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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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3.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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4.发明授权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应用公开(公告)号：US08859580B2
公开(公告)日：2014-10-14
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： C07D221/26 , C07D417/06 , C07D401/06 , C07D471/08 , C07D498/08 , C07D413/14 , C07D413/06 , C07D405/06 , C07D401/14 , C07D451/06 , C07D403/06
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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5.发明申请Urea derivatives of substituted nortropanes, medicaments containing such compounds and their use 有权取代的正丙胺的脲衍生物，含有这些化合物的药物及其用途公开(公告)号：US20110275595A1
公开(公告)日：2011-11-10
申请号：US13124259
申请日：2009-10-22
IPC分类号： A61K31/695 , A61K31/501 , A61K31/46 , C07D451/02 , C07F7/02 , A61P3/00 , A61P3/10 , A61K31/5377 , A61P3/04
CPC分类号： C07D451/02 , C07D519/00
摘要： The present invention relates to compounds defined by formula I wherein the groups R1, Y1 to Y4, V, W, and X are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 β-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，其中基团R1，Y1至Y4，V，W和X如权利要求1所定义，具有有价值的药理活性。 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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6.发明申请Alicyclic carboxylic acid derivatives of benzomorphans and related scaffolds, medicaments containing such compounds and their use 有权苯并呋喃和相关支架的脂环族羧酸衍生物，含有这些化合物的药物及其应用公开(公告)号：US20110269791A1
公开(公告)日：2011-11-03
申请号：US12991722
申请日：2009-05-12
申请人： Stefan Peters , Matthias Eckhardt , Bradford S. Hamilton , Frank Himmelsbach , Joerg Kley , Thorsten Lehmann-Lintz
发明人： Stefan Peters , Matthias Eckhardt , Bradford S. Hamilton , Frank Himmelsbach , Joerg Kley , Thorsten Lehmann-Lintz
IPC分类号： A61K31/439 , A61K31/4985 , A61P3/10 , A61K31/397 , A61P3/00 , A61P3/06 , C07D471/04 , C07D221/26
CPC分类号： C07D221/26 , C07D221/22 , C07D401/06 , C07D401/08 , C07D401/12 , C07D405/06 , C07D405/12 , C07D471/18 , C07D491/08 , C07D491/18
摘要： The present invention relates to compounds defined by Formula (I), wherein the groups A, B, 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，其中基团A，B，X，m，n和o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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7.发明授权Alicyclic carboxylic acid derivatives of benzomorphans and related scaffolds, medicaments containing such compounds and their use 有权苯并呋喃和相关支架的脂环族羧酸衍生物，含有这些化合物的药物及其应用公开(公告)号：US09073870B2
公开(公告)日：2015-07-07
申请号：US14191951
申请日：2014-02-27
IPC分类号： A61K31/439 , C07D221/22 , C07D221/26 , C07D471/18 , C07D491/18 , C07D401/06 , C07D401/08 , C07D401/12 , C07D405/06 , C07D405/12 , C07D491/08
CPC分类号： C07D221/26 , C07D221/22 , C07D401/06 , C07D401/08 , C07D401/12 , C07D405/06 , C07D405/12 , C07D471/18 , C07D491/08 , C07D491/18
摘要： The present invention relates to compounds defined by formula I wherein the groups A, B, 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，其中基团A，B，X，m，n和o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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8.发明授权Aryl- and heteroarylcarbonyl derivatives of substituted nortropanes, medicaments containing such compounds and their use 有权取代的正丙胺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：US08609690B2
公开(公告)日：2013-12-17
申请号：US13059233
申请日：2009-08-21
IPC分类号： A61K31/541 , C07D451/02 , A61K31/46 , A61K31/498 , A61K31/519
CPC分类号： C07D451/02 , C07D519/00
摘要： The present invention relates to compounds defined by formula (I) wherein the groups R1 and R2 are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 β-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，其中基团R1和R2如权利要求1所定义，具有有价值的药理活性。 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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9.发明授权1,1′-diadamantyl carboxylic acids, medicaments containing such compounds and their use 有权1,1'-二十二烷基羧酸，含有这些化合物的药物及其用途公开(公告)号：US08309597B2
公开(公告)日：2012-11-13
申请号：US13054949
申请日：2009-07-24
IPC分类号： A61K31/40 , A61K31/445 , A61K31/397 , A61K31/5375 , C07D211/08 , C07D205/04 , C07D265/30
CPC分类号： C07D295/185 , C07C62/06 , C07C62/38 , C07C69/00 , C07C69/753 , C07C211/35 , C07C233/32 , C07C233/57 , C07C233/58 , C07C233/60 , C07C255/45 , C07C271/24 , C07C2601/08 , C07C2601/14 , C07C2603/74 , C07D205/04 , C07D207/08 , C07D209/08 , C07D209/44 , C07D211/56 , C07D213/64 , C07D217/04 , C07D223/16 , C07D235/16 , C07D239/74 , C07D241/04 , C07D257/04 , C07D263/56 , C07D271/06
摘要： The present invention relates to compounds defined by formula (I) wherein the group R is 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.
摘要翻译： 本发明涉及由式（I）定义的化合物，其中基团R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被该酶抑制影响的疾病，如代谢疾病。
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10.发明申请Aryl- and Heteroarylcarbonyl derivatives of substituted nortropanes, medicaments containing such compounds and their use 有权取代的正丙胺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：US20120115853A1
公开(公告)日：2012-05-10
申请号：US13059233
申请日：2009-08-21
IPC分类号： A61K31/541 , C07D451/02 , A61K31/46 , A61K31/498 , A61K31/519
CPC分类号： C07D451/02 , C07D519/00
摘要： The present invention relates to compounds defined by formula (I) wherein the groups R1 and R2 are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 β-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，其中基团R1和R2如权利要求1所定义，具有有价值的药理活性。 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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