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1.发明申请INTERMEDIATES AND PROCESSES FOR THE PREPARATION OF FLUOROGLYCOSIDE DERIVATIVES 审中-公开制备荧光素衍生物的中间体和方法
公开(公告)号：WO2010077623A1
公开(公告)日：2010-07-08
申请号：PCT/US2009/067079
申请日：2009-12-08
申请人： SANOFI-AVENTIS , GESSLER, Simon , GILL, Harpal S. , LEE, George E. , PLETTENBURG, Oliver , PODESCHWA, Michael , POWERS, Matthew R. , ROSSEN, Kai , SHRIMP, II, Frederick L. , SUBOTKOWSKI, Witold , VANASSE, Benoit J. , WEHLAN, Hermut A. , WEIBERTH, Franz J. , YU, Yong , ZHANG, Jiuqing
发明人： GESSLER, Simon , GILL, Harpal S. , LEE, George E. , PLETTENBURG, Oliver , PODESCHWA, Michael , POWERS, Matthew R. , ROSSEN, Kai , SHRIMP, II, Frederick L. , SUBOTKOWSKI, Witold , VANASSE, Benoit J. , WEHLAN, Hermut A. , WEIBERTH, Franz J. , YU, Yong , ZHANG, Jiuqing
IPC分类号： C07D231/20 , C07H5/02 , C07H13/08
CPC分类号： C07D231/20
摘要： The present invention provides processes for producing (2 S ,3 R ,4 R ,5 S ,6 R )-5-fluoro-6- hydroxymethyl-2-[4-(4-methoxy-benzyl)-5-trifluoromethyl-1 H -pyrazol-3-yloxy]- tetrahydro-pyran-3,4-diol or a tautomer or hydrate thereof, of high purity and in a relatively high yield suitable for use on an industrial scale. The present invention is also directed to synthetic intermediates that are useful for the preparation of (2 S ,3 R ,4 R ,5 S ,6 R )-5-fluoro-6-hydroxymethyl-2-[4-(4-methoxy- benzyl)-5-trifluoromethyl-1 H -pyrazol-3-yloxy]-tetrahydro-pyran-3,4-diol or a tautomer or hydrate thereof.
摘要翻译： 本发明提供（2S，3R，4R，5S，6R）-5-氟-6-羟甲基-2- [4-（4-甲氧基 - 苄基）-5-三氟甲基-1H-吡唑-3-基] 氧基] - 四氢 - 吡喃-3,4-二醇或其互变异构体或水合物，其具有高纯度和相对高的产率，适用于工业规模。 本发明还涉及可用于制备（2S，3R，4R，5S，6R）-5-氟-6-羟甲基-2- [4-（4-甲氧基 - 苄基）-5 - 三氟甲基-1H-吡唑-3-基氧基] - 四氢 - 吡喃-3,4-二醇或其互变异构体或水合物。
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2.发明申请PIPERIDINYL-SUBSTITUTED ISOQUINOLONE DERIVATIVES AS RHO-KINASE INHIBITORS 审中-公开作为RHO-激酶抑制剂的哌啶取代的异喹啉衍生物
公开(公告)号：WO2007012421A1
公开(公告)日：2007-02-01
申请号：PCT/EP2006/007139
申请日：2006-07-20
申请人： SANOFI-AVENTIS DEUTSCHLAND GMBH , PLETTENBURG, Oliver , HOFMEISTER, Armin , KADEREIT, Dieter , BRENDEL, Joachim , LOEHN, Matthias
发明人： PLETTENBURG, Oliver , HOFMEISTER, Armin , KADEREIT, Dieter , BRENDEL, Joachim , LOEHN, Matthias
IPC分类号： C07D401/12 , A61K31/4725 , A61P9/12
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14
摘要： The invention relates to 6-piperidinyl-substituted isoquinolone derivatives of the formula (I) or isoquinoline derivatives of the formula (I´) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
摘要翻译： 本发明涉及式（I）的6-哌啶基取代的异喹啉酮衍生物或式（I'）的异喹啉衍生物，其用于治疗和/或预防与Rho-激酶和/或Rho-激酶介导的磷酸化相关的疾病 的肌球蛋白轻链磷酸酶，以及含有这些化合物的组合物。
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公开(公告)号：WO2009156099A8
公开(公告)日：2010-03-11
申请号：PCT/EP2009004420
申请日：2009-06-19
申请人： SANOFI AVENTIS , PLETTENBURG OLIVER , LORENZ KATRIN , LOEHN MATTHIAS , WESTON JOHN , KLEEMANN HEINZ-WERNER
IPC分类号： C07D217/24 , A61K31/472 , A61K31/4725 , A61P9/12 , A61P43/00 , C07D217/02 , C07D217/22 , C07D405/12 , C07D409/12 , C07D417/12
CPC分类号： C07D417/12 , C07D217/02 , C07D217/22 , C07D217/24 , C07D405/12 , C07D409/12
摘要： The invention relates to 6-substituted isoquinoline and isoquinolinone derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
摘要翻译： 本发明涉及用于治疗和/或预防与肌球蛋白轻链磷酸酶的Rho-激酶和/或Rho-激酶介导的磷酸化有关的疾病的式（I）的6-取代异喹啉和异喹啉酮衍生物， 化合物。
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4.发明申请
公开(公告)号：WO2009156100A1
公开(公告)日：2009-12-30
申请号：PCT/EP2009/004421
申请日：2009-06-19
申请人： SANOFI-AVENTIS , PLETTENBURG, Oliver , LORENZ, Katrin , WESTON, John , LOEHN, Matthias , KLEEMANN, Heinz-Werner , DUCLOS, Olivier , JEANNOT, Frédéric
发明人： PLETTENBURG, Oliver , LORENZ, Katrin , WESTON, John , LOEHN, Matthias , KLEEMANN, Heinz-Werner , DUCLOS, Olivier , JEANNOT, Frédéric
IPC分类号： C07D217/24 , A61K31/472 , A61P9/00 , A61P27/00 , A61P25/00 , A61P37/00
CPC分类号： C07D217/24
摘要： The invention relates to substituted isoquinoline and isoquinolinones of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
摘要翻译： 本发明涉及可用于治疗和/或预防与肌球蛋白轻链磷酸酶的Rho-激酶和/或Rho-激酶介导的磷酸化相关疾病的式（I）的取代异喹啉和异喹啉酮，以及含有这些化合物的组合物。
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公开(公告)号：WO2007000240A1
公开(公告)日：2007-01-04
申请号：PCT/EP2006/005648
申请日：2006-06-13
申请人： SANOFI-AVENTIS DEUTSCHLAND GMBH , PLETTENBURG, Oliver , HOFMEISTER, Armin , KADEREIT, Dieter , PEUKERT, Stefan , RUF, Sven , RITTER, Kurt , LÖHN, Matthias , IVASHCHENKO, Yuri , MONECKE, Peter , DREYER, Matthias , KANNT, Aimo
发明人： PLETTENBURG, Oliver , HOFMEISTER, Armin , KADEREIT, Dieter , PEUKERT, Stefan , RUF, Sven , RITTER, Kurt , LÖHN, Matthias , IVASHCHENKO, Yuri , MONECKE, Peter , DREYER, Matthias , KANNT, Aimo
IPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D217/02 , C07D217/22 , A61K31/4725 , A61P11/00 , A61P27/00
CPC分类号： C07D405/14 , C07D401/12 , C07D401/14 , C07D409/14
摘要： The invention relates to 6-piperidinyl-substituted isoquinoline derivatives of the formula (I); useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
摘要翻译： 本发明涉及式（I）的6-哌啶基取代的异喹啉衍生物; 可用于治疗和/或预防与Rho激酶和/或Rho激酶介导的肌球蛋白轻链磷酸酶的磷酸化相关的疾病，以及含有这些化合物的组合物。
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6.发明申请A NOVEL CRYSTALLINE HETEROAROMATIC FLUOROGLYCOSIDE HYDRATE, PROCESSES FOR MAKING, METHODS OF USE AND PHARMACEUTICAL COMPOSITIONS THEREOF 审中-公开新型水晶异氟醚水合物，其制备方法，使用方法及其药物组合物
公开(公告)号：WO2010066690A1
公开(公告)日：2010-06-17
申请号：PCT/EP2009/066551
申请日：2009-12-07
申请人： SANOFI-AVENTIS , BERCHTOLD, Harald , NAGEL, Norbert , BAUMGARTNER, Bruno , PLETTENBURG, Oliver , WEIBERTH, Franz , HARPAL, Gill , YU, Yong , LIEBERMAN, Harvey , SECORD, Elisabeth , GORDONOV, Boris , DONEGHAN, Tim , BYARD, Steve
发明人： BERCHTOLD, Harald , NAGEL, Norbert , BAUMGARTNER, Bruno , PLETTENBURG, Oliver , WEIBERTH, Franz , HARPAL, Gill , YU, Yong , LIEBERMAN, Harvey , SECORD, Elisabeth , GORDONOV, Boris , DONEGHAN, Tim , BYARD, Steve
IPC分类号： C07H17/02 , A61K31/7056
CPC分类号： C07H17/02
摘要： The invention relates to a crystalline hydrate of the formula (I) in which n has a value of from 0.9 to 1.1. The compound is suitable, for example, as an antidiabetic.
摘要翻译： 本发明涉及式（I）的结晶水合物，其中n的值为0.9至1.1。 该化合物例如作为抗糖尿病剂是合适的。
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7.发明申请
公开(公告)号：WO2008077555A3
公开(公告)日：2009-05-07
申请号：PCT/EP2007011168
申请日：2007-12-19
IPC分类号： C07D401/12 , A61K31/4725 , A61P3/00 , A61P7/00 , A61P9/00 , A61P25/00 , C07D401/14 , C07D405/14 , C07D451/06
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D451/06
摘要： The invention relates to 6-substituted isoquinoline and isochinolone derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
摘要翻译： 本发明涉及可用于治疗和/或预防与肌球蛋白轻链磷酸酶的Rho-激酶和/或Rho-激酶介导的磷酸化有关的疾病的式（I）的6-取代异喹啉和异诺酮酮衍生物， 化合物。
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8.发明申请
公开(公告)号：WO2008077556A1
公开(公告)日：2008-07-03
申请号：PCT/EP2007/011169
申请日：2007-12-19
申请人： SANOFI-AVENTIS , PLETTENBURG, Oliver , LORENZ, Katrin , GOERLITZER, Jochen , LÖHN, Matthias , BISCARRAT, Sandrine , JEANNOT, Frédéric , DUCLOT, Olivier
发明人： PLETTENBURG, Oliver , LORENZ, Katrin , GOERLITZER, Jochen , LÖHN, Matthias , BISCARRAT, Sandrine , JEANNOT, Frédéric , DUCLOT, Olivier
IPC分类号： C07D217/24 , A61K31/472 , A61P9/12
CPC分类号： C07D217/24
摘要： The invention relates to 6-substituted isoquinoline and isoquinolinone derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
摘要翻译： 本发明涉及用于治疗和/或预防与肌球蛋白轻链磷酸酶的Rho-激酶和/或Rho-激酶介导的磷酸化有关的疾病的式（I）的6-取代异喹啉和异喹啉酮衍生物， 化合物。
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9.发明申请
公开(公告)号：WO2008077553A1
公开(公告)日：2008-07-03
申请号：PCT/EP2007/011166
申请日：2007-12-19
IPC分类号： C07D217/22 , C07D217/24 , C07D401/12 , A61K31/472 , A61P9/00 , A61P11/06
CPC分类号： C07D217/22 , C07D217/24 , C07D401/12
摘要： The invention relates to 6-substituted isoquinoline and isoquinolinone derivatives of the Formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
摘要翻译： 本发明涉及可用于治疗和/或预防与肌球蛋白轻链磷酸酶的Rho-激酶和/或Rho-激酶介导的磷酸化有关的疾病的式（I）的6-取代异喹啉和异喹啉酮衍生物， 化合物。
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公开(公告)号：WO2008077552A1
公开(公告)日：2008-07-03
申请号：PCT/EP2007/011165
申请日：2007-12-19
IPC分类号： C07D401/12 , C07D401/14 , C07D409/14 , A61K31/4725 , A61P9/00
CPC分类号： C07D401/12 , C07D401/14 , C07D409/14
摘要： The invention relates to 6-substituted isoquinoline and isochinolone derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
摘要翻译： 本发明涉及可用于治疗和/或预防与肌球蛋白轻链磷酸酶的Rho-激酶和/或Rho-激酶介导的磷酸化有关的疾病的式（I）的6-取代异喹啉和异诺酮酮衍生物， 化合物。
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