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    • 2. 发明申请
      US20050054661A1 Corticotropin releasing factor antagonists 失效
    • Corticotropin releasing factor antagonists
    • 促肾上腺皮质激素释放因子拮抗剂
    • US20050054661A1
    • 2005-03-10
    • US10480958
    • 2002-06-11
    • Romano Di Fabio , Chiara Marchionni , Fabrizio Micheli , Alessandra Pasquarello , Yves St-Denis
    • Romano Di Fabio , Chiara Marchionni , Fabrizio Micheli , Alessandra Pasquarello , Yves St-Denis
    • A61K31/519 , A61K51/00 , A61K51/04 , A61P1/04 , A61P25/00 , A61P25/22 , A61P25/24 , A61P43/00 , C07D239/70 , C07D239/94 , C07D471/04 , C07D487/04 , C07D487/02
    • C07D487/04 , A61K51/0459 , C07B2200/05 , C07D239/70 , C07D239/94 , C07D471/04
    • The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof wherein R is aryl or heteroaryl and each of the above groups R may be substituted by 1 to 4 groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, —COR4, nitro, —NR3R4 cyano, or a group R5; R1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR3R4 or cyano; R2 corresponds to a group CHR6R7; R3 is hydrogen, C1-C6 alkyl; R4 independently from R3, has the same meanings; R5 is C3-C7 cycloalkyl, which may contain one or more double bonds; aryl; or a 5-6 membered heterocycle; wherein each of the above groups R5 may be substituted by one or more groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, C1-C6 dialkylamino, nitro or cyano; R6 is hydrogen, C2-C6 alkenyl or C1-C6 alkyl, wherein each of the above groups R6 may be substituted by one or more groups selected from: C1-C6 alkoxy and hydroxy; R7 independently from R6, has the same meanings; X is carbon or nitrogen; to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).
    • 本发明提供式（I）化合物，其包括立体异构体，前药和药学上可接受的盐或溶剂合物，其中R是芳基或杂芳基，并且上述基团中的每一个R可以被1至4个选自以下的基团取代：卤素，C 1 -C 6 烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，-COR 4，硝基，-NR 3 R 4氰基或基团R 5; R 1是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷基，卤代C 1 -C 6烷氧基，卤素，NR 3 R 4或氰基; R2对应于CHR6R7基团; R3是氢，C1-C6烷基; R4独立于R3，具有相同的含义; R5是C3-C7环烷基，其可以含有一个或多个双键; 芳基; 或5-6元杂环; 其中每个上述基团R 5可以被一个或多个选自以下的基团取代：卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6 烷氧基，C1-C6二烷基氨基，硝基或氰基; R 6是氢，C 2 -C 6烯基或C 1 -C 6烷基，其中上述基团R 6可以被一个或多个选自以下的基团取代：C 1 -C 6烷氧基和羟基; R7独立于R6，具有相同的含义; X是碳或氮; 其制备方法，含有它们的药物组合物及其用于治疗由促肾上腺皮质激素释放因子（CRF）介导的病症的用途。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 3. 发明授权
      US07462622B2 Pyrrolo[2, 3-d] pyrimidine derivatives as corticotropin releasing factor antagonists 失效
    • Pyrrolo[2, 3-d] pyrimidine derivatives as corticotropin releasing factor antagonists
    • 吡咯并[2,3-d]嘧啶衍生物作为促肾上腺皮质激素释放因子拮抗剂
    • US07462622B2
    • 2008-12-09
    • US10480958
    • 2002-06-11
    • Romano Di Fabio , Chiara Marchionni , Fabrizio Micheli , Alessandra Pasquarello , Bendetta Perini , Yves St-Denis
    • Romano Di Fabio , Chiara Marchionni , Fabrizio Micheli , Alessandra Pasquarello , Bendetta Perini , Yves St-Denis
    • A61K31/519 , C07D487/04 , A61P25/24 , A61P25/22
    • C07D487/04 , A61K51/0459 , C07B2200/05 , C07D239/70 , C07D239/94 , C07D471/04
    • The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof wherein R is aryl or heteroaryl and each of the above groups R may be substituted by 1 to 4 groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, —COR4, nitro, —NR3R4 cyano, or a group R5; R1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR3R4 or cyano; R2 corresponds to a group CHR6R7; R3 is hydrogen, C1-C6 alkyl; R4 independently from R3, has the same meanings; R5 is C3-C7 cycloalkyl, which may contain one or more double bonds; aryl; or a 5-6 membered heterocycle;  wherein each of the above groups R5 may be substituted by one or more groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, C1-C6 dialkylamino, nitro or cyano; R6 is hydrogen, C2-C6 alkenyl or C1-C6 alkyl, wherein each of the above groups R6 may be substituted by one or more groups selected from: C1-C6 alkoxy and hydroxy; R7 independently from R6, has the same meanings; X is carbon or nitrogen; to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).
    • 本发明提供式（I）化合物，其包括立体异构体，前药和药学上可接受的盐或溶剂合物，其中R是芳基或杂芳基，并且上述基团中的每一个R可以被1至4个选自以下的基团取代：卤素，C 1 -C 6 烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，-COR 4，硝基，-NR 3 R 4氰基或基团R 5; R 1是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷基，卤代C 1 -C 6烷氧基，卤素，NR 3 R 4或氰基; R2对应于CHR6R7基团; R3是氢，C1-C6烷基; R4独立于R3，具有相同的含义; R5是C3-C7环烷基，其可以含有一个或多个双键; 芳基; 或5-6元杂环; 其中每个上述基团R 5可以被一个或多个选自以下的基团取代：卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6 烷氧基，C1-C6二烷基氨基，硝基或氰基; R 6是氢，C 2 -C 6烯基或C 1 -C 6烷基，其中上述基团R 6可以被一个或多个选自以下的基团取代：C 1 -C 6烷氧基和羟基; R7独立于R6，具有相同的含义; X是碳或氮; 其制备方法，含有它们的药物组合物及其用于治疗由促肾上腺皮质激素释放因子（CRF）介导的病症的用途。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 8. 发明申请
      US20100063078A1 SPIROCOMPOUNDS USEFUL AS MODULATORS FOR DOPAMINE D3 RECEPTORS 失效
    • SPIROCOMPOUNDS USEFUL AS MODULATORS FOR DOPAMINE D3 RECEPTORS
    • US20100063078A1
    • 2010-03-11
    • US12297253
    • 2007-04-24
    • Barbara Bertani , Romano Di Fabio , Fabrizio Micheli , Alessandra Pasquarello , Luca Tarsi , Silvia Terreni
    • Barbara Bertani , Romano Di Fabio , Fabrizio Micheli , Alessandra Pasquarello , Luca Tarsi , Silvia Terreni
    • A61K31/506 , C07D413/14 , C07D417/14 , C07D409/14 , A61K31/427 , A61K31/422 , A61P25/00
    • C07D403/06 , C07D409/14 , C07D413/14 , C07D417/14 , C07D491/10
    • The present invention relates to novel compounds of formula (I) or salts thereof: wherein A is a substituent selected in the group consisting of P, P1, P2 and P3 wherein P is P1 is P2 is P3 is p is an integer ranging from 0 to 4; R4 is selected in the group consisting of halogen, hydroxy, cyano, C1-4 alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl, SF5 and a 5- or 6-membered monocyclic heteroaryl group; and when p is an integer ranging from 2 to 4, each R4 may be the same or different; R2 is hydrogen or C1-4alkyl; q is 3, 4 or 5; n is 0, 1 or 2; X is —CR1R3— or —O—; R1 is selected in the group consisting of hydrogen, C1-4 alkyl and fluorine; R3 is selected in the group consisting of hydrogen, C1-4alkyl and fluorine; R5 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, C3-7 cycloalkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and NR′R″; or R5 is a phenyl group, a 5-14 membered heterocyclic group; and any of such phenyl or heterocyclic group is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, haloC1-4alkyl, C1-4 alkoxy, C1-4alkanoyl and SF5; R6 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, C3-7 cycloalkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and NR′R″; or R6 is a phenyl group, a 5-14 membered heterocyclic group and any of such phenyl or heterocyclic group is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, haloC1-4alkyl, C1-4 alkoxy, C1-4alkanoyl and SF5; R7 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, C3-7 cycloalkyl, C1-4alkoxy, haloC1-4 alkoxy, C1-4 alkanoyl and NR′R″; or R7 is a phenyl group, a 5-14 membered heterocyclic group; and any of such phenyl or heterocyclic group is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, haloC1-4alkyl, C1-4 alkoxy, C1-4alkanoyl and SF5; R8 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, C3-7 cycloalkyl, C1-4alkoxy, haloC1-4 alkoxy, C1-4 alkanoyl and NR′R″; or R8 is a phenyl group, a 5-14 membered heterocyclic group; and any of such phenyl or heterocyclic group is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, haloC1-4alkyl, C1-4 alkoxy, C1-4alkanoyl and SF5; R9 is selected in the group consisting of hydrogen, a phenyl group, a heterocyclyl group, a 5- or 6-membered monocyclic heteroaryl group, and a 8- to 11-membered heteroaryl bicyclic, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4 alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; R10 is C1-4alkyl; R11 is hydrogen or C1-4alkyl; R′ is H, C1-4 alkyl or C1-4 alkanoyl; R″ is defined as R′; R′ and R″ taken together with the interconnecting nitrogen atom may form a 5-, 6-membered saturated or unsaturated heterocyclic ring; wherein R5, R6, R7 and R8 are not simultaneously other than hydrogen; wherein only one R2 group ma be different from hydrogen and wherein when n is 0, X is a group —CR1R3—; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, premature ejaculation or to enhance cognition.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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