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公开(公告)号：US5919780A
公开(公告)日：1999-07-06
申请号：US981505
申请日：1997-12-11
申请人： Gary L. Bolton , Annette M Doherty , James S. Kaltenbronn , John Quin, III , Jeffrey D. Scholten , Judith Sebolt-Leopold , Harold Zinnes
发明人： Gary L. Bolton , Annette M Doherty , James S. Kaltenbronn , John Quin, III , Jeffrey D. Scholten , Judith Sebolt-Leopold , Harold Zinnes
IPC分类号： C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D521/00 , A01N43/62
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要： Compounds of formula I ##STR1## wherein X is N or C--R.sup.9, Y is N--R.sup.10, CH.sub.2, O, S, SO, SO.sub.2, C.dbd.O or CH--OH,R is H or alkyl,R.sup.1 is heteroaryl,n is 1-5, andR.sup.2 -R.sup.10 are H or various substituents,are useful as inhibitors of protein farnesyl transferase and for the treatment of proliferative diseases including cancer, restenosis and psoriasis, and as antiviral agents.
摘要翻译： PCT No.PCT / US96 / 08528 Sec。 371 1997年12月11日第 102（e）日期1997年12月11日PCT Filted 1996年6月4日PCT公布。 公开号WO97 / 00252 日期1997年1月3日其中X为N或C-R9，Y为N-R10，CH2，O，S，SO，SO2，C = O或CH-OH的式I化合物，R为H或烷基，R1为 杂芳基，n为1-5，R2-R10为H或各种取代基，可用作蛋白法呢基转移酶的抑制剂和用于治疗增殖性疾病，包括癌症，再狭窄和牛皮癣以及作为抗病毒剂。
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公开(公告)号：US5620997A
公开(公告)日：1997-04-15
申请号：US456149
申请日：1995-05-31
申请人： Gary L. Bolton , John M. Domagala , Edward F. Elslager , Rocco D. Gogliotti , Terri S. Purchase , Joseph P. Sanchez , Bharat K. Trivedi
发明人： Gary L. Bolton , John M. Domagala , Edward F. Elslager , Rocco D. Gogliotti , Terri S. Purchase , Joseph P. Sanchez , Bharat K. Trivedi
IPC分类号： A61K31/428 , A61K31/437 , A61K31/4439 , A61K31/506 , A61K31/519 , A61K31/5377 , A61P9/10 , A61P29/00 , A61P31/12 , A61P31/14 , C07D275/04 , C07D417/04 , C07D513/04 , C07D513/14 , C07D275/06 , A61K31/41
CPC分类号： C07D275/04 , C07D513/04 , C07D513/14
摘要： Isothiazolones having the general structure ##STR1## where A is a monocyclic or bicyclic ring which may contain up to 3 heteroatoms selected from O, S, and N; R.sup.1 and R.sup.2 are substituent groups such as alkyl, alkoxy, hydroxy, nitro, cyano, amino, and carboxy; and R.sup.5 is alkyl, cycloalkyl, phenyl, and Het. The isothiazolones are useful as anti-retroviral agents, anti-inflammatory agents, and anti-atherosclerotic agents.
摘要翻译： 具有一般结构
的异噻唑酮，其中A是可以含有至多3个选自O，S和N的杂原子的单环或双环; R1和R2是取代基，例如烷基，烷氧基，羟基，硝基，氰基，氨基和羧基; R5是烷基，环烷基，苯基和Het。 异噻唑酮可用作抗逆转录病毒剂，抗炎剂和抗动脉粥样硬化剂。 -
3.发明授权Natural product analogs including an anti-inflammatory cyanoenone pharmacore and methods of use 有权天然产物类似物，包括抗炎氰基酮药物及其使用方法公开(公告)号：US09233998B2
公开(公告)日：2016-01-12
申请号：US13552530
申请日：2012-07-18
申请人： Eric Anderson , Gary L. Bolton , Deborah A. Ferguson , Xin Jiang , Robert M. Kral, Jr. , Patrick M. O'Brien , Melean Visnick
发明人： Eric Anderson , Gary L. Bolton , Deborah A. Ferguson , Xin Jiang , Robert M. Kral, Jr. , Patrick M. O'Brien , Melean Visnick
IPC分类号： C07C255/46 , C07D317/26 , C07J41/00 , C07D311/74 , C07D493/10 , C07F7/18 , C07J21/00 , C07J53/00 , C07J71/00
CPC分类号： C07C255/46 , C07C2601/16 , C07D311/74 , C07D317/26 , C07D493/10 , C07F7/1804 , C07J21/003 , C07J41/0055 , C07J41/0094 , C07J53/001 , C07J71/0005
摘要： This invention provides novel compounds comprising the following anti-inflammatory pharmacore: wherein X, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
摘要翻译： 本发明提供包含以下抗炎药物的新化合物：其中X，R 1和R 2在本文中定义。 还提供了包含这种化合物的药物组合物，试剂盒和制品，用于制备化合物的方法和中间体，以及使用该化合物和组合物的方法。
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公开(公告)号：US20100048887A1
公开(公告)日：2010-02-25
申请号：US12426889
申请日：2009-04-20
申请人： Eric Anderson , Gary L. Bolton , Deborah A. Ferguson , Xin Jiang , Robert M. Kral, JR. , Patrick M. O'Brien , Melean Visnick
发明人： Eric Anderson , Gary L. Bolton , Deborah A. Ferguson , Xin Jiang , Robert M. Kral, JR. , Patrick M. O'Brien , Melean Visnick
IPC分类号： C07J21/00 , C07C49/203 , C07D317/10 , C07F7/02 , C07C39/205 , C07C49/603 , C07D311/02 , C07J71/00 , C07J1/00 , C07J51/00
CPC分类号： C07C255/46 , C07C2601/16 , C07D311/74 , C07D317/26 , C07D493/10 , C07F7/1804 , C07J21/003 , C07J41/0055 , C07J41/0094 , C07J53/001 , C07J71/0005
摘要： This invention provides novel compounds comprising the following anti-inflammatory pharmacore: wherein X, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
摘要翻译： 本发明提供包含以下抗炎药物的新化合物：其中X，R 1和R 2在本文中定义。 还提供了包含这种化合物的药物组合物，试剂盒和制品，用于制备化合物的方法和中间体，以及使用该化合物和组合物的方法。
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公开(公告)号：US06306959B1
公开(公告)日：2001-10-23
申请号：US09171258
申请日：1998-10-15
申请人： Gary L. Bolton , Richard J. Booth , Mark W. Creswell , John C. Hodges , Joseph S. Warmus , Michael W. Wilson
发明人： Gary L. Bolton , Richard J. Booth , Mark W. Creswell , John C. Hodges , Joseph S. Warmus , Michael W. Wilson
IPC分类号： C08G6348
CPC分类号： C07D295/215 , B01J20/265 , C07B2200/11 , C07C231/24 , C07C273/189 , C08F8/00 , C08F8/10 , C08F8/26 , C08F8/30 , C08F8/32 , C08F8/34 , C08F8/36 , C08F8/42 , C08F8/48 , C08F2810/20 , C08G85/00 , C40B40/04 , C40B50/08 , C40B99/00 , Y10S530/81 , Y10S530/815 , Y10S530/816 , Y10S530/817 , C08F212/08
摘要： Novel polymer-supported quenching reagents of Formula (I): P-L-Q, wherein P is a polymer of low chemical reactivity which is soluble or insoluble; Q is one or more quenching reagents, or an acid or base addition salts thereof, that are capable of selective covalent reaction with unwanted byproducts, or excess reagents; and L is one or more chemically robust linkers that join P and Q; are described, as well as methods for their preparation and methods for their use in the rapid purification of synthetic intermediates and products in organic synthesis, combinatorial chemistry and automated organic synthesis.
摘要翻译： 式（I）的新型聚合物支持的猝灭试剂：P-L-Q，其中P是可溶或不溶性的化学反应性低的聚合物; Q是能够与不想要的副产物或过量试剂选择性共价反应的一种或多种猝灭试剂或其酸或碱加成盐; L是连接P和Q的一个或多个化学稳定的接头; 以及其制备方法及其用于快速纯化有机合成，组合化学和自动化有机合成中的合成中间体和产物的方法。
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公开(公告)号：US08513436B2
公开(公告)日：2013-08-20
申请号：US13330378
申请日：2011-12-19
申请人： Eric Anderson , Gary L. Bolton , Bradley Caprathe , Xin Jiang , Chitase Lee , William H. Roark , Melean Visnick
发明人： Eric Anderson , Gary L. Bolton , Bradley Caprathe , Xin Jiang , Chitase Lee , William H. Roark , Melean Visnick
IPC分类号： C07D487/00 , C07D239/70 , C07D271/06 , C07D271/10 , C07D261/02 , C07D257/04
CPC分类号： C07C255/47 , C07D231/54 , C07D239/70 , C07D401/04 , C07D403/04 , C07D413/04 , C07D417/04 , C07D487/04
摘要： Disclosed herein are novel antioxidant inflammation modulators, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds and compositions thereof are also provided.
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公开(公告)号：US20120283450A1
公开(公告)日：2012-11-08
申请号：US13552530
申请日：2012-07-18
申请人： Eric Anderson , Gary L. Bolton , Deborah A. Ferguson , Xin Jiang , Robert M. Kral, JR. , Patrick M. O'Brien , Melean Visnick
发明人： Eric Anderson , Gary L. Bolton , Deborah A. Ferguson , Xin Jiang , Robert M. Kral, JR. , Patrick M. O'Brien , Melean Visnick
IPC分类号： C07C255/46 , C07F7/10 , C07J21/00 , C07J71/00 , C07J41/00 , C07D317/30 , C07D311/62
CPC分类号： C07C255/46 , C07C2601/16 , C07D311/74 , C07D317/26 , C07D493/10 , C07F7/1804 , C07J21/003 , C07J41/0055 , C07J41/0094 , C07J53/001 , C07J71/0005
摘要： This invention provides novel compounds comprising the following anti-inflammatory pharmacore: wherein X, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
摘要翻译： 本发明提供包含以下抗炎药物的新化合物：其中X，R 1和R 2在本文中定义。 还提供了包含这种化合物的药物组合物，试剂盒和制品，用于制备化合物的方法和中间体，以及使用该化合物和组合物的方法。
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8.发明授权Dehydroandrosterone analogs including an anti-inflammatory pharmacore and methods of use 有权脱氢雄甾酮类似物，包括抗炎药物及其使用方法公开(公告)号：US08258329B2
公开(公告)日：2012-09-04
申请号：US12426889
申请日：2009-04-20
申请人： Eric Anderson , Gary L. Bolton , Deborah A. Ferguson , Xin Jiang , Robert M. Kral, Jr. , Patrick M. O'Brien , Melean Visnick
发明人： Eric Anderson , Gary L. Bolton , Deborah A. Ferguson , Xin Jiang , Robert M. Kral, Jr. , Patrick M. O'Brien , Melean Visnick
CPC分类号： C07C255/46 , C07C2601/16 , C07D311/74 , C07D317/26 , C07D493/10 , C07F7/1804 , C07J21/003 , C07J41/0055 , C07J41/0094 , C07J53/001 , C07J71/0005
摘要： This invention provides novel compounds comprising the following anti-inflammatory pharmacore: wherein X, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
摘要翻译： 本发明提供包含以下抗炎药物的新化合物：其中X，R 1和R 2在本文中定义。 还提供了包含这种化合物的药物组合物，试剂盒和制品，用于制备化合物的方法和中间体，以及使用该化合物和组合物的方法。
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9.发明申请PYRAZOLYL AND PYRIMIDINYL TRICYCLIC ENONES AS ANTIOXIDANT INFLAMMATION MODULATORS 有权作为抗氧化剂炎症调节剂的吡唑并吡啶并吡啶二酮公开(公告)号：US20120196880A1
公开(公告)日：2012-08-02
申请号：US13330378
申请日：2011-12-19
申请人： Eric Anderson , Gary L. Bolton , Bradley Caprathe , Xin Jiang , Chitase Lee , William H. Roark , Melean Visnick
发明人： Eric Anderson , Gary L. Bolton , Bradley Caprathe , Xin Jiang , Chitase Lee , William H. Roark , Melean Visnick
IPC分类号： A61K31/416 , C07D401/04 , A61K31/4439 , C07D471/04 , A61P29/00 , C07D239/70 , A61K31/517 , C07D487/04 , A61P9/10 , C07D231/54 , A61K31/437
CPC分类号： C07C255/47 , C07D231/54 , C07D239/70 , C07D401/04 , C07D403/04 , C07D413/04 , C07D417/04 , C07D487/04
摘要： Disclosed herein are novel antioxidant inflammation modulators, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds and compositions thereof are also provided.
摘要翻译： 本文公开了新型抗氧化剂炎症调节剂，包括下式的那些：其中变量在本文中定义。 还提供了包含这些化合物的药物组合物，试剂盒和制品。 还提供了可用于制备化合物的方法和中间体，以及使用该化合物及其组合物的方法。
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公开(公告)号：US06506701B1
公开(公告)日：2003-01-14
申请号：US09804860
申请日：2001-03-13
申请人： Gary L. Bolton , Richard J. Booth , Mark W. Creswell , John C. Hodges , Joseph S. Warmus , Michael W. Wilson
发明人： Gary L. Bolton , Richard J. Booth , Mark W. Creswell , John C. Hodges , Joseph S. Warmus , Michael W. Wilson
IPC分类号： B01J2034
CPC分类号： C07D295/215 , B01J20/265 , C07B2200/11 , C07C231/24 , C07C273/189 , C08F8/00 , C08F8/10 , C08F8/26 , C08F8/30 , C08F8/32 , C08F8/34 , C08F8/36 , C08F8/42 , C08F8/48 , C08F2810/20 , C08G85/00 , C40B40/04 , C40B50/08 , C40B99/00 , Y10S530/81 , Y10S530/815 , Y10S530/816 , Y10S530/817 , C08F212/08
摘要： Novel polymer-supported quenching reagents of Formula I, P—L—Q I wherein P is a polymer of low chemical reactivity which is soluble or insoluble; Q is one or more quenching reagents, or an acid or base addition salts thereof, that are capable of selective covalent reaction with unwanted byproducts, or excess reagents; and L is one or more chemically robust linkers that join P and Q; are described, as well as methods for their preparation and methods for their use in the rapid purification of synthetic intermediates and products in organic synthesis, combinatorial chemistry and automated organic synthesis.
摘要翻译： 式I的新型聚合物支持的猝灭试剂，其中P是可溶或不溶的低化学反应性的聚合物; Q是一种或多种猝灭试剂或其酸或碱加成盐，其能够与不想要的 副产物或多余试剂; 和L是连接P和Q的一种或多种化学稳定的接头;其描述及其制备方法及其用于快速纯化有机合成，组合化学和自动化有机合成中的合成中间体和产物的方法。
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