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公开(公告)号：US08471024B2
公开(公告)日：2013-06-25
申请号：US12919156
申请日：2009-02-11
IPC分类号： A61K31/4355 , C07D491/048
CPC分类号： C07D491/048
摘要： The present invention relates to Tetrahydrofuropyridones compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
摘要翻译： 本发明涉及可用作HIF脯氨酰羟化酶抑制剂治疗贫血和类似病症的四氢呋喃吡啶酮化合物。
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公开(公告)号：US08372863B2
公开(公告)日：2013-02-12
申请号：US12919199
申请日：2009-02-11
申请人： Matthew J. Clements , Vincent J. Colandrea , John S. Debenham , Jeffrey J. Hale , Christina B. Madsen-Duggan , Thomas F. Walsh
发明人： Matthew J. Clements , Vincent J. Colandrea , John S. Debenham , Jeffrey J. Hale , Christina B. Madsen-Duggan , Thomas F. Walsh
IPC分类号： A61K31/44 , C07D221/02
CPC分类号： C07D471/04
摘要： The present invention relates to tetrahydro-1H-pyrrolo fused pyridone compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
摘要翻译： 本发明涉及可用作HIF脯氨酰羟化酶抑制剂治疗贫血和类似病症的四氢-1H-吡咯稠合吡啶酮化合物。
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3.发明授权(3,4-disubstituted)propanoic carboxylates as S1P (Edg) receptor agonists 失效（3,4-二取代）丙酸羧酸酯作为S1P（Edg）受体激动剂公开(公告)号：US07605171B2
公开(公告)日：2009-10-20
申请号：US10575790
申请日：2004-12-13
申请人： Vincent J. Colandrea , George A. Doherty , Jeffrey J. Hale , Pei Huo , Irene E. Legiec , Leslie Toth , Petr Vachal , Lin Yan
发明人： Vincent J. Colandrea , George A. Doherty , Jeffrey J. Hale , Pei Huo , Irene E. Legiec , Leslie Toth , Petr Vachal , Lin Yan
IPC分类号： A61K31/443 , A61K31/4245 , C07D413/04 , C07D271/06
CPC分类号： C07D271/06 , A61K31/4245 , A61K31/427 , A61K31/443 , A61K31/506 , C07D285/12 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/04
摘要： The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by modulating leukocyte trafficking, sequestering lymphocytes in secondary lymphoid tissues, and enhancing vascular integrity. The invention is also directed to pharmaceutical compositions containing such compounds and methods of treatment or prevention.
摘要翻译： 本发明包括式I的化合物及其药学上可接受的盐。 化合物是S1P1 / Edg1受体激动剂，因此通过调节白细胞运输，隔离淋巴细胞在次级淋巴组织中并增强血管完整性具有免疫抑制，抗炎和止血活性。 本发明还涉及含有这些化合物和治疗或预防方法的药物组合物。
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4.发明申请SUBSTITUTED CYCLOPROPLY COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT 有权取代的环状化合物，包含这些化合物的组合物和处理方法公开(公告)号：US20140057893A1
公开(公告)日：2014-02-27
申请号：US14110332
申请日：2012-04-05
申请人： Scott Edmondson , Zhiqiang Guo , Harold B. Wood , Andrew W. Stamford , Michael W. Miller , Duane E. DeMong , Gregori J. Morriello , Rajan Anand , Vincent J. Colandrea , Megan Macala , Milana Maletic , Cheng Zhu , Yuping Zhu , Wanying Sun , Kake Zhao , Yong Huang , Joel M. Harris , Lehua Chang , Nam Fung Kar , Zhiyong Hu , Liping Wang , Bowei Wang , Ping Liu , Jason W. Szewczyk , William B. Geiss
发明人： Scott Edmondson , Zhiqiang Guo , Harold B. Wood , Andrew W. Stamford , Michael W. Miller , Duane E. DeMong , Gregori J. Morriello , Rajan Anand , Vincent J. Colandrea , Megan Macala , Milana Maletic , Cheng Zhu , Yuping Zhu , Wanying Sun , Kake Zhao , Yong Huang , Joel M. Harris , Lehua Chang , Nam Fung Kar , Zhiyong Hu , Liping Wang , Bowei Wang , Ping Liu , Jason W. Szewczyk , William B. Geiss
IPC分类号： C07D513/04 , C07D413/14 , C07D413/04 , C07D498/04 , C07D405/04 , C07D471/04 , C07D487/04 , C07D401/12 , C07D211/22
CPC分类号： C07D513/04 , A61K9/4858 , C07D211/22 , C07D401/12 , C07D405/04 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/04
摘要： Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included
摘要翻译： 公开了取代的式I的环丙基化合物及其药学上可接受的盐可用于治疗或预防2型糖尿病和类似病状。 该化合物可用作G蛋白偶联受体GPR-119的激动剂。 还包括药物组合物和治疗方法
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公开(公告)号：US08354403B2
公开(公告)日：2013-01-15
申请号：US13392662
申请日：2010-08-17
申请人： Scott D. Edmondson , Richard Berger , Lehua Chang , Vincent J. Colandrea , Jeffrey J. Hale , Bart Harper , Nam Fung Kar , Bing Li , Greg J. Morriello , Christopher R. Moyes , Deyou Sha , Dong-Ming Shen , Liping Wang , Harvey Wendt , Cheng Zhu
发明人： Scott D. Edmondson , Richard Berger , Lehua Chang , Vincent J. Colandrea , Jeffrey J. Hale , Bart Harper , Nam Fung Kar , Bing Li , Greg J. Morriello , Christopher R. Moyes , Deyou Sha , Dong-Ming Shen , Liping Wang , Harvey Wendt , Cheng Zhu
IPC分类号： A61K31/536 , A61K31/438 , A61K31/4245 , C07D265/12 , C07D221/20 , C07D413/14
CPC分类号： C07D403/14 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/10 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10 , C07D491/048 , C07D491/107 , C07D491/147 , C07D491/20 , C07D495/10 , C07D495/20 , C07D497/10 , C07D498/04 , C07D513/04 , C07D513/20
摘要： The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor.
摘要翻译： 本发明提供式（I）化合物，其药物组合物及其用于治疗或预防由β-肾上腺素能受体激活介导的疾病的方法。
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6.发明授权Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment 有权取代的环丙基化合物，含有这些化合物的组合物和处理方法公开(公告)号：US08957062B2
公开(公告)日：2015-02-17
申请号：US14110332
申请日：2012-04-05
申请人： Scott Edmondson , Zhiqiang Guo , Harold B. Wood , Andrew W. Stamford , Michael W. Miller , Duane E. DeMong , Gregori J. Morriello , Rajan Anand , Vincent J. Colandrea , Megan Macala , Milana Maletic , Cheng Zhu , Yuping Zhu , Wanying Sun , Kake Zhao , Yong Huang , Joel M. Harris , Lehua Chang , Nam Fung Kar , Zhiyong Hu , Liping Wang , Bowei Wang , Ping Liu , Jason W. Szewczyk , William B. Geiss
发明人： Scott Edmondson , Zhiqiang Guo , Harold B. Wood , Andrew W. Stamford , Michael W. Miller , Duane E. DeMong , Gregori J. Morriello , Rajan Anand , Vincent J. Colandrea , Megan Macala , Milana Maletic , Cheng Zhu , Yuping Zhu , Wanying Sun , Kake Zhao , Yong Huang , Joel M. Harris , Lehua Chang , Nam Fung Kar , Zhiyong Hu , Liping Wang , Bowei Wang , Ping Liu , Jason W. Szewczyk , William B. Geiss
IPC分类号： C07D513/04 , C07D401/12 , C07D413/14 , C07D413/04 , C07D211/22 , C07D405/04 , C07D471/04 , C07D487/04 , C07D498/04 , A61K9/48 , C07D417/14 , C07D495/04
CPC分类号： C07D513/04 , A61K9/4858 , C07D211/22 , C07D401/12 , C07D405/04 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/04
摘要： Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.
摘要翻译： 公开了取代的式I的环丙基化合物及其药学上可接受的盐可用于治疗或预防2型糖尿病和类似病症。 该化合物可用作G蛋白偶联受体GPR-119的激动剂。 还包括药物组合物和治疗方法。
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公开(公告)号：US08796258B2
公开(公告)日：2014-08-05
申请号：US13812536
申请日：2012-02-23
申请人： Rajan Anand , James M. Apgar , Tesfaye Biftu , Ping Chen , Lin Chu , Vincent J. Colandrea , Guizhen Dong , James F. Dropinski , Danqing Feng , Jacqueline D. Hicks , Jinlong Jiang , Alexander J. Kim , Kenneth J. Leavitt , Bing Li , Xiaoxia Qian , Iyassu Sebhat , Lan Wei , Robert R. Wilkening , Zhicai Wu
发明人： Rajan Anand , James M. Apgar , Tesfaye Biftu , Ping Chen , Lin Chu , Vincent J. Colandrea , Guizhen Dong , James F. Dropinski , Danqing Feng , Jacqueline D. Hicks , Jinlong Jiang , Alexander J. Kim , Kenneth J. Leavitt , Bing Li , Xiaoxia Qian , Iyassu Sebhat , Lan Wei , Robert R. Wilkening , Zhicai Wu
IPC分类号： A61K31/00 , C07D513/02
CPC分类号： A61K31/5377 , A61K31/351 , A61K31/366 , A61K31/397 , A61K31/437 , A61K31/4412 , A61K31/496 , A61K31/4985 , A61K31/519 , A61K45/06 , C07D471/04 , C07D519/00 , A61K2300/00
摘要： Novel compounds of structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
摘要翻译： 结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制由AMPK激活的蛋白激酶介导的疾病。 本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖症，高胆固醇血症和高血压。
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公开(公告)号：US20120157432A1
公开(公告)日：2012-06-21
申请号：US13392662
申请日：2010-08-17
申请人： Scott D. Edmondson , Richard Berger , Lehua Chang , Vincent j. Colandrea , Jeffrey J. Hale , Bart Harper , Nam Fung Kar , Bing Li , Greg J. Morriello , Christopher R. Moyes , Deyou Sha , Dong-Ming Shen , Liping Wang , Harvey Wendt , Cheng Zhu
发明人： Scott D. Edmondson , Richard Berger , Lehua Chang , Vincent j. Colandrea , Jeffrey J. Hale , Bart Harper , Nam Fung Kar , Bing Li , Greg J. Morriello , Christopher R. Moyes , Deyou Sha , Dong-Ming Shen , Liping Wang , Harvey Wendt , Cheng Zhu
IPC分类号： A61K31/4025 , A61K31/4155 , C07D403/12 , A61K31/497 , C07D413/14 , A61K31/4245 , C07D209/96 , A61K31/407 , C07D401/14 , A61K31/4439 , C07D487/04 , A61K31/519 , C07D401/12 , A61K31/454 , C07D221/20 , A61K31/438 , A61K31/4545 , C07D265/12 , A61K31/536 , A61K31/501 , A61K31/496 , A61P13/02 , C07D403/14
CPC分类号： C07D403/14 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/10 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10 , C07D491/048 , C07D491/107 , C07D491/147 , C07D491/20 , C07D495/10 , C07D495/20 , C07D497/10 , C07D498/04 , C07D513/04 , C07D513/20
摘要： The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of β3-adrenoceptor.
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公开(公告)号：US20100331358A1
公开(公告)日：2010-12-30
申请号：US12919156
申请日：2009-02-11
IPC分类号： A61K31/4355 , C07D471/04 , A61P7/00
CPC分类号： C07D491/048
摘要： The present invention relates to Tetrahydrofuropyridones compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
摘要翻译： 本发明涉及可用作HIF脯氨酰羟化酶抑制剂治疗贫血和类似病症的四氢呋喃吡啶酮化合物。
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10.发明授权公开(公告)号：US07157490B2
公开(公告)日：2007-01-02
申请号：US10481352
申请日：2003-11-03
申请人： Vincent J. Colandrea , Scott D. Edmondson , Robert J. Mathvink , Anthony Mastracchio , Ann E. Weber , Jinyou Xu
发明人： Vincent J. Colandrea , Scott D. Edmondson , Robert J. Mathvink , Anthony Mastracchio , Ann E. Weber , Jinyou Xu
IPC分类号： C07D277/04 , C07D207/04 , A61K31/40 , A61K31/426
CPC分类号： C07D205/04 , C07D207/10 , C07D211/38 , C07D213/64 , C07D295/185 , C07D401/10 , C07D401/12 , C07D403/06 , C07D403/10 , C07D403/12 , C07D413/10 , C07D413/12 , C07D417/10 , C07D471/04 , C07D487/04
摘要： The present invention is directed to phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
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