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公开(公告)号：WO2009114313A2
公开(公告)日：2009-09-17
申请号：PCT/US2009/035684
申请日：2009-03-02
申请人： INTERNATIONAL PARTNERSHIP FOR MICROBICIDES , THOMPSON, Andrew, S. , CHENG, Hua , PIKUL, Stanislaw
IPC分类号： A61K31/497 , C07F3/02
摘要： New synthetic methods and intermediates are provided for the synthesis of antiviral compounds.
摘要翻译： 提供新的合成方法和中间体用于合成抗病毒化合物。
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公开(公告)号：WO2005016264A3
公开(公告)日：2005-11-17
申请号：PCT/US2004024775
申请日：2004-08-02
发明人： PADIA JANAK K , O'BRIEN SEAN , LU JIEMIN , PIKUL STANISLAW
IPC分类号： A61K20060101 , A61K31/165 , A61K31/47 , A61K31/498 , A61K31/517 , A61K31/52 , A61K31/535 , A61K31/538 , C07C237/04 , C07D203/14 , C07D207/14 , C07D207/16 , C07D211/46 , C07D211/58 , C07D211/60 , C07D211/62 , C07D213/38 , C07D213/74 , C07D215/12 , C07D215/38 , C07D217/04 , C07D231/06 , C07D237/26 , C07D239/42 , C07D241/42 , C07D265/30 , C07D265/36 , C07D295/112 , C07D295/185 , C07D307/68 , C07D307/79 , C07D333/54 , C07D491/10
CPC分类号： C07D203/14 , C07C237/04 , C07D207/14 , C07D207/16 , C07D211/46 , C07D211/58 , C07D211/60 , C07D211/62 , C07D213/38 , C07D213/74 , C07D215/38 , C07D217/04 , C07D231/06 , C07D239/42 , C07D241/42 , C07D295/112 , C07D295/185 , C07D307/68 , C07D307/79 , C07D333/54 , C07D491/10
摘要： Diamine derivatives of quinones, and related compounds, including salts thereof, that modulate the levels of gene expression in cellular systems, such as cancer cells, are disclosed, along with methods for preparing such compounds and derivatives, as well as pharmaceutical compositions containing these compounds and derivatives as active ingredients. Methods of using these as compounds and derivatives as therapeutic agents are also described.
摘要翻译： 公开了醌类的二胺衍生物和调节细胞系统如癌细胞中基因表达水平的相关化合物，包括其盐，以及制备这些化合物和衍生物的方法以及含有这些化合物的药物组合物 和衍生物作为活性成分。 还描述了将其用作化合物和衍生物作为治疗剂的方法。
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公开(公告)号：WO2005013903A3
公开(公告)日：2005-06-09
申请号：PCT/US2004025343
申请日：2004-08-05
发明人： PADIA JANAK K , O'BRIEN SEAN , LU JIEMIN , PIKUL STANISLAW
IPC分类号： A01N37/18 , A01N43/42 , A01N43/58 , A01N43/60 , A61K20060101 , A61K31/16 , A61K31/165 , A61K31/47 , A61K31/495 , A61K31/50 , C07D239/72 , C07D491/107 , C12N15/12
CPC分类号： C07D211/44 , C07C233/32 , C07C233/41 , C07C235/14 , C07D213/38 , C07D213/74 , C07D215/38 , C07D295/135 , C07D295/185 , C07D307/68 , C07D307/79 , C07D403/12 , C07D409/12 , C07D491/10
摘要： Chemical agents, such as derivatives of quinone, and including salts thereof, that modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.
摘要翻译： 公开了调节细胞系统（包括癌细胞）中基因表达水平的醌类衍生物的化学试剂，包括其盐，以及制备这些试剂的方法，以及含有这些试剂如活性成分的药物组合物 以及使用它们作为治疗剂的方法。
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4.发明申请DIFLUOROBUTYRIC ACID DERIVATIVES AND THEIR USE AS METALLOPROTEASE INHIBITORS 审中-公开二茂铁酸衍生物及其作为金属蛋白酶抑制剂的用途
公开(公告)号：WO0170693A3
公开(公告)日：2002-01-03
申请号：PCT/US0108781
申请日：2001-03-20
申请人： PROCTER & GAMBLE , PIKUL STANISLAW , MIELING GLEN EDWARD , SOLINSKY KELLY MICHELLE , ALMSTEAD NEIL GREGORY , BISWANATH DE , NATCHUS MICHAEL GEORGE
发明人： PIKUL STANISLAW , MIELING GLEN EDWARD , SOLINSKY KELLY MICHELLE , ALMSTEAD NEIL GREGORY , DE BISWANATH , NATCHUS MICHAEL GEORGE
IPC分类号： A61K31/192 , A61K31/198 , A61K31/341 , A61K31/405 , A61K31/4164 , A61K31/426 , A61K31/428 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61P1/02 , A61P9/00 , A61P17/00 , A61P17/02 , A61P19/00 , A61P19/02 , A61P21/00 , A61P25/28 , A61P27/00 , A61P27/02 , A61P29/00 , A61P31/04 , A61P31/20 , A61P31/22 , A61P33/04 , A61P35/00 , C07C45/44 , C07C57/58 , C07C59/64 , C07C69/734 , C07C323/56 , C07C323/59 , C07D207/34 , C07D209/12 , C07D209/18 , C07D213/48 , C07D213/55 , C07D213/70 , C07D213/84 , C07D233/58 , C07D233/84 , C07D277/16 , C07D277/36 , C07D277/74 , C07D307/46 , C07D307/54 , C07D333/24 , C07C47/23 , C07C47/24 , C07C47/277 , C07C57/30 , C07C323/62
CPC分类号： C07D213/70 , C07C45/44 , C07C69/734 , C07C323/56 , C07D207/34 , C07D209/12 , C07D209/18 , C07D213/48 , C07D213/55 , C07D213/84 , C07D233/84 , C07D277/16 , C07D277/36 , C07D277/74 , C07D307/46 , C07D307/54 , C07D333/24 , C07C47/277
摘要： Compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess metalloprotease activity. In particular, the compounds have a structure according to the following Formula (I): where A, G, R , R , R , X, Y and Z have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of Formula I, pharmaceutically-acceptable salts, biohydrolyzable, esters thereof and conjugates thereof. Also described are pharmaceutical compositions comprising these compounds, and methods of treating metalloprotease-related maladies using the compounds or the pharmaceutical compositions. This invention also includes intermediates useful for the synthesis of the compounds of Formula (I).
摘要翻译： 作为金属蛋白酶抑制剂的化合物，其有效治疗以过量金属蛋白酶活性为特征的病症。 特别地，化合物具有下式（I）的结构：其中A，G，R 1，R 2，R 3，X，Y和Z具有说明书中描述的含义。 本发明还包括式I的光学异构体，非对映异构体和对映异构体，其药学上可接受的盐，可生物水解的酯，其酯及其缀合物。 还描述了包含这些化合物的药物组合物，以及使用该化合物或药物组合物治疗金属蛋白酶相关疾病的方法。 本发明还包括可用于合成式（I）化合物的中间体。
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公开(公告)号：WO0170682A3
公开(公告)日：2002-01-31
申请号：PCT/US0108784
申请日：2001-03-20
申请人： PROCTER & GAMBLE , NATCHUS MICHAEL GEORGE , PIKUL STANISLAW , ALMSTEAD NEIL GREGORY , LAUFERSWEILER MATTHEW J , BOOKLAND ROGER GUNNARD , TULLIS JOSHUA S , BISWANATH DE
发明人： NATCHUS MICHAEL GEORGE , PIKUL STANISLAW , ALMSTEAD NEIL GREGORY , LAUFERSWEILER MATTHEW J , BOOKLAND ROGER GUNNARD , TULLIS JOSHUA S , DE BISWANATH
IPC分类号： C07D233/78 , A61K31/198 , A61K31/357 , A61K31/36 , A61K31/4015 , A61K31/4164 , A61K31/4166 , A61K31/421 , A61K31/426 , A61K31/535 , A61K31/5375 , A61P19/02 , A61P29/00 , A61P35/00 , A61P35/04 , A61P43/00 , C07C311/29 , C07D207/26 , C07D207/27 , C07D233/72 , C07D235/02 , C07D263/20 , C07D263/24 , C07D265/10 , C07D265/32 , C07D275/02 , C07D295/096 , C07D317/72 , C07D319/08 , C07C311/19 , C07C311/25
CPC分类号： C07D207/27 , C07C311/29 , C07C2601/14 , C07D233/72 , C07D235/02 , C07D263/20 , C07D265/10 , C07D265/32 , C07D275/02 , C07D295/096 , C07D317/72 , C07D319/08
摘要： Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to Formula (I) where R , R , n, A, E, E', L, L', G and Z have the meanings described in the specification and the claims, as well as optical isomers, diastereomers and enantiomers of Formula (I), and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also described are pharmaceutical compositions comprising these compounds, and methods of treating metalloprotease-related maladies using the compounds or the pharmaceutical compositions.
摘要翻译： 公开了作为金属蛋白酶抑制剂的化合物，其有效治疗以这些酶的过量活性为特征的病症。 特别地，化合物具有式（I）的结构，其中R 1，R 2，n，A，E，E'，L，L'，G和Z具有说明书和 权利要求书，以及式（I）的光学异构体，非对映异构体和对映体及其药学上可接受的盐，生物可水解的酰胺，酯和酰亚胺。 还描述了包含这些化合物的药物组合物，以及使用该化合物或药物组合物治疗金属蛋白酶相关疾病的方法。
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公开(公告)号：WO2009114313A3
公开(公告)日：2010-03-04
申请号：PCT/US2009035684
申请日：2009-03-02
发明人： THOMPSON ANDREW S , CHENG HUA , PIKUL STANISLAW
摘要： New synthetic methods and intermediates are provided for the synthesis of antiviral compounds.
摘要翻译： 提供新的合成方法和中间体用于合成抗病毒化合物。
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7.发明申请DERIVATIVES OF 3-HYDROXY-PYRROLE-2,4-DICARBOXYLIC ACID AND USES THEREOF 审中-公开3-羟基吡咯烷-2,4-二羧酸的衍生物及其用途
公开(公告)号：WO2005011675A1
公开(公告)日：2005-02-10
申请号：PCT/US2004/024473
申请日：2004-07-28
申请人： AVALON PHARMACEUTICALS , CHOLODY, Wieslaw, M. , PETUKHOVA, Valentina , O'BRIEN, Sean , OHLER, Norman , PIKUL, Stanislaw
IPC分类号： A61K31/40
CPC分类号： C07D401/12 , C07D207/36 , C07D405/12 , C07D453/02 , C07D487/08
摘要： Chemical agents of the general formula (1) and (11), such as derivatives of 3-hydroxy-pyrrole containing hydroxamic acid, and including salts thereof, that modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.
摘要翻译： 公开了通式（1）和（11）的化学试剂，例如含有羟基异羟肟酸的3-羟基吡咯的衍生物及其盐，其调节包括癌细胞在内的细胞系统中的基因表达水平 制备这种试剂的方法，以及含有这些试剂如活性成分的药物组合物和使用它们作为治疗剂的方法。
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8.发明申请CARBOCYCLIC SIDE CHAIN CONTAINING, N-SUBSTITUTED METALLOPROTEASE INHIBITORS 审中-公开含有碳链的侧链，N-取代的金属蛋白酶抑制剂
公开(公告)号：WO0170720A3
公开(公告)日：2002-02-28
申请号：PCT/US0108782
申请日：2001-03-20
申请人： PROCTER & GAMBLE , NATCHUS MICHAEL GEORGE , PIKUL STANISLAW , ALMSTEAD NEIL GREGORY , LAUFERSWEILER MATTHEW J , BISWANATH DE
发明人： NATCHUS MICHAEL GEORGE , PIKUL STANISLAW , ALMSTEAD NEIL GREGORY , LAUFERSWEILER MATTHEW J , DE BISWANATH
IPC分类号： C07D295/14 , A61K31/198 , A61K31/357 , A61K31/36 , A61K31/4015 , A61K31/4172 , A61K31/421 , A61K31/425 , A61K31/535 , A61P19/02 , A61P29/00 , A61P35/00 , C07C311/29 , C07D207/26 , C07D207/27 , C07D233/72 , C07D233/74 , C07D235/02 , C07D263/20 , C07D263/22 , C07D265/10 , C07D265/32 , C07D275/02 , C07D295/155 , C07D317/72 , C07D319/08 , C07C311/19 , C07C311/25
CPC分类号： C07D207/27 , C07C311/29 , C07C2601/14 , C07D233/72 , C07D235/02 , C07D263/20 , C07D265/10 , C07D265/32 , C07D275/02 , C07D295/155 , C07D317/72 , C07D319/08
摘要： Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where R , R , R , n, A, E, E', L, L', G and Z have the meanings described in the specification and the claims, as well as optical isomers, diastereomers and enantiomers of Formula I, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also described are pharmaceutical compositions comprising these compounds, and methods of treating metalloprotease-related maladies using the compounds or the pharmaceutical compositions.
摘要翻译： 公开了作为金属蛋白酶抑制剂的化合物，其有效治疗以这些酶的过量活性为特征的病症。 特别地，化合物具有下式（I）的结构：其中R 1，R 2，R 3，n，A，E，E'，L，L'，G和Z 具有说明书和权利要求书中描述的含义，以及式I的光学异构体，非对映异构体和对映异构体及其药学上可接受的盐，可生物水解的酰胺，酯和酰亚胺。 还描述了包含这些化合物的药物组合物，以及使用该化合物或药物组合物治疗金属蛋白酶相关疾病的方法。
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公开(公告)号：WO2013131255A1
公开(公告)日：2013-09-12
申请号：PCT/CN2012/072020
申请日：2012-03-07
发明人： CHEN, Yi-Jing , PIKUL, Stanislaw
IPC分类号： C07D213/75 , C07D213/74 , C07C43/235 , C07C43/164
CPC分类号： C07D213/74 , C07C43/2055 , C07C43/307 , C07C43/315 , C07D213/75 , C07D317/22 , C07D319/06
摘要： The present invention provides novel processes for the preparation of N-substituted benzamides having the formula VIc: (formula) In some embodiments, the invention provides a process for preparation of roflumilast and other pharmaceutically active species. Novel compounds, including intermediates for the synthesis of roflumilast, are also provided.
摘要翻译： 本发明提供用于制备具有式VIc的N-取代苯甲酰胺的新方法：（式）在一些实施方案中，本发明提供了制备罗氟司特和其它药学活性物质的方法。 还提供了新型化合物，包括合成罗氟司特的中间体。
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公开(公告)号：WO2005016264A2
公开(公告)日：2005-02-24
申请号：PCT/US2004/024775
申请日：2004-08-02
发明人： PADIA, Janak, K. , O'BRIEN, Sean , LU, Jiemin , PIKUL, Stanislaw
IPC分类号： A61K
CPC分类号： C07D203/14 , C07C237/04 , C07D207/14 , C07D207/16 , C07D211/46 , C07D211/58 , C07D211/60 , C07D211/62 , C07D213/38 , C07D213/74 , C07D215/38 , C07D217/04 , C07D231/06 , C07D239/42 , C07D241/42 , C07D295/112 , C07D295/185 , C07D307/68 , C07D307/79 , C07D333/54 , C07D491/10
摘要： Diamine derivatives of quinones, and related compounds, including salts thereof, that modulate the levels of gene expression in cellular systems, such as cancer cells, are disclosed, along with methods for preparing such compounds and derivatives, as well as pharmaceutical compositions containing these compounds and derivatives as active ingredients. Methods of using these as compounds and derivatives as therapeutic agents are also described.
摘要翻译： 公开了调节细胞系统如癌细胞中基因表达水平的醌的二胺衍生物以及相关化合物及其盐，包括其盐，以及制备这些化合物和衍生物的方法， 以及含有这些化合物和衍生物作为活性成分的药物组合物。 还描述了使用这些化合物和衍生物作为治疗剂的方法。
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