专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US06861429B2 2,3-diaryl-pyrazolo[1,5-b]pyridazines derivatives, their preparation and their use as cyclooxygenase 2 (COX-2) inhibitors 失效
标题翻译： 2,3-二芳基 - 吡唑并[1,5-b]哒嗪衍生物，其制备及其作为环加氧酶2（COX-2）抑制剂的用途
公开(公告)号：US06861429B2
公开(公告)日：2005-03-01
申请号：US10212513
申请日：2002-08-05
申请人： Paul John Beswick , Charanjit Bountra , Ian Baxter Campbell , Neil Matthews , Alan Naylor
发明人： Paul John Beswick , Charanjit Bountra , Ian Baxter Campbell , Neil Matthews , Alan Naylor
IPC分类号： A61K31/00 , A61K31/50 , A61K31/5025 , A61P1/04 , A61P3/10 , A61P7/06 , A61P9/00 , A61P11/00 , A61P11/06 , A61P17/00 , A61P17/02 , A61P19/02 , A61P19/06 , A61P25/06 , A61P25/16 , A61P25/28 , A61P27/02 , A61P27/16 , A61P29/00 , A61P35/00 , C07D487/04 , A61K31/4985
CPC分类号： C07D487/04 , A61K31/50 , Y02P20/55
摘要： The invention provides a pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt, solvate, ester or salt or solvate of such ester, of a compound of formula (I) in which: R0 is halogen, C1-6alkyl, C1-6alkoxy, C1-6alkoxy substituted by one or more fluorine atoms, or O(CH2)nNR4R5; R1 and R2 are independently selected from H, C1-6alkyl, C1-6alkyl substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5, (CH2)nSC1-6alkyl or C(O)NR4R5; with the proviso that when R0 is at the 4-position and is halogen, at least one of R1 and R2 is C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5 or (CH2)nSC1-6alkyl, C(O)NR4R5; R3 is C1-6alkyl or NH2; R4 and R5 are independently selected from H and C1-6alkyl or, together with the nitrogen atom to which they are attached, form a 4-8 membered saturated ring; and n is 1-4; and a sodium channel inhibitor.
摘要翻译：本发明提供包含式（I）化合物或其药学上可接受的盐，溶剂化物，酯或盐或溶剂合物的药物组合物，其中：R 0是卤素，C1 1-6烷基，C 1-6烷氧基，被一个或多个氟原子取代的C 1-6烷氧基，或O（CH 2）n NR 4 R 5; R 1和R 2独立地选自H，C 1-6烷基被一个或多个氟原子取代的C 1-6烷基，C 1-6烷氧基，C 1-6羟烷基，SC 1-6烷基，C（O）H，C（O）C 1-6烷基，C 1-6烷基磺酰基，被一个或多个氟原子，O（CH 2）n CO 2 C 1-6烷基，O（CH 2）nSC 1-6烷基，（CH 2）n NR 4 R 5，（CH 2）nSC 1-6烷基或C（O）NR 4 R 5 ; 条件是当R 0在4-位且是卤素时，R 1和R 2中的至少一个是C 1-6烷基磺酰基，被一个或多个氟原子取代的C 1-6烷氧基，O（ O（CH 2）n C 1-6烷基，（CH 2）n NR 4 R 5或（CH 2）nSC 1-6烷基，C（O）NR 4 R 5; R 3，是C 1-6烷基或NH 2; R 4和R 5独立地选自H和C 1-6烷基，或与它们所连接的氮原子一起形成4-8元饱和环; 和n为1-4;和钠通道抑制剂。

2. 发明授权

US06451794B1 2,3-Diaryl-pyrazolo[1,5-b]pyridazines derivatives, their preparation and their use as cyclooxygenase 2(COX-2) inhibitors 失效
标题翻译： 2,3-二芳基 - 吡唑并[1,5-b]哒嗪衍生物，其制备及其作为环氧合酶2（COX-2）抑制剂的用途
公开(公告)号：US06451794B1
公开(公告)日：2002-09-17
申请号：US09508029
申请日：2000-06-13
申请人： Paul John Beswick , Ian Baxter Campbell , Neil Mathews , Alan Naylor
发明人： Paul John Beswick , Ian Baxter Campbell , Neil Mathews , Alan Naylor
IPC分类号： A61K314985
CPC分类号： C07D487/04 , A61K31/50 , Y02P20/55
摘要： The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof in which: R0 is halogen, C1-6alkyl, C1-6alkoxy, C1-6alkoxy substituted by one or more fluorine atoms, or O(CH2)nNR4R5; R1 and R2 are independently selected from H, C1-6alkyl, C1-6alkyl, substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5, (CH2)nSC1-6alkyl or C(O)NR4R5; with the proviso that when R0 is at the 4-position and is halogen, at least one of R1 and R2 is C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5 or (CH2)nSC1-6alkyl, C(O)NR4R5; R3 is C1-6alkyl or NH2; R4 and R5 are independently selected from H, or C1-6alkyl or, together with the nitrogen atom to which they are attached, form a 4-8 membered saturated ring; and n is 1-4. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.
摘要翻译：本发明提供式（I）化合物及其药学上可接受的衍生物，其中：R 0是卤素，C 1-6烷基，C 1-6烷氧基，被一个或多个氟原子取代的C 1-6烷氧基或O（CH 2）n NR 4 R 5; R 1和R 2独立地选自被一个或多个氟原子取代的H，C 1-6烷基，C 1-6烷基，C 1-6烷氧基，C 1-6羟烷基，SC 1-6烷基，C（O）H，C（O）C 1-6烷基（C 1-6烷基磺酰基），被一个或多个氟原子取代的C 1-6烷氧基，O（CH 2）n CO 2 C 1-6烷基，O（CH 2）nSC 1-6烷基，（CH 2）n NR 4 R 5，（CH 2）nSC 1-6烷基或C（O）NR 4 R 5; 条件是当R 0在4-位且是卤素时，R 1和R 2中的至少一个是C 1-6烷基磺酰基，被一个或多个氟原子取代的C 1-6烷氧基，O（CH 2）n CO 2 C 1-6烷基，O（CH 2））nSC1-6烷基，（CH2）nNR4R5或（CH2）nSC1-6烷基，C（O）NR4R5; R3是C1-6烷基或NH2; R 4和R 5独立地选自H或C 1-6烷基，或与它们所连接的氮原子一起形成4-8元饱和环; n为1-4。式（I）化合物是COX-2的有效和选择性抑制剂，可用于治疗疼痛，发热，各种病症和疾病的炎症。

3. 发明授权

US06831097B2 2,3-diaryl-pyrazolo[1,5-B]pyridazines derivatives, their preparation and their use as cyclooxygenase 2 (COX-2) inhibitors 失效
标题翻译： 2,3-二芳基 - 吡唑并[1,5-B]哒嗪衍生物，它们的制备及其作为环加氧酶2（COX-2）抑制剂的用途
公开(公告)号：US06831097B2
公开(公告)日：2004-12-14
申请号：US10212514
申请日：2002-08-05
申请人： Paul John Beswick , Ian Baxter Campbell , Neil Mathews , Alan Naylor
发明人： Paul John Beswick , Ian Baxter Campbell , Neil Mathews , Alan Naylor
IPC分类号： A61K315025
CPC分类号： C07D487/04 , A61K31/50 , Y02P20/55
摘要： The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof in which: R0 is halogen, C1-6alkyl, C1-6alkoxy, C1-6alkoxy substituted by one or more fluorine atoms, or O(CH2)nNR4R5; R1 and R2 are independently selected from H, C1-6alkyl, C1-6alkyl substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5, (CH2)nSC1-6alkyl or C(O)NR4R5; with the proviso that when R0 is at the 4-position and is halogen, at least one of R1 and R2 is C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5 or (CH2)nSC1-6alkyl, C(O)NR4R5; R3 is C1-6alkyl or NH2; R4 and R5 are independently selected from H, or C1-6alkyl or, together with the nitrogen atom to which they are attached, form a 4-8 membered saturated ring; and n is 1-4. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.
摘要翻译：本发明提供式（I）化合物及其药学上可接受的衍生物，其中：R 0是卤素，C 1-6烷基，C 1-6烷氧基，被一个或多个氟原子取代的C 1-6烷氧基或O（CH 2）n NR R 5和R 2独立地选自H，C 1-6烷基，被一个或多个氟原子取代的C 1-6烷基，C 1-6烷氧基，C 1-6羟烷基，SC 1-6烷基， C（O）H，C（O）C 1-6烷基，C 1-6烷基磺酰基，被一个或多个氟原子取代的C 1-6烷氧基，O（CH 2）n CO 2 C 1-6烷基，O（CH 2）nSC 1-6烷基，（CH 2）n NR R 5，（CH 2）nSC 1-6烷基或C（O）NR 4 R 5; 条件是当R 0在4-位且是卤素时，R 1和R 2中的至少一个是C 1-6烷基磺酰基，被一个或多个氟原子取代的C 1-6烷氧基，O（ O（CH 2）n C 1-6烷基，（CH 2）n NR 4 R 5或（CH 2）nSC 1-6烷基，C（O）NR 4 R 5; R 3，是C 1-6烷基或NH 2; R 4和R 5独立地选自H或C 1-6烷基，或与它们所连接的氮原子一起形成4-8元饱和环; 而且是1-4.式（I）的化合物是COX-2的有效和选择性抑制剂，并且可用于治疗疼痛，发热，各种病症和疾病的炎症。

4. 发明授权

US08288388B2 3-pyridylcarbonyl-piperazinylsulfonyl derivatives 有权
标题翻译： 3-吡啶基羰基 - 哌嗪基磺酰基衍生物
公开(公告)号：US08288388B2
公开(公告)日：2012-10-16
申请号：US12503125
申请日：2009-07-15
申请人： Paul John Beswick , Alister Campbell , Andrew Cridland , Robert James Gleave , Jag Paul Heer , Neville Hubert Nicholson , Lee William Page , Sadie Vile
发明人： Paul John Beswick , Alister Campbell , Andrew Cridland , Robert James Gleave , Jag Paul Heer , Neville Hubert Nicholson , Lee William Page , Sadie Vile
IPC分类号： A61K31/496 , C07D401/06
CPC分类号： C07D213/81
摘要： The present invention relates to novel piperazine derivatives; to processes for their preparation; to pharmaceutical compositions containing the derivatives; and to the use of the derivatives in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial.
摘要翻译：本发明涉及新的哌嗪衍生物; 进行准备; 含有该衍生物的药物组合物; 以及在治疗中使用衍生物治疗阻断Cav2.2钙通道有益的疾病。

5. 发明授权

US06495606B1 Nitric oxide synthase inhibitors 失效
公开(公告)号：US06495606B1
公开(公告)日：2002-12-17
申请号：US09994969
申请日：2001-11-26
申请人： Paul John Beswick , Savvas Kleanthous , Robert John Young
发明人： Paul John Beswick , Savvas Kleanthous , Robert John Young
IPC分类号： A61K3113
CPC分类号： C07C323/58 , Y02P20/55
摘要： The present invention relates to novel amidino compounds of formula (I), or a salt, solvate, or physiologically functional derivative thereof; wherein R1 is selected from C1-4 alkyl, C3-4 cycloalkyl, C1-4 hydroxyalkyl, and C1-4 haloalkyl; to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use as selective inhibitors of inducible nitric oxide synthase.

6. 发明申请

US20120302746A1 3-PYRIDYLCARBONYL-PIPERAZINYLSULFONYL DERIVATIVES 有权
标题翻译： 3-吡啶基亚苄基 - 哌嗪基衍生物
公开(公告)号：US20120302746A1
公开(公告)日：2012-11-29
申请号：US13568211
申请日：2012-08-07
申请人： Paul John Beswick , Alister Campbell , Andrew Cridland , Robert James Gleave , Jag Paul Heer , Neville Hubert Nicholson , Lee William Page , Sadie Vile
发明人： Paul John Beswick , Alister Campbell , Andrew Cridland , Robert James Gleave , Jag Paul Heer , Neville Hubert Nicholson , Lee William Page , Sadie Vile
IPC分类号： C07D401/06 , C07D401/14 , C07D405/14 , C07D413/14
CPC分类号： C07D213/81
摘要： The present invention relates to novel piperazine derivatives; to processes for their preparation; to pharmaceutical compositions containing the derivatives; and to the use of the derivatives in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial.
摘要翻译：本发明涉及新的哌嗪衍生物; 进行准备; 含有该衍生物的药物组合物; 以及在治疗中使用衍生物治疗阻断Cav2.2钙通道有益的疾病。

7. 发明申请

US20100022555A1 Novel Derivatives 有权
标题翻译：新型衍生品
公开(公告)号：US20100022555A1
公开(公告)日：2010-01-28
申请号：US12503125
申请日：2009-07-15
申请人： Paul John Beswick , Alister Campbell , Andrew Cridland , Robert James Gleave , Jag Paul Heer , Neville Hubert Nicholson , Lee William Page , Sadie Vile
发明人： Paul John Beswick , Alister Campbell , Andrew Cridland , Robert James Gleave , Jag Paul Heer , Neville Hubert Nicholson , Lee William Page , Sadie Vile
IPC分类号： A61K31/497 , C07D401/06 , A61P25/00 , A61P29/00
CPC分类号： C07D213/81
摘要： The present invention relates to novel piperazine derivatives; to processes for their preparation; to pharmaceutical compositions containing the derivatives; and to the use of the derivatives in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial.
摘要翻译：本发明涉及新型哌嗪衍生物; 进行准备; 含有该衍生物的药物组合物; 以及在治疗中使用衍生物治疗阻断Cav2.2钙通道有益的疾病。

8. 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。

9. 发明授权

US07196107B2 Thia-and oxazoles and their use as ppars activators 失效
标题翻译： Thia和恶唑及其作为ppars激活剂的用途
公开(公告)号：US07196107B2
公开(公告)日：2007-03-27
申请号：US10451307
申请日：2001-12-18
申请人： Paul John Beswick , Vipulkumar Patel , Michael Lawrence Sierra
发明人： Paul John Beswick , Vipulkumar Patel , Michael Lawrence Sierra
IPC分类号： A61K31/426 , A61K31/421 , C07D277/20 , C07D263/30
CPC分类号： C07D277/24
摘要： A compound of formula (I) or pharmaceutically acceptable salts and solvates thereof. R1 and R2 are independently H or C1-3alkyl, m is 0–3; X1 is NH, NCH3, O, S; R3, R4 and R5 are independently H, CH3, CF3, OCH3, allyl or halogen; X2 is (CR10R11)n wherein n is 1 or 2; R10 and R11 independently represent H, fluorine or C1-16alkyl; R26 and R27 are independently H, C1-3 alkyl or R26 and R27 together with the carbon atom to which they are bonded form a 3–5 membered cycloalklyl ring. R6 and R7 independently represent H, fluorine or C1-16alkyl; R9 is C1-6alkyl or CF3; One of Y and Z is N, the other is S or O; Each R8 independently represents CF3, OCH3, CH3 or halogen; y is O, 1, 2, 3, 4, 5. Use of a compound of formula (I) for the manufacture of a medicament for the prevention or treatment of a hPPAR mediated disease or condition, such as dyslipidemia, syndrome X, heart failure, hypercholesteremia, cardiovascular disease, type II diabetes mellitus, type 1 diabetes, insulin resistance hyperlipidemia, obesity, anorexia bulimia, inflammation and anorexia nervosa
摘要翻译：式（I）化合物或其药学上可接受的盐和溶剂化物。 R 1和R 2独立地为H或C 1-3烷基，m为0-3; X 1是NH，NCH 3，O，S; R 3，R 4和R 5独立地为H，CH 3，CF 3， OCH 3，OCH 3，烯丙基或卤素; 其中n为1或2;（3）其中n为1或2; R 10和R 11独立地代表H，氟或C 1-16烷基; R 26和R 27独立地是H，C 1-3烷基或R 26和R 26， 27与它们所键合的碳原子一起形成3-5元环烯基环。 R 6和R 7独立地表示H，氟或C 1-16烷基; R 9是C 1-6烷基或CF 3 N; Y和Z之一是N，另一个是S或O; 每个R 8独立地表示CF 3，OCH 3，CH 3或卤素; y是O，1,2,3,4,5。式（I）化合物在制备用于预防或治疗hPPAR介导的疾病或病症如血脂异常，综合征X，心脏的药物中的用途失败，高胆固醇血症，心血管疾病，II型糖尿病，1型糖尿病，胰岛素抵抗性高脂血症，肥胖，厌食症，炎症和神经性厌食

10. 发明授权

US07091237B2 Furan and thiophene derivatives that activate human peroxisome proliferator activated receptors 失效
标题翻译：激活人类过氧化物酶体增殖物激活受体的呋喃和噻吩衍生物
公开(公告)号：US07091237B2
公开(公告)日：2006-08-15
申请号：US10476194
申请日：2002-05-09
申请人： Paul John Beswick , Christopher Charles Hamlett , Vipulkumar Patel , Michael Lawrence Sierra , Nigel Grahame Ramsden
发明人： Paul John Beswick , Christopher Charles Hamlett , Vipulkumar Patel , Michael Lawrence Sierra , Nigel Grahame Ramsden
IPC分类号： A61K31/38 , A61K31/34 , C07D333/24 , C07D307/02
CPC分类号： C07D307/38 , C07D307/42 , C07D333/16 , C07D333/18 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/12
摘要： A compound of formula (I) or pharmaceutically acceptable salts and solvates thereof, for the treatment of a hPPAR mediated disease or condition
摘要翻译：用于治疗hPPAR介导的疾病或病症的式（I）化合物或其药学上可接受的盐和溶剂合物

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式