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1. 发明申请

WO2008071169A2 METHOD FOR THE PRODUCTION OF SPECIFIC INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE, IN PARTICULAR TYPE 1 WITH BASIC NOR-OLEANAN OR NOR-URSAN FRAMEWORKS 审中-公开
标题翻译： PROCESS FOR11β-羟基类固醇脱氢酶的特异性抑制剂的制备中，特别是II型1 WITH NOR齐墩果烷OR NOR Ursan BASIC框架
公开(公告)号：WO2008071169A2
公开(公告)日：2008-06-19
申请号：PCT/DE2007002218
申请日：2007-12-10
申请人： UKSH SCHLESWIG HOLSTEIN , BLUM ANDREAS , MASER EDMUND
发明人： BLUM ANDREAS , MASER EDMUND
CPC分类号： C07J63/00 , A61K31/56
摘要： The invention relates to a method for modifying non-specific inhibitors of 11 beta hydroxysteroid dehydrogenase (11 beta HSD) with a basic pentacyclic framework of the oleanan and ursan type, in order to be able to synthesize chemical compounds which inhibit 11 beta hydroxysteroid dehydrogenase and which, preferably, inhibit the substantially specific iso form of 11 beta hydroxysteroid dehydrogenase type 1, and which thus have substantially no inhibiting effect on the iso form of 11 beta hydroxysteroid dehydrogenase type 2 (11 beta HSD2). The invention further relates to novel chemical compounds with basic nor-oleanan or non-ursan frameworks. These inhibitors act as substantially specific inhibitors of 11 beta HSD1 and are thus suitable for the treatment and prevention of diabetes, metabolic syndrome, adiposis, corpulence, overweight, hyperlipoproteinemia, hypoglycemia, hyperinsulinemia, arteriosclerosis, dementia, depressions, osteoporosis, glaucoma, or virus diseases.
摘要翻译：本发明涉及一种方法，用于修改所述11β-羟基类固醇脱氢酶（11β-HSD）的与齐墩果烷和乌苏烷型pentacyclischem骨干，这使得能够制造出抑制11β-羟基类固醇脱氢酶和化学化合物的非特异性作用酶抑制剂优选基本上特定1型抑制11β-羟基类固醇脱氢酶（11β-HSD1）的同种型，而2型包括（11β-HSD2）实质上靠在11β-羟基类固醇脱氢酶的同种型没有抑制活性。此外，本发明涉及具有去甲齐墩果烷或标准Ursan骨干新化合物。这些抑制剂充当11β-HSD1是基本上特异性抑制剂，并因此关于治疗和预防某些糖尿病，代谢综合征，肥胖症，肥胖，肥胖症，高脂蛋白血症，高血糖症，高胰岛素血症，动脉粥样硬化，痴呆，抑郁症，Osteroporese，青光眼或病毒疾病的合适的。

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