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1. 发明申请

WO03062255A2 SUGAR MODIFIED NUCLEOSIDES AS VIRAL REPLICATION INHIBITORS 审中-公开
标题翻译：糖改性核苷作为病毒复制抑制剂
公开(公告)号：WO03062255A2
公开(公告)日：2003-07-31
申请号：PCT/US0231556
申请日：2002-10-02
申请人： RIBAPHARM INC , HONG ZHI , AN HAOYUN , DING YILI , GIRARDET JEAN-LUC , ZHONG WEIDONG
发明人： HONG ZHI , AN HAOYUN , DING YILI , GIRARDET JEAN-LUC , ZHONG WEIDONG
IPC分类号： C07H19/044 , C07H19/16 , C07H
CPC分类号： C07H19/16 , A61K31/7076 , C07H19/044 , C07H19/067 , C07H19/10 , C07H19/11 , C07H19/167 , C07H19/20 , C07H19/213
摘要： Various 2'-modified nucleoside analogs and corresponding prodrugs are provided, and particularly contemplated methods of use include use as antiviral agents, and especially as antiviral agents against HCV.
摘要翻译：提供了各种2'-修饰的核苷类似物和相应的前药，并且特别预期的使用方法包括用作抗病毒剂，特别是作为抗HCV的抗病毒剂。

2. 发明申请

WO03051897B1 NUCLEOSIDE ANALOG LIBRARIES AND COMPOUNDS 审中-公开
标题翻译：核苷类似物文库和化合物
公开(公告)号：WO03051897B1
公开(公告)日：2003-08-21
申请号：PCT/US0240365
申请日：2002-12-17
申请人： RIBAPHARM INC , AN HAOYUN , GIRARDET JEAN-LUC , RAMASAMY KANDA , DING YILI , HONG ZHI
发明人： AN HAOYUN , GIRARDET JEAN-LUC , RAMASAMY KANDA , DING YILI , HONG ZHI
IPC分类号： C07B61/00 , C07H19/06 , C07H19/16 , C07H19/23 , C07H21/00 , C07H19/00 , A01N43/04 , A61K31/70
CPC分类号： C07H19/06 , C07B2200/11 , C07H19/16 , C07H19/23 , C07H21/00 , C40B40/00
摘要： Nucleoside analog libraries are prepared in a combinatorial library approach. In some preferred aspects, diverse heterocyclic bases and/or diverse nucleoside substituents are prepared using solid phase-coupled nucleosides in a series of at least two modification reactions. Particularly preferred compounds include various pyrazolopyrimidine, pyrrolidinopyrimidinone, and benzimidazole nucleoside analogs generated using contemplated libraries, which may be useful in the treatment of various conditions, particularly viral infections and neoplastic diseases.
摘要翻译：核苷类似物文库以组合文库方法制备。在一些优选的方面，使用固相耦合的核苷在一系列至少两个修饰反应中制备不同的杂环碱基和/或不同的核苷取代基。特别优选的化合物包括使用考虑的文库产生的各种吡唑并嘧啶，吡咯烷并嘧啶酮和苯并咪唑核苷类似物，其可用于治疗各种病症，特别是病毒感染和肿瘤疾病。

3. 发明申请

WO03051881B1 SUBSTITUTED PURINE NUCLEOSIDE LIBRARIES AND COMPOUNDS BY SOLID-PHASE COMBINATORIAL STRATEGIES 审中-公开
标题翻译：用固相组合策略替代嘌呤核苷文库和化合物
公开(公告)号：WO03051881B1
公开(公告)日：2003-08-28
申请号：PCT/US0240414
申请日：2002-12-17
申请人： RIBAPHARM INC , AN HAOYUN , GUNIC ESMIR , KOH YUNG-HYO , CHEN HUANMING , BARAWKAR DINESH , ZHANG WEIJIAN , GIRARDET JEAN-LUC , RONG FRANK , HONG ZHI
发明人： AN HAOYUN , GUNIC ESMIR , KOH YUNG-HYO , CHEN HUANMING , BARAWKAR DINESH , ZHANG WEIJIAN , GIRARDET JEAN-LUC , RONG FRANK , HONG ZHI
IPC分类号： C07B61/00 , C07D473/00 , C07H19/06 , C07H19/16 , C07H21/00
CPC分类号： C07D473/00 , C07B2200/11 , C07H19/06 , C07H19/16 , C07H21/00 , C40B40/00
摘要： Nucleoside analog libraries are prepared in a combinatorial library approach. In some preferred aspects, library diversity is generated using solid phase-coupled nucleosides in a series of at least two modification reactions, and contemplated libraries and compounds include various 2-C-substituted purines, 3-deoxy/aza-6-substituted purines, substituted 2-thioadenosines, 2-amino-6,8-disubstituted purines, 2,8-disubstituted guanosines, 6-substituted purines, 2,6-disubstituted adenosines, and 6,8-disubstituted adenosines. Particularly preferred compounds include nucleoside analogs generated using contemplated libraries, which may be useful in treatment of various conditions, particularly viral infections and neoplastic diseases.
摘要翻译：核苷类似物文库以组合文库方法制备。在一些优选的方面，使用固相耦合的核苷在一系列至少两个修饰反应中产生文库多样性，并且考虑的文库和化合物包括各种2-C-取代的嘌呤，3-脱氧/氮杂-6-取代的嘌呤，取代的2-硫代腺苷，2-氨基-6,8-二取代的嘌呤，2,8-二取代的鸟苷，6-取代的嘌呤，2,6-二取代的腺苷和6,8-二取代的腺苷。特别优选的化合物包括使用考虑的文库产生的核苷类似物，其可用于治疗各种病症，特别是病毒感染和肿瘤疾病。

4. 发明申请

WO03061576A2 DEAZAPURINE NUCLEOSIDE ANALOGS AND THEIR USE AS THERAPEUTIC AGENTS 审中-公开
标题翻译： DEAZAPURINE NUCLEOSIDE ANALOGS AND THEIR USE as THERAPEUTIC AGENTS
公开(公告)号：WO03061576A2
公开(公告)日：2003-07-31
申请号：PCT/US0301545
申请日：2003-01-17
申请人： RIBAPHARM INC , AN HAOYUN , DING YILI , CHAMAKURA VARAPRASAD , HONG ZHI
发明人： AN HAOYUN , DING YILI , CHAMAKURA VARAPRASAD , HONG ZHI
IPC分类号： C07H19/044 , C07H19/16 , A61K
CPC分类号： C07H19/16 , C07H19/044
摘要： Methods, compositions, and uses for various deazapurine nucleoside libraries and library compounds are provided. Particularly preferred deazapurine nucleosides include 7−deazapurine nucleosides, 7−deaza−8−azapurine nucleosides, toyocamycin nucleoside analogs, 3−deazapurine nucleosides, and 9−deazapurine nucleosides, while preferred uses especially inlcude use of such compounds as pharmacological, and particularly antiviral agents.
摘要翻译：提供各种脱氮嘌呤核苷文库和文库化合物的方法，组合物和用途。特别优选的脱氮嘌呤核苷包括7-脱氮嘌呤核苷，7-脱氮-8-氮杂嘌呤核苷，益多霉素核苷类似物，3-脱氮嘌呤核苷和9-脱氮嘌呤核苷，而优选的用途尤其是使用药理学，特别是抗病毒剂。

5. 发明申请

WO2004030611A3 NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：非核苷酸逆转录酶抑制剂
公开(公告)号：WO2004030611A3
公开(公告)日：2004-06-17
申请号：PCT/US0327433
申请日：2003-08-22
申请人： RIBAPHARM INC , GIRARDET JEAN-LUC , ZHANG ZHIJUN , HAMATAKE ROBERT , HERNANDEZ MARTHA DE LA ROSA , GUNIC ESMIR , HONG ZHI , KIM HONGWOO , KOH YUNG-HYO , NILAR SHAHUL , SHAW STEPHANIE , YAO NANHUA
发明人： GIRARDET JEAN-LUC , ZHANG ZHIJUN , HAMATAKE ROBERT , HERNANDEZ MARTHA DE LA ROSA , GUNIC ESMIR , HONG ZHI , KIM HONGWOO , KOH YUNG-HYO , NILAR SHAHUL , SHAW STEPHANIE , YAO NANHUA
IPC分类号： A61K31/13 , A61K31/4196 , A61K31/4709 , C07D233/84 , C07D249/08 , C07D249/10 , C07D401/04 , C07D401/12 , C07D401/14 , A01N33/02
CPC分类号： C07D249/08 , A61K31/4196 , A61K31/4709 , C07D233/84 , C07D249/10 , C07D401/04 , C07D401/12 , C07D401/14
摘要： Various carbonyl amides are employed in vitro and in vivo as non-nucleoside inhibitors of a reverse transcriptase, and particularly of HIV reverse transcriptase. Therefore, contemplated compounds may be employed in the treatment of HIV infected patients. Further contemplated aspects include pharmaceutical compositions comprising therapeutically effective amounts of contemplated compounds.
摘要翻译：各种羰基酰胺在体外和体内被用作逆转录酶的非核苷抑制剂，特别是HIV逆转录酶的非核苷抑制剂。因此，预期的化合物可用于治疗HIV感染患者。进一步考虑的方面包括包含治疗有效量的预期化合物的药物组合物。

6. 发明申请

WO2008058285A2 4-CYANOPHENYLAMINO-SUBSTITUTED BICYCLIC HETEROCYCLIC COMPOUNDS AS HIV INHIBITORS 审中-公开
标题翻译：作为艾滋病毒抗体的4-氰基亚氨基取代的双环杂环化合物
公开(公告)号：WO2008058285A2
公开(公告)日：2008-05-15
申请号：PCT/US2007084342
申请日：2007-11-09
申请人： ARDEA BIOSCIENCES INC , GIRARDET JEAN-LUC , HONG ZHI , SHAW STEPHANIE , KOH YUNG-HYO
发明人： GIRARDET JEAN-LUC , HONG ZHI , SHAW STEPHANIE , KOH YUNG-HYO
IPC分类号： A61K31/519
CPC分类号： C07D495/04
摘要： This application concerns certain 4-cyanophenylamino-substituted bicyclic heterocycles of formula (I) where the dashed line represents a double bond that may be located either between A and C(V) or between C(V) and D, where A is S or C(Z); D is S or C(W); provided that one and only one of A and D is S; where T is NH, O, or S; and where other substituents are defined herein. These compounds are non-nucleoside reverse transcriptase inhibitors and have potential as anti-HIV treatment.
摘要翻译：本申请涉及式（I）的某些4-氰基苯基氨基取代的双环杂环，其中虚线表示可以位于A和C（V）之间或C（V）和D之间的双键，其中A是S或 C（Z）; D为S或C（W）; A和D中只有一个是S; 其中T是NH，O或S; 并且其中其它取代基在本文中定义。这些化合物是非核苷逆转录酶抑制剂，具有抗HIV治疗的潜力。

7. 发明申请

WO2006026356A3 S-TRIAZOLYL a-MERCAPTOACETANILDES AS INHIBITORS OF HIV REVERSE TRANSCRIPTASE 审中-公开
标题翻译：作为艾滋病病毒逆转录酶抑制剂的S-三唑并吡啶甲酰胺
公开(公告)号：WO2006026356A3
公开(公告)日：2006-08-10
申请号：PCT/US2005030259
申请日：2005-08-25
申请人： VALEANT RES & DEV , GIRARDET JEAN-LUC , KOH YUNG-HYO , DE LA ROSA MARTHA , GUNIC ESMIR , HONG ZHI , LANG STANLEY , KIM HONG WOO
发明人： GIRARDET JEAN-LUC , KOH YUNG-HYO , DE LA ROSA MARTHA , GUNIC ESMIR , HONG ZHI , LANG STANLEY , KIM HONG WOO
IPC分类号： A61K31/4196 , C07D249/08
CPC分类号： C07D249/12 , C07D249/14 , C07D401/04 , C07D401/12 , C07D405/12
摘要： A series of S-triazolyl a-mercaptoacetanilides having general structure (1) are provided, where Q is CO 2 H, CONR 2 , SO 3 H, or SO 2 NR 2 . The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.
摘要翻译：提供一系列具有一般结构（1）的S-三唑基α-巯基乙酰替苯胺，其中Q是CO 2 H，CONR 2，SO 3

8. 发明申请

WO2007027248A3 3', 5' - CYCLIC NUCLEOSIDE ANALOGUES FOR TREATMENT OF HCV 审中-公开
标题翻译： 3'，5' - 用于治疗HCV的循环核苷类似物
公开(公告)号：WO2007027248A3
公开(公告)日：2007-11-29
申请号：PCT/US2006019114
申请日：2006-05-16
申请人： VALEANT RES & DEV , GUNIC ESMIR , HONG ZHI , GIRARDET JEAN-LUC
发明人： GUNIC ESMIR , HONG ZHI , GIRARDET JEAN-LUC
IPC分类号： C07H19/00 , A01N43/04 , A61K31/70
CPC分类号： C07H19/00
摘要： This invention provides compounds according to formula (I) where B is a 6-membered monocyclic nitrogen-containing heteroaryl group or a 5 + 6 fused bicyclic nitrogen-containing heteroaryl group, and A is selected from Groups (1), (2), (3), and (4) where Groups (1), (2), (3), and (4), are defined herein. These compounds are useful in the treatment of Hepatitis C infection.
摘要翻译：本发明提供式（I）化合物，其中B为6-元单环含氮杂芳基或5 + 6稠合双环含氮杂芳基，A选自（1），（2），（3）和（4）其中组（1），（2），（3）和（4）在本文中定义。这些化合物可用于治疗丙型肝炎感染。

9. 发明申请

WO2004061409A3 PARALLEL INDUCIBLE CELL-BASED KINASE SCREEN 审中-公开
标题翻译：平行诱导的基于细胞的激酶屏
公开(公告)号：WO2004061409A3
公开(公告)日：2004-10-14
申请号：PCT/US0240757
申请日：2002-12-19
申请人： RIBAPHARM INC , HONG ZHI , RICKETTS WILLIAM , DIAZ PAUL
发明人： HONG ZHI , RICKETTS WILLIAM , DIAZ PAUL
IPC分类号： C12Q1/02 , C12Q1/48 , G01N20060101
CPC分类号： C12Q1/485 , G01N2500/10
摘要： A parallel inducible cell-based kinase screen (PICKS) includes a plurality of cells that express a kinase gene under the control of an inducer and a reporter gene, wherein the cells are derived from a single cell line, and wherein the reporter gene generates a signal in response to catalytic activity or inhibition of the expressed kinases. Particularly preferred systems include cells expressing kinases from a single kinase signaling pathway, kinases from a kinase family, and/or kinases from various different kinase signaling pathways. Consequently, contemplated systems provide a platform for screening for novel kinase inhibitors, inhibition specificity of particular kinase inhibitors, and for analysis of inter-pathway and/or intra-pathway inhibition of a kinase inhibitor.
摘要翻译：平行诱导型基于细胞的激酶筛选（PICKS）包括多个在诱导剂和报道基因控制下表达激酶基因的细胞，其中所述细胞来源于单细胞系，并且其中所述报道基因产生响应催化活性或抑制表达的激酶而发出信号。特别优选的系统包括表达来自单一激酶信号传导途径的激酶，来自激酶家族的激酶和/或来自各种不同激酶信号传导途径的激酶的细胞。因此，所设想的系统提供了用于筛选新型激酶抑制剂，抑制特定激酶抑制剂的特异性以及用于分析激酶抑制剂的途径间和/或途径内抑制的平台。

10. 发明申请

WO02100354B1 PYRROLO[2,3-D]PYRIMIDINE NUCLEOSIDE ANALOGS 审中-公开
标题翻译：吡咯并[2,3-D]嘧啶核苷类似物
公开(公告)号：WO02100354B1
公开(公告)日：2004-04-15
申请号：PCT/US0206347
申请日：2002-02-28
申请人： RIBAPHARM INC , TAM ROBERT , WANG GUANGYI , LAU JOHNSON , HONG ZHI
发明人： TAM ROBERT , WANG GUANGYI , LAU JOHNSON , HONG ZHI
IPC分类号： C07D487/04 , A61K31/519 , A61K31/70 , A61K31/7064 , A61P1/04 , A61P3/10 , A61P17/00 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/02 , A61P37/04 , A61P37/06 , C07H19/04 , C07H19/056 , C07H19/14 , C07H19/167 , C07H19/173 , C07D487/02 , C07H19/22
CPC分类号： A61K31/70 , C07H19/056 , C07H19/14
摘要： Compositions and methods for pyrrolo[2,3-d]pyrimidine nucleoside analogs having substituents at the C4' and C5' positions of the ribofuranose moiety are presented. Contemplated compositions exhibit, among other things, anti-cancer and immunomodulating effects at reduced cytotoxicity.
摘要翻译：提出了在呋喃核糖部分的C4'和C5'位具有取代基的吡咯并[2,3-d]嘧啶核苷类似物的组合物和方法。考虑的组合物尤其表现出抗细胞毒性降低的抗癌和免疫调节作用。

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