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11.发明授权Triazole derivatives as inhibitors of 11-β-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：US07504402B2
公开(公告)日：2009-03-17
申请号：US11011889
申请日：2004-12-14
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 , C07D401/04 , C07D403/04 , C07D413/02
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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公开(公告)号：US06849636B2
公开(公告)日：2005-02-01
申请号：US10739716
申请日：2003-12-18
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 , 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.
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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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公开(公告)号：US5741775A
公开(公告)日：1998-04-21
申请号：US489976
申请日：1995-06-13
摘要： There are disclosed compounds of the general formula ##STR1## wherein all substituents are defined herein. The compounds are useful as antibiotic and antifungal agents.
摘要翻译： 公开了通式“IMAGE”的化合物，其中所有取代基均在本文中定义。 该化合物可用作抗生素和抗真菌剂。
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公开(公告)号：US5330973A
公开(公告)日：1994-07-19
申请号：US495198
申请日：1990-03-19
IPC分类号： A61K31/40 , A61K38/00 , A61P31/00 , A61P31/04 , A61P31/10 , A61P33/02 , C07D487/14 , C07K7/56 , C07K5/12 , C07K7/06 , A61K37/02
摘要： The present invention is directed to water-soluble derivatives of antibiotic lipopeptides. The derivatives have good solubility properties in aqueous medium, rendering them more useful as therapeutic agents.
摘要翻译： 本发明涉及抗生素脂肽的水溶性衍生物。 该衍生物在水性介质中具有良好的溶解性，使其更有用作治疗剂。
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公开(公告)号：US5233023A
公开(公告)日：1993-08-03
申请号：US738058
申请日：1991-07-30
CPC分类号： C07K7/56
摘要： A facile process for preparing a compound of the formula ##STR1## or a salt thereof, wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, X.sup.1 Y and Z are as defined in the specification, by direct phosphorylation of the corresponding phenolic compound with tetrabenzyl pyrophosphate in the presence of lithium hydroxide is described.
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公开(公告)号：US20110172225A1
公开(公告)日：2011-07-14
申请号：US12680472
申请日：2008-09-25
申请人： James M. Balkovec , Phieng Siliphaivanh , Frances A. Bouffard , Roland A. Bouffard , Michael R. Peel , Weiming Fan , Ahmed Mamai , Sarah Dimick Gray
发明人： James M. Balkovec , Phieng Siliphaivanh , Frances A. Bouffard , Roland A. Bouffard , Michael R. Peel , Weiming Fan , Ahmed Mamai , Sarah Dimick Gray
IPC分类号： A61K31/5377 , C07D311/78 , C07D405/12 , C07D407/12 , C07D413/12 , C07D405/14 , A61K31/352 , A61K31/453 , A61K31/4025 , A61K31/422 , A61K31/4178 , A61K31/496 , A61K31/4545 , A61K31/454 , A61P31/10
CPC分类号： C07J71/0005
摘要： Novel derivatives of enfumafungin are disclosed herein, along with their, pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-β-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.
摘要翻译： 本文公开了enfumafungin的新型衍生物及其药学上可接受的盐，水合物和前药。 还公开了包含这种化合物的组合物，制备这些化合物的方法和使用这些化合物作为抗真菌剂和/或（1,3） - ＆bgr-D-葡聚糖合酶抑制剂的方法。 所公开的化合物，其药学上可接受的盐，水合物和前药，以及包含这些化合物，盐，水合物和前药的组合物可用于治疗和/或预防真菌感染和相关疾病和病症。
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公开(公告)号：US20090258913A1
公开(公告)日：2009-10-15
申请号：US12083047
申请日：2006-10-16
申请人： Sherman T. Waddell , James M. Balkovec , Nancy J. Kevin , Xin Gu
发明人： Sherman T. Waddell , James M. Balkovec , Nancy J. Kevin , Xin Gu
IPC分类号： A61K31/4245 , C07D413/08 , A61P3/10
CPC分类号： C07D413/08
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.
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公开(公告)号：US20080262051A1
公开(公告)日：2008-10-23
申请号：US12082933
申请日：2008-04-15
IPC分类号： A61K31/4245 , A61P35/00
CPC分类号： A61K31/4196 , A61K31/4245
摘要： The present invention provides a method for the treatment or prevention of conditions which can be ameliorated by Smo antagonism, which method comprises administration to a patient in need thereof of an effective amount of a compound of formula I or a composition comprising a compound of formula I: or a pharmaceutically acceptable salt or solvate thereof; wherein: 2 of X, Y and Z represent nitrogen atoms, and the other represents an oxygen atom; R1 and R2 are taken together with the atom to which they are attached and represent a cyclobutyl ring, optionally substituted with 1-2 fluorine atoms, and R3 represents hydrogen or a fluorine atom; or R1 represents methyl, R2 represents methyl or a fluorine atom and R3 represents a fluorine atom.
摘要翻译： 本发明提供了治疗或预防可通过Smo拮抗作用改善的病症的方法，该方法包括向有需要的患者施用有效量的式I化合物或包含式I化合物的组合物 ：或其药学上可接受的盐或溶剂合物; 其中：X，Y和Z中的2个表示氮原子，另一个表示氧原子; R 1和R 2与它们所连接的原子一起表示任选被1-2个氟原子取代的环丁基环，R“ 3表示氢或氟原子; 或R 1表示甲基，R 2表示甲基或氟原子，R 3表示氟原子。
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