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1. 发明申请

WO2014081996A1 NOVEL COMPOUNDS AS DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS 审中-公开
标题翻译：新型化合物作为二乙酰胆碱酯酶抑制剂
公开(公告)号：WO2014081996A1
公开(公告)日：2014-05-30
申请号：PCT/US2013/071380
申请日：2013-11-22
申请人： GLAXOSMITHKLINE LLC
发明人： CHEUNG, Mui , TANGIRALA, Raghuram, S.
IPC分类号： A61K31/519
CPC分类号： A61K31/519
摘要： This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1 ), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGA T-1 activity may have therapeutic benefit.
摘要翻译：本发明涉及作为酰基辅酶A：二酰基甘油酰基转移酶1（DGAT-1）的抑制剂的新化合物，含有它们的药物组合物，其制备方法及其在治疗中的用途，单独使用或与体重管理疗法组合或其他甘油三酸酯降低治疗用于预防或治疗与DGAT-1功能障碍相关的疾病或其中DGA T-1活性的调节可具有治疗益处。

2. 发明申请

WO2011119701A1 TRPV4 ANTAGONISTS 审中-公开
公开(公告)号：WO2011119701A1
公开(公告)日：2011-09-29
申请号：PCT/US2011/029579
申请日：2011-03-23
申请人： GLAXOSMITHKLINE LLC , BROOKS, Carl, A. , CHEUNG, Mui , EIDAM, Hilary, S. , FOX, Ryan, M. , HILFIKER, Mark, A. , MANAS, Eric, S. , YE, Guosen
发明人： BROOKS, Carl, A. , CHEUNG, Mui , EIDAM, Hilary, S. , FOX, Ryan, M. , HILFIKER, Mark, A. , MANAS, Eric, S. , YE, Guosen
IPC分类号： A01N43/42 , A61K31/47
CPC分类号： C07D401/06 , C07D401/14
摘要： The present invention relates to quinoline analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
摘要翻译：本发明涉及喹啉类似物，含有它们的药物组合物及其作为TRPV4拮抗剂的用途。

3. 发明申请

WO2011119693A1 TRPV4 ANTAGONISTS 审中-公开
标题翻译： TRPV4拮抗剂
公开(公告)号：WO2011119693A1
公开(公告)日：2011-09-29
申请号：PCT/US2011/029570
申请日：2011-03-23
申请人： GLAXOSMITHKLINE LLC , BROOKS, Carl, A. , CHEUNG, Mui , FOX, Ryan, M. , GOODMAN, Krista, B. , HILFIKER, Mark, A. , YE, Guosen
发明人： BROOKS, Carl, A. , CHEUNG, Mui , FOX, Ryan, M. , GOODMAN, Krista, B. , HILFIKER, Mark, A. , YE, Guosen
IPC分类号： A61K31/497
CPC分类号： A61K31/5377 , A61K31/4709 , A61K31/497
摘要： The present invention relates to indole or benzothiophene analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
摘要翻译：本发明涉及吲哚或苯并噻吩类似物，含有它们的药物组合物以及它们作为TRPV4拮抗剂的用途。

4. 发明申请

WO2014081994A1 NOVEL COMPOUNDS AS DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS 审中-公开
标题翻译：新型化合物作为二乙酰胆碱酯酶抑制剂
公开(公告)号：WO2014081994A1
公开(公告)日：2014-05-30
申请号：PCT/US2013/071376
申请日：2013-11-22
申请人： GLAXOSMITHKLINE LLC
发明人： CHEUNG, Mui , TANGIRALA, Raghuram, S.
IPC分类号： A61K31/553
CPC分类号： C07D498/04 , C07D519/00
摘要： This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1 ), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit.
摘要翻译：本发明涉及作为酰基辅酶A：二酰基甘油酰基转移酶1（DGAT-1）的抑制剂的新化合物，含有它们的药物组合物，其制备方法及其在治疗中的用途，单独使用或与体重管理疗法组合或其他甘油三酸酯降低治疗用于预防或治疗与DGAT-1功能障碍有关的疾病或DGAT-1活性调节可能具有治疗益处。

5. 发明申请

WO2011119704A1 TRPV4 ANTAGONISTS 审中-公开
标题翻译： TRPV4拮抗剂
公开(公告)号：WO2011119704A1
公开(公告)日：2011-09-29
申请号：PCT/US2011/029584
申请日：2011-03-23
申请人： GLAXOSMITHKLINE LLC , BROOKS, Carl, A. , CHEUNG, Mui , EIDAM, Hilary, S. , FOX, Ryan, M , HILFKER, Mark, A. , MANAS, Eric, S. , YE, Guosen
发明人： BROOKS, Carl, A. , CHEUNG, Mui , EIDAM, Hilary, S. , FOX, Ryan, M , HILFKER, Mark, A. , MANAS, Eric, S. , YE, Guosen
IPC分类号： A01N43/42 , A61K31/47
CPC分类号： C07D413/14 , C07D401/14
摘要： The present invention relates to quinoline analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
摘要翻译：本发明涉及喹啉类似物，含有它们的药物组合物及其作为TRPV4拮抗剂的用途。

6. 发明申请

WO2012174342A1 TRPV4 ANTAGONISTS 审中-公开
公开(公告)号：WO2012174342A1
公开(公告)日：2012-12-20
申请号：PCT/US2012/042607
申请日：2012-06-15
申请人： GLAXOSMITHKLINE LLC , BROOKS, Carl , CHEUNG, Mui , EIDAM, Hilary, Schenck , GOODMAN, Krista, B. , HAMMOND, Marlys , HILFIKER, Mark, A. , PATTERSON, Jaclyn, R. , STOY, Patrick , YE, Guosen
发明人： BROOKS, Carl , CHEUNG, Mui , EIDAM, Hilary, Schenck , GOODMAN, Krista, B. , HAMMOND, Marlys , HILFIKER, Mark, A. , PATTERSON, Jaclyn, R. , STOY, Patrick , YE, Guosen
IPC分类号： A01N43/52 , A61K31/415
CPC分类号： C07D413/14 , C07D263/52 , C07D413/06 , C07D413/08
摘要： The present invention relates to spirocarbamate analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
摘要翻译：本发明涉及螺氨酸甲酯类似物，含有它们的药物组合物及其作为TRPV4拮抗剂的用途。

7. 发明申请

WO2012162129A1 NOVEL COMPOUNDS AS DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS 审中-公开
标题翻译：新型化合物作为二乙酰胆碱酯酶抑制剂
公开(公告)号：WO2012162129A1
公开(公告)日：2012-11-29
申请号：PCT/US2012/038523
申请日：2012-05-18
申请人： GLAXOSMITHKLINE LLC , QIN, Donghui , CHEUNG, Mui , JOSHI, Hemant , TANGIRALA, Raghuram , BETHI, Sridhar, Reddy
发明人： QIN, Donghui , CHEUNG, Mui , JOSHI, Hemant , TANGIRALA, Raghuram , BETHI, Sridhar, Reddy
IPC分类号： C07D498/04
CPC分类号： C07D519/00 , C07D498/04
摘要： This invention relates to novel compounds which are inhibitors of acyl coenzymeA: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, hypertriglyceridemia, hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, hepatitis C virus infection and acne or other skin disorders.
摘要翻译：本发明涉及作为酰基辅酶A：二酰基甘油酰基转移酶1（DGAT-1）的抑制剂的新化合物，含有它们的药物组合物，其制备方法及其在治疗中用于预防或治疗与DGAT有关的疾病 -1功能障碍或DGAT-1活性的调节可能具有治疗益处，包括但不限于肥胖症，肥胖相关疾病，高甘油三酯血症，高脂蛋白血症，乳糜微粒血症，血脂异常，非酒精性脂肪性肝炎，糖尿病，胰岛素抵抗，代谢综合征，丙型肝炎病毒感染和痤疮或其他皮肤疾病。

8. 发明申请

WO2014081995A1 NOVEL COMPOUNDS AS DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS 审中-公开
标题翻译：新型化合物作为二乙酰胆碱酯酶抑制剂
公开(公告)号：WO2014081995A1
公开(公告)日：2014-05-30
申请号：PCT/US2013/071378
申请日：2013-11-22
申请人： GLAXOSMITHKLINE LLC
发明人： CHEUNG, Mui , TANGIRALA, Raghuram, S.
IPC分类号： A61K31/519
CPC分类号： C07D487/04
摘要： This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit.
摘要翻译：本发明涉及作为酰基辅酶A：二酰基甘油酰基转移酶1（DGAT-1）的抑制剂的新化合物，含有它们的药物组合物，其制备方法及其在治疗中的用途，单独使用或与体重管理疗法组合或其他甘油三酸酯降低治疗用于预防或治疗与DGAT-1功能障碍相关的疾病或DGAT-1活性调节可能具有治疗益处。

9. 发明申请

WO2014074761A2 NOVEL COMPOUNDS AS DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS 审中-公开
标题翻译：新型化合物作为二乙酰胆碱酯酶抑制剂
公开(公告)号：WO2014074761A2
公开(公告)日：2014-05-15
申请号：PCT/US2013/069024
申请日：2013-11-08
申请人： GLAXOSMITHKLINE LLC
发明人： CHEUNG, Mui , TANGIRALA, Raghuram, S.
IPC分类号： A61K31/501
CPC分类号： C07D213/72 , A61K31/122 , A61K31/50 , C07D213/74 , C07D237/20 , C07D277/42 , C07D401/12 , C07D405/12 , C07D417/12
摘要： This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, genetic (Type 1, Type 5 hyperlipidemia) and acquired forms of hypertriglyceridemia or hyperlipoproteinemia- related disorders, caused by but not limited to lipodystrophy, hypothyroidism, medications (beta blockers, thiazides, estrogen, glucocorticoids, transplant) and other factors (pregnancy, alcohol intake), hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, cardiovascular outcomes, angina, excess hair growth (including syndromes associated with hirsutism), nephrotic syndrome, fibrosis such as mycocardial, renal and liver fibrosis, hepatitis C virus infection and acne or other skin disorders.
摘要翻译：本发明涉及作为酰基辅酶A：二酰基甘油酰基转移酶1（DGAT-1）的抑制剂的新化合物，含有它们的药物组合物，其制备方法及其在治疗中的用途，单独使用或与体重管理疗法组合或其他甘油三酸酯降低治疗用于预防或治疗与DGAT-1功能障碍有关的疾病或其中DGAT-1活性的调节可具有治疗益处，包括但不限于肥胖症，肥胖相关疾病，遗传（1型，5型高脂血症）并且获得由但不限于脂肪营养不良，甲状腺机能减退，药物（β受体阻滞剂，噻嗪类，雌激素，糖皮质激素，移植物）和其他因素（怀孕，酒精摄入），高脂蛋白血症，乳糜微粒血症，血脂异常，非酒精性脂肪性肝炎，糖尿病，胰岛素抵抗，代谢综合征，心血管疾病心绞痛，过度毛发生长（包括与多毛症相关的综合征），肾病综合征，纤维化如心肌梗死，肾和肝纤维化，丙型肝炎病毒感染和痤疮或其他皮肤疾病。

10. 发明申请

WO2011119694A1 TRPV4 ANTAGONISTS 审中-公开
公开(公告)号：WO2011119694A1
公开(公告)日：2011-09-29
申请号：PCT/US2011/029572
申请日：2011-03-23
申请人： GLAXOSMITHKLINE LLC , CHEUNG, Mui , EIDAM, Hilary, Schenck , GOODMAN, Krista, B. , HILFIKER, Mark, A.
发明人： CHEUNG, Mui , EIDAM, Hilary, Schenck , GOODMAN, Krista, B. , HILFIKER, Mark, A.
IPC分类号： A61K31/27
CPC分类号： A61K31/375 , C07D471/04
摘要： The present invention relates to naphthyridine analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
摘要翻译：本发明涉及萘啶类似物，含有它们的药物组合物及其作为TRPV4拮抗剂的用途。

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