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公开(公告)号：US20140094462A1
公开(公告)日：2014-04-03
申请号：US13781000
申请日：2013-02-28
申请人： Sara Buhrlage , Chris Dockendorff , Mike Foley , Han-Je Kim , Andrew Germain , Lawrence MacPherson , Partha Nag , Stuart Schreiber , Amal Ting , Michel Weiwer , Willmen Youngsaye
发明人： Sara Buhrlage , Chris Dockendorff , Mike Foley , Han-Je Kim , Andrew Germain , Lawrence MacPherson , Partha Nag , Stuart Schreiber , Amal Ting , Michel Weiwer , Willmen Youngsaye
IPC分类号： C07D498/04 , C07D413/04 , C07D273/01
CPC分类号： C07D273/01 , C07D273/02 , C07D413/04 , C07D413/12 , C07D498/04 , C07D498/08
摘要： Sonic Hedgehog modulators and methods of use thereof are provided for.
摘要翻译： 提供了声刺猬调节剂及其使用方法。
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公开(公告)号：US20060078969A1
公开(公告)日：2006-04-13
申请号：US11175021
申请日：2005-07-05
申请人： Gerald Crabtree , Stuart Schreiber , David Spencer , Thomas Wandless , Steffan Ho , Peter Belshaw
发明人： Gerald Crabtree , Stuart Schreiber , David Spencer , Thomas Wandless , Steffan Ho , Peter Belshaw
IPC分类号： C07K14/705 , C07H21/04 , C12P21/04
CPC分类号： C07K14/705 , A61K38/00 , A61K47/6425 , C07D498/18 , C07F5/025 , C07H19/01 , C07K7/645 , C07K14/395 , C07K14/7051 , C07K14/71 , C07K2319/00 , C07K2319/02 , C07K2319/03 , C07K2319/035 , C07K2319/09 , C07K2319/20 , C07K2319/32 , C07K2319/42 , C07K2319/43 , C07K2319/60 , C07K2319/71 , C07K2319/715 , C07K2319/81 , C07K2319/90 , C12N15/1055 , C12N15/62 , C12N15/63 , C12N15/67 , C12P15/00
摘要： Dimerization and oligomerization of proteins are general biological control mechanisms that contribute to the activation of cell membrane receptors, transcription factors, vesicle fusion proteins, and other classes of intra- and extracellular proteins. We have developed a general procedure for the regulated (inducible) dimerization or oligomerization of intracellular proteins. In principle, any two target proteins can be induced to associate by treating the cells or organisms that harbor them with cell permeable, synthetic ligands. To illustrate the practice of this invention, we have induced: (1) the intracellular aggregation of the cytoplasmic tail of the ζ chain of the T cell receptor (TCR)-CD3 complex thereby leading to signaling and transcription of a reporter gene, (2) the homodimerization of the cytoplasmic tail of the Fas receptor thereby leading to cell-specific apoptosis (programmed cell death) and (3) the heterodimerization of a DNA-binding domain (Gal4) and a transcription-activation domain (VP16) thereby leading to direct transcription of a reporter gene. Regulated intracellular protein association with our cell permeable, synthetic ligands offers new capabilities in biological research and medicine, in particular, in gene therapy. Using gene transfer techniques to introduce our artificial receptors, one can turn on or off the signaling pathways that lead to the overexpression of therapeutic proteins by administering orally active “dimerizers” or “de-dimerizers”, respectively. Since cells from different recipients can be configured to have the pathway overexpress different therapeutic proteins for use in a variety of disorders, the dimerizers have the potential to serve “universal drugs”. They can also be viewed as cell permeable, organic replacements for therapeutic antisense agents or for proteins that would otherwise require intravenous injection or intracellular expression (e.g., the LDL receptor or the CFTR protein).
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公开(公告)号：US20060052424A1
公开(公告)日：2006-03-09
申请号：US10706877
申请日：2003-11-12
IPC分类号： A61K31/426 , A61K31/421 , A61K31/4166
CPC分类号： C07D487/04 , A61K31/4015 , A61K31/407 , A61K31/4166 , A61K31/421 , A61K31/426 , C07D491/10 , C07D495/10 , C12N9/6421
摘要： Compounds related to lactacystin and lactacystin β-lactone, pharmaceutical compositions containing the compounds, and methods of use.
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公开(公告)号：US20080070916A1
公开(公告)日：2008-03-20
申请号：US11714689
申请日：2007-03-06
IPC分类号： A61K31/438 , A61K31/435 , A61K31/5377 , A61P35/00 , C07D413/14 , C07D455/04 , C07D471/10 , C40B40/04
CPC分类号： C07D471/04 , C07D309/30 , C07D405/04 , C07D405/14 , C07D407/04 , C07D409/04 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/10
摘要： The present invention provides novel dihydropyrancarboxamide compounds of formula (I): and collections of these compounds, and provides methods for the synthesis of these compounds; wherein R1-R6 are as defined herein. Additionally, the present invention provides pharmaceutical compositions and methods for treating disorders such as proliferative diseases, and cancer, to name a few.
摘要翻译： 本发明提供新的式（I）二氢吡喃甲酰胺化合物：这些化合物的收集，并提供这些化合物的合成方法; 其中R 1〜R 6如本文所定义。 此外，本发明提供了用于治疗诸如增殖性疾病和癌症等疾病的药物组合物和方法。
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公开(公告)号：US20060035325A1
公开(公告)日：2006-02-16
申请号：US11038326
申请日：2005-01-18
IPC分类号： C07K14/715 , C07H21/04 , C12P21/06 , C12N15/86
CPC分类号： C07D498/18 , A61K38/00 , A61K47/6425 , A61K48/00 , C07F5/025 , C07H19/01 , C07K7/645 , C07K14/395 , C07K14/705 , C07K14/7051 , C07K14/71 , C07K2319/00 , C07K2319/02 , C07K2319/03 , C07K2319/035 , C07K2319/09 , C07K2319/20 , C07K2319/32 , C07K2319/42 , C07K2319/43 , C07K2319/60 , C07K2319/71 , C07K2319/715 , C07K2319/81 , C07K2319/90 , C12N15/62 , C12N15/63 , C12P15/00
摘要： We have developed a general procedure for the regulated (inducible) dimerization or oligomerization of intracellular proteins and disclose methods and materials for using that procedure to regulatably initiate cell-specific apoptosis (programmed cell death) in genetically engineered cells.
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公开(公告)号：US5447915A
公开(公告)日：1995-09-05
申请号：US920597
申请日：1992-08-28
申请人： Stuart Schreiber , Steven Burakoff
发明人： Stuart Schreiber , Steven Burakoff
IPC分类号： A61K38/00 , A61P31/12 , C07K5/06 , C07K5/078 , C07K5/08 , C07K5/097 , C07K5/12 , C07K7/64 , C12N7/06 , G01N33/566 , G01N33/569
CPC分类号： C07K5/06165 , C07K5/0823 , C07K7/64 , A61K38/00 , Y10S435/974
摘要： This invention relates to antiviral peptide compounds and to methods of inhibiting infection of human cells by viruses. This invention pertains more specifically to peptides that are chemically blocked at the amino- and carboxy-termini. In particular the invention relates to peptides comprised of prolylalanine or prolylphenylalanine compounds that have antiviral activity. The invention is specifically directed to methods for preventing infection of human cells in vivo and in vitro with the human immunodeficiency virus HIV-1 and methods for treating human infected with this and other viruses. The invention also relates to the diagnostic and therapeutic use of these antiviral peptide compounds.
摘要翻译： PCT No.PCT / US91 / 01142 Sec。 371日期：1992年8月28日 102（e）日期1992年8月28日PCT 1991年2月21日PCT PCT。 出版物WO91 / 13088 1991年9月5日，本发明涉及抗病毒肽化合物以及通过病毒抑制人细胞感染的方法。 本发明更具体涉及在氨基和羧基末端被化学封端的肽。 特别地，本发明涉及由具有抗病毒活性的脯氨酰丙氨酸或脯氨酰苯丙氨酸化合物组成的肽。 本发明具体涉及用人体免疫缺陷病毒HIV-1和/或用于治疗感染了这种和其他病毒的人的体内和体外人体细胞感染的方法。 本发明还涉及这些抗病毒肽化合物的诊断和治疗应用。
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公开(公告)号：US08951938B2
公开(公告)日：2015-02-10
申请号：US12340933
申请日：2008-12-22
申请人： Young-Tae Chang , Young-Hoon Ahn , Yun Kyung Kim , Bridget Wagner , Hyman A. Carrinski , Paul Clemons , Stuart Schreiber
发明人： Young-Tae Chang , Young-Hoon Ahn , Yun Kyung Kim , Bridget Wagner , Hyman A. Carrinski , Paul Clemons , Stuart Schreiber
CPC分类号： G01N33/5073 , G01N33/5061 , Y10S436/80
摘要： The present invention relates to the use of rosamine derivative compounds, as described herein, in detecting differentiated forms of a cell type of interest in a sample and in screening for compounds which inhibit differentiation of the cell type of interest. The candidate compound has the following structure:
摘要翻译： 本发明涉及如本文所述的用于检测样品中感兴趣的细胞类型的分化形式以及筛选抑制感兴趣的细胞类型分化的化合物的用途。 候选化合物具有以下结构：
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公开(公告)号：US20100323420A1
公开(公告)日：2010-12-23
申请号：US12684064
申请日：2010-01-07
CPC分类号： C07D498/18 , A61K38/00 , A61K47/6425 , A61K48/00 , C07F5/025 , C07H19/01 , C07K7/645 , C07K14/395 , C07K14/705 , C07K14/7051 , C07K14/71 , C07K2319/00 , C07K2319/02 , C07K2319/03 , C07K2319/035 , C07K2319/09 , C07K2319/20 , C07K2319/32 , C07K2319/42 , C07K2319/43 , C07K2319/60 , C07K2319/71 , C07K2319/715 , C07K2319/81 , C07K2319/90 , C12N15/62 , C12N15/63 , C12P15/00
摘要： We have developed a general procedure for the regulated (inducible) dimerization or oligomerization of intracellular proteins and disclose methods and materials for using that procedure to regulatably initiate cell-specific apoptosis (programmed cell death) in genetically engineered cells.
摘要翻译： 我们已经开发了细胞内蛋白质的调节（诱导型）二聚化或寡聚化的一般程序，并且公开了使用该方法在基因工程细胞中调节启动细胞特异性凋亡（程序性细胞死亡）的方法和材料。
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公开(公告)号：US20070093413A1
公开(公告)日：2007-04-26
申请号：US10919217
申请日：2004-08-16
CPC分类号： C12N9/80 , A01K2217/05 , A01K2217/075 , A61K31/00 , A61K31/165 , A61K31/407 , A61K38/00 , A61K48/00 , C07K5/126 , C07K14/4702 , C07K14/4703 , C07K2319/00 , C12N9/16
摘要： The present invention concerns the discovery that proteins encoded by a family of genes, termed here HDx-related genes, which are involved in the control of chromatin structure and, thus in transcription and translation. The present invention makes available compositions and methods that can be utilized, for example to control cell proliferation and differentiation in vitro and in vivo.
摘要翻译： 本发明涉及由一系列基因（称为HDx相关基因）编码的蛋白质的发现，其涉及染色质结构的控制，因此涉及转录和翻译。 本发明提供可用于例如在体外和体内控制细胞增殖和分化的组合物和方法。
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公开(公告)号：US20060239909A1
公开(公告)日：2006-10-26
申请号：US11386959
申请日：2006-03-22
申请人： Kenneth Anderson , James Bradner , Edward Greenberg , Teru Hideshima , Nicholas Kwiatkowski , Ralph Mazitschek , Stuart Schreiber , Jared Shaw , Stephen Haggarty
发明人： Kenneth Anderson , James Bradner , Edward Greenberg , Teru Hideshima , Nicholas Kwiatkowski , Ralph Mazitschek , Stuart Schreiber , Jared Shaw , Stephen Haggarty
IPC分类号： A61K51/00 , A61K39/395 , A61K33/36
CPC分类号： A61K38/05 , A61K31/35 , A61K31/357 , A61K31/422 , A61K31/4965 , A61K31/69 , A61K38/50 , A61K45/06 , A61K49/0008 , G01N33/5011 , A61K2300/00
摘要： The invention relates to methods of treating protein degradation disorders, such cellular proliferative disorders (e.g., cancer) and protein deposition disorders (e.g., neurodegenerative disorders). The invention provides methods and pharmaceutical compositions for treating these diseases using aggresome inhibitors or combinations of aggresome inhibitors and proteasome inhibitors. The invention further relates to methods and pharmaceutical compositions for treating multiple myeloma. New HDAC/TDAC inhibitors and aggresome inhibitors are also provided as well as synthetic methodologies for preparing these compounds.
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