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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

WO2004006867A2 NOVEL 2-AMINO-9-[(2-HYDROXYMETHYL) CYCLOPROPYLIDENEMETHYL] PURINES AS ANTIVIRAL AGENTS 审中-公开
标题翻译：新型2-氨基-9- [（2-羟甲基）环丙基咪唑]作为抗病毒剂
公开(公告)号：WO2004006867A2
公开(公告)日：2004-01-22
申请号：PCT/US2003/007909
申请日：2003-03-13
申请人： WAYNE STATE UNIVERSITY , THE REGENTS OF THE UNIVERSITY OF MICHIGAN , ZEMLICKA, Jiri , DRACH, John, C.
发明人： ZEMLICKA, Jiri , DRACH, John, C.
IPC分类号： A61K
CPC分类号： C07D473/00 , C07F9/65616
摘要： Compounds which are active against viruses have the Formulas (1) and (2), wherein B is 2-aminopurine-9-yl, which may be unsubstituted or substituted in the 6 position with NHR 1 , OR 2 , or SR 3 ; R l is selected from the group consisting of alkyl, alkenyl, alkynyl, and C 4-18 cycloalkyl, any of which may be optionally substituted with one or more members of the group consisting of hydroxy, halo, amino, acyl, cycloalkyl, heterocyclyl and aryl; R 2 is selected from the group consisting of C 2-18 alkyl, alkenyl, alkynyl, and cycloalkyl, any of which may be branched or unbranched and optionally substituted with one or more members of the group consisting of hydroxy, halo, amino, acyl, cycloalkyl, heterocyclyl, and aryl; and R 3 is selected from the group consisting of alkyl, alkenyl, alkynyl, and cycloalkyl, any of which may be branched or unbranched and optionally substituted with one or more members of the group consisting of hydroxy, halo, amino, acyl, cycloalkyl, heterocyclyl and aryl.
摘要翻译：对病毒有活性的化合物具有式（1）和（2），其中B是2-氨基嘌呤-9-基，其可以是未取代的或在6位被NHR1，OR2或SR3取代; R 1选自烷基，烯基，炔基和C 4-18环烷基，其中任何一个可以任选地被羟基，卤素，氨基，酰基，环烷基，杂环基和芳基中的一个或多个成员取代 ; R2选自C2-18烷基，烯基，炔基和环烷基，其中任何一个可以是支链或非支链的，并且任选被一个或多个由羟基，卤素，氨基，酰基，环烷基，杂环基和芳基; 并且R 3选自烷基，烯基，炔基和环烷基，其中任何一个可以是支链或非支链的，并且任选被一个或多个由羟基，卤素，氨基，酰基，环烷基，杂环基和芳基。

3. 发明申请

WO1994008456A1 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：WO1994008456A1
公开(公告)日：1994-04-28
申请号：PCT/US1993010104
申请日：1993-10-20
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN
发明人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN , TOWNSEND, Leroy, B. , DRACH, John, C.
IPC分类号： A01N43/04
CPC分类号： C07D235/24 , A61K31/4184 , A61K31/52 , A61K31/7056 , C07H19/052 , 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).
摘要翻译：本发明涉及新型多取代苯并咪唑及其组合物及其在治疗病毒感染中的用途。本发明的多取代的苯并咪唑和组合物显示抗疱疹家族病毒，特别是人巨细胞病毒（HCMV）和单纯疱疹病毒（HSV）的抗病毒特性。

4. 发明申请

WO1995023151A1 PYRROLO(2,3-D)PYRIMIDINE DERIVATIVES AS ANTIVIRALS 审中-公开
标题翻译：吡咯（2,3-D）吡啶衍生物作为抗病毒剂
公开(公告)号：WO1995023151A1
公开(公告)日：1995-08-31
申请号：PCT/US1995002287
申请日：1995-02-23
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN
发明人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN , TOWNSEND, Leroy, B. , DRACH, John, C. , RENAU, Thomas, E.
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： This invention relates to a novel class of 4,5,6,7-substituted non-nucleoside, non-phosphorylatable pyrrolo[2,3-d]pyrimidines which exhibit both significantly lower levels of cytotoxicity and superior antiviral activity than known nucleoside, non-nucleoside, and non-nucleoside, non-phosphorylatable pyrrolo[2,3-d]pyrimidine derivatives, particularly against human DNA viruses such as cytomegalovirus (HCMV) and herpes simplex virus type 1 (HSV-1). These compounds are represented by formula (I) wherein R is -NH2 or -NHCH3; R is -CN, -CSNH2, or -CSeNH2; R is -H or -NH2; and R is selected from the group consisting of aryls and aralkyls having 6 to 30 carbon atoms; aliphatic oxy-hydrocarbyls having 2 to 15 carbon atoms, lacking free hydroxyl groups and further lacking acyl or acyl derivatized groups; and oxy-hydrocarbyls having 6 to 30 carbon atoms, at least one aryl or aralkyl group, and only one oxy-group; with the proviso that if R is -CN and R is -H, then R is -NH2 and R is -CH2C6H4-2-CH3.
摘要翻译：本发明涉及一类新颖的4,5,6,7-取代的非核苷，不可磷酸化的吡咯并[2,3-d]嘧啶，其显示出比已知的核苷非特异性的显着更低的细胞毒性水平和更好的抗病毒活性核苷和非核苷，不可磷酸化的吡咯并[2,3-d]嘧啶衍生物，特别是针对人DNA病毒如巨细胞病毒（HCMV）和1型单纯疱疹病毒（HSV-1）。这些化合物由式（I）表示，其中R 4是-NH 2或-NHCH 3; R 5是-CN，-CSNH 2或-CSeNH 2; R 6是-H或-NH 2; R 7选自具有6〜30个碳原子的芳基和芳烷基; 具有2至15个碳原子的脂族烃基，缺少游离羟基并进一步缺乏酰基或酰基衍生基团; 和具有6至30个碳原子的烃基，至少一个芳基或芳烷基和仅一个氧基; 条件是如果R 5是-CN且R 6是-H，那么R 4是-NH 2，R 7是-CH 2 C 6 H 4 -2-CH 3。

5. 发明授权

EP1490015B1 NOVEL 2-AMINO-9-((2-HYDROXYMETHYL) CYCLOPROPYLIDENEMETHYL) PURINES AS ANTIVIRAL AGENTS 有权
标题翻译： NEW 2-氨基-9 - （（2-羟甲基）CYCLOPROPYLIDENMETHYL） - 嘌呤作为抗病毒剂
公开(公告)号：EP1490015B1
公开(公告)日：2009-09-23
申请号：EP03764294.9
申请日：2003-03-13
申请人： WAYNE STATE UNIVERSITY , THE REGENTS OF THE UNIVERSITY OF MICHIGAN
发明人： ZEMLICKA, Jiri , DRACH, John, C. , CHEN, Xinchao
IPC分类号： A61K6/00 , C07D473/18 , C07D473/16 , C07D473/24 , A61K31/522 , A61P31/18 , A61P31/22 , C07F9/6506
CPC分类号： C07D473/00 , C07F9/65616
摘要： Compounds which are active against viruses have the Formulas (I) and (II), wherein B is 2-aminopurine-9-yl, which may be unsubstituted or substituted in the 6 position with NHR1, OR2, or SR3; Rl is selected from the group consisting of alkyl, alkenyl, alkynyl, and C4-18 cycloalkyl, any of which may be optionally substituted with one or more members of the group consisting of hydroxy, halo, amino, acyl, cycloalkyl, heterocyclyl and aryl; R2 is selected from the group consisting of C2-18 alkyl, alkenyl, alkynyl, and cycloalkyl, any of which may be branched or unbranched and optionally substituted with one or more members of the group consisting of hydroxy, halo, amino, acyl, cycloalkyl, heterocyclyl, and aryl; and R3 is selected from the group consisting of alkyl, alkenyl, alkynyl, and cycloalkyl, any of which may be branched or unbranched and optionally substituted with one or more members of the group consisting of hydroxy, halo, amino, acyl, cycloalkyl, heterocyclyl and aryl.

6. 发明公开

EP1000080A1 LYXOFURANOSYL BENZIMIDAZOLES AS ANTIVIRAL AGENTS 失效
标题翻译： LYX非呋喃酰基苯并咪唑作为抗病毒药物
公开(公告)号：EP1000080A1
公开(公告)日：2000-05-17
申请号：EP98937254.5
申请日：1998-07-29
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN , GLAXO GROUP LIMITED
发明人： TOWNSEND, Leroy, B. , DRACH, John, C. , BIRON, Karen,K. , BOYD, Frank,L. Jr.
IPC分类号： C07H19/052 , A61K31/70
CPC分类号： C07H19/052 , Y02P20/55
摘要： The present invention pertains to D- and L-lyxofuranosyl benzimidazole compounds. In one embodiment, the present invention pertains to D- and L-lyxofuranosyl benzimidazole compounds selected from the group consisting of compounds having a formula selected from the following: (beta-D), (beta-L), (alpha-L) and (alpha-D) wherein R?2, R4, R5, R6, and R7¿ are independently the same or different and independently selected from the group consisting of: -H, -F, -Cl, -Br, -I, -NO¿2?, -N(R?8)¿2, -OR?8, -SR12¿, and -CF¿3?, wherein R?8¿ is independently -H or an alkyl group having 1-6 carbon atoms and wherein R12 is independently -H or a hydrocarbyl group having 1-10 carbon atoms; and R?9, R10 and R11¿ are independently the same or different and are H or a hydroxyl protecting group; anomeric and optical isomers thereof; and pharmaceutically acceptable salts and prodrug derivatives thereof. The present invention also pertains to antiviral compositions using these compounds, methods of treating a viral infection using these compounds, and the use of these compounds in the preparation of a medicament for use in the treatment of a viral infection.
摘要翻译：本发明涉及D-和L-左旋呋喃糖基苯并咪唑化合物。在一个实施方案中，本发明涉及选自具有选自以下结构式的化合物的D-和L-来苏呋喃糖基苯并咪唑化合物：（β-D），（β-L），（α-L）和（α-D）其中R 2，R 4，R 5，R 6和R 7'独立地相同或不同并且独立地选自：-H，-F，-Cl，-Br，-I， - -N（R 8）2，-OR 8，-SR 12和-CF 3，其中R 8独立地为-H或具有1-6个碳原子的烷基并且其中R 12独立地为-H或具有1-10个碳原子的烃基; R9，R10和R11独立地是相同或不同的，并且是H或羟基保护基; 它们的端基异构体和光学异构体; 及其药学上可接受的盐和前药衍生物。本发明还涉及使用这些化合物的抗病毒组合物，使用这些化合物治疗病毒感染的方法，以及这些化合物在制备用于治疗病毒感染的药物中的用途。

7. 发明公开

EP1490015A2 NOVEL 2-AMINO-9-((2-HYDROXYMETHYL) CYCLOPROPYLIDENEMETHYL) PURINES AS ANTIVIRAL AGENTS 有权
标题翻译： NEW 2-氨基-9 - （（2-羟甲基）CYCLOPROPYLIDENMETHYL） - 嘌呤作为抗病毒剂
公开(公告)号：EP1490015A2
公开(公告)日：2004-12-29
申请号：EP03764294.9
申请日：2003-03-13
申请人： Wayne State University , THE REGENTS OF THE UNIVERSITY OF MICHIGAN
发明人： ZEMLICKA, Jiri , DRACH, John, C.
IPC分类号： A61K6/00
CPC分类号： C07D473/00 , C07F9/65616
摘要： Compounds which are active against viruses have the Formulas (I) and (II), wherein B is 2-aminopurine-9-yl, which may be unsubstituted or substituted in the 6 position with NHR1, OR2, or SR3; Rl is selected from the group consisting of alkyl, alkenyl, alkynyl, and C4-18 cycloalkyl, any of which may be optionally substituted with one or more members of the group consisting of hydroxy, halo, amino, acyl, cycloalkyl, heterocyclyl and aryl; R2 is selected from the group consisting of C2-18 alkyl, alkenyl, alkynyl, and cycloalkyl, any of which may be branched or unbranched and optionally substituted with one or more members of the group consisting of hydroxy, halo, amino, acyl, cycloalkyl, heterocyclyl, and aryl; and R3 is selected from the group consisting of alkyl, alkenyl, alkynyl, and cycloalkyl, any of which may be branched or unbranched and optionally substituted with one or more members of the group consisting of hydroxy, halo, amino, acyl, cycloalkyl, heterocyclyl and aryl.

8. 发明公开

EP1165560A1 2-HYDROXY METHYLCYCLOPRO PYLIDENEMETHYL PURINES AND -PYRIMIDINES AS ANTIVIRAL AGENTS 有权
标题翻译： 2-羟基甲基环庚基甲基嘌呤和作为抗病毒剂的嘧啶
公开(公告)号：EP1165560A1
公开(公告)日：2002-01-02
申请号：EP00913872.8
申请日：2000-03-10
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN , BOARD OF GOVERNORS OF WAYNE STATE UNIVERSITY
发明人： ZEMLICKA, Jiri , QIU, Yao-Ling , DRACH, John, C. , PTAK, Roger, G.
IPC分类号： C07D473/16 , C07D473/18 , A61K31/52 , A61K31/522
CPC分类号： C07D239/47 , C07D239/54 , C07D473/00 , C07D473/16 , C07D473/18 , C07D473/34 , C07F9/65061 , C07F9/65616
摘要： Compounds which are active against viruses have Formulas (1, 2, 3 and 4) wherein B is a purine or pyrimidine heterocyclic ring and is preferably selected from the group consisting of 6-aminopurine (adenine), 2,6-diaminopurine, 2-amino-6-azidopurine, 2-amino-6-cyclopropylaminopurine, 6-hydroxypurine (hypoxanthine), 2-amino-6-halo substituted purines, 2-amino-6-alkoxy substituted purines, 2-amino-6-hydroxypurine (guanine), 3-deazapurines, 7-deaza-purines, 8-azapurines, cytosine, 5-halo substituted cytosines, 5-alkyl substituted cytosines, thymine, uracil and 6-azapyrimidines; X is O; and, R1 and R2 are alkyl or aryl groups. The compounds of the present invention also include the R- and S-enantiomers of the above compounds. The R1X and/or R2X can also be amino acid residues with X as NH.
摘要翻译：对病毒具有活性的化合物具有式（1,2,3和4），其中B是嘌呤或嘧啶杂环并且优选选自6-氨基嘌呤（腺嘌呤），2,6-二氨基嘌呤，2-氨基嘌呤，氨基-6-叠氮基嘌呤，2-氨基-6-环丙基氨基嘌呤，6-羟基嘌呤（次黄嘌呤），2-氨基-6-卤代嘌呤，2-氨基-6-烷氧基取代的嘌呤，2-氨基-6-羟基嘌呤（鸟嘌呤），3-脱氮嘌呤，7-脱氮嘌呤，8-氮杂嘌呤，胞嘧啶，5-卤代取代的胞嘧啶，5-烷基取代的胞嘧啶，胸腺嘧啶，尿嘧啶和6-氮杂嘧啶; X是O; 并且，R1和R2是烷基或芳基。本发明的化合物还包括上述化合物的R-和S-对映体。 R1X和/或R2X也可以是X为NH的氨基酸残基。

9. 发明授权

EP1165560B1 2-HYDROXY METHYLCYCLOPRO PYLIDENEMETHYL PURINES AS ANTIVIRAL AGENTS 有权
标题翻译： 2-羟基甲基环丙烷甲基嘌呤作为抗病毒药物
公开(公告)号：EP1165560B1
公开(公告)日：2004-11-17
申请号：EP00913872.8
申请日：2000-03-10
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN , BOARD OF GOVERNORS OF WAYNE STATE UNIVERSITY
发明人： ZEMLICKA, Jiri , QIU, Yao-Ling , DRACH, John, C. , PTAK, Roger, G.
IPC分类号： C07D473/16 , C07D473/18 , A61K31/52 , A61K31/522 , A61P31/18 , A61P31/22
CPC分类号： C07D239/47 , C07D239/54 , C07D473/00 , C07D473/16 , C07D473/18 , C07D473/34 , C07F9/65061 , C07F9/65616
摘要： Compounds which are active against viruses have Formulas (1, 2, 3 and 4) wherein B is a purine or pyrimidine heterocyclic ring and is preferably selected from the group consisting of 6-aminopurine (adenine), 2,6-diaminopurine, 2-amino-6-azidopurine, 2-amino-6-cyclopropylaminopurine, 6-hydroxypurine (hypoxanthine), 2-amino-6-halo substituted purines, 2-amino-6-alkoxy substituted purines, 2-amino-6-hydroxypurine (guanine), 3-deazapurines, 7-deaza-purines, 8-azapurines, cytosine, 5-halo substituted cytosines, 5-alkyl substituted cytosines, thymine, uracil and 6-azapyrimidines; X is O; and, R1 and R2 are alkyl or aryl groups. The compounds of the present invention also include the R- and S-enantiomers of the above compounds. The R1X and/or R2X can also be amino acid residues with X as NH.
摘要翻译：对病毒具有活性的化合物具有式（1,2,3和4），其中B是嘌呤或嘧啶杂环并且优选选自6-氨基嘌呤（腺嘌呤），2,6-二氨基嘌呤，2-氨基嘌呤，氨基-6-叠氮基嘌呤，2-氨基-6-环丙基氨基嘌呤，6-羟基嘌呤（次黄嘌呤），2-氨基-6-卤代嘌呤，2-氨基-6-烷氧基取代的嘌呤，2-氨基-6-羟基嘌呤（鸟嘌呤），3-脱氮嘌呤，7-脱氮嘌呤，8-氮杂嘌呤，胞嘧啶，5-卤代取代的胞嘧啶，5-烷基取代的胞嘧啶，胸腺嘧啶，尿嘧啶和6-氮杂嘧啶; X是O; 并且，R1和R2是烷基或芳基。本发明的化合物还包括上述化合物的R-和S-对映体。 R1X和/或R2X也可以是X为NH的氨基酸残基。

10. 发明公开

EP0746559A1 PYRROLO(2,3-D)PYRIMIDINE DERIVATIVES AS ANTIVIRALS 失效
标题翻译：吡咯并（2,3-d）嘧啶衍生物作为抗病毒化合物
公开(公告)号：EP0746559A1
公开(公告)日：1996-12-11
申请号：EP95911092.0
申请日：1995-02-23
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN
发明人： TOWNSEND, Leroy, B. , DRACH, John, C. , RENAU, Thomas, E.
IPC分类号： A61K31 , A61P31 , C07D487
CPC分类号： C07D487/04
摘要： This invention relates to a novel class of 4,5,6,7-substituted non-nucleoside, non-phosphorylatable pyrrolo[2,3-d]pyrimidines which exhibit both significantly lower levels of cytotoxicity and superior antiviral activity than known nucleoside, non-nucleoside, and non-nucleoside, non-phosphorylatable pyrrolo[2,3-d]pyrimidine derivatives, particularly against human DNA viruses such as cytomegalovirus (HCMV) and herpes simplex virus type 1 (HSV-1). These compounds are represented by formula (I) wherein R4 is -NH¿2? or -NHCH3; R?5¿ is -CN, -CSNH¿2?, or -CSeNH2; R?6¿ is -H or -NH¿2?; and R?7¿ is selected from the group consisting of aryls and aralkyls having 6 to 30 carbon atoms; aliphatic oxy-hydrocarbyls having 2 to 15 carbon atoms, lacking free hydroxyl groups and further lacking acyl or acyl derivatized groups; and oxy-hydrocarbyls having 6 to 30 carbon atoms, at least one aryl or aralkyl group, and only one oxy-group; with the proviso that if R5 is -CN and R6 is -H, then R4 is -NH¿2? and R?7¿ is -CH¿2?C6H4-2-CH3.

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