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1. 发明授权

US08071768B2 Alkylquinoline and alkylquinazoline kinase modulators 有权
标题翻译：烷基喹啉和烷基喹唑啉激酶调节剂
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。

2. 发明授权

US07825244B2 Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis 有权
标题翻译：用于合成烷基喹啉和烷基喹唑啉激酶调节剂的中间体及其相关合成方法
公开(公告)号：US07825244B2
公开(公告)日：2010-11-02
申请号：US11422352
申请日：2006-06-06
申请人： Nand Baindur , Michael David Gaul , Kevin Douglas Kreutter , Guozhang Xu
发明人： Nand Baindur , Michael David Gaul , Kevin Douglas Kreutter , Guozhang Xu
IPC分类号： C07D239/88 , C07D239/94 , C07D215/12 , C07D215/14
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 synthesis 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R1，R2，R99和X如本文所定义，这些化合物在合成蛋白酪氨酸激酶抑制剂，特别是FLT3和/或c- 套件和/或TrkB。

3. 发明申请

US20070021436A1 INTERMEDIATES USEFUL IN THE SYNTHESIS OF ALKYLQUINOLINE AND ALKYLQUINAZOLINE KINASE MODULATORS, AND RELATED METHODS OF SYNTHESIS 有权
标题翻译：有用的合成烷基喹啉和碱性激酶激酶调节剂的中间体及相关的合成方法
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。

4. 发明申请

US20060281772A1 ALKYLQUINOLINE AND ALKYLQUINAZOLINE KINASE MODULATORS 有权
标题翻译：烷基胆碱和碱性氨基酸激酶调节剂
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。

5. 发明申请

US20070004763A1 AMINOQUINOLINE AND AMINOQUINAZOLINE KINASE MODULATORS 审中-公开
标题翻译：氨基喹啉和氨基喹啉激酶调节剂
公开(公告)号：US20070004763A1
公开(公告)日：2007-01-04
申请号：US11422355
申请日：2006-06-06
申请人： Nand Baindur , Michael Gaul , Kevin Kreutter , Christian Baumann , Alexander Kim , Guozhang Xu , Bao-Ping Zhao
发明人： Nand Baindur , Michael Gaul , Kevin Kreutter , Christian Baumann , Alexander Kim , Guozhang Xu , Bao-Ping Zhao
IPC分类号： A61K31/517 , C07D403/04 , C07D401/04 , A61K31/4709
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04
摘要： The invention is directed to aminoquinoline and aminoquinazoline compounds of Formula I: where R1, R2, R3, B, Z, Q, p, q and X are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of FLT3 and/or TrkB, the use of such compounds to reduce or inhibit kinase activity of FLT3 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 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的氨基喹啉和氨基喹唑啉化合物：其中R 1，R 2，R 3，B，Z，Q， p，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TrkB的抑制剂，使用这些化合物来降低或抑制细胞中FLT3和/或TrkB的激酶活性或受试者，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。

6. 发明授权

US09045389B2 Biphenyl derivatives useful as glucagon receptor antagonists 有权
标题翻译：可用作胰高血糖素受体拮抗剂的联苯衍生物
公开(公告)号：US09045389B2
公开(公告)日：2015-06-02
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： A61K31/166 , C07C229/52 , C07C237/36
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。

7. 发明申请

US20110200587A1 AMINOTHIAZOLONES AS ESTROGEN RELATED RECEPTOR-ALPHA MODULATORS 有权
公开(公告)号：US20110200587A1
公开(公告)日：2011-08-18
申请号：US13028284
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 , C07D453/02 , A61K31/4985 , A61K31/427 , A61K31/5377 , A61K31/496 , A61K31/4439 , A61K31/454 , A61K31/439 , A61K31/506 , A61P19/08 , A61P19/06 , A61P19/10 , A61P35/04 , A61P35/00 , A61P19/02 , A61P17/06 , A61P1/02 , A61P29/00 , A61P11/00 , 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.

8. 发明申请

US20070254896A1 SUBSTITUTED PYRIMIDINE KINASE INHIBITORS 有权
标题翻译：取代的吡咯嗪激酶抑制剂
公开(公告)号：US20070254896A1
公开(公告)日：2007-11-01
申请号：US11690305
申请日：2007-03-23
申请人： Jeannene Butler , Peter Connolly , Angel Fuentes-Pesquera , Lee Greenberger , Shenlin Huang , Kenneth LaMontagne , Ronghua Li , Guozhang Xu
发明人： Jeannene Butler , Peter Connolly , Angel Fuentes-Pesquera , Lee Greenberger , Shenlin Huang , Kenneth LaMontagne , Ronghua Li , Guozhang Xu
IPC分类号： A61K31/505 , A61P25/00 , A61P35/00 , C07D239/30 , C07D239/34
CPC分类号： C07D401/12 , C07D239/47 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/14 , 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 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，其用于治疗慢性或急性蛋白激酶介导的疾病，病症或病症的合成和用途。

9. 发明授权

US08445690B2 Aminothiazolones as estrogen related receptor-alpha modulators 有权
公开(公告)号：US08445690B2
公开(公告)日：2013-05-21
申请号：US13028284
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.

10. 发明授权

US08344009B2 Substituted phenoxy thiazolidinediones as estrogen related receptor-á modulators 有权
标题翻译：取代苯氧基噻唑烷二酮作为雌激素相关受体α调节剂
公开(公告)号：US08344009B2
公开(公告)日：2013-01-01
申请号：US12899812
申请日：2010-10-07
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，升高的血糖水平和胰岛素抵抗。

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