Alkyl-heterocycle carbamate derivatives, their preparation and their therapeutic application
    5.
    发明授权
    Alkyl-heterocycle carbamate derivatives, their preparation and their therapeutic application 有权
    烷基杂环氨基甲酸酯衍生物,其制备及其治疗应用

    公开(公告)号:US09000010B2

    公开(公告)日:2015-04-07

    申请号:US13574188

    申请日:2011-01-19

    IPC分类号: A61K31/454 C07D417/12

    CPC分类号: C07D417/12 A61K31/454

    摘要: The invention relates to compounds corresponding to the general formula (I): in which R2 represents a hydrogen, fluorine, hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or —NR8R9; n and m represent, independently of one another, an integer equal to 1, 2 or 3, it being understood that the sum m+n is at most equal to 5; A represents a covalent bond, an oxygen, a C1-6-alkylene or —O—C1-6-alkylene; R1 represents a phenyl or a heterocycle which is optionally substituted; R3 represents a hydrogen, fluorine, C1-6-alkyl or trifluoromethyl; R4 represents an optionally substituted 5-membered heterocycle; in the form of the base or of an addition salt with an acid; with the exclusion of 5-methylisoxazol-3-ylmethyl 4-hydroxy-4-(4-chlorophenyl)piperidine-1-carboxylate. The invention also relates to a process for the preparation of the compounds of formula (I), to compositions comprising them and to their therapeutic application.

    摘要翻译: 本发明涉及对应于通式(I)的化合物:其中R 2表示氢,氟,羟基,氰基,三氟甲基,C 1-6 - 烷基,C 1-6 - 烷氧基或-NR 8 R 9; n和m彼此独立地表示等于1,2或3的整数,可以理解,和m + n最多等于5; A表示共价键,氧,C 1-6 - 亚烷基或-O-C 1-6 - 亚烷基; R 1表示任选被取代的苯基或杂环; R 3表示氢,氟,C 1-6 - 烷基或三氟甲基; R4表示任选取代的5元杂环; 以碱的形式或与酸的加成盐; 除去5-羟基-4-(4-氯苯基)哌啶-1-甲酸5-甲基异恶唑-3-基甲酯。 本发明还涉及制备式(I)化合物的方法,包括它们的组合物及其治疗应用。

    Alkylthiazol carbamate derivatives, preparation thereof and therapeutic use thereof
    6.
    发明授权
    Alkylthiazol carbamate derivatives, preparation thereof and therapeutic use thereof 有权
    烷基噻唑氨基甲酸酯衍生物,其制备及其治疗用途

    公开(公告)号:US08912218B2

    公开(公告)日:2014-12-16

    申请号:US13003713

    申请日:2009-07-21

    IPC分类号: C07D401/04 C07D417/14

    CPC分类号: C07D417/14

    摘要: The invention relates to the novel products of formula (I): in which: Ra represents H, Hal, aryl or heteroaryl, which is optionally substituted; Rb represents H, Rc, —COORc-CO—Rc or —CO—NRcRd; where Rc represents alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd represents H, alk or cycloalkyl; these products being in all the isomer forms and the salts, as medicaments, in particular as MET inhibitors.

    摘要翻译: 本发明涉及式(I)的新产物:其中:R a表示任选取代的H,Hal,芳基或杂芳基; Rb表示H,Rc,-COORc-CO-Rc或-CO-NRcRd; 其中R c代表烷基,环烷基,杂环烷基,芳基和杂芳基,全部任意取代; Rd表示H,烷基或环烷基; 这些产品是所有异构体形式和盐,作为药物,特别是作为MET抑制剂。

    ALKYL-HETEROCYCLE CARBAMATE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
    7.
    发明申请
    ALKYL-HETEROCYCLE CARBAMATE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION 有权
    烷基 - 杂环碳酸酯衍生物,其制备及其治疗应用

    公开(公告)号:US20120295909A1

    公开(公告)日:2012-11-22

    申请号:US13574188

    申请日:2011-01-19

    CPC分类号: C07D417/12 A61K31/454

    摘要: The invention relates to compounds corresponding to the general formula (I): in which R2 represents a hydrogen, fluorine, hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or —NR8R9; n and m represent, independently of one another, an integer equal to 1, 2 or 3, it being understood that the sum m+n is at most equal to 5; A represents a covalent bond, an oxygen, a C1-6-alkylene or —O—C1-6-alkylene; R1 represents a phenyl or a heterocycle which is optionally substituted; R3 represents a hydrogen, fluorine, C1-6-alkyl or trifluoromethyl; R4 represents an optionally substituted 5-membered heterocycle; in the form of the base or of an addition salt with an acid; with the exclusion of 5-methylisoxazol-3-ylmethyl 4-hydroxy-4-(4-chlorophenyl)piperidine-1-carboxylate. The invention also relates to a process for the preparation of the compounds of formula (I), to compositions comprising them and to their therapeutic application.

    摘要翻译: 本发明涉及对应于通式(I)的化合物:其中R 2表示氢,氟,羟基,氰基,三氟甲基,C 1-6 - 烷基,C 1-6 - 烷氧基或-NR 8 R 9; n和m彼此独立地表示等于1,2或3的整数,可以理解,和m + n最多等于5; A表示共价键,氧,C 1-6 - 亚烷基或-O-C 1-6 - 亚烷基; R 1表示任选被取代的苯基或杂环; R 3表示氢,氟,C 1-6 - 烷基或三氟甲基; R4表示任选取代的5元杂环; 以碱的形式或与酸的加成盐; 除去5-羟基-4-(4-氯苯基)哌啶-1-甲酸5-甲基异恶唑-3-基甲酯。 本发明还涉及制备式(I)化合物的方法,包括它们的组合物及其治疗应用。