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1. 发明申请

US20070093508A1 Non-basic melanin concentrating hormone receptor-1 antagonists 有权
公开(公告)号：US20070093508A1
公开(公告)日：2007-04-26
申请号：US11586147
申请日：2006-10-25
申请人： Saleem Ahmad , Khehyong Ngu , William Washburn
发明人： Saleem Ahmad , Khehyong Ngu , William Washburn
IPC分类号： A61K31/519 , C07D498/02
CPC分类号： C07D495/04
摘要： The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.

2. 发明申请

US20050085497A1 HMG-CoA reductase inhibitors and method 有权
标题翻译： HMG-CoA还原酶抑制剂及方法
公开(公告)号：US20050085497A1
公开(公告)日：2005-04-21
申请号：US10946055
申请日：2004-09-21
申请人： Saleem Ahmad , Jeffrey Robl , Khehyong Ngu
发明人： Saleem Ahmad , Jeffrey Robl , Khehyong Ngu
IPC分类号： A61K31/505 , A61K31/506 , A61P3/06 , C07D213/74 , C07D239/42 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D45/02
CPC分类号： C07D213/74 , C04B35/632 , C07D239/42 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12
摘要： Compounds are provided having the following structure which are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids, for example, lowering LDL cholesterol and/or increasing HDL cholesterol, and treating hyperlipidemia, dyslipidemia, hormone replacement therapy, hypercholsterolemia, hypertriglyceridemia and atherosclerosis as well as Alzheimer's disease and osteoporosis wherein X is N or CR5; and pharmaceutically acceptable salts thereof, wherein R1 to R7 are as defined herein. A method for treating the above diseases employing the above compounds is also provided.
摘要翻译：提供具有以下结构的化合物，其为HMG CoA还原酶抑制剂，因此具有抑制胆固醇生物合成，调节血清脂质，例如降低LDL胆固醇和/或增加HDL胆固醇，以及治疗高脂血症，血脂异常，激素替代疗法，高胆固醇血症，高甘油三酯血症和动脉粥样硬化以及阿尔茨海默病和骨质疏松症，其中X是N或CR 5; 和其药学上可接受的盐，其中R 1至R 7如本文所定义。还提供了使用上述化合物治疗上述疾病的方法。

3. 发明申请

US20050070588A1 Imidazolyl inhibitors of 15-lipoxygenase 有权
标题翻译： 15-脂氧合酶的咪唑基抑制剂
公开(公告)号：US20050070588A1
公开(公告)日：2005-03-31
申请号：US10932594
申请日：2004-09-01
申请人： David Weinstein , Khehyong Ngu , Jeffrey Robl
发明人： David Weinstein , Khehyong Ngu , Jeffrey Robl
IPC分类号： C07D233/54 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/14 , C07D417/04 , C07D471/10 , C07D487/08 , C07D233/38 , A61K31/4172 , A61K31/4178
CPC分类号： C04B35/632 , C07D233/64 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/14 , C07D417/04 , C07D471/10 , C07D487/08
摘要： The present invention provides imidazolyl inhibitors of 15-LO, pharmaceutical compositions containing such inhibitors and methods for treating diseases related to the 15-LO cascade using such compounds and compositions.
摘要翻译：本发明提供15-LO的咪唑基抑制剂，含有这种抑制剂的药物组合物和使用这些化合物和组合物治疗与15-LO级联相关的疾病的方法。

4. 发明申请

US20140080788A1 NOVEL BICYCLIC NITROGEN CONTAINING HETEROARYL TGR5 RECEPTOR MODULATORS 有权
标题翻译：新型双相含氮异氰酸酯TGR5受体调节剂
公开(公告)号：US20140080788A1
公开(公告)日：2014-03-20
申请号：US14113593
申请日：2012-04-27
申请人： Jeffrey A. Robl , Jun Li , Lawrence J. Kennedy , Steven J. Walker , Haixia Wang , William N. Washburn , Saleem Ahmad , Khehyong Ngu
发明人： Jeffrey A. Robl , Jun Li , Lawrence J. Kennedy , Steven J. Walker , Haixia Wang , William N. Washburn , Saleem Ahmad , Khehyong Ngu
IPC分类号： C07D401/04 , A61K45/06 , C07D215/08 , A61K31/47 , A61K31/473 , C07D221/16 , C07D413/04 , A61K31/5377 , C07D403/04 , A61K31/55 , A61K31/553 , C07D417/04 , A61K31/496 , C07D401/12 , C07D401/14 , A61K31/506 , C07D405/14 , C07D409/14 , C07F9/60 , A61K31/675 , A61K31/5415 , A61K31/4747 , A61K31/554 , A61K31/4709
CPC分类号： C07D401/04 , A61K31/47 , A61K31/4709 , A61K31/473 , A61K31/4747 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/5415 , A61K31/55 , A61K31/553 , A61K31/554 , A61K31/675 , A61K45/06 , C07D215/08 , C07D221/16 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07F9/60
摘要： Novel compounds of Formula I:or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein m, Q, T, U, V, ring A, X, Y, R3, R4, R4a, R5a, R5b, R5c, R5d, R5e, R6a, R6b, and R6c are defined herein, are provided which are TGR5 G protein-coupled receptor modulators. TGR5 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring TGR5 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 TGR5 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.
摘要翻译：式I的新型化合物或其对映体，非对映体，互变异构体，前药或其盐，其中m，Q，T，U，V，环A，X，Y，R 3，R 4，R 4a，R 5a，R 5b，R 5c，本文定义的R5e，R6a，R6b和R6c是TGR5G蛋白偶联受体调节剂。 TGR5G蛋白偶联受体调节剂可用于治疗，预防或减缓需要TGR5G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TGR5G蛋白偶联受体的活性相关的疾病或病症的方法。

5. 发明授权

US08563583B2 Pyridone analogs useful as melanin concentrating hormone receptor-1 antagonists 有权
标题翻译：可用作黑色素浓缩激素受体-1拮抗剂的吡啶酮类似物
公开(公告)号：US08563583B2
公开(公告)日：2013-10-22
申请号：US13255129
申请日：2010-03-09
申请人： Saleem Ahmad , William N. Washburn , Andres S. Hernandez , Jeffrey A. Robl , Khehyong Ngu , Zhenghua Wang
发明人： Saleem Ahmad , William N. Washburn , Andres S. Hernandez , Jeffrey A. Robl , Khehyong Ngu , Zhenghua Wang
IPC分类号： A61K31/44 , C07D213/78
CPC分类号： C07D213/38 , A61K31/4412 , A61K31/4427 , C07D213/26 , C07D213/30 , C07D213/32 , C07D213/68 , C07D401/04
摘要： MCHR1 antagonists are provided having the following Formula I: wherein all of the variables are defined herein. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety.
摘要翻译：提供具有以下式I的MCHR1拮抗剂：其中所有变量在本文中定义。这些化合物可用于治疗MCHR1介导的疾病，例如肥胖症，糖尿病，IBD，抑郁症和焦虑症。

6. 发明申请

US20110003759A1 NON-BASIC MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS AND METHODS 有权
标题翻译：非基因麦芽宁浓度HORMONE受体-1拮抗剂和方法
公开(公告)号：US20110003759A1
公开(公告)日：2011-01-06
申请号：US12881234
申请日：2010-09-14
申请人： Philip D. Stein , Sharon N. Bisaha , Saleen Ahmad , Khehyong Ngu , William N. Washburn
发明人： Philip D. Stein , Sharon N. Bisaha , Saleen Ahmad , Khehyong Ngu , William N. Washburn
IPC分类号： A61K31/497 , C07D241/18 , C07D401/12 , C07D403/12 , A61K31/4965 , A61K31/7034 , A61K31/5513 , A61P3/10 , A61P25/24 , A61P25/22 , A61P25/30 , A61P25/16 , A61P25/18 , A61P19/02 , A61P17/00
CPC分类号： C07D241/18 , C07D401/12
摘要： The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1, R2, R3, R8, and R9 are defined herein.Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.
摘要翻译：本申请提供化合物，包括其中R 1，R 2，R 3，R 8和R 9在本文中定义的根据式I的所有立体异构体，溶剂合物，前药和药学上可接受的形式。另外，本申请提供含有至少一种根据式I的化合物和任选的至少一种另外的治疗剂的药物组合物。最后，本申请提供了通过施用治疗有效剂量的根据式I的化合物治疗患有MCHR-1调节的疾病或病症例如肥胖，糖尿病，抑郁或焦虑的患者的方法。

7. 发明申请

US20060178386A1 Dihydroquinazolinones as 5HT modulators 有权
标题翻译：二氢喹唑啉酮作为5HT调节剂
公开(公告)号：US20060178386A1
公开(公告)日：2006-08-10
申请号：US11350997
申请日：2006-02-09
申请人： Saleem Ahmad , Khehyong Ngu
发明人： Saleem Ahmad , Khehyong Ngu
IPC分类号： A61K31/519 , C07D487/14
CPC分类号： C07D487/04
摘要： The present application 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：本申请提供5-羟色胺受体的调节剂，含有这种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。

8. 发明授权

US06541276B2 Methods for solid-phase synthesis of hydroxylamine compounds and derivatives and combinatorial libraries thereof 失效
标题翻译：羟胺化合物及其衍生物及其组合文库的固相合成方法
公开(公告)号：US06541276B2
公开(公告)日：2003-04-01
申请号：US08958638
申请日：1997-10-27
申请人： Dinesh V. Patel , Khehyong Ngu
发明人： Dinesh V. Patel , Khehyong Ngu
IPC分类号： G01N33543
CPC分类号： C07C259/06 , C07C259/04 , C40B40/00
摘要： A novel method for generating hydroxylamine, hydroxamic acid, hydroxyurea, and hydroxylsulfonamide compounds is disclosed. The method involves the nucleophilic attack of an alkoxyamine on a suitable solid phase support. Techniques of combinatorial chemistry can then be applied to the immobilized alkoxyamine to generate a diverse set of compounds. Cleavage of the compounds from the support yields a library of hydroxylamine or hydroxylamine derivative compounds, which can be screened for biological activity (e.g., inhibition of metalloproteases).
摘要翻译：公开了产生羟胺，异羟肟酸，羟基脲和羟基磺酰胺化合物的新方法。该方法涉及烷基胺在合适的固相载体上的亲核攻击。然后将组合化学的技术应用于固定化的烷氧基胺以产生不同组合的化合物。从支持物中切割化合物产生羟胺或羟胺衍生物化合物的文库，其可以筛选生物活性（例如抑制金属蛋白酶）。

9. 发明授权

US07745447B2 Substituted thieno[3,2-D]pyrimidines as non-basic melanin concentrating hormone receptor-1 antagonists 有权
标题翻译：取代的噻吩并[3,2-D]嘧啶作为非碱性黑色素浓缩激素受体-1拮抗剂
公开(公告)号：US07745447B2
公开(公告)日：2010-06-29
申请号：US11586147
申请日：2006-10-25
申请人： William N. Washburn , Saleem Ahmad , Khehyong Ngu
发明人： William N. Washburn , Saleem Ahmad , Khehyong Ngu
IPC分类号： C07D495/04 , A61K31/519 , A61P25/22 , A61P3/04 , A61P3/10
CPC分类号： C07D495/04
摘要： The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.
摘要翻译：本申请提供化合物，包括根据式I的所有立体异构体，溶剂合物，前药和药学上可接受的形式。另外，本申请提供含有至少一种根据式I的化合物和任选的至少一种另外的治疗剂的药物组合物。最后，本申请提供了通过施用治疗有效剂量的根据式I的化合物治疗患有MCHR-1调节的疾病或病症例如肥胖，糖尿病，抑郁或焦虑的患者的方法。

10. 发明授权

US07317032B2 Imidazolyl inhibitors of 15-lipoxygenase 有权
标题翻译： 15-脂氧合酶的咪唑基抑制剂
公开(公告)号：US07317032B2
公开(公告)日：2008-01-08
申请号：US10932594
申请日：2004-09-01
申请人： David S. Weinstein , Khehyong Ngu , Jeffrey A. Robl
发明人： David S. Weinstein , Khehyong Ngu , Jeffrey A. Robl
IPC分类号： A61K31/415 , C07D233/00
CPC分类号： C04B35/632 , C07D233/64 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/14 , C07D417/04 , C07D471/10 , C07D487/08
摘要： The present invention provides imidazolyl inhibitors of 15-LO, pharmaceutical compositions containing such inhibitors and methods for treating diseases related to the 15-LO cascade using such compounds and compositions.
摘要翻译：本发明提供15-LO的咪唑基抑制剂，含有这种抑制剂的药物组合物和使用这些化合物和组合物治疗与15-LO级联有关的疾病的方法。

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