公开(公告)号：US08071768B2

公开(公告)日：2011-12-06

申请号：US11422349

申请日：2006-06-06

申请人： Nand Baindur ,  Michael David Gaul ,  Kevin Douglas Kreutter ,  Christian Andrew Baumann ,  Alexander J. Kim ,  Guozhang Xu ,  Robert W. Tuman ,  Dana L. Johnson

发明人： Nand Baindur ,  Michael David Gaul ,  Kevin Douglas Kreutter ,  Christian Andrew Baumann ,  Alexander J. Kim ,  Guozhang Xu ,  Robert W. Tuman ,  Dana L. Johnson

IPC分类号： C07D401/00 ,  C07D413/00

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

摘要： The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula I: wherein R1, R2, R3, B, Z, G, Q and X are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of FLT3 and/or c-kit and/or TrkB, the use of such compounds to reduce or inhibit kinase activity of FLT3 and/or c-kit and/or TrkB in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to FLT3 and/or c-kit and/or TrkB. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.

摘要翻译： 本发明涉及式I的烷基喹啉和烷基喹唑啉化合物：其中R 1，R 2，R 3，B，Z，G，Q和X如本文所定义，使用这些化合物作为蛋白质酪氨酸激酶调节剂，特别是FLT3抑制剂， /或c-kit和/或TrkB，使用这些化合物降低或抑制细胞或受试者中FLT3和/或c-kit和/或TrkB的激酶活性，以及​​使用这些化合物预防或治疗 在受试者中是与FLT3和/或c-kit和/或TrkB相关的细胞增殖性病症和/或病症。 本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如癌症和其它细胞增殖性疾病的病症的方法。

公开(公告)号：US20110150864A1

公开(公告)日：2011-06-23

申请号：US12969984

申请日：2010-12-16

申请人： Gilles BIGNAN ,  Micheal Gaul ,  Guozhang Xu ,  Bao-Ping Zhao

发明人： Gilles BIGNAN ,  Micheal Gaul ,  Guozhang Xu ,  Bao-Ping Zhao

IPC分类号： C07D417/14 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/427 ,  A61K31/551 ,  C07D487/08 ,  A61K31/55 ,  C07D491/04 ,  A61K31/541 ,  A61K31/4545 ,  C07D471/10 ,  A61K31/438 ,  C07D487/04 ,  A61K31/4985 ,  C07D498/04 ,  A61K31/437 ,  C07D498/08 ,  A61P35/00 ,  A61K39/395 ,  A61P19/08 ,  A61P19/10 ,  A61P19/02 ,  A61P29/00 ,  A61P11/00 ,  A61P1/02 ,  A61P3/08 ,  A61P3/10 ,  A61P3/06 ,  A61P3/00 ,  A61P9/00 ,  A61P9/10

CPC分类号： C07D417/14 ,  C07D417/06 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D491/04 ,  C07D498/08

摘要： The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.

摘要翻译： 本发明涉及式（I）化合物，制备这些化合物的方法，组合物，中间体及其衍生物，用于治疗包括但不限于强直性脊柱炎，动脉粥样硬化，关节炎（如类风湿性关节炎，感染性关节炎，儿童期 关节炎，牛皮癣关节炎，反应性关节炎），骨相关疾病（包括与骨形成相关的疾病），乳腺癌（包括对抗雌激素治疗无反应的那些），心血管疾病，软骨相关疾病（如软骨损伤/损失， 软骨变性和与软骨形成相关的软骨变性，软骨发育不全，软骨肉瘤，慢性背部损伤，慢性支气管炎，慢性炎症性气道疾病，慢性阻塞性肺病，糖尿病，能量稳态障碍，痛风，假性血糖，脂质障碍，代谢综合征，多发性 骨髓瘤，肥胖症，骨关节炎，成骨不全，骨质溶解骨 骨质疏松症，骨质疏松症，佩吉特氏病，牙周病，风湿性多肌痛，莱特综合征，重复性应激损伤，高血糖症，升高的血糖水平和胰岛素抵抗。

公开(公告)号：US20070270425A1

公开(公告)日：2007-11-22

申请号：US11609450

申请日：2006-12-12

申请人： Guozhang Xu ,  Lily Lee ,  Terry Hughes ,  Steven Wetter ,  Peter Connolly ,  Marta Abad ,  Stuart Emanuel ,  Prabha Karnachi ,  Steven Middleton

发明人： Guozhang Xu ,  Lily Lee ,  Terry Hughes ,  Steven Wetter ,  Peter Connolly ,  Marta Abad ,  Stuart Emanuel ,  Prabha Karnachi ,  Steven Middleton

IPC分类号： A61K31/5377 ,  A61P43/00 ,  C07D239/48 ,  C07D413/02

CPC分类号： C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D407/12 ,  C07D413/04 ,  C07D417/12

摘要： The present invention is directed to substituted pyrimidine compounds of formula (I): and forms thereof, their synthesis and use for treating, preventing or ameliorating a chronic or acute protein kinase mediated disease, disorder or condition.

摘要翻译： 本发明涉及式（I）的取代嘧啶化合物及其形式，其合成和用途，用于治疗，预防或改善慢性或急性蛋白激酶介导的疾病，病症或病症。

公开(公告)号：US20120157412A1

公开(公告)日：2012-06-21

申请号：US13406822

申请日：2012-02-28

申请人： Kathleen A. Battista ,  Gilles C. Bignan ,  Guozhang Xu ,  Lily Lee ,  Terry V. Hughes ,  Steven K. Wetter ,  Peter J. Connolly ,  Marta C. Abad ,  Stuart L. Emanuel ,  Prabha S. Karnachi ,  Steven A. Middleton

发明人： Kathleen A. Battista ,  Gilles C. Bignan ,  Guozhang Xu ,  Lily Lee ,  Terry V. Hughes ,  Steven K. Wetter ,  Peter J. Connolly ,  Marta C. Abad ,  Stuart L. Emanuel ,  Prabha S. Karnachi ,  Steven A. Middleton

IPC分类号： A61K31/675 ,  C07D403/12 ,  C07D413/14 ,  C07D413/12 ,  C07D405/12 ,  C07D417/12 ,  C07F9/6512 ,  C07D401/12 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61P19/08 ,  A61P19/02 ,  A61P25/00 ,  A61P3/10 ,  A61P27/02 ,  A61P1/00 ,  A61P3/00 ,  A61P35/00 ,  A61P17/00 ,  A61P31/12 ,  A61P9/00 ,  A61P11/00 ,  A61P13/12 ,  A61P35/02 ,  A61P35/04 ,  A61P17/06 ,  A61P17/14 ,  A61P25/28 ,  A61P25/16 ,  A61P25/24 ,  A61P27/06 ,  A61P9/10 ,  A61P11/06 ,  C07D239/48

CPC分类号： C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D407/12 ,  C07D413/04 ,  C07D417/12

摘要： The present invention is directed to substituted pyrimidine compounds of formula (I): and forms thereof, their synthesis and use for treating, preventing or ameliorating a chronic or acute protein kinase mediated disease, disorder or condition.

摘要翻译： 本发明涉及式（I）的取代嘧啶化合物及其形式，其合成和用途，用于治疗，预防或改善慢性或急性蛋白激酶介导的疾病，病症或病症。

公开(公告)号：US20110237625A1

公开(公告)日：2011-09-29

申请号：US12899812

申请日：2010-10-07

申请人： Michael Gaul ,  Alexander Kim ,  Lily Lee Searle ,  Raymond J. Patch ,  Dionisios Rentzeperis ,  Guozhang Xu ,  Xizhen Zhu

发明人： Michael Gaul ,  Alexander Kim ,  Lily Lee Searle ,  Raymond J. Patch ,  Dionisios Rentzeperis ,  Guozhang Xu ,  Xizhen Zhu

IPC分类号： A61K31/454 ,  C07D277/34 ,  A61K31/426 ,  C07D263/44 ,  A61K31/421 ,  A61P19/00 ,  A61P11/00 ,  A61P35/00 ,  A61P3/00 ,  A61P9/12

CPC分类号： C07D277/34 ,  C07D263/44

摘要： The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.

摘要翻译： 本发明涉及式（I）化合物，制备这些化合物的方法，组合物，中间体及其衍生物，用于治疗包括但不限于强直性脊柱炎，动脉粥样硬化，关节炎（如类风湿性关节炎，感染性关节炎，儿童期 关节炎，牛皮癣关节炎，反应性关节炎），骨相关疾病（包括与骨形成相关的疾病），乳腺癌（包括对抗雌激素治疗无反应的那些），心血管疾病，软骨相关疾病（如软骨损伤/损失， 软骨变性和与软骨形成相关的软骨变性，软骨发育不全，软骨肉瘤，慢性背部损伤，慢性支气管炎，慢性炎症性气道疾病，慢性阻塞性肺病，糖尿病，能量稳态障碍，痛风，假性血糖，脂质障碍，代谢综合征，多发性 骨髓瘤，肥胖症，骨关节炎，成骨不全，骨质溶解骨 骨质疏松症，骨质疏松症，佩吉特氏病，牙周病，风湿性多肌痛，莱特综合征，重复性应激损伤，高血糖症，升高的血糖水平和胰岛素抵抗。

公开(公告)号：US07846953B2

公开(公告)日：2010-12-07

申请号：US12043269

申请日：2008-03-06

申请人： Michael Gaul ,  Alexander Kim ,  Lily Lee Searle ,  Raymond Patch ,  Dionisois Rentzeperis ,  Guozhang Xu ,  Xizhen Zhu

发明人： Michael Gaul ,  Alexander Kim ,  Lily Lee Searle ,  Raymond Patch ,  Dionisois Rentzeperis ,  Guozhang Xu ,  Xizhen Zhu

IPC分类号： A61K31/426 ,  C07D277/04

CPC分类号： C07D277/34 ,  C07D263/44

摘要： The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.

摘要翻译： 本发明涉及式（I）化合物，制备这些化合物的方法，组合物，中间体及其衍生物，用于治疗包括但不限于强直性脊柱炎，动脉粥样硬化，关节炎（如类风湿性关节炎，感染性关节炎，儿童期 关节炎，牛皮癣关节炎，反应性关节炎），骨相关疾病（包括与骨形成相关的疾病），乳腺癌（包括对抗雌激素治疗无反应的那些），心血管疾病，软骨相关疾病（如软骨损伤/损失， 软骨变性和与软骨形成相关的软骨变性，软骨发育不全，软骨肉瘤，慢性背部损伤，慢性支气管炎，慢性炎症性气道疾病，慢性阻塞性肺病，糖尿病，能量稳态障碍，痛风，假性血糖，脂质障碍，代谢综合征，多发性 骨髓瘤，肥胖症，骨关节炎，成骨不全，骨质溶解骨 骨质疏松症，骨质疏松症，佩吉特氏病，牙周病，风湿性多肌痛，莱特综合征，重复性应激损伤，高血糖症，升高的血糖水平和胰岛素抵抗。

公开(公告)号：US20090111855A1

公开(公告)日：2009-04-30

申请号：US12043269

申请日：2008-03-06

申请人： Michael Gaul ,  Alexander Kim ,  Lily Lee Searle ,  Raymond J. Patch ,  Dionisios Rentzeperis ,  Guozhang Xu ,  Xizhen Zhu

发明人： Michael Gaul ,  Alexander Kim ,  Lily Lee Searle ,  Raymond J. Patch ,  Dionisios Rentzeperis ,  Guozhang Xu ,  Xizhen Zhu

IPC分类号： A61K31/454 ,  C07D277/34 ,  A61K31/426 ,  A61K31/421 ,  C07D263/44 ,  A61P3/04

CPC分类号： C07D277/34 ,  C07D263/44

摘要： The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.

摘要翻译： 本发明涉及式（I）化合物，制备这些化合物的方法，组合物，中间体及其衍生物，用于治疗包括但不限于强直性脊柱炎，动脉粥样硬化，关节炎（如类风湿性关节炎，感染性关节炎，儿童期 关节炎，牛皮癣关节炎，反应性关节炎），骨相关疾病（包括与骨形成相关的疾病），乳腺癌（包括对抗雌激素治疗无反应的那些），心血管疾病，软骨相关疾病（如软骨损伤/损失， 软骨变性和与软骨形成相关的软骨变性，软骨发育不全，软骨肉瘤，慢性背部损伤，慢性支气管炎，慢性炎症性气道疾病，慢性阻塞性肺病，糖尿病，能量稳态障碍，痛风，假性血糖，脂质障碍，代谢综合征，多发性 骨髓瘤，肥胖症，骨关节炎，成骨不全，骨质溶解骨 骨质疏松症，骨质疏松症，佩吉特氏病，牙周病，风湿性多肌痛，莱特综合征，重复性应激损伤，高血糖，升高的血糖水平和胰岛素抵抗。

公开(公告)号：US08796256B2

公开(公告)日：2014-08-05

申请号：US13114084

申请日：2011-05-24

申请人： Gilles Bignan ,  Wing Cheung ,  Micheal Gaul ,  Hui Huang ,  Xun Li ,  Raymond Patch ,  Sharmila Patel ,  Mark Player ,  Guozhang Xu ,  Bao-Ping Zhao ,  Jian Liu

发明人： Gilles Bignan ,  Wing Cheung ,  Micheal Gaul ,  Hui Huang ,  Xun Li ,  Raymond Patch ,  Sharmila Patel ,  Mark Player ,  Guozhang Xu ,  Bao-Ping Zhao ,  Jian Liu

IPC分类号： C07D417/06

CPC分类号： C07D417/06

摘要： The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.

摘要翻译： 本发明涉及式（I）化合物，制备这些化合物的方法，组合物，中间体及其衍生物，用于治疗包括但不限于强直性脊柱炎，动脉粥样硬化，关节炎（如类风湿性关节炎，感染性关节炎，儿童期 关节炎，牛皮癣关节炎，反应性关节炎），骨相关疾病（包括与骨形成相关的疾病），乳腺癌（包括对抗雌激素治疗无反应的那些），心血管疾病，软骨相关疾病（如软骨损伤/损失， 软骨变性和与软骨形成相关的软骨变性，软骨发育不全，软骨肉瘤，慢性背部损伤，慢性支气管炎，慢性炎症性气道疾病，慢性阻塞性肺病，糖尿病，能量稳态障碍，痛风，假性血糖，脂质障碍，代谢综合征，多发性 骨髓瘤，肥胖症，骨关节炎，成骨不全，骨质溶解骨 骨质疏松症，骨质疏松症，佩吉特氏病，牙周病，风湿性多肌痛，莱特综合征，重复性应激损伤，高血糖，升高的血糖水平和胰岛素抵抗。

公开(公告)号：US20110200586A1

公开(公告)日：2011-08-18

申请号：US13028266

申请日：2011-02-16

申请人： Gilles BIGNAN ,  Micheal Gaul ,  Guozhang Xu ,  Bao-Ping Zhao

发明人： Gilles BIGNAN ,  Micheal Gaul ,  Guozhang Xu ,  Bao-Ping Zhao

IPC分类号： A61K39/395 ,  C07D417/10 ,  C07D417/14 ,  C07D413/14 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/4985 ,  A61P19/08 ,  A61P19/06 ,  A61P19/10 ,  A61P35/04 ,  A61P35/00 ,  A61P19/02 ,  A61P17/06 ,  A61P29/00 ,  A61P11/00 ,  A61P1/02 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P7/02

CPC分类号： C07D417/06 ,  C07D417/14

摘要： The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.

摘要翻译： 本发明涉及式（I）化合物，制备这些化合物的方法，组合物，中间体及其衍生物，用于治疗包括但不限于强直性脊柱炎，动脉粥样硬化，关节炎（如类风湿性关节炎，感染性关节炎，儿童期 关节炎，牛皮癣关节炎，反应性关节炎），骨相关疾病（包括与骨形成相关的疾病），乳腺癌（包括对抗雌激素治疗无反应的那些），心血管疾病，软骨相关疾病（如软骨损伤/损失， 软骨变性和与软骨形成相关的软骨变性，软骨发育不全，软骨肉瘤，慢性背部损伤，慢性支气管炎，慢性炎症性气道疾病，慢性阻塞性肺病，糖尿病，能量稳态障碍，痛风，假性血糖，脂质障碍，代谢综合征，多发性 骨髓瘤，肥胖症，骨关节炎，成骨不全，骨质溶解骨 骨质疏松症，骨质疏松症，佩吉特氏病，牙周病，风湿性多肌痛，莱特综合征，重复性应激损伤，高血糖症，升高的血糖水平和胰岛素抵抗。

公开(公告)号：US07550474B2

公开(公告)日：2009-06-23

申请号：US10816544

申请日：2004-04-01

申请人： Kevin D. Kreutter ,  Lily Lee ,  Tianbao Lu ,  Venkatraman Mohan ,  Sharmila Patel ,  Hui Huang ,  Guozhang Xu ,  Mark Fitzgerald

发明人： Kevin D. Kreutter ,  Lily Lee ,  Tianbao Lu ,  Venkatraman Mohan ,  Sharmila Patel ,  Hui Huang ,  Guozhang Xu ,  Mark Fitzgerald

IPC分类号： A61K31/435 ,  C07D221/02 ,  C07D335/00 ,  C07D309/00 ,  C07C321/00

CPC分类号： C07D213/73 ,  C07C279/00 ,  C07C291/04 ,  C07D213/26 ,  C07D213/89 ,  C07D215/12 ,  C07D413/12 ,  C07D487/04

摘要： Phenyl acetamide compounds are described, including compounds of Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R3-R6, R11, B, Y and W are set forth in the specification. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as thrombin and factor Xa. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.

摘要翻译： 描述了苯基乙酰胺化合物，包括式I化合物或其溶剂合物，水合物或其药学上可接受的盐; 其中R3-R6，R11，B，Y和W在说明书中列出。 本发明的化合物是蛋白酶的有效抑制剂，特别是胰蛋白酶样的丝氨酸蛋白酶，如凝血酶和因子Xa。 描述了抑制血小板损失，抑制血小板聚集体形成，抑制纤维蛋白形成，抑制血栓形成和抑制栓塞形成的组合物。 本发明化合物的其它用途是作为凝血剂或者物理上连接于用于血液收集，血液循环和血液储存（例如导管，血液透析机，采血注射器和管）中使用的装置的制造中使用的材料的抗凝剂， 血线和支架。 另外，化合物可以被可检测地标记并用于血栓的体内成像。