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1.发明申请17-carbamoyloxy cortisol derivatives as selective glucocorticoid receptor modulators 失效17-氨甲酰氧基皮质醇衍生物作为选择性糖皮质激素受体调节剂公开(公告)号：US20060063746A1
公开(公告)日：2006-03-23
申请号：US10540757
申请日：2004-01-16
申请人： Amjad Ali , James Balkovec , Donald Graham , Mark Greenlee , Gayle Taylor
发明人： Amjad Ali , James Balkovec , Donald Graham , Mark Greenlee , Gayle Taylor
CPC分类号： C07J41/005 , C07J43/00
摘要： The present invention encompasses compounds of Formula (I) or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharamaceutical compositions and methods of use are also included.
摘要翻译： 本发明包括式（I）化合物或其药学上可接受的盐或水合物，其可用作治疗各种自身免疫性和炎性疾病或病症的选择性糖皮质激素受体配体。 还包括制药组合物和使用方法。
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![Octahydro-2-h-naphtho[1,2-f]indole-4-carboxamide derivatives as selective glucocorticoid receptor modulators](/abs-image/US/2005/11/03/US20050245588A1/abs.jpg.150x150.jpg)
2.发明申请Octahydro-2-h-naphtho[1,2-f]indole-4-carboxamide derivatives as selective glucocorticoid receptor modulators 审中-公开八氢-2-H-萘并[1,2-f]吲哚-4-甲酰胺衍生物作为选择性糖皮质激素受体调节剂公开(公告)号：US20050245588A1
公开(公告)日：2005-11-03
申请号：US10527615
申请日：2003-09-17
申请人： Amjad Ali , Susan Aster , James Balkovec , Donald Graham , Julianne Hunt , Florida Kallashi , Peter Sinclair , James Tata , Gayle Taylor , Joung Goulet
发明人： Amjad Ali , Susan Aster , James Balkovec , Donald Graham , Julianne Hunt , Florida Kallashi , Peter Sinclair , James Tata , Gayle Taylor , Joung Goulet
IPC分类号： A61K20060101 , A61K31/4162 , C07D231/44 , C07D231/54 , C07D417/00
CPC分类号： C07J71/0047 , C07D231/54 , C07D401/12 , C07D403/04 , C07D409/12 , C07D413/04 , C07D417/04 , C07D491/113
摘要： The present invention encompasses compounds of Formula I: or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.
摘要翻译： 本发明包括式I化合物或其药学上可接受的盐或水合物，其可用作治疗各种自身免疫性和炎性疾病或病症的选择性糖皮质激素受体配体。 还包括药物组合物和使用方法。
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公开(公告)号：US20060217563A1
公开(公告)日：2006-09-28
申请号：US10551933
申请日：2004-04-19
申请人： Amjad Ali , James Balkovec , Richard Beresis , Steven Colletti , Donald Graham , Gool Patel , Cameron Smith
发明人： Amjad Ali , James Balkovec , Richard Beresis , Steven Colletti , Donald Graham , Gool Patel , Cameron Smith
IPC分类号： C07D487/10
CPC分类号： C07D495/10 , C07D487/10 , C07D491/10
摘要： The present invention encompasses compounds of Formula (I) and Formula (II) or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use
摘要翻译： 本发明包括式（I）和式（II）的化合物或其药学上可接受的盐或水合物，其可用作治疗各种自身免疫性和炎性疾病或病症的选择性糖皮质激素受体配体。 药物组合物和使用方法
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![1H-benzo[F]indazol-5-YL derivatives as selective glucocorticoid receptor modulators](/abs-image/US/2008/03/27/US20080076795A1/abs.jpg.150x150.jpg)
4.发明申请1H-benzo[F]indazol-5-YL derivatives as selective glucocorticoid receptor modulators 失效1H-苯并[F]吲唑-5-YL衍生物作为选择性糖皮质激素受体调节剂公开(公告)号：US20080076795A1
公开(公告)日：2008-03-27
申请号：US11904186
申请日：2007-09-26
IPC分类号： A61K31/416 , A61K31/4184 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61P29/00 , A61P37/00 , C07D231/54 , C07D401/02 , C07D403/02 , C07D405/02 , C07D409/02 , C07D417/02
CPC分类号： C07D417/06 , C07D231/54 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/10 , C07D405/06 , C07D405/10 , C07D409/06
摘要： The present invention encompasses compounds of Formula I: or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.
摘要翻译： 本发明包括式I化合物或其药学上可接受的盐或水合物，其可用作用于治疗多种自身免疫性和炎性疾病或病症的选择性糖皮质激素受体配体。 还包括药物组合物和使用方法。
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5.发明申请1h-benzo{f}indazol-5-yl derivatives as selective glucocorticoid receptor modulators 失效1h-苯并{f}吲唑-5-基衍生物作为选择性糖皮质激素受体调节剂公开(公告)号：US20050256315A1
公开(公告)日：2005-11-17
申请号：US10508897
申请日：2003-04-08
IPC分类号： A61K31/416 , A61K31/4184 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61P1/04 , A61P1/16 , A61P3/00 , A61P3/04 , A61P3/10 , A61P3/14 , A61P7/04 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/14 , A61P19/08 , A61P21/00 , A61P21/02 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P27/16 , A61P29/00 , A61P31/04 , A61P31/18 , A61P31/22 , A61P35/00 , A61P35/02 , A61P37/00 , A61P37/04 , A61P37/06 , A61P37/08 , A61P43/00 , C07D231/54 , C07D231/56 , C07D249/16 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/10 , C07D405/06 , C07D405/10 , C07D409/06 , C07D417/06
CPC分类号： C07D417/06 , C07D231/54 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/10 , C07D405/06 , C07D405/10 , C07D409/06
摘要： The present invention encompasses compounds of Formula I: (I) or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharamaceutical compositions and methods of use are also included.
摘要翻译： 本发明包括式I化合物：（I）或其药学上可接受的盐或水合物，其可用作治疗各种自身免疫性和炎性疾病或病症的选择性糖皮质激素受体配体。 还包括制药组合物和使用方法。
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公开(公告)号：US20060074120A1
公开(公告)日：2006-04-06
申请号：US10544899
申请日：2004-02-20
申请人： Amjad Ali , Richard Beresis , Steven Colletti , Donald Graham , James Tata , Christopher Thompson
发明人： Amjad Ali , Richard Beresis , Steven Colletti , Donald Graham , James Tata , Christopher Thompson
IPC分类号： C07D231/54 , A61K31/4162
CPC分类号： C07D409/12 , C07D231/54 , C07D401/12 , C07D403/06 , C07D403/12 , C07D409/04
摘要： The present invention encompasses compounds of Formula (I) or pharmaceutically acceptable salts or hydrates thereof, which are useful as novel non-steroidal selective glucocorticoid receptor modulators for treating a variety of autoimmune and inflammatory diseases or conditions, and possess advantages over steroidal glucocorticoid ligands with respect to undesireable side-effects, efficacy, toxicity and/or metabolism. Pharmaceutical compositions and methods of use are also included.
摘要翻译： 本发明包括式（I）化合物或其药学上可接受的盐或水合物，其可用作新型非甾体选择性糖皮质激素受体调节剂，用于治疗多种自身免疫性和炎性疾病或病症，并且具有超过甾族糖皮质激素配体的优点， 尊重不良的副作用，功效，毒性和/或代谢。 还包括药物组合物和使用方法。
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7.发明申请Triazole derivatives as inhibitors of 11-beta hydroxysteroid dehydrogenase-1 有权作为11-β羟基类固醇脱氢酶-1抑制剂的三唑衍生物公开(公告)号：US20060258695A1
公开(公告)日：2006-11-16
申请号：US10558454
申请日：2004-05-26
申请人： Sherman Waddell , Gina Santorelli , Milana Maletic , Aaron Leeman , Xin Gu , Donald Graham , James Balkovec , Susan Aster
发明人： Sherman Waddell , Gina Santorelli , Milana Maletic , Aaron Leeman , Xin Gu , Donald Graham , James Balkovec , Susan Aster
IPC分类号： C07D487/02 , A61K31/4196 , A61K31/506 , A61K31/4245
CPC分类号： C07D249/08 , C07D249/16 , C07D413/08 , C07D487/04
摘要： Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.
摘要翻译： 结构式I的三唑衍生物是11b-羟基类固醇脱氢酶-1的选择性抑制剂。 该化合物可用于治疗糖尿病，例如非胰岛素依赖性糖尿病（NIDDM），高血糖症，肥胖症，胰岛素抵抗，血脂异常，高脂血症，高血压，代谢综合征和与NIDDM相关的其他症状。
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8.发明申请Triazole derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1 有权作为11-β-羟基类固醇脱氢酶-1抑制剂的三唑衍生物公开(公告)号：US20050154038A1
公开(公告)日：2005-07-14
申请号：US11011889
申请日：2004-12-14
申请人： Sherman Waddell , Gina Santorelli , Milana Maletic , Aaron Leeman , Xin Gu , Donald Graham , James Balkovec , Susan Aster
发明人： Sherman Waddell , Gina Santorelli , Milana Maletic , Aaron Leeman , Xin Gu , Donald Graham , James Balkovec , Susan Aster
IPC分类号： A61K31/4196 , A61P3/10 , C07D249/00 , C07D249/08 , C07D401/04 , C07D403/04 , C07D403/08 , C07D405/04 , C07D409/04 , C07D413/02 , C07D413/08 , C07D417/08
CPC分类号： C07D249/08 , C07D401/04 , C07D403/04 , C07D403/08 , C07D405/04 , C07D409/04 , C07D413/08 , C07D417/08
摘要： Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.
摘要翻译： 结构式I的三唑衍生物是11b-羟基类固醇脱氢酶-1的选择性抑制剂。 该化合物可用于治疗糖尿病，例如非胰岛素依赖性糖尿病（NIDDM），高血糖症，肥胖症，胰岛素抵抗，血脂异常，高脂血症，高血压，代谢综合征和与NIDDM相关的其他症状。
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9.发明申请11-Beta-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia 失效用于治疗糖尿病，肥胖和血脂异常的11-β-羟基类固醇脱氢酶1抑制剂公开(公告)号：US20050070720A1
公开(公告)日：2005-03-31
申请号：US10502967
申请日：2003-01-28
申请人： James Balkovec , Rolf Thieringer , Steven Mundt , Anne Hermanowski-Vosatka , Donald Graham , Gool Patel , Susan Aster , Sherman Waddell , Steven Olson , Milana Maletic
发明人： James Balkovec , Rolf Thieringer , Steven Mundt , Anne Hermanowski-Vosatka , Donald Graham , Gool Patel , Susan Aster , Sherman Waddell , Steven Olson , Milana Maletic
IPC分类号： A61K31/4196 , A61K31/437 , A61K31/438 , A61K31/439 , A61K31/4439 , A61K31/55 , A61K31/551 , A61K31/554 , A61K45/00 , A61K45/06 , A61P1/18 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/50 , A61P9/10 , A61P13/12 , A61P25/00 , A61P27/02 , A61P43/00 , C07D249/08 , C07D249/12 , C07D249/14 , C07D401/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/06 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/08 , C07D491/14 , C07D491/147 , C07D491/20 , C07D513/04
CPC分类号： A61K31/4196 , A61K45/06 , C07D249/08 , C07D249/12 , C07D249/14 , C07D401/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D471/04 , C07D487/04 , C07D491/14 , C07D513/04 , A61K2300/00
摘要： Compounds having Formula (I), including pharmaceutically acceptable salts and prodrugs thereof: are selective inhibitors of the 11β-HSD1 enzyme. They inhibit the 11β-HSD1-mediated conversion of cortisone and other 11-keto-glucocorticoids to cortisol and other 11β-hydroxy-glucocorticoids. The 11β-HSD1 inhibitors therefore decrease the amount of cortisol in target tissues, thereby modulating the effects of cortisol. Modulation of cortisol may be effective in controlling non-insulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM or with excess cortisol in the body.
摘要翻译： 具有式（I）的化合物，包括其药学上可接受的盐和前药：是11beta-HSD1酶的选择性抑制剂。 它们抑制了11beta-HSD1介导的可的松和其他11-酮糖皮质激素转化为皮质醇和其他11β-羟基 - 糖皮质激素的转化。 因此，11beta-HSD1抑制剂减少了靶组织中皮质醇的量，从而调节皮质醇的作用。 调节皮质醇可能有效控制非胰岛素依赖型糖尿病（NIDDM），高血糖症，肥胖症，胰岛素抵抗，血脂异常，高脂血症，高血压，综合征X，以及与NIDDM相关的其他症状或体内过量的皮质醇。
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公开(公告)号：US20070149761A1
公开(公告)日：2007-06-28
申请号：US10584810
申请日：2005-01-06
申请人： Donald Graham , Amy Simcoe , Steven Ludmerer , Osvaldo Flores , Robert LaFemina
发明人： Donald Graham , Amy Simcoe , Steven Ludmerer , Osvaldo Flores , Robert LaFemina
IPC分类号： C12Q1/68 , C07K14/00 , C07K16/00 , A61K38/00 , C07K17/00 , C07K2/00 , C07K4/00 , C07K5/00 , C07K7/00
CPC分类号： C07K14/005 , C07H21/00 , C07H21/04 , C12N9/127 , C12N2770/24222 , G01N2333/18 , G01N2333/9125 , G01N2500/04
摘要： The present invention features NS5B polypeptides from different clinically important HCV genotypes. The polypeptides can be used individually, or as part of a panel of RNA-dependent RNA polymerases, to evaluate the effectiveness of a compound to inhibit NS5B activity.
摘要翻译： 本发明特征来自不同临床重要HCV基因型的NS5B多肽。 多肽可以单独使用或作为一组RNA依赖性RNA聚合酶的一部分使用，以评估化合物抑制NS5B活性的有效性。
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