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1. 发明申请

WO2005087764A1 TETRAHYDROBENZAZEPINE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS (ANTIPSYCHOTIC AGENTS) 审中-公开
标题翻译：作为DOPAMINE D3受体（抗生素代谢物）的调节剂的四氢苯并噻吩衍生物
公开(公告)号：WO2005087764A1
公开(公告)日：2005-09-22
申请号：PCT/EP2005/002635
申请日：2005-03-04
申请人： GLAXO GROUP LIMITED , ARISTA, Luca , BONANOMI, Giorgio , DAMIANI, Federica , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna
发明人： ARISTA, Luca , BONANOMI, Giorgio , DAMIANI, Federica , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna
IPC分类号： C07D413/14
CPC分类号： C07D403/14 , C07D401/14 , C07D413/14
摘要： The present invention relates to novel compounds of formula (I) or a 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 D 3 receptors, e.g. as agents to treat various aspects 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，例如，作为治疗各方面药物依赖的药剂或作为抗精神病药。

2. 发明申请

WO2005080382A1 AZABICYCLO (3.1.0) HEXANE DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
标题翻译： AZ Y Y 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 S S S S
公开(公告)号：WO2005080382A1
公开(公告)日：2005-09-01
申请号：PCT/EP2005/001940
申请日：2005-02-21
申请人： GLAXO GROUP LIMITED , ARISTA, Luca , BONANOMI, Giorgio , CAPELLI, Anna Maria , DAMIANI, Federica , DI FABIO, Romano , GENTILE, Gabriella , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna , TERRENI, Silvia
发明人： ARISTA, Luca , BONANOMI, Giorgio , CAPELLI, Anna Maria , DAMIANI, Federica , DI FABIO, Romano , GENTILE, Gabriella , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D403/12
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; R 1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl; or corresponds to a group R 5 ; R 2 is hydrogen or C 1-4 alkyl; R 3 is C 1-4 alkyl; R 4 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, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyl; R 5 is a moiety selected from the group consisting of: isoxazolyl, -CH 2 -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, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyl; and when R 1 is chlorine and p is 1, such R 1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R 1 corresponds to R 5 , 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 D 3 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。

3. 发明申请

WO2006133945A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2006133945A1
公开(公告)日：2006-12-21
申请号：PCT/EP2006/005767
申请日：2006-06-13
申请人： GLAXO GROUP LIMITED , ARISTA, Luca , BONANOMI, Giorgio , HAMPRECHT, Dieter , MICHELI, Fabrizio
发明人： ARISTA, Luca , BONANOMI, Giorgio , HAMPRECHT, Dieter , MICHELI, Fabrizio
IPC分类号： C07D403/12 , A61K31/41 , A61P25/00
CPC分类号： C07D403/12
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; R 1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C 1-4 alkyl, halo C 1-4 alkyl, C 1-4 alkoxy, halo C 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to a group R 5 ; R 2 is hydrogen or C 1-4 alkyl; R 3 is C 1-4 alkyl; R 4 is hydrogen, C 1-4 alkyl or C 1-6 cycloalkyl optionally substituted by 1or 2 substituents selected from the group consisting of: halogen, cyano, C 1-4 alkyl, halo C 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyl; R 5 is a moiety selected from the group consisting of: isoxazolyl, -CH 2 -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, C 1-4 alkyl, halo C 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyl; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D 3 receptors, e.g. to treat drug dependency, or as antipsychotic agents, or 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，卤素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R 5; R 2是氢或C 1-4烷基; R 3是C 1-4烷基; R 4是氢，任选被1或2个选自以下的取代基取代的C 1-4 - 烷基或C 1-6 - 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; R 5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，并且这样的基团任选地被一个或两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; 其制备方法，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D 3受体的调节剂，例如。治疗药物依赖性，或作为抗精神病药物，或治疗强迫性强迫性疾病或早泄。

4. 发明申请

WO2006133946A1 AZAB I CYCLO [3 . 1 . 0] HEXANE DERIVATIVES AS DOPAMIN D3 RECEPTOR MODULATORS 审中-公开
标题翻译： AZAB I CYCLO [3。 1。 0] HEXANE衍生物作为DOPAMIN D3受体调节剂
公开(公告)号：WO2006133946A1
公开(公告)日：2006-12-21
申请号：PCT/EP2006/005768
申请日：2006-06-13
申请人： GLAXO GROUP LIMITED , ARISTA, Luca , CARDULLO, Francesca , CHECCHIA, Anna , HAMPRECHT, Dieter , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
发明人： ARISTA, Luca , CARDULLO, Francesca , CHECCHIA, Anna , HAMPRECHT, Dieter , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D403/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D413/14 , C07D401/14 , A61K31/435 , A61K31/41 , A61P25/00
CPC分类号： C07D417/14 , C07D401/14 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salt thereof: (I), processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D 3 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：（I）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D的调节剂 > 3个受体，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。

5. 发明申请

WO2007022934A2 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2007022934A2
公开(公告)日：2007-03-01
申请号：PCT/EP2006/008201
申请日：2006-08-18
申请人： GLAXO GROUP LIMITED , ARISTA, Luca , CHECCHIA, Anna , GENTILE, Gabriella , HAMPRECHT, Dieter , MICHELI, Fabrizio
发明人： ARISTA, Luca , CHECCHIA, Anna , GENTILE, Gabriella , HAMPRECHT, Dieter , MICHELI, Fabrizio
IPC分类号： C07D403/06 , C07D403/12
CPC分类号： C07D403/06 , C07D403/12
摘要： The present invention relates to novel compounds of formula (I) or a salt thereof: Formula (I), wherein: p is 0, 1, 2, 3, 4 or 5; R 1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; n is 3 or 4; R 2 is hydrogen or C 1-4 alkyl; n is 2 or 3; X is -CH 2 -, -O- or -S-; Z may be -CH- or N; A is a group P or P1, wherein P is Formula (Ia)and P1 is Formula (Ib) ; and Y is hydrogen, -OH, C 1-4 alkyl, haloC 1-4 alkyl, 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, C 1-4 alkoxy and haloC 1-4 alkoxy; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D 3 receptors, e.g. to treat substace 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：式（I），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; R 2是氢或C 1-4烷基; n为2或3; X是-CH 2 - ， - O-或-S-; Z可以是-CH-或N; A是基团P或P1，其中P是式（Ia），P1是式（Ib）; 和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取代选自一个或两个选自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; 其制备方法，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D 3受体的调节剂，例如。治疗类别相关疾病，作为抗精神病药物早泄或认知障碍。

6. 发明申请

WO2006087169A1 COMPOUNDS WHICH POTENTIATE GLUTAMATE RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：可能的谷氨酸受体的化合物及其在医药中的应用
公开(公告)号：WO2006087169A1
公开(公告)日：2006-08-24
申请号：PCT/EP2006/001342
申请日：2006-02-13
申请人： GLAXO GROUP LIMITED , ANDREOTTI, Daniele , ARISTA, Luca , CARDULLO, Francesca , SPADA, Simone , THEWLIS, Kevin, Michael , WARD, Simon, Edward
发明人： ANDREOTTI, Daniele , ARISTA, Luca , CARDULLO, Francesca , SPADA, Simone , THEWLIS, Kevin, Michael , WARD, Simon, Edward
IPC分类号： C07D213/61 , C07D213/42 , C07D317/58 , C07D333/20 , C07D213/65 , C07D277/64 , A61K31/4418 , A61K31/36 , A61K31/381 , A61K31/426 , A61P25/18
CPC分类号： C07D277/64 , C07D213/42 , C07D213/61 , C07D213/65 , C07D317/58 , C07D333/20
摘要： This invention relates to potentiation of the glutamate receptor by novel compounds of formula (I): The invention also relates to the use of the derivatives in treating diseases and conditions mediated by potentiation of the glutamate receptor, compositions containing the derivatives and processes for their preparation.
摘要翻译：本发明涉及通过式（I）的新化合物增强谷氨酸受体：本发明还涉及该衍生物在治疗由谷氨酸受体增强介导的疾病和病症中的用途，含有衍生物的组合物及其制备方法。

7. 发明申请

WO2004099143A1 CYCLIC AMINE DERIVATIVES, PROCESSES FOR THEIR PREPARATION, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：循环胺衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：WO2004099143A1
公开(公告)日：2004-11-18
申请号：PCT/EP2004/005005
申请日：2004-05-07
申请人： GLAXO GROUP LIMITED , ALVARO, Giuseppe , ARISTA, Luca , CARDULLO, Francesca , D'ADAMO, Lucilla , FERIANI, Aldo , GIOVANNINI, Riccardo , SERI, Catia
发明人： ALVARO, Giuseppe , ARISTA, Luca , CARDULLO, Francesca , D'ADAMO, Lucilla , FERIANI, Aldo , GIOVANNINI, Riccardo , SERI, Catia
IPC分类号： C07D211/34
CPC分类号： C07D405/04 , C07D211/34 , C07D405/12
摘要： A compound of formula (I) wherein R represents a radical selected from i) ii) iii) iv) where the substituents R1, R2, R3, R4, R4, R 7 and the indices m, n and p are as defined in the description; 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.
摘要翻译：式（I）化合物，其中R表示选自i）ii）iii）iv）中的基团，其中取代基R 1，R 2，R 3，R 4，R 4，R 7和索引m，n和p如说明书中所定义 ; 或其药学上可接受的盐和溶剂合物; 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. 发明申请

WO2022266426A1 6-(HETEROCYCLOALKYL-OXY)-QUINAZOLINE DERIVATIVES AND USES THEREOF 审中-公开
公开(公告)号：WO2022266426A1
公开(公告)日：2022-12-22
申请号：PCT/US2022/033963
申请日：2022-06-17
申请人： BLACK DIAMOND THERAPEUTICS, INC. , WRONA, Iwona , LUCAS, Matthew C. , CIBLAT, Stephane , PADILLA, Fernando , ARISTA, Luca , FLOHR, Alexander , JEWETT, Ivan
发明人： WRONA, Iwona , LUCAS, Matthew C. , CIBLAT, Stephane , PADILLA, Fernando , ARISTA, Luca , FLOHR, Alexander , JEWETT, Ivan
IPC分类号： A61P35/00 , C07D401/12 , C07D401/14 , C07D471/04 , C07D487/04 , C07D519/00 , A61K31/517 , A61K31/519
摘要： The present disclosure relates to compounds of Formula (I): and pharmaceutically acceptable salts and stereoisomers thereof, useful in the treatment of cancers associated with ErbB oncogenic activity, including methods of preparing the compounds, compositions comprising the compounds, and methods of using the compounds (e.g., in the treatment of cancer).

9. 发明申请

WO2022266425A1 3-CYANO-QUINOLINE DERIVATIVES AND USES THEREOF 审中-公开
公开(公告)号：WO2022266425A1
公开(公告)日：2022-12-22
申请号：PCT/US2022/033962
申请日：2022-06-17
申请人： BLACK DIAMOND THERAPEUTICS, INC. , WRONA, Iwona , LUCAS, Matthew C. , CIBLAT, Stephane , PADILLA, Fernando , ARISTA, Luca , FLOHR, Alexander
发明人： WRONA, Iwona , LUCAS, Matthew C. , CIBLAT, Stephane , PADILLA, Fernando , ARISTA, Luca , FLOHR, Alexander
IPC分类号： A61P35/00 , C07D401/04 , C07D401/12 , C07D471/04 , C07D519/00
摘要： The present disclosure relates to compounds of Formula (I): and pharmaceutically acceptable salts and stereoisomers thereof, useful in the treatment of cancers associated with ErbB oncogenic activity, including methods of preparing the compounds, compositions comprising the compounds, and methods of using the compounds (e.g., in the treatment of cancer).

10. 发明申请

WO2022170052A1 QUINAZOLINE DERIVATIVES, PYRIDOPYRIMIDINE DERIVATIVES, PYRIMIDOPYRIMIDINE DERIVATIVES, AND USES THEREOF 审中-公开
公开(公告)号：WO2022170052A1
公开(公告)日：2022-08-11
申请号：PCT/US2022/015249
申请日：2022-02-04
申请人： BLACK DIAMOND THERAPEUTICS, INC. , ARISTA, Luca , FLOHR, Alexander
发明人： ARISTA, Luca , FLOHR, Alexander
IPC分类号： C07D401/12 , C07D239/94 , C07D403/12 , C07C217/58 , A61P35/00
摘要： The present disclosure relates to compounds of Formula (I) or a stereoisomer, polymorph, hydrate, solvate, or pharmaceutically acceptable salt thereof. The present disclosure also relates to uses of the compounds, e.g., in treating or preventing cancer.

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