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1.发明授权2-saccharinylmethyl aryl carboxylates useful as proteolytic enzyme inhibitors and compositions and method of use thereof 失效可用作蛋白水解酶抑制剂的2-糖基甲基芳基羧酸盐及其组合物及其使用方法
公开(公告)号：US5597841A
公开(公告)日：1997-01-28
申请号：US445118
申请日：1995-05-19
申请人： Richard P. Dunlap , Neil W. Boaz , Albert J. Mura , Virendra Kumar , Chakrapani Subramanyam , Ranjit C. Desai , Dennis J. Hlasta , Manohar T. Saindane , Malcolm R. Bell , John J. Court , Robert P. Farrell
发明人： Richard P. Dunlap , Neil W. Boaz , Albert J. Mura , Virendra Kumar , Chakrapani Subramanyam , Ranjit C. Desai , Dennis J. Hlasta , Manohar T. Saindane , Malcolm R. Bell , John J. Court , Robert P. Farrell
IPC分类号： C07D275/06 , C07D413/12 , C07D417/04 , C07D417/12 , C07F9/6541 , A61K31/425
CPC分类号： C07D275/06 , C07D413/10 , C07D413/12 , C07D417/04 , C07D417/12 , C07F9/6541
摘要： 4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl aryl carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with an arylcarboxylic acid in the presence of an acid-acceptor.
摘要翻译： 可用于治疗退行性疾病的4-R4-R5-2-糖基甲基芳基羧酸盐通过在酸 - 受体存在下使4-R 4 -R 5 - 2-卤代甲基糖精与芳基羧酸反应来制备。
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2.发明授权2-saccharinylmethyl phosphates, phosphonates and phosphinates useful as proteolytic enzyme inhibitors and compositions and method of use thereof 失效可用作蛋白水解酶抑制剂的2-糖基甲基磷酸酯，膦酸酯和次膦酸酯及其组合物及其使用方法
公开(公告)号：US5296496A
公开(公告)日：1994-03-22
申请号：US988424
申请日：1992-12-08
申请人： Ranjit C. Desai , John J. Court , Dennis J. Hlasta
发明人： Ranjit C. Desai , John J. Court , Dennis J. Hlasta
IPC分类号： A61K31/675 , A61K31/67 , A61P1/00 , A61P11/00 , A61P29/00 , A61P43/00 , C07D275/06 , C07D279/02 , C07F20060101 , C07F9/06 , C07F9/08 , C07F9/32 , C07F9/40 , C07F9/6541 , C07F9/6547 , C07F9/6558 , C07F9/6574 , A61K31/425
CPC分类号： C07F9/65583 , C07F9/6541 , C07F9/65586 , C07F9/65742 , C07F9/65744
摘要： 4-R.sub.1 -R.sub.2 -R.sub.3 -2-Saccharinylmethyl and 4,7-C-4,5,6,7-tetrahydro-2-saccharinylmethyl phosphates, phosphonates and phosphinates of formulas I and IIA respectively herein, useful in the treatment of degenerative diseases, and compositions containing them, methods for using them to treat degenerative diseases, and processes for their preparation by reaction of the corresponding 2-halomethylsaccharins with a phosphate, phosphonate or phosphinic acid of formula III herein in the presence of an acid-acceptor.
摘要翻译： 本文分别具有式I和IIA的4-R1-R2-R3-2-糖基甲基和4,7-C-4,5,6,7-四氢-2-糖基甲基磷酸酯，膦酸酯和次膦酸酯，其可用于治疗退行性 疾病和含有它们的组合物，使用它们治疗退行性疾病的方法，以及通过相应的2-卤代甲基糖精与本文在酸受体存在下的式III的磷酸酯，膦酸酯或次膦酸的反应来制备它们的方法。
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3.发明授权2-saccharinylmethyl aryl carboxylates useful as proteolytic enzyme inhibitors and compositions and method of use thereof 失效可用作蛋白水解酶抑制剂的2-糖基甲基芳基羧酸盐及其组合物及其使用方法
公开(公告)号：US5512589A
公开(公告)日：1996-04-30
申请号：US116416
申请日：1993-09-03
申请人： Richard P. Dunlap , Neil W. Boaz , Albert J. Mura , Virendra Kumar , Chakrapani Subramanyam , Ranjit C. Desai , Dennis J. Hlasta , Manohar T. Saindane , Malcolm R. Bell , John J. Court , Robert P. Farrell
发明人： Richard P. Dunlap , Neil W. Boaz , Albert J. Mura , Virendra Kumar , Chakrapani Subramanyam , Ranjit C. Desai , Dennis J. Hlasta , Manohar T. Saindane , Malcolm R. Bell , John J. Court , Robert P. Farrell
IPC分类号： C07D275/06 , C07D413/12 , C07D417/04 , C07D417/12 , C07F9/6541 , A61K31/425 , A61K31/445 , A61K31/495 , A61K31/535
CPC分类号： C07D275/06 , C07D413/10 , C07D413/12 , C07D417/04 , C07D417/12 , C07F9/6541
摘要： A compound having the formula: ##STR1## wherein Ar, R.sup.4 and R.sup.5 are defined herein have pharmaceutical utility as proteolytic enzyme inhibitors.
摘要翻译： 具有下式的化合物：其中Ar，R 4和R 5在本文中定义为具有药理作用的蛋白水解酶抑制剂。
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公开(公告)号：US5250696A
公开(公告)日：1993-10-05
申请号：US860340
申请日：1992-03-30
申请人： Richard P. Dunlap , Neil W. Boaz , Albert J. Mura , Virendra Kumar , Chakrapani Subramanyam , Ranjit C. Desai , Dennis J. Hlasta , Manohar T. Saindane , Malcolm R. Bell , John J. Court
发明人： Richard P. Dunlap , Neil W. Boaz , Albert J. Mura , Virendra Kumar , Chakrapani Subramanyam , Ranjit C. Desai , Dennis J. Hlasta , Manohar T. Saindane , Malcolm R. Bell , John J. Court
IPC分类号： C07D275/06 , C07D417/04 , C07D417/12 , C07F9/6541
CPC分类号： C07D275/06 , C07D417/04 , C07D417/12 , C07F9/6541
摘要： 4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl aryl carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with an arylcarboxylic acid in the presence of an acid-acceptor.
摘要翻译： 可用于治疗退行性疾病的4-R4-R5-2-糖基甲基芳基羧酸盐通过在酸 - 受体存在下使4-R 4 -R 5 - 2-卤代甲基糖精与芳基羧酸反应来制备。
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5.发明授权2-heterocyclyloxymethyl and 2-heterocyclylthiomethyl-1,2,5-thiadiazolidin-3-one 1,1-dioxides and compositions and method of use thereof 失效2-杂环基氧基甲基和2-杂环基硫甲基-1,2,5-噻二唑烷-3-酮1,1-二氧化物及其使用方法
公开(公告)号：US5494925A
公开(公告)日：1996-02-27
申请号：US348421
申请日：1994-12-02
申请人： John J. Court , Ranjit C. Desai , Dennis J. Hlasta
发明人： John J. Court , Ranjit C. Desai , Dennis J. Hlasta
IPC分类号： A61K31/41 , A61K31/415 , A61K31/425 , A61K31/433 , A61P43/00 , C07D285/12 , C07D285/125 , C07D417/12 , C07D513/04
CPC分类号： C07D285/125 , C07D417/12 , C07D513/04
摘要： 2-Heterocyclyloxymethyl and 2-heterocyclylthiomethyL-1,2,5-thiadiazolidin-3-one 1,1-dioxides, pharmaceutical compositions containing them and methods for the treatment of degenerative diseases utilizing them.
摘要翻译： 2-杂环氧基甲基和2-杂环基硫代甲基-1,2,5-噻二唑烷-3-酮1,1-二氧化物，含有它们的药物组合物和用于治疗其使用的退行性疾病的方法。
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6.发明授权2-saccharinylmethyl and 4,5,6,7-tetrahydro-2-saccharinylmethyl phosphates, phosphonates and phosphinates useful as proteolytic enzyme inhibitors and compositions and method of use thereof 失效可用作蛋白水解酶抑制剂的2-糖基甲基和4,5,6,7-四氢-2-糖基甲基磷酸酯，膦酸酯和次膦酸酯及其组合物及其使用方法
公开(公告)号：US5187173A
公开(公告)日：1993-02-16
申请号：US814741
申请日：1991-12-27
IPC分类号： A61K31/675 , A61K31/67 , A61P29/00 , C07D275/06 , C07D279/02 , C07F20060101 , C07F9/06 , C07F9/08 , C07F9/32 , C07F9/40 , C07F9/6541 , C07F9/6547 , C07F9/6558 , C07F9/6574
CPC分类号： C07F9/65583 , C07F9/6541 , C07F9/65742 , C07F9/65744
摘要： 4-R.sub.1 -R.sub.2 -R.sub.3 -2-Saccharinylmethyl, 4-R.sub.4 -4-R.sub.5 -6-R.sub.6 -4,5,6,7-tetrahydro-2-saccharinylmethyl and 4,7-C-4,5,6,7-tetrahydro-2-saccharinylmethyl phosphates, phosphonates and phosphinates of formulas I, II and IIA respectively herein, useful in the treatment of degenerative diseases, and compositions containing them, methods for using them to treat degenerative diseases, and processes for their preparation by reaction of the corresponding 2-halomethylsaccharins with a phosphate, phosphonate or phosphinic acid of formula III herein in the presence of an acid-acceptor.
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公开(公告)号：US5128339A
公开(公告)日：1992-07-07
申请号：US782016
申请日：1991-10-24
申请人： Richard P. Dunlap , Neil W. Boaz , Albert J. Mura , Virendra Kumar , Chakrapani Subramanyam , Ranjit C. Desai , Dennis J. Hlasta , Manohar T. Saindane , Malcolm R. Bell , John J. Court
发明人： Richard P. Dunlap , Neil W. Boaz , Albert J. Mura , Virendra Kumar , Chakrapani Subramanyam , Ranjit C. Desai , Dennis J. Hlasta , Manohar T. Saindane , Malcolm R. Bell , John J. Court
IPC分类号： C07D275/06 , C07D417/04 , C07D417/12 , C07F9/6541
CPC分类号： C07D275/06 , C07D417/04 , C07D417/12 , C07F9/6541 , Y10S514/825 , Y10S514/851 , Y10S514/863
摘要： 4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl aryl carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with an arylcarboxylic acid in the presence of an acid-acceptor.
摘要翻译： 可用于治疗退行性疾病的4-R4-R5-2-糖基甲基芳基羧酸盐通过在酸 - 受体存在下使4-R 4 -R 5 - 2-卤代甲基糖精与芳基羧酸反应来制备。
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8.发明授权2-(pyrazol-5-yl-oxymethyl)-1,2-benzisothiazol-3 (2H)-One 1, 1-dioxides and compositions and method of use thereof 失效2-（吡唑-5-基 - 氧甲基）-1,2-苯并异噻唑-3（2H） - 1,1-二氧化物及其组合物及其使用方法
公开(公告)号：US5750550A
公开(公告)日：1998-05-12
申请号：US529121
申请日：1995-09-15
IPC分类号： C07C69/38 , C07D417/12 , C07D417/14 , A61K31/425 , C07D275/04
CPC分类号： C07D417/12 , C07C69/38 , C07D417/14
摘要： 2-(Pyrazol-5-yl-oxymethyl)-1,2-benzisothiazol-3(2H)-one 1,1-dioxides, pharmaceutical compositions containing them and methods for the treatment of degenerative diseases utilizing them.
摘要翻译： 2-（吡唑-5-基 - 氧甲基）-1,2-苯并异噻唑-3（2H） - 酮1,1-二氧化物，含有它们的药物组合物和利用它们治疗退行性疾病的方法。
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9.发明授权2-saccharinylmethyl heterocyclic carboxylates useful as proteolytic enzyme inhibitors and compositions and method of use thereof 失效可用作蛋白水解酶抑制剂的2-糖基甲基杂环羧酸盐及其组合物及其使用方法
公开(公告)号：US5563163A
公开(公告)日：1996-10-08
申请号：US445247
申请日：1995-05-19
申请人： Richard P. Dunlap , Dennis J. Hlasta , Ranjit C. Desai , Lee H. Latimer , Chakrapani Subramanyam , John J. Court , Malcolm R. Bell , Virendra Kumar
发明人： Richard P. Dunlap , Dennis J. Hlasta , Ranjit C. Desai , Lee H. Latimer , Chakrapani Subramanyam , John J. Court , Malcolm R. Bell , Virendra Kumar
IPC分类号： A61K31/425 , A61K9/20 , A61K9/48 , A61K31/428 , A61K31/44 , A61P1/00 , A61P11/00 , A61P35/00 , A61P43/00 , C07D275/06 , C07D417/12 , C07D275/04
CPC分类号： C07D417/12
摘要： 4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl heterocyclic carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with either a heterocyclic carboxylic acid in the presence of an acid-acceptor or the alkali metal salt of a heterocyclic carboxylic acid.
摘要翻译： 可用于治疗退行性疾病的4-R4-R5-2-糖基甲基杂环羧酸盐通过在酸受体存在下使4-R 4 -R 5 -2-卤代甲基糖精与杂环羧酸反应来制备， 杂环羧酸的碱金属盐。
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公开(公告)号：US5488062A
公开(公告)日：1996-01-30
申请号：US287681
申请日：1994-08-09
申请人： Richard P. Dunlap , Dennis J. Hlasta , Ranjit C. Desai , Lee H. Latimer , Chakrapani Subramanyam , John J. Court , Malcolm R. Bell , Virendra Kumar
发明人： Richard P. Dunlap , Dennis J. Hlasta , Ranjit C. Desai , Lee H. Latimer , Chakrapani Subramanyam , John J. Court , Malcolm R. Bell , Virendra Kumar
IPC分类号： A61K31/425 , A61K9/20 , A61K9/48 , A61K31/428 , A61K31/44 , A61P1/00 , A61P11/00 , A61P35/00 , A61P43/00 , C07D275/06 , C07D417/12
CPC分类号： C07D417/12
摘要： 4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl heterocyclic carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with either a heterocyclic carboxylic acid in the presence of an acid-acceptor or the alkali metal salt of a heterocyclic carboxylic acid.
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