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    • 8. 发明申请
    • CRYSTALLINE STRUCTURE OF OXIDOSQUALENE SYNTHASE
    • 氧化亚烷基合成酶的结晶结构
    • US20090270506A1
    • 2009-10-29
    • US12041258
    • 2008-03-03
    • ARMIN RUFTANJA SCHULZ-GASCHRALF THOMA
    • ARMIN RUFTANJA SCHULZ-GASCHRALF THOMA
    • A61K31/192C12N9/90C12Q1/00A61P35/00G06F19/00A61P3/10A61P9/00C07C229/00
    • C12N9/90C07K16/40C07K2299/00C12Y504/99007
    • The present invention relates to crystal forms of mammalian OSC and the crystal structure information obtained from them, to methods of preparing such crystal forms, and to their use for the identification and/or design of inhibitors of OSC activity. A further subject matter of the invention are methods for the identification and/or design of inhibitor compounds of OSC activity, the inhibitor compounds of OSC activity identified by these methods and their use in pharmaceutical compositions for the treatment and/or prevention of diseases which are associated with OSC comprising hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, parasite infections and gallstones, and/or treatment and/or prophylaxis of impaired glucose tolerance, diabetes, tumors and/or hyperproliferative disorders, preferably for the treatment and/or prophylaxis of hypercholesterolemia and/or hyperlipemia.
    • 本发明涉及哺乳动物OSC的结晶形式和从它们获得的晶体结构信息,制备这种晶型的方法及其用于鉴定和/或设计OSC活性抑制剂的用途。 本发明的另一主题是用于鉴定和/或设计OSC活性的抑制剂化合物的方法,通过这些方法鉴定的OSC活性的抑制剂化合物及其在药物组合物中的用途,用于治疗和/或预防 与OSC相关,包括高胆固醇血症,高脂血症,动脉硬化,血管疾病,真菌病,寄生虫感染和胆结石,和/或治疗和/或预防糖耐量异常,糖尿病,肿瘤和/或过度增殖性疾病,优选用于治疗和/或预防 的高胆固醇血症和/或高脂血症。
    • 10. 发明公开
    • Crystal structure of oxidosqualene cyclase
    • Kristallstruktur von Oxidosqualenzyklase
    • EP1498482A2
    • 2005-01-19
    • EP04015106.0
    • 2004-06-28
    • F. HOFFMANN-LA ROCHE AG
    • Ruf, ArminSchulz-Gasch, TanjaThoma, Ralf
    • C12N9/90C30B7/00G01N23/20G06F17/50G01F19/00
    • C12Y504/99007C07K16/40C07K2299/00C12N9/90C30B7/00
    • The present invention relates to crystal forms of mammmalian OSC and the crystal structure information obtained from them, to methods of preparing such crystal forms, and to their use for the identification and/or design of inhibitors of OSC activity. A further subject matter of the invention are methods for the identification and/or design of inhibitor compounds of OSC activity, the inhibitor compounds of OSC activity identified by these methods and their use in pharmaceutical compositions for the treatment and/or prevention of diseases which are associated with OSC comprising hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, parasite infections and gallstones, and/or treatment and/or prophylaxis of impaired glucose tolerance, diabetes, tumors and/or hyperproliferative disorders, preferably for the treatment and/or prophylaxis of hypercholesterolemia and/or hyperlipemia.
    • 本发明涉及乳制品OSC的结晶形式及其获得的晶体结构信息,制备这种晶型的方法及其用于鉴定和/或设计OSC活性抑制剂的用途。 本发明的另一主题是用于鉴定和/或设计OSC活性的抑制剂化合物的方法,通过这些方法鉴定的OSC活性的抑制剂化合物及其在药物组合物中的用途,用于治疗和/或预防 与包括高胆固醇血症,高脂血症,动脉硬化,血管疾病,真菌病,寄生虫感染和胆结石的OSC相关联,和/或治疗和/或预防葡萄糖耐量降低,糖尿病,肿瘤和/或过度增殖性疾病,优选用于治疗和/或预防 的高胆固醇血症和/或高脂血症。