Derivatives of dioxan-2-alkyl carbamates, preparation thereof and application thereof in therapeutics
    11.
    发明授权
    Derivatives of dioxan-2-alkyl carbamates, preparation thereof and application thereof in therapeutics 有权
    二烷基-2-烷基氨基甲酸酯的衍生物,其制备及其在治疗中的应用

    公开(公告)号:US07777057B2

    公开(公告)日:2010-08-17

    申请号:US12510326

    申请日:2009-07-28

    IPC分类号: C07D319/06

    摘要: A compound corresponding to general formula (I): in which R1 represents a phenyl or naphthalenyl group optionally substituted with one or more halogen atoms or hydroxyl, cyano, nitro, (C1-C3)alkyl, (C1-C3)alkoxy, trifluoromethyl, trifluoromethoxy, benzyloxy, (C3-C6)cycloalkyl-O— or (C3-C6)cycloalkyl(C1-C3)alkoxy groups; R2 represents either a group of general formula CHR3CONHR4 in which R3 represents a hydrogen atom or a methyl group and R4 represents a hydrogen atom or a (C1-C3)alkyl, (C3-C5)cycloalkyl or (pyridin-4-yl)methyl group; or a 2,2,2-trifluoroethyl group; or an (imidazol-2-yl)methyl group; or a (benzimidazol-2-yl)methyl group; or a phenyl group optionally substituted with one or more halogen atoms or cyano, nitro, (C1-C3)alkyl, (C1-C3)alkoxy, trifluoromethyl or trifluoromethoxy groups; and n represents a number ranging from 1 to 3; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate. Also disclosed and claimed are the pharmaceutical compositions derived therefrom and their therapeutic use in treating a wide variety of diseases.

    摘要翻译: 氰基,硝基,(C1-C3)烷基,(C1-C3)烷氧基,三氟甲基,(C1-C3)烷氧基, 三氟甲氧基,苄氧基,(C3-C6)环烷基-O-或(C3-C6)环烷基(C1-C3)烷氧基; R 2表示通式CHR 3 CONHR 4的基团,其中R 3表示氢原子或甲基,R 4表示氢原子或(C 1 -C 3)烷基,(C 3 -C 5)环烷基或(吡啶-4-基)甲基 组; 或2,2,2-三氟乙基; 或(咪唑-2-基)甲基; 或(苯并咪唑-2-基)甲基; 或任选被一个或多个卤素原子取代的苯基或氰基,硝基,(C 1 -C 3)烷基,(C 1 -C 3)烷氧基,三氟甲基或三氟甲氧基; n表示1〜3的数; 以碱的形式,与酸的加成盐,水合物或溶剂合物的形式。 还公开并要求保护的是由其衍生的药物组合物及其治疗各种疾病的治疗用途。

    Alkyl-heterocycle carbamate derivatives, their preparation and their therapeutic application
    15.
    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
    16.
    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
    19.
    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。