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1.发明授权11-&bgr;-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia 有权用于治疗糖尿病，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：US06730690B2
公开(公告)日：2004-05-04
申请号：US10457682
申请日：2003-06-09
申请人： Steven H. Olson , James M. Balkovec , Yuping Zhu
发明人： Steven H. Olson , James M. Balkovec , Yuping Zhu
IPC分类号： A61K314196
CPC分类号： C07D249/08
摘要： Compounds having Formula I, including pharmaceutically acceptable salts, hydrates and solvates thereof: are selective inhibitors of the 11&bgr;-HSD1 enzyme. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dylsipidemia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM.
摘要翻译： 具有式I的化合物，包括其药学上可接受的盐，水合物和溶剂化物：是11beta-HSD1酶的选择性抑制剂。 这些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，甲状腺脂肪血症，高脂血症，高血压，X综合征和与NIDDM相关的其他症状。
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2.发明授权11-beta-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia 有权用于治疗糖尿病，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：US07179802B2
公开(公告)日：2007-02-20
申请号：US10697547
申请日：2003-10-30
申请人： Steven H. Olson , James M. Balkovec , Yuping Zhu
发明人： Steven H. Olson , James M. Balkovec , Yuping Zhu
IPC分类号： A61K31/55 , A61P3/06 , C07D487/02
CPC分类号： C07D249/08
摘要： Compounds having Formula I, including pharmaceutically acceptable salts, hydrates and solvates thereof: are selective inhibitors of the 11β-HSD1 enzyme. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dylsipidernia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM.
摘要翻译： 具有式I的化合物，包括其药学上可接受的盐，水合物和溶剂化物：是11beta-HSD1酶的选择性抑制剂。 这些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，二亚型癫痫，高脂血症，高血压，综合征X和与NIDDM相关的其他症状。
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3.发明授权Substituted succinic acid metallo-&bgr;-lactamase inhibitors and their use in treating bacterial infections 失效取代的琥珀酸金属-β-内酰胺酶抑制剂及其在治疗细菌感染中的应用公开(公告)号：US06630510B1
公开(公告)日：2003-10-07
申请号：US09697415
申请日：2000-10-26
IPC分类号： C07C5510
CPC分类号： C07D307/91 , C07C57/38 , C07C57/58 , C07C59/64 , C07C69/612 , C07C69/734 , C07D231/12 , C07D233/56 , C07D249/08 , C07D333/20 , C07D405/06 , C07D409/06
摘要： This invention relates to novel substituted succinic acid metallo-&bgr;-lactamase inhibitors which are useful potentiators of &bgr;-lactam antibiotics. Accordingly, the present invention provides a method of treating bacterial infections in animals or humans which comprises administering, together with a b-lactam antibiotic, a therapeutically effective amount of a compound of formula I: including pharmaceutically acceptable salts, prodrugs, anhydrides, and solvates thereof.
摘要翻译： 本发明涉及新型取代的琥珀酸金属-β-内酰胺酶抑制剂，其是β-内酰胺抗生素的有效增强剂。 因此，本发明提供了治疗动物或人类细菌感染的方法，其包括与β-内酰胺抗生素一起施用治疗有效量的式I化合物：包括其药学上可接受的盐，前药，酸酐和溶剂合物 其中。
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4.发明授权11-β-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：US07329683B2
公开(公告)日：2008-02-12
申请号：US10502967
申请日：2003-01-28
申请人： James M. Balkovec , Rolf Thieringer , Steven S. Mundt , Anne Hermanowski-Vosatka , Donald W. Graham , Gool F. Patel , Susan D. Aster , Sherman T. Waddell , Steven H. Olson , Milana Maletic
发明人： James M. Balkovec , Rolf Thieringer , Steven S. Mundt , Anne Hermanowski-Vosatka , Donald W. Graham , Gool F. Patel , Susan D. Aster , Sherman T. Waddell , Steven H. Olson , Milana Maletic
IPC分类号： A61K31/4196 , C07D249/16
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及其他与NIDDM相关的症状或与身体中过量的皮质醇有关
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5.发明授权Triazole derivatives as inhibitors of 11-β hydroxysteroid dehydrogenase-1 有权作为11-和bgr的抑制剂的三唑衍生物 羟基类固醇脱氢酶-1公开(公告)号：US08026264B2
公开(公告)日：2011-09-27
申请号：US10558454
申请日：2004-05-26
申请人： Sherman T. Waddell , Gina M. Santorelli , Milana M. Maletic , Aaron H. Leeman , Xin Gu , Donald W. Graham , James M. Balkovec , Susan D. Aster
发明人： Sherman T. Waddell , Gina M. Santorelli , Milana M. Maletic , Aaron H. Leeman , Xin Gu , Donald W. Graham , James M. Balkovec , Susan D. Aster
IPC分类号： A61K31/4196 , C07D249/08
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11-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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![1H-benzo[F]indazol-5-YL derivatives as selective glucocorticoid receptor modulators](/abs-image/US/2009/12/01/US07625937B2/abs.jpg.150x150.jpg)
6.发明授权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：US07625937B2
公开(公告)日：2009-12-01
申请号：US11904186
申请日：2007-09-26
IPC分类号： A61K31/416 , A61K31/415 , C07D487/00
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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7.发明申请TRIAZOLE DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE-1 审中-公开作为11-羟基脱氢酶脱氢酶-1的抑制剂的三唑衍生物公开(公告)号：US20090181994A1
公开(公告)日：2009-07-16
申请号：US12364902
申请日：2009-02-03
申请人： Sherman T. Waddell , Gina M. Santorelli , Milana M. Maletic , Aaron H. Leeman , Xin Gu , Donald W. Graham , James M. Balkovec , Susan D. Aster
发明人： Sherman T. Waddell , Gina M. Santorelli , Milana M. Maletic , Aaron H. Leeman , Xin Gu , Donald W. Graham , James M. Balkovec , Susan D. Aster
IPC分类号： A61K31/4196 , C07D249/08 , A61K31/506 , A61P25/28
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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8.发明授权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：US07282591B2
公开(公告)日：2007-10-16
申请号：US10508897
申请日：2003-04-08
IPC分类号： C07D487/14
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：US06864278B2
公开(公告)日：2005-03-08
申请号：US10484234
申请日：2002-07-12
申请人： James M. Balkovec , Bruno Tse
发明人： James M. Balkovec , Bruno Tse
IPC分类号： A61P31/10 , C07D309/12 , C07D493/04 , C07C69/753 , A61K31/19 , C07C69/757
CPC分类号： C07D493/04 , C07D309/12
摘要： Sordarin derivatives prepared from C-11-hydroxysordarin are antifungal agents useful in the treatment and/or prevention of human and animal fungal infections, as well as in the control of phytopathogenic fungi in crops.
摘要翻译： 由C-11-羟基司他丁制备的Sordarin衍生物是用于治疗和/或预防人和动物真菌感染以及控制作物中植物病原真菌的抗真菌剂。
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公开(公告)号：US5948753A
公开(公告)日：1999-09-07
申请号：US58657
申请日：1993-05-04
摘要： Certain propanolamine compounds are described which have a cyclohexapeptidyl nucleus and which possess antibiotic activity with physical properties suitable for direct use in therapeutic compositions. A process for their preparation is also described.
摘要翻译： 描述了具有环己基肽基核并且具有适于直接用于治疗组合物的物理性质的抗生素活性的某些丙醇胺化合物。 还描述了其制备方法。
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