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公开(公告)号：US08410300B2
公开(公告)日：2013-04-02
申请号：US12311122
申请日：2007-09-20
申请人： Brent Richard Stranix , Jean-Francois Lavallee , Nicolas LeBerre , Valerie Perron , Dominik Herbart , Guy Milot , Chandra Panchal
发明人： Brent Richard Stranix , Jean-Francois Lavallee , Nicolas LeBerre , Valerie Perron , Dominik Herbart , Guy Milot , Chandra Panchal
IPC分类号： C07C309/32
CPC分类号： C07C311/41 , C07C271/22 , C07C311/42 , C07C2601/14 , C07D213/56 , C07D213/82 , C07D265/36 , C07D307/79 , C07D317/62 , C07D319/18 , C07D405/12 , C07D413/12 , C07F9/06 , C07F9/091 , C07F9/58
摘要： The present invention provides HIV protease inhibitors of formulas I, IA, IB, Ib or II, or pharmaceutically acceptable salts thereof, wherein R2 may be, for example, 2-pyridyl-CH2—, 3 -pyridyl-CH2—, 4-pyridyl-CH2—, a sulfonyl group as described in the formulas herein including benzenesulfonyl or thiophenesulfonyl groups, R2a—CO—, R2a being selected from the group consisting of piperonyl, 2-pyrazinyl (unsubstituted or substituted with H, or an alkyl of 1 to 4 carbon atoms) or a picolylamine group as described herein, wherein R3 may be, for example, a phenyl group or diphenylmethyl group as described herein, and wherein Cx may be, for example, COOH, CONR5R6, CH2OH or CH2OR7.
摘要翻译： 本发明提供式I，IA，IB，Ib或II的HIV蛋白酶抑制剂或其药学上可接受的盐，其中R 2可以是例如2-吡啶基-CH 2 - ，3-吡啶基-CH 2 - ，4-吡啶基 -CH 2 - ，如本文所述的磺酰基，包括苯磺酰基或噻吩磺酰基，R2a-CO-，R2a选自胡椒基，2-吡嗪基（未取代或被H取代或由1至 4个碳原子）或吡啶甲基胺，其中R 3可以是例如本文所述的苯基或二苯基甲基，并且其中C x可以是例如COOH，CONR 5 R 6，CH 2 OH或CH 2 OR 7。
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公开(公告)号：US08283366B2
公开(公告)日：2012-10-09
申请号：US13004533
申请日：2011-01-11
IPC分类号： C07D213/62 , C07D213/78 , A61K31/44
CPC分类号： C07D213/81 , A61K31/44 , A61K45/06 , C07D491/04 , A61K2300/00
摘要： The present invention relates to compounds of Formula I or pharmaceutically acceptable salts, solvates or formulations thereof. Compounds of Formula I inhibit HIV-integrase enzyme and are useful for preventing and treating of HIV infection, acquired immune deficiency syndrome (AIDS), AIDS-related complex (ARC), hepatitis C, and other diseases and conditions caused or mediated by HIV infection.
摘要翻译： 本发明涉及式I化合物或其药学上可接受的盐，溶剂合物或制剂。 式I的化合物抑制HIV整合酶，并且可用于预防和治疗HIV感染，获得性免疫缺陷综合征（AIDS），AIDS相关复合物（ARC），丙型肝炎以及由HIV感染引起或介导的其他疾病和病症 。
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3.发明授权Lysine-based prodrugs of aspartyl protease inhibitors and processes for their preparation 有权天冬氨酰蛋白酶抑制剂的赖氨酸类前体药物及其制备方法公开(公告)号：US08227450B2
公开(公告)日：2012-07-24
申请号：US12086184
申请日：2006-11-30
申请人： Guy Milot , Stephane Branchaud , Brent R. Stranix
发明人： Guy Milot , Stephane Branchaud , Brent R. Stranix
IPC分类号： A61K31/661 , C07F9/09
CPC分类号： C07F9/091
摘要： The present invention provides processes for synthesizing lysine based compounds of the formula; wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, wherein X may be, for example, NH2, Y may be H, F, Cl, or Br, and wherein n, X′, Y′, R2, R3, R4, R5 and R6 are as defined herein.
摘要翻译： 本发明提供了用于合成下式的赖氨酸的化合物的方法： 其中R 1可以是例如（HO）2 P（O） - ，（NaO）2 P（O） - ，其中X可以是例如NH 2，Y可以是H，F，Cl或Br，其中 n，X'，Y'，R 2，R 3，R 4，R 5和R 6如本文所定义。
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公开(公告)号：US07129245B2
公开(公告)日：2006-10-31
申请号：US10629817
申请日：2003-07-29
申请人： Douglas Wade Beight , Trelia Joyce Craft , Carl Penman Denny , Jeffry Bernard Franciskovich , Theodore Goodson, Jr. , Steven Edward Hall , David Kent Herron , Sajan Joseph , Valentine Joseph Klimkowski , Jeffrey Alan Kyle , John Joseph Masters , David Mendel , Guy Milot , Marta Maria Pi{hacek over (n)}elro-Nú{hacek over (n)}ez , Jason Scott Sawyer , Robert Theodore Shuman , Gerald Floyd Smith , Anne Louise Tebbe , Jennifer Marie Tinsley , Leonard Crayton Weir , James Howard Wikel , Michael Robert Wiley , Ying Kwong Yee
发明人： Douglas Wade Beight , Trelia Joyce Craft , Carl Penman Denny , Jeffry Bernard Franciskovich , Theodore Goodson, Jr. , Steven Edward Hall , David Kent Herron , Sajan Joseph , Valentine Joseph Klimkowski , Jeffrey Alan Kyle , John Joseph Masters , David Mendel , Guy Milot , Marta Maria Pi{hacek over (n)}elro-Nú{hacek over (n)}ez , Jason Scott Sawyer , Robert Theodore Shuman , Gerald Floyd Smith , Anne Louise Tebbe , Jennifer Marie Tinsley , Leonard Crayton Weir , James Howard Wikel , Michael Robert Wiley , Ying Kwong Yee
IPC分类号： A61K31/506 , C07D239/04
CPC分类号： C07D213/75 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
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公开(公告)号：US06689780B1
公开(公告)日：2004-02-10
申请号：US09857749
申请日：2001-06-08
申请人： Douglas Wade Beight , Trelia Joyce Craft , Jeffry Bernard Franciskovich , Theodore Goodson, Jr. , Steven Edward Hall , David Kent Herron , Sajan Joseph , Valentine Joseph Klimkowski , Jeffrey Alan Kyle , John Joseph Masters , David Mendel , Guy Milot , Marta Maria Piñeiro-Nuñez , Jason Scott Sawyer , Robert Theodore Shuman , Gerald Floyd Smith , Anne Louise Tebbe , Jennifer Marie Tinsley , Leonard Crayton Weir , James Howard Wikel , Michael Robert Wiley , Ying Kwong Yee
发明人： Douglas Wade Beight , Trelia Joyce Craft , Jeffry Bernard Franciskovich , Theodore Goodson, Jr. , Steven Edward Hall , David Kent Herron , Sajan Joseph , Valentine Joseph Klimkowski , Jeffrey Alan Kyle , John Joseph Masters , David Mendel , Guy Milot , Marta Maria Piñeiro-Nuñez , Jason Scott Sawyer , Robert Theodore Shuman , Gerald Floyd Smith , Anne Louise Tebbe , Jennifer Marie Tinsley , Leonard Crayton Weir , James Howard Wikel , Michael Robert Wiley , Ying Kwong Yee
IPC分类号： C07D40114
CPC分类号： C07D213/82 , C07D401/12 , C07D401/14 , C07D405/14 , C07D417/14
摘要： This application relates to heteroaromatic amides (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
摘要翻译： 本申请涉及本文定义的杂芳族酰胺（或其药学上可接受的盐），其药物组合物及其作为因子Xa抑制剂的用途，以及其制备方法及其中间体。
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公开(公告)号：US06417200B1
公开(公告)日：2002-07-09
申请号：US09445970
申请日：2000-05-09
申请人： Douglas Wade Beight , Trelia Joyce Craft , Jeffry Bernard Franciskovich , Theodore Goodson, Jr. , Steven Edward Hall , David Kent Herron , Valentine Joseph Klimkowski , John Joseph Masters , David Mendel , Guy Milot , Jason Scott Sawyer , Robert Theodore Shuman , Gerald Floyd Smith , Anne Louise Tebbe , Jennifer Marie Tinsley , Leonard Crayton Weir , James Howard Wikel , Michael Robert Wiley , Ying Kwong Yee
发明人： Douglas Wade Beight , Trelia Joyce Craft , Jeffry Bernard Franciskovich , Theodore Goodson, Jr. , Steven Edward Hall , David Kent Herron , Valentine Joseph Klimkowski , John Joseph Masters , David Mendel , Guy Milot , Jason Scott Sawyer , Robert Theodore Shuman , Gerald Floyd Smith , Anne Louise Tebbe , Jennifer Marie Tinsley , Leonard Crayton Weir , James Howard Wikel , Michael Robert Wiley , Ying Kwong Yee
IPC分类号： A61K31445
CPC分类号： C07C271/66 , A61K31/00 , C07C257/18 , C07C259/18 , C07C271/64 , C07D209/44 , C07D211/60 , C07D261/20 , C07D333/38
摘要： This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
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公开(公告)号：US08664248B2
公开(公告)日：2014-03-04
申请号：US13605502
申请日：2012-09-06
IPC分类号： A61K31/44 , C07D213/62 , C07D213/78
CPC分类号： C07D213/81 , A61K31/44 , A61K45/06 , C07D491/04 , A61K2300/00
摘要： The present invention relates to methods of treating hepatitis C infection, HIV infection, AIDS, or AIDS-related complex, or inhibiting HIV replication by administering a compound of Formula I wherein: X is H or OH; Y is H or OH; R1 is H or halogen (F, Cl, Br, I); R2 is H or halogen (F, Cl, Br, I); R3 is H, C1-6 alkyl, C1-6 fluoroalkyl, or benzyl; R4 is H, C1-6 alkyl, or benzyl; and R5 is H or C1-6 alkyl; or pharmaceutically acceptable salts thereof, to a mammal.
摘要翻译： 本发明涉及通过施用式I化合物治疗丙型肝炎感染，HIV感染，AIDS或AIDS相关复合物或抑制HIV复制的方法，其中：X是H或OH; Y是H或OH; R1是H或卤素（F，Cl，Br，I）; R2是H或卤素（F，Cl，Br，I）; R3是H，C1-6烷基，C1-6氟烷基或苄基; R4是H，C1-6烷基或苄基; 并且R 5是H或C 1-6烷基; 或其药学上可接受的盐。
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公开(公告)号：US20110178120A1
公开(公告)日：2011-07-21
申请号：US12995890
申请日：2009-06-04
申请人： Brent Stranix , Francis Beaulieu , Jean-Emmanuel Bouchard , Guy Milot , Wang Zhigang , Réjean Ruel
发明人： Brent Stranix , Francis Beaulieu , Jean-Emmanuel Bouchard , Guy Milot , Wang Zhigang , Réjean Ruel
IPC分类号： A61K31/436 , C07D213/81 , C07D405/12 , C07D491/056 , C07D401/12 , A61K31/4412 , A61K31/444 , A61K31/44 , A61K31/443 , C12N5/071 , A61P31/18
CPC分类号： C07D213/81 , C07D405/12 , C07D491/04
摘要： The present invention relates to pyridoxine (vitamin B6) derived compounds of formula (I), pharmaceutically acceptable salts, or solvates thereof, wherein R1, R2, R4, A, L B1 and B2 are as defined in the specification, and pharmaceutical compositions comprising the compounds. Compounds of formula (I) inhibit Human Immunodeficiency Virus (HIV)-integrase enzyme and are useful for preventing and treating HIV infection and AIDS.
摘要翻译： 本发明涉及衍生自式（I）的吡哆醇（维生素B6）衍生化合物，其药学上可接受的盐或溶剂化物，其中R1，R2，R4，A，L B1和B2如说明书中所定义， 化合物。 式（I）化合物抑制人类免疫缺陷病毒（HIV） - 整合酶，可用于预防和治疗HIV感染和艾滋病。
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9.发明申请LYSINE-BASED PRODRUGS OF ASPARTYL PROTEASE INHIBITORS AND PROCESSES FOR THEIR PREPARATION 有权基于蛋白质的ASPARTYL蛋白酶抑制剂的制剂及其制备方法公开(公告)号：US20100130765A1
公开(公告)日：2010-05-27
申请号：US12086184
申请日：2006-11-30
IPC分类号： C07F9/09
CPC分类号： C07F9/091
摘要： The present invention provides processes for synthesizing lysine based compounds of the formula; , wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, wherein X may be, for example, NH2, Y may be H, F, Cl, or Br, and wherein n, X′, Y′, R2, R3, R4, R5 and R6 are as defined herein.
摘要翻译： 本发明提供了用于合成下式的赖氨酸的化合物的方法： 其中R 1可以是例如（HO）2 P（O） - ，（NaO）2 P（O） - ，其中X可以是例如NH 2，Y可以是H，F，Cl或Br，和 其中n，X'，Y'，R 2，R 3，R 4，R 5和R 6如本文所定义。
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公开(公告)号：US06716855B2
公开(公告)日：2004-04-06
申请号：US10374124
申请日：2003-02-25
申请人： Douglas Wade Beight , Trelia Joyce Craft , Jeffry Bernard Franciskovich , Theodore Goodson, Jr. , Steven Edward Hall , David Kent Herron , Sajan Joseph , Valentine Joseph Klimkowski , Jeffrey Alan Kyle , John Joseph Masters , David Mendel , Guy Milot , Marta Maria Piñeiro-Núñez , Jason Scott Sawyer , Robert Theodore Shuman , Gerald Floyd Smith , Anne Louise Tebbe , Jennifer Marie Tinsley , Leonard Crayton Weir , James Howard Wikel , Michael Robert Wiley , Ying Kwong Yee
发明人： Douglas Wade Beight , Trelia Joyce Craft , Jeffry Bernard Franciskovich , Theodore Goodson, Jr. , Steven Edward Hall , David Kent Herron , Sajan Joseph , Valentine Joseph Klimkowski , Jeffrey Alan Kyle , John Joseph Masters , David Mendel , Guy Milot , Marta Maria Piñeiro-Núñez , Jason Scott Sawyer , Robert Theodore Shuman , Gerald Floyd Smith , Anne Louise Tebbe , Jennifer Marie Tinsley , Leonard Crayton Weir , James Howard Wikel , Michael Robert Wiley , Ying Kwong Yee
IPC分类号： A61K3144
CPC分类号： C07D295/135 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/14
摘要： This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
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