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1. 发明授权

US08030322B2 Spirocompounds useful as modulators for dopamine D3 receptors 失效
标题翻译：螺环化合物可用作多巴胺D3受体的调节剂
公开(公告)号：US08030322B2
公开(公告)日：2011-10-04
申请号：US12297253
申请日：2007-04-24
申请人： Barbara Bertani , Romano Di Fabio , Fabrizio Micheli , Alessandra Pasquarello , Luca Tarsi , Silvia Terreni
发明人： Barbara Bertani , Romano Di Fabio , Fabrizio Micheli , Alessandra Pasquarello , Luca Tarsi , Silvia Terreni
IPC分类号： C07D403/06 , C07D409/14 , A61K31/421 , A61K31/506
CPC分类号： C07D403/06 , C07D409/14 , C07D413/14 , C07D417/14 , C07D491/10
摘要： The present invention relates to compounds of formula (I) or salts thereof wherein A, X, R2, R4 and n are defined herein, 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.
摘要翻译：本发明涉及式（I）化合物或其盐，其中A，X，R2，R4和n如本文所定义，其制备方法，在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，如多巴胺D3受体的调节剂，例如治疗药物依赖性，作为抗精神病药，治疗强迫性强迫症，早泄或增强认知。

2. 发明申请

US20100063078A1 SPIROCOMPOUNDS USEFUL AS MODULATORS FOR DOPAMINE D3 RECEPTORS 失效
公开(公告)号：US20100063078A1
公开(公告)日：2010-03-11
申请号：US12297253
申请日：2007-04-24
申请人： Barbara Bertani , Romano Di Fabio , Fabrizio Micheli , Alessandra Pasquarello , Luca Tarsi , Silvia Terreni
发明人： Barbara Bertani , Romano Di Fabio , Fabrizio Micheli , Alessandra Pasquarello , Luca Tarsi , Silvia Terreni
IPC分类号： A61K31/506 , C07D413/14 , C07D417/14 , C07D409/14 , A61K31/427 , A61K31/422 , A61P25/00
CPC分类号： C07D403/06 , C07D409/14 , C07D413/14 , C07D417/14 , C07D491/10
摘要： 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.

3. 发明申请

US20070249642A1 Azabicyclo[3.1.0]hex-3-yl}alkyl)pyrimidinedione 失效
标题翻译：氮杂双环[3.1.0]己-3-基}烷基）嘧啶二酮
公开(公告)号：US20070249642A1
公开(公告)日：2007-10-25
申请号：US11693756
申请日：2007-03-30
申请人： Barbara Bertani , Giorgio Bonanomi , Anna Capelli , Anna Checchia , Romano Di Fabio , Gabriella Gentile , Fabrizio Micheli , Alessandra Pasquarello , Giovanna Tedesco , Silvia Terreni
发明人： Barbara Bertani , Giorgio Bonanomi , Anna Capelli , Anna Checchia , Romano Di Fabio , Gabriella Gentile , Fabrizio Micheli , Alessandra Pasquarello , Giovanna Tedesco , Silvia Terreni
IPC分类号： A61K31/513 , C07D403/02
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/14
摘要： The present invention relates to novel compounds of formula (I)′ or a salt thereof: wherein G is selected from a group consisting of: phenyl, a 5- or 6-membered monocyclic heteroaryl group, or a 8- to 11-membered heteroaryl bicyclic group; A is a group P1 or a group P2 wherein P1 is and the other groups are define in herein.
摘要翻译：本发明涉及新的式（I）化合物或其盐：其中G选自：苯基，5或6元单环杂芳基或8至11元杂芳基双环基团 A是P1组或P2组，其中P1是本文定义的另一组。

4. 发明授权

US08222266B2 Azabicyclo [3.1.0] hexyl derivatives as modulators of dopamine D3 receptors 失效
标题翻译：氮杂双环[3.1.0]己基衍生物作为多巴胺D3受体的调节剂
公开(公告)号：US08222266B2
公开(公告)日：2012-07-17
申请号：US12295304
申请日：2007-03-30
申请人： Barbara Bertani , Anna Checchia , Romano Di Fabio , Gabriella Gentile , Fabrizio Micheli , Alessandra Pasquarello , Silvia Terreni
发明人： Barbara Bertani , Anna Checchia , Romano Di Fabio , Gabriella Gentile , Fabrizio Micheli , Alessandra Pasquarello , Silvia Terreni
IPC分类号： C07D403/06 , A61K31/513
CPC分类号： C07D401/14 , C07D403/06 , C07D405/14
摘要： The present invention relates to certain azabicyclo compounds of formula (I)′: wherein the various groups are defined herein and that are modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.
摘要翻译：本发明涉及某些式（I）'的氮杂二环化合物：其中各种基团在本文中定义，并且是多巴胺D3受体的调节剂，例如，治疗药物依赖性，作为抗精神病药，治疗强迫性强迫性疾病或早泄。

5. 发明授权

US07727988B2 Azabicyclo[3.1.0]hex-3-yl}alkyl)pyrimidinedione 失效
标题翻译：氮杂双环[3.1.0]己-3-基}烷基）嘧啶二酮
公开(公告)号：US07727988B2
公开(公告)日：2010-06-01
申请号：US11693756
申请日：2007-03-30
申请人： Barbara Bertani , Giorgio Bonanomi , Anna Maria Capelli , Anna Checchia , Romano Di Fabio , Gabriella Gentile , Fabrizio Micheli , Alessandra Pasquarello , Giovanna Tedesco , Silvia Terreni
发明人： Barbara Bertani , Giorgio Bonanomi , Anna Maria Capelli , Anna Checchia , Romano Di Fabio , Gabriella Gentile , Fabrizio Micheli , Alessandra Pasquarello , Giovanna Tedesco , Silvia Terreni
IPC分类号： C07D401/14 , A61K31/513
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/14
摘要： The present invention relates to novel compounds of formula (I)′ or a salt thereof: wherein G is selected from a group consisting of: phenyl, a 5- or 6-membered monocyclic heteroaryl group, or a 8- to 11-membered heteroaryl bicyclic group; A is a group P1 or a group P2 wherein P1 is and the other groups are define in herein.
摘要翻译：本发明涉及新的式（I）化合物或其盐：其中G选自：苯基，5或6元单环杂芳基或8至11元杂芳基双环基团 A是P1组或P2组，其中P1是本文定义的另一组。

6. 发明申请

US20100069416A1 Azabicyclo [3.1.0] Hexyl Derivatives as Modulators of Dopamine D3 Receptors 失效
标题翻译：偶氮二环[3.1.0]己基衍生物作为多巴胺D3受体的调节剂
公开(公告)号：US20100069416A1
公开(公告)日：2010-03-18
申请号：US12295304
申请日：2007-03-30
申请人： Barbara Bertani , Anna Checchia , Romano Di Fabio , Gabriella Gentile , Alessandra Pasquarello , Silvia Terreni
发明人： Barbara Bertani , Anna Checchia , Romano Di Fabio , Gabriella Gentile , Alessandra Pasquarello , Silvia Terreni
IPC分类号： A61K31/506 , C07D403/06 , C07D401/14 , C07D417/14 , A61P25/00 , A61P25/30 , A61P15/12
CPC分类号： C07D401/14 , C07D403/06 , C07D405/14
摘要： The present invention relates to certain azabicyclo compounds of formula (I)′: wherein the various groups are defined herein and that are modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.
摘要翻译：本发明涉及某些式（I）'的氮杂二环化合物：其中各种基团在本文中定义，并且是多巴胺D3受体的调节剂，例如，治疗药物依赖性，作为抗精神病药，治疗强迫性强迫性疾病或早泄。

7. 发明授权

US07855298B2 Azabicyclo (3.1.0.) hexane derivatives useful as modulators of dopamine D3 receptors 有权
标题翻译：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
公开(公告)号：US07855298B2
公开(公告)日：2010-12-21
申请号：US10598200
申请日：2005-02-21
申请人： Luca Arista , Giorgio Bonanomi , Anna Maria Capelli , Federica Damiani , Romano Di Fabio , Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli , Luca Tarsi , Giovanna Tedesco , Silvia Terreni
发明人： Luca Arista , Giorgio Bonanomi , Anna Maria Capelli , Federica Damiani , Romano Di Fabio , Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli , Luca Tarsi , Giovanna Tedesco , Silvia Terreni
IPC分类号： C07D215/38
CPC分类号： C07D495/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/08
摘要： 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.
摘要翻译：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。

8. 发明授权

US07799815B2 Triazole derivatives as modulators of dopamine D3 receptors 有权
标题翻译：三唑衍生物作为多巴胺D3受体的调节剂
公开(公告)号：US07799815B2
公开(公告)日：2010-09-21
申请号：US12064128
申请日：2006-08-18
申请人： Giorgio Bonanomi , Romano Di Fabio , Elettra Fazzolari , Dieter Hamprecht , Fabrizio Micheli , Luca Tarsi , Silvia Terreni
发明人： Giorgio Bonanomi , Romano Di Fabio , Elettra Fazzolari , Dieter Hamprecht , Fabrizio Micheli , Luca Tarsi , Silvia Terreni
IPC分类号： A01N43/64 , A61K31/41 , C07D249/08 , C07D249/00 , C07D249/12
CPC分类号： C07D403/14 , C07D413/14
摘要： The present invention relates to novel compounds of formula (I) or a salt thereof: wherein: G is a 5- or 6-membered heteroaromatic group, or is a 9- or 10-membered bicyclic heteroaromatic group containing one or two heteroatoms independently selected from nitrogen and oxygen, wherein G is not pyridyl, indazolyl or benzothiazolyl; p is an integer ranging from 0 to 4; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl or SF5; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is S or —CH2—; 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 and C1-4alkanoyl; R5 is isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl or 2-pyrrolidinonyl, wherein each group is optionally substituted by one or two substituents selected from: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; 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.
摘要翻译：本发明涉及新的式（I）化合物或其盐：其中：G是5-或6-元杂芳族基团，或是含有一个或两个独立选择的杂原子的9或10元双环杂芳族基团氮和氧，其中G不是吡啶基，吲唑基或苯并噻唑基; p为0〜4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SF 5; 或对应于R5组; R2是氢或C1-4烷基; n为2或3; X是S或-CH 2 - ; 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烷氧基和C 1-4烷酰基; R5是异恶唑基，-CH2-N-吡咯基，1,1-二氧化-2-异噻唑烷基，噻吩基，噻唑基，吡啶基或2-吡咯烷基，其中每个基团任选被一个或两个选自以下的取代基取代：卤素，氰基，C1 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基和C 1-4烷酰基; 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。治疗与物质相关的疾病，作为抗精神病药，早泄或认知障碍。

9. 发明申请

US20100160336A1 Azabicyclo (3.1.0) Hexane Derivatives Useful As Modulators Of Dopamine D3 Receptors 有权
标题翻译：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
公开(公告)号：US20100160336A1
公开(公告)日：2010-06-24
申请号：US12639282
申请日：2009-12-16
申请人： Luca Arista , Giorgio Bonanomi , Anna Maria Capelli , Federica Damiani , Romano Di Fabio , Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli , Luca Tarsi , Giovanna Tedesco , Silvia Terreni
发明人： Luca Arista , Giorgio Bonanomi , Anna Maria Capelli , Federica Damiani , Romano Di Fabio , Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli , Luca Tarsi , Giovanna Tedesco , Silvia Terreni
IPC分类号： A61K31/50 , C07D403/14
CPC分类号： C07D495/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/08
摘要： 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.
摘要翻译：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. 发明授权

US08263782B2 Azabicyclo (3.1.0) hexane derivatives useful as modulators of dopamine D3 receptors 有权
公开(公告)号：US08263782B2
公开(公告)日：2012-09-11
申请号：US12639129
申请日：2009-12-16
申请人： Luca Arista , Giorgio Bonanomi , Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli , Anna Maria Capelli , Federica Damiani , Romano Di Fabio , Luca Tarsi , Giovanna Tedesco , Silvia Terreni
发明人： Luca Arista , Giorgio Bonanomi , Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli , Anna Maria Capelli , Federica Damiani , Romano Di Fabio , Luca Tarsi , Giovanna Tedesco , Silvia Terreni
IPC分类号： C07D215/38
CPC分类号： C07D495/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/08
摘要： 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.

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