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公开(公告)号:US20080090865A1
公开(公告)日:2008-04-17
申请号:US11794591
申请日:2006-01-24
申请人: Min Ge , Lihu Yang , Changyou Zhou , Songnian Lin , Eric Cline
发明人: Min Ge , Lihu Yang , Changyou Zhou , Songnian Lin , Eric Cline
IPC分类号: A61K31/47 , A61K31/435 , A61P3/10 , C07D215/00 , C07D221/02
CPC分类号: C07D413/12 , C07D215/20 , C07D413/04 , C07D417/04 , C07D417/12
摘要: Bicyclic compounds containing a fused pyridine ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
摘要翻译: 含有稠合吡啶环的双环化合物,包括其药学上可接受的盐和前体药物,是G蛋白偶联受体40(GPR40)的激动剂,可用作治疗性化合物,特别是治疗2型糖尿病, 通常与该疾病有关,包括肥胖症和脂质疾病,例如混合或糖尿病性血脂异常,高脂血症,高胆固醇血症和高甘油三酯血症。
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公开(公告)号:US08039484B2
公开(公告)日:2011-10-18
申请号:US12441733
申请日:2007-10-26
申请人: Min Ge , Songnian Lin , Shawn P. Walsh , Lihu Yang , Changyou Zhou
发明人: Min Ge , Songnian Lin , Shawn P. Walsh , Lihu Yang , Changyou Zhou
IPC分类号: A61K31/47 , A61K31/192 , A61K31/277 , C07D487/02 , C07D217/24 , C07D213/36 , C07D209/34 , C07D311/34 , C07D333/56
CPC分类号: C07D333/60 , C07C59/72 , C07C59/90 , C07C235/46 , C07C255/54 , C07C2602/08 , C07C2602/10 , C07D207/34 , C07D209/34 , C07D209/46 , C07D213/61 , C07D215/233 , C07D217/24 , C07D307/80 , C07D311/58 , C07D333/48 , C07D405/12 , C07D487/04
摘要: Diaryl ethers in which one of the aryl groups is a phenyl fused to a cycloalkyl or heterocyclic ring, to which is attached an acetic acid group, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that often accompany this disease, including insulin resistance, obesity and lipid disorders.
摘要翻译: 其中一个芳基是与环烷基或杂环稠合的苯基,其中连接有乙酸基的二芳基醚是G-蛋白偶联受体40(GPR40)的激动剂,并且可用作治疗化合物,特别是在 治疗2型糖尿病以及经常伴随该疾病的病症,包括胰岛素抵抗,肥胖和脂质疾病。
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公开(公告)号:US20100105725A1
公开(公告)日:2010-04-29
申请号:US12441733
申请日:2007-10-26
申请人: Min Ge , Songnian Lin , Shawn P. Walsh , Lihu Yang , Changyou Zhou
发明人: Min Ge , Songnian Lin , Shawn P. Walsh , Lihu Yang , Changyou Zhou
IPC分类号: A61K31/47 , A61K31/192 , A61K31/277 , C07D487/02 , C07C255/52 , C07C59/84 , C07D217/24 , C07D213/36 , C07D209/34 , C07D311/34 , C07D333/56
CPC分类号: C07D333/60 , C07C59/72 , C07C59/90 , C07C235/46 , C07C255/54 , C07C2602/08 , C07C2602/10 , C07D207/34 , C07D209/34 , C07D209/46 , C07D213/61 , C07D215/233 , C07D217/24 , C07D307/80 , C07D311/58 , C07D333/48 , C07D405/12 , C07D487/04
摘要: Diaryl ethers in which one of the aryl groups is a phenyl fused to a cycloalkyl or heterocyclic ring, to which is attached an acetic acid group, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that often accompany this disease, including insulin resistance, obesity and lipid disorders.
摘要翻译: 其中一个芳基是与环烷基或杂环稠合的苯基,其中连接有乙酸基的二芳基醚是G-蛋白偶联受体40(GPR40)的激动剂,并且可用作治疗化合物,特别是在 治疗2型糖尿病以及经常伴随该疾病的病症,包括胰岛素抵抗,肥胖和脂质疾病。
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公开(公告)号:US07759493B2
公开(公告)日:2010-07-20
申请号:US11794705
申请日:2006-01-30
申请人: Min Ge , Lihu Yang , Changyou Zhou , Songnian Lin , Haifeng Tang , Eric Dean Cline , Sunita Malkani
发明人: Min Ge , Lihu Yang , Changyou Zhou , Songnian Lin , Haifeng Tang , Eric Dean Cline , Sunita Malkani
IPC分类号: A61K31/421 , A61K31/4245 , A61K31/426 , A61K31/4436 , A61K31/4725 , A61K31/443 , A61K31/4439 , C07D417/12 , C07D413/12 , C07D233/72 , C07D277/34 , C07D271/06 , C07D263/44
CPC分类号: C07D263/44 , C07D233/74 , C07D271/07 , C07D277/34 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12
摘要: Bicyclic compounds containing a phenyl or pyridyl ring fused to a cycloalkyl or heterocyclic ring, to which is attached a 5-membered heterocyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
摘要翻译: 包含与环烷基或杂环稠合的苯基或吡啶环的双环化合物,其连接有5元杂环,包括其药学上可接受的盐和前药,是G蛋白偶联受体40(GPR40)的激动剂,并且是有用的 作为治疗性化合物,特别是治疗2型糖尿病,以及通常与该疾病相关的病症,包括肥胖症和脂质疾病,例如混合或糖尿病性血脂异常,高脂血症,高胆固醇血症和高甘油三酯血症。
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公开(公告)号:US20090312303A1
公开(公告)日:2009-12-17
申请号:US11794705
申请日:2006-01-30
申请人: Min Ge , Lihu Yang , Changyou Zhou , Songnian Lin , Haifeng Tang , Eric Dean Cline , Sunita Malkani
发明人: Min Ge , Lihu Yang , Changyou Zhou , Songnian Lin , Haifeng Tang , Eric Dean Cline , Sunita Malkani
IPC分类号: A61K31/427 , C07D277/04 , C07D417/12 , C07D263/04 , A61K31/4439 , A61K31/4709 , A61K31/422 , A61K31/397 , A61P3/10
CPC分类号: C07D263/44 , C07D233/74 , C07D271/07 , C07D277/34 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12
摘要: Bicyclic compounds containing a phenyl or pyridyl ring fused to a cycloalkyl or heterocyclic ring, to which is attached a 5-membered heterocyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
摘要翻译: 包含与环烷基或杂环稠合的苯基或吡啶环的双环化合物,其连接有5元杂环,包括其药学上可接受的盐和前药,是G蛋白偶联受体40(GPR40)的激动剂,并且是有用的 作为治疗性化合物,特别是治疗2型糖尿病,以及通常与该疾病相关的病症,包括肥胖症和脂质疾病,例如混合或糖尿病性血脂异常,高脂血症,高胆固醇血症和高甘油三酯血症。
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公开(公告)号:US07361765B2
公开(公告)日:2008-04-22
申请号:US10577587
申请日:2004-10-25
申请人: Dongwei Cai , Fred Fleitz , Min Ge , Scott Hoerrner , Gary Javadi , Mark Jensen , Robert Larsen , Wenjie Li , Dorian Nelson , Elizabeth Szumigala , Lihu Yang , Changyou Zhou
发明人: Dongwei Cai , Fred Fleitz , Min Ge , Scott Hoerrner , Gary Javadi , Mark Jensen , Robert Larsen , Wenjie Li , Dorian Nelson , Elizabeth Szumigala , Lihu Yang , Changyou Zhou
IPC分类号: C07D471/02
CPC分类号: C07C271/24 , C07C303/40 , C07C2601/10 , C07D207/327 , C07D401/04 , C07C311/20
摘要: The present invention provides an efficient synthesis for the preparation of ((1R,3S)-3-isopropyl-3-{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopentyl)[(3S,4S)-3-m ethoxytetrahydro-2H-pyran-4-yl]amine and its succinate salt. The present invention additionally provides an efficient syntheses for the preparation of intermediates (3R)-3-methoxytetrahydro-4H-pyran-4-one; (1S,4S)-4-(2,5-dimethyl-1H-pyrrol-1-yl)-1-isopropylcyclopent-2-ene-1-carboxylic acid; and 3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,6-naphthyridine; and for the preparation of the precursor (3S,4S)-N-((1S,4S)-4-isopropyl-4-{[3-(tri-fluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopent-2-en-1-yl)-3-methoxytetrahydro-2H-pyran-4-amine. The invention additionally resides in the superior properties of the succinate salt of ((1R,3S)-3-isopropyl-3-1{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopentyl)[(3S,4S)-3-methoxytetrahydro-2H-pyran-4-yl]amine
摘要翻译: 本发明提供了制备((1R,3S)-3-异丙基-3 - {[3-(三氟甲基)-7,8-二氢-1,6-二氮杂萘-6(5H) ]羰基}环戊基)[(3S,4S)-3-甲氧基四氢-2H-吡喃-4-基]胺及其琥珀酸盐。 本发明另外提供了制备中间体(3R)-3-甲氧基四氢-4H-吡喃-4-酮的有效合成方法; (1S,4S)-4-(2,5-二甲基-1H-吡咯-1-基)-1-异丙基环戊-2-烯-1-羧酸; 和3-(三氟甲基)-5,6,7,8-四氢-1,6-萘啶; 制备前体(3S,4S)-N - ((1S,4S)-4-异丙基-4 - {[3-(三氟甲基)-7,8-二氢-1,6-萘啶-2-基] (5H) - 基]羰基}环戊-2-烯-1-基)-3-甲氧基四氢-2H-吡喃-4-胺。 本发明另外存在((1R,3S)-3-异丙基-3-1 {[3-(三氟甲基)-7,8-二氢-1,6-二氮杂萘-6(5H))的琥珀酸盐的优异性质 ) - 基]羰基}环戊基)[(3S,4S)-3-甲氧基四氢-2H-吡喃-4-基]胺
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公开(公告)号:US20070265332A1
公开(公告)日:2007-11-15
申请号:US11801841
申请日:2007-05-11
申请人: Min Ge , Jiafang He , Fiona Wai Yu Lau , Gui-Bai Liang , Songnian Lin , Weiguo Liu , Shawn P. Walsh , Lihu Yang
发明人: Min Ge , Jiafang He , Fiona Wai Yu Lau , Gui-Bai Liang , Songnian Lin , Weiguo Liu , Shawn P. Walsh , Lihu Yang
IPC分类号: A61K31/381 , A61K31/343 , A61K31/192 , A61K31/195
CPC分类号: C07D213/643 , C07C62/34 , C07C62/38 , C07C229/50 , C07C2603/08 , C07D307/93 , C07D311/94 , C07D333/78 , C07D405/04 , C07D407/12 , C07D413/12 , C07D417/12
摘要: Tricyclic compounds containing a cyclopropyl carboxylic acid or carboxylic acid derivative (e.g. amide) fused to a bicyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
摘要翻译: 与环双环稠合的环状羧酸或羧酸衍生物(如酰胺)的三环化合物(包括其药学上可接受的盐和前体药物)是G-蛋白偶联受体40(GPR40)的激动剂,可用作治疗性化合物,特别是在 2型糖尿病的治疗,以及经常与该疾病相关的病症,包括肥胖症和脂质疾病,例如混合或糖尿病性血脂异常,高脂血症,高胆固醇血症和高甘油三酯血症。
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公开(公告)号:US20070135475A1
公开(公告)日:2007-06-14
申请号:US10577587
申请日:2004-10-25
申请人: Dongwei Cai , Fred Fleitz , Min Ge , Scott Hoerner , Gary Javadi , Mark Jensen , Robert Larsen , Wenjie Lie , Dorian Nelson , Elizabeth Szumigala , Lihu Yang , Changyou Zhou
发明人: Dongwei Cai , Fred Fleitz , Min Ge , Scott Hoerner , Gary Javadi , Mark Jensen , Robert Larsen , Wenjie Lie , Dorian Nelson , Elizabeth Szumigala , Lihu Yang , Changyou Zhou
IPC分类号: A61K31/4745 , C07D471/02
CPC分类号: C07C271/24 , C07C303/40 , C07C2601/10 , C07D207/327 , C07D401/04 , C07C311/20
摘要: The present invention provides an efficient synthesis for the preparation of ((1R,3S)-3-isopropyl-3-{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopentyl)[(3S,4S)-3-m ethoxytetrahydro-2H-pyran-4-yl]amine and its succinate salt. The present invention additionally provides an efficient syntheses for the preparation of intermediates (3R)-3-methoxytetrahydro-4H-pyran-4-one; (1S,4S)-4-(2,5-dimethyl-1H-pyrrol-1-yl)-1-isopropylcyclopent-2-ene-1-carboxylic acid; and 3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,6-naphthyridine; and for the preparation of the precursor (3S,4S)-N-((1S,4S)-4-isopropyl-4-{[3-(tri-fluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopent-2-en-1-yl)-3-methoxytetrahydro-2H-pyran-4-amine. The invention additionally resides in the superior properties of the succinate salt of ((1R,3S)-3-isopropyl-3-1{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopentyl)[(3S,4S)-3-methoxytetrahydro-2H-pyran-4-yl]amine.
摘要翻译: 本发明提供了制备((1R,3S)-3-异丙基-3 - {[3-(三氟甲基)-7,8-二氢-1,6-二氮杂萘-6(5H) ]羰基}环戊基)[(3S,4S)-3-甲氧基四氢-2H-吡喃-4-基]胺及其琥珀酸盐。 本发明另外提供了制备中间体(3R)-3-甲氧基四氢-4H-吡喃-4-酮的有效合成方法; (1S,4S)-4-(2,5-二甲基-1H-吡咯-1-基)-1-异丙基环戊-2-烯-1-羧酸; 和3-(三氟甲基)-5,6,7,8-四氢-1,6-萘啶; 制备前体(3S,4S)-N - ((1S,4S)-4-异丙基-4 - {[3-(三氟甲基)-7,8-二氢-1,6-萘啶-2-基] (5H) - 基]羰基}环戊-2-烯-1-基)-3-甲氧基四氢-2H-吡喃-4-胺。 本发明另外存在((1R,3S)-3-异丙基-3-1 {[3-(三氟甲基)-7,8-二氢-1,6-二氮杂萘-6(5H))的琥珀酸盐的优异性质 ) - 基]羰基}环戊基)[(3S,4S)-3-甲氧基四氢-2H-吡喃-4-基]胺。
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公开(公告)号:US07442808B2
公开(公告)日:2008-10-28
申请号:US11801841
申请日:2007-05-11
申请人: Min Ge , Jiafang He , Fiona Wai Yu Lau , Gui-Bai Liang , Songnian Lin , Weiguo Liu , Shawn P. Walsh , Lihu Yang
发明人: Min Ge , Jiafang He , Fiona Wai Yu Lau , Gui-Bai Liang , Songnian Lin , Weiguo Liu , Shawn P. Walsh , Lihu Yang
IPC分类号: C07D495/00 , C07D307/92 , C07D209/94 , C07D209/00 , C07C229/00 , C07C62/00 , A61K31/38 , A61K31/34 , A61K31/19 , A61K31/195 , A61K31/40
CPC分类号: C07D213/643 , C07C62/34 , C07C62/38 , C07C229/50 , C07C2603/08 , C07D307/93 , C07D311/94 , C07D333/78 , C07D405/04 , C07D407/12 , C07D413/12 , C07D417/12
摘要: Tricyclic compounds containing a cyclopropyl carboxylic acid or carboxylic acid derivative (e.g. amide) fused to a bicyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
摘要翻译: 与环双环稠合的环状羧酸或羧酸衍生物(如酰胺)的三环化合物(包括其药学上可接受的盐和前体药物)是G-蛋白偶联受体40(GPR40)的激动剂,可用作治疗性化合物,特别是在 2型糖尿病的治疗,以及经常与该疾病相关的病症,包括肥胖症和脂质疾病,例如混合或糖尿病性血脂异常,高脂血症,高胆固醇血症和高甘油三酯血症。
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公开(公告)号:US20090253673A1
公开(公告)日:2009-10-08
申请号:US12227545
申请日:2007-07-06
申请人: Min Ge , Eric Cline , Lihu Yang , Sander G. Mills
发明人: Min Ge , Eric Cline , Lihu Yang , Sander G. Mills
IPC分类号: A61K31/4155 , C07D403/06 , C07D401/06 , C07D231/12 , C07D231/38 , C07D413/12 , C07D417/12 , A61K31/415 , A61K31/454 , A61K31/496 , A61K31/4178 , A61K31/422 , A61K31/4245 , A61K31/4439 , A61K31/497 , A61K31/506 , A61K31/427 , A61P3/04 , A61P3/10
CPC分类号: C07D403/12 , C07D231/38 , C07D401/06 , C07D401/12 , C07D403/14 , C07D405/06 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要: Certain novel N-acylated spiropiperidine derivatives are ligands of the human ghrelin receptor(s) and, in particular, are antagonists/inverse agonists of the human ghrelin receptor. They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of the ghrelin receptor, such as obesity, diabetes, and metabolic syndrome.
摘要翻译: 某些新的N-酰化螺哌啶衍生物是人类生长素释放肽受体的配体,特别是人类生长素释放肽受体的拮抗剂/反向激动剂。 因此,它们可用于治疗,控制或预防响应于调节生长素释放肽受体的疾病和病症,例如肥胖,糖尿病和代谢综合征。
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