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公开(公告)号：US20160324821A1
公开(公告)日：2016-11-10
申请号：US15187872
申请日：2016-06-21
申请人： Lili Feng , Sven Erik Godtfredsen , Paul Allen Sutton , Mahavir Prashad , Michael J. Girgis , Bin Hu , Yugang Liu , Thomas J. Blacklock , Piotr Henryk Karpinski
发明人： Lili Feng , Sven Erik Godtfredsen , Paul Allen Sutton , Mahavir Prashad , Michael J. Girgis , Bin Hu , Yugang Liu , Thomas J. Blacklock , Piotr Henryk Karpinski
IPC分类号： A61K31/216 , C07D257/04 , C07C233/47 , A61K31/41
CPC分类号： A61K31/216 , A61K31/41 , A61K31/4422 , A61K31/5415 , A61K45/06 , A61K2300/00 , C07C233/47 , C07D207/50 , C07D257/04
摘要： A method for treatment of a cardiovascular or renal condition or disease with a specific combination, linked pro-drug or a compound of an angiotensin receptor antagonist and a NEPi.
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![Compounds containing S-N-valeryl-N-{[2′-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl)-valine and (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester moieties and cations](/abs-image/US/2016/07/12/US09388134B2/abs.jpg.150x150.jpg)
2.发明授权Compounds containing S-N-valeryl-N-{[2′-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl)-valine and (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester moieties and cations 有权含有SN-戊酰基-N - {[2' - （1H-四唑-5-基） - 联苯-4-基] - 甲基） - 缬氨酸和（2R，4S）-5-联苯-4-基-4 - （3-羧基 - 丙酰基氨基）-2-甲基 - 戊酸乙酯部分和阳离子公开(公告)号：US09388134B2
公开(公告)日：2016-07-12
申请号：US14311788
申请日：2014-06-23
申请人： Lili Feng , Sven Erik Godtfredsen , Paul Allen Sutton , Mahavir Prashad , Michael J. Girgis , Bin Hu , Yugang Liu , Thomas J. Blacklock , Piotr Henryk Karpinski
发明人： Lili Feng , Sven Erik Godtfredsen , Paul Allen Sutton , Mahavir Prashad , Michael J. Girgis , Bin Hu , Yugang Liu , Thomas J. Blacklock , Piotr Henryk Karpinski
IPC分类号： A61K31/41 , C07D207/50 , A61K31/216 , A61K45/06 , A61K31/4422 , A61K31/5415 , C07C233/47 , C07D257/04
CPC分类号： A61K31/216 , A61K31/41 , A61K31/4422 , A61K31/5415 , A61K45/06 , A61K2300/00 , C07C233/47 , C07D207/50 , C07D257/04
摘要： A method for treatment of a cardiovascular or renal condition or disease with a specific combination, linked pro-drug or a compound of an angiotensin receptor antagonist and a NEPi.
摘要翻译： 用于特异性组合，连接的前药或血管紧张素受体拮抗剂和NEPi的化合物治疗心血管或肾脏疾病或疾病的方法。
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3.发明申请COMPOUNDS CONTAINING S-N-VALERYL-N--VALINE AND (2R,4S)-5-BIPHENYL-4-YL-4-(3-CARBOXY-PROPIONYLAMINO)-2-METHYL-PENTANOIC ACID ETHYL ESTER MOIETIES AND CATIONS 审中-公开含有S-N-戊基-N-（+） - （2R，4S）-5-联苯-4-基-4-（3-羧基 - 丙酰氨基）-2-甲基 - 戊酸乙酯的化合物和方法公开(公告)号：US20150057322A1
公开(公告)日：2015-02-26
申请号：US14311788
申请日：2014-06-23
申请人： Li Feng , Sven Erik Godtfredsen , Paul Allen Sutton , Mahavir Prashad , Michael J. Girgis , Bin Hu , Yugang Liu , Thomas J. Blacklock , Piotr Henryk Karpinski
发明人： Li Feng , Sven Erik Godtfredsen , Paul Allen Sutton , Mahavir Prashad , Michael J. Girgis , Bin Hu , Yugang Liu , Thomas J. Blacklock , Piotr Henryk Karpinski
IPC分类号： C07D207/50
CPC分类号： A61K31/216 , A61K31/41 , A61K31/4422 , A61K31/5415 , A61K45/06 , A61K2300/00 , C07C233/47 , C07D207/50 , C07D257/04
摘要： A method for treatment of a cardiovascular or renal condition or disease with a specific combination, linked pro-drug or a compound of an angiotensin receptor antagonist and a NEPi.
摘要翻译： 用于特异性组合，连接的前药或血管紧张素受体拮抗剂和NEPi的化合物治疗心血管或肾脏疾病或疾病的方法。
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![Compounds containing S-N-valeryl-N-{[2′-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl}-valine and (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester moieties and cations](/abs-image/US/2014/11/04/US08877938B2/abs.jpg.150x150.jpg)
4.发明授权Compounds containing S-N-valeryl-N-{[2′-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl}-valine and (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester moieties and cations 有权含有N-戊酰基-N - {[2' - （1H-四唑-5-基） - 联苯-4-基] - 甲基} - 缬氨酸和（2R，4S）-5-联苯-4-基-4 - （3-羧基 - 丙酰基氨基）-2-甲基 - 戊酸乙酯部分和阳离子公开(公告)号：US08877938B2
公开(公告)日：2014-11-04
申请号：US11722360
申请日：2006-11-08
申请人： Lili Feng , Sven Erik Godtfredsen , Bin Hu , Yugang Liu , Piotr Karpinski , Paul Allen Sutton , Mahavir Prashad , Michael J. Girgis , Thomas J. Blacklock
发明人： Lili Feng , Sven Erik Godtfredsen , Bin Hu , Yugang Liu , Piotr Karpinski , Paul Allen Sutton , Mahavir Prashad , Michael J. Girgis , Thomas J. Blacklock
IPC分类号： C07D257/04 , C07C233/47 , A61K31/41 , A61K31/4422 , A61K31/5415
CPC分类号： A61K31/216 , A61K31/41 , A61K31/4422 , A61K31/5415 , A61K45/06 , A61K2300/00 , C07C233/47 , C07D207/50 , C07D257/04
摘要： A compound of an angiotensin receptor antagonist (ARB), a neutral endopeptidase inhibitor (NEPi) and one or more monovalent cations are useful for the treatment of hypertension and/or heart failure. ARB includes S—N-valeryl-N-{[2′-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl}-valine in the anion form, NEPi includes (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester in the anion form and cation includes monovalent cations such as Na+. The compound includes trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbamoyl)propionate-(S)-3′-methyl-2′-(pentanoyl{2″-(tetrazol-5-ylate)biphenyl-4′-ylmethyl}amino)butyrate] hemipentahydrate.
摘要翻译： 血管紧张素受体拮抗剂（ARB），中性内肽酶抑制剂（NEPi）和一种或多种一价阳离子的化合物可用于治疗高血压和/或心力衰竭。 ARB包括阴离子形式的S-N-戊酰基-N - {[2' - （1H-四唑-5-基） - 联苯-4-基] - 甲基} - 缬氨酸，NEPi包括（2R，4S）-5 - 联苯-4-基-4-（3-羧基 - 丙酰基氨基）-2-甲基 - 戊酸乙酯，包括一价阳离子如Na +。 该化合物包括[3 - （（1S，3R）-1-联苯-4-基甲基-3-乙氧基羰基-1-丁基氨基甲酰基）丙酸乙酯 - （S）-3'-甲基-2' - （戊酰基{2“ （四唑-5-基）联苯-4-基甲基}氨基）丁酸乙酯]半水合物。
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公开(公告)号：US20090156585A1
公开(公告)日：2009-06-18
申请号：US11722360
申请日：2006-11-08
申请人： Lili Feng , Sven Erik Godtfredsen , Bin Hu , Yugang Liu , Piotr Karpinski , Paul Allen Sutton , Mahavir Prashad , Michael J. Girgis , Thomas J. Blacklock
发明人： Lili Feng , Sven Erik Godtfredsen , Bin Hu , Yugang Liu , Piotr Karpinski , Paul Allen Sutton , Mahavir Prashad , Michael J. Girgis , Thomas J. Blacklock
IPC分类号： A61K31/41 , C07D257/04 , C07D403/10 , A61K31/4178 , A61P9/10 , A61P25/00 , A61K31/549 , A61K31/4422 , A61P9/00 , A61K31/216 , C07D409/06 , C07C229/34
CPC分类号： A61K31/216 , A61K31/41 , A61K31/4422 , A61K31/5415 , A61K45/06 , A61K2300/00 , C07C233/47 , C07D207/50 , C07D257/04
摘要： A specific combination, linked pro-drug or a compound of an angiotensin receptor antagonist and a NEPi are used in the treatment of hypertension.
摘要翻译： 联合的原药或血管紧张素受体拮抗剂和NEPi的化合物用于治疗高血压。
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公开(公告)号：US20080300410A1
公开(公告)日：2008-12-04
申请号：US12093825
申请日：2006-11-16
申请人： Mahavir Prashad , Yugang Liu , Bin Hu , Michael J. Girgis , Frank Schaefer
发明人： Mahavir Prashad , Yugang Liu , Bin Hu , Michael J. Girgis , Frank Schaefer
IPC分类号： C07D211/32
CPC分类号： C07D211/26 , C07D213/26
摘要： The present invention relates to salts of aryl compounds as discussed below and to methods of manufacture thereof, as well as other subject matter. More particularly, the invention relates to salts useful as intermediates for the synthesis of the cinnamanilide of formula (Y): where Ra is selected from H, OH, C1, C2, C3 or C4 alkyl; and R1 is C1, C2, C3 or C4 alkyl.
摘要翻译： 本发明涉及如下所述的芳基化合物的盐及其制备方法以及其它主题。 更具体地，本发明涉及可用作合成式（Y）的肉桂酰苯胺的中间体的盐：其中R a选自H，OH，C 1，C 2，C 3或C 4烷基; 并且R 1是C 1，C 2，C 3或C 4烷基。
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公开(公告)号：US20090247581A1
公开(公告)日：2009-10-01
申请号：US12085056
申请日：2006-11-16
申请人： Mahavir Prashad , Yugang Liu , Bin Hu , Michael J. Girgis , Frank Schaefer
发明人： Mahavir Prashad , Yugang Liu , Bin Hu , Michael J. Girgis , Frank Schaefer
IPC分类号： C07D211/26 , A61K31/445
CPC分类号： C07D211/26 , C07B57/00
摘要： The present invention relates to a process for the synthesis of (S)-2′[2-1-(methyl-2-piperidyl) ethyl] cinnamanilide (I) or salts or pharmaceutically acceptable prodrugs thereof:
摘要翻译： 本发明涉及合成（S）-2'[2-1-（甲基-2-哌啶基）乙基]肉桂酰苯胺（I）或其盐或其药学上可接受的前药的方法：
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公开(公告)号：US08008263B2
公开(公告)日：2011-08-30
申请号：US12249186
申请日：2008-10-10
申请人： Shawn D. Britt , Lech Andrzej Ciszewski , Jiping Fu , Subramanian Karur , Yugang Liu , Peichao Lu , David Thomas Parker , Mahavir Prashad , Prakash Raman , Pascal Rigollier , Mohindra Seepersaud , Aregahegn Yifru , Rui Zheng
发明人： Shawn D. Britt , Lech Andrzej Ciszewski , Jiping Fu , Subramanian Karur , Yugang Liu , Peichao Lu , David Thomas Parker , Mahavir Prashad , Prakash Raman , Pascal Rigollier , Mohindra Seepersaud , Aregahegn Yifru , Rui Zheng
CPC分类号： C07D401/12 , C07D403/12 , C07K5/0812 , C07K5/1016
摘要： The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.
摘要翻译： 本申请描述了可用于治疗，预防和/或改善人类疾病的有机化合物。
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公开(公告)号：US08258128B2
公开(公告)日：2012-09-04
申请号：US12224734
申请日：2007-02-21
申请人： Pietro Bollinger , Mahavir Prashad , Bernhard Riss , Janet Dawson King , Peter C. Hiestand , Yugang Liu , Jonathan King , Vincent Schmid , Friedrich Schuerch
发明人： Pietro Bollinger , Mahavir Prashad , Bernhard Riss , Janet Dawson King , Peter C. Hiestand , Yugang Liu , Jonathan King , Vincent Schmid , Friedrich Schuerch
CPC分类号： C07D495/04
摘要： The present invention relates to novel aza-thia-benzoazulene derivatives of formula I as defined in the claims, their preparation, the use of these novel compounds for the preparation of pharmaceutical compositions, the use of these novel compounds and compositions for managing arthritis and arthritis-related conditions as well as in the treatment of pain in animals and humans. More particularly, the present invention relates to pharmaceutical, preferably veterinary compositions and methods for reducing inflammation and pain associated with acute inflammation of body parts, particularly joints, due to injury or due to arthritic conditions or other disease conditions.
摘要翻译： 本发明涉及权利要求中定义的式I的新型氮杂 - 硫杂 - 苯并薁衍生物，其制备方法，这些新化合物在制备药物组合物中的用途，这些新化合物的使用和用于治疗关节炎和关节炎的组合物 相关条件以及治疗动物和人类的疼痛。 更具体地，本发明涉及用于减少由于损伤或由于关节炎病症或其他疾病状况而引起的身体部位，特别是关节的急性炎症的炎症和疼痛的药物，优选兽医组合物和方法。
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10.发明授权Fused pyridine derivatives for use as vanilloid receptor antagonists for treating pain 失效用作治疗疼痛的香草素受体拮抗剂的稠合吡啶衍生物公开(公告)号：US07915264B2
公开(公告)日：2011-03-29
申请号：US10469756
申请日：2002-03-25
申请人： Andrew James Culshaw , Peter Gull , Allan Hallett , Hong-Yong Kim , Max Peter Seiler , Kaspar Zimmermann , Yugang Liu , Mahavir Prashad
发明人： Andrew James Culshaw , Peter Gull , Allan Hallett , Hong-Yong Kim , Max Peter Seiler , Kaspar Zimmermann , Yugang Liu , Mahavir Prashad
IPC分类号： A61K31/519 , C07D471/04
CPC分类号： C07D471/04
摘要： The invention provides compounds of formula (I) wherein R1, R2, R3, R4, and R5 are as defined in the description, and the preparation thereof. The compounds of formula (I) are useful as pharmaceuticals.
摘要翻译： 本发明提供式（I）化合物，其中R 1，R 2，R 3，R 4和R 5如说明书中所定义，及其制备。 式（I）的化合物可用作药物。
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