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    • 5. 发明申请
    • Cyclic Amine Derivatives, Processes For Their Preparation, And Pharmaceutical Compositions Containing Them
    • 环胺衍生物,其制备方法以及含有它们的药物组合物
    • US20090192194A1
    • 2009-07-30
    • US11869945
    • 2007-10-10
    • Giuseppe AlvaroLuca AristaFrancesca CardulloLucilla D'AdamoAldo FerianiRiccardo GiovanniniCatia Seri
    • Giuseppe AlvaroLuca AristaFrancesca CardulloLucilla D'AdamoAldo FerianiRiccardo GiovanniniCatia Seri
    • A61K31/445C07D401/02C07D211/22A61P25/22
    • C07D405/04C07D211/34C07D405/12
    • A compound of formula (I) wherein R is a radical selected from in which R7 is halogen, cyano, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl or trifluoromethoxy; p is an integer from 0 to 3; R1 is hydrogen, halogen, cyano, C2-4 alkenyl, C1-4 alkyl optionally substituted by halogen, cyano or C1-4 alkoxy; R2 is hydrogen or C1-4 alkyl; R3 and R4 independently are hydrogen, C1-4 alkyl or R3 together with R4 is C3-7 cycloalkyl; R5 is phenyl substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or (SO)rC1-4 alkyl, naphthyl substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or (SO)rC1-4 alkyl, a 9 to 10 membered fused bicyclic heterocyclic group substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or (SO)rC1-4 alkyl or R5 is a 5 or 6 membered heteroaryl group substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or (SO)rC1-4 alkyl; R6 is hydrogen or (CH2)qR8; R8 is hydrogen, C3-7 cycloalkyl, C1-4 alkoxy, amine, C1-4 alkylamine, (C1-4 alkyl)2amine, OC(O)NR9R10 or C(O)NR9R10; R9 and R10 independently are hydrogen, C1-4 alkyl or C3-7 cycloalkyl; m is zero or 1; n is 1 or 2; q is an integer from 1 to 4; r is 1 or 2; or pharmaceutically acceptable salts and solvates thereof; processes for their preparation to pharmaceutical compositions containing them and their use in the treatment of conditions mediated by tachykinins and/or by selective inhibition of serotonin reuptake transporter protein.
    • 式(I)化合物,其中R为选自其中R 7为卤素,氰基,C 1-4烷基,C 1-4烷氧基,三氟甲基或三氟甲氧基的基团; p是0至3的整数; R 1是氢,卤素,氰基,C 2-4链烯基,任选地被卤素,氰基或C 1-4烷氧基取代的C 1-4烷基; R2是氢或C1-4烷基; R3和R4独立地是氢,C1-4烷基或R3与R4一起是C3-7环烷基; R5是被1-3个独立地选自三氟甲基,C1-4烷基,氰基,C1-4烷氧基,三氟甲氧基,卤素或(SO)rC1-4烷基取代的苯基,被1至3个独立地选自三氟甲基, C 1-4烷基,氰基,C 1-4烷氧基,三氟甲氧基,卤素或(SO)r C 1-4烷基,被1至3个独立地选自三氟甲基,C 1-4烷基,氰基的1-3元基团取代的9至10元稠合双环杂环基 ,C 1-4烷氧基,三氟甲氧基,卤素或(SO)rC 1-4烷基或R 5是被1-3个独立地选自三氟甲基,C 1-4烷基,氰基,C 1-4烷氧基, 三氟甲氧基,卤素或(SO)rC 1-4烷基; R6是氢或(CH2)qR8; R 8为氢,C 3-7环烷基,C 1-4烷氧基,胺,C 1-4烷基胺,(C 1-4烷基)2胺,OC(O)NR 9 R 10或C(O)NR 9 R 10; R9和R10独立地是氢,C1-4烷基或C3-7环烷基; m为零或1; n为1或2; q是1至4的整数; r为1或2; 或其药学上可接受的盐和溶剂化物; 其制备方法用于含有它们的药物组合物及其用于治疗由速激肽介导的病症和/或通过选择性抑制5-羟色胺再摄取转运蛋白。
    • 8. 发明授权
    • Azabicyclo (3, 1, 0) hexan 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
    • US07745458B2
    • 2010-06-29
    • US12064123
    • 2006-08-18
    • Luca AristaAnna ChecchiaGabriella GentileDieter HamprechtFabrizio Micheli
    • Luca AristaAnna ChecchiaGabriella GentileDieter HamprechtFabrizio Micheli
    • A01N43/42A61K31/44C07D239/00C07D239/02C07D261/04C07D261/14C07D233/00C07D233/14C07D233/60
    • C07D403/06C07D403/12
    • The present invention relates to novel compounds of formula (I) or a salt thereof: wherein: p is 0, 1, 2, 3, 4 or 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; n is 3 or 4; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is —CH2—, —O— or —S—; Z may be —CH— or N; A is a group P or P1, wherein P is and P1 is and Y is hydrogen, —OH, C1-4alkyl, haloC1-4alkyl, phenyl or a heteroaromatic group, wherein the phenyl and the heteroaromatic group are optionally substituted by one or two substituents selected from a group consisting of C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and haloC1-4alkoxy; 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 substance related disorders, as antipsychotic agents premature ejaculation or cognition impairment.
    • 本发明涉及新的式(I)化合物或其盐:其中:p为0,1,2,3,4或5; 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烷酰基和SF 5; n为3或4; R2是氢或C1-4烷基; n为2或3; X是-CH 2 - , - O-或-S-; Z可以是-CH-或N; A是P或P1基团,其中P是和P1是且Y是氢,-OH,C 1-4烷基,卤代C 1-4烷基,苯基或杂芳基,其中苯基和杂芳基任选被一个或两个 选自C 1-4烷基,卤代C 1-4烷基,C 1-4烷氧基和卤代C 1-4烷氧基的取代基; 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。 治疗物质相关疾病,作为抗精神病药物早泄或认知障碍。
    • 9. 发明申请
    • AZABICYCLO (3, 1, 0) HEXAN DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE D3 RECEPTORS
    • AZ Y Y O O O O O S S S S S S S S S S S S S S S S S S S S S S
    • US20090221618A1
    • 2009-09-03
    • US12064123
    • 2006-08-18
    • Luca AristaAnna ChecchiaGabriella GentileDieter HamprechtFabrizio Micheli
    • Luca AristaAnna ChecchiaGabriella GentileDieter HamprechtFabrizio Micheli
    • A61K31/506C07D403/06
    • C07D403/06C07D403/12
    • The present invention relates to novel compounds of formula (I) or a salt thereof: wherein: p is 0, 1, 2, 3, 4 or 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; n is 3 or 4; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is —CH2—, —O— or —S—; Z may be —CH— or N; A is a group P or P1, wherein P is and P1 is ; and Y is hydrogen, —OH, C1-4alkyl, haloC1-4alkyl, phenyl or a heteroaromatic group, wherein the phenyl and the heteroaromatic group are optionally substituted by one or two substituents selected from a group consisting of C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and haloC1-4alkoxy; 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 substance related disorders, as antipsychotic agents premature ejaculation or cognition impairment.
    • 本发明涉及新的式(I)化合物或其盐:其中:p为0,1,2,3,4或5; 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烷酰基和SF 5; n为3或4; R2是氢或C1-4烷基; n为2或3; X是-CH 2 - , - O-或-S-; Z可以是-CH-或N; A是P或P1组,其中P和P1是; 并且Y是氢,-OH,C 1-4烷基,卤代C 1-4烷基,苯基或杂芳基,其中苯基和杂芳基任选被一个或两个选自C 1-4烷基,卤代C 1-4烷基 ,C 1-4烷氧基和卤代C 1-4烷氧基; 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。 治疗物质相关疾病,作为抗精神病药物早泄或认知障碍。
    • 10. 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。