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1. 发明授权

US08889683B2 Substituted quinoxalines as inhibitors of fatty acid binding protein 有权
标题翻译：取代喹喔啉作为脂肪酸结合蛋白的抑制剂
公开(公告)号：US08889683B2
公开(公告)日：2014-11-18
申请号：US13242426
申请日：2011-09-23
申请人： Clifford Cheng , Gerald W. Shipps, Jr. , Xiaohua Huang , Ying Huang , Ning Shao , Ashwin Rao , Anandan Palani , Peter Orth , Johannes H. Voigt , Robert J. Herr , Lana Michele Rossiter , Qi Zeng , Xianfeng Sun
发明人： Clifford Cheng , Gerald W. Shipps, Jr. , Xiaohua Huang , Ying Huang , Ning Shao , Ashwin Rao , Anandan Palani , Peter Orth , Johannes H. Voigt , Robert J. Herr , Lana Michele Rossiter , Qi Zeng , Xianfeng Sun
IPC分类号： A61K31/498 , C07D241/44 , C07D401/14 , C07D403/14 , C07D413/06 , C07D401/06 , C07D403/12 , C07D403/06
CPC分类号： C07D403/06 , C07D241/44 , C07D401/06 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/06
摘要： The present invention relates to novel quinoxaline compounds of Formula I: as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the quinoxaline compounds and the use of the quinoxaline compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
摘要翻译：本发明涉及式I的新型喹喔啉化合物：作为脂肪酸结合蛋白（“FABP”）抑制剂，包含喹喔啉化合物的药物组合物和喹喔啉化合物用于治疗或预防心血管疾病，代谢紊乱，肥胖症或肥胖相关疾病，糖尿病，血脂异常，糖尿病并发症，葡萄糖耐量降低或空腹血糖受损。

2. 发明申请

US20070066630A1 Nitrogen-containing heterocyclic compounds and methods of use thereof 有权
标题翻译：含氮杂环化合物及其使用方法
公开(公告)号：US20070066630A1
公开(公告)日：2007-03-22
申请号：US11600216
申请日：2006-11-15
申请人： Anandan Palani , Jing Su , Dong Xiao , Xianhai Huang , Ashwin Rao , Xiao Chen , Haiqun Tang , Jun Qin , Ying Huang , Robert Aslanian , Brian McKittrick , Sylvia Degrado
发明人： Anandan Palani , Jing Su , Dong Xiao , Xianhai Huang , Ashwin Rao , Xiao Chen , Haiqun Tang , Jun Qin , Ying Huang , Robert Aslanian , Brian McKittrick , Sylvia Degrado
IPC分类号： A61K31/519 , C07D491/02
CPC分类号： C07D491/052
摘要： The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, esters, and tautomers thereof, wherein: Q is selected from the group consisting of: L is selected from the group consisting of: pharmaceutically compositions comprising one or more compounds of formula (I), and methods of using the compounds of formula (I).
摘要翻译：本发明提供式（I）化合物及其药学上可接受的盐，溶剂合物，酯和互变异构体，其中：Q选自：L选自：包含一种或多种式（I）化合物和使用式（I）化合物的方法。

3. 发明申请

US20080019978A1 NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF 有权
标题翻译：含氮杂环化合物及其使用方法
公开(公告)号：US20080019978A1
公开(公告)日：2008-01-24
申请号：US11771538
申请日：2007-06-29
申请人： Anandan Palani , Jing Su , Dong Xiao , Xianhai Huang , Ashwin Rao , Xiao Chen , Haiqun Tang , Jun Qin , Ying Huang , Robert Aslanian , Brian McKittrick , Sylvia Degrado
发明人： Anandan Palani , Jing Su , Dong Xiao , Xianhai Huang , Ashwin Rao , Xiao Chen , Haiqun Tang , Jun Qin , Ying Huang , Robert Aslanian , Brian McKittrick , Sylvia Degrado
IPC分类号： A61K31/519 , A61K31/397 , A61K31/56 , A61K31/60 , A61K38/16 , A61K39/395 , A61P1/00 , A61P11/00 , A61P3/00 , A61P3/10 , A61P35/00 , A61P9/00 , C07D239/70
CPC分类号： C07D491/04 , C07D471/04
摘要： The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, esters, and tautomers thereof, wherein: Q is selected from the group consisting of: and L is selected from the group consisting of: pharmaceutically compositions comprising one or more compounds of formula (I), and methods of using the compounds of formula (I).
摘要翻译：本发明提供式（I）的化合物及其药学上可接受的盐，溶剂合物，酯和互变异构体，其中：Q选自：和L选自：药物组合物，其包含一种或多种更多的式（I）化合物和使用式（I）化合物的方法。

4. 发明申请

US20060264489A1 Heterocycles as nicotinic acid receptor agonists for the treatment of dyslipidemia 有权
标题翻译：杂环作为治疗血脂异常的烟酸受体激动剂
公开(公告)号：US20060264489A1
公开(公告)日：2006-11-23
申请号：US11432133
申请日：2006-05-11
申请人： Anandan Palani , Jing Su , Dong Xiao , Xianhai Huang , Ashwin Rao , Xiao Chen , Haiqun Tang , Jun Qin , Ying Huang , Robert Aslanian , Brian McKittrick
发明人： Anandan Palani , Jing Su , Dong Xiao , Xianhai Huang , Ashwin Rao , Xiao Chen , Haiqun Tang , Jun Qin , Ying Huang , Robert Aslanian , Brian McKittrick
IPC分类号： A01N43/50
CPC分类号： C07D471/04 , C07D491/04 , C07D491/052
摘要： A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, or tautomer thereof, wherein: Q is selected from the group consisting of: and L is selected from the group consisting of: or a pharmaceutically acceptable salt, solvate, ester, or tautomer thereof, are useful in treating diseases, disorders, or conditions such as metabolic syndrome and dyslipidemia.
摘要翻译：具有式（I）的通式结构的化合物或其药学上可接受的盐，溶剂化物，酯或互变异构体，其中：Q选自：和L选自：或其药学上可接受的盐可接受的盐，溶剂合物，酯或互变异构体，可用于治疗疾病，病症或病症如代谢综合征和血脂异常。

5. 发明授权

US08592383B2 Cycloalkyl-fused tetrahydroquinolines as CRTH2 receptor modulators 有权
标题翻译：环烷基稠合四氢喹啉作为CRTH2受体调节剂
公开(公告)号：US08592383B2
公开(公告)日：2013-11-26
申请号：US13523354
申请日：2012-06-14
申请人： Xianhai Huang , Jason Brubaker , Scott L. Peterson , John W. Butcher , Joshua T. Close , Michelle Martinez , Rachel Nicola MacCoss , Joon O. Jung , Phieng Siliphaivanh , Hongjun Zhang , Robert G. Aslanian , Purakkattle Johny Biju , Li Dong , Ying Huang , Kevin D. McCormick , Anandan Palani , Ning Shao , Wei Zhou
发明人： Xianhai Huang , Jason Brubaker , Scott L. Peterson , John W. Butcher , Joshua T. Close , Michelle Martinez , Rachel Nicola MacCoss , Joon O. Jung , Phieng Siliphaivanh , Hongjun Zhang , Robert G. Aslanian , Purakkattle Johny Biju , Li Dong , Ying Huang , Kevin D. McCormick , Anandan Palani , Ning Shao , Wei Zhou
IPC分类号： C07D221/16 , C07D401/10 , C07D413/10 , A61K31/473 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/706 , A61P11/00 , A61P11/06 , A61P37/08 , C07H15/26
CPC分类号： C07D221/16 , A61K31/473 , A61K31/501 , A61K31/506 , A61K31/5377 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/10 , C07D417/12
摘要： The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R1, R2, R7, R8, R8a, E, Y, Z, n, u, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.
摘要翻译：本发明提供一些式（I）的环烷基稠合的四氢喹啉及其药学上可接受的盐和酯，其中R1，R2，R7，R8，R8a，E，Y，Z，n，u和t如本文所定义。本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗与不受控制或不适当刺激CRTH2功能相关的疾病或病症的方法。

6. 发明申请

US20140128367A1 CYCLOALKYL-FUSED TETRAHYDROQUINOLINES AS CRTH2 RECEPTOR MODULATORS 审中-公开
标题翻译：作为CRTH2受体调节剂的环丙基二烯丙基四氢喹啉
公开(公告)号：US20140128367A1
公开(公告)日：2014-05-08
申请号：US14126579
申请日：2012-06-14
申请人： Xianhai Huang , Jason Brubaker , Scott L. Peterson , John W. Butcher , Joshua T. Close , Michelle Martinez , Rachel Nicola MacCoss , Joon O. Jung , Phieng Siliphaivanh , Hongjun Zhang , Robert G. Aslanian , Purakkattle Johny Biju , Li Dong , Ying Huang , Kevin D. McCormick , Anandan Palani , Ning Shao , Wei Zhou
发明人： Xianhai Huang , Jason Brubaker , Scott L. Peterson , John W. Butcher , Joshua T. Close , Michelle Martinez , Rachel Nicola MacCoss , Joon O. Jung , Phieng Siliphaivanh , Hongjun Zhang , Robert G. Aslanian , Purakkattle Johny Biju , Li Dong , Ying Huang , Kevin D. McCormick , Anandan Palani , Ning Shao , Wei Zhou
IPC分类号： C07D221/16 , A61K31/5377 , C07D401/12 , A61K31/506 , A61K31/501 , A61K31/473 , C07D401/10
CPC分类号： C07D221/16 , A61K31/473 , A61K31/501 , A61K31/506 , A61K31/5377 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/10 , C07D417/12
摘要： The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R1, R2, R7, R8a, E, Y, Z, n, u, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.
摘要翻译：本发明提供一些式（I）的环烷基稠合的四氢喹啉及其药学上可接受的盐和酯，其中R1，R2，R7，R8a，E，Y，Z，n，u和t如本文所定义。本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗与不受控制或不适当刺激CRTH2功能相关的疾病或病症的方法。

7. 发明申请

US20120329743A1 CYCLOALKYL-FUSED TETRAHYDROQUINOLINES AS CRTH2 RECEPTOR MODULATORS 有权
标题翻译：作为CRTH2受体调节剂的环丙基二烯丙基四氢喹啉
公开(公告)号：US20120329743A1
公开(公告)日：2012-12-27
申请号：US13523354
申请日：2012-06-14
申请人： Xianhai Huang , Jason Brubaker , Scott L. Peterson , John W. Butcher , Joshua T. Close , Michelle Martinez , Rachel Nicola MacCoss , Joon O. Jung , Phieng Siliphaivanh , Hongjun Zhang , Robert G. Aslanian , Purakkattle Johny Biju , Li Dong , Ying Huang , Kevin D. McCormick , Anandan Palani , Ning Shao , Wei Zhou
发明人： Xianhai Huang , Jason Brubaker , Scott L. Peterson , John W. Butcher , Joshua T. Close , Michelle Martinez , Rachel Nicola MacCoss , Joon O. Jung , Phieng Siliphaivanh , Hongjun Zhang , Robert G. Aslanian , Purakkattle Johny Biju , Li Dong , Ying Huang , Kevin D. McCormick , Anandan Palani , Ning Shao , Wei Zhou
IPC分类号： C07D221/16 , C07D413/10 , A61K31/5377 , C07D401/10 , A61P11/00 , A61K31/501 , C07H15/26 , A61K31/706 , A61P11/06 , A61P37/08 , A61K31/473 , A61K31/506
CPC分类号： C07D221/16 , A61K31/473 , A61K31/501 , A61K31/506 , A61K31/5377 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/10 , C07D417/12
摘要： The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R1, R2, R7, R8, R8a, E, Y, Z, n, u, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.
摘要翻译：本发明提供一些式（I）的环烷基稠合的四氢喹啉及其药学上可接受的盐和酯，其中R1，R2，R7，R8，R8a，E，Y，Z，n，u和t如本文所定义。本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗与不受控制或不适当刺激CRTH2功能相关的疾病或病症的方法。

8. 发明授权

US07723342B2 Heterocycles as nicotinic acid receptor agonists for the treatment of dyslipidemia 有权
标题翻译：杂环作为治疗血脂异常的烟酸受体激动剂
公开(公告)号：US07723342B2
公开(公告)日：2010-05-25
申请号：US11432133
申请日：2006-05-11
申请人： Anandan Palani , Jing Su , Dong Xiao , Xianhai Huang , Ashwin U. Rao , Xiao Chen , Haiqun Tang , Jun Qin , Ying Huang , Robert G. Aslanian , Brian A. McKittrick
发明人： Anandan Palani , Jing Su , Dong Xiao , Xianhai Huang , Ashwin U. Rao , Xiao Chen , Haiqun Tang , Jun Qin , Ying Huang , Robert G. Aslanian , Brian A. McKittrick
IPC分类号： C07D491/052 , A61K31/519 , A61P35/00 , A61P29/00 , A61P3/10 , A61P9/00 , A61P11/00
CPC分类号： C07D471/04 , C07D491/04 , C07D491/052
摘要： A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, or tautomer thereof, wherein: Q is selected from the group consisting of: and L is selected from the group consisting of: or a pharmaceutically acceptable salt, solvate, ester, or tautomer thereof, are useful in treating diseases, disorders, or conditions such as metabolic syndrome and dyslipidemia.
摘要翻译：具有式（I）的通式结构的化合物或其药学上可接受的盐，溶剂化物，酯或互变异构体，其中：Q选自：和L选自：或其药学上可接受的盐可接受的盐，溶剂合物，酯或互变异构体，可用于治疗疾病，病症或病症如代谢综合征和血脂异常。

9. 发明申请

US20120231017A1 HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS 有权
公开(公告)号：US20120231017A1
公开(公告)日：2012-09-13
申请号：US13415404
申请日：2012-03-08
申请人： ZHAONING ZHU , Brian McKittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voigt , Corey O. Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert D. Mozzola , John P. Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Xiaoiang Liu , Tao Guo , Thuy X. E. Le , Kurt W. Sainoz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse , Ying Huang , Guoqing Li , Jianping Pan , Jeffrey A. Misiaszek , Gaifa Lai , Jingqi Duo , Chuanxing Qu , Yuefei Shao
发明人： ZHAONING ZHU , Brian McKittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voigt , Corey O. Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert D. Mozzola , John P. Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Xiaoiang Liu , Tao Guo , Thuy X. E. Le , Kurt W. Sainoz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse , Ying Huang , Guoqing Li , Jianping Pan , Jeffrey A. Misiaszek , Gaifa Lai , Jingqi Duo , Chuanxing Qu , Yuefei Shao
IPC分类号： A61K39/395 , C07D239/70 , C07F5/02 , C07D403/10 , A61K31/513 , A61K31/506 , C07D409/04 , C07D409/14 , C07D401/04 , C07D405/14 , C07D417/14 , C07D417/04 , C07D413/14 , C07D413/10 , A61K31/5377 , A61P29/00 , A61P9/00 , A61P25/28 , A61P31/10 , A61P33/02 , C07D495/04 , A61P25/00 , A61P31/04 , C07D239/22
CPC分类号： C07D233/88 , A61K31/4168 , A61K31/4178 , C07D239/22 , C07D401/06 , C07D401/10 , C07D403/06 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/10 , C07D417/14 , C07D495/10
摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

10. 发明授权

US08012953B2 Macrocyclic beta-secretase inhibitors 有权
标题翻译：大环β-分泌酶抑制剂
公开(公告)号：US08012953B2
公开(公告)日：2011-09-06
申请号：US12571840
申请日：2009-10-01
申请人： Andrew W. Stamford , Ying Huang , Guoqing Li , Corey O. Strickland , Johannes H. Voigt
发明人： Andrew W. Stamford , Ying Huang , Guoqing Li , Corey O. Strickland , Johannes H. Voigt
IPC分类号： A61K31/33 , C07D513/00
CPC分类号： C07D498/04 , C07D413/06
摘要： Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, n and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of β-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
摘要翻译：公开了下式的新化合物或其药学上可接受的盐或溶剂化物，其中R1，R2，R3，n和X如说明书中所定义。还公开了包含式I化合物的药物组合物。还公开了治疗认知或神经变性疾病如阿尔茨海默病的方法。还公开了治疗认知或神经退行性疾病的方法，包括向需要这种治疗的患者施用至少一种式I化合物和至少一种选自除了那些的那些之外的其他化合物式I，HMG-CoA还原酶抑制剂，γ-分泌酶抑制剂，非甾体抗炎剂，N-甲基-D-天冬氨酸受体拮抗剂，胆碱酯酶抑制剂和抗淀粉样蛋白抗体。

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