) ou hétérocycloalkyle (C3-C7)); N(alkyle(C1 -C10) ou hétérocycloalkyle (C3-C7))2; ainsi que les isomères et sels desdits produits de formule (I) et leur application en thérapeutique pour le traitement du cancer.

    摘要翻译: 本发明涉及式(I)的新型9H-吡咯并[2,3-b:5,4-c']二吡啶并吡唑啉,其中:Z2,Z3和Z4为CH,CRa,CRs或N; R3为H,Hal; CF 3,CHF 2; OH,烷氧基; NH 2,NH(烷基),N(烷基)2; C(O)O烷基; CONH(烷基),CON(烷基)2; C1-C10烷基; 芳基; 杂; R6是杂芳基; R a是CONH 2,CONH烷基,CONH环烷基; CONH杂环烷基; CON(烷基)2; CON(烷基)(杂环烷基); CONHN(烷基)2; C(O)杂环烷基; Rs是H; Hal,OH; O-烷基(C1-C10); NH2; N(烷基(C1-C10)或环烷基(C3-C7))2; NHC(O)R3A; N(烷基(C1-C10)C(O)R3a; NHS(O2)R3a; N(烷基(C1-C10)S(O2)R3a; CO2R3a; SR3a; S(O)R3a; S(O2)R3a; R a和R 5任选地形成一个循环; R 3a选自Hal,CF 3,C 1 -C 10烷基; C 3 -C 7环烷基; C 2 -C 6烯基; C 2 -C 6炔基; OH; O-烷基(C 1 -C 10) -C(C 1 -C 10)或环烷基(C 3 -C 7)); NH(C 1 -C 10)或环烷基(C 3 -C 7) - (烷基(C1-C10)或杂环烷基(C3-C7)); N(烷基(C1-C10)或杂环烷基(C3-C7))2,以及所述式 )及其用于治疗癌症的治疗用途。

    AZACARBOLINE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF AS KINASE INHIBITORS
    2.
    发明申请
    AZACARBOLINE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF AS KINASE INHIBITORS 审中-公开
    氨基胆碱衍生物,其制备方法及其作为激酶抑制剂的治疗用途

    公开(公告)号:WO2009150381A3

    公开(公告)日:2010-02-18

    申请号:PCT/FR2009051100

    申请日:2009-06-11

    CPC分类号: C07D471/14 C07D213/73

    摘要: The invention relates to novel azacarbolines having formula (I), wherein R3, R4 independently represent H, hal, CF3, substituted oxy, optionally substituted alkoxy, optionally substituted amino, substituted carbonyl, optionally substituted carboxyl, optionally substituted amide, sulphur, such as optionally substituted sulphides, sulphoxides or sulphones, linear, branched or cyclic C1-C10 alkyl optionally comprising an optionally substituted heteroatom, optionally substituted linear, branched or cyclic C2-C7 alkenyl, optionally substituted linear or branched C2-C6 alkynyl, optionally substituted aryl or heteroaryl, optionally substituted heterocycloalkyl, R6 represents heteroaryl, C(O)NR1aR1b, heterocycloalkyl or -C(O)heterocycloalkyl, all of which may be optionally substituted; in the form of a base or an acid addition salt. The invention also relates to the therapeutic use of said azacarbolines for the treatment of cancer and to synthesis methods.

    摘要翻译: 本发明涉及具有式(I)的新型氮杂环丁烷,其中R 3,R 4独立地表示H,卤素,CF 3,取代的氧,任选取代的烷氧基,任选取代的氨基,取代的羰基,任选取代的羧基,任选取代的酰胺,硫, 任选取代的直链,支链或环状C 2 -C 7烯基,任选取代的直链或支链C 2 -C 6炔基,任选取代的芳基或任选取代的直链或支链C 2 -C 6炔基, 杂芳基,任选取代的杂环烷基,R 6表示杂芳基,C(O)NR 1a R 1b,杂环烷基或-C(O)杂环烷基,其全部可以任选被取代; 以碱或酸加成盐的形式存在。 本发明还涉及所述azacarbolines用于治疗癌症和合成方法的治疗用途。

    NOVEL PYRETHRINOID ESTERS DERIVED FROM ISOXAZOLIC OR ISOTHIAZOLIC ALCOHOL, PREPARATION METHOD THEREFOR AND USE THEREOF AS PESTICIDES
    3.
    发明申请
    NOVEL PYRETHRINOID ESTERS DERIVED FROM ISOXAZOLIC OR ISOTHIAZOLIC ALCOHOL, PREPARATION METHOD THEREFOR AND USE THEREOF AS PESTICIDES 审中-公开
    从ISOXAZOLIC或异硫酸醇衍生的新型吡咯烷酮,其制备方法及其作为杀虫剂的用途

    公开(公告)号:WO1993016054A1

    公开(公告)日:1993-08-19

    申请号:PCT/FR1993000119

    申请日:1993-02-05

    发明人: ROUSSEL-UCLAF

    IPC分类号: C07D261/08

    CPC分类号: A01N53/00 C07D261/08

    摘要: Compounds of formula (I), wherein the radical (a) is in position 3 or 5; X is a hydrogen atom, a cyano radical or a saturated or unsaturated alkyl radical; Y in position 4 or 5 is a hydrogen atom, an NO2, NH2 or C=N radical, a straight or branched saturated or unsaturated alkyl radical containing up to 8 carbon atoms and optionally substituted by one or more halogen atoms, a radical -(CH2)nOH where the OH radical is optionally etherified or esterified, with n being the number 0, 1, 2, 3 or 4, or a radical (b), NHalc1 or (c), wherein alc1 and alc2, which are the same or different, are an alkyl radical containing up to 8 carbon atoms; Z is an oxygen or sulphur atom; and R is the residue of an acid used in pyrethrinoid synthesis. The compounds of formula (I) have interesting pesticidal properties.