公开(公告)号：US20080004253A1

公开(公告)日：2008-01-03

申请号：US11824202

申请日：2007-06-28

Applicant: Bryan James Branstetter ,  James Guy Breitenbucher ,  Alec D. Lebsack ,  Wei Xiao

Inventor： Bryan James Branstetter ,  James Guy Breitenbucher ,  Alec D. Lebsack ,  Wei Xiao

IPC: A61K31/55 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/519 ,  C07D498/02

CPC classification number: C07D513/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US08637527B2

公开(公告)日：2014-01-28

申请号：US13611936

申请日：2012-09-12

Applicant: Bryan James Branstetter ,  J. Guy Breitenbucher ,  Alec D. Lebsack ,  Jing Liu ,  Jason C Rech ,  Wei Xiao

Inventor： Bryan James Branstetter ,  J. Guy Breitenbucher ,  Alec D. Lebsack ,  Jing Liu ,  Jason C Rech ,  Wei Xiao

IPC: 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 classification number: C07D513/04 ,  A61K31/497 ,  A61K31/519 ,  A61K31/5377 ,  C07D473/16 ,  C07D473/18 ,  C07D473/24 ,  C07D473/34 ,  C07D498/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US08288397B2

公开(公告)日：2012-10-16

申请号：US12316848

申请日：2008-12-16

Applicant: Bryan James Branstetter ,  J. Guy Breitenbucher ,  Alec D. Lebsack ,  Jing Liu ,  Jason C Rech ,  Wei Xiao

Inventor： Bryan James Branstetter ,  J. Guy Breitenbucher ,  Alec D. Lebsack ,  Jing Liu ,  Jason C Rech ,  Wei Xiao

IPC: 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 classification number: C07D513/04 ,  A61K31/497 ,  A61K31/519 ,  A61K31/5377 ,  C07D473/16 ,  C07D473/18 ,  C07D473/24 ,  C07D473/34 ,  C07D498/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07776891B2

公开(公告)日：2010-08-17

申请号：US11659608

申请日：2005-08-12

Applicant: Weichao Chen ,  Alec D. Lebsack ,  Benito Munoz ,  Shankar Venkatraman ,  Bowei Wang

Inventor： Weichao Chen ,  Alec D. Lebsack ,  Benito Munoz ,  Shankar Venkatraman ,  Bowei Wang

IPC: A61K31/44 ,  C07D401/02

CPC classification number: C07K5/06139 ,  C07K5/06191

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20090156599A1

公开(公告)日：2009-06-18

申请号：US12316848

申请日：2008-12-16

Applicant: Bryan James Branstetter ,  J. Guy Breitenbucher ,  Alec D. Lebsack ,  Jing Liu ,  Jason C. Rech ,  Wei Xiao

Inventor： Bryan James Branstetter ,  J. Guy Breitenbucher ,  Alec D. Lebsack ,  Jing Liu ,  Jason C. Rech ,  Wei Xiao

IPC: A61K31/5377 ,  C07D471/04 ,  C07D413/14 ,  A61P25/28 ,  A61P9/10 ,  A61K31/497 ,  A61K31/519

CPC classification number: C07D513/04 ,  A61K31/497 ,  A61K31/519 ,  A61K31/5377 ,  C07D473/16 ,  C07D473/18 ,  C07D473/24 ,  C07D473/34 ,  C07D498/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20160046600A1

公开(公告)日：2016-02-18

申请号：US14777481

申请日：2014-03-13

Applicant: 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

Inventor： 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: C07D401/12 ,  C07D405/14 ,  C07D417/12 ,  C07D417/14 ,  C07D413/14 ,  C07D401/14

CPC classification number: C07D417/14 ,  A61K31/428 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/12

Abstract: 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.

公开(公告)号：US08673895B2

公开(公告)日：2014-03-18

申请号：US11726756

申请日：2007-03-21

Applicant: Bryan James Branstetter ,  James Guy Breitenbucher ,  Natalie A. Hawryluk ,  Alec D. Lebsack ,  Jeffrey E. Merit

Inventor： Bryan James Branstetter ,  James Guy Breitenbucher ,  Natalie A. Hawryluk ,  Alec D. Lebsack ,  Jeffrey E. Merit

IPC: A61P11/00 ,  A61P29/00 ,  A61K31/55 ,  C07D487/02

CPC classification number: C07D487/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20130005687A1

公开(公告)日：2013-01-03

申请号：US13611936

申请日：2012-09-12

Applicant: Bryan James Branstetter ,  J. Guy Breitenbucher ,  Alec D. Lebsack ,  Jing Liu ,  Jason C. Rech ,  Wei Xiao

Inventor： Bryan James Branstetter ,  J. Guy Breitenbucher ,  Alec D. Lebsack ,  Jing Liu ,  Jason C. Rech ,  Wei Xiao

IPC: 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 classification number: C07D513/04 ,  A61K31/497 ,  A61K31/519 ,  A61K31/5377 ,  C07D473/16 ,  C07D473/18 ,  C07D473/24 ,  C07D473/34 ,  C07D498/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20160039790A1

公开(公告)日：2016-02-11

申请号：US14777492

申请日：2014-03-13

Applicant: 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

Inventor： 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: C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D403/12

CPC classification number: C07D401/12 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/506 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14

Abstract: 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.

公开(公告)号：US20090156598A1

公开(公告)日：2009-06-18

申请号：US12316827

申请日：2008-12-16

Applicant: Alec D. Lebsack

Inventor： Alec D. Lebsack

IPC: A61K31/52 ,  C07D473/34 ,  C07D413/14 ,  A61K31/5377 ,  A61K31/496 ,  C07D403/14 ,  C07D401/14 ,  A61P1/00 ,  A61P29/00 ,  A61P7/00 ,  A61P43/00

CPC classification number: A61K31/496 ,  A61K31/52 ,  A61K31/5377 ,  C07D473/16 ,  C07D473/18 ,  C07D473/24 ,  C07D473/34

Abstract: 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.

Abstract translation: 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。