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81. 发明授权

US06384036B1 Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors 失效
标题翻译：双磺酰胺羟乙基氨基酸逆转录病毒蛋白酶抑制剂
公开(公告)号：US06384036B1
公开(公告)日：2002-05-07
申请号：US09635896
申请日：2000-08-11
申请人： John N. Freskos , Daniel P. Getman , John J. Talley , James A. Sikorski
发明人： John N. Freskos , Daniel P. Getman , John J. Talley , James A. Sikorski
IPC分类号： A61K3118
CPC分类号： C07C311/29 , C07D235/26 , C07D235/32 , C07D277/82 , C07D295/26 , C07D307/79 , C07D317/62 , C07D319/18 , C07D405/12
摘要： Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.
摘要翻译：双亚磺酰氨基羟乙基氨基化合物作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶的抑制剂。本发明涉及下式的逆转录病毒蛋白酶抑制化合物：或其药学上可接受的盐，前药或酯，其中变量如本文所定义。

82. 发明授权

US06342608B1 Process for making substituted pyrazoles 失效
标题翻译：制备取代的吡唑的方法
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。

83. 发明授权

US06242612B1 Process for making substituted pyrazoles 失效
标题翻译：制备取代的吡唑的方法
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。

85. 发明授权

US5965588A Sulfonylalkanoylamino hydroxyethylamimo sulfonamides useful as retroviral protease inhibitors 失效
标题翻译：用作逆转录病毒蛋白酶抑制剂的磺酰基烷酰氨基羟乙基咪唑磺酰胺
公开(公告)号：US5965588A
公开(公告)日：1999-10-12
申请号：US48034
申请日：1998-03-26
申请人： Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel Getman , Gary A. DeCrescenzo , John N. Freskos
发明人： Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel Getman , Gary A. DeCrescenzo , John N. Freskos
IPC分类号： A61K31/225 , A61K31/18 , A61K31/63 , A61P31/12 , C07C311/18 , C07C317/44 , C07C327/38 , C07D307/79 , C07D319/16 , A61K31/38 , A61K31/44
CPC分类号： A61K31/63 , A61K31/18 , C07C317/44
摘要： Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
摘要翻译：含磺酰胺的羟乙基胺化合物作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶的抑制剂。

86. 发明授权

US5753688A Substituted pyrazolyl benzenesulfonamides for the treatment of gastrointestinal conditions 失效
标题翻译：取代的吡唑基苯磺酰胺用于治疗胃肠道疾病
公开(公告)号：US5753688A
公开(公告)日：1998-05-19
申请号：US534757
申请日：1995-09-27
申请人： John J. Talley , Thomas D. Penning , Paul W. Collins , Donald J. Rogier, Jr. , James W. Malecha , Julie M. Miyashiro , Stephen R. Bertenshaw , Ish K. Khanna , Matthew J. Graneto , Roland S. Rogers , Jeffery S. Carter
发明人： John J. Talley , Thomas D. Penning , Paul W. Collins , Donald J. Rogier, Jr. , James W. Malecha , Julie M. Miyashiro , Stephen R. Bertenshaw , Ish K. Khanna , Matthew J. Graneto , Roland S. Rogers , Jeffery S. Carter
IPC分类号： A61K31/415 , A61K31/4155 , A61K31/416 , A61K31/4178 , A61K31/4245 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/505 , A61K31/506 , A61P5/14 , A61P9/00 , A61P19/02 , A61P25/04 , A61P25/06 , A61P29/00 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/18 , C07D231/54 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D495/04 , A61K31/63
CPC分类号： C07D495/04 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/54 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
摘要： A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: ##STR1## or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类吡唑基苯磺酰胺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（I）或其药学上可接受的盐。

87. 发明授权

US5703263A Process for making chiral alpha-amino phosphonates and selected novel chiral alpha-amino phosphonates 失效
公开(公告)号：US5703263A
公开(公告)日：1997-12-30
申请号：US408237
申请日：1995-03-22
申请人： John J. Talley
发明人： John J. Talley
IPC分类号： C07F9/38 , C07F9/40
CPC分类号： C07F9/4006 , C07F9/3808 , C07F9/4015
摘要： This invention is selected novel chiral (essentially pure) alpha-amino phosphonates, process for the preparation which is a catalytic asymmetric hydrogenation of olefins and novel intermediates therefor. The alpha-amino phosphonates are useful as antibiotics and/or as intermediates in the preparation of phosphorus-containing analogs of peptides, i.e., phosphonopeptides or pseudopeptides having known uses, such as in antibiotics, antibiotic enhancers, or enzyme inhibitors.

88. 发明授权

US5654462A Process for making chiral alpha-amino phosphonates and selected novel chiral alpha-amino phosphonates 失效
标题翻译：制备手性α-氨基膦酸酯和选定的新型手性α-氨基膦酸酯的方法
公开(公告)号：US5654462A
公开(公告)日：1997-08-05
申请号：US404006
申请日：1995-03-14
申请人： John J. Talley
发明人： John J. Talley
IPC分类号： C07F9/38 , C07F9/40
CPC分类号： C07F9/4006 , C07F9/3808 , C07F9/4015
摘要： This invention is selected novel chiral (essentially pure) alpha-amino phosphonates, process for the preparation which is a catalytic asymmetric hydrogenation of olefins and novel intermediates therefor. The alpha-amino phosphonates are useful as antibiotics and/or as intermediates in the preparation of phosphorus-containing analogs of peptides, i.e., phosphonopeptides or pseudopeptides having known uses, such as in antibiotics, antibiotic enhancers, or enzyme inhibitors.
摘要翻译：本发明选择新的手性（基本上纯的）α-氨基膦酸盐，其制备方法是烯烃的催化不对称氢化及其新型中间体。 α-氨基膦酸盐可用作制备含磷类似物的肽的抗生素和/或作为中间体，即具有已知用途的膦肽或假肽，例如抗生素，抗生素增强剂或酶抑制剂。

89. 发明授权

US5643924A Retroviral protease inhibitors 失效
公开(公告)号：US5643924A
公开(公告)日：1997-07-01
申请号：US455237
申请日：1995-05-31
申请人： John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , Kathryn L. Reed , Ko-Chung Lin , John Nicholas Freskos , Michael Clare , Donald Joseph Rogier, Jr. , Robert M. Heintz , Michael L. Vazquez , Richard A. Mueller
发明人： John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , Kathryn L. Reed , Ko-Chung Lin , John Nicholas Freskos , Michael Clare , Donald Joseph Rogier, Jr. , Robert M. Heintz , Michael L. Vazquez , Richard A. Mueller
IPC分类号： A61K31/40 , A61K31/4427 , A61K31/445 , A61K31/4468 , A61K31/47 , A61K31/472 , A61K38/55 , A61P31/12 , C07D207/16 , C07D211/60 , C07D217/26 , C07D241/04 , C07D401/12 , C07K5/06 , C07K14/81 , A61K31/44
CPC分类号： C07D401/12 , C07D207/16 , C07D211/60 , C07D217/26
摘要： N-heterocyclic moiety containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

90. 发明授权

US5565482A Heteroarylpyranopyrazolyl derivatives for the treatment of inflammation 失效
标题翻译：异芳基吡喃并吡唑衍生物用于治疗炎症
公开(公告)号：US5565482A
公开(公告)日：1996-10-15
申请号：US536925
申请日：1995-09-29
申请人： John J. Talley , Stephen R. Bertenshaw , Matthew J. Graneto , Donald J. Rogier
发明人： John J. Talley , Stephen R. Bertenshaw , Matthew J. Graneto , Donald J. Rogier
IPC分类号： C07D491/04 , C07D491/044 , C07D491/048 , C07D491/052 , C07D495/04 , A61K31/415 , C07D491/14
CPC分类号： C07D491/04 , C07D495/04
摘要： A class of benzopyranopyrazolyl derivatives is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein A is --(CH.sub.2).sub.m --X--(CH.sub.2).sub.n --; wherein X is S(O).sub.p or O; wherein m is 0 or 1; wherein n is 0 or 1; wherein p is 0 or 1; wherein B is selected from phenyl and five and six membered heteroaryl; wherein R.sup.1 is selected from lower haloalkyl, cyano, formyl, lower alkoxycarbonyl, lower alkoxy, lower N-alkylaminocarbonyl, N-phenylaminocarbonyl, lower N,N-dialkylaminocarbonyl and lower N-alkyl-N-phenylaminocarbonyl; wherein R.sup.2 is phenyl substituted at a substitutable position with a radical selected from lower alkylsulfonyl and sulfamyl; and wherein R.sup.4 is one or more radicals selected from hydrido, halo, lower alkylthio, lower alkylsulfinyl, lower alkyl, cyano, carboxyl, lower alkoxycarbonyl, aminocarbonyl, lower haloalkyl, hydroxyl, lower alkoxy, amino, lower N-alkylamino, lower N,N-dialkylamino, lower hydroxyalkyl and lower haloalkoxy; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类苯并吡喃并吡唑基衍生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（I）定义，其中A是 - （CH 2）m -X-（CH 2）n - ; 其中X是S（O）p或O; 其中m为0或1; 其中n为0或1; 其中p为0或1; 其中B选自苯基和五元和六元杂芳基; 其中R 1选自低级卤代烷基，氰基，甲酰基，低级烷氧基羰基，低级烷氧基，低级N-烷基氨基羰基，N-苯基氨基羰基，低级N，N-二烷基氨基羰基和低级N-烷基-N-苯基氨基羰基。其中R2是在可取代的位置被选自低级烷基磺酰基和氨磺酰基的基团取代的苯基; 氰基，羧基，低级烷氧基羰基，氨基羰基，低级卤代烷基，羟基，低级烷氧基，氨基，低级N-烷基氨基，低级N，低级烷基氨基，低级烷基氨基，低级烷基氨基， N-二烷基氨基，低级羟烷基和低级卤代烷氧基; 或其药学上可接受的盐。

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