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![CRYSTALLINE FORM OF 4-(BETA-D-GLUCOPYRANOS-1-YL)-1-METHYL-2-[4-((S)-TETRAHYDROFURAN-3-YLOXY)-BENZYL]-BENZENE, A METHOD FOR ITS PREPARATION AND THE USE THEREOF FOR PREPARING MEDICAMENTS](/abs-image/US/2010/12/16/US20100317847A1/abs.jpg.150x150.jpg)
11.发明申请CRYSTALLINE FORM OF 4-(BETA-D-GLUCOPYRANOS-1-YL)-1-METHYL-2-[4-((S)-TETRAHYDROFURAN-3-YLOXY)-BENZYL]-BENZENE, A METHOD FOR ITS PREPARATION AND THE USE THEREOF FOR PREPARING MEDICAMENTS 有权4-（β-D-吡喃葡萄糖-1-基）-1-甲基-2- [4 - （（S） - 异丙基呋喃-3-基） - 苯基] - 苯基的晶体形式及其制备方法 用于制备药物公开(公告)号：US20100317847A1
公开(公告)日：2010-12-16
申请号：US12446003
申请日：2007-10-26
CPC分类号： C07H7/00 , C07D407/12 , C07H7/04
摘要： The invention relates to a crystalline form of 4-(β-D-glucopyranos-1-yl)-1-methyl-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, to a method for the preparation thereof, as well as to the use thereof for preparing medicaments.
摘要翻译： 本发明涉及4-（（bgr。-D-吡喃葡萄糖-1-基）-1-甲基-2- [4 - （（S） - 四氢呋喃-3-基氧基） - 苄基] - 苯的结晶形式， 其制备方法以及其制备药物的用途。
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![Crystalline form of 4-(beta-D-glucopyranos-1-yl)-1-methyl-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, a method for its preparation and the use thereof for preparing medicaments](/abs-image/US/2012/10/09/US08283326B2/abs.jpg.150x150.jpg)
12.发明授权Crystalline form of 4-(beta-D-glucopyranos-1-yl)-1-methyl-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, a method for its preparation and the use thereof for preparing medicaments 有权4-（β-D-吡喃葡萄糖-1-基）-1-甲基-2- [4 - （（S） - 四氢呋喃-3-基氧基） - 苄基] - 苯的结晶形式，其制备方法和 其用于制备药物公开(公告)号：US08283326B2
公开(公告)日：2012-10-09
申请号：US12446003
申请日：2007-10-26
CPC分类号： C07H7/00 , C07D407/12 , C07H7/04
摘要： The invention relates to a crystalline form of 4-(β-D-glucopyranos-1-yl)-1-methyl-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, to a method for the preparation thereof, as well as to the use thereof for preparing medicaments.
摘要翻译： 本发明涉及4-（（bgr。-D-吡喃葡萄糖-1-基）-1-甲基-2- [4 - （（S） - 四氢呋喃-3-基氧基） - 苄基] - 苯的结晶形式， 其制备方法以及其制备药物的用途。
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公开(公告)号：US08569292B2
公开(公告)日：2013-10-29
申请号：US12990306
申请日：2009-04-30
申请人： David A. Claremon , Linghang Zhuang , Katerina Leftheris , Colin M. Tice , Zhenrong Xu , Yuanjie Ye , Suresh B. Singh , Salvacion Cacatian , Frank Himmelsbach , Matthias Eckhardt , Wei Zhao
发明人： David A. Claremon , Linghang Zhuang , Katerina Leftheris , Colin M. Tice , Zhenrong Xu , Yuanjie Ye , Suresh B. Singh , Salvacion Cacatian , Frank Himmelsbach , Matthias Eckhardt , Wei Zhao
IPC分类号： C07D413/10 , C07D413/14 , A61K31/5355
CPC分类号： C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14
摘要： This invention relates to novel compounds of the Formula I, Ik, Iq1-21, Ir1-21, Is1-21, It1-7, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
摘要翻译： 本发明涉及式I，Ik，Iq1-21，Ir1-21，Is1-21，It1-7，其药学上可接受的盐及其药物组合物的新型化合物，其可用于治疗与 哺乳动物中11β-HSD1的调节或抑制。 本发明进一步涉及新化合物的药物组合物及其用于减少或控制细胞中皮质醇产生或抑制细胞中可的松转化为皮质醇的方法。
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![8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions](/abs-image/US/2012/02/21/US08119648B2/abs.jpg.150x150.jpg)
14.发明授权公开(公告)号：US08119648B2
公开(公告)日：2012-02-21
申请号：US12143219
申请日：2008-06-20
申请人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Michael Mark , Roland Maier , Ralf Lotz
发明人： Frank Himmelsbach , Elke Langkopf , Matthias Eckhardt , Michael Mark , Roland Maier , Ralf Lotz
IPC分类号： A61P3/10 , A61P3/04 , A61P19/02 , C07D473/06 , C07D519/00 , A61K31/53
CPC分类号： C07D473/04 , C07D473/06 , C07D473/08 , C07D519/00
摘要： The present invention relates to substituted xanthines of general formula wherein R1 to R3 are as defined herein, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
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公开(公告)号：US20110312950A1
公开(公告)日：2011-12-22
申请号：US13147454
申请日：2010-02-13
IPC分类号： A61K31/5355 , C07D265/10 , C07D417/10 , C07D473/12 , C07D471/04 , A61P3/10 , A61P3/06 , A61P9/00 , A61P9/12 , A61P3/04 , A61P35/00 , A61P9/10 , A61P19/10 , A61P5/00 , A61P25/28 , A61P25/22 , A61P25/24 , A61P25/00 , A61P15/00 , A61P1/16 , C07D413/10
CPC分类号： C07D413/10 , C07D417/10
摘要： This invention relates to novel compounds of the Formula Formulas (I), (Ia1-20), (Ib1-20), (Ic1-20), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
摘要翻译： 本发明涉及式（I），（Ia1-20），（Ib1-20），（Ic1-20），其药学上可接受的盐及其药物组合物的新化合物，其可用于治疗 与哺乳动物中11＆amp; bgr-HSD1的调节或抑制相关的疾病。 本发明进一步涉及新化合物的药物组合物及其用于减少或控制细胞中皮质醇产生或抑制细胞中可的松转化为皮质醇的方法。
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16.发明授权Imidazoles and triazoles, their preparation, and their use as pharmaceutical compositions 有权咪唑和三唑，它们的制备及其作为药物组合物的用途公开(公告)号：US07906539B2
公开(公告)日：2011-03-15
申请号：US12192589
申请日：2008-08-15
IPC分类号： A61K31/41 , A61K31/426 , A61K31/4192 , C07D249/08 , C07D233/00
CPC分类号： C07D471/04 , C07D249/14 , C07D401/04 , C07D401/12 , C07D401/14
摘要： The present invention relates to imidazoles and triazoles of general formula wherein R1 to R4 and X are defined as in claims 1 to 8, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译： 本发明涉及通式的咪唑和三唑，其中R 1至R 4和X如权利要求1至8中所定义，互变异构体，对映异构体，非对映异构体，其混合物及其盐具有有价值的药理学性质，特别是 对二肽基肽酶-IV（DPP-IV）的活性具有抑制作用。
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![8-(piperazin-1yl)- and 8-([1,4]diazepan-1yl)-xanthines, the preparation thereof and their use as pharmaceutical composition](/abs-image/US/2009/06/23/US07550455B2/abs.jpg.150x150.jpg)
17.发明授权8-(piperazin-1yl)- and 8-([1,4]diazepan-1yl)-xanthines, the preparation thereof and their use as pharmaceutical composition 有权8-（哌嗪-1-基） - 和8 - （[1,4]二氮杂环庚烷-1-基） - 黄嘌呤，其制备及其作为药物组合物的用途公开(公告)号：US07550455B2
公开(公告)日：2009-06-23
申请号：US10979468
申请日：2004-11-02
IPC分类号： C07D473/06 , C07D519/00 , A61K31/522 , A61P3/10 , A61P3/04
CPC分类号： C07D519/00 , C07D473/04
摘要： The present invention relates to substituted xanthines of the general formula in which R1 to R3 and n are as defined in claims 1 to 8, their tautomers, their enantiomers, their diastereomers, their mixtures, their prodrugs and their salts, which have valuable pharmacological properties, in particular an inhibitory action on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译： 本发明涉及通式的取代黄嘌呤，其中R 1至R 3和n如权利要求1至8中所定义，其互变异构体，其对映异构体，它们的非对映异构体，其混合物，其前药及其盐具有有价值的药理学性质 ，特别是对二肽基肽酶-IV（DPP-IV）的活性的抑制作用。
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![8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions](/abs-image/US/2009/03/10/US07501426B2/abs.jpg.150x150.jpg)
18.发明授权8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions 有权8- [3-氨基 - 哌啶-1-基] - 黄嘌呤，它们的制备及其作为药物组合物的用途公开(公告)号：US07501426B2
公开(公告)日：2009-03-10
申请号：US11060703
申请日：2005-02-17
IPC分类号： C07D473/06 , A61K31/522 , A61P3/10 , A61P19/02 , A61P3/04
CPC分类号： C07D473/04
摘要： Disclosed are substituted xanthines of the formula wherein R is defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译： 公开了下式的取代黄嘌呤：其中R如权利要求1所定义，互变异构体，立体异构体，其混合物及其盐具有有价值的药理学性质，特别是对二肽基肽酶-IV酶活性的抑制作用 DPP-IV）。
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19.发明授权3-methyl-7-butinyl-xanthines, the preparation thereof and their use as pharmaceutical compositions 有权3-甲基-7-丁烯基 - 黄嘌呤，其制备及其作为药物组合物的用途公开(公告)号：US07495002B2
公开(公告)日：2009-02-24
申请号：US11218056
申请日：2005-09-01
申请人： Elke Langkopf , Matthias Eckhardt , Frank Himmelsbach , Mohammad Tadayyon , Leo Thomas , Ralf R. H. Lotz
发明人： Elke Langkopf , Matthias Eckhardt , Frank Himmelsbach , Mohammad Tadayyon , Leo Thomas , Ralf R. H. Lotz
IPC分类号： C07D473/06 , C07D519/00 , A61K31/522 , A61P3/10
CPC分类号： C07D473/00
摘要： The present invention relates to new substituted xanthines of general formula wherein R1, R2 and X are defined as in the claims, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译： 本发明涉及通式的新的取代黄嘌呤：其中R 1，R 2和X如权利要求中所定义，互变异构体，对映异构体，非对映异构体，其混合物及其盐具有有价值的药理学性质，特别是抑制 对二肽基肽酶-IV（DPP-IV）酶活性的影响。
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20.发明授权Imidazopyridazinediones, their preparation and their use as pharmaceutical compositions 有权咪唑并哒嗪酮，其制备及其作为药物组合物的用途公开(公告)号：US07432262B2
公开(公告)日：2008-10-07
申请号：US11676019
申请日：2007-02-16
申请人： Matthias Eckhardt , Frank Himmelsbach , Iris Kauffmann-Hefner , Elke Langkopf , Mohammad Tadayyon , Leo Thomas
发明人： Matthias Eckhardt , Frank Himmelsbach , Iris Kauffmann-Hefner , Elke Langkopf , Mohammad Tadayyon , Leo Thomas
IPC分类号： A61K31/503
CPC分类号： C07D487/04
摘要： The invention relates to substituted imidazopyridazinediones of general formula wherein R1 to R4 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
摘要翻译： 本发明涉及通式的取代的咪唑并哒嗪酮，其中R 1至R 4定义如权利要求1，互变异构体，对映异构体，非对映异构体，其混合物和 其具有有价值的药理学性质，特别是对二肽基肽酶-IV（DPP-IV）的活性的抑制作用。
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