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3. 发明申请

US20100184758A1 BETA CARBOLINE DERIVATIVES AS ANTIDIABETIC COMPOUNDS 审中-公开
标题翻译：作为抗菌化合物的碳氢化合物衍生物
公开(公告)号：US20100184758A1
公开(公告)日：2010-07-22
申请号：US12668822
申请日：2008-07-15
申请人： Peter H. Dobbelaar , Wu Du , Liangqin Guo , William K. Hagmann , Shuwen He , Tianying Jian , Jian Liu , Ravi P. Nargund , Alexander Pasternak , Shrenik K. Shah , Quang T. Truong , Zhixiong Ye , James Deliureficio , Raman Bakshi
发明人： Peter H. Dobbelaar , Wu Du , Liangqin Guo , William K. Hagmann , Shuwen He , Tianying Jian , Jian Liu , Ravi P. Nargund , Alexander Pasternak , Shrenik K. Shah , Quang T. Truong , Zhixiong Ye , James Deliureficio , Raman Bakshi
IPC分类号： A61K31/5377 , C07D471/14 , A61K31/437 , C07D413/14 , C07D403/14 , A61K31/501 , A61K31/4995 , A61K31/506 , A61P3/10 , A61P3/04 , A61P3/00 , A61P3/06 , A61P9/12
CPC分类号： C07D471/04
摘要： Beta-carboline derivatives of structural formula I are selective antagonists of the somatostatin subtype receptor 3 (SSTR3) and are useful for the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including hyperglycemia, insulin resistance, obesity, lipid disorders, and hypertension. The compounds are also useful for the treatment of depression and anxiety.
摘要翻译：结构式I的β-咔啉衍生物是生长抑素亚型受体3（SSTR3）的选择性拮抗剂，可用于治疗2型糖尿病和通常与该疾病相关的病症，包括高血糖症，胰岛素抵抗，肥胖症，脂质障碍和高血压。这些化合物也可用于治疗抑郁症和焦虑症。

4. 发明授权

US07064202B1 Camptothecin intermediates and prodrugs and methods of preparation thereof 失效
标题翻译：喜树碱中间体和前药及其制备方法
公开(公告)号：US07064202B1
公开(公告)日：2006-06-20
申请号：US10843821
申请日：2004-05-12
申请人： Thomas G. Burke, deceased , Dennis P. Curran , Wu Du
发明人： Thomas G. Burke, deceased , Dennis P. Curran , Wu Du
IPC分类号： C07D413/04 , C07D487/12
CPC分类号： C07D487/14
摘要： The present invention relates to novel intermediates and prodrugs of camptothecin and related analogs.
摘要翻译：本发明涉及喜树碱和相关类似物的新型中间体和前药。

5. 发明授权

US06372906B1 Synthesis of silyl camptothecins and silyl homocamptothecins 有权
标题翻译：甲硅烷基喜树碱和甲硅烷基高丝念菌素的合成
公开(公告)号：US06372906B1
公开(公告)日：2002-04-16
申请号：US09833757
申请日：2001-04-12
申请人： Dennis P. Curran , Wu Du
发明人： Dennis P. Curran , Wu Du
IPC分类号： C07D49122
CPC分类号： C07D491/22 , C07F7/0814
摘要： A method of synthesizing 7-silyl camptothecins and 7-silyl homocamptothecins includes the step of mixing a camptothecin or a homocamptothecin having hydrogen at the C7 position with a silyl radical generator and a silyl radical precursor under conditions to generate a silyl radical. SiR1R2R3 wherein R1, R2 and R3 are independently a C1-10 alkyl group, a C2-10 alkenyl group, a C2-10 alkynyl group, an aryl group, —(CH2)mR11 or SiR12R13R14, wherein m is an integer within the range of 1 through 10 and R11 is a hydroxy group, an alkoxy group, an amino group, an alkylamino group, a dialkylamino group, F, Cl, a cyano group, —SRc or a nitro group, and wherein R12, R13 and R14 are independently the same or different an alkyl group or an aryl group.
摘要翻译：合成7-甲硅烷基喜树碱和7-甲硅烷基高丝念珠菌的方法包括在产生甲硅烷基的条件下将喜树碱或在C7位具有氢的高喜树碱与甲硅烷基自由基产生剂和甲硅烷基自由基前体混合的步骤。 SiR1R2R3，其中R1，R2和R3独立地为C1-10烷基，C2-10烯基，C2-10炔基，芳基， - （CH2）mR11或SiR12R13R14，其中m是在该范围内的整数 1至10，R 11为羟基，烷氧基，氨基，烷基氨基，二烷基氨基，F，Cl，氰基，-SRc或硝基，其中R12，R13和R14为独立地相同或不同的烷基或芳基。

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