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公开(公告)号：US06525059B1
公开(公告)日：2003-02-25
申请号：US09513351
申请日：2000-02-24
申请人： Ashok Anantanarayan , Michael Clare , Paul W. Collins , Joyce Zuowu Crich , Rajesh Devraj , Daniel L. Flynn , Lifeng Geng , Matthew J. Graneto , Cathleen E. Hanau , Gunnar J. Hanson , Susan J. Hartmann , Michael Hepperle , He Huang , Francis J. Koszyk , Shuyuan Liao , Suzanne Metz , Richard A. Partis , Thao D. Perry , Shashidhar N. Rao , Shaun Raj Selness , Michael S. South , Michael A. Stealey , John Jeffrey Talley , Michael L. Vazquez , Richard M. Weier , Xiangdong Xu , Ish K. Khanna , Yi Yu
发明人： Ashok Anantanarayan , Michael Clare , Paul W. Collins , Joyce Zuowu Crich , Rajesh Devraj , Daniel L. Flynn , Lifeng Geng , Matthew J. Graneto , Cathleen E. Hanau , Gunnar J. Hanson , Susan J. Hartmann , Michael Hepperle , He Huang , Francis J. Koszyk , Shuyuan Liao , Suzanne Metz , Richard A. Partis , Thao D. Perry , Shashidhar N. Rao , Shaun Raj Selness , Michael S. South , Michael A. Stealey , John Jeffrey Talley , Michael L. Vazquez , Richard M. Weier , Xiangdong Xu , Ish K. Khanna , Yi Yu
IPC分类号： A61K31506
CPC分类号： C07D409/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D413/14 , C07D417/14 , C07D453/02 , C07D471/04 , C07D473/00 , C07D487/04
摘要： A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA wherein R1, R 2, R3 and R4 are as described in the specification.
摘要翻译： 描述了一类吡唑衍生物用于治疗p38激酶介导的病症。 特别感兴趣的化合物由式IA定义，其中R 1，R 2，R 3和R 4如说明书中所述。
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公开(公告)号：US06509361B1
公开(公告)日：2003-01-21
申请号：US09674653
申请日：2001-02-12
IPC分类号： A61K314439
CPC分类号： C07D231/12 , C07D401/04 , C07D401/14
摘要： The present invention contemplates 1,5-diaryl-substituted pyrazole compounds that, inter alia, inhibit the activity of p38 MAP kinase. Also contemplated by the invention are processes for the preparation of the contemplated compounds and for the use of a contemplated compound in treating a mammalian host having a p38 kinase- or TNF-mediated disease.
摘要翻译： 本发明考虑了1,5-二芳基取代的吡唑化合物，其特别是抑制p38MAP激酶的活性。 本发明还考虑了制备预期化合物的方法，以及用于预期化合物治疗具有p38激酶或TNF介导的疾病的哺乳动物宿主的方法。
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33.发明授权Process for preparing prodrugs of benzenesulfonamide-containing cox-2 inhibitors 有权制备含苯磺酰胺的cox-2抑制剂的前药的方法公开(公告)号：US06436967B1
公开(公告)日：2002-08-20
申请号：US09661859
申请日：2000-09-14
申请人： John J Talley , James W Malecha , Stephen Bertenshaw , Matthew J Graneto , Jeffery Carter , Jinglin Li , Srinivasan Nagarajan , David L Brown , Donald J Rogier, Jr. , Thomas D Penning , Ish K Khanna , Xiangdong Xu , Richard M Weier
发明人： John J Talley , James W Malecha , Stephen Bertenshaw , Matthew J Graneto , Jeffery Carter , Jinglin Li , Srinivasan Nagarajan , David L Brown , Donald J Rogier, Jr. , Thomas D Penning , Ish K Khanna , Xiangdong Xu , Richard M Weier
IPC分类号： A61K3144
CPC分类号： C07D207/33 , A61K31/18 , A61K31/415 , A61K31/42 , A61K31/635 , C07C311/16 , C07C311/51 , C07C2601/10 , C07D231/12 , C07D233/64 , C07D261/08 , C07D263/32 , C07D307/58 , C07D401/04 , C07D417/04 , C07D495/04
摘要： This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to prodrugs of compounds which selectively inhibit cyclooxygenase-2. The use of non-steroidal antiinflammatory drugs (NSAIDs) in treating pain and the swelling associated with inflammation also produce severe side effects, including life threatening ulcers. The recent discovery of an inducible enzyme associated with inflammation (“prostaglandin G/H synthase II” or “cyclooxygenase-2 (COX-2)”) provides a viable target of inhibition which more effectively reduces inflammation and produces fewer and less drastic side effects.
摘要翻译： 本发明涉及抗炎药物领域，具体涉及选择性抑制环加氧酶-2的化合物的前药。非甾体抗炎药（NSAID）在治疗疼痛和与炎症有关的肿胀中的应用也产生严重的副作用， 包括危及生命的溃疡。 最近发现与炎症相关的可诱导酶（“前列腺素G / H合酶II”或“环加氧酶-2（COX-2）”）提供了可行的抑制靶标，其更有效地减少炎症并产生越来越少的副作用 。
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公开(公告)号：US06342608B1
公开(公告)日：2002-01-29
申请号：US09772743
申请日：2001-01-30
申请人： Michael L. Vazquez , Susan J. Hartmann , Suzanne Metz , John J. Talley , David L. Brown , Richard M. Weier , Michael A. Stealey , Xiaodong Xu
发明人： Michael L. Vazquez , Susan J. Hartmann , Suzanne Metz , John J. Talley , David L. Brown , Richard M. Weier , Michael A. Stealey , Xiaodong Xu
IPC分类号： C07D23120
CPC分类号： C07D401/14 , C07D231/18 , C07D339/00 , C07D401/04 , C07D405/14 , C07D409/06
摘要： This invention relates to a novel process of preparing selected 5-substituted pyrazoles useful as p38 kinase and COX-2 inhibitors.
摘要翻译： 本发明涉及制备用作p38激酶和COX-2抑制剂的选择的5-取代的吡唑的新方法。
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公开(公告)号：US06242612B1
公开(公告)日：2001-06-05
申请号：US09633726
申请日：2000-08-07
申请人： Matthew J. Graneto , Michael L. Vazquez , Susan J. Hartmann , Suzanne Metz , John J. Talley , David L. Brown , Richard M. Weier , Michael A. Stealey , Xiangdong Xu
发明人： Matthew J. Graneto , Michael L. Vazquez , Susan J. Hartmann , Suzanne Metz , John J. Talley , David L. Brown , Richard M. Weier , Michael A. Stealey , Xiangdong Xu
IPC分类号： C07D23120
CPC分类号： C07D401/14 , C07D231/18 , C07D339/00 , C07D401/04 , C07D405/14 , C07D409/06
摘要： This invention relates to a novel process of preparing selected 5-substituted pyrazoles useful as p38 kinase and COX-2 inhibitors.
摘要翻译： 本发明涉及制备用作p38激酶和COX-2抑制剂的选择的5-取代的吡唑的新方法。
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公开(公告)号：US5686470A
公开(公告)日：1997-11-11
申请号：US387150
申请日：1995-02-10
IPC分类号： C07D213/61 , C07D213/64 , C07D213/70 , C07D213/76 , C07D213/82 , C07D213/85 , A61K31/44 , C07D401/04 , C07D405/10
CPC分类号： C07D213/64 , C07D213/61 , C07D213/70 , C07D213/76 , C07D213/82 , C07D213/85
摘要： A class of substituted pyridyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II ##STR1## wherein R.sup.1 is selected from hydrido, halo, alkoxy, haloalkoxy, aryl, alkylthio, alkylamino, aralkoxy, azido and allyloxy; wherein R.sup.2 is selected from hydrido, cyano, hydroxyalkyl, haloalkyl, aminoalkyl, aminocarbonyl and alkylcarbonylaminoalkyl; and wherein R.sup.5 and R.sup.6 are one or more radicals independently selected from halo, alkylsulfonyl, aminosulfonyl, alkoxy and alkylthio; provided one of R.sup.5 and R.sup.6 is substituted with alkylsulfonyl, aminosulfonyl, or haloalkylsulfonyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译： 描述了一类取代的吡啶基化合物用于治疗炎症和炎症相关疾病。 特别感兴趣的化合物由式II（II）定义，其中R 1选自氢，卤素，烷氧基，卤代烷氧基，芳基，烷硫基，烷基氨基，芳烷氧基，叠氮基和烯丙氧基; 氰基，羟基烷基，卤代烷基，氨基烷基，氨基羰基和烷基羰基氨基烷基; 并且其中R 5和R 6是一个或多个独立地选自卤素，烷基磺酰基，氨基磺酰基，烷氧基和烷硫基的基团; 其中R5和R6之一被烷基磺酰基，氨基磺酰基或卤代烷基磺酰基取代; 或其药学上可接受的盐。
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公开(公告)号：US5637707A
公开(公告)日：1997-06-10
申请号：US658775
申请日：1996-06-05
IPC分类号： A61K31/435 , A61K31/436 , A61K31/445 , A61K31/451 , A61P31/12 , A61P31/14 , C07D211/46 , C07D491/04 , C07D491/056 , C07D491/20 , C07F7/18
CPC分类号： C07D491/04 , C07D211/46
摘要： Novel 2-alkyl carbinol derivatives of deoxynojirimycin (DNJ) and the chemical synthesis of these derivatives and intermediates therefor from DNJ and their method of inhibiting lentiviruses are disclosed.
摘要翻译： 公开了脱氧野尻霉素（DNJ）的新型2-烷基甲醇衍生物及其衍生物及其中间体的化学合成及其抑制慢病毒的方法。
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38.发明授权Heteroaralkyl and heteroarylthioalkyl thiophenolic compounds as 5-lipoxgenase inhibitors 失效杂芳基烷基和杂芳硫基烷基硫代酚化合物作为5-脂氧合酶抑制剂
公开(公告)号：US5635514A
公开(公告)日：1997-06-03
申请号：US328212
申请日：1994-10-25
IPC分类号： C07D209/08 , C07D215/22 , C07D215/227 , C07D235/06 , C07D263/58 , C07D471/04 , A61K31/44 , A61K31/47
CPC分类号： C07D215/227 , C07D209/08 , C07D235/06 , C07D263/58 , C07D471/04
摘要： Compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising a therapeutically-effective amount of the compounds or salts in combination with a pharmaceutically-acceptable carrier and methods for treating 5-lipoxygenase mediated conditions, inflammation-associated disorders and allergies.
摘要翻译： 式I化合物及其药学上可接受的盐，包含治疗有效量的化合物或盐与药学上可接受的载体组合的药物组合物和用于治疗5-脂氧合酶介导的病症的方法， 相关疾病和过敏。
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39.发明授权1,2-aryl and heteroaryl substituted imidazolyl compounds for the treatment of inflammation 失效用于治疗炎症的1,2-芳基和杂芳基取代的咪唑基化合物
公开(公告)号：US5616601A
公开(公告)日：1997-04-01
申请号：US464154
申请日：1995-06-05
申请人： Ish K. Khanna , Richard M. Weier , Paul W. Collins , Yi Yu , Xiangdong Xu , Richard A. Partis , Francis J. Koszyk
发明人： Ish K. Khanna , Richard M. Weier , Paul W. Collins , Yi Yu , Xiangdong Xu , Richard A. Partis , Francis J. Koszyk
IPC分类号： C07D233/30 , A61K31/415 , A61K31/4166 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61P25/04 , A61P29/00 , A61P43/00 , C07D233/32 , C07D233/54 , C07D233/64 , C07D233/90 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/04 , C07D409/04 , C07D419/04 , C07D213/53
CPC分类号： C07D233/64 , C07D233/32 , C07D233/90 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D419/04
摘要： A class of imidazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: ##STR1## wherein R.sup.1 -R.sup.6 are as described in the specification; or a pharmaceutically-acceptable salt thereof.
摘要翻译： 描述了一类咪唑基化合物用于治疗炎症和炎症相关疾病。 特别感兴趣的化合物由式I定义：其中R 1 -R 6如说明书中所述; 或其药学上可接受的盐。
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公开(公告)号：US5523406A
公开(公告)日：1996-06-04
申请号：US294296
申请日：1994-08-23
IPC分类号： A61K31/435 , A61K31/436 , A61K31/445 , A61K31/451 , A61P31/12 , A61P31/14 , C07D211/46 , C07D491/04 , C07D491/056 , C07D491/20 , C07F7/18 , C07D211/40 , C07D491/06
CPC分类号： C07D491/04 , C07D211/46
摘要： Novel 2-alkyl carbinol derivatives of deoxynojirimycin (DNJ) and the chemical synthesis of these derivatives and intermediates therefor from DNJ and their method of inhibiting lentiviruses are disclosed.
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