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1.发明申请BENZENESULFONYL-CHROMANE, THIOCHROMANE, TETRAHYDRONAPHTHALENE AND RELATED GAMMA SECRETASE INHIBITORS 有权苯并呋喃酮，噻吗啉，四氢萘酮和相关的游离氨基酸酶抑制剂公开(公告)号：US20120264736A1
公开(公告)日：2012-10-18
申请号：US13267324
申请日：2011-10-06
申请人： Theodros Asberom , Thomas A. Bara , Chad E. Bennett , Duane A. Burnett , Mary Ann Caplen , John W. Clader , David J. Cole , Martin S. Domalski , Hubert B. Josien , Chad E. Knutson , Hongmei Li , Mark D. McBriar , Dmitri A. Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara K. Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
发明人： Theodros Asberom , Thomas A. Bara , Chad E. Bennett , Duane A. Burnett , Mary Ann Caplen , John W. Clader , David J. Cole , Martin S. Domalski , Hubert B. Josien , Chad E. Knutson , Hongmei Li , Mark D. McBriar , Dmitri A. Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara K. Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
IPC分类号： A61K31/352 , C07D409/12 , A61K31/381 , C07D405/12 , A61K31/4433 , A61K31/496 , C07D487/08 , A61K31/4995 , C07D405/14 , A61K31/4545 , C07D413/08 , A61K31/5377 , C07D493/04 , C07D491/052 , A61P25/28 , C07D311/80
CPC分类号： C07D311/22 , C07C317/14 , C07C317/20 , C07C317/44 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07D311/80 , C07D311/92 , C07D311/94 , C07D313/08 , C07D335/06 , C07D405/12 , C07D409/12 , C07D491/04 , C07D493/04
摘要： This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.
摘要翻译： 本发明公开了具有下式的新型γ分泌酶抑制剂：R2和R3，或R2和R4，或R3和R4与它们所连接的原子一起可以形成稠合的环烷基或稠合的杂环烷基环。 环烷基环或杂环烷基环可任选被一个或多个取代基取代。 一种或多种式（I）化合物或包含这些化合物的制剂可以是有用的，例如， 治疗阿尔茨海默病。
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2.发明申请N-PHENYL IMIDAZOLE CARBOXAMIDE INHIBITORS OF 3-PHOSPHOINOSITIDE-DEPENDENT PROTEIN KINASE-1 失效3-磷酸腺苷依赖性蛋白激酶-1的N-苯基咪唑酰胺酰胺抑制剂公开(公告)号：US20130079326A1
公开(公告)日：2013-03-28
申请号：US13699547
申请日：2011-05-24
申请人： Hon-Chung Tsui , Sunil Paliwal , Hyunjin M. Kim , Angela D. Kerekes , Mary Ann Caplen , Sara J. Esposite , Brian A. McKittrick , Thierry Olivier Fischmann , Ronald J. Doll , Matthew Paul Rainka
发明人： Hon-Chung Tsui , Sunil Paliwal , Hyunjin M. Kim , Angela D. Kerekes , Mary Ann Caplen , Sara J. Esposite , Brian A. McKittrick , Thierry Olivier Fischmann , Ronald J. Doll , Matthew Paul Rainka
IPC分类号： A61K45/06 , A61K31/454 , C07D401/14 , A61K31/4545 , C07D405/14 , A61K31/4178 , A61K31/4995 , A61K31/437 , C07D413/14 , A61K31/5377 , A61K31/551 , C07D403/04 , C07D409/14 , A61K31/506
CPC分类号： A61K45/06 , A61K31/4178 , A61K31/437 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/4995 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/69 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/08 , C07D491/10 , C07D498/08 , A61K2300/00
摘要： The present invention provide Imidazole Carboxamide Compounds of Formula (I): wherein D, T, R1, R2, R3, and R6 are as defined herein, and pharmaceutically acceptable salts of such Imidazole Carboxamide Compounds. The Imidazole Carboxamide Compounds are useful in the treatment of cancer and other aberrant conditions that result from overstimulation of the PDK-1 signaling pathway.
摘要翻译： 本发明提供式（I）的咪唑羧酰胺化合物：其中D，T，R 1，R 2，R 3和R 6如本文所定义，以及这些咪唑羧酰胺化合物的药学上可接受的盐。 咪唑羧酰胺化合物可用于治疗由过度刺激PDK-1信号通路引起的癌症和其他异常病症。
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公开(公告)号：US20110224193A1
公开(公告)日：2011-09-15
申请号：US13129821
申请日：2009-11-17
申请人： Pauline C. Ting , Robert Aslanian , Jianhua Cao , Mary Ann Caplen , Tin-Yau Chan , Hyunjin Kim , Jae-Hun Kim , Rongze Kuang , Joe F. Lee , Heping Wu
发明人： Pauline C. Ting , Robert Aslanian , Jianhua Cao , Mary Ann Caplen , Tin-Yau Chan , Hyunjin Kim , Jae-Hun Kim , Rongze Kuang , Joe F. Lee , Heping Wu
IPC分类号： A61K31/5513 , C07D413/14 , A61K31/4545 , A61K31/497 , A61P3/00 , A61P3/04 , A61P3/10 , A61P9/00 , A61P3/08
CPC分类号： C07D413/12 , A61K31/422 , A61K31/427 , C07D213/74 , C07D401/04 , C07D403/14 , C07D407/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/08 , C07D493/10
摘要： The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the 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. An illustrative compound of the invention is shown with this abstract.
摘要翻译： 本发明涉及作为二酰基甘油酰基转移酶（“DGAT”）抑制剂的新型杂环化合物，包含杂环化合物的药物组合物和用于治疗或预防心血管疾病，代谢障碍，肥胖症或肥胖相关障碍的化合物的用途， 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。 本摘要显示了本发明的说明性化合物。
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公开(公告)号：US20110224137A1
公开(公告)日：2011-09-15
申请号：US13129843
申请日：2009-11-17
申请人： Pauline C. Ting , Robert Aslanian , Mary Ann Caplen , Jianhua Cao , Tin-Yau Chan , David Kim , Hyunjin Kim , Jae-Hun Kim , Rongze Kuang , Joe F. Lee , John Schwerdt , Heping Wu , Nicolas Zorn
发明人： Pauline C. Ting , Robert Aslanian , Mary Ann Caplen , Jianhua Cao , Tin-Yau Chan , David Kim , Hyunjin Kim , Jae-Hun Kim , Rongze Kuang , Joe F. Lee , John Schwerdt , Heping Wu , Nicolas Zorn
IPC分类号： A61K38/28 , C07D409/14 , C07D243/08 , C07D401/14 , C07D221/00 , C07D211/06 , A61K31/497 , A61K31/551 , A61K31/4545 , A61K31/438 , A61K31/454 , A61P3/04 , A61P3/10
CPC分类号： C07D413/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04
摘要： The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the 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. An illustrative compound of the invention is shown below: formula (I).
摘要翻译： 本发明涉及作为二酰基甘油酰基转移酶（“DGAT”）抑制剂的新型杂环化合物，包含杂环化合物的药物组合物和用于治疗或预防心血管疾病，代谢障碍，肥胖症或肥胖相关障碍的化合物的用途， 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。 本发明的说明性化合物如下所示：式（I）。
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5.发明授权N-phenyl imidazole carboxamide inhibitors of 3-phosphoinositide-dependent protein kinase-1 失效3-磷酸肌醇依赖性蛋白激酶-1的N-苯基咪唑甲酰胺抑制剂公开(公告)号：US08623857B2
公开(公告)日：2014-01-07
申请号：US13699547
申请日：2011-05-24
申请人： Hon-Chung Tsui , Sunil Paliwal , Hyunjin M. Kim , Angela D. Kerekes , Mary Ann Caplen , Sara J. Esposite , Brian A. McKittrick , Thierry Olivier Fischmann , Ronald J. Doll , Matthew Paul Rainka , Ang Li
发明人： Hon-Chung Tsui , Sunil Paliwal , Hyunjin M. Kim , Angela D. Kerekes , Mary Ann Caplen , Sara J. Esposite , Brian A. McKittrick , Thierry Olivier Fischmann , Ronald J. Doll , Matthew Paul Rainka , Ang Li
IPC分类号： C07D498/08 , C07D243/00 , C07D401/14 , C07D409/14 , C07D405/14 , C07D413/14 , C07D403/04 , A61K31/5386 , A61K31/5377 , A61K31/506 , A61K31/551 , A61K31/454 , A61K31/4545 , A61K31/4178 , A61K31/437 , A61K31/4995 , A61K45/06
CPC分类号： A61K45/06 , A61K31/4178 , A61K31/437 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/4995 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/69 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/08 , C07D491/10 , C07D498/08 , A61K2300/00
摘要： The present invention provide Imidazole Carboxamide Compounds of Formula (I): wherein D, T, R1, R2, R3, and R6 are as defined herein, and pharmaceutically acceptable salts of such Imidazole Carboxamide Compounds. The Imidazole Carboxamide Compounds are useful in the treatment of cancer and other aberrant conditions that result from overstimulation of the PDK-1 signaling pathway.
摘要翻译： 本发明提供式（I）的咪唑羧酰胺化合物：其中D，T，R 1，R 2，R 3和R 6如本文所定义，以及这些咪唑羧酰胺化合物的药学上可接受的盐。 咪唑羧酰胺化合物可用于治疗由过度刺激PDK-1信号通路引起的癌症和其他异常病症。
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6.发明授权Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors 有权苯磺酰基 - 苯并二氢吡喃，二氢苯并噻喃，四氢萘和相关的γ分泌酶抑制剂公开(公告)号：US08067621B2
公开(公告)日：2011-11-29
申请号：US11654821
申请日：2007-01-18
申请人： Theodros Asberom , Thomas A. Bara , Chad E. Bennett , Duane A. Burnett , Mary Ann Caplen , John W. Clader , David J. Cole , Martin S. Domalski , Hubert B. Josien , Chad E. Knutson , Hongmei Li , Mark D. McBriar , Dmitri A. Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara K. Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
发明人： Theodros Asberom , Thomas A. Bara , Chad E. Bennett , Duane A. Burnett , Mary Ann Caplen , John W. Clader , David J. Cole , Martin S. Domalski , Hubert B. Josien , Chad E. Knutson , Hongmei Li , Mark D. McBriar , Dmitri A. Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara K. Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
IPC分类号： C07D493/00 , A61K31/35
CPC分类号： C07D311/22 , C07C317/14 , C07C317/20 , C07C317/44 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07D311/80 , C07D311/92 , C07D311/94 , C07D313/08 , C07D335/06 , C07D405/12 , C07D409/12 , C07D491/04 , C07D493/04
摘要： This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substitutents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.
摘要翻译： 本发明公开了具有下式的新型γ分泌酶抑制剂：R2和R3，或R2和R4，或R3和R4与它们所连接的原子一起可以形成稠合的环烷基或稠合的杂环烷基环。 环烷基环或杂环烷基环可任选被一个或多个取代基取代。 一种或多种式（I）化合物或包含这些化合物的制剂可以是有用的，例如， 治疗阿尔茨海默病。
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公开(公告)号：US20110224136A1
公开(公告)日：2011-09-15
申请号：US13129830
申请日：2009-11-17
申请人： Pauline C. Ting , Robert Aslanian , Mary Ann Caplen , Jianhua Cao , David Kim , Hyunjin Kim , Rongze Kuang , Joe F. Lee , John Schwerdt , Heping Wu , Gang Zhou , Nicolas Zorn
发明人： Pauline C. Ting , Robert Aslanian , Mary Ann Caplen , Jianhua Cao , David Kim , Hyunjin Kim , Rongze Kuang , Joe F. Lee , John Schwerdt , Heping Wu , Gang Zhou , Nicolas Zorn
IPC分类号： A61K38/28 , C07D409/14 , C07D413/14 , C07D401/14 , C07D211/32 , A61K31/4965 , A61K31/497 , A61K31/5377 , A61K31/445 , A61K31/454 , A61K31/4545 , A61P3/04 , A61P3/10
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14 , C07D413/04 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the 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. An illustrative compound of the invention is shown below.
摘要翻译： 本发明涉及作为二酰基甘油酰基转移酶（“DGAT”）抑制剂的新型杂环化合物，包含杂环化合物的药物组合物和用于治疗或预防心血管疾病，代谢障碍，肥胖症或肥胖相关障碍的化合物的用途， 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。 本发明的说明性化合物如下所示。
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8.发明申请Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors 有权苯磺酰基 - 苯并二氢吡喃，二氢苯并噻喃，四氢萘和相关的γ分泌酶抑制剂公开(公告)号：US20070197581A1
公开(公告)日：2007-08-23
申请号：US11654821
申请日：2007-01-18
申请人： Theodros Asberom , Thomas Bara , Chad Bennett , Duane Burnett , Mary Ann Caplen , John Clader , David Cole , Martin Domalski , Hubert Josien , Chad Knutson , Hongmei Li , Mark McBriar , Dmitri Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
发明人： Theodros Asberom , Thomas Bara , Chad Bennett , Duane Burnett , Mary Ann Caplen , John Clader , David Cole , Martin Domalski , Hubert Josien , Chad Knutson , Hongmei Li , Mark McBriar , Dmitri Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
IPC分类号： A61K31/4741 , A61K31/473 , A61K31/353 , A61K31/19
CPC分类号： C07D311/22 , C07C317/14 , C07C317/20 , C07C317/44 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07D311/80 , C07D311/92 , C07D311/94 , C07D313/08 , C07D335/06 , C07D405/12 , C07D409/12 , C07D491/04 , C07D493/04
摘要： This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substitutents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.
摘要翻译： 本发明公开了下式的新型γ分泌酶抑制剂：R 2和R 3，或R 2和R 4 O / >或R 3和R 4与它们所连接的原子一起可以形成稠合的环烷基或稠合的杂环烷基环。 环烷基环或杂环烷基环可任选被一个或多个取代基取代。 一种或多种式（I）化合物或包含这些化合物的制剂可以是有用的，例如， 治疗阿尔茨海默病。
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公开(公告)号：US08716312B2
公开(公告)日：2014-05-06
申请号：US13129843
申请日：2009-11-17
申请人： Pauline C. Ting , Robert Aslanian , Mary Ann Caplen , Jianhua Cao , Tin-Yau Chan , David Kim , Hyunjin Kim , Jae-Hun Kim , Rongze Kuang , Joe F. Lee , John Schwerdt , Heping Wu , Nicolas Zorn
发明人： Pauline C. Ting , Robert Aslanian , Mary Ann Caplen , Jianhua Cao , Tin-Yau Chan , David Kim , Hyunjin Kim , Jae-Hun Kim , Rongze Kuang , Joe F. Lee , John Schwerdt , Heping Wu , Nicolas Zorn
IPC分类号： A61P3/00 , A61P9/00 , A61K31/445 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
CPC分类号： C07D413/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04
摘要： The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the 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. An illustrative compound of the invention is shown below:
摘要翻译： 本发明涉及作为二酰基甘油酰基转移酶（“DGAT”）抑制剂的新型杂环化合物，包含杂环化合物的药物组合物和用于治疗或预防心血管疾病，代谢障碍，肥胖症或肥胖相关障碍的化合物的用途， 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。 本发明的说明性化合物如下所示：
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10.发明授权Substituted n-aryl amidines as selective D1 dopamine receptor antagonists for the treatment of obesity and CNS disorders 失效取代的正芳基脒作为治疗肥胖和CNS疾病的选择性D1多巴胺受体拮抗剂公开(公告)号：US07423149B2
公开(公告)日：2008-09-09
申请号：US11018990
申请日：2004-12-21
申请人： Duane A. Burnett , Wen-Lian Wu , Martin S. Domalski , Mary Ann Caplen , Richard Spring , Jean E. Lachowicz
发明人： Duane A. Burnett , Wen-Lian Wu , Martin S. Domalski , Mary Ann Caplen , Richard Spring , Jean E. Lachowicz
IPC分类号： C07D241/04 , C07D295/00 , C07D211/00 , C07C257/00
CPC分类号： C07D295/205 , A61K45/06 , C07C255/57 , C07C257/14 , C07C257/18 , C07D209/08 , C07D209/86 , C07D211/14 , C07D213/53 , C07D215/26 , C07D215/48 , C07D233/64 , C07D295/073 , C07D295/112 , C07D295/155 , C07D317/58 , C07D319/18 , C07D333/20 , C07D405/12
摘要： The present invention provides compounds, which, are novel antagonists for D1 receptors as well as methods for preparing such compounds. In another embodiment, the invention provides pharmaceutical compositions comprising such D1 receptor antagonists as well as methods of using them to treat CNS disorders, obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
摘要翻译： 本发明提供了作为D 1受体的新型拮抗剂的化合物以及制备这些化合物的方法。 在另一个实施方案中，本发明提供包含这种D 1受体拮抗剂的药物组合物以及使用它们治疗CNS障碍，肥胖，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法。
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