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1. 发明授权

US07262210B2 Fluorinated pyridine N-oxide thrombin modulators and process for N-oxidation of nitrogen containing heteroaryls 有权
标题翻译：氟化吡啶N-氧化物凝血酶调节剂和含氮杂芳基的N-氧化方法
公开(公告)号：US07262210B2
公开(公告)日：2007-08-28
申请号：US11385056
申请日：2006-03-21
申请人： Kevin Kreutter , Tianbao Lu , Yu Kai Lee , Christopher Teleha , Mark Player , Xizhen Zhu
发明人： Kevin Kreutter , Tianbao Lu , Yu Kai Lee , Christopher Teleha , Mark Player , Xizhen Zhu
IPC分类号： A61K31/44 , C07D213/00
CPC分类号： C07D213/89 , C07D215/60 , C07D239/24 , C07D241/10
摘要： The present invention describes compounds of Formula I or a pharmaceutically acceptable salt thereof, for the prophylaxis, or treatment of diseases and conditions related to thrombin activity in a mammal. The present invention also relates to a novel method of N-oxidation of nitrogen containing heteroaryls.
摘要翻译：本发明描述了式I化合物或其药学上可接受的盐，用于预防或治疗与哺乳动物中凝血酶活性相关的疾病和病症。本发明还涉及含氮杂芳基的N-氧化的新方法。

2. 发明申请

US20070225282A1 PYRIDINES AND PYRIDINE N-OXIDES AS MODULATORS OF THROMBIN 有权
标题翻译：吡啶和吡啶N-氧化物作为THROMBIN的调节剂
公开(公告)号：US20070225282A1
公开(公告)日：2007-09-27
申请号：US11685544
申请日：2007-03-13
申请人： Mark Player , Tianbao Lu , Huaping Hu , Xizhen Zhu , Christopher Teleha , Kevin Kreutter
发明人： Mark Player , Tianbao Lu , Huaping Hu , Xizhen Zhu , Christopher Teleha , Kevin Kreutter
IPC分类号： A61K31/5377 , A61K31/4439 , C07D413/14
CPC分类号： C07D213/89 , C07D213/74 , C07D213/84 , C07D401/14 , C07D413/14
摘要： The present invention describes compounds of Formula I: wherein W, X, Y, Z, and Q are defined herein, or a pharmaceutically acceptable salt thereof, for the prophylaxis, or treatment of diseases and conditions related to thrombin activity in a mammal.
摘要翻译：本发明描述了式I的化合物：其中W，X，Y，Z和Q在本文中定义，或其药学上可接受的盐，用于预防或治疗与哺乳动物中凝血酶活性相关的疾病和病症。

3. 发明申请

US20060241148A1 Fluorinated pyridine N-oxide thrombin modulators and process for N-oxidation of nitrogen containing heteroaryls 有权
标题翻译：氟化吡啶N-氧化物凝血酶调节剂和含氮杂芳基的N-氧化方法
公开(公告)号：US20060241148A1
公开(公告)日：2006-10-26
申请号：US11385056
申请日：2006-03-21
申请人： Kevin Kreutter , Tianbao Lu , Yu Lee , Christopher Teleha , Mark Player , Xizhen Zhu
发明人： Kevin Kreutter , Tianbao Lu , Yu Lee , Christopher Teleha , Mark Player , Xizhen Zhu
IPC分类号： A61K31/444 , C07D213/84 , C07D401/02
CPC分类号： C07D213/89 , C07D215/60 , C07D239/24 , C07D241/10
摘要： The present invention describes compounds of Formula I or a pharmaceutically acceptable salt thereof, for the prophylaxis, or treatment of diseases and conditions related to thrombin activity in a mammal. The present invention also relates to a novel method of N-oxidation of nitrogen containing heteroaryls.
摘要翻译：本发明描述了式I化合物或其药学上可接受的盐，用于预防或治疗与哺乳动物中凝血酶活性相关的疾病和病症。本发明还涉及含氮杂芳基的N-氧化的新方法。

4. 发明授权

US07829584B2 Pyridines and pyridine N-oxides as modulators of thrombin 有权
标题翻译：吡啶和吡啶N-氧化物作为凝血酶的调节剂
公开(公告)号：US07829584B2
公开(公告)日：2010-11-09
申请号：US11685544
申请日：2007-03-13
申请人： Mark R. Player , Tianbao Lu , Huaping Hu , Xizhen Zhu , Christopher Teleha , Kevin Kreutter
发明人： Mark R. Player , Tianbao Lu , Huaping Hu , Xizhen Zhu , Christopher Teleha , Kevin Kreutter
IPC分类号： C07D213/00 , A61K31/44
CPC分类号： C07D213/89 , C07D213/74 , C07D213/84 , C07D401/14 , C07D413/14
摘要： The present invention describes compounds of Formula I: wherein W, X, Y, Z, and Q are defined herein, or a pharmaceutically acceptable salt thereof, for the prophylaxis, or treatment of diseases and conditions related to thrombin activity in a mammal.
摘要翻译：本发明描述了式I的化合物：其中W，X，Y，Z和Q在本文中定义，或其药学上可接受的盐，用于预防或治疗与哺乳动物中凝血酶活性相关的疾病和病症。

5. 发明授权

US08022209B2 Substituted nitrogen-containing heteroaryl derivatives useful as modulators of the histamine H4 receptor 有权
标题翻译：取代的含氮杂芳基衍生物可用作组胺H 4受体的调节剂
公开(公告)号：US08022209B2
公开(公告)日：2011-09-20
申请号：US12283488
申请日：2008-09-11
申请人： Michael D. Gaul , Bao-Ping Zhao , Xizhen Zhu
发明人： Michael D. Gaul , Bao-Ping Zhao , Xizhen Zhu
IPC分类号： C07D403/00
CPC分类号： C07D409/04 , C07D213/74 , C07D239/42 , C07D251/22 , C07D401/04 , C07D405/04 , C07D405/10 , C07D409/14
摘要： The present invention relates to substituted nitrogen-containing heteroaryl derivatives, pharmaceutical compositions containing them, and methods of using any of these derivatives and compositions for H4 receptor activity modulation and the treatment of states mediated by histamine H4 receptor activity.
摘要翻译：本发明涉及取代的含氮杂芳基衍生物，含有它们的药物组合物，以及使用任何这些衍生物和组合物用于H 4受体活性调节和由组胺H 4受体活性介导的状态的治疗的方法。

6. 发明申请

US20080085984A1 PREPARATION OF RADIOLABELLED HALOAROMATICS VIA POLYMER-BOUND INTERMEDIATES 有权
标题翻译：通过聚合物中间体制备无定形血红蛋白
公开(公告)号：US20080085984A1
公开(公告)日：2008-04-10
申请号：US11850306
申请日：2007-09-05
申请人： Duncan Hunter , Xizhen Zhu
发明人： Duncan Hunter , Xizhen Zhu
IPC分类号： C08G79/12
CPC分类号： C07C277/08 , A61K51/0406 , C07B2200/05 , C07C279/06
摘要： According to a first aspect of the invention, a process is disclosed for the preparation of radiolabelled haloaromatic compounds. According to a second aspect of the invention, intermediate precursor insoluble polymer compounds used in the preparation of the radiolabelled haloaromatics are disclosed, as well as processes for the preparation of the intermediate precursor insoluble polymer compounds.
摘要翻译：根据本发明的第一方面，公开了制备放射性标记的卤代芳族化合物的方法。根据本发明的第二方面，公开了用于制备放射性标记的卤代芳烃的中间体前体不溶性聚合物化合物，以及制备中间体前体不溶性聚合物化合物的方法。

7. 发明授权

US06461585B1 Preparation of radiolabelled haloaromatics via polymer-bound intermediates 有权
标题翻译：通过聚合物结合的中间体制备放射性标记的卤代芳族化合物
公开(公告)号：US06461585B1
公开(公告)日：2002-10-08
申请号：US09529017
申请日：2000-07-18
申请人： Duncan H. Hunter , Xizhen Zhu
发明人： Duncan H. Hunter , Xizhen Zhu
IPC分类号： A61K5100
CPC分类号： C07C277/08 , A61K51/0406 , C07B2200/05 , C07C279/06
摘要： According to a first aspect of the invention, a process is disclosed for the preparation of radiolabelled haloaromatic compounds. According to a second aspect of the invention, intermediate precursor insoluble polymer compounds used in the preparation of the radiolabelled haloaromatic are disclosed, as well as processes for the preparation of the intermediate precursor insoluble polymer compounds.
摘要翻译：根据本发明的第一方面，公开了制备放射性标记的卤代芳族化合物的方法。根据本发明的第二方面，公开了用于制备放射性标记的卤代芳族化合物的中间体前体不溶性聚合物化合物，以及制备中间体前体不溶性聚合物化合物的方法。

8. 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。

9. 发明申请

US20100274052A1 PREPARATION OF RADIOLABELLED HALOAROMATICS VIA POLYMER-BOUND INTERMEDIATES 审中-公开
标题翻译：通过聚合物中间体制备无定形血红蛋白
公开(公告)号：US20100274052A1
公开(公告)日：2010-10-28
申请号：US12702009
申请日：2010-02-08
申请人： Duncan H. Hunter , Xizhen Zhu
发明人： Duncan H. Hunter , Xizhen Zhu
IPC分类号： C07C279/02
CPC分类号： C07C277/08 , A61K51/0406 , C07B2200/05 , C07C279/06
摘要： According to a first aspect of the invention, a process is disclosed for the preparation of radiolabelled haloaromatic compounds. According to a second aspect of the invention, intermediate precursor insoluble polymer compounds used in the preparation of the radiolabelled haloaromatics are disclosed, as well as processes for the preparation of the intermediate precursor insoluble polymer compounds.
摘要翻译：根据本发明的第一方面，公开了制备放射性标记的卤代芳族化合物的方法。根据本发明的第二方面，公开了用于制备放射性标记的卤代芳烃的中间体前体不溶性聚合物化合物，以及制备中间体前体不溶性聚合物化合物的方法。

10. 发明申请

US20090069305A1 Substituted nitrogen-containing heteroaryl derivatives useful as modulators of the histamine H4 receptor 有权
标题翻译：取代的含氮杂芳基衍生物可用作组胺H 4受体的调节剂
公开(公告)号：US20090069305A1
公开(公告)日：2009-03-12
申请号：US12283488
申请日：2008-09-11
申请人： Michael D. Gaul , Bao-Ping Zhao , Xizhen Zhu
发明人： Michael D. Gaul , Bao-Ping Zhao , Xizhen Zhu
IPC分类号： A61K31/551 , C07D403/14 , C07D409/02 , A61K31/5377 , A61K31/496 , A61K31/4436 , A61P11/06 , A61P9/10 , A61P1/00 , A61P37/02 , A61P7/06 , A61P29/00 , A61P27/02 , A61P17/06 , A61P19/02 , A61P9/00 , A61P37/08 , A61K31/4439 , A61K31/53 , C07D413/14 , C07D401/14
CPC分类号： C07D409/04 , C07D213/74 , C07D239/42 , C07D251/22 , C07D401/04 , C07D405/04 , C07D405/10 , C07D409/14
摘要： The present invention relates to substituted nitrogen-containing heteroaryl derivatives, pharmaceutical compositions containing them, and methods of using any of these derivatives and compositions for H4 receptor activity modulation and the treatment of states mediated by histamine H4 receptor activity.
摘要翻译：本发明涉及取代的含氮杂芳基衍生物，含有它们的药物组合物，以及使用任何这些衍生物和组合物用于H 4受体活性调节和由组胺H 4受体活性介导的状态的治疗的方法。

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