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41. 发明授权

US07244843B2 Modulators of serotonin receptors 有权
标题翻译：血清素受体的调节剂
公开(公告)号：US07244843B2
公开(公告)日：2007-07-17
申请号：US10958325
申请日：2004-10-05
申请人： Dean A. Wacker , Jeffrey G. Varnes
发明人： Dean A. Wacker , Jeffrey G. Varnes
IPC分类号： C07D245/00 , C07D487/00 , C07D243/10 , C07D273/00 , C07D241/36
CPC分类号： C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention provides modulators of serotonin receptors, pharmaceutical compositions containing such modulators and methods for treating various diseases, conditions and disorders associated with modulation of serotonin receptors such as, for example: metabolic diseases, which includes but is not limited to obesity, diabetes, diabetic complications, atherosclerosis, impared glucose tolerance and dyslipidemia; central nervous system diseases which includes but is not limited to, anxiety, depression, obsessive compulsive disorder, panic disorder, psychosis, schizophrenia, sleep disorder, sexual disorder and social phobias; cephalic pain; migraine; and gastrointestinal disorders using such compounds and compositions.
摘要翻译：本发明提供5-羟色胺受体的调节剂，含有这些调节剂的药物组合物和用于治疗与调节血清素受体相关的各种疾病，病症和病症的方法，所述调节剂包括但不限于肥胖，糖尿病，糖尿病并发症，动脉粥样硬化，葡萄糖耐量异常和血脂异常; 包括但不限于焦虑，抑郁，强迫症，惊恐障碍，精神病，精神分裂症，睡眠障碍，性障碍和社交恐惧症的中枢神经系统疾病; 头痛偏头痛和使用这些化合物和组合物的胃肠道疾病。

42. 发明授权

US07230022B2 Substituted fused bicyclic amines as modulators of chemokine receptor activity 有权
标题翻译：取代的稠合双环胺作为趋化因子受体活性的调节剂
公开(公告)号：US07230022B2
公开(公告)日：2007-06-12
申请号：US11060483
申请日：2005-02-17
申请人： Douglas G. Batt , Percy H. Carter , Dean A. Wacker
发明人： Douglas G. Batt , Percy H. Carter , Dean A. Wacker
IPC分类号： A61K31/4035 , A61K31/41 , C07D257/04 , C07D209/44
CPC分类号： C07D403/12 , C07D217/04 , C07D401/04 , C07D401/14 , C07D403/10
摘要： The present application describes modulators of CCR3 of formula (Ia) and (Ib): or pharmaceutically acceptable salt forms thereof, wherein Z, R1, R2, R3, R4, R5, R5′, R6, a, b, c, d, and u are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using said modulators are disclosed.
摘要翻译：本申请描述了式（Ia）和（Ib）的CCR3的调节剂：或其药学上可接受的盐形式，其中Z，R 1，R 2，R SUP R 3，R 4，R 5，R 5，R 6，S 6， b，c，d和u如本文所定义。此外，公开了使用所述调节剂治疗和预防炎症性疾病如哮喘和过敏性疾病以及自身免疫病态如类风湿性关节炎和动脉粥样硬化的方法。

43. 发明授权

US08476283B2 [6,5]—bicyclic GPR119 G protein-coupled receptor agonists 有权
标题翻译： [6,5] - 双环GPR119 G蛋白偶联受体激动剂
公开(公告)号：US08476283B2
公开(公告)日：2013-07-02
申请号：US13307698
申请日：2011-11-30
申请人： John M. Fevig , Dean A. Wacker
发明人： John M. Fevig , Dean A. Wacker
IPC分类号： A01N43/90 , A61K31/519 , C07D487/00
CPC分类号： C07D471/04 , C07D473/34 , C07D487/04
摘要： Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n2, n3, n4, A, B, D, E, G, J, Y, R1 and R2 are defined herein.
摘要翻译：提供了新的化合物，它们是GPR119G蛋白偶联受体调节剂。 GPR119 G蛋白偶联受体调节剂可用于治疗，预防或减缓需要GPR119 G蛋白偶联受体调节剂治疗的疾病进展。这些新化合物具有以下结构：或其立体异构体或前药或其药学上可接受的盐，其中n2，n3，n4，A，B，D，E，G，J，Y，R1和R2如本文所定义。

44. 发明授权

US08372837B2 Pyridone and pyridazone analogues as GPR119 modulators 有权
标题翻译：吡啶酮和哒嗪类似物作为GPR119调节剂
公开(公告)号：US08372837B2
公开(公告)日：2013-02-12
申请号：US13003914
申请日：2009-07-15
申请人： Dean A. Wacker , Karen A. Rossi , Ying Wang , Gang Wu
发明人： Dean A. Wacker , Karen A. Rossi , Ying Wang , Gang Wu
IPC分类号： C07D401/12 , C07D401/14 , A61K31/501 , A61P7/12 , A61P3/10 , A61P3/04
CPC分类号： C07D403/14 , A61K31/4545 , A61K31/501 , A61K31/506 , A61K45/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/14
摘要： Novel compounds of structure Formula (I) or an enantiomer, a diastereomer, or a pharmaceutically acceptable salt thereof, wherein Z, R1, R2, R21, T1, T2, T3 and T4 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.
摘要翻译：其中Z，R1，R2，R21，T1，T2，T3和T4在本文中定义的结构式（I）的新型化合物或其对映异构体，非对映异构体或其药学上可接受的盐是GPR119G蛋白 - 偶联受体调节剂。 GPR119 G蛋白偶联受体调节剂可用于治疗，预防或减缓需要GPR119 G蛋白偶联受体调节剂治疗的疾病进展。因此，本公开还涉及包含这些新化合物的组合物以及通过使用任何这些新化合物或包含任何这些新化合物的组合物来治疗与GPR119G蛋白偶联受体的活性有关的疾病或病症的方法。

45. 发明授权

US08232404B2 Pyridone GPR119 G protein-coupled receptor agonists 有权
标题翻译：吡啶酮GPR119 G蛋白偶联受体激动剂
公开(公告)号：US08232404B2
公开(公告)日：2012-07-31
申请号：US13159497
申请日：2011-06-14
申请人： Dean A. Wacker , Karen A. Rossi , Ying Wang
发明人： Dean A. Wacker , Karen A. Rossi , Ying Wang
IPC分类号： A61K31/445 , C07D211/68
CPC分类号： C07D401/12 , C07D401/14
摘要： Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure Formula I or Formula IA.
摘要翻译：提供了新的化合物，它们是GPR119G蛋白偶联受体调节剂。 GPR119 G蛋白偶联受体调节剂可用于治疗，预防或减缓需要GPR119 G蛋白偶联受体调节剂治疗的疾病进展。这些新化合物具有结构式I或式IA。

46. 发明申请

US20110245227A1 PYRIDONE GPR119 G PROTEIN-COUPLED RECEPTOR AGONISTS 有权
标题翻译： PYRIDONE GPR119 G蛋白偶联受体激动剂
公开(公告)号：US20110245227A1
公开(公告)日：2011-10-06
申请号：US13159497
申请日：2011-06-14
申请人： Dean A. Wacker , Karen A. Rossi , Ying Wang
发明人： Dean A. Wacker , Karen A. Rossi , Ying Wang
IPC分类号： A61K31/454 , A61K31/506 , A61K31/4545 , A61K31/4439 , A61K31/4418 , C07D401/14 , C07D401/12 , C07D413/12 , C07D213/69 , A61P31/18 , A61P3/10 , A61P17/02 , A61P25/00 , A61P3/04 , A61P9/00 , A61P9/10 , A61P9/12 , A61P33/00 , A61P25/28 , A61P3/06 , A61P31/00 , A61P27/06 , A61P13/00 , A61P19/08
CPC分类号： C07D401/12 , C07D401/14
摘要： Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure Formula I or Formula IA.
摘要翻译：提供了新的化合物，它们是GPR119G蛋白偶联受体调节剂。 GPR119 G蛋白偶联受体调节剂可用于治疗，预防或减缓需要GPR119 G蛋白偶联受体调节剂治疗的疾病进展。这些新化合物具有结构式I或式IA。

47. 发明授权

US08003796B2 Pyridone GPR119 G protein-coupled receptor agonists 有权
标题翻译：吡啶酮GPR119 G蛋白偶联受体激动剂
公开(公告)号：US08003796B2
公开(公告)日：2011-08-23
申请号：US12173856
申请日：2008-07-16
申请人： Dean A. Wacker , Karen A. Rossi , Ying Wang
发明人： Dean A. Wacker , Karen A. Rossi , Ying Wang
IPC分类号： C07D211/68 , C07D401/00 , A01N43/40
CPC分类号： C07D401/12 , C07D401/14
摘要： Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure Formula I or Formula IA.
摘要翻译：提供了新的化合物，它们是GPR119G蛋白偶联受体调节剂。 GPR119 G蛋白偶联受体调节剂可用于治疗，预防或减缓需要GPR119 G蛋白偶联受体调节剂治疗的疾病进展。这些新化合物具有结构式I或式IA。

48. 发明授权

US07928230B2 Method for modulating GPR119 G protein-coupled receptor and selected compounds 有权
标题翻译：调节GPR119 G蛋白偶联受体和选定化合物的方法
公开(公告)号：US07928230B2
公开(公告)日：2011-04-19
申请号：US12173864
申请日：2008-07-16
申请人： Dean A. Wacker , Karen A. Rossi , Ying Wang
发明人： Dean A. Wacker , Karen A. Rossi , Ying Wang
IPC分类号： C07D401/00
CPC分类号： C07D401/12 , C07D401/14
摘要： A method of modulating the activity of the GPR119 G protein-coupled receptor comprising administering to a mammalian patient in need thereof a therapeutically effective amount of at least one compound of Formula I or Formula IA and, optionally, an additional therapeutic agent.
摘要翻译：调节GPR119G蛋白偶联受体的活性的方法，包括向有需要的哺乳动物患者施用治疗有效量的至少一种式I或式IA化合物和任选的另外的治疗剂。

49. 发明授权

US07910583B2 [6,6] and [6,7]-bicyclic GPR119 G protein-coupled receptor agonists 有权
公开(公告)号：US07910583B2
公开(公告)日：2011-03-22
申请号：US12112080
申请日：2008-04-30
申请人： John M. Fevig , Dean A. Wacker
发明人： John M. Fevig , Dean A. Wacker
IPC分类号： C07D498/04 , A61K31/5383
CPC分类号： C07D413/04 , C07D413/14 , C07D471/04 , C07D498/04
摘要： Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n1, n2, n3, n4, A, B, D, E, G, Y, Z, R1 and R2 are defined herein.

50. 发明授权

US07479496B2 Substituted spiro azabicyclics as modulators of chemokine receptor activity 有权
标题翻译：取代的螺氮氮杂双环作为趋化因子受体活性的调节剂
公开(公告)号：US07479496B2
公开(公告)日：2009-01-20
申请号：US11060246
申请日：2005-02-17
申请人： Douglas G. Batt , Dean A. Wacker , George V. De Lucca
发明人： Douglas G. Batt , Dean A. Wacker , George V. De Lucca
IPC分类号： A61K31/44 , C07D215/00
CPC分类号： C07D401/12 , C07D205/04 , C07D403/12 , C07D417/12
摘要： The present application describes modulators of CCR3 of formula (Ia) and (Ib): or pharmaceutically acceptable salt forms thereof, wherein Z, R1, R2, R3, R4, R5, R5′, R6, a, b, c, d, and u are as defined herein in the specification. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using modulators of formula (Ia) and (Ib) are disclosed.
摘要翻译：本申请描述了式（Ia）和（Ib）的CCR3或其药学上可接受的盐形式的调节剂：其中Z，R1，R2，R3，R4，R5，R5'，R6，a，b，c，并且u如说明书中所定义。此外，公开了使用式（Ia）和（Ib）的调节剂治疗和预防炎性疾病如哮喘和过敏性疾病以及类风湿性关节炎和动脉粥样硬化的自身免疫病态的方法。

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