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61. 发明申请

US20130243725A1 2'-SUBSTITUTED CARBA-NUCLEOSIDE ANALOGS FOR ANTIVIRAL TREATMENT 有权
标题翻译： 2'-取代的CARBA-核苷类似物用于抗病毒治疗
公开(公告)号：US20130243725A1
公开(公告)日：2013-09-19
申请号：US13793557
申请日：2013-03-11
申请人： GILEAD SCIENCES, INC.
发明人： Michael O'Neil Hanrahan Clarke
IPC分类号： C07H19/12 , A61K45/06 , A61K31/706
CPC分类号： C07H19/23 , A61K31/706 , A61K45/06 , C07H19/12
摘要： Provided are compounds of Formula I, as well as pharmaceutical compositions containing compounds of Formula I and methods for treating Orthomyxoviridae virus infections by administering these compounds. The compounds, compositions, and methods provided are particularly useful for the treatment of Human Influenza virus infections.
摘要翻译：提供式I的化合物，以及含有式I化合物的药物组合物和通过施用这些化合物治疗正粘病毒科病毒感染的方法。提供的化合物，组合物和方法特别可用于治疗人类流感病毒感染。

62. 发明授权

US08513406B2 Pharmaceutical compositions comprising forms of 5-azacytidine 有权
标题翻译：包含5-氮杂胞苷形式的药物组合物
公开(公告)号：US08513406B2
公开(公告)日：2013-08-20
申请号：US13587770
申请日：2012-08-16
申请人： Dumitru Ionescu , Peter Blumbergs , Gary L. Silvey
发明人： Dumitru Ionescu , Peter Blumbergs , Gary L. Silvey
IPC分类号： A61K31/7068 , C07H19/12
CPC分类号： A61K31/7068 , A61K31/706 , C07H19/048 , C07H19/12
摘要： The invention provides novel polymorphic and pseudopolymorphic crystalline forms of 5-azacytidine, along with methods for preparing said forms, wherein 5-azacytidine is represented by the formula: The invention also includes pharmaceutical compositions comprising said forms.
摘要翻译：本发明提供5-氮杂胞苷的新型多晶型和假多晶型结晶形式，以及制备所述形式的方法，其中5-氮杂胞苷由下式表示：本发明还包括包含所述形式的药物组合物。

63. 发明申请

US20130059809A1 PHARMACEUTICAL COMPOSITIONS COMPRISING FORMS OF 5-AZACYTIDINE 有权
标题翻译：包含5-AZACYTIDINE的形式的药物组合物
公开(公告)号：US20130059809A1
公开(公告)日：2013-03-07
申请号：US13587768
申请日：2012-08-16
申请人： Dumitru Ionescu , Peter Blumbergs , Gary L. Silvey
发明人： Dumitru Ionescu , Peter Blumbergs , Gary L. Silvey
IPC分类号： A61K31/706 , A61P7/00 , C07H19/12
CPC分类号： A61K31/7068 , A61K31/706 , C07H19/048 , C07H19/12
摘要： The invention provides novel polymorphic and pseudopolymorphic crystalline forms of 5-azacytidine, along with methods for preparing said forms, wherein 5-azacytidine is represented by the formula: The invention also includes pharmaceutical compositions comprising said forms.
摘要翻译：本发明提供5-氮杂胞苷的新型多晶型和假多晶型结晶形式，以及制备所述形式的方法，其中5-氮杂胞苷由下式表示：本发明还包括包含所述形式的药物组合物。

64. 发明申请

US20120108535A1 2-FLUORINATED RIBOSES AND ARABINOSES AND METHODS OF USE AND SYNTHESIS 有权
标题翻译： 2-氟化R ES ES AND。。。。。。。。。。。。。。。。。。。。。
公开(公告)号：US20120108535A1
公开(公告)日：2012-05-03
申请号：US13381587
申请日：2010-07-01
申请人： Anthony A. Sauve , Yana Cen
发明人： Anthony A. Sauve , Yana Cen
IPC分类号： A61K31/7028 , C07H19/048 , C07H23/00
CPC分类号： C07H23/00 , C07H19/048 , C07H19/056 , C07H19/06 , C07H19/073 , C07H19/12 , C07H19/16 , C07H19/173 , C07H19/19
摘要： Disclosed are halogenated 2-deoxy-lactone, 2′-deoxy-nucleosides, and derivatives thereof, for example, a compound of formula (I). Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one compound or salt of the invention, and a method of treating a disorder is selected from the group consisting of an abnormal cellular proliferation, a viral infection, and an autoimmune disorder.
摘要翻译：公开了卤化的2-脱氧内酯，2'-脱氧核苷及其衍生物，例如式（I）的化合物。还公开了包含药学上可接受的载体和本发明的至少一种化合物或盐的组合物，治疗病症的方法选自异常细胞增殖，病毒感染和自身免疫性疾病。

65. 发明授权

US08058424B2 Synthesis of 5-azacytidine 有权
标题翻译： 5-氮杂胞苷的合成
公开(公告)号：US08058424B2
公开(公告)日：2011-11-15
申请号：US12973701
申请日：2010-12-20
申请人： Dumitru Ionescu , Peter Blumbergs
发明人： Dumitru Ionescu , Peter Blumbergs
IPC分类号： C07H19/00 , C07H19/048 , C07H5/04 , C07H5/06 , C08B37/00 , A01N43/04 , A61K31/70
CPC分类号： C07H19/12
摘要： The present invention provides a method for the preparation of 5-azacytidine, wherein 5-azacytidine is represented by the structure: The method involves the silylation of 5-azacytosine, followed by the coupling of silylated 5-azacytosine to a protected β-D-ribofuranose derivative. The coupling reaction is catalyzed by trimethylsilyl trifluoromethanesulfonate (TMS-Triflate).
摘要翻译：本发明提供了制备5-氮杂胞苷的方法，其中5-氮杂胞苷由以下结构表示：该方法包括5-氮杂胞嘧啶的甲硅烷基化，然后将甲硅烷基化的5-氮杂胞嘧啶与保护的B-D - 呋喃核糖衍生物。偶联反应由三氟甲磺酸三甲基甲硅烷基酯（TMS-Triflate）催化。

66. 发明申请

US20100249394A1 PROCESSES FOR PRODUCING DECITABINE 审中-公开
标题翻译：生产方法的方法
公开(公告)号：US20100249394A1
公开(公告)日：2010-09-30
申请号：US12731760
申请日：2010-03-25
申请人： Yunqi Liu , Gregory H. Lambeth , Brian W. Nixon
发明人： Yunqi Liu , Gregory H. Lambeth , Brian W. Nixon
IPC分类号： C07H19/12
CPC分类号： C07H19/12
摘要： New processes for producing decitabine are provided.
摘要翻译：提供了生产地西他滨的新工艺。

67. 发明授权

US07723512B2 Oligonucleotides comprising a non-phosphate backbone linkage 有权
标题翻译：包含非磷酸骨架键的寡核苷酸
公开(公告)号：US07723512B2
公开(公告)日：2010-05-25
申请号：US12496250
申请日：2009-07-01
申请人： Muthiah Manoharan , Kallanthottathil G. Rajeev
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev
IPC分类号： C07H19/00 , C07H19/22
CPC分类号： C12N15/111 , C07H19/04 , C07H19/12 , C07H19/16 , C07H19/167 , C07H19/173 , C07H21/02 , C12N15/1136 , C12N15/1137 , C12N2310/14 , C12N2310/312 , C12N2320/51
摘要： One aspect of the present invention relates to a ribonucleoside substituted with a phosphonamidite group at the 3′-position. In certain embodiments, the phosphonamidite is an alkyl phosphonamidite. Another aspect of the present invention relates to a double-stranded oligonucleotide comprising at least one non-phosphate linkage. Representative non-phosphate linkages include phosphonate, hydroxylamine, hydroxylhydrazinyl, amide, and carbamate linkages. In certain embodiments, the non-phosphate linkage is a phosphonate linkage. In certain embodiments, a non-phosphate linkage occurs in only one strand. In certain embodiments, a non-phosphate linkage occurs in both strands. In certain embodiments, a ligand is bound to one of the oligonucleotide strands comprising the double-stranded oligonucleotide. In certain embodiments, a ligand is bound to both of the oligonucleotide strands comprising the double-stranded oligonucleotide. In certain embodiments, the oligonucleotide strands comprise at least one modified sugar moiety. Another aspect of the present invention relates to a single-stranded oligonucleotide comprising at least one non-phosphate linkage. Representative non-phosphate linkages include phosphonate, hydroxylamine, hydroxylhydrazinyl, amide, and carbamate linkages. In certain embodiments, the non-phosphate linkage is a phosphonate linkage. In certain embodiments, a ligand is bound to the oligonucleotide strand. In certain embodiments, the oligonucleotide comprises at least one modified sugar moiety.
摘要翻译：本发明的一个方面涉及在3'-位被亚磷酰胺基取代的核糖核苷。在某些实施方案中，亚磷酰胺是烷基亚磷酰胺。本发明的另一方面涉及包含至少一种非磷酸键的双链寡核苷酸。代表性的非磷酸酯键包括膦酸酯，羟胺，羟基肼基，酰胺和氨基甲酸酯键。在某些实施方案中，非磷酸酯键是膦酸酯键。在某些实施方案中，非磷酸酯键仅出现在一条链中。在某些实施方案中，在两条链中都发生非磷酸连接。在某些实施方案中，配体与包含双链寡核苷酸的寡核苷酸链之一结合。在某些实施方案中，配体与包含双链寡核苷酸的两条寡核苷酸链结合。在某些实施方案中，寡核苷酸链包含至少一个修饰的糖部分。本发明的另一方面涉及包含至少一种非磷酸键的单链寡核苷酸。代表性的非磷酸酯键包括膦酸酯，羟胺，羟基肼基，酰胺和氨基甲酸酯键。在某些实施方案中，非磷酸酯键是膦酸酯键。在某些实施方案中，配体与寡核苷酸链结合。在某些实施方案中，寡核苷酸包含至少一个修饰的糖部分。

68. 发明申请

US20100087637A1 Synthesis of Decitabine 有权
标题翻译：地西他滨的合成
公开(公告)号：US20100087637A1
公开(公告)日：2010-04-08
申请号：US12572578
申请日：2009-10-02
申请人： Julian Paul Henschke , Xiaoheng Zhang , Jianbo Yu , Kun Hu , Lijun Mei
发明人： Julian Paul Henschke , Xiaoheng Zhang , Jianbo Yu , Kun Hu , Lijun Mei
IPC分类号： C07H19/12
CPC分类号： C07H13/08 , C07H19/12
摘要： A method for producing a β-enriched protected decitabine comprising: a) coupling a protected 2-deoxy-ribofuranose with a protected 5-azacytosine in the presence of a catalyst to form a reaction mixture comprising the protected decitabine of formula I; and b) quenching the reaction mixture of step a) with a base. The β-enriched protected decitabine so made may be deprotected to produce a decitabine product in a high yield and purity.
摘要翻译：一种生产富集的受保护的地西他滨的方法，包括：a）在催化剂存在下将受保护的2-脱氧 - 呋喃核糖与受保护的5-氮杂胞嘧啶偶联，形成包含式I的受保护的地西他滨的反应混合物; 和b）将碱的步骤a）的反应混合物淬灭。如此制备的富含生物保护的地西他滨可以去保护以产生高产率和纯度的地西他滨产品。

69. 发明申请

US20100062992A1 Salts of 5-Azacytidine 审中-公开
标题翻译： 5-氮杂胞苷的盐
公开(公告)号：US20100062992A1
公开(公告)日：2010-03-11
申请号：US12557374
申请日：2009-09-10
申请人： Sanjeev Redkar , Pasit Phiasivongsa
发明人： Sanjeev Redkar , Pasit Phiasivongsa
IPC分类号： A61K31/706 , C07H19/12 , A61P35/00 , A61P9/10 , A61P17/02
CPC分类号： C07H19/12
摘要： The present invention relates to salts of 5-azacytidine as well as methods for synthesizing the salts described herein. Pharmaceutical compositions and methods of using the 5-azacytidine salts are also provided, including methods of administering the salts or pharmaceutical compositions thereof to treat conditions, such as cancer and hematological disorders.
摘要翻译：本发明涉及5-氮杂胞苷的盐以及本文所述盐的合成方法。还提供了使用5-氮杂胞苷盐的药物组合物和方法，包括给予其盐或其药物组合物以治疗诸如癌症和血液病症的病症的方法。

70. 发明授权

US07642247B2 1,3,5-triazines for treatment of viral diseases 有权
公开(公告)号：US07642247B2
公开(公告)日：2010-01-05
申请号：US11671964
申请日：2007-02-06
申请人： Richard Daifuku , Alexander Gall , Dmitri Sergueev
发明人： Richard Daifuku , Alexander Gall , Dmitri Sergueev
IPC分类号： A61K31/706 , A61K31/7068 , C07H19/12
CPC分类号： C07D515/22 , C07H19/12
摘要： The present invention provides compounds and methods for treatment of viral diseases and cancer.

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