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1. 发明申请

WO2005034943A1 INDOLE ANTIVIRAL COMPOSITIONS AND METHODS 审中-公开
标题翻译：包括抗病毒组合物和方法
公开(公告)号：WO2005034943A1
公开(公告)日：2005-04-21
申请号：PCT/US2004/032895
申请日：2004-10-06
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN , TOWNSEND, Leroy, B. , DRACH, John, C.
发明人： TOWNSEND, Leroy, B. , DRACH, John, C.
IPC分类号： A61K31/405
CPC分类号： A61K31/405 , A61K31/655 , A61K31/7052 , C07H19/04
摘要： The present invention provides novel chemical compounds and methods for their use. In particular, the present invention provides indole derivatives (e.g. as shown in Formula (I)) and related compounds and methods of using indole derivatives and related compounds as therapeutic agents to treat a number of conditions, including those associated with viral infection and cardiovascular diseases.
摘要翻译：本发明提供了新颖的化合物及其使用方法。特别地，本发明提供吲哚衍生物（例如如式（I）所示）和相关化合物和使用吲哚衍生物和相关化合物作为治疗剂的方法来治疗许多病症，包括与病毒感染和心血管疾病相关的病症。

2. 发明申请

WO1997027205A1 IMIDAZO[1,2-A]PYRIDINE C-NUCLEOSIDES AS ANTIVIRAL AGENTS 审中-公开
标题翻译：咪唑并[1,2-A]吡啶C - 核苷酸作为抗病毒剂
公开(公告)号：WO1997027205A1
公开(公告)日：1997-07-31
申请号：PCT/US1997001602
申请日：1997-01-22
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN , TOWNSEND, Leroy, B. , DRACH, John, C.
发明人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN
IPC分类号： C07H19/052
CPC分类号： C07D471/04 , C07H7/06 , C07H9/04 , C07H11/00 , C07H19/052
摘要： This invention pertains to nucleoside analogs which have antiviral activity and improved metabolic stability, compositions comprising them, and methods of antiviral treatment employing them. More particularly, this invention pertains to imidazo [1,2-a]pyridine C-nucleosides, as exemplified by compounds such imidazo[1,2-a]pyridine C5-nucleosides and imidazo[1,2-a]pyridine C3-nucleosides, and may be represented by formula (I), wherein exactly one of Q and Q is a sugar-like moiety; exactly one of Q and Q is -H; and Q , Q , Q and Q are independently imidazo[1,2-a]pyridine substituents, such as -H, -F, -Cl, -Br, and -I.
摘要翻译：本发明涉及具有抗病毒活性和改善的代谢稳定性的核苷类似物，包含它们的组合物以及使用它们的抗病毒治疗方法。更具体地，本发明涉及咪唑并[1,2-a]吡啶C-核苷，例如咪唑并[1,2-a]吡啶C5-核苷和咪唑并[1,2-a]吡啶C 3 - 核苷并且可以由式（I）表示，其中Q 3和Q 5中的仅一个是糖状部分; Q 3和Q 5中的正好一个是-H; 和Q 2，Q 6，Q 7和Q 8独立地是咪唑并[1,2-a]吡啶取代基，例如-H，-F，-Cl，-Br和-I 。

3. 发明申请

WO1997007125A1 5'-SUBSTITUTED-RIBOFURANOSYL BENZIMIDAZOLES AS ANTIVIRAL AGENTS 审中-公开
标题翻译：作为抗病毒剂的5'-取代的呋喃甲酰苯胺
公开(公告)号：WO1997007125A1
公开(公告)日：1997-02-27
申请号：PCT/US1996013187
申请日：1996-08-16
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN , TOWNSEND, Leroy, B. , DRACH, John, C.
发明人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN
IPC分类号： C07H19/052
CPC分类号： C07H19/052
摘要： The present invention relates to polysubstituted benzimidazoles, having formula (I), wherein Q is substituted benzimidazole group attached at the benzimidazole 1-position; R is a halogen or atomic number 9 to 53, inclusive (i.e., -F, -Cl, -Br, or -I); azido (i.e., -N3); or -X-R1, wherein X is a chalcogen of atomic number 8 to 16, inclusive (i.e., -O- or -S-), and R1 may be straight or branched chain alkyl of 1 to 8 carbon atoms; and R2 and R3 may be the same or different and are separately -O-C(=O)CH3 (i.e., -OAc) or hydroxy (i.e., -OH); and pharmaceutically acceptable salts and operative combinations thereof. Also provided by this invention are compositions comprising a polysubstituted benzimidazoles as defined above and methods of use thereof.
摘要翻译：本发明涉及具有式（I）的多取代的苯并咪唑，其中Q是在苯并咪唑1-位连接的取代的苯并咪唑基; R是卤素或原子序数9至53，包括（即-F，-Cl，-Br或-I）; 叠氮基（即-N3）; 或-X-R 1，其中X是原子数为8〜16的硫族元素（即-O-或-S-），R 1可以是1〜8个碳原子的直链或支链烷基; 并且R 2和R 3可以相同或不同，并且分别是-O-C（= O）CH 3（即，-OAc）或羟基（即-OH）; 及其药学上可接受的盐和操作组合。本发明还提供了包含如上所定义的多取代苯并咪唑及其使用方法的组合物。

4. 发明申请

WO1992007867A1 POLYSUBSTITUTED BENZIMIDAZOLES AS ANTIVIRAL AGENTS 审中-公开
标题翻译：多元苯并咪唑作为抗病毒剂
公开(公告)号：WO1992007867A1
公开(公告)日：1992-05-14
申请号：PCT/US1991008124
申请日：1991-10-31
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN , TOWNSEND, Leroy, B. , DRACH, John, C.
发明人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN
IPC分类号： C07H17/02
CPC分类号： A61K31/70 , A61K31/415 , A61K31/4184 , A61K31/52 , A61K31/7056 , C07D235/24 , C07D235/26 , C07D235/30 , C07H19/052 , Y10S514/934 , A61K2300/00
摘要： This invention relates to novel polysubstituted benzimidazoles and compositions and their use in the treatment of viral infections. The polysubstituted benzimidazoles and compositions of the present invention exhibit antiviral properties against viruses of the herpes family, particularly human cytomegalovirus (HCMV) and herpes simplex viruses (HSV).

5. 发明申请

WO1997027204A1 MODIFIED BENZIMIDAZOLE NUCLEOSIDES AS ANTIVIRAL AGENTS 审中-公开
标题翻译：改性的苯并咪唑核苷作为抗病毒剂
公开(公告)号：WO1997027204A1
公开(公告)日：1997-07-31
申请号：PCT/US1997000764
申请日：1997-01-22
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN , GLAXO GROUP LIMITED , TOWNSEND, Leroy, B. , DRACH, John, C. , FREEMAN, George, A.
发明人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN , GLAXO GROUP LIMITED
IPC分类号： C07H19/052
CPC分类号： C07D471/04 , C07H7/06 , C07H9/04 , C07H11/00 , C07H19/052
摘要： This invention pertains to nucleoside analogs which have antiviral activity and improved metabolic stability. More specifically, this invention pertains to modified sugar benzimidazole nucleosides, as exemplified by compounds such as benzimidazole nucleosides possessing a fluorinated sugar-like moiety (for example, a 2'-fluoro-furanosyl moiety or a 3'-fluoro-furanosyl moiety), and may be represented by formula (I) wherein R is a fluorinated sugar-like moiety; and R , R , R , R and R are benzimidazole substituents, such as -H, halogens (e.g., -F, -C1, -Br, -I), -NO2, -NR2 (where R is independently -H or an alkyl group having 1-6 carbon atoms), -OR (where R is -H or an alkyl group having 1-6 carbon atoms), -SR (where R is -H or a hydrocarbyl of 1-10 carbon atoms), and -CF3. In one embodiment, R is 2'-fluoro-furanosyl or 3'-fluoro-furanosyl; R is -H, -F, -C1, -Br, -I, or -NR2, wherein R is independently -H or an alkyl group having 1-6 carbon atoms; R , R , R and R are independently -H, -F, -C1, -Br, or -I.
摘要翻译：本发明涉及具有抗病毒活性和改善的代谢稳定性的核苷类似物。更具体地，本发明涉及改性糖苯并咪唑核苷，例如化合物例如具有氟化糖样部分的苯并咪唑核苷（例如2'-氟 - 呋喃糖基部分或3'-氟 - 呋喃糖基部分），并且可以由式（I）表示，其中R 1是氟化糖样部分; R 2，R 4，R 5，R 6和R 7是苯并咪唑取代基，例如-H，卤素（例如-F，-C1，-Br，-I），-NO 2，-NR 2（其中R独立地是-H或具有1-6个碳原子的烷基），-OR（其中R是-H或具有1-6个碳原子的烷基），-SR（其中R 是-H或1-10个碳原子的烃基）和-CF 3。在一个实施方案中，R 1是2'-氟 - 呋喃糖基或3'-氟 - 呋喃糖基; R 2是-H，-F，-C 1，-Br，-I或-NR 2，其中R独立地是-H或具有1-6个碳原子的烷基; R 4，R 5，R 6和R 7独立地是-H，-F，-C 1，-Br或-I。

6. 发明申请

WO1996007646A1 ANTIVIRAL NUCLEOSIDE ANALOGUES CONTAINING A SUBSTITUTED BENZIMIDAZOLE BASE ATTACHED TO A CARBOCYCLIC RING 审中-公开
标题翻译：含有取代的苯并咪唑基的偶氮核苷类似物与碳环结合
公开(公告)号：WO1996007646A1
公开(公告)日：1996-03-14
申请号：PCT/US1995011366
申请日：1995-09-11
申请人： THE WELLCOME FOUNDATION LIMITED , THE REGENTS OF THE UNIVERSITY OF MICHIGAN , TOWNSEND, Leroy, B. , DALUGE, Susan, Mary
发明人： THE WELLCOME FOUNDATION LIMITED , THE REGENTS OF THE UNIVERSITY OF MICHIGAN
IPC分类号： C07D235/20
CPC分类号： C07D403/04 , C07D235/30
摘要： Antiviral nucleoside analogues contain a substituted benzimidazole base attached to a carbocyclic ring in place of the conventional sugar residue. In formulae (I) and (I-1), R is H, CH3 or CH2OH; R is H or OH; R is H or OH; or R and R together form a bond; R is amino, cyclopropylamino, cyclobutylamino, isopropylamino, tert-butylamino or -NR R where R and R together with the nitrogen atom to which they are attached form a 4, 5 or 6-membered heterocyclic ring; R is H and R and R are Cl, excluding the compound (+/-)-(1R*, 2S*, 3S*, 5S*)-5-[5,6-Dichloro-2-(cyclopropylamino)-1 H -benzimidazol-1-yl]-3-(hydroxymethyl)-1,2-cyclopentanediol and provided that at least one of R , R and R is or contains OH. The compounds have activity against herpes virus especially cytomegalovirus and also hepatitis B virus infections.
摘要翻译：抗病毒核苷类似物包含与碳环连接的取代的苯并咪唑碱代替常规的糖残基。在式（I）和（I-1）中，R 1是H，CH 3或CH 2 OH; R 2是H或OH; R 3是H或OH; 或R 2和R 3一起形成键; R 4是氨基，环丙基氨基，环丁基氨基，异丙基氨基，叔丁基氨基或-NR 8 R 9，其中R 8和R 9与它们所连接的氮原子一起形成4， 5或6元杂环; 不包括化合物（+/-） - （1R *，2S *，3S *，5S *） - 5- [5,6-二氯苯基]，R 5为H且R 6和R 7为Cl -2-（环丙基氨基）-1H-苯并咪唑-1-基] -3-（羟基甲基）-1,2-环戊二醇，条件是R 1，R 2， >和R 3是或含有OH。该化合物具有抗疱疹病毒特异性巨细胞病毒和乙型肝炎病毒感染的活性。

7. 发明申请

WO1993018009A1 ANTIVIRAL NUCLEOSIDE ANALOGUES 审中-公开
标题翻译：抗病毒核苷酸类似物
公开(公告)号：WO1993018009A1
公开(公告)日：1993-09-16
申请号：PCT/GB1993000479
申请日：1993-03-08
申请人： THE WELLCOME FOUNDATION LIMITED , THE REGENTS OF THE UNIVERSITY OF MICHIGAN , TOWNSEND, Leroy, B. , DRACH, John, Charles , GOOD, Steven, Spencer , DALUGE, Susan, Mary , MARTIN, Michael, Tolar
发明人： THE WELLCOME FOUNDATION LIMITED , THE REGENTS OF THE UNIVERSITY OF MICHIGAN
IPC分类号： C07D235/06
CPC分类号： C07D235/06 , C07D235/08 , C07D235/24 , C07D235/26 , C07D235/28 , C07D235/30
摘要： Antiviral nucleoside analogues contain a substituted benzimidazole base attached to a carbocyclic ring in a place of the conventional sugar residue. Particularly preferred compounds include those in which the 2-,5- and 6- positions of the benzimidazole base are substituted by halogen. The compounds have activity against herpes virus especially cytomegalovirus and also hepatitis B virus infections.
摘要翻译：抗病毒核苷类似物在常规糖残基的位置含有连接到碳环上的取代的苯并咪唑碱。特别优选的化合物包括其中苯并咪唑碱的2-，5-和6-位被卤素取代的化合物。该化合物具有抗疱疹病毒特异性巨细胞病毒和乙型肝炎病毒感染的活性。

8. 发明申请

WO9856761A2 BENZIMIDAZOLE DERIVATIVES 审中-公开
标题翻译：苯并咪唑衍生物
公开(公告)号：WO9856761A2
公开(公告)日：1998-12-17
申请号：PCT/EP9803380
申请日：1998-06-08
申请人： GLAXO GROUP LTD , UNIV MICHIGAN , DRACH JOHN CHARLES , TOWNSEND LEROY B , BOYD FRANK LESLIE JR , CHAMBERLAIN STANLEY DAWES , DALUGE SUSAN MARY , DEATON DAVID NORMAN , ANDERSEN MARC W , FREEMAN GEORGE ANDREW
发明人： DRACH JOHN CHARLES , TOWNSEND LEROY B , BOYD FRANK LESLIE JR , CHAMBERLAIN STANLEY DAWES , DALUGE SUSAN MARY , DEATON DAVID NORMAN , ANDERSEN MARC W , FREEMAN GEORGE ANDREW
IPC分类号： C07D235/06 , A61K31/4184 , A61K31/7056 , A61P31/12 , A61P31/22 , C07C20060101 , C07D235/18 , C07D235/24 , C07D235/26 , C07D235/28 , C07D235/30 , C07D405/04 , C07H20060101 , C07H19/052 , C07D
CPC分类号： C07D235/24 , C07D235/30 , C07D405/04 , C07H19/052
摘要： The present invention relates to certain bezimidazole derivatives and their use in medical therapy particularly for the treatment or prophylaxis of virus infections such as those caused by herpes viruses. The invention also relates to the preparation of the benzimidazole derivatives and pharmaceutical formulations containing them.
摘要翻译：本发明涉及某些苯扎咪唑衍生物及其在药物治疗中的用途，特别是用于治疗或预防由疱疹病毒引起的病毒感染。本发明还涉及苯并咪唑衍生物的制备和含有它们的药物制剂。

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