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1. 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。

2. 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。

3. 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。

4. 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.

5. 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.

6. 发明授权

US07279474B2 Substituted pyrrolo[2,3-d]pyrimidines as antagonists of the corticotropin releasing factor (CRF) 失效
标题翻译：取代的吡咯并[2,3-d]嘧啶作为促肾上腺皮质激素释放因子（CRF）的拮抗剂
公开(公告)号：US07279474B2
公开(公告)日：2007-10-09
申请号：US10476368
申请日：2002-04-30
申请人： Anna Maria Capelli , Chiara Marchionni , Fabrizio Micheli , Alessandra Pasquarello , Benedetta Perini , Yves St-Denis , Romano Di Fabio
发明人： Anna Maria Capelli , Chiara Marchionni , Fabrizio Micheli , Alessandra Pasquarello , Benedetta Perini , Yves St-Denis , Romano Di Fabio
IPC分类号： A61K31/5355 , A61K31/519 , C07D487/04 , C07D413/14 , A61P25/24 , A61P25/22
CPC分类号： C07D487/04 , A61K51/0459 , A61K51/0463 , A61K51/0465 , C07D239/70 , C07D239/94 , C07D471/04
摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof wherein the variables are as defined in the description, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF)
摘要翻译：本发明提供了式（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，其中变量如本说明书所定义，其制备方法，含有它们的药物组合物及其在治疗由促肾上腺皮质激素释放因子（CRF）

7. 发明授权

US07863299B2 Triazolyl derivatives of azabicyclo [3.1.0] hexane as dopamine D3 receptor modulators 失效
标题翻译：氮杂双环[3.1.0]己烷的三唑基衍生物作为多巴胺D3受体调节剂
公开(公告)号：US07863299B2
公开(公告)日：2011-01-04
申请号：US12064118
申请日：2006-08-18
申请人： Anna Maria Capelli , Elettra Fazzolari , Fabrizio Micheli , Giovanna Tedesco , Silvia Terreni
发明人： Anna Maria Capelli , Elettra Fazzolari , Fabrizio Micheli , Giovanna Tedesco , Silvia Terreni
IPC分类号： A61K31/428 , A61K31/4196 , A61K31/4439 , C07D403/14 , C07D417/14
CPC分类号： C07D413/14
摘要： The present invention relates to novel compounds of formula (IC) or a salt thereof: wherein: 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; m1, m2, m3, and m4 are 0; m5, m6 and m7 are each independently 0, 1 or 2 wherein the sum of m5, m6 and m7 is 1 or 2; R6 is C1-6alkyl; R7 is halogen, C1-6alkyl or haloC1-6alkyl; 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; with the proviso that when m5=m6=1, R7 is not chlorine; 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：本发明涉及新型式（IC）化合物或其盐：其中：p为0至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; m1，m2，m3，m4为0; m5，m6和m7各自独立地为0,1或2，其中m5，m6和m7的和为1或2; R6是C1-6烷基; R7是卤素，C1-6烷基或卤代C 1-6烷基; 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; 条件是当m5 = m6 = 1时，R7不是氯; 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。

8. 发明授权

US08283474B2 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：US08283474B2
公开(公告)日：2012-10-09
申请号：US12639282
申请日：2009-12-16
申请人： Anna Maria Capelli , Giovanna Tedesco
发明人： Anna Maria Capelli , Giovanna Tedesco
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.
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。

9. 发明授权

US08835412B2 Isoxazolidine derivatives 有权
标题翻译：异恶唑烷衍生物
公开(公告)号：US08835412B2
公开(公告)日：2014-09-16
申请号：US13421128
申请日：2012-03-15
申请人： Eleonora Ghidini , Anna Maria Capelli
发明人： Eleonora Ghidini , Anna Maria Capelli
IPC分类号： A61K31/58 , C07J71/00
CPC分类号： C07J71/00 , C07J71/0068
摘要： Anti-inflammatory and antiallergic compounds of the glucocorticosteroid series according to formula (I) defined herein are useful for treating diseases of the respiratory tract characterized by airway obstruction.
摘要翻译：根据本文定义的式（I）的糖皮质激素系列的抗炎和抗过敏化合物可用于治疗以气道阻塞为特征的呼吸道疾病。

10. 发明申请

US20130035320A1 PYRROLIDINE DERIVATIVES 失效
标题翻译：吡咯烷衍生物
公开(公告)号：US20130035320A1
公开(公告)日：2013-02-07
申请号：US13561134
申请日：2012-07-30
申请人： Eleonora Ghidini , Anna Maria Capelli
发明人： Eleonora Ghidini , Anna Maria Capelli
IPC分类号： A61K31/58 , A61P37/08 , A61P29/00 , C07J71/00
CPC分类号： C07J71/0052 , A61K31/58
摘要： Novel anti-inflammatory and antiallergic compounds of the glucocorticosteroid series according to formulae (I) and (I′) are effective for the prevention and/or treatment of diseases in which the number, activity, and movement of inflammatory cells is implicated.
摘要翻译：根据式（I）和（I'）的糖皮质激素系列的新型抗炎和抗过敏化合物对于预防和/或治疗涉及炎症细胞的数量，活性和运动的疾病是有效的。

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