公开(公告)号：US20070021436A1

公开(公告)日：2007-01-25

申请号：US11422352

申请日：2006-06-06

申请人： Nand Baindur ,  Michael Gaul ,  Kevin Kreutter ,  Guozhang Xu

发明人： Nand Baindur ,  Michael Gaul ,  Kevin Kreutter ,  Guozhang Xu

IPC分类号： A61K31/517 ,  A61K31/4709 ,  C07D403/14 ,  C07D401/14

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

摘要： The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: wherein R1, R2, R99, and X are as defined herein, the use of such compounds in the sysnthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.

摘要翻译： 本发明涉及式C的烷基喹啉和烷基喹唑啉化合物：其中R 1，R 2，R 99和X如本文所定义 ，这些化合物在蛋白酪氨酸激酶抑制剂，特别是FLT3和/或c-kit和/或TrkB的抑制剂的使用中的应用。

公开(公告)号：US20060281772A1

公开(公告)日：2006-12-14

申请号：US11422349

申请日：2006-06-06

申请人： Nand Baindur ,  Michael Gaul ,  Kevin Kreutter ,  Christian Baumann ,  Alexander Kim ,  Guozhang Xu ,  Robert Tuman ,  Dana Johnson

发明人： Nand Baindur ,  Michael Gaul ,  Kevin Kreutter ,  Christian Baumann ,  Alexander Kim ,  Guozhang Xu ,  Robert Tuman ,  Dana Johnson

IPC分类号： A61K31/517 ,  A61K31/4709 ,  C07D403/04 ,  C07D401/04

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，使用这些化合物如蛋白酪氨酸激酶调节剂，特别是FLT3和/或c-kit和/或TrkB的抑制剂，使用这些化合物来降低或抑制FLT3和/或 c-kit和/或TrkB，以及这些化合物在受试者中用于预防或治疗细胞增殖性疾病和/或与FLT3和/或c-kit和/或TrkB相关的疾病的用途。 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：US20060281764A1

公开(公告)日：2006-12-14

申请号：US11422362

申请日：2006-06-06

申请人： Michael Gaul ,  Guozhang Xu ,  Christian Baumann

发明人： Michael Gaul ,  Guozhang Xu ,  Christian Baumann

IPC分类号： C07D403/04 ,  A61K31/506

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14

摘要： The invention is directed to aminopyrimidine compounds of Formula I: where R3, B, Z, Q, p, q and R1 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的氨基嘧啶化合物：其中R 3，B，Z，Q，p，q和R 1'如本文所定义，使用这样的 作为蛋白质酪氨酸激酶调节剂的化合物，特别是FLT3和/或c-kit和/或TrkB的抑制剂，使用这些化合物来降低或抑制细胞中FLT3和/或c-kit和/或TrkB的激酶活性 受试者以及这些化合物在受试者中预防或治疗细胞增殖性疾病和/或与FLT3和/或c-kit和/或TrkB相关的疾病的用途。 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：US08748624B2

公开(公告)日：2014-06-10

申请号：US13478534

申请日：2012-05-23

申请人： Devraj Chakravarty ,  Kevin Kreutter ,  Mark Powell ,  Brian Shook ,  Fengbin Song ,  Guozhang Xu ,  Shyh-Ming Yang ,  Rui Zhang ,  Bao-Ping Zhao

发明人： Devraj Chakravarty ,  Kevin Kreutter ,  Mark Powell ,  Brian Shook ,  Fengbin Song ,  Guozhang Xu ,  Shyh-Ming Yang ,  Rui Zhang ,  Bao-Ping Zhao

IPC分类号： A61K31/44 ,  C07D211/70

CPC分类号： C07D213/81

摘要： The present invention is directed to picolanmido-propanoic acid derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.

摘要翻译： 本发明涉及吡啶甲酰 - 丙酸衍生物，含有它们的药物组合物及其在治疗和/或预防通过拮抗一种或多种胰高血糖素受体而改善的病症和病症的用途，包括例如代谢性疾病如II型糖尿病 和肥胖。

公开(公告)号：US08426604B2

公开(公告)日：2013-04-23

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： C07D417/14 ,  C07D211/32 ,  C07D415/00 ,  C07D419/00 ,  A61K31/4439 ,  A61K31/427 ,  A61K31/495 ,  A61K31/44 ,  A61K31/535 ,  A61K31/501 ,  A61K31/445 ,  A61K31/00

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，升高的血糖水平和胰岛素抵抗。

公开(公告)号：US08399681B2

公开(公告)日：2013-03-19

申请号：US13566214

申请日：2012-08-03

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： C07D277/14 ,  C07D211/32 ,  C07D513/00 ,  C07D413/14 ,  C07D223/02 ,  C07D243/08 ,  C07D295/04 ,  A61K31/397 ,  A61K31/55 ,  A61K31/535 ,  A61K31/50 ,  A61K31/497 ,  A61K31/445

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：US20120302641A1

公开(公告)日：2012-11-29

申请号：US13478568

申请日：2012-05-23

申请人： Devraj Chakravarty ,  Michael Greco ,  Brian Shook ,  Guozhang Xu ,  Rui Zhang

发明人： Devraj Chakravarty ,  Michael Greco ,  Brian Shook ,  Guozhang Xu ,  Rui Zhang

IPC分类号： A61K31/197 ,  A61P13/12 ,  A61P3/04 ,  C07C237/36 ,  A61P3/10

CPC分类号： C07C237/36

摘要： The present invention is directed to biphenyl derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.

摘要翻译： 本发明涉及联苯衍生物，含有它们的药物组合物及其在治疗和/或预防通过拮抗一种或多种胰高血糖素受体，包括例如代谢性疾病如II型糖尿病和肥胖症而改善的病症和病症中的用途。

公开(公告)号：US20120302610A1

公开(公告)日：2012-11-29

申请号：US13478534

申请日：2012-05-23

申请人： Devraj Chakravarty ,  Kevin Kreutter ,  Mark Powell ,  Brian Shook ,  Fengbin Song ,  Guozhang Xu ,  Shyh-Ming Yang ,  Rui Zhang ,  Bao-Ping Zhao

发明人： Devraj Chakravarty ,  Kevin Kreutter ,  Mark Powell ,  Brian Shook ,  Fengbin Song ,  Guozhang Xu ,  Shyh-Ming Yang ,  Rui Zhang ,  Bao-Ping Zhao

IPC分类号： A61K31/4418 ,  A61P13/12 ,  A61P3/04 ,  C07D213/81 ,  A61P3/10

CPC分类号： C07D213/81

摘要： The present invention is directed to picolanmido-propanoic acid derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.

摘要翻译： 本发明涉及吡啶甲酰 - 丙酸衍生物，含有它们的药物组合物及其在治疗和/或预防通过拮抗一种或多种胰高血糖素受体而改善的病症和病症的用途，包括例如代谢性疾病如II型糖尿病 和肥胖。

公开(公告)号：US20120302544A1

公开(公告)日：2012-11-29

申请号：US13566214

申请日：2012-08-03

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： A61K31/454 ,  A61K31/5377 ,  A61K31/427 ,  A61P19/00 ,  A61P19/04 ,  A61P19/06 ,  A61P19/10 ,  A61P35/04 ,  A61P35/00 ,  A61P19/08 ,  A61P19/02 ,  A61P1/02 ,  A61P11/00 ,  A61P11/08 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P9/00 ,  A61P9/10 ,  A61P3/10 ,  A61K31/4985 ,  A61K31/496

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：US08263781B2

公开(公告)日：2012-09-11

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： C07D277/14 ,  C07D211/32 ,  C07D513/00 ,  C07D413/14 ,  C07D223/02 ,  C07D243/08 ,  C07D295/04 ,  A61K31/397 ,  A61K31/55 ,  A61K31/535 ,  A61K31/50 ,  A61K31/497 ,  A61K31/445 ,  A61K31/425

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，假性呕吐，脂质障碍，代谢综合征 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。