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51. 发明申请

US20100093610A1 ROMIDEPSIN-BASED TREATMENTS FOR CANCER 审中-公开
标题翻译：基于ROMIDEPSIN的癌症治疗
公开(公告)号：US20100093610A1
公开(公告)日：2010-04-15
申请号：US12521392
申请日：2007-12-28
申请人： Nicholas H. Vrolijk , Gregory L. Verdine
发明人： Nicholas H. Vrolijk , Gregory L. Verdine
IPC分类号： A61K38/07 , A61P35/00
CPC分类号： C07K11/02 , A61F13/15252 , A61F13/49 , A61F13/505 , A61K38/15 , A61K38/1816 , A61K45/06 , C12P21/02 , A61K2300/00
摘要： The invention provides an improved process for preparing romidepsin. The process involves producing, purifying, or storing romidepsin under conditions that prevent the formation of undesired adducts. Purifying romidepsin at an apparent pH lower than approximately 6.0 (e.g., between an apparent pH of 4.0 and 6.0) has been discovered to prevent the reduction of the disulfide bond of romidepsin and the subsequent formation of dimerized, oligomerized, or polymerized adducts. The invention also provides pharmaceutical compositions of monomeric romidepsin free of dimerized, oligomerized, or polymerized adducts.
摘要翻译：本发明提供了一种制备罗美甜素的改进方法。该方法包括在防止形成不需要的加合物的条件下生产，纯化或存储罗非曲松。已经发现在表观pH低于约6.0（例如，表观pH为4.0和6.0之间）的情况下净化罗非曲松，以防止罗非替辛的二硫键的还原和随后形成二聚，低聚或聚合的加合物。本发明还提供了不含二聚，低聚或聚合的加合物的单体罗非替克的药物组合物。

52. 发明申请

US20100081611A1 STABILIZED MAML PEPTIDES AND USES THEREOF 有权
标题翻译：稳定的乳腺肽及其用途
公开(公告)号：US20100081611A1
公开(公告)日：2010-04-01
申请号：US12478504
申请日：2009-06-04
申请人： James Bradner , Raymond Moellering , Gregory L. Verdine
发明人： James Bradner , Raymond Moellering , Gregory L. Verdine
IPC分类号： A61K38/12 , C07K7/50 , A61P35/00 , C07K7/08
CPC分类号： C07K14/47 , A61K38/00
摘要： Stably cross-linked a polypeptides related to human MAML are described. These cross-linked polypeptides contain at least two modified amino acids that together form an internal cross-link or tether that can help to stabilize the alpha-helical secondary structure that is thought to be important for binding of MAML peptides to the Notch transcription complex, a complex that includes ICN and CSL.
摘要翻译：描述了稳定交联的与人MAML相关的多肽。这些交联的多肽含有至少两个修饰的氨基酸，它们一起形成可以有助于稳定被认为对MAML肽与Notch转录复合物的结合重要的α-螺旋二级结构的内部交联或系链，一个包含ICN和CSL的复合体。

53. 发明授权

US06686148B1 Methods for targeting RNA molecules 失效
标题翻译：靶向RNA分子的方法
公开(公告)号：US06686148B1
公开(公告)日：2004-02-03
申请号：US09515721
申请日：2000-02-29
申请人： Ling X. Shen , Gregory L. Verdine , James P. Basilion , Vincent P. Stanton, Jr.
发明人： Ling X. Shen , Gregory L. Verdine , James P. Basilion , Vincent P. Stanton, Jr.
IPC分类号： C12Q168
CPC分类号： G01N33/5008 , C12N15/111 , C12N2310/11 , C12N2310/315 , C12N2320/11 , G01N2500/04
摘要： Methods are described for identifying an RNA target for an allele-specific RNA inhibitor by identifying a sequence variance in an RNA encoded by a gene of interest, and determining whether the secondary structure of the RNA comprising the variance differs from that of an otherwise identical RNA not comprising the variance.
摘要翻译：描述了通过鉴定由目的基因编码的RNA的序列方差，以及确定包含方差的RNA的二级结构是否不同于其它相同的RNA的方法来鉴定等位基因特异性RNA抑制剂的RNA靶标的方法不包括方差。

54. 发明授权

US06369237B1 DNA glycosylase inhibitors, and uses related thereto 失效
标题翻译： DNA糖基化酶抑制剂及其用途
公开(公告)号：US06369237B1
公开(公告)日：2002-04-09
申请号：US08812653
申请日：1997-03-07
申请人： Gregory L. Verdine , Li Deng
发明人： Gregory L. Verdine , Li Deng
IPC分类号： C07D20700
CPC分类号： C07F9/65616 , C07D207/12
摘要： The present invention pertains to novel inhibitors of DNA glycosylases. The invention is based at least in part on the observation that specific substituted pyrrolidines, and analogs thereof, are capable of specifically inhibiting DNA glycosylases, e.g., as transition state analogs, and consequently are useful for modulation of DNA repair. Such compounds can, for example, be used for treating subjects having a disorder associated with excessive cell proliferation, such as in the treatment of various cancers. Furthermore, these glycosylase inhibitors can be used as anti-bacterial, anti-viral and anti-fungal agents.
摘要翻译：本发明涉及DNA糖基化酶的新型抑制剂。本发明至少部分地基于以下观察结果：特异性取代的吡咯烷及其类似物能够特异性抑制DNA糖基化酶，例如作为转变态类似物，因此可用于调节DNA修复。这样的化合物可以例如用于治疗与过度细胞增殖相关的病症的受试者，例如治疗各种癌症。此外，这些糖基化酶抑制剂可以用作抗菌，抗病毒和抗真菌剂。

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