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11. 发明申请

US20030114493A1 C10 carbonate substituted taxanes 失效
公开(公告)号：US20030114493A1
公开(公告)日：2003-06-19
申请号：US09776274
申请日：2001-02-02
发明人： Robert A. Holton
IPC分类号： A61K031/4427 , A61K031/381 , A61K031/337
CPC分类号： C07D305/14
摘要： Taxanes having a carbonate substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.

12. 发明申请

US20030069277A1 Synthesis of epothilones, intermediates thereto and analogues thereof 审中-公开
公开(公告)号：US20030069277A1
公开(公告)日：2003-04-10
申请号：US10135433
申请日：2002-04-30
发明人： Samuel J. Danishefsky , Peter Bertinato , Dai-Shi Su , Dongfang Meng , Ting-Chao Chou , Ted Kamenecka , Erik J. Sorensen , Aaron Balog , Kenneth A. Savin , Scott Kuduk , Christina Harris , Xiu-Guo Zhang , Joseph R. Bertino
IPC分类号： C07D417/02 , C07D413/02 , C07D47/02 , A61K031/4427 , A61K031/4178 , A61K031/427 , A61K031/365
CPC分类号： A61K31/704 , A61K31/335 , A61K31/337 , A61K31/425 , A61K31/475 , A61K31/70 , A61K45/06 , C07C59/76 , C07C69/007 , C07C69/738 , C07D277/24 , C07D313/00 , C07D413/06 , C07D417/06 , C07D417/14 , C07D493/04 , C07F7/1804 , C07F7/1892 , A61K2300/00
摘要： The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof, useful in the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. Also provided are intermediates useful for preparing said epothilones.

13. 发明申请

US20020086884A1 Anticancer agents based on regulation of protein prenylation 失效
标题翻译：基于蛋白异戊烯化调节的抗癌剂
公开(公告)号：US20020086884A1
公开(公告)日：2002-07-04
申请号：US09983232
申请日：2001-10-23
发明人： Seth D. Rose , Scott R. Lefler , Steven R. Ottersberg , Ann Y. Kim , Karl J. Okolotowicz , Rosemarie F. Hartman
IPC分类号： A61K031/665 , C07C069/63 , A61K031/4427 , A61K031/4178 , A61K031/336
CPC分类号： A61K31/66 , A61K31/20 , C07C69/63 , C07C217/46 , C07C219/20 , C07D303/32 , C07D303/48 , C07F9/091
摘要： Oncoproteins such as Ras and RhoB are known to induce cell division in an unrestrained manner when such proteins are localized at the inner surface of a cancer cell membrane. The localization is effected by the prenylation reaction, whereby a hydrophobic group (e.g. a farnesyl group) is attached to the protein in the presence of an enzyme (e.g. farnesyl protein transferase). Deactivation of the prenylation enzyme through covalent modification can therefore ultimately result in the mitigation and/or cessation of cancer cell growth. Various prenylation inhibitors having the necessary structural groups to bond covalently, or essentially irreversibly, to the prenylation enzyme include carbonyl or thiocarbonyl compounds (or masked versions of these compounds) and alpha oxo-epoxides bonded to a hydrophobic, substrate-mimicking group. The carbonyl or thiocarbonyl compounds also contain a nucleofugal atom or group to enhance the tendency to form covalent bonds.
摘要翻译：已知当诸如Ras和RhoB的癌蛋白定位在癌细胞膜的内表面时，诸如Ras和RhoB的癌蛋白以无限制的方式诱导细胞分裂。定位通过异戊烯化反应进行，由此在酶（例如法呢基蛋白转移酶）的存在下将疏水基团（例如法呢基）连接到蛋白质上。因此，通过共价修饰来停用异戊烯基化酶可最终导致癌细胞生长的缓解和/或停止。具有与异戊烯基化酶共价或基本上不可逆地键合的必需结构基团的各种异戊二烯基化抑制剂包括与疏水性底物模拟基团键合的羰基或硫代羰基化合物（或这些化合物的掩蔽型）和α氧代环氧化物。羰基或硫代羰基化合物还含有核原子或基团以增强形成共价键的倾向。

14. 发明申请

US20020065305A1 C7 heterosubstituted acetate taxanes 失效
标题翻译： C7异取代乙酸酯紫杉烷
公开(公告)号：US20020065305A1
公开(公告)日：2002-05-30
申请号：US09776393
申请日：2001-02-02
发明人： Robert A. Holton
IPC分类号： A61K031/4427 , A61K031/337 , A61K031/381 , C07D35/14
CPC分类号： C07D409/12 , C07D305/14 , C07D405/12 , C07D405/14 , C07D407/12 , C07D407/14 , C07D409/14
摘要： Taxanes having a heterosubstituted acetate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.
摘要翻译： C（7）具有异构取代的乙酸酯取代基，C（10）的羟基取代基，C（2），C（9），C（14）和侧链取代基的紫杉烷。

15. 发明申请

US20010027200A1 PPARgamma modulators 失效
标题翻译： PPARγ调节剂
公开(公告)号：US20010027200A1
公开(公告)日：2001-10-04
申请号：US09741415
申请日：2000-12-19
申请人： Tularik Inc.
发明人： Fabienne De la Brouse-Elwood , Jin-Long Chen , Timothy D. Cushing , John A. Flygare , Jonathan B. Houze , Juan C. Jaen , Lawrence R. McGee , Shi-Chang Miao , Steven Marc Rubenstein , Patrick C. Kearney
IPC分类号： A61K031/4427 , A61K031/4412
CPC分类号： C07D213/70 , C07C311/21 , C07D213/65 , C07D215/20 , C07D217/04 , C07D405/12
摘要： Modulators of PPARnull activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.
摘要翻译：提供了PPARγ活性的调节剂，其可用于治疗诸如II型糖尿病和肥胖症的药物组合物和方法。

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