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1.再颁专利公开(公告)号：USRE43802E1
公开(公告)日：2012-11-13
申请号：US13238923
申请日：2011-09-21
申请人： Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , John N. Freskos , Deborah E. Bertenshaw , Robert M. Heintz
发明人： Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , John N. Freskos , Deborah E. Bertenshaw , Robert M. Heintz
IPC分类号： A61K31/36
CPC分类号： C07C311/05 , A61K38/00 , C07C311/11 , C07C311/13 , C07C311/14 , C07C311/18 , C07C311/20 , C07C311/24 , C07C311/29 , C07C311/32 , C07C311/41 , C07C311/46 , C07C317/04 , C07C317/10 , C07C317/14 , C07C317/28 , C07C317/44 , C07C323/49 , C07C323/67 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07D209/08 , C07D213/30 , C07D213/64 , C07D213/73 , C07D213/81 , C07D213/82 , C07D213/89 , C07D215/48 , C07D233/64 , C07D239/26 , C07D277/24 , C07D277/82 , C07D307/20 , C07D307/42 , C07D307/79 , C07D317/62 , C07D333/34 , C07D405/12 , C07D417/12 , C07K5/06026 , C07K5/06139
摘要： α- and β-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
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2.发明授权α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors 失效α-和α-氨基酸羟乙基氨基磺酰胺，可用作逆转录病毒蛋白酶抑制剂公开(公告)号：US07829564B2
公开(公告)日：2010-11-09
申请号：US11952520
申请日：2007-12-07
申请人： Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , John N. Freskos , Robert M. Heintz , Deborah E. Bertenshaw
发明人： Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , John N. Freskos , Robert M. Heintz , Deborah E. Bertenshaw
IPC分类号： A61K31/44 , A61K31/46 , A61K31/535
CPC分类号： C07C311/05 , A61K38/00 , C07C311/11 , C07C311/13 , C07C311/14 , C07C311/18 , C07C311/20 , C07C311/24 , C07C311/29 , C07C311/32 , C07C311/41 , C07C311/46 , C07C317/04 , C07C317/10 , C07C317/14 , C07C317/28 , C07C317/44 , C07C323/49 , C07C323/67 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07D209/08 , C07D213/30 , C07D213/64 , C07D213/73 , C07D213/81 , C07D213/82 , C07D213/89 , C07D215/48 , C07D233/64 , C07D239/26 , C07D277/24 , C07D277/82 , C07D307/20 , C07D307/42 , C07D307/79 , C07D317/62 , C07D333/34 , C07D405/12 , C07D417/12 , C07K5/06026 , C07K5/06139
摘要： α-and β-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
摘要翻译： α-和β-氨基酸羟基氨基磺酰胺化合物作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶的抑制剂。
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3.发明授权α- and β-Amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors 失效可用作逆转录病毒蛋白酶抑制剂的α-氨基酸和β-氨基酸羟乙基氨基磺酰胺公开(公告)号：US07531538B2
公开(公告)日：2009-05-12
申请号：US11433797
申请日：2006-05-15
申请人： Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , John N. Freskos , Deborah E. Bertenshaw , Robert M. Heintz
发明人： Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , John N. Freskos , Deborah E. Bertenshaw , Robert M. Heintz
IPC分类号： A61K31/18 , C07C311/00
CPC分类号： C07C311/05 , A61K38/00 , C07C311/11 , C07C311/13 , C07C311/14 , C07C311/18 , C07C311/20 , C07C311/24 , C07C311/29 , C07C311/32 , C07C311/41 , C07C311/46 , C07C317/04 , C07C317/10 , C07C317/14 , C07C317/28 , C07C317/44 , C07C323/49 , C07C323/67 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07D209/08 , C07D213/30 , C07D213/42 , C07D213/64 , C07D213/73 , C07D213/74 , C07D213/81 , C07D213/82 , C07D213/89 , C07D215/48 , C07D217/26 , C07D233/64 , C07D239/26 , C07D241/18 , C07D241/44 , C07D261/08 , C07D263/34 , C07D263/56 , C07D277/24 , C07D277/62 , C07D277/82 , C07D307/20 , C07D307/42 , C07D307/45 , C07D307/79 , C07D307/85 , C07D317/62 , C07D333/32 , C07D333/34 , C07D333/48 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D493/04 , C07K5/06026 , C07K5/06139
摘要： α- and β-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
摘要翻译： α-和β-氨基酸羟乙基氨基磺酰胺化合物作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶的抑制剂。
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4.发明授权α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors 失效可用作逆转录病毒蛋白酶抑制剂的α-和β-氨基酸羟乙基氨基磺酰胺公开(公告)号：US07320983B2
公开(公告)日：2008-01-22
申请号：US11526101
申请日：2006-09-25
申请人： Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , John N. Freskos , Robert M. Heintz , Deborah E. Bertenshaw
发明人： Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , John N. Freskos , Robert M. Heintz , Deborah E. Bertenshaw
IPC分类号： A61K31/36 , C07D317/50
CPC分类号： C07C311/05 , A61K38/00 , C07C311/11 , C07C311/13 , C07C311/14 , C07C311/18 , C07C311/20 , C07C311/24 , C07C311/29 , C07C311/32 , C07C311/41 , C07C311/46 , C07C317/04 , C07C317/10 , C07C317/14 , C07C317/28 , C07C317/44 , C07C323/49 , C07C323/67 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07D209/08 , C07D213/30 , C07D213/64 , C07D213/73 , C07D213/81 , C07D213/82 , C07D213/89 , C07D215/48 , C07D233/64 , C07D239/26 , C07D277/24 , C07D277/82 , C07D307/20 , C07D307/42 , C07D307/79 , C07D317/62 , C07D333/34 , C07D405/12 , C07D417/12 , C07K5/06026 , C07K5/06139
摘要： α- and β-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
摘要翻译： α-和β-氨基酸羟乙基氨基磺酰胺化合物作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶的抑制剂。
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5.发明授权Formulation, solubilization, purification, and refolding of tissue factor pathway inhibitor 失效组织因子途径抑制剂的制剂，溶解，纯化和重折叠公开(公告)号：US07226757B2
公开(公告)日：2007-06-05
申请号：US11337518
申请日：2006-01-24
申请人： Glenn J. Dorin , Bo H. Arve , Gregory L. Pattison , Robert F. Halenbeck , Kirk Johnson , Bao-Lu Chen , Raisharan K. Rana , Maninder S. Hora , Hassan Madani , Michael Tsang , Mark E. Gustafson , Gary S. Bild , Gary V. Johnson
发明人： Glenn J. Dorin , Bo H. Arve , Gregory L. Pattison , Robert F. Halenbeck , Kirk Johnson , Bao-Lu Chen , Raisharan K. Rana , Maninder S. Hora , Hassan Madani , Michael Tsang , Mark E. Gustafson , Gary S. Bild , Gary V. Johnson
CPC分类号： C07K14/475 , A23L7/111 , A23L7/165 , A23L9/10 , A23L9/22 , A23L19/09 , A23L19/18 , A23L21/15 , A23L29/212 , A23L29/219 , A23P20/12 , A61K9/0019 , A61K9/08 , A61K38/57 , A61K47/02 , A61K47/12 , A61K47/183 , A61K47/36 , C07K1/1136 , C07K14/8114 , Y10S514/97 , Y10S514/973
摘要： Compositions are described that are suitable for formulating TFPI. Solubilizers and stabilizers facilitate the preparation of pharmaceutically acceptable compositions of TFPI at various concentrations.
摘要翻译： 描述了适合配制TFPI的组合物。 增溶剂和稳定剂有助于制备各种浓度的TFPI的药学上可接受的组合物。
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公开(公告)号：US20040082647A1
公开(公告)日：2004-04-29
申请号：US10419266
申请日：2003-04-21
申请人： G.D. SEARLE, LLC
发明人： Kevin A. Babiak , Andrew Carpenter , Shine Chou , Pierre-Jean Colson , Payman Farid , Robert Hett , Christian H. Huber , Kevin J. Koeller , Jon P. Lawson , James Li , Eduardo K. Mar , Lawrence M. Miller , Vladislav Orlovski , James C. Peterson , Mark J. Pozzo , Claire A. Przybyla , Samuel J. Tremont , Jay S. Trivedi , Grace M. Wagner , Gerald A. Weisenburger , Benxin Zhi
IPC分类号： C07D337/16 , A61K031/38
CPC分类号： C07D409/12 , A61K31/235 , A61K31/38 , A61K31/495 , C07D337/08 , C07D487/08 , A61K2300/00
摘要： Among its several embodiments, the present invention provides an improved process for the preparation of tetrahydrobenzothiepine-1,1-dioxide compounds; the provision of a process for preparing a diastereomeric mixture of tetrahydrobenzothiepine-1,1-dioxide compounds from a single diastereomer of such compounds; the provision of a process for the preparation of 3-bromo-2-substituted propionaldehyde compounds; and the provision of a process for the preparation of 3-thio-2-substituted propionaldehyde compounds.
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7.发明申请Novel mono- and di-fluorinated benzothiepine compouds as inhibitors of apical sodium co-dependent bile acid transport (ASBT) and taurocholate uptake 失效新型单 - 和二 - 氟化苯并噻ine作为顶端钠依赖性胆汁酸转运（ASBT）和牛磺胆酸摄取抑制剂公开(公告)号：US20040067872A1
公开(公告)日：2004-04-08
申请号：US10286987
申请日：2002-11-04
申请人： G.D. SEARLE, LLC
IPC分类号： A61K038/10 , A61K031/7048 , A61K038/04 , A61K031/38 , C07K007/06 , C07K005/04 , C07K017/00
CPC分类号： C07D409/12 , C07D337/08 , C07D487/08 , C07D495/04
摘要： Mono-fluorinated and di-fluorinated benzothiepine apical sodium co-dependent bile acid transport (ASBT) inhibitors are disclosed together with methods of making the same, methods of using the same to treat hyperlipidemic conditions as well as pharmaceutical compositions containing the same compounds.
摘要翻译： 公开了单氟化和二氟化苯并噻庚因顶端钠共依赖性胆汁酸转运（ASBT）抑制剂及其制备方法，使用其来治疗高脂血症的方法以及含有相同化合物的药物组合物。
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公开(公告)号：US20040058908A1
公开(公告)日：2004-03-25
申请号：US10266743
申请日：2002-10-09
申请人： G.D. SEARLE, LLC
发明人： Bradley T. Keller , David B. Reitz , Joseph R. Schuh , James A. Sikorski , Samuel J. Tremont , Rodney W. Lappe
IPC分类号： A61K031/554
CPC分类号： A61K45/06 , A61K31/38 , A61K31/554 , A61K31/575 , A61K2300/00
摘要： The present invention provides combinations of cardiovascular therapeutic compounds for the prophylaxis or treatment of cardiovascular disease including hypercholesterolemia and atherosclerosis. Combinations disclosed include an ileal bile acid transport inhibitor combined with a cholesteryl ester transport protein (CETP) inhibitor, a fibric acid derivative, a nicotinic acid derivative, a microsomal triglyceride transfer protein inhibitor, a cholesterol abosrption antagonist, a phytosterol, a stanol, an antihypertensive agent, or others. Further combinations include a CETP inhibitor with a fibric acid derivative, a nicotinic acid derivative, a bile acid sequestrant, a microsomal triglyceride transfer protein inhibitor, a cholesterol abosrption antagonist, or others.
摘要翻译： 本发明提供了用于预防或治疗心血管疾病（包括高胆固醇血症和动脉粥样硬化）的心血管治疗化合物的组合。 所公开的组合包括与胆固醇酯转运蛋白（CETP）抑制剂，纤维酸衍生物，烟酸衍生物，微粒体甘油三酯转运蛋白抑制剂，胆固醇抗体拮抗剂，植物甾醇，甾烷醇， 抗高血压药等。 进一步的组合包括具有纤维酸衍生物的CETP抑制剂，烟酸衍生物，胆汁酸螯合剂，微粒体甘油三酯转移蛋白抑制剂，胆固醇抗体拮抗剂等。
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9.发明申请Combinations of ileal bile acid transport inhibitors and fibric acid derivatives for cardiovascular indications 审中-公开回肠胆汁酸转运抑制剂和纤维酸衍生物用于心血管适应症的组合公开(公告)号：US20040048846A1
公开(公告)日：2004-03-11
申请号：US10652306
申请日：2003-09-02
申请人： G.D. SEARLE, LLC
IPC分类号： A61K031/554
CPC分类号： A61K45/06 , A61K31/192 , A61K31/216 , A61K31/554 , Y10S514/824 , A61K2300/00
摘要： The present invention provides combinations of cardiovascular therapeutic compounds for the prophylaxis or treatment of cardiovascular disease including hypercholesterolemia, atherosclerosis, or hyperlipidemia. Combinations disclosed include an ileal bile acid transport inhibitor combined with a fibric acid derivative.
摘要翻译： 本发明提供用于预防或治疗包括高胆固醇血症，动脉粥样硬化或高脂血症的心血管疾病的心血管治疗化合物的组合。 公开的组合包括与纤维酸衍生物组合的回肠胆汁酸转运抑制剂。
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公开(公告)号：US20030109558A1
公开(公告)日：2003-06-12
申请号：US10245506
申请日：2002-09-18
申请人： G.D. Searle, LLC
发明人： James A. Sikorski , Kevin C. Glenn
IPC分类号： A61K031/4422 , A61K031/44
CPC分类号： A61K31/585 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/455 , A61K31/55 , A61K31/575 , A61K31/785 , A61K45/06 , Y10S514/824 , A61K2300/00
摘要： The present invention provides combinations of cardiovascular therapeutic compounds for the prophylaxis or treatment of cardiovascular disease including hypercholesterolemia, atherosclerosis, or hyperlipidemia. Combinations disclosed include a nicotinic acid derivative combined with a cholesteryl ester transfer protein (CETP) inhibitor.
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