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1. 发明授权

US07947683B2 3-(1,2,4-triazol-3-ylalkyl) azabicyclo (3.1.0) hexane derivatives as modulators of dopamine D3 receptors 失效
标题翻译： 3-（1,2,4-三唑-3-基烷基）氮杂双环（3.1.0）己烷衍生物作为多巴胺D3受体的调节剂
公开(公告)号：US07947683B2
公开(公告)日：2011-05-24
申请号：US11911027
申请日：2006-04-12
申请人： Giorgio Bonanomi , Anna Checchia , Elettra Fazzolari , Dieter Hamprecht , Fabrizio Micheli , Luca Tarsi , Silvia Terreni
发明人： Giorgio Bonanomi , Anna Checchia , Elettra Fazzolari , Dieter Hamprecht , Fabrizio Micheli , Luca Tarsi , Silvia Terreni
IPC分类号： C07D249/08 , C07D403/14 , C07D401/14 , C07D263/30 , C07D417/14 , A61K31/4196 , A61K31/501 , A61K31/4439 , A61K31/426 , A61K31/4709 , A61P25/18
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salt thereof: 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 cognition impairment.
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：其制备方法，用于这些方法的中间体，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，例如，治疗药物依赖性，作为抗精神病药，治疗强迫性强迫症，早泄或认知障碍。

2. 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。

3. 发明申请

US20090221593A1 TRIAZOLE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 有权
标题翻译：作为DOPAMINE D3受体的调节剂的三唑衍生物
公开(公告)号：US20090221593A1
公开(公告)日：2009-09-03
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： A61K31/422 , C07D413/14 , A61K31/4709 , A61K31/423 , A61K31/498 , A61K31/506
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。

4. 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。

5. 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。

6. 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.

7. 发明申请

US20100152195A1 Azabicyclo (3.1.0) Hexane Derivatives Useful As Modulators Of Dopamine D3 Receptors 有权
公开(公告)号：US20100152195A1
公开(公告)日：2010-06-17
申请号：US12639129
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： A61K31/501 , C07D403/12 , C07D417/14 , A61K31/428 , A61K31/4196 , A61K31/4439 , C07D401/14 , A61K31/4965
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.

8. 发明申请

US20070142438A1 Azabicyclo (3.1.0.) hexane derivatives useful as modulators of dopamine d3 receptors 有权
公开(公告)号：US20070142438A1
公开(公告)日：2007-06-21
申请号：US10598200
申请日：2005-02-21
申请人： Luca Arista , Giorgio Bonanomi , Anna 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 Capelli , Federica Damiani , Romano Di Fabio , Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli , Luca Tarsi , Giovanna Tedesco , Silvia Terreni
IPC分类号： A61K31/4439 , A61K31/4196 , A61K31/428 , C07D417/14 , 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: 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, halo1-4alkoxy, 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, halo1-4alkyl, 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.

9. 发明申请

US20100016287A1 COMPOUNDS HAVING AFFINITY FOR DOPAMINE D3 RECEPTOR AND USES THEREOF" 失效
标题翻译：具有DOPAMINE D3受体的亲和性的化合物及其用途“
公开(公告)号：US20100016287A1
公开(公告)日：2010-01-21
申请号：US11569880
申请日：2005-05-31
申请人： Giorgio Bonanomi , Federica Damiani , Gabriella Gentile , Dieter Wolfgang Hamprecht , Fabrizio Micheli , Luca Tarsi , Giovanna Tedesco , Silvia Terreni
发明人： Giorgio Bonanomi , Federica Damiani , Gabriella Gentile , Dieter Wolfgang Hamprecht , Fabrizio Micheli , Luca Tarsi , Giovanna Tedesco , Silvia Terreni
IPC分类号： A61K31/55 , C07D498/04 , A61P25/00
CPC分类号： C07D513/04 , C07D487/04
摘要： Compounds of formula (I) wherein A is a 5 or 6 membered heteroaromatic ring or a 5 or 6 membered heterocyclic ring, and which are useful for treating mental disorders such as schizophrenia are set out herein.
摘要翻译：本文列出了其中A为5或6元杂芳环或5或6元杂环，可用于治疗精神障碍如精神分裂症的式（I）化合物。

10. 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。

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