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公开(公告)号：US5773469A
公开(公告)日：1998-06-30
申请号：US665653
申请日：1996-06-18
申请人： Ramesh M. Kanojia , James P. Demers , Dennis J. Hlasta , Sigmond G. Johnson , Dieter H. Klaubert
发明人： Ramesh M. Kanojia , James P. Demers , Dennis J. Hlasta , Sigmond G. Johnson , Dieter H. Klaubert
IPC分类号： A61K31/137 , A61K31/155 , A61K31/404 , A61K31/44 , A61K31/4409 , A61K31/445 , A61K31/4465 , C07C43/225 , C07C217/58 , C07C217/60 , C07C217/62 , C07C271/16 , C07C279/08 , C07C279/24 , C07D209/48 , C07D211/70 , C07D213/30 , C07D213/38 , A61K31/135 , C07C217/02 , C07C321/28
CPC分类号： C07D209/48 , A61K31/137 , A61K31/155 , A61K31/404 , A61K31/44 , A61K31/4409 , A61K31/445 , A61K31/4465 , C07C217/58 , C07C217/60 , C07C217/62 , C07C271/16 , C07C279/08 , C07C279/24 , C07C43/225 , C07D211/70 , C07D213/30 , C07D213/38 , C07B2200/09 , C07C2102/10 , C07C2103/18
摘要： The invention relates to diaryl antimicrobial compounds of the general formula: ##STR1## where G, E L, J, q, m, X, Ar, W, p, n and A are as described herein, pharmaceutical compositions containing the compounds, methods for their production and their use in treating bacterial infections.
摘要翻译： 本发明涉及以下通式的二芳基抗微生物化合物：其中G，EL，J，q，m，X，Ar，W，p，n和A如本文所述，含有该化合物的药物组合物， 其生产及其在治疗细菌感染中的应用。
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2.发明授权4,4-disubstituted piperidine derivatives useful as inhibitors of dipeptidyl peptidase-1 (DPP-1) 有权可用作二肽基肽酶-1（DPP-1）抑制剂的4,4-二取代哌啶衍生物公开(公告)号：US08686152B2
公开(公告)日：2014-04-01
申请号：US13043609
申请日：2011-03-09
IPC分类号： C07D409/06 , C07D405/06 , A61K31/4525 , A61K31/4535
CPC分类号： C07D409/14 , C12N5/0606
摘要： The present invention is directed to 4,4-di-substituted piperidine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.
摘要翻译： 本发明涉及4,4-二取代哌啶衍生物，含有它们的药物组合物及其用于治疗由DPP-1调节的病症和状况的用途。
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3.发明申请公开(公告)号：US20120077847A1
公开(公告)日：2012-03-29
申请号：US13245137
申请日：2011-09-26
申请人： Michael N. Greco , Margery A. Connelly , Shyamali Ghosh , Dennis J. Hlasta , Edward C. Lawson , Eric Strobel , Michele A. Weidner-Wells , Hong Ye
发明人： Michael N. Greco , Margery A. Connelly , Shyamali Ghosh , Dennis J. Hlasta , Edward C. Lawson , Eric Strobel , Michele A. Weidner-Wells , Hong Ye
IPC分类号： A61K31/4245 , C07D285/12 , C07D417/12 , A61P7/00 , A61K31/4439 , A61P9/10 , A61P3/06 , C07D271/107 , A61K31/433
CPC分类号： C07D271/10 , C07D249/08 , C07D285/12 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention is directed to α-ketoamide derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by endothelial lipase, for example, cardiovascular disorders.
摘要翻译： 本发明涉及α-酮酰胺衍生物，含有它们的药物组合物及其用于治疗由内皮脂肪酶调节的病症和状况的用途，例如心血管疾病。
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公开(公告)号：US06583179B2
公开(公告)日：2003-06-24
申请号：US09745283
申请日：2000-12-21
申请人： Steven J. Coats , Louis J. Fitzpatrick , Dennis J. Hlasta , Carolina L. Lanter , Mark J. Macielag , Ke Pan , Ralph A. Rivero , Stephen S. Palmer
发明人： Steven J. Coats , Louis J. Fitzpatrick , Dennis J. Hlasta , Carolina L. Lanter , Mark J. Macielag , Ke Pan , Ralph A. Rivero , Stephen S. Palmer
IPC分类号： A61K3118
CPC分类号： C07D295/185 , C07C237/22 , C07C275/28 , C07C311/13 , C07C311/19 , C07C311/29 , C07C311/46 , C07C2601/02 , C07C2601/14 , C07D333/18 , C07D333/34 , C07D405/12 , C07D409/04
摘要： The present invention is directed to a series of novel substituted aminoalkylamide derivatives, pharmaceutical compositions containing them and their use in the treatment of reproductive disorders and affective conditions. Further, the compounds of the invention are antagonists of follicle stimulating hormone, a hormone associated with the human reproductive system.
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5.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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公开(公告)号：US5371074A
公开(公告)日：1994-12-06
申请号：US67637
申请日：1993-05-24
申请人： Richard P. Dunlap , Neil W. Boaz , Albert J. Mura , Dennis J. Hlasta , Ranjit C. Desai , Chakrapani Subramanyam , Lee H. Latimer , Eric P. Lodge
发明人： Richard P. Dunlap , Neil W. Boaz , Albert J. Mura , Dennis J. Hlasta , Ranjit C. Desai , Chakrapani Subramanyam , Lee H. Latimer , Eric P. Lodge
IPC分类号： A61K31/425 , A61K31/415 , A61K31/428 , A61K31/47 , A61P29/00 , A61P43/00 , C07D275/04 , C07D275/06 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D513/04 , C07F9/6541 , A61K31/535
CPC分类号： C07D275/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D513/04 , C07F9/6541
摘要： Novel 2-substituted saccharins which inhibit the enzymatic activity of proteolytic enzymes, are useful in the treatment of degenerative diseases and have the formula 0010wherein:L is --O--, --S--, --SO-- or --SO.sub.2 --; m and n are each independently 0 or 1; R.sub.1 is halo, lower-alkanoyl, 1-oxophenalenyl, phenyl or substituted phenyl, heterocyclyl or substitued heterocyclyl or, when L is --O-- and n is 1, cycloheptatrienon-2-yl or, when L is --S-- and n is 1, cyano or lower-alkoxythiocarbonyl or, when L is --SO.sub.2 -- and n is 1, lower-alkyl or trifluoromethyl; R.sub.2 is hydrogen, lower-alkoxycarbonyl, phenyl or phenylthio; and R.sub.3 and R.sub.4 are each hydrogen or various substituents and processes for preparation and pharmaceutical compositions and method of use thereof are disclosed.
摘要翻译： 抑制蛋白水解酶的酶活性的新型2-取代糖精可用于治疗退行性疾病，并具有式0010其中：L是-O - ， - S - ， - SO-或-SO 2 - ; m和n各自独立地为0或1; R 1为卤素，低级烷酰基，1-氧代对苯二烯基，苯基或取代的苯基，杂环基或取代的杂环基，或当L为-O-并且n为1时，环庚三烯-2-基或当L为-S-且n为 1，氰基或低级烷氧基硫代羰基，或当L为-SO 2 - 且n为1时，为低级烷基或三氟甲基; R2是氢，低级烷氧基羰基，苯基或苯硫基; 并且R 3和R 4各自为氢或各种取代基和制备方法，并且公开了药物组合物及其使用方法。
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7.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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公开(公告)号：US20110152321A1
公开(公告)日：2011-06-23
申请号：US12970247
申请日：2010-12-16
IPC分类号： A61K31/454 , C07D209/18 , A61K31/4045 , C07D401/14 , C07D417/12 , A61K31/427 , C07D403/12 , A61K31/4184 , A61P19/02 , A61P11/06 , A61P11/00 , A61P1/00
CPC分类号： C07D209/14 , C07D209/32 , C07D209/42 , C07D409/12 , C07D409/14 , C07D417/12
摘要： The present invention is directed to novel bicyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.
摘要翻译： 本发明涉及新颖的双环衍生物，含有它们的药物组合物及其用于治疗由DPP-1调节的病症和状况的用途。
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9.发明授权Method of producing highly functionalized 1,3-diamino-propan-2-ols from solid support 有权从固体支持物制备高度官能化的1,3-二氨基 - 丙-2-醇的方法公开(公告)号：US07408008B2
公开(公告)日：2008-08-05
申请号：US11006145
申请日：2004-12-07
申请人： Steve J. Coats , Dennis J. Hlasta , Mark J. Schulz
发明人： Steve J. Coats , Dennis J. Hlasta , Mark J. Schulz
IPC分类号： C08F8/30
CPC分类号： C07C315/04 , C07B2200/11 , C07C233/37 , C07C233/40 , C07C233/62 , C07C233/78 , C07C235/50 , C07C235/84 , C07C237/20 , C07C237/22 , C07C237/34 , C07C271/20 , C07C303/40 , C07C319/20 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/50 , C07D213/38 , C07D215/54 , C07D295/13 , C07D307/22 , C07D333/20 , C40B40/04 , C40B50/14 , C07C317/44 , C07C323/60 , C07C311/37
摘要： The invention is directed to compounds and methods of synthesizing hydroxyethlamino amides and their use in treatment of aspartyl protease mediated diseases and conditions.
摘要翻译： 本发明涉及合成羟乙基氨基酰胺的化合物和方法及其在治疗天冬氨酰蛋白酶介导的疾病和病症中的用途。
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公开(公告)号：US07259263B2
公开(公告)日：2007-08-21
申请号：US11170042
申请日：2005-06-29
IPC分类号： C07D223/64 , C07D263/24 , C07D413/06 , C07D471/02
CPC分类号： C07D413/06 , C07D233/64 , C07D263/20 , C07D405/04
摘要： The invention relates to methods of synthesizing 2-substituted azole compunds of formula (I): The invention is also relates to compounds of formula (I) and to intermediate compounds in the synthesis method.
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