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21. 发明授权

US06436967B1 Process for preparing prodrugs of benzenesulfonamide-containing cox-2 inhibitors 有权
标题翻译：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。

22. 发明授权

US07037941B2 Alpha-and Beta-amino acid hydroxyethylamino sulfamic acid derivatives useful as retroviral protease inhibitors 失效
标题翻译：可用作逆转录病毒蛋白酶抑制剂的α-和β-氨基酸羟乙基氨基氨基磺酸衍生物
公开(公告)号：US07037941B2
公开(公告)日：2006-05-02
申请号：US10178956
申请日：2002-06-25
申请人： Michael L Vazquez , Richard A Mueller , John J Talley , Daniel P Getman , Gary A DeCrescenzo , Eric T Sun
发明人： Michael L Vazquez , Richard A Mueller , John J Talley , Daniel P Getman , Gary A DeCrescenzo , Eric T Sun
IPC分类号： A61K31/18 , C07C331/02
CPC分类号： C07D295/26 , A61K38/00 , C07C307/06 , C07C2601/14 , C07D215/48 , C07D303/36 , C07D401/12 , C07K5/06026 , C07K5/06139
摘要： Certain Alpha- and Beta-amino acid hydroxyethylamino sulfamic acid derivatives represented by the following formula are useful as retroviral protease inhibitors:
摘要翻译：由下式表示的某些α-和β-氨基酸羟乙氨基氨基磺酸衍生物可用作逆转录病毒蛋白酶抑制剂：

23. 发明授权

US06444678B1 &agr;- and &bgr;-amino acid hydroxyethylamino sulfamic acid derivatives useful as retroviral protease inhibitors 失效
标题翻译：可用作逆转录病毒蛋白酶抑制剂的α-和β-氨基酸羟乙基氨基氨基磺酸衍生物
公开(公告)号：US06444678B1
公开(公告)日：2002-09-03
申请号：US09633063
申请日：2000-08-04
申请人： Michael L Vazquez , Richard A Mueller , John J Talley , Daniel P Getman , Gary A DeCrescenzo , Eric T Sun
发明人： Michael L Vazquez , Richard A Mueller , John J Talley , Daniel P Getman , Gary A DeCrescenzo , Eric T Sun
IPC分类号： A61K31495
CPC分类号： C07D295/26 , A61K38/00 , C07C307/06 , C07C2601/14 , C07D215/48 , C07D303/36 , C07D401/12 , C07K5/06026 , C07K5/06139
摘要： Certain Alpha- and Beta-amino acid hydroxyethylamino sulfamic acid derivatives represented by the following formula are useful as retroviral protease inhibitors:
摘要翻译：由下式表示的某些α-和β-氨基酸羟乙氨基氨基磺酸衍生物可用作逆转录病毒蛋白酶抑制剂：

24. 发明授权

US07135489B2 Crystalline form of 4-[5-methyl-3-phenylisoxazol-4-yl] benzenesulfonamide 失效
公开(公告)号：US07135489B2
公开(公告)日：2006-11-14
申请号：US10205732
申请日：2002-07-26
申请人： John J Talley , John R Medich , Kathleen T McLaughlin , Henry T Gaud , Edward E Yonan
发明人： John J Talley , John R Medich , Kathleen T McLaughlin , Henry T Gaud , Edward E Yonan
IPC分类号： A61K31/42 , C07D261/08
CPC分类号： H01L23/4006 , C07D261/08 , H01L23/427 , H01L2924/0002 , H01L2924/00
摘要： A stable crystalline form of 4-[5-methyl-3-phenylisoxazol-4-yl]benzenesulfonamide is described. This crystal structure, designated Form B, is more stable, has favorable handling properties and is characterized by its melting point, x-ray and other physical characterizations.

25. 发明授权

US06156768A Alpha- and beta-amino acid hydroxyethylamino sulfamic acid derivatives useful as retroviral protease inhibitors 失效
标题翻译：可用作逆转录病毒蛋白酶抑制剂的α-氨基酸和β-氨基酸羟基氨基氨基磺酸衍生物
公开(公告)号：US06156768A
公开(公告)日：2000-12-05
申请号：US379545
申请日：1995-02-02
申请人： Michael L Vazquez , Richard A Mueller , John J Talley , Daniel P Getman , Gary A DeCrescenzo , Eric T Sun
发明人： Michael L Vazquez , Richard A Mueller , John J Talley , Daniel P Getman , Gary A DeCrescenzo , Eric T Sun
IPC分类号： A61K31/16 , A61K31/195 , A61K31/40 , A61K38/00 , C07C307/06 , C07D215/48 , C07D295/26 , C07K5/06 , C07K5/078 , C07D401/12 , A61K31/4709
CPC分类号： C07D295/26 , C07C307/06 , C07D215/48 , C07D303/36 , C07D401/12 , C07K5/06026 , C07K5/06139 , A61K38/00 , C07C2101/14
摘要： Certain Alpha- and Beta-amino acid hydroxyethylamino sulfamic acid derivatives represented by the following formula are useful as retroviral protease inhibitors: ##STR1##
摘要翻译： PCT No.PCT / US93 / 10552 Sec。 371日期：1995年2月2日 102（e）1995年2月2日PCT PCT 1993年10月29日PCT公布。公开号WO94 / 10134 日期1994年5月11日由下式表示的α-和β-氨基酸羟乙氨基氨基磺酸衍生物可用作逆转录病毒蛋白酶抑制剂：

26. 发明授权

US6045773A Method of detecting cyclooxygenase-2 失效
标题翻译：环氧合酶-2检测方法
公开(公告)号：US6045773A
公开(公告)日：2000-04-04
申请号：US256739
申请日：1999-02-24
申请人： Peter C Isakson , Karen Seibert , John J Talley
发明人： Peter C Isakson , Karen Seibert , John J Talley
IPC分类号： C07D231/12 , A61K31/415 , A61K31/42 , A61K31/421 , A61K49/06 , A61K51/00 , A61K51/04 , C07D261/08 , C07D263/32
CPC分类号： A61K49/06 , A61K51/04 , A61K51/0453 , A61K51/0455 , A61K2123/00
摘要： The invention relates to a method of detecting concentrations of cyclooxygenase-2 in a mammal, the method comprising: administering to the mammal a diagnostically effective amount of a cyclooxygenase-2 selective agent, which is capable of being detected in vivo; and b) detecting the agent so the concentration of cyclooxygenase-2 is detected.
摘要翻译：本发明涉及一种检测哺乳动物环氧合酶-2浓度的方法，该方法包括：向哺乳动物施用能够在体内检测的诊断有效量的环加氧酶-2选择剂; b）检测试剂，检测环氧合酶-2的浓度。

27. 发明授权

US06441014B2 Crystalline form of 4-[5-methyl-3-phenylisoxazol-4-yl] benzenesulfonamide 失效
标题翻译：结晶形式的4- [5-甲基-3-苯基异恶唑-4-基]苯磺酰胺
公开(公告)号：US06441014B2
公开(公告)日：2002-08-27
申请号：US09741213
申请日：2000-12-19
申请人： John J Talley , John R Medich , Kathleen T McLaughlin , Henry T Gaud , Edward E Yonan
发明人： John J Talley , John R Medich , Kathleen T McLaughlin , Henry T Gaud , Edward E Yonan
IPC分类号： A61K3142
CPC分类号： H01L23/4006 , C07D261/08 , H01L23/427 , H01L2924/0002 , H01L2924/00
摘要： A stable crystalline form of 4-[5-methyl-3-phenylisoxazol-4-yl]benzenesulfonamide is described. This crystal structure, designated Form B, is more stable, has favorable handling properties and is characterized by its melting point, x-ray and other physical characterizations.
摘要翻译：描述了4- [5-甲基-3-苯基异恶唑-4-基]苯磺酰胺的稳定结晶形式。这种晶体结构称为B型，更稳定，具有良好的操作性能，其特点是熔点，X射线等物理特性。

28. 发明授权

US6028072A 3,4-substituted pyrazoles for the treatment of inflammation 失效
公开(公告)号：US6028072A
公开(公告)日：2000-02-22
申请号：US776090
申请日：1997-06-09
申请人： Len F Lee , Thomas D Penning , Steven W Kramer , John J Talley
发明人： Len F Lee , Thomas D Penning , Steven W Kramer , John J Talley
IPC分类号： A61K31/415 , A61K31/44 , A61K31/4427 , A61K31/47 , A61K31/505 , A61P19/02 , A61P25/04 , A61P29/00 , C07D231/12 , C07D401/04 , C07D401/14 , C07D403/04 , A01N43/54 , C07D231/00 , C07D231/02 , C07D401/00
CPC分类号： C07D231/12
摘要： A class of pyrazolyl 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 is selected from hydrido, C.sub.1 -C.sub.20 -alkyl, C.sub.2 -C.sub.20 -alkenyl, C.sub.2 -C.sub.20 -alkynyl, C.sub.1 -C.sub.20 -haloalkyl, aryl-C.sub.1 -C.sub.20 -alkyl, heterocyclic-C.sub.1 -C.sub.20 -alkyl, heteroaryl-C.sub.1 -C.sub.20 -alkyl, C.sub.1 -C.sub.20 -hydroxyalkyl, C.sub.1 -C.sub.10 -alkoxyalkyl, C.sub.1 -C.sub.20 -cyanoalkyl, C.sub.1 -C.sub.20 -aminoalkyl, C.sub.1 -C.sub.20 -alkylamino-C.sub.1 -C.sub.20 -alkyl, carboxy-C.sub.1 -C.sub.20 -alkyl, C.sub.1 -C.sub.20 -alkoxycarbonyl-C.sub.1 -C.sub.20 -alkyl, C.sub.1 -C.sub.20 -alkylaminocarbonyl-C.sub.1 -C.sub.20 -alkyl, N-hydroxyaminocarbonyl-C.sub.1 -C.sub.20 -alkyl, N-hydroxy-N-C.sub.1 -C.sub.20 -alkyl-aminocarbonyl-C.sub.1 -C.sub.20 -alkyl, arylaminocarbonyl-C.sub.1 -C.sub.20 -alkyl and aminocarbonyl-C.sub.1 -C.sub.20 -alkyl;wherein R.sup.2 is aryl substituted at a substitutable position with a radical selected from C.sub.1 -C.sub.20 -alkylsulfonyl and aminosulfonyl;wherein R.sup.3 is heteroaryl, wherein R.sup.3 is optionally substituted at a substitutable position with one or more radicals independently selected from halo, C.sub.1 -C.sub.10 -alkylthio, C.sub.1 -C.sub.10 -alkylsulfinyl, C.sub.1 -C.sub.20 -alkyl, cyano, carboxyl, C.sub.1 -C.sub.10 -alkoxycarbonyl, aminocarbonyl, C.sub.1 -C.sub.20 -alkylaminocarbonyl, arylaminocarbonyl, N-C.sub.1 -C.sub.20 -alkyl-N-arylaminocarbonyl, C.sub.1 -C.sub.20 -haloalkyl, hydroxyl, C.sub.1 -C.sub.10 -alkoxy, C.sub.1 -C.sub.20 -hydroxyalkyl, C.sub.1 -C.sub.10 -haloalkoxy, amino, C.sub.1 -C.sub.20 -alkylamino, arylamino, heterocyclo and nitro; andwherein R.sup.4 is selected from hydrido, C.sub.1 -C.sub.20 -alkyl, C.sub.1 -C.sub.20 -haloalkyl, cyano, acyl, C.sub.1 -C.sub.10 -alkoxy, carboxyl, carboxy-C.sub.1 -C.sub.20 -alkyl, C.sub.1 -C.sub.10 -alkoxycarbonyl, C.sub.1 -C.sub.10 -alkoxycarbonyl-C.sub.1 -C.sub.20 -alkyl, aryl-C.sub.1 -C.sub.10 -alkoxycarbonyl-C.sub.1 -C.sub.20 -alkyl, aminocarbonyl, C.sub.1 -C.sub.20 -alkylaminocarbonyl, arylaminocarbonyl, N-C.sub.1 -C.sub.20 -alkyl-N-arylaminocarbonyl, aminocarbonyl-C.sub.1 -C.sub.20 -alkyl, C.sub.1 -C.sub.20 -hydroxyalkyl and aryl-C.sub.1 -C.sub.10 -alkoxyalkyl;or a pharmaceutically-acceptable salt thereof.

29. 发明授权

US5985902A Substituted isoxazole for the treatment of inflammation 失效
标题翻译：取代的异恶唑用于治疗炎症
公开(公告)号：US5985902A
公开(公告)日：1999-11-16
申请号：US801768
申请日：1997-02-18
申请人： John J Talley , Srinivasan Nagarajan , Roland S Rogers
发明人： John J Talley , Srinivasan Nagarajan , Roland S Rogers
IPC分类号： A61K31/42 , A61K31/4439 , A61P1/00 , A61P1/02 , A61P1/04 , A61P3/10 , A61P7/00 , A61P7/06 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/12 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/06 , A61P19/08 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/12 , A61P35/00 , A61P37/00 , A61P43/00 , C07D261/08 , C07D261/10 , C07D261/12 , C07D261/18 , C07D413/04 , A61K31/44 , C07D413/06 , C07D413/12
CPC分类号： C07D261/10 , C07D261/08 , C07D261/12 , C07D261/18 , C07D413/04
摘要： A class of substituted isoxazolyl 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 hydroxyl, lower alkyl, carboxyl, lower carboxyalkyl, lower aminocarbonylalkyl, lower alkoxycarbonylalkyl, lower aralkyl, lower alkoxyalkyl, lower aralkoxyalkyl, lower alkylthioalkyl, lower aralkylthioalkyl, lower alkylaminoalkyl, lower aryloxyalkyl, lower arylthioalkyl, lower haloalkyl, lower hydroxylalkyl, cycloalkyl, cycloalkylalkyl, and aralkyl; wherein R.sup.3 is selected from cycloalkyl, cycloalkenyl, aryl, and heteroaryl; wherein R.sup.3 is optionally substituted at a substitutable position with one or more radicals independently selected from lower alkylsulfinyl, lower alkyl, cyano, carboxyl, lower alkoxycarbonyl, lower haloalkyl, hydroxyl, lower hydroxyalkyl, lower haloalkoxy, amino, lower alkylamino, lower arylamino, lower aminoalkyl, nitro, halo, lower alkoxy, aminosulfonyl, and lower alkylthio; and wherein R.sup.4 is selected from lower alkyl, hydroxyl and amino; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类用于治疗炎症和炎症相关疾病的取代的异恶唑基化合物。特别感兴趣的化合物由式II定义，其中R1选自羟基，低级烷基，羧基，低级羧基烷基，低级氨基羰基烷基，低级烷氧基羰基烷基，低级芳烷基，低级烷氧基烷基，低级芳烷氧基烷基，低级烷硫基烷基，低级芳烷硫基烷基，低级烷基氨基烷基，低级芳氧基烷基低级芳基硫代烷基，低级卤代烷基，低级羟基烷基，环烷基，环烷基烷基和芳烷基; 其中R 3选自环烷基，环烯基，芳基和杂芳基; 其中R 3在可取代的位置任选被一个或多个独立地选自低级烷基亚磺酰基，低级烷基，氰基，羧基，低级烷氧基羰基，低级卤代烷基，羟基，低级羟烷基，低级卤代烷氧基，氨基，低级烷基氨基，低级芳基氨基，低级氨基烷基，硝基，卤素，低级烷氧基，氨基磺酰基和低级烷硫基; 并且其中R 4选自低级烷基，羟基和氨基; 或其药学上可接受的盐。

30. 发明授权

US5908852A 1,3,5 trisubstituted pyrazole compounds for treatment of inflammation 失效
标题翻译：用于治疗炎症的1,3,5三取代吡唑化合物
公开(公告)号：US5908852A
公开(公告)日：1999-06-01
申请号：US647911
申请日：1996-05-30
申请人： John J Talley , Donald J Rogier, Jr. , Thomas D. Penning , Stella S Yu
发明人： John J Talley , Donald J Rogier, Jr. , Thomas D. Penning , Stella S Yu
IPC分类号： C07D231/12 , C07D231/16 , A61K31/415 , C07D405/04 , C07D405/09
CPC分类号： C07D231/12 , C07D231/16
摘要： A class of 1,3,5-substituted pyrazoles is described for the treatment of inflammation, including treatment of pain and disorders such as arthritis. Compounds of particular interest are of Formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as described herein; or a pharmaceutically-acceptable salt thereof.
摘要翻译： PCT No.PCT / US94 / 12722 Sec。 371日期：1996年5月30日 102（e）日期1996年5月30日PCT 1994年11月14日PCT PCT。 WO95 / 15318 PCT公开号日期：1995年6月8日描述了一类1,3,5-取代的吡唑用于治疗炎症，包括治疗疼痛和疾病如关节炎。特别感兴趣的化合物是式I，其中R 1，R 2，R 3和R 4如本文所述; 或其药学上可接受的盐。

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