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1. 发明申请

US20100004452A1 5-QUINOLINONE DERIVATIVES AS 5HT1A RECEPTOR MODULATORS FOR TREATING SEXUAL DYSFUNCTION, COGNITION IMPAIRMENT, PSYCHOTIC DISORDERS, ANXIETY, DEPRESSION, ETC. 审中-公开
标题翻译： 5-Quinolinone衍生物作为5HT1A受体调节剂，用于治疗性功能障碍，认知障碍，心理障碍，异常，呕吐等。
公开(公告)号：US20100004452A1
公开(公告)日：2010-01-07
申请号：US12442148
申请日：2007-09-24
申请人： Barbara Bertani , Steven Mark Bromidge , Massimo Gianotti , Alessandra Pasquarello , Valeria Zucchelli
发明人： Barbara Bertani , Steven Mark Bromidge , Massimo Gianotti , Alessandra Pasquarello , Valeria Zucchelli
IPC分类号： C07D401/14
CPC分类号： C07D401/12 , C07D401/14 , C07D487/08
摘要： Disclosed are compounds of formula (I) wherein R1 is C1-6alkyl, halo or haloC1-6alkyl; R2 is hydrogen or C1-6alkyl; is a single or double bond; each R3 and R4, which may be the same or different, are hydrogen, C1-6alkyl or haloC1-6alkyl; wherein i) when is a double bond p and q are 1, and ii) when is a single bond, p and q are 2, and one of R3 and one of R4, together with their interconnecting atoms, forms a cyclopropane ring which may be substituted by one or two halo or methyl groups, which groups may be the same or different; X is CH or N; when present each R5, which may be the same or different, is C1-6alkyl or halo; or two R5 groups may join to form a bridge, which bridge contains one or two atoms; n is 0, 1, 2 or 3; when present each R6 which may be the same or different, is C1-6alkyl or halo; and m is 0, 1, 2 or 3.
摘要翻译：公开了式（I）的化合物，其中R 1是C 1-6烷基，卤素或卤代C 1-6烷基; R2是氢或C1-6烷基; “img id =”CUSTOM-CHARACTER-00001“he =”2.79mm“wi =”6.35mm“file =”US20100004452A1-20100107-P00001.TIF“img-content =”character“img-format =”tif“/> 是单键或双键; 每个R 3和R 4可以相同或不同，是氢，C 1-6烷基或卤代C 1-6烷基; 其中i）当是双键p，q是1，ii）当是单键，p和q是2，R 3和R 4中的一个连同它们的互连原子一起形成环丙烷环，被一个或两个卤素或甲基取代，这些基团可以相同或不同; X是CH或N; 当存在时，每个可以相同或不同的R 5是C 1-6烷基或卤素; 或两个R5基团可以连接形成桥，该桥包含一个或两个原子; n为0,1,2或3; 当存在每个可以相同或不同的R 6是C 1-6烷基或卤素时; m为0,1,2或3。

2. 发明申请

US20090076274A1 BENZOXAZINONE DERIVATIVES, PREPARATION THEREOF AND USES IN THE TREATMENT OF CNS AND OTHER DISORDERS 审中-公开
标题翻译：苄唑胺酮衍生物，其制备方法和用于治疗CNS和其他疾病的用途
公开(公告)号：US20090076274A1
公开(公告)日：2009-03-19
申请号：US12269313
申请日：2008-11-12
申请人： Barbara Bertani , Manuela Borriello , Andrea Bozzoli , Steven Mark Bromidge , Enrica Granci , Colin Leslie , Halina Serfinowska , Luigi Stasi , Antonio Vong , Valeria Zucchelli
发明人： Barbara Bertani , Manuela Borriello , Andrea Bozzoli , Steven Mark Bromidge , Enrica Granci , Colin Leslie , Halina Serfinowska , Luigi Stasi , Antonio Vong , Valeria Zucchelli
IPC分类号： C07D405/02
CPC分类号： C07D413/12 , C07D265/36 , C07D413/14 , C07D471/04 , C07D495/04
摘要： Intermediates useful in the preparation of compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein A, R1, R2, R3, , p, q, and X are as defined in the specification.
摘要翻译：公开了可用于制备式（I）化合物及其可药用盐的中间体：其中A，R1，R2，R3，，p，q和X如规范中所定义。

3. 发明授权

US08217168B2 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：US08217168B2
公开(公告)日：2012-07-10
申请号：US12680792
申请日：2008-10-01
申请人： Barbara Bertani , Susanna Cremonesi , Stefano Fontana , Alessandra Pasquarello
发明人： Barbara Bertani , Susanna Cremonesi , Stefano Fontana , Alessandra Pasquarello
IPC分类号： C07D403/06 , C07D403/14 , C07D401/14 , C07D417/14 , C07D207/36 , C07D209/02 , A61K31/53 , A61P25/18 , A61P25/30 , A61P15/12
CPC分类号： C07D403/06 , C07D207/36 , C07D209/02 , C07D401/14 , C07D417/14
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; p is an integer ranging from 0 to 5; R1 is halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R6; and when p is an integer ranging from 2 to 5, each R1 may be the same or different; R2 is hydrogen or C1-4alkyl; n is 3, 4, 5 or 6; R6 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 R6 group is optionally substituted by one or two substituents selected from: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R4 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, C3-7 cycloalkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and NR′R″; or R4 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, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl, haloC1-4alkoxy and SF5; R7 is hydrogen or C1-2alkyl; 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; and their use in therapy, as modulators of dopamine D3 receptors.
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元杂芳基二环组; p为0〜5的整数。 R 1是卤素，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; 或对应于基团R6; 并且当p是2至5的整数时，每个R 1可以相同或不同; R2是氢或C1-4烷基; n为3,4,5或6; R6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，这些R 6基团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; R4选自：氢，卤素，羟基，氰基，C 1-4烷基，C 3-7环烷基，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NR'R“; 或R 4为苯基，5-14元杂环基; 任何这样的苯基或杂环基团任选被1,2,3或4个选自以下的取代基取代：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，卤代C 1-4烷氧基和SF5; R7是氢或C1-2烷基; R'是H，C 1-4烷基或C 1-4烷酰基; R“定义为R'; R'和R“与互连氮原子一起可以形成5-，6-元饱和或不饱和杂环; 及其在治疗中的用途，作为多巴胺D3受体的调节剂。

4. 发明授权

US08178549B2 Azabicyclo [3. 1. O] hexyl derivatives as modulators of dopamine D3 receptors 失效
标题翻译：氮杂双环[3。 O]己基衍生物作为多巴胺D3受体的调节剂
公开(公告)号：US08178549B2
公开(公告)日：2012-05-15
申请号：US12680785
申请日：2008-10-01
申请人： Barbara Bertani , Francesca Cardullo , Paolo Dambruoso , Paola Marzorati , Fabrizio Micheli , Alessandra Pasquarello , Catia Seri , Giovanna Tedesco
发明人： Barbara Bertani , Francesca Cardullo , Paolo Dambruoso , Paola Marzorati , Fabrizio Micheli , Alessandra Pasquarello , Catia Seri , Giovanna Tedesco
IPC分类号： C07D403/14 , C07D413/14 , A61K31/513
CPC分类号： C07D413/14 , C07D403/14 , C07D417/14 , C07D491/052
摘要： The present invention relates to novel compounds of formula (I) or a salt thereof: wherein R1 is a 5-membered heteroaryl group, optionally fused with a 6-membered hetero or carbocycle; such 5 or 11-membered system, may be 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, haloC1-4alkoxy and SF5; and n is 1 or 2; 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, or premature ejaculation.
摘要翻译：本发明涉及新的式（I）化合物或其盐：其中R 1是5元杂芳基，任选地与6元杂或碳环稠合; 这样的5或11元系可以任选被1,2,3或4个选自以下的取代基取代：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，卤代C 1-4烷基， 4烷氧基和SF5; n为1或2; 它们在治疗中的用途，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，治疗强迫性强迫性疾病或早泄。

5. 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。

6. 发明授权

US08163927B2 Azabicyclo [3.1.0] hexane derivatives as modulators of dopamine D3 receptors 失效
标题翻译：氮杂二环[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：US08163927B2
公开(公告)日：2012-04-24
申请号：US12295024
申请日：2007-03-30
申请人： Barbara Bertani , Fabrizio Micheli , Alessandra Pasquarello , Silvia Terreni
发明人： Barbara Bertani , Fabrizio Micheli , Alessandra Pasquarello , Silvia Terreni
IPC分类号： A61K31/4439 , A61K31/444
CPC分类号： C07D401/06 , C07D401/14
摘要： The present invention relates to certain azabicyclic compounds of formula (I)′: wherein the several groups are defined herein and 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）'的氮杂双环化合物：其中数个基团在本文中定义，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. 发明申请

US20060264429A1 Benzoxazinone derivatives, preparation thereof and uses in the treatment of cns and other disorders 审中-公开
标题翻译：苯并恶嗪酮衍生物，其制备方法及其用途
公开(公告)号：US20060264429A1
公开(公告)日：2006-11-23
申请号：US10535711
申请日：2003-11-20
申请人： Barbara Bertani , Manuela Borriello , Andrea Bozzoli , Steven Bromidge , Enrica Granci , Colin Leslie , Halina Serfinowska , Luigi Stasi , Antonio Vong , Valeria Zucchelli
发明人： Barbara Bertani , Manuela Borriello , Andrea Bozzoli , Steven Bromidge , Enrica Granci , Colin Leslie , Halina Serfinowska , Luigi Stasi , Antonio Vong , Valeria Zucchelli
IPC分类号： A61K31/538 , C07D417/14
CPC分类号： C07D413/12 , C07D265/36 , C07D413/14 , C07D471/04 , C07D495/04
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein A, R1, R2, R3, p, q, A and X are as defined in the specification. Preparation of the compounds and uses in the treatment of CNS and other disorders, including depression and anxiety, are also disclosed.
摘要翻译：公开了式（I）化合物及其药学上可接受的盐：其中A，R1，R2，R3，p，q，A和X如说明书中所定义。还公开了化合物的制备和用于治疗CNS和其它障碍，包括抑郁和焦虑的用途。

8. 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。

9. 发明申请

US20100210672A1 AZABICYCLO [3. 1. O] HEXYL DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 失效
标题翻译： AZABICYCLO [3。作为DOPAMINE D3受体的调节剂的HEXYL衍生物
公开(公告)号：US20100210672A1
公开(公告)日：2010-08-19
申请号：US12680785
申请日：2008-10-01
申请人： Barbara Bertani , Francesca Cardullo , Paolo Dambruoso , Paola Marzorati , Fabrizio Micheli , Alessandra Pasquarello , Catia Seri , Giovanna Tedesco
发明人： Barbara Bertani , Francesca Cardullo , Paolo Dambruoso , Paola Marzorati , Fabrizio Micheli , Alessandra Pasquarello , Catia Seri , Giovanna Tedesco
IPC分类号： A61K31/506 , C07D403/14 , A61P25/18 , A61P25/30
CPC分类号： C07D413/14 , C07D403/14 , C07D417/14 , C07D491/052
摘要： The present invention relates to novel compounds of formula (I) or a salt thereof: whereinR1 is a 5-membered heteroaryl group, optionally fused with a 6-membered hetero or carbocycle; such 5 or 11-membered system, may be 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, haloC1-4alkoxy and SF5; and n is 1 or 2; 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, or premature ejaculation.
摘要翻译：本发明涉及新的式（I）化合物或其盐：其中R 1是5元杂芳基，任选地与6元杂或碳环稠合; 这样的5或11元系可以任选被1,2,3或4个选自以下的取代基取代：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，卤代C 1-4烷基， 4烷氧基和SF5; n为1或2; 它们在治疗中的用途，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，治疗强迫性强迫性疾病或早泄。

10. 发明申请

US20100063097A1 Azabicyclo [3.1.0] Hexane Derivatives as Modulators of Dopamine D3 Receptors 失效
标题翻译：氮杂二环[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：US20100063097A1
公开(公告)日：2010-03-11
申请号：US12295024
申请日：2007-03-30
申请人： Barbara Bertani , Fabrizio Micheli , Alessandra Pasquarello , Silvia Terreni
发明人： Barbara Bertani , Fabrizio Micheli , Alessandra Pasquarello , Silvia Terreni
IPC分类号： A61K31/4439 , C07D401/06 , C07D401/14 , A61P25/00 , A61K31/444 , A61P25/30
CPC分类号： C07D401/06 , C07D401/14
摘要： The present invention relates to certain azabicyclic compounds of formula (I)′: wherein the several groups are defined herein and 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）'的氮杂双环化合物：其中数个基团在本文中定义，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。

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