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1. 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。

2. 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。

3. 发明申请

WO2003104440A3 2,2-BIS(HYDROXYMETHYL)CYCLOPROPYLIDENEMETHYL - PURINES AND -PYRIMIDINES AS ANTIVIRAL AGENTS 审中-公开
公开(公告)号：WO2003104440A3
公开(公告)日：2003-12-18
申请号：PCT/US2003/007916
申请日：2003-03-14
申请人： WAYNE STATE UNIVERSITY , THE REGENTS OF THE UNIVERSITY OF MICHIGAN , ZEMLICKA, Jiri , ZHOU, Shaoman , DRACH,John, C.
发明人： ZEMLICKA, Jiri , ZHOU, Shaoman , DRACH,John, C.
IPC分类号： C07D473/16
摘要： Compounds which are active against viruses have the following formulas: Formula (I), Formula (II), wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include 6-aminopurine (adenine), 6-hydroxypurine (hypoxanthine), 2-amino-6-hydroxypurine (guanine), 2,6-diamino-purine, 2-amino-6-azidopurine, 2-amino-6-halo substituted purines such as 2-amino6-chloropurine, 2-amino-6-fluoropurine, 2-amino-6-alkoxypurines such as 2-amino-6-methoxypurine, 2-amino-6-cyclopropylaminopurine, 2-amino-6-alkylamino or 2-amino-6-dialkylamino substituted purines, 2-amino-6-thiopurine, 2-amino-6-alkylthio substituted purines, 3-deazapurines, 7-deazapurines and 8-azapurines. The pyrimidine incorporates cytosine, uracil and thymine, 5-halo substituted cytosines and uracils, 5-alkyl substituted cytosines and uracils including derivatives with a saturated or unsaturated alkyl group and 6-azapyrimidines.

4. 发明申请

WO2003104440A2 2,2-BIS(HYDROXYMETHYL)CYCLOPROPYLIDENEMETHYL - PURINES AND -PYRIMIDINES AS ANTIVIRAL AGENTS 审中-公开
标题翻译： 2,2-BIS（羟甲基）环丙基二乙烯基 - 嘌呤和嘧啶类作为抗病毒剂
公开(公告)号：WO2003104440A2
公开(公告)日：2003-12-18
申请号：PCT/US2003/007916
申请日：2003-03-14
申请人： WAYNE STATE UNIVERSITY , THE REGENTS OF THE UNIVERSITY OF MICHIGAN , ZEMLICKA, Jiri , ZHOU, Shaoman , DRACH,John, C.
发明人： ZEMLICKA, Jiri , ZHOU, Shaoman , DRACH,John, C.
IPC分类号： C12N
CPC分类号： C07D239/36 , C07D239/54 , C07D473/18 , C07D473/30 , C07D473/34 , C07D473/40
摘要： Compounds which are active against viruses have the following formulas: Formula (I), Formula (II), wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include 6-aminopurine (adenine), 6-hydroxypurine (hypoxanthine), 2-amino-6-hydroxypurine (guanine), 2,6-diamino-purine, 2-amino-6-azidopurine, 2-amino-6-halo substituted purines such as 2-amino6-chloropurine, 2-amino-6-fluoropurine, 2-amino-6-alkoxypurines such as 2-amino-6-methoxypurine, 2-amino-6-cyclopropylaminopurine, 2-amino-6-alkylamino or 2-amino-6-dialkylamino substituted purines, 2-amino-6-thiopurine, 2-amino-6-alkylthio substituted purines, 3-deazapurines, 7-deazapurines and 8-azapurines. The pyrimidine incorporates cytosine, uracil and thymine, 5-halo substituted cytosines and uracils, 5-alkyl substituted cytosines and uracils including derivatives with a saturated or unsaturated alkyl group and 6-azapyrimidines.
摘要翻译：对病毒有活性的化合物具有下式：式（I），式（II），其中B是嘌呤或嘧啶杂环或碱基。在优选的实施方案中，嘌呤包括6-氨基嘌呤（腺嘌呤），6-羟基嘌呤（次黄嘌呤），2-氨基-6-羟基嘌呤（鸟嘌呤），2,6-二氨基嘌呤，2-氨基-6-叠氮基嘌呤，2 2-氨基-6-氯嘌呤，2-氨基-6-氟嘌呤，2-氨基-6-氟代嘌呤，2-氨基-6-甲氧基嘌呤，2-氨基-6-环丙基氨基嘌呤，2 2-氨基-6-烷基氨基或2-氨基-6-二烷基氨基取代的嘌呤，2-氨基-6-硫嘌呤，2-氨基-6-烷硫基取代的嘌呤，3-脱氮嘌呤，7-脱氮嘌呤和8-氮杂嘌呤。嘧啶含有胞嘧啶，尿嘧啶和胸腺嘧啶，5-卤素取代的胞嘧啶和尿嘧啶，5-烷基取代的胞嘧啶和尿嘧啶，包括具有饱和或不饱和烷基的衍生物和6-氮杂嘧啶。

5. 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。

6. 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.

7. 发明授权

EP1490368B1 2,2-BIS(HYDROXYMETHYL)CYCLOPROPYLIDENEMETHYL - PURINES AND -PYRIMIDINES AS ANTIVIRAL AGENTS 有权转让
标题翻译： 2,2-双（羟甲基）亚环丙基甲基嘌呤和嘧啶作为抗病毒剂
公开(公告)号：EP1490368B1
公开(公告)日：2011-08-03
申请号：EP03748894.7
申请日：2003-03-14
申请人： WAYNE STATE UNIVERSITY , THE REGENTS OF THE UNIVERSITY OF MICHIGAN
发明人： ZEMLICKA, Jiri , DRACH,John, C. , ZHOU, Shaoman
IPC分类号： C07D473/16 , C07D473/18 , C07D239/32 , C07D239/48 , C07D239/52 , A61K31/52 , A61K31/522 , A61K31/505 , A61P31/22
CPC分类号： C07D239/36 , C07D239/54 , C07D473/18 , C07D473/30 , C07D473/34 , C07D473/40
摘要： Compounds which are active against viruses have the following formulas: Formula (I), Formula (II), wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include 6-aminopurine (adenine), 6-hydroxypurine (hypoxanthine), 2-amino-6-hydroxypurine (guanine), 2,6-diamino-purine, 2-amino-6-azidopurine, 2-amino-6-halo substituted purines such as 2-amino6-chloropurine, 2-amino-6-fluoropurine, 2-amino-6-alkoxypurines such as 2-amino-6-methoxypurine, 2-amino-6-cyclopropylaminopurine, 2-amino-6-alkylamino or 2-amino-6-dialkylamino substituted purines, 2-amino-6-thiopurine, 2-amino-6-alkylthio substituted purines, 3-deazapurines, 7-deazapurines and 8-azapurines. The pyrimidine incorporates cytosine, uracil and thymine, 5-halo substituted cytosines and uracils, 5-alkyl substituted cytosines and uracils including derivatives with a saturated or unsaturated alkyl group and 6-azapyrimidines.

8. 发明公开

EP1490368A2 2,2-BIS(HYDROXYMETHYL)CYCLOPROPYLIDENEMETHYL - PURINES AND -PYRIMIDINES AS ANTIVIRAL AGENTS 有权转让
标题翻译： 2,2-双（羟甲基）亚环丙基甲基嘌呤和嘧啶作为抗病毒剂
公开(公告)号：EP1490368A2
公开(公告)日：2004-12-29
申请号：EP03748894.7
申请日：2003-03-14
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： C07D473/16 , C07D473/18 , C07D239/32 , C07D239/48 , C07D239/52 , A61K31/52 , A61K31/522 , A61K31/505 , A61P31/22
CPC分类号： C07D239/36 , C07D239/54 , C07D473/18 , C07D473/30 , C07D473/34 , C07D473/40
摘要： Compounds which are active against viruses have the following formulas: Formula (I), Formula (II), wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include 6-aminopurine (adenine), 6-hydroxypurine (hypoxanthine), 2-amino-6-hydroxypurine (guanine), 2,6-diamino-purine, 2-amino-6-azidopurine, 2-amino-6-halo substituted purines such as 2-amino6-chloropurine, 2-amino-6-fluoropurine, 2-amino-6-alkoxypurines such as 2-amino-6-methoxypurine, 2-amino-6-cyclopropylaminopurine, 2-amino-6-alkylamino or 2-amino-6-dialkylamino substituted purines, 2-amino-6-thiopurine, 2-amino-6-alkylthio substituted purines, 3-deazapurines, 7-deazapurines and 8-azapurines. The pyrimidine incorporates cytosine, uracil and thymine, 5-halo substituted cytosines and uracils, 5-alkyl substituted cytosines and uracils including derivatives with a saturated or unsaturated alkyl group and 6-azapyrimidines.

9. 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.

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