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公开(公告)号：US07244721B2
公开(公告)日：2007-07-17
申请号：US10052386
申请日：2002-01-18
申请人： Anil K. Saksena , Viyyoor Moopil Girijavallabhan , Raymond G. Lovey , Edwin Jao , Frank Bennett , Jinping L. Mc Cormick , Haiyan Wang , Russell E. Pike , Stephane L. Bogen , Tin-Yau Chan , Yi-Tsung Liu , Zhaoning Zhu , F. George Njoroge , Ashok Arasappan , Tejal Parekh , Ashit K. Ganguly , Kevin X. Chen , Srikanth Venkatraman , Henry A. Vaccaro , Patrick A. Pinto , Bama Santhanam , Scott Jeffrey Kemp , Odile Esther Levy , Marguerita Lim-Wilby , Susan Y. Tamura , Wanli Wu , Siska Hendrata , Yuhua Huang , Jesse K. Wong , Latha G. Nair
发明人： Anil K. Saksena , Viyyoor Moopil Girijavallabhan , Raymond G. Lovey , Edwin Jao , Frank Bennett , Jinping L. Mc Cormick , Haiyan Wang , Russell E. Pike , Stephane L. Bogen , Tin-Yau Chan , Yi-Tsung Liu , Zhaoning Zhu , F. George Njoroge , Ashok Arasappan , Tejal Parekh , Ashit K. Ganguly , Kevin X. Chen , Srikanth Venkatraman , Henry A. Vaccaro , Patrick A. Pinto , Bama Santhanam , Scott Jeffrey Kemp , Odile Esther Levy , Marguerita Lim-Wilby , Susan Y. Tamura , Wanli Wu , Siska Hendrata , Yuhua Huang , Jesse K. Wong , Latha G. Nair
IPC分类号： A61K31/497 , A61K31/407 , A61K31/454 , A61K31/4025
CPC分类号： C07K5/0804 , A61K38/00 , C07K5/0202 , C07K5/0812 , C07K5/0827 , C07K7/02
摘要： The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
摘要翻译： 本发明公开了具有HCV蛋白酶抑制活性的新型化合物及其制备方法。 在另一个实施方案中，本发明公开了包含这些化合物的药物组合物以及使用它们来治疗与HCV蛋白酶相关的病症的方法。
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公开(公告)号：US4851423A
公开(公告)日：1989-07-25
申请号：US940125
申请日：1986-12-10
IPC分类号： C07D249/08 , A61K31/075 , A61K31/095 , A61K31/12 , A61K31/15 , A61K31/165 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/421 , A61K31/435 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61K31/443 , A61K31/496 , A61K31/505 , A61K31/52 , A61P7/02 , A61P29/00 , A61P31/12 , C07C45/00 , C07C49/00 , C07C67/00 , C07C313/00 , C07C317/24 , C07C317/26 , C07C317/44 , C07C323/12 , C07C323/20 , C07C323/22 , C07C323/25 , C07C323/36 , C07C323/41 , C07C323/47 , C07C323/65 , C07D213/30 , C07D213/69 , C07D213/70 , C07D233/54 , C07D233/56 , C07D233/58 , C07D233/60 , C07D233/61 , C07D233/64 , C07D233/84 , C07D233/90 , C07D233/91 , C07D233/94 , C07D235/06 , C07D235/12 , C07D235/26 , C07D235/28 , C07D239/54 , C07D257/04 , C07D257/06 , C07D263/32 , C07D277/24 , C07D277/36 , C07D295/08 , C07D295/092 , C07D307/20 , C07D405/04 , C07D405/06 , C07D413/06 , C07D413/12 , C07D471/04 , C07D473/00 , C07D473/34 , C07D487/04 , C07D493/04 , C07D521/00
CPC分类号： C07D213/30 , C07D213/69 , C07D213/70 , C07D231/12 , C07D233/56 , C07D233/64 , C07D233/90 , C07D233/94 , C07D235/06 , C07D235/26 , C07D235/28 , C07D239/54 , C07D249/08 , C07D257/04 , C07D257/06 , C07D277/36 , C07D295/088 , C07D307/20 , C07D405/06 , C07D413/06 , C07D413/12 , C07D471/04 , C07D473/00 , C07D473/34 , C07D487/04 , C07D493/04
摘要： The disclosed invention is compounds represented by the formulaZ--X--Q--Y--W, IZ--X--Q--Y--W'--Y--Q--X--Z IIand pharmaceutically acceptable acid addition salts and quarternary amine salts thereof, whereinZ is phenyl, naphthyl or adamantyl; substituted phenyl wherein the substituents are one or more of halogen, lower alkoxy, phenoxy, nitrile, nitro, phenylsulfonyl, methylsulfonyl, isoxazol-2-yl, lower alkanoyl, benzoyl, lower alkoxycarbonyl, lower alkyl, loweralkylthio, phenyl, phenylaminothiocarbonyl, or lower alkylaminothiocarbonyl; 5 or 6 membered unsubstituted or substituted heterocyclic ring containing at least one nitrogen and one carbon in the ring, wherein the substituents are one or more of carboxyl, hydroxymethyl, loweralkyl, loweralkylcarbonyl or aryl lower alkyl; or tertiary butyl;X and Y are each independently a bond, -O-, ##STR1## Q is a divalent substituted or unsubstituted straight or branched chain lower alkanediyl, -lower alkanedinyl- cycloalkanediyl- lower alkanediyl-, lower alkendiyl, lower alkynediyl, phenylene, tetrahydrofurandiyl or tetrahydropyrandiyl;W is a monovalent substituted or unsubstituted aromatic heterocyclic single or fused ring containing from 5 to 10 ring atoms, at least one hetero atom of which is a nitrogen atom, wherein the substituents are hydroxy, amino, carbamoyl, carboxyl, nitrile, nitro, oxo, lower alkoxy carbonyl, halogen, sulfamyl, lower alkyl, lower alkylthio, lower alkoxy, hydroxyloweralkyl, lower alkoxycarbonylloweralkyl, amino loweralkyl, carboxyloweralkyl, guanidino, thioureido, lower alkylsulfonylamino, aminocarbonylloweralkyl, allyloxycarbonylmethyl or carbamoyloxylowralkyl; andW' is divalent W.The compounds have antiviral activity, antiinflammatory activity and are PAF inhibitors.
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公开(公告)号：US4503064A
公开(公告)日：1985-03-05
申请号：US576499
申请日：1984-02-02
IPC分类号： C07D205/09 , C07D233/54 , C07D409/12 , C07D499/88 , C07F7/08 , C07F7/18 , C07D499/00 , A61K31/425
CPC分类号： C07D233/64 , C07D205/09 , C07D409/12 , C07D499/88 , C07F7/0812 , C07F7/0818 , C07F7/1804
摘要： There is disclosed 2-(oximinoalkylthio)penems and their pharmaceutically acceptable salts and esters and their use as antibacterials.
摘要翻译： 公开了2-（肟基烷硫基）penem及其药学上可接受的盐和酯及其作为抗菌剂的用途。
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4.发明授权5R,6S,8R-2-(1-Methyl-2-imidazolylmethy lthio)-6-(1-hydroxyethyl)penem-3-carboxylic acid 失效5R，6S，8R-2-（1-甲基-2-咪唑基甲硫基）-6-（1-羟乙基）青霉烯-3-羧酸
公开(公告)号：US4435412A
公开(公告)日：1984-03-06
申请号：US458511
申请日：1983-01-17
IPC分类号： C07D205/09 , C07D233/54 , C07D409/12 , C07D499/88 , C07F7/08 , C07F7/18 , C07D501/36 , A61K31/425
CPC分类号： C07D233/64 , C07D205/09 , C07D409/12 , C07D499/88 , C07F7/0812 , C07F7/0818 , C07F7/1804 , Y02P20/55
摘要： There is disclosed the antibacterial 5R,6S,8R-2-(1-methyl-2-imidazolylmethylthio)-6-(1-hydroxyethyl)penem-3-carboxylic acid, its pharmaceutically acceptable salts and esters as well as compositions containing them and methods for their use.
摘要翻译： 公开了抗菌5R，6S，8R-2-（1-甲基-2-咪唑基甲硫基）-6-（1-羟乙基）青霉烯-3-羧酸，其药学上可接受的盐和酯以及含有它们的组合物， 使用方法
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公开(公告)号：US07592419B2
公开(公告)日：2009-09-22
申请号：US10948367
申请日：2004-09-23
申请人： Srikanth Venkatraman , F. George Njoroge , Wanli Wu , Viyyoor M. Girijavallabhan , Brian McKittrick , Jing Su , Francisco Velazquez , Patrick A. Pinto
发明人： Srikanth Venkatraman , F. George Njoroge , Wanli Wu , Viyyoor M. Girijavallabhan , Brian McKittrick , Jing Su , Francisco Velazquez , Patrick A. Pinto
CPC分类号： C07D245/04 , A61K31/33 , A61K38/12 , A61K38/21 , A61K38/212 , C04B35/632 , C07D401/12 , C07D403/12 , C07D409/12 , C07D487/04 , C07D513/04 , C07K5/0217 , C07K5/0802 , A61K2300/00
摘要： The present invention discloses novel compounds which have HCV protease inhibitory activity as well as pharmaceutical compositions comprising such compounds and methods of using them to treat disorders associated with the HCV protease. The novel compounds typically include a 15-20 member macrocycle and have the general structure of structural Formula 1: wherein Z′, L′, M′, R1, X and D are defined herein.
摘要翻译： 本发明公开了具有HCV蛋白酶抑制活性的新化合物以及包含这些化合物的药物组合物及其用于治疗与HCV蛋白酶相关的病症的方法。 新化合物通常包括15-20个成员大环，并且具有结构式1的一般结构：其中Z'，L'，M'，R 1，X和D在本文中定义。
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公开(公告)号：US5459144A
公开(公告)日：1995-10-17
申请号：US169809
申请日：1993-12-17
IPC分类号： C07D213/30 , C07D213/69 , C07D213/70 , C07D233/54 , C07D233/70 , C07D233/90 , C07D233/94 , C07D235/06 , C07D235/26 , C07D235/28 , C07D239/54 , C07D257/04 , C07D257/06 , C07D277/36 , C07D295/092 , C07D307/20 , C07D401/06 , C07D405/06 , C07D413/06 , C07D413/12 , C07D471/04 , C07D473/00 , C07D473/32 , C07D473/34 , C07D487/04 , C07D493/04 , C07D521/00 , A61K31/505 , A61K31/415 , A61K31/425 , A61K31/44 , C07D211/70 , C07D405/12 , C07D471/02 , C07D487/00
CPC分类号： C07D213/30 , C07D213/69 , C07D213/70 , C07D231/12 , C07D233/56 , C07D233/64 , C07D233/70 , C07D233/90 , C07D233/94 , C07D235/06 , C07D235/26 , C07D235/28 , C07D239/54 , C07D249/08 , C07D257/04 , C07D257/06 , C07D277/36 , C07D295/088 , C07D307/20 , C07D401/06 , C07D405/06 , C07D413/06 , C07D413/10 , C07D471/04 , C07D473/00 , C07D473/32 , C07D473/34 , C07D487/04 , C07D493/04
摘要： The invention relates to compounds of the formula ##STR1## wherein Z, X, Q, Y, W, and W' are as described herein. These compounds have antiviral activity, and certain of these compounds have antiinflammatory activity and are PAF inhibitors.
摘要翻译： 本发明涉及下式化合物：其中Z，X，Q，Y，W和W'如本文所述。 这些化合物具有抗病毒活性，并且这些化合物中的某些具有抗炎活性并且是PAF抑制剂。
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公开(公告)号：US5272167A
公开(公告)日：1993-12-21
申请号：US809474
申请日：1991-12-18
IPC分类号： C07D213/30 , C07D213/69 , C07D213/70 , C07D233/54 , C07D233/70 , C07D233/90 , C07D233/94 , C07D235/06 , C07D235/26 , C07D235/28 , C07D239/54 , C07D257/04 , C07D257/06 , C07D277/36 , C07D295/092 , C07D307/20 , C07D401/06 , C07D405/06 , C07D413/06 , C07D413/12 , C07D471/04 , C07D473/00 , C07D473/32 , C07D473/34 , C07D487/04 , C07D493/04 , C07D521/00 , C07D401/12 , A61K31/415
CPC分类号： C07D213/30 , C07D213/69 , C07D213/70 , C07D231/12 , C07D233/56 , C07D233/64 , C07D233/70 , C07D233/90 , C07D233/94 , C07D235/06 , C07D235/26 , C07D235/28 , C07D239/54 , C07D249/08 , C07D257/04 , C07D257/06 , C07D277/36 , C07D295/088 , C07D307/20 , C07D401/06 , C07D405/06 , C07D413/06 , C07D413/10 , C07D471/04 , C07D473/00 , C07D473/32 , C07D473/34 , C07D487/04 , C07D493/04
摘要： Compounds of the formulaZ--X--Q--Y--Wpharmaceutically acceptable acid addition, basic addition salts or quaternary amine salts thereof, whereinZ is phenyl, substituted phenyl, wherein the substituents are independently one or more of halogen, lower alkylthio, loweralkylsulfonyl, lower alkoxy, oxazol-2-yl; imidazo-1-yl; lower alkyl substituted imidazo-1-yl; or tert-butyl;X is a bond, ##STR1## Q is lower alkane-diyl or 5, 6, or 7 carbon atoms optionally substituted by --OH; loweralkylnediyl of 6-8 carbon atoms; methylcyclohexylmethyl; tetrahydrofurandiyl; or (C.sub.1 -C.sub.2) lower alkane-diyl tetrahydrofurandiyl-C.sub.1 -C.sub.2 loweralkanediyl; wherein the tetrahydrofuran ring is substituted by 0-2 hydroxy groups;Y is a bond; andW is benzimidazol-1-yl or benzimidazol-2-yl are described. These compounds have antiviral activity, antiinflammatory activity and are PAF inhibitors.
摘要翻译： PCT No.PCT / US90 / 03694 Sec。 371 1991年12月18日第 102（e）1991年12月18日授权PCT 1990年7月6日PCT。化学式ZXQYW药学上可接受的酸加成盐，其碱加成盐或季胺盐，其中Z是苯基，取代的苯基，其中取代基独立地 一个或多个卤素，低级烷硫基，低级烷基磺酰基，低级烷氧基，恶唑-2-基; 咪唑-1-基; 低级烷基取代的咪唑-1-基; 或叔丁基; X是一个键，Q是低级烷基 - 二基或5,6或7个任选被-OH取代的碳原子; 6-8个碳原子的低级烷基烷基; 甲基环己基甲基; 四氢呋喃二基; 或（C1-C2）低级烷基二基四氢呋喃二基C1-C2低级烷二基; 其中四氢呋喃环被0-2个羟基取代; Y是一个债券; 和W是苯并咪唑-1-基或苯并咪唑-2-基。 这些化合物具有抗病毒活性，抗炎活性，是PAF抑制剂。
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公开(公告)号：US4530793A
公开(公告)日：1985-07-23
申请号：US445295
申请日：1982-11-29
IPC分类号： C07D205/09 , C07D233/54 , C07D409/12 , C07D499/88 , C07F7/08 , C07F7/18 , C07D499/00 , A61K31/545
CPC分类号： C07D233/64 , C07D205/09 , C07D409/12 , C07D499/88 , C07F7/0812 , C07F7/0818 , C07F7/1804
摘要： Processes for the production of 6-hydroxyethyl-2-substituted thio penem-3-carboxylates are disclosed as well as novel penems.
摘要翻译： 公开了用于生产6-羟乙基-2-取代的硫代青霉烯-3-羧酸酯的方法以及新颖的青铜。
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公开(公告)号：USRE43298E1
公开(公告)日：2012-04-03
申请号：US13068159
申请日：2011-04-22
申请人： Anil K. Saksena , Viyyoor Moopil Girijavallabhan , Raymond G. Lovey , Edwin Jao , Frank Bennett , Jinping L. McCormick , Haiyan Wang , Russell E. Pike , Stephane L. Bogen , Tin-Yau Chan , Yi-Tsung Liu , Zhaoning Zhu , F. George Njoroge , Ashok Arasappan , Tejal Parekh , Ashit K. Ganguly , Kevin X. Chen , Srikanth Venkatraman , Henry M. Vaccaro , Patrick A. Pinto , Bama Santhanam , Scott Jeffrey Kemp , Odile Esther Levy , Marguerita Lim-Wilby , Susan Y. Tamura , Wanli Wu , Siska Hendrata , Yuhua Huang
发明人： Anil K. Saksena , Viyyoor Moopil Girijavallabhan , Raymond G. Lovey , Edwin Jao , Frank Bennett , Jinping L. McCormick , Haiyan Wang , Russell E. Pike , Stephane L. Bogen , Tin-Yau Chan , Yi-Tsung Liu , Zhaoning Zhu , F. George Njoroge , Ashok Arasappan , Tejal Parekh , Ashit K. Ganguly , Kevin X. Chen , Srikanth Venkatraman , Henry M. Vaccaro , Patrick A. Pinto , Bama Santhanam , Scott Jeffrey Kemp , Odile Esther Levy , Marguerita Lim-Wilby , Susan Y. Tamura , Wanli Wu , Siska Hendrata , Yuhua Huang
IPC分类号： A61K38/00 , A01N37/18 , A61P1/16 , A61P31/12 , A61K39/12 , G01N33/53 , A61K38/07 , A61K38/06 , C07K5/08 , C07K5/10
CPC分类号： C07K5/0202 , A61K38/00 , C07K5/0812 , C07K5/0827 , C07K7/02
摘要： The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
摘要翻译： 本发明公开了具有HCV蛋白酶抑制活性的新型化合物及其制备方法。 在另一个实施方案中，本发明公开了包含这些化合物的药物组合物以及使用它们来治疗与HCV蛋白酶相关的病症的方法。
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公开(公告)号：US08143305B2
公开(公告)日：2012-03-27
申请号：US12675897
申请日：2008-08-27
申请人： Gopinadhan N. Anilkumar , Frank Bennett , Tin-Yau Chan , Kevin X. Chen , Mousumi Sannigrahi , Francisco Velazquez , Srikanth Venkatraman , Qingbei Zeng , Jose S. Duca , Charles A. Lesburg , Joseph A. Kozlowski , F. George Njoroge , Stuart B. Rosenblum , Neng-Yang Shih , Stephen J. Gavalas , Yueheng Jiang , Patrick A. Pinto , Haiyan Pu , Oleg B. Selyutin , Bancha Vibulbhan , Li Wang , Wanli Wu , Weiying Yang , Yuhua Huang , Hsueh-Cheng Huang , Robert Palermo , Boris Feld
发明人： Gopinadhan N. Anilkumar , Frank Bennett , Tin-Yau Chan , Kevin X. Chen , Mousumi Sannigrahi , Francisco Velazquez , Srikanth Venkatraman , Qingbei Zeng , Jose S. Duca , Charles A. Lesburg , Joseph A. Kozlowski , F. George Njoroge , Stuart B. Rosenblum , Neng-Yang Shih , Stephen J. Gavalas , Yueheng Jiang , Patrick A. Pinto , Haiyan Pu , Oleg B. Selyutin , Bancha Vibulbhan , Li Wang , Wanli Wu , Weiying Yang , Yuhua Huang , Hsueh-Cheng Huang , Robert Palermo , Boris Feld
IPC分类号： A01N43/38 , A61K31/40 , C07D209/04
CPC分类号： C07D417/14 , C07D209/42 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention relates to 2,3-Substituted Indole Derivatives, compositions comprising at least one 2,3-Substituted Indole Derivative, and methods of using the 2,3-Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
摘要翻译： 本发明涉及2,3-取代的吲哚衍生物，包含至少一种2,3-取代的吲哚衍生物的组合物和使用2,3-取代的吲哚衍生物用于治疗或预防病毒感染或病毒相关的方法 病人无序。
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