公开(公告)号：US08293917B2

公开(公告)日：2012-10-23

申请号：US12990248

申请日：2009-05-01

申请人： Brian Nicholas Cook ,  Christian Harcken ,  Thomas Wei-Ho Lee ,  Pingrong Liu ,  Jord Lord ,  Can Mao ,  Wang Mao ,  Brian Christopher Raudenbush ,  Hossein Razavi ,  Christopher Ronald Sarko ,  Alen David Swinamer

发明人： Brian Nicholas Cook ,  Christian Harcken ,  Thomas Wei-Ho Lee ,  Pingrong Liu ,  Jord Lord ,  Can Mao ,  Wang Mao ,  Brian Christopher Raudenbush ,  Hossein Razavi ,  Christopher Ronald Sarko ,  Alen David Swinamer

IPC分类号： C07D401/00 ,  A61K31/44

CPC分类号： C07D401/12 ,  C07D231/14 ,  C07D405/14 ,  C07D417/12

摘要： Disclosed are compounds of the formula (I) which block the interaction of CCR1 and its ligands and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

摘要翻译： 公开了式（I）的化合物，其阻断CCR1及其配体的相互作用，因此可用于治疗通过CCR1的活性介导或维持的多种疾病和病症，包括自身免疫疾病，例如类风湿性关节炎和多发性 硬化。 还公开了包含这些化合物的药物组合物，使用这些化合物治疗各种疾病和病症的方法，制备这些化合物的方法和可用于这些方法的中间体。

公开(公告)号：US08063065B2

公开(公告)日：2011-11-22

申请号：US12969753

申请日：2010-12-16

申请人： Brian Nicholas Cook ,  Darren Di Salvo ,  Christian Harcken ,  Daniel Kuzmich ,  Thomas Wai-Ho Lee ,  Pingrong Liu ,  John Lord ,  Can Mao ,  Jochen Neu ,  Brian Christopher Raudenbush ,  Hossein Razavi ,  Alan David Swinamer

发明人： Brian Nicholas Cook ,  Darren Di Salvo ,  Christian Harcken ,  Daniel Kuzmich ,  Thomas Wai-Ho Lee ,  Pingrong Liu ,  John Lord ,  Can Mao ,  Jochen Neu ,  Brian Christopher Raudenbush ,  Hossein Razavi ,  Alan David Swinamer

IPC分类号： A61K31/437 ,  C07D515/04

CPC分类号： C07D471/04

摘要： Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.

摘要翻译： 公开了式（I）化合物，其可用于治疗通过包括自身免疫疾病如类风湿性关节炎和多发性硬化的CCR1的活性介导或持续的多种疾病和病症。 还公开了制备方法和使用方法。

公开(公告)号：US07879873B2

公开(公告)日：2011-02-01

申请号：US12564129

申请日：2009-09-22

申请人： Brian Nicholas Cook ,  Darren DiSalvo ,  Daniel Robert Fandrick ,  Christian Harcken ,  Daniel Kuzmich ,  Thomas Wai-Ho Lee ,  Pingrong Liu ,  John Lord ,  Can Mao ,  Jochen Neu ,  Brian Christopher Raudenbush ,  Hossein Razavi ,  Jonathan Timothy Reeves ,  Jinhua J. Song ,  Alan David Swinamer ,  Zhulin Tan

发明人： Brian Nicholas Cook ,  Darren DiSalvo ,  Daniel Robert Fandrick ,  Christian Harcken ,  Daniel Kuzmich ,  Thomas Wai-Ho Lee ,  Pingrong Liu ,  John Lord ,  Can Mao ,  Jochen Neu ,  Brian Christopher Raudenbush ,  Hossein Razavi ,  Jonathan Timothy Reeves ,  Jinhua J. Song ,  Alan David Swinamer ,  Zhulin Tan

IPC分类号： A61K31/437 ,  C07D515/04

CPC分类号： C07D471/04

摘要： Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.

公开(公告)号：US20130065918A1

公开(公告)日：2013-03-14

申请号：US13414991

申请日：2012-03-08

申请人： Jehrod Burnett Brenneman ,  John D. Huber ,  Brian Christopher Raudenbush ,  Christopher Ronald Sarko

发明人： Jehrod Burnett Brenneman ,  John D. Huber ,  Brian Christopher Raudenbush ,  Christopher Ronald Sarko

IPC分类号： A61K31/4725 ,  A61K31/4439 ,  C07D401/14 ,  C07D409/14 ,  C07D405/14 ,  C07D413/14 ,  A61P9/00 ,  A61P29/00 ,  A61P1/16 ,  A61P13/12 ,  A61P11/00 ,  A61P15/00 ,  A61P25/28 ,  A61P25/16 ,  C07D417/14

CPC分类号： C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, A and B are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

摘要翻译： 本发明涉及式（I）化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5，R 6，A和B如本文所定义。 本发明还涉及包含这些化合物的药物组合物，使用这些化合物治疗各种疾病和病症的方法，制备这些化合物的方法和可用于这些方法的中间体。

公开(公告)号：US08569339B2

公开(公告)日：2013-10-29

申请号：US13414991

申请日：2012-03-08

申请人： Jehrod Burnett Brenneman ,  John D. Huber ,  Brian Christopher Raudenbush ,  Christopher Ronald Sarko

发明人： Jehrod Burnett Brenneman ,  John D. Huber ,  Brian Christopher Raudenbush ,  Christopher Ronald Sarko

IPC分类号： A61K31/4725 ,  A61K31/4439 ,  C07D401/14 ,  C07D409/14 ,  C07D405/14 ,  C07D413/14 ,  A61P9/00 ,  A61P29/00 ,  A61P1/16

CPC分类号： C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, A and B are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

摘要翻译： 本发明涉及式（I）化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5，R 6，A和B如本文所定义。 本发明还涉及包含这些化合物的药物组合物，使用这些化合物治疗各种疾病和病症的方法，制备这些化合物的方法和可用于这些方法的中间体。

公开(公告)号：US20080293782A1

公开(公告)日：2008-11-27

申请号：US12096421

申请日：2006-12-06

申请人： David Barnes ,  Gary Mark Coppola ,  Robert Edson Damon ,  Katsumasa Nakajima ,  Brian Christopher Raudenbush ,  Travis Stams ,  Sidney Wolf Topiol ,  Thalaththani Ralalage Vedananda

发明人： David Barnes ,  Gary Mark Coppola ,  Robert Edson Damon ,  Katsumasa Nakajima ,  Brian Christopher Raudenbush ,  Travis Stams ,  Sidney Wolf Topiol ,  Thalaththani Ralalage Vedananda

IPC分类号： A61K31/433 ,  C07D285/10 ,  A61P3/10 ,  A61P3/04 ,  A61P9/10 ,  A61P25/28 ,  A61P35/00

CPC分类号： C07D285/10 ,  C07D417/10

摘要： Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.

摘要翻译： 式的化合物是蛋白酪氨酸磷酸酶（PTPases）的抑制剂，因此可用于治疗由PTPase活性介导的病症。 本发明的化合物也可以用作以磷酸酪氨酸结合区如SH2结构域为特征的其它酶的抑制剂。 因此，式（I）化合物可用于预防和/或治疗与大，小血管的肥胖，葡萄糖不耐受，糖尿病，高血压和缺血性疾病相关的胰岛素抵抗，伴随2型糖尿病的病症 ，包括高脂血症，高甘油三酯血症，动脉粥样硬化，血管再狭窄，肠易激综合征，胰腺炎，脂肪细胞肿瘤，以及诸如脂肪肉瘤，血脂异常和其它指示胰岛素抵抗的疾病。 此外，本发明的化合物可用于治疗和/或预防癌症，骨质疏松症，神经变性和感染性疾病以及涉及炎症和免疫系统的疾病。