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公开(公告)号：US06921821B2
公开(公告)日：2005-07-26
申请号：US10459682
申请日：2003-06-11
申请人： Christopher Blackburn , Su-Jen Lai , Jennifer L. Che , Martin P. Maguire , Michael A. Patane , Matthew J. LaMarche , Courtney A. Cullis , James Brown , Anil Vasudevan , Jennifer C. Freeman , Mathew M. Mulhern , John K. Lynch , Ju Gao , Dariusz Wodka , Andrew J. Souers , Rajesh Iyengar , Mary Katherin Verzal , Philip R. Kym
发明人： Christopher Blackburn , Su-Jen Lai , Jennifer L. Che , Martin P. Maguire , Michael A. Patane , Matthew J. LaMarche , Courtney A. Cullis , James Brown , Anil Vasudevan , Jennifer C. Freeman , Mathew M. Mulhern , John K. Lynch , Ju Gao , Dariusz Wodka , Andrew J. Souers , Rajesh Iyengar , Mary Katherin Verzal , Philip R. Kym
IPC分类号： C07D403/14 , A61K31/453 , A61K31/4535 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/517 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P15/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D451/04 , C07D205/08 , C07D239/02 , C07D401/00
CPC分类号： C07D405/14 , C07D401/14 , C07D405/12 , C07D409/14 , C07D413/14
摘要： This invention provides compounds that are antagonists of melanin concentrating hormone receptor-1 (MCH-R1). The compounds are represented by formula I: where m is zero or one, n is zero to two, Y is oxygen or —N(R9)—, R1, R2, R3, R4, R5, R9 and Ring A are defined in the specification. Coumarin and quinolone compounds where R1 and R2 together form a fused benzo ring are preferred. The invention also provides compounds of formula VI where the coumarin moiety is replaced by a quinazolinone ring. The compounds are useful for treating MCH-R1-related disorders, particularly overweight conditions including obesity.
摘要翻译： 本发明提供了作为黑色素浓缩激素受体-1（MCH-R1）的拮抗剂的化合物。 化合物由式I表示：其中m为0或1，n为0至2，Y为氧或-N（R 9） - ，R 1， R 2，R 3，R 4，R 5，R 9和R 9，和 环A在规范中定义。 其中R 1和R 2一起形成稠合苯并环的香豆素和喹诺酮化合物是优选的。 本发明还提供式VI的化合物，其中香豆素部分被喹唑啉酮环代替。 该化合物可用于治疗MCH-R1相关疾病，特别是超重状况，包括肥胖症。
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公开(公告)号：US08901152B2
公开(公告)日：2014-12-02
申请号：US13549651
申请日：2012-07-16
IPC分类号： A61K31/445 , A61K31/425 , C07D498/08 , C07D417/14 , C07D213/40 , C07D417/12 , C07D277/82 , C07D417/04 , C07D213/75 , C07D405/04 , C07D277/28
CPC分类号： C07D417/04 , C07D213/40 , C07D213/75 , C07D277/28 , C07D277/82 , C07D405/04 , C07D417/12 , C07D417/14 , C07D498/08
摘要： The present invention relates to compounds of formula (I): wherein Q, G1, G2, and G3, are defined herein. Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.
摘要翻译： 本发明涉及式（I）化合物：其中Q，G1，G2和G3在本文中定义。 还公开了治疗DGAT-1相关疾病或病症的药物组合物和方法。
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公开(公告)号：US20120238581A1
公开(公告)日：2012-09-20
申请号：US13484539
申请日：2012-05-31
申请人： Andrew J. Souers , Ju Gao , Todd M. Hasen , Rajesh R. Iyengar , Philip R. Kym , Bo Liu , Zhonghua Pei , Vince S. Yeh , Gang Zhao , Zhili Xin
发明人： Andrew J. Souers , Ju Gao , Todd M. Hasen , Rajesh R. Iyengar , Philip R. Kym , Bo Liu , Zhonghua Pei , Vince S. Yeh , Gang Zhao , Zhili Xin
IPC分类号： A61K31/415 , C07D405/14 , A61K31/4155 , C07D405/12 , C07D413/12 , A61K31/422 , C07D249/08 , A61K31/4196 , C07D413/14 , C07D403/12 , C07D277/42 , A61K31/426 , C07D401/12 , A61K31/4439 , C07D241/12 , A61K31/4965 , C07D487/04 , A61K31/519 , A61P3/10 , A61P3/04 , A61P3/06 , A61P3/00 , A61P1/16 , A61K31/454 , A61K31/455 , C07D231/20
CPC分类号： C07D487/04 , C07C59/54 , C07C275/42 , C07D211/60 , C07D231/12 , C07D231/20 , C07D249/08 , C07D263/48 , C07D277/40 , C07D401/04 , C07D407/12 , C07D407/14 , C07D413/12 , C07D413/14
摘要： Compounds of formula (I), or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof. Pharmaceutical compositions of formula (I) and related methods for treating or preventing metabolic diseases or conditions.
摘要翻译： 式（I）化合物或其药学上可接受的盐，前药，前药的盐或其组合。 式（I）的药物组合物和治疗或预防代谢疾病或病症的相关方法。
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24.发明授权公开(公告)号：US07521439B2
公开(公告)日：2009-04-21
申请号：US11491337
申请日：2006-07-21
申请人： Richard D. Bishop , Russell Drew Cink , Bradley D. Gates , Lars T. Hagberg , Peer B. Jacobsen , Philip R. Kym , Chunqiu Lai , Marvin Robert Leanna , James T. Link , Steven J. Richards , Noah Tu , Tom W. von Geldern
发明人： Richard D. Bishop , Russell Drew Cink , Bradley D. Gates , Lars T. Hagberg , Peer B. Jacobsen , Philip R. Kym , Chunqiu Lai , Marvin Robert Leanna , James T. Link , Steven J. Richards , Noah Tu , Tom W. von Geldern
IPC分类号： A61K31/56
CPC分类号： C07J1/00 , Y10S514/866 , Y10S514/909
摘要： This invention relates to novel compounds that are liver selective glucocorticoid receptor antagonists, to methods of preparing such compounds, and to methods for using such compounds in the regulation of metabolism, especially lowering serum glucose levels, insulin levels, or lipid levels, and/or decreasing body weight.
摘要翻译： 本发明涉及作为肝脏选择性糖皮质激素受体拮抗剂的新型化合物，制备这些化合物的方法，以及使用这些化合物来调节代谢的方法，特别是降低血清葡萄糖水平，胰岛素水平或脂质水平，和/或 减轻体重。
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公开(公告)号：US07220752B2
公开(公告)日：2007-05-22
申请号：US10433015
申请日：2001-11-28
IPC分类号： A61K31/435 , A61K31/425 , A61K31/36 , C07D265/30 , C07D211/34 , C07D277/30 , C07D317/44
CPC分类号： C07D213/30 , C07C59/90 , C07C69/76 , C07C205/35 , C07C323/12 , C07D277/24 , C07D295/088 , C07D317/62
摘要： This invention relates to novel compounds that are liver selective glucocorticoid receptor antagonists, to methods of preparing such compounds, and to methods for using such compounds in therapy and in the regulation of metabolism, especially lowering blood glucose levels. The compounds referred to are compounds according to the formula 1: wherein the variables are as defined herein.
摘要翻译： 本发明涉及作为肝选择性糖皮质激素受体拮抗剂的新型化合物，制备这些化合物的方法，以及在治疗和调节代谢中尤其是降低血糖水平使用这些化合物的方法。 所指的化合物是根据式1的化合物：其中变量如本文所定义。
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26.发明授权Antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor 失效黑色素浓缩激素对黑色素浓缩激素受体的拮抗作用公开(公告)号：US07071182B2
公开(公告)日：2006-07-04
申请号：US11022453
申请日：2004-12-22
申请人： Andrew J. Souers , Christine A. Collins , Ju Gao , Andrew S. Judd , Philip R. Kym , Mathew M. Mulhern , Hing L. Sham , Dariusz Wodka
发明人： Andrew J. Souers , Christine A. Collins , Ju Gao , Andrew S. Judd , Philip R. Kym , Mathew M. Mulhern , Hing L. Sham , Dariusz Wodka
IPC分类号： A61K31/55 , A61K31/5377 , A61K31/454 , A61K31/416 , A61K31/4439
CPC分类号： C07D403/14 , C07D231/56 , C07D401/04 , C07D401/06 , C07D403/06 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04
摘要： The present invention relates to the antagonism of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in reproduction and sexual behavior, thyroid hormone secretion, diuresis and water/electrolyte homeostasis, sensory processing, memory, sleeping, arousal, anxiety, depression, seizures, neurodegeneration and psychiatric disorders.
摘要翻译： 本发明涉及黑色素浓缩激素（MCH）通过黑色素浓缩激素受体的作用的拮抗作用，其可用于预防或治疗进食障碍，体重增加，肥胖，生殖和性行为异常，甲状腺激素 分泌，利尿和水/电解质体内平衡，感觉加工，记忆，睡眠，唤醒，焦虑，抑郁，癫痫发作，神经变性和精神疾病。
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公开(公告)号：US08202878B2
公开(公告)日：2012-06-19
申请号：US11947005
申请日：2007-11-29
申请人： Andrew J. Souers , Ju Gao , Todd M. Hansen , Rajesh R. Iyengar , Philip R. Kym , Bo Liu , Zhonghua Pei , Vince S. Yeh , Gang Zhao , Zhili Xin
发明人： Andrew J. Souers , Ju Gao , Todd M. Hansen , Rajesh R. Iyengar , Philip R. Kym , Bo Liu , Zhonghua Pei , Vince S. Yeh , Gang Zhao , Zhili Xin
IPC分类号： C07D487/04 , A61K31/519 , A61P3/04 , A61P3/10 , C07D231/20 , A61K31/4152
CPC分类号： C07D487/04 , C07C59/54 , C07C275/42 , C07D211/60 , C07D231/12 , C07D231/20 , C07D249/08 , C07D263/48 , C07D277/40 , C07D401/04 , C07D407/12 , C07D407/14 , C07D413/12 , C07D413/14
摘要： The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, a pharmaceutical composition of formula (I), and related methods for treating or preventing metabolic diseases or conditions.
摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，式（I）的药物组合物以及用于治疗或预防代谢性疾病或病症的相关方法。
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公开(公告)号：US20080312282A1
公开(公告)日：2008-12-18
申请号：US12112635
申请日：2008-04-30
IPC分类号： A61K31/426 , C07D277/28 , A61K31/454 , A61P3/04 , C07D417/02
CPC分类号： C07D417/04 , C07D213/40 , C07D213/75 , C07D277/28 , C07D277/82 , C07D405/04 , C07D417/12 , C07D417/14 , C07D498/08
摘要： The present invention relates to compounds of formula (I): wherein Q, G1, G2, and G3, are defined herein. Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.
摘要翻译： 本发明涉及式（I）化合物：其中Q，G1，G2和G3在本文中定义。 还公开了治疗DGAT-1相关疾病或病症的药物组合物和方法。
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公开(公告)号：US08076344B2
公开(公告)日：2011-12-13
申请号：US12112643
申请日：2008-04-30
申请人： Gang Liu , Zhili Xin , Philip R. Kym , Andrew J. Souers
发明人： Gang Liu , Zhili Xin , Philip R. Kym , Andrew J. Souers
IPC分类号： A01N43/90 , A61K31/519 , C07D487/00
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of formula (I): wherein R1, R2, and R3, are defined herein. Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.
摘要翻译： 本发明涉及式（I）化合物：其中R 1，R 2和R 3在本文中定义。 还公开了治疗DGAT-1相关疾病或病症的药物组合物和方法。
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30.发明授权Thienopyridones as AMPK activators for the treatment of diabetes and obesity 有权噻吩并吡啶酮作为治疗糖尿病和肥胖症的AMPK激活剂公开(公告)号：US07119205B2
公开(公告)日：2006-10-10
申请号：US10847144
申请日：2004-05-17
申请人： Rajesh R. Iyengar , Andrew S. Judd , Gang Zhao , Philip R. Kym , Hing L. Sham , Yugui Gu , Gang Liu , Mei Liu , Hongyu Zhao , Richard F. Clark , Ernst U. Frevert , Barbara L. Cool , Tianyuan Zhang , Robert F. Keyes , Todd M. Hansen , Zhili Xin
发明人： Rajesh R. Iyengar , Andrew S. Judd , Gang Zhao , Philip R. Kym , Hing L. Sham , Yugui Gu , Gang Liu , Mei Liu , Hongyu Zhao , Richard F. Clark , Ernst U. Frevert , Barbara L. Cool , Tianyuan Zhang , Robert F. Keyes , Todd M. Hansen , Zhili Xin
IPC分类号： C07D471/102 , A61K31/395
CPC分类号： C07D495/04
摘要： The present invention relates to compounds that activate AMP-activated protein kinase (AMPK), including the preparation of the compounds, compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders such as diabetes, metabolic syndrome, and obesity.
摘要翻译： 本发明涉及活化AMP-活化蛋白激酶（AMPK）的化合物，包括化合物的制备，含有这些化合物的组合物以及该化合物在预防或治疗诸如糖尿病，代谢综合征和肥胖症中的用途 。
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