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1.发明申请ARYL-AND HETEROARYLCARBONYL DERIVATIVES OF HEXAHYDROINDENOPYRIDINE AND OCTAHYDROBENZOQUINOLINE 有权四氢呋喃并吡咯啉的亚芳基和异丁烯基衍生物公开(公告)号：US20110136800A1
公开(公告)日：2011-06-09
申请号：US12940387
申请日：2010-11-05
IPC分类号： A61K31/473 , C07D401/10 , C07D413/14 , C07D498/04 , A61K31/5377 , A61K31/498 , A61K31/501 , A61K31/437 , A61P3/00 , A61P3/10
CPC分类号： C07D221/10 , C07D221/06 , C07D221/16 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/14 , C07D417/06 , C07D471/04 , C07D498/04
摘要： The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
摘要翻译： 本发明涉及由式I定义的化合物，其中变量R1，R2，R3，R4和m如权利要求1所定义，具有有价值的药理学活性。 特别地，化合物是11β-羟基类固醇脱氢酶（HSD）1的抑制剂，因此适用于治疗和预防可受该酶抑制影响的疾病，例如代谢疾病，特别是2型糖尿病，肥胖症和 血脂异常
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2.发明授权Aryl- and heteroarylcarbonyl derivatives of hexahydroindenopyridine and octahydrobenzoquinoline 有权六氢茚基吡啶和八氢苯并喹啉的芳基和杂芳基羰基衍生物公开(公告)号：US08497281B2
公开(公告)日：2013-07-30
申请号：US12940387
申请日：2010-11-05
IPC分类号： C07D401/06 , A61K31/352
CPC分类号： C07D221/10 , C07D221/06 , C07D221/16 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/14 , C07D417/06 , C07D471/04 , C07D498/04
摘要： The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
摘要翻译： 本发明涉及由式I定义的化合物，其中变量R1，R2，R3，R4和m如权利要求1所定义，具有有价值的药理学活性。 特别地，化合物是11β-羟基类固醇脱氢酶（HSD）1的抑制剂，因此适用于治疗和预防可受该酶抑制影响的疾病，如代谢疾病，特别是2型糖尿病，肥胖症和血脂异常 。
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3.发明授权公开(公告)号：US09328072B2
公开(公告)日：2016-05-03
申请号：US13922889
申请日：2013-06-20
IPC分类号： C07D401/06 , C07D417/06 , C07D413/14 , C07D221/06 , C07D471/04 , C07D221/10 , C07D401/12 , C07D401/14 , C07D405/14 , C07D498/04
CPC分类号： C07D221/10 , C07D221/06 , C07D221/16 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/14 , C07D417/06 , C07D471/04 , C07D498/04
摘要： The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
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4.发明申请ARYL-AND HETEROARYLCARBONYL DERIVATIVES OF HEXAHYDROINDENOPYRIDINE AND OCTAHYDROBENZOQUINOLINE 有权四氢呋喃并吡咯啉的亚芳基和异丁烯基衍生物公开(公告)号：US20140031544A1
公开(公告)日：2014-01-30
申请号：US13922889
申请日：2013-06-20
IPC分类号： C07D401/06 , C07D498/04 , C07D221/06 , C07D471/04 , C07D417/06
CPC分类号： C07D221/10 , C07D221/06 , C07D221/16 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/14 , C07D417/06 , C07D471/04 , C07D498/04
摘要： The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
摘要翻译： 本发明涉及由式I定义的化合物，其中变量R1，R2，R3，R4和m如权利要求1所定义，具有有价值的药理学活性。 特别地，化合物是11β-羟基类固醇脱氢酶（HSD）1的抑制剂，因此适用于治疗和预防可受该酶抑制影响的疾病，如代谢疾病，特别是2型糖尿病，肥胖症和血脂异常 。
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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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公开(公告)号：US08846668B2
公开(公告)日：2014-09-30
申请号：US13054954
申请日：2009-07-23
申请人： Frank Himmelsbach , Matthias Eckhardt , Bradford S. Hamilton , Annette Schuler-Metz , Linghang Zhuang
发明人： Frank Himmelsbach , Matthias Eckhardt , Bradford S. Hamilton , Annette Schuler-Metz , Linghang Zhuang
IPC分类号： A61K31/535 , C07D413/00
CPC分类号： C07D413/10 , C07D413/14
摘要： This invention relates to novel compounds of the Formula (I), (Ia1-10), (Ib1-10), (Ic1-10), (Id1-7), (Ie1-5) 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），（Ia1-10），（Ib1-10），（Ic1-10），（Id1-7），（Ⅰe1-5）其药学上可接受的盐的新型化合物和药物组合物 其可用于治疗与哺乳动物中11β-HSD1的调节或抑制相关的疾病的治疗。 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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公开(公告)号：US20120108578A1
公开(公告)日：2012-05-03
申请号：US13054954
申请日：2009-07-23
申请人： Frank Himmelsbach , Matthias Eckhardt , Bradford S. Hamilton , Annette Schuler-Metz , Linghang Zhuang
发明人： Frank Himmelsbach , Matthias Eckhardt , Bradford S. Hamilton , Annette Schuler-Metz , Linghang Zhuang
IPC分类号： A61K31/5355 , A61P37/02 , C07D413/10
CPC分类号： C07D413/10 , C07D413/14
摘要： This invention relates to novel compounds of the Formula (I), (Ia1-10), (Ib1-10), (Ic1-10), (Id1-7), (Ie1-5) 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），（Ia1-10），（Ib1-10），（Ic1-10），（Id1-7），（Ⅰe1-5）其药学上可接受的盐的新型化合物和药物组合物 其可用于治疗与哺乳动物中11β-HSD1的调节或抑制相关的疾病的治疗。 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.发明授权公开(公告)号：US08933072B2
公开(公告)日：2015-01-13
申请号：US13703708
申请日：2011-06-15
申请人： Matthias Eckhardt , Frank Himmelsbach , Katerina Leftheris , Suresh B. Singh , Colin M. Tice , Zhenrong Xu , Yuanjie Ye , Linghang Zhuang
发明人： Matthias Eckhardt , Frank Himmelsbach , Katerina Leftheris , Suresh B. Singh , Colin M. Tice , Zhenrong Xu , Yuanjie Ye , Linghang Zhuang
IPC分类号： C07D413/14 , C07D413/12 , C07D413/10 , A61K31/5355
CPC分类号： C07D417/14 , A61K31/5355 , C07D413/10 , C07D413/14
摘要： Disclosed are compounds represented by Formula (I): or pharmaceutically acceptable salts, enantiomers or diastereomers thereof. Also disclosed are pharmaceutical compositions comprising the compounds of Formula (I) or pharmaceutically acceptable salts, enantiomers or diastereomers thereof for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. Values for the variables of Formula (I) are defined herein.
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公开(公告)号：US08809376B2
公开(公告)日：2014-08-19
申请号：US13869144
申请日：2013-04-24
IPC分类号： A61K31/44 , C07D307/87
CPC分类号： C07D307/80 , A61K31/343 , A61K31/443 , A61K45/06 , C07D405/12 , A61K2300/00
摘要： The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
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10.发明申请Aryl-and Heteroarylcarbonyl derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use 有权苯并吡喃和相关支架的芳基和杂芳基羰基衍生物，含有这些化合物的药物及其用途公开(公告)号：US20110190262A1
公开(公告)日：2011-08-04
申请号：US12742680
申请日：2008-11-14
申请人： Frank Himmelsbach , Matthias Eckhardt , Bradford S. Hamilton , Armin Heckel , Joerg Kley , Thorsten Lehmann-Lintz , Herbert Nar , Stefan Peters , Annette Schuler-Metz , Matthias Zentgraf
发明人： Frank Himmelsbach , Matthias Eckhardt , Bradford S. Hamilton , Armin Heckel , Joerg Kley , Thorsten Lehmann-Lintz , Herbert Nar , Stefan Peters , Annette Schuler-Metz , Matthias Zentgraf
IPC分类号： A61K31/439 , C07D221/26 , C07D401/06 , C07D405/06 , C07D401/10 , C07D413/10 , C07D417/06 , C07D221/22 , C07D413/06 , C07D491/08 , C07D451/06 , C07D471/08 , C07D401/14 , C07D413/14 , C07D498/08 , C07D403/06 , C07D223/14 , A61K31/496 , A61K31/5377 , A61K31/517 , A61K31/498 , A61K31/5513 , A61K31/506 , A61K31/4985 , A61K31/501 , A61K31/497 , A61K31/4184 , A61K31/55 , A61P3/00 , A61P3/10 , A61P3/04 , A61P3/06
CPC分类号： C07D221/26 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/06 , C07D413/06 , C07D413/14 , C07D417/06 , C07D451/06 , C07D471/08 , C07D498/08
摘要： The present invention relates to compounds defined by formula I wherein the groups R1 to R3, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.
摘要翻译： 本发明涉及由式I定义的化合物，其中R 1至R 3，X，m，n和o基团如权利要求1中所定义，具有有价值的药理学活性。 特别地，化合物是11β-羟基类固醇脱氢酶（HSD）1的抑制剂，因此适用于治疗和预防可受该酶抑制影响的疾病，如代谢疾病，特别是2型糖尿病，肥胖症和血脂异常。
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