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    • 5. 发明授权
    • Azabicyclo (3.1.0.) hexane derivatives useful as modulators of dopamine D3 receptors
    • 可用作多巴胺D3受体调节剂的氮杂双环(3.1.0。)己烷衍生物
    • US07855298B2
    • 2010-12-21
    • US10598200
    • 2005-02-21
    • Luca AristaGiorgio BonanomiAnna Maria CapelliFederica DamianiRomano Di FabioGabriella GentileDieter HamprechtFabrizio MicheliLuca TarsiGiovanna TedescoSilvia Terreni
    • Luca AristaGiorgio BonanomiAnna Maria CapelliFederica DamianiRomano Di FabioGabriella GentileDieter HamprechtFabrizio MicheliLuca TarsiGiovanna TedescoSilvia Terreni
    • C07D215/38
    • C07D495/04C07D401/14C07D403/04C07D403/12C07D403/14C07D405/14C07D413/14C07D417/14C07D471/08
    • The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: 1. wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, —CH2—N -pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2 -pyrrolidinonyl, and such a group is optionally substituted by one or two substituents selected from: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; and when R1 is chlorine and p is 1, such R1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R1 corresponds to R5, p is 1; or a salt thereof which are useful as modulators of dopamine D3 receptors, e.g. to treat drug dependency or as antipsychotic agents.
    • 本发明涉及新的式(I)化合物或其药学上可接受的盐:1.其中G选自:苯基,吡啶基,苯并噻唑基,吲唑基; p为0〜5的整数。 R 1独立地选自:卤素,羟基,氰基,C 1-4烷基,卤代C 1-4烷基,C 1-4烷氧基,卤代C 1-4烷氧基,C 1-4烷酰基; 或对应于R5组; R2是氢或C1-4烷基; R3是C1-4烷基; R 4是氢或苯基,杂环基,5或6元杂芳族基团或8至11元双环基团,其中任何基团任选被1,2,3或4个取代基取代 选自:卤素,氰基,C 1-4烷基,卤代C 1-4烷基,C 1-4烷氧基,C 1-4烷酰基; R5是选自以下的部分:异恶唑基,-CH 2 -N-吡咯基,1,1-二氧化-2-异噻唑烷基,噻吩基,噻唑基,吡啶基,2-吡咯烷基,任选地被一个或多个 选自以下的两个取代基:卤素,氰基,C 1-4烷基,卤代C 1-4烷基,C 1-4烷氧基,C 1-4烷酰基; 当R1为氯且p为1时,该R1不存在于与分子的其余部分的连接键的邻位; 当R1对应于R5时,p为1; 或其盐,其可用作多巴胺D3受体的调节剂,例如, 治疗药物依赖或作为抗精神病药。
    • 6. 发明申请
    • Azabicyclo (3.1.0) Hexane Derivatives Useful As Modulators Of Dopamine D3 Receptors
    • 可用作多巴胺D3受体调节剂的氮杂双环(3.1.0)己烷衍生物
    • US20100160336A1
    • 2010-06-24
    • US12639282
    • 2009-12-16
    • Luca AristaGiorgio BonanomiAnna Maria CapelliFederica DamianiRomano Di FabioGabriella GentileDieter HamprechtFabrizio MicheliLuca TarsiGiovanna TedescoSilvia Terreni
    • Luca AristaGiorgio BonanomiAnna Maria CapelliFederica DamianiRomano Di FabioGabriella GentileDieter HamprechtFabrizio MicheliLuca TarsiGiovanna TedescoSilvia Terreni
    • A61K31/50C07D403/14
    • C07D495/04C07D401/14C07D403/04C07D403/12C07D403/14C07D405/14C07D413/14C07D417/14C07D471/08
    • The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituents selected from: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; and when R1 is chlorine and p is 1, such R1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R1 corresponds to R5, p is 1; 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 or as antipsychotic agents.
    • 本发明涉及新的式(I)化合物或其药学上可接受的盐:其中G选自:苯基,吡啶基,苯并噻唑基,吲唑基; p为0〜5的整数。 R 1独立地选自:卤素,羟基,氰基,C 1-4烷基,卤代C 1-4烷基,C 1-4烷氧基,卤代C 1-4烷氧基,C 1-4烷酰基; 或对应于R5组; R2是氢或C1-4烷基; R3是C1-4烷基; R 4是氢或苯基,杂环基,5或6元杂芳族基团或8至11元双环基团,其中任何基团任选被1,2,3或4个取代基取代 选自:卤素,氰基,C 1-4烷基,卤代C 1-4烷基,C 1-4烷氧基,C 1-4烷酰基; R5是选自以下的部分:异恶唑基,-CH 2 -N-吡咯基,1,1-二氧化-2-异噻唑烷基,噻吩基,噻唑基,吡啶基,2-吡咯烷酮基,任选地被一个或多个 选自以下的两个取代基:卤素,氰基,C 1-4烷基,卤代C 1-4烷基,C 1-4烷氧基,C 1-4烷酰基; 当R1为氯且p为1时,该R1不存在于与分子的其余部分的连接键的邻位; 当R1对应于R5时,p为1; 它们的制备方法,这些方法中使用的中间体,含有它们的药物组合物及其在治疗中的用途,作为多巴胺D3受体的调节剂。 治疗药物依赖或作为抗精神病药。
    • 10. 发明申请
    • Condensed n-heterocyclic compounds and their use as crf receptor antagonists
    • 缩合的N-杂环化合物及其作为crf受体拮抗剂的用途
    • US20070004708A1
    • 2007-01-04
    • US10552493
    • 2004-04-07
    • Daniele AndreottiGiovannie BernasconiEmiliano CastiglioniStefania ContiniRomano Di FabioElettra FazzolariAldo FerianiGabriella GentileMario MattioliAnna MingardiFabio SabbatiniYves St-Denis
    • Daniele AndreottiGiovannie BernasconiEmiliano CastiglioniStefania ContiniRomano Di FabioElettra FazzolariAldo FerianiGabriella GentileMario MattioliAnna MingardiFabio SabbatiniYves St-Denis
    • A61K31/549A61K31/519A61K31/496A61K31/501A61K31/4745C07D487/02C07D471/02
    • C07D471/04C07D487/04
    • The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof (Formula (I)) wherein the dashed line may represent a double bond; R is aryl or heteroaryl, each of which may be substituted by 1 to 4 groups J selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 lkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, —C(O)R2, nitro, hydroxy, —NR3R4, cyano and or a group Z; R1 is hydrogen, C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 thioalkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR3R4 or cyano; D, G is —C— optionally substituted; X is carbon or nitrogen; Y is nitrogen or —C— optionally substituted; W is a 4-8 membered ring, which may be saturated or may contain one to three double bonds, and in which:—one carbon atom is replaced by a carbonyl or S(O)m; and—one to four carbon atoms may optionally be replaced by oxygen, nitrogen or NR12, S(O)m, carbonyl, and such ring may be further substituted by 1 to 8 substituents; Z is a 5-6 membered heterocycle, which may be substituted by 1 to 8 R5 groups or a phenyl ring, which may be substituted by 1 to 4 substituents; m is an integer from 0 to 2. 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).
    • 本发明提供了包含立体异构体,前体药物和药学上可接受的盐或溶剂合物(式(I))的式(I)化合物,其中虚线可以表示双键; R是芳基或杂芳基,其各自可以被1-4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,卤素 C 1 -C 6烷氧基,-C(O)R 2,硝基,羟基,-NR 3 R 4,氰基和/或Z ; R 1是氢,C 3 -C 7环烷基,C 1 -C 6烷基,C 1 -C 6烷氧基,C 1 -C 6硫代烷基,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; D,G是-C-任选取代的; X是碳或氮; Y是氮或-C-任选取代的; W是4-8元环,其可以是饱和的或可以含有一至三个双键,并且其中: - 一个碳原子被羰基或S(O)m取代; 一至四个碳原子可以任选地被氧,氮或NR 12,S(O)m H,羰基取代,并且这种环可进一步被1 至8个取代基; Z是5-6元杂环,其可被1至8个R 5取代基或可被1至4个取代基取代的苯环; m为0至2的整数。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。