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1. 发明申请

US20100075968A1 Imidazolidine Carboxamide Derivatives as P2X7 Modulators 失效
标题翻译：咪唑烷羧酰胺衍生物作为P2X7调节剂
公开(公告)号：US20100075968A1
公开(公告)日：2010-03-25
申请号：US12594381
申请日：2008-04-02
申请人： Paul John Beswick , David Kenneth Dean , Robert James Gleave , Andrew Peter Moses , Daryl Simon Walter
发明人： Paul John Beswick , David Kenneth Dean , Robert James Gleave , Andrew Peter Moses , Daryl Simon Walter
IPC分类号： A61K31/5377 , C07D233/02 , A61K31/4164 , C07D401/02 , A61K31/4439 , C07D239/02 , A61K31/506 , A61K31/454 , C07D413/02 , C07D241/10 , A61K31/497 , C07D403/02 , A61K31/501 , A61P29/00 , A61P25/00
CPC分类号： C07D233/36 , C07D401/04 , C07D401/06 , C07D403/04
摘要： The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders/diseases mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease, in particular pain such as inflammatory pain, neuropathic pain or visceral pain.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐：该化合物或盐调节P2X7受体功能并且能够拮抗ATP在P2X7受体（P2X7受体拮抗剂）下的作用。本发明还提供了这样的化合物或其盐或其药物组合物在治疗或预防P2X7受体介导的病症/疾病中的用途，例如疼痛，炎症或神经变性疾病，特别是疼痛，例如炎性疼痛，神经性疼痛或内脏痛。

2. 发明授权

US07932282B2 Imidazolidine carboxamide derivatives as P2X7 modulators 失效
标题翻译：咪唑烷羧酰胺衍生物作为P2X7调节剂
公开(公告)号：US07932282B2
公开(公告)日：2011-04-26
申请号：US12594381
申请日：2008-04-02
申请人： Paul John Beswick , David Kenneth Dean , Robert James Gleave , Andrew Peter Moses , Daryl Simon Walter
发明人： Paul John Beswick , David Kenneth Dean , Robert James Gleave , Andrew Peter Moses , Daryl Simon Walter
IPC分类号： A61K31/4164 , C07D233/02
CPC分类号： C07D233/36 , C07D401/04 , C07D401/06 , C07D403/04
摘要： The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders/diseases mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease, in particular pain such as inflammatory pain, neuropathic pain or visceral pain.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐：该化合物或盐调节P2X7受体功能并能够拮抗ATP在P2X7受体（P2X7受体拮抗剂）下的作用。本发明还提供了这样的化合物或其盐或其药物组合物在治疗或预防P2X7受体介导的病症/疾病中的用途，例如疼痛，炎症或神经变性疾病，特别是疼痛，例如炎性疼痛，神经性疼痛或内脏痛。

3. 发明申请

US20110046137A1 Pyrazole Derivatives as P2X7 Modulators 审中-公开
标题翻译：吡唑衍生物作为P2X7调节剂
公开(公告)号：US20110046137A1
公开(公告)日：2011-02-24
申请号：US12599416
申请日：2008-05-08
申请人： Paul John Beswick , Laura Jane Chambers , Iain Patrick Chessell , David John Davies , Emmanuel Hubert Demont , Robert James Gleave , David George Hubert Livermore , Pamela Joan Theobald , Mythily Vimal , Daryl Simon Walter
发明人： Paul John Beswick , Laura Jane Chambers , Iain Patrick Chessell , David John Davies , Emmanuel Hubert Demont , Robert James Gleave , David George Hubert Livermore , Pamela Joan Theobald , Mythily Vimal , Daryl Simon Walter
IPC分类号： A61K31/415 , C07D231/12 , C07D403/06 , A61K31/4178 , C07D401/04 , A61K31/4439 , C07D417/04 , A61K31/427 , C07D403/04 , A61K31/501 , A61K31/506 , C07D471/08 , A61K31/439 , C07D413/06 , A61K31/5377 , A61P29/00 , A61P25/28
CPC分类号： C07D231/12 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/10 , C07D405/04 , C07D405/12 , C07D417/04 , C07D417/06 , C07D471/08
摘要： The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: The pyrazole derivatives of formula (I) or salts thereof modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also relates to the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders/diseases mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐：式（I）的吡唑衍生物或其盐调节P2X7受体功能，并能够拮抗ATP在P2X7受体（P2X7受体）拮抗剂）。本发明还涉及这些化合物或其盐或其药物组合物在治疗或预防P2X7受体介导的疾病/疾病中的用途，例如疼痛，炎症或神经变性疾病。

4. 发明申请

US20100168171A1 Piperidinone Carboxamide Derivatives as P2X7 Modulators 审中-公开
标题翻译：哌啶酮甲酰胺衍生物作为P2X7调节剂
公开(公告)号：US20100168171A1
公开(公告)日：2010-07-01
申请号：US12593044
申请日：2008-03-20
申请人： Paul John Beswick , Robert James Gleave , Jon Graham Anthony Steadman , Daryl Simon Walter
发明人： Paul John Beswick , Robert James Gleave , Jon Graham Anthony Steadman , Daryl Simon Walter
IPC分类号： A61K31/45 , C07D211/78 , A61P29/00 , A61P25/28
CPC分类号： C07D211/78
摘要： The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: The compounds or salts modulate P2X7 receptor function and are capable of interfering with the effects of ATP at the P2X7 receptor. The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease, in particular pain such as inflammatory pain, neuropathic pain or visceral pain.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐：该化合物或盐调节P2X7受体功能并能够干扰ATP在P2X7受体上的作用。本发明还提供了这样的化合物或其盐或其药物组合物在治疗或预防P2X7受体介导的病症中的用途，例如疼痛，炎症或神经变性疾病，特别是疼痛，例如炎性疼痛，神经性疼痛或内脏痛。

5. 发明申请

US20090149524A1 N-(Phenylmethyl)-2-(1H-Pyrazol-4-yl) Acetamide Derivatives as P2X7 Antagonists for the Treatment of Pain, Inflammation and Neurodegeneration 审中-公开
标题翻译： N-（苯基甲基）-2-（1H-吡唑-4-基）乙酰胺衍生物作为P2X7拮抗剂用于治疗疼痛，炎症和神经退行性疾病
公开(公告)号：US20090149524A1
公开(公告)日：2009-06-11
申请号：US12303260
申请日：2007-06-05
申请人： Paul John Beswick , Laura J. Chambers , David John Davies , David Kenneth Dean , Emmanuel Hubert Demont , Susan Roomans , Daryl Simon Walter
发明人： Paul John Beswick , Laura J. Chambers , David John Davies , David Kenneth Dean , Emmanuel Hubert Demont , Susan Roomans , Daryl Simon Walter
IPC分类号： A61K31/415 , C07D231/10 , A61P25/28
CPC分类号： C07D231/12
摘要： The present invention relates to novel pyrazole derivatives of formula (I) which bind to the P2X7 receptor and are capable of interfering with the effects of ATP at the P2X7 receptor: and the use of such compounds or pharmaceutical compositions thereof in the treatment of disorders mediated by the P2X7 receptor, for example pain, inflammation and neurodegeneration.
摘要翻译：本发明涉及结合P2X7受体并能够干扰ATP在P2X7受体上的作用的式（I）的吡唑衍生物，以及这些化合物或其药物组合物在治疗疾病介导中的用途通过P2X7受体，例如疼痛，炎症和神经变性。

6. 发明申请

US20100056595A1 Pyrazole Derivatives as P2X7 Modulators 审中-公开
标题翻译：吡唑衍生物作为P2X7调节剂
公开(公告)号：US20100056595A1
公开(公告)日：2010-03-04
申请号：US12595099
申请日：2008-04-10
申请人： Paul John Beswick , David Kenneth Dean , Daryl Simon Walter
发明人： Paul John Beswick , David Kenneth Dean , Daryl Simon Walter
IPC分类号： A61K31/415 , C07D231/12 , A61P25/00
CPC分类号： C07D231/16 , C07D231/12
摘要： The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 represents C1-6 alkyl or C3-6 cycloalkyl, either of which is optionally substituted with 1, 2 or 3 halogen atoms; and R2 represents hydrogen, halogen, C1-6 alkyl or C3-6 cycloalkyl; and either of said C1-6 alkyl or C3-6 cycloalkyl is optionally substituted with 1, 2 or 3 halogen atoms. The pyrazole compounds of formula (I) or salts thereof modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also relates to the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders/diseases mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐：其中R1表示C1-6烷基或C3-6环烷基，其任一个任选被1,2或3个卤素原子取代; 并且R 2表示氢，卤素，C 1-6烷基或C 3-6环烷基; 并且所述C 1-6烷基或C 3-6环烷基中的任一个任选被1,2或3个卤素原子取代。式（I）的吡唑化合物或其盐调节P2X7受体功能，并且能够拮抗ATP在P2X7受体（P2X7受体拮抗剂）下的作用。本发明还涉及这些化合物或其盐或其药物组合物在治疗或预防P2X7受体介导的疾病/疾病中的用途，例如疼痛，炎症或神经变性疾病。

7. 发明申请

US20100144727A1 Oxazolidine and Morpholine Carboxamide Derivatives as P2X7 Modulators 审中-公开
标题翻译：恶唑烷和吗啉酰胺衍生物作为P2X7调节剂
公开(公告)号：US20100144727A1
公开(公告)日：2010-06-10
申请号：US12593357
申请日：2008-03-20
申请人： Paul John Beswick , Daryl Simon Walter
发明人： Paul John Beswick , Daryl Simon Walter
IPC分类号： A61K31/421 , C07D263/20 , C07D265/32 , A61K31/5375 , A61P25/00 , A61P29/00
CPC分类号： C07D263/24 , C07D265/32
摘要： The present invention relates to a compound of formula (I): The compounds modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of such compounds, or pharmaceutical compositions thereof, in the treatment or prevention of disorders mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease, in particular pain such as inflammatory pain, neuropathic pain or visceral pain.
摘要翻译：本发明涉及式（I）化合物：该化合物调节P2X7受体功能并且能够拮抗ATP在P2X7受体上的作用。本发明还提供了这些化合物或其药物组合物在治疗或预防P2X7受体介导的病症中的用途，例如疼痛，炎症或神经变性疾病，特别是疼痛，例如炎性疼痛，神经性疼痛或内脏疼痛。

8. 发明申请

US20100210705A1 Pyrrole and Isoindole Carboxamide Derivatives as P2X7 Modulators 失效
标题翻译：吡咯和异吲哚羧酰胺衍生物作为P2X7调节剂
公开(公告)号：US20100210705A1
公开(公告)日：2010-08-19
申请号：US12532868
申请日：2008-03-20
申请人： Robert James Gleave , David George Hubert Livermore , Daryl Simon Walter
发明人： Robert James Gleave , David George Hubert Livermore , Daryl Simon Walter
IPC分类号： A61K31/4035 , C07D207/38 , A61K31/4015 , C07D209/46 , A61P25/28 , A61P1/00 , A61P19/02
CPC分类号： C07D207/38 , C07D209/46
摘要： The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein: R2 represents hydrogen, halogen, C1-6 alkyl, C6-10 arylmethyl-, C2-6 alkenyl, C2-6 alkynyl or C3-6 cycloalkylmethyl-; and any of said C1-6 alkyl, C6-10 arylmethyl-, C2-6 alkenyl, C2-6 alkynyl or C3-6 cycloalkylmethyl- is optionally substituted with 1, 2 or 3 halogen atoms; and R3 represents hydrogen, fluorine or methyl; or R2 and R3 together with the carbon atoms to which they are attached form a benzene ring optionally substituted with 1, 2 or 3 substituents, which may be the same or different, selected from the group consisting of C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl. The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment of disorders mediated by the P2X7 receptor, for example pain, inflammation or neurodegeneration.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐：其中：R 2表示氢，卤素，C 1-6烷基，C 6-10芳甲基 - ，C 2-6烯基，C 2-6炔基或C 3 -C 6炔基， 6环烷基甲基 - ; 任何所述C 1-6烷基，C 6-10芳基甲基 - ，C 2-6烯基，C 2-6炔基或C 3-6环烷基甲基 - 任选被1,2或3个卤原子取代; 并且R 3表示氢，氟或甲基; 或R 2和R 3与它们所连接的碳原子一起形成任选被1,2或3个取代基取代的苯环，所述取代基可以相同或不同，选自C 1-6烷基，C 2-6 烯基和C 2-6炔基。化合物或盐调节P2X7受体功能，并能够拮抗ATP在P2X7受体上的作用。本发明还提供了这些化合物或其盐或其药物组合物在治疗P2X7受体介导的病症中的用途，例如疼痛，炎症或神经变性。

9. 发明申请

US20090197928A1 Novel Receptor Antagonists and Their Methods of Use 审中-公开
标题翻译：新型受体拮抗剂及其使用方法
公开(公告)号：US20090197928A1
公开(公告)日：2009-08-06
申请号：US12303262
申请日：2007-06-05
申请人： Paul John Beswick , Daryl Simon Walter
发明人： Paul John Beswick , Daryl Simon Walter
IPC分类号： A61K31/42 , C07D261/06 , A61P25/28
CPC分类号： C07D261/08
摘要： The present invention relates to novel isoxazole derivatives of formula (I) which bind to the P2X7 receptor and are capable of interfering with the effects of ATP at the P2X7 receptor: and the use of such compounds or pharmaceutical compositions thereof in the treatment of disorders mediated by the P2X7 receptor, for example pain, inflammation and neurodegeneration.
摘要翻译：本发明涉及结合P2X7受体并能够干扰ATP在P2X7受体上的作用的式（I）的异恶唑衍生物，以及这些化合物或其药物组合物在治疗疾病介导中的应用通过P2X7受体，例如疼痛，炎症和神经变性。

10. 发明授权

US07935832B2 Pyrrole and isoindole carboxamide derivatives as P2X7 modulators 失效
标题翻译：吡咯和异吲哚羧酰胺衍生物作为P2X7调节剂
公开(公告)号：US07935832B2
公开(公告)日：2011-05-03
申请号：US12532868
申请日：2008-03-20
申请人： Robert James Gleave , David George Hubert Livermore , Daryl Simon Walter
发明人： Robert James Gleave , David George Hubert Livermore , Daryl Simon Walter
IPC分类号： C07D209/44 , C07D207/24 , C07D213/02 , C07D401/06 , A61K31/44 , A61K31/40
CPC分类号： C07D207/38 , C07D209/46
摘要： The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein: R2 represents hydrogen, halogen, C1-6 alkyl, C6-10 arylmethyl-, C2-6 alkenyl, C2-6 alkynyl or C3-6 cycloalkylmethyl-; and any of said C1-6 alkyl, C6-10 arylmethyl-, C2-6 alkenyl, C2-6 alkynyl or C3-6 cycloalkylmethyl- is optionally substituted with 1, 2 or 3 halogen atoms; and R3 represents hydrogen, fluorine or methyl; or R2 and R3 together with the carbon atoms to which they are attached form a benzene ring optionally substituted with 1, 2 or 3 substituents, which may be the same or different, selected from the group consisting of C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl. The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment of disorders mediated by the P2X7 receptor, for example pain, inflammation or neurodegeneration.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐：其中：R 2表示氢，卤素，C 1-6烷基，C 6-10芳甲基 - ，C 2-6烯基，C 2-6炔基或C 3 -C 6炔基， 6环烷基甲基 - ; 任何所述C 1-6烷基，C 6-10芳基甲基 - ，C 2-6烯基，C 2-6炔基或C 3-6环烷基甲基 - 任选被1,2或3个卤素原子取代; 并且R 3表示氢，氟或甲基; 或R 2和R 3与它们所连接的碳原子一起形成任选被1,2或3个取代基取代的苯环，所述取代基可以相同或不同，选自C 1-6烷基，C 2-6 烯基和C 2-6炔基。化合物或盐调节P2X7受体功能，并能够拮抗ATP在P2X7受体上的作用。本发明还提供了这些化合物或其盐或其药物组合物在治疗P2X7受体介导的病症中的用途，例如疼痛，炎症或神经变性。

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