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公开(公告)号：US07776891B2
公开(公告)日：2010-08-17
申请号：US11659608
申请日：2005-08-12
申请人： Weichao Chen , Alec D. Lebsack , Benito Munoz , Shankar Venkatraman , Bowei Wang
发明人： Weichao Chen , Alec D. Lebsack , Benito Munoz , Shankar Venkatraman , Bowei Wang
IPC分类号： A61K31/44 , C07D401/02
CPC分类号： C07K5/06139 , C07K5/06191
摘要： Compounds of Formula (I) are antagonists of VLA-4, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of inflammatory bowel disease including ulcerative colitis and Crohn's disease, multiple sclerosis, asthma, and rheumatoid arthritis.
摘要翻译： 式（I）化合物是VLA-4的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病理学。 这些化合物可以配制成药物组合物，并且适用于治疗包括溃疡性结肠炎和克罗恩病，多发性硬化，哮喘和类风湿性关节炎的炎性肠病。
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公开(公告)号：US20160046600A1
公开(公告)日：2016-02-18
申请号：US14777481
申请日：2014-03-13
申请人： Wenying CHAI , Charlotte DECKHUT , Curt A. DVORAK , Wendy ECCLES , James P. EDWARDS , Steven D. GOLDBERG , Paul J. KRAWCZUK , Alec D. LEBSACK , Jing LIU , Virginia M. TANIS , Kyle T. TARANTINO , JANSSEN PHARMACEUTICA NV
发明人： Wenying Chai , Charlotte Deckhut , Curt A. Dvorak , Wendy Eccles , James P. Edwards , Steven D. Goldberg , Paul J. Krawczuk , Alec D. Lebsack , Jing Liu , Virginia M. Tanis , Kyle T. Tarantino
IPC分类号： C07D401/12 , C07D405/14 , C07D417/12 , C07D417/14 , C07D413/14 , C07D401/14
CPC分类号： C07D417/14 , A61K31/428 , A61K31/4709 , A61K31/4725 , A61K31/506 , A61K31/5377 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/12
摘要： The present invention relates to compounds of Formula (I), and solvates, hydrates, and pharmaceutically acceptable salts thereof, wherein ring A, R1, R5 and R6 are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
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公开(公告)号：US08673895B2
公开(公告)日：2014-03-18
申请号：US11726756
申请日：2007-03-21
申请人： Bryan James Branstetter , James Guy Breitenbucher , Natalie A. Hawryluk , Alec D. Lebsack , Jeffrey E. Merit
发明人： Bryan James Branstetter , James Guy Breitenbucher , Natalie A. Hawryluk , Alec D. Lebsack , Jeffrey E. Merit
IPC分类号： A61P11/00 , A61P29/00 , A61K31/55 , C07D487/02
CPC分类号： C07D487/04
摘要： Certain tetrahydro-pyrimidoazepine compounds are described, which are useful as TRPV1 modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by TRPV1. Thus, the compounds may be administered to treat, e.g., pain, itch, cough, asthma, or inflammatory bowel disease.
摘要翻译： 描述了某些四氢嘧啶并氮杂化合物，其可用作TRPV1调节剂。 这样的化合物可以用于治疗由TRPV1介导的疾病状态，病症和状况的药物组合物和方法。 因此，可以施用化合物以治疗，例如疼痛，瘙痒，咳嗽，哮喘或炎症性肠病。
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4.发明申请公开(公告)号：US20130005687A1
公开(公告)日：2013-01-03
申请号：US13611936
申请日：2012-09-12
申请人： Bryan James Branstetter , J. Guy Breitenbucher , Alec D. Lebsack , Jing Liu , Jason C. Rech , Wei Xiao
发明人： Bryan James Branstetter , J. Guy Breitenbucher , Alec D. Lebsack , Jing Liu , Jason C. Rech , Wei Xiao
IPC分类号： C07D513/04 , A61K31/519 , C07D239/48 , A61K31/5377 , C07D473/34 , A61K31/52 , C07D473/24 , C07D473/18 , C07D473/16 , C07F7/10 , A61K31/695 , A61P29/00 , A61P27/16 , A61P11/00 , A61P1/00 , A61P13/00 , A61P7/00 , A61P25/00 , A61P17/04 , A61P19/02 , A61P11/10 , A61P11/06 , C07D498/04
CPC分类号： C07D513/04 , A61K31/497 , A61K31/519 , A61K31/5377 , C07D473/16 , C07D473/18 , C07D473/24 , C07D473/34 , C07D498/04
摘要： Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
摘要翻译： 描述了一些TRPV1调节的咪唑并，恶唑并噻唑并噻吩并嘧啶化合物。 所述化合物可用于治疗由TRPV1活性介导的疾病状态，病症和状况的药物组合物和方法，例如疼痛，关节炎，瘙痒，咳嗽，哮喘或炎症性肠病。
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公开(公告)号：US20080004253A1
公开(公告)日：2008-01-03
申请号：US11824202
申请日：2007-06-28
IPC分类号： A61K31/55 , A61K31/541 , A61K31/5377 , A61K31/519 , C07D498/02
CPC分类号： C07D513/04
摘要： Certain TRPV1-modulating thiazolopyrimidine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
摘要翻译： 描述了某些TRPV1调节性噻唑并嘧啶化合物。 所述化合物可用于治疗由TRPV1活性介导的疾病状态，病症和状况的药物组合物和方法，例如疼痛，关节炎，瘙痒，咳嗽，哮喘或炎症性肠病。
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公开(公告)号：US08637527B2
公开(公告)日：2014-01-28
申请号：US13611936
申请日：2012-09-12
申请人： Bryan James Branstetter , J. Guy Breitenbucher , Alec D. Lebsack , Jing Liu , Jason C Rech , Wei Xiao
发明人： Bryan James Branstetter , J. Guy Breitenbucher , Alec D. Lebsack , Jing Liu , Jason C Rech , Wei Xiao
IPC分类号： C07D487/04 , A61K31/519 , A61K31/397 , A61K31/496 , A61K31/497 , A61P25/02 , A61P29/00 , A61P19/02 , C07D473/34 , C07D473/28 , C07D473/32 , A61K31/52
CPC分类号： C07D513/04 , A61K31/497 , A61K31/519 , A61K31/5377 , C07D473/16 , C07D473/18 , C07D473/24 , C07D473/34 , C07D498/04
摘要： Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
摘要翻译： 描述了一些TRPV1调节的咪唑并，恶唑并噻唑并噻吩并嘧啶化合物。 所述化合物可用于治疗由TRPV1活性介导的疾病状态，病症和状况的药物组合物和方法，例如疼痛，关节炎，瘙痒，咳嗽，哮喘或炎症性肠病。
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公开(公告)号：US08288397B2
公开(公告)日：2012-10-16
申请号：US12316848
申请日：2008-12-16
申请人： Bryan James Branstetter , J. Guy Breitenbucher , Alec D. Lebsack , Jing Liu , Jason C Rech , Wei Xiao
发明人： Bryan James Branstetter , J. Guy Breitenbucher , Alec D. Lebsack , Jing Liu , Jason C Rech , Wei Xiao
IPC分类号： C07D487/04 , C07D473/34 , C07D513/04 , C07D295/04 , A61K31/519 , A61K31/429 , A61K31/5377 , A61K31/496 , A61K31/5355 , C07D473/18 , C07D473/16 , C07D473/24 , C07D498/04 , A61K31/52 , A61K31/424
CPC分类号： C07D513/04 , A61K31/497 , A61K31/519 , A61K31/5377 , C07D473/16 , C07D473/18 , C07D473/24 , C07D473/34 , C07D498/04
摘要： Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
摘要翻译： 描述了一些TRPV1调节的咪唑并，恶唑并噻唑并噻吩并嘧啶化合物。 所述化合物可用于治疗由TRPV1活性介导的疾病状态，病症和状况的药物组合物和方法，例如疼痛，关节炎，瘙痒，咳嗽，哮喘或炎症性肠病。
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公开(公告)号：US20090156599A1
公开(公告)日：2009-06-18
申请号：US12316848
申请日：2008-12-16
申请人： Bryan James Branstetter , J. Guy Breitenbucher , Alec D. Lebsack , Jing Liu , Jason C. Rech , Wei Xiao
发明人： Bryan James Branstetter , J. Guy Breitenbucher , Alec D. Lebsack , Jing Liu , Jason C. Rech , Wei Xiao
IPC分类号： A61K31/5377 , C07D471/04 , C07D413/14 , A61P25/28 , A61P9/10 , A61K31/497 , A61K31/519
CPC分类号： C07D513/04 , A61K31/497 , A61K31/519 , A61K31/5377 , C07D473/16 , C07D473/18 , C07D473/24 , C07D473/34 , C07D498/04
摘要： Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
摘要翻译： 描述了一些TRPV1调节的咪唑并，恶唑并噻唑并噻吩并嘧啶化合物。 所述化合物可用于治疗由TRPV1活性介导的疾病状态，病症和状况的药物组合物和方法，例如疼痛，关节炎，瘙痒，咳嗽，哮喘或炎症性肠病。
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公开(公告)号：US20160039790A1
公开(公告)日：2016-02-11
申请号：US14777492
申请日：2014-03-13
申请人： Wenying CHAI , Curt A. DVORAK , Wendy ECCLES , James P. EDWARDS , Steven D. GOLDBERG , Paul J. KRAWCZUK , Alec D. LEBSACK , Jing LIU , Daniel J. PIPPEL , Zachary S. SALES , Virginia M. TANIS , Mark S. TICHENOR , John J.M. WIENER , JANSSEN PHARMACEUTICA NV
发明人： Wenying Chai , Curt A. Dvorak , Wendy Eccles , James P. Edwards , Steven D. Goldberg , Paul J. Krawczuk , Alec D. Lebsack , Jing Liu , Daniel J. Pippel , Zachary S. Sales , Virginia M. Tanis , Mark S. Tichenor , John J. M. Wiener
IPC分类号： C07D401/12 , C07D401/14 , C07D403/14 , C07D403/12
CPC分类号： C07D401/12 , A61K31/4184 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/506 , C07D401/14 , C07D403/12 , C07D403/14
摘要： The present invention relates to compounds of Formula (I), and solvates, hydrates, and pharmaceutically acceptable salts thereof, wherein X1, X1′, X1″, R1, R2 and R3 are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
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公开(公告)号：US20090156598A1
公开(公告)日：2009-06-18
申请号：US12316827
申请日：2008-12-16
申请人： Alec D. Lebsack
发明人： Alec D. Lebsack
IPC分类号： A61K31/52 , C07D473/34 , C07D413/14 , A61K31/5377 , A61K31/496 , C07D403/14 , C07D401/14 , A61P1/00 , A61P29/00 , A61P7/00 , A61P43/00
CPC分类号： A61K31/496 , A61K31/52 , A61K31/5377 , C07D473/16 , C07D473/18 , C07D473/24 , C07D473/34
摘要： Certain TRPV1-modulating imidazolopyrimidine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
摘要翻译： 描述了某些TRPV1调节性咪唑并嘧啶化合物。 所述化合物可用于治疗由TRPV1活性介导的疾病状态，病症和状况的药物组合物和方法，例如疼痛，关节炎，瘙痒，咳嗽，哮喘或炎症性肠病。
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