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公开(公告)号：US07393865B2
公开(公告)日：2008-07-01
申请号：US11156252
申请日：2005-06-17
IPC分类号： A61K31/44 , A61K31/425 , A61K31/381 , C07D277/20 , C07D333/52 , C07D409/06
CPC分类号： C07D409/04 , C07D333/58 , C07D417/04
摘要： Compounds having the following structure (I): including stereoisomers, prodrugs, and pharmaceutically acceptable salts, esters and solvates thereof, wherein R1, R2, R3a, R3b, L1, L2 and n are as defined herein. Such compounds generally function as H1 receptor ligands, and thus have utility as sleep inducing agents. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.
摘要翻译： 具有以下结构（I）的化合物：包括其立体异构体，前药和药学上可接受的盐，酯和溶剂化物，其中R 1，R 2，R 3a R 3b，L 1，L 2和n如本文所定义。 这些化合物通常用作H 1 H 1受体配体，因此可用作睡眠诱导剂。 还公开了含有结构（I）化合物的药物组合物以及与其用途有关的方法。
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12.发明授权Modified oligonucleotides and intermediates useful in nucleic acid therapeutics 失效用于核酸治疗的修饰寡核苷酸和中间体
公开(公告)号：US5625050A
公开(公告)日：1997-04-29
申请号：US221425
申请日：1994-03-31
申请人： Graham Beaton , Eric F. Fisher
发明人： Graham Beaton , Eric F. Fisher
IPC分类号： C07D473/18 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K31/7088 , A61P31/12 , A61P35/00 , C07D405/04 , C07D473/34 , C07H19/06 , C07H19/16 , C07H21/00 , C07H21/02 , C07H21/04
摘要： The present invention provides nuclease resistant 3'-carbon modified oligonucleotides that can be used in the field of nucleic acid therapeutics and diagnostics. The modified oligonucleotides of the present invention have at least one modified internucleotide linkage wherein the divalent oxygen moiety at the 3'-position of the internucleotide linkage is replaced by a tetravalent carbon moiety. The 3'-carbon modified internucleotide linkage is preferably a 3'-methylene or 3'-hydroxymethylene linkage. Also provided are a method and monomeric nucleoside and nucleotide intermediates for making the modified oligonucleotides of the present invention.
摘要翻译： 本发明提供可用于核酸治疗和诊断领域的耐核酸酶3'-碳修饰的寡核苷酸。 本发明的经修饰的寡核苷酸具有至少一个修饰的核苷酸间键，其中核苷酸间键的3'-位上的二价氧部分被四价碳部分代替。 3'-碳修饰的核苷酸间键优选为3'-亚甲基或3'-羟基亚甲基键。 还提供了用于制备本发明的修饰的寡核苷酸的方法和单体核苷和核苷酸中间体。
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公开(公告)号：US06924284B2
公开(公告)日：2005-08-02
申请号：US10222749
申请日：2002-08-15
申请人： Graham Beaton , Wilna J. Moree , Jaimie K. Rueter , Russell S. Dahl , David L. McElligott , Phyllis Goldman , Anthony J. Demaggio , Erik Christenson , Dan Herendeen , Kerry W. Fowler , Danwen Huang , Jaimie E. Bertino , Lisa H. Bourdon , David J. Fairfax , Qin Jiang , Helge A. Reisch , Ren Hua Song , Pavel E. Zhichkin
发明人： Graham Beaton , Wilna J. Moree , Jaimie K. Rueter , Russell S. Dahl , David L. McElligott , Phyllis Goldman , Anthony J. Demaggio , Erik Christenson , Dan Herendeen , Kerry W. Fowler , Danwen Huang , Jaimie E. Bertino , Lisa H. Bourdon , David J. Fairfax , Qin Jiang , Helge A. Reisch , Ren Hua Song , Pavel E. Zhichkin
IPC分类号： A61K31/502 , A61K31/5025 , A61K31/5377 , A61K41/00 , A61K49/00 , A61P9/00 , A61P9/10 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/28 , A61P35/00 , A61P43/00 , C07D237/32 , C07D237/34 , C07D241/44 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D237/52
CPC分类号： C07D401/12 , A61K41/0038 , A61K49/001 , C07D237/32 , C07D237/34 , C07D241/44 , C07D403/12 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The present invention provides compounds comprising a bicyclic aryl moiety, such as 2H-phthalazin-1-one or derivatives thereof, compositions comprising the same, and methods for producing and using the same. In particular, the present invention provides compounds of the formula: or a pharmaceutically acceptable salt, a hydrate, a solvate, or a prodrug thereof; where Q1, Q2 and Y are those defined herein.
摘要翻译： 本发明提供包含双环芳基部分的化合物，例如2H-酞嗪-1-酮或其衍生物，包含它们的组合物，及其制备和使用方法。 特别地，本发明提供下式的化合物：或其药学上可接受的盐，水合物，溶剂化物或前药; 其中Q 1，Q 2和Y是本文定义的那些。
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