专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明专利

AU2003296360A8 Dioxolane thymine and combinations for use against 3tc/ azt resistant strains of hiv 未知
公开(公告)号：AU2003296360A8
公开(公告)日：2004-06-30
申请号：AU2003296360
申请日：2003-12-08
申请人： UNIV EMORY , THE UNIVERSITY OF GEORGIA RESEARCH FOUNDATION INC
发明人： CHU CHUNG K , SCHINAZI RAYMOND F
IPC分类号： A61K31/505 , A61K31/513 , A61K31/52 , A61K31/65 , A61K31/675 , A61K31/70 , A61K45/06
摘要： The present invention relates to the use of a dioxolane thymine compound according to the chemical structure of Formula (I): where R1 is H, an acyl group, a C1-C20 alkyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group, for use in the treatment of HIV infections which exhibit resistance to 3TC and/or AZT. Preferably, compounds according to the present invention are combined with at least one anti-HIV agent which inhibits HIV by a mechanism other than through the inhibition of thymidine kinase (TK). These agents include those selected from among nuleocoside reverse transcriptase inhibitors (NRTI), non-nucloeoside reverse transcriptase inhibitors, protease inhibitors, fusion inhibitors, among others. These agents are generally selected from the group consisting of 3TC (Lamivudine), AZT (Zidovudine), (-)-FTC, ddI (Didanosine), ddC (zalcitabine), abacavir (ABC), tenofovir (PMPA), D-D4FC (Reverset), D4T (Stavudine), Racivir, L-D4FC, NVP (Nevirapine), DLV (Delavirdine), EFV (Efavirenz), SQVM (Saquinavir mesylate), RTV (Ritonavir), IDV (Indinavir), SQV (Saquinavir), NFV (Nelfinavir), APV (Amprenavir), LPV (Lopinavir), fuseon and mixtures thereof. The TK dependent agents, such as AZT and D4T, may be used in combination with one of the dioloxane thymine compounds according to the present invention, but the use of such agents may be less preferred. In preferred compositions according to the present invention, R1 is preferably H or a C2-C18 acyl group or a monophosphate group. Pharmaceutical compositions and methods of reducing the likelihood that a patient at risk for contract an HIV infection will contract the infection are other aspects of the present invention.

2. 发明专利

JP2002114787A ENANTIOMERICALLY PURE beta-D-DIOXOLANE-NUCLEOSIDE 审中-公开
公开(公告)号：JP2002114787A
公开(公告)日：2002-04-16
申请号：JP2001251947
申请日：2001-08-22
申请人： UNIV OF GEORGIA RES FOUNDATION , UNIV EMORY
发明人： CHU CHUNG K , SCHINAZI RAYMOND F
IPC分类号： C07D473/18 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/52 , A61K31/522 , A61K31/53 , A61K31/675 , A61K31/7076 , A61K38/21 , A61P31/12 , A61P31/18 , A61P37/04 , C07D327/04 , C07D405/04 , C07D411/04 , C07D473/00 , C07D473/16 , C07D473/30 , C07D473/34 , C07D473/40 , C07D497/08 , C07F9/6561
摘要： PROBLEM TO BE SOLVED: To obtain an organic compound having antiviral activity, especially enantiomerically pure β-D-dioxolane-nucleoside. SOLUTION: A method and composition for the treatment of humans infected with HIV that includes administration of an HIV treatment amount of an enantiomerically pure β-D-dioxolanyl purine nucleoside of formula (I) (R is OH, Cl, NH2 or H) or a pharmaceutically acceptable salt or derivative of the compound, optionally in a pharmaceutically acceptable carrier or diluent.

3. 发明专利

JP2001097973A ENANTIOMERICALLY PURE beta-D-(-)-dioxolane-nucleoside 失效
公开(公告)号：JP2001097973A
公开(公告)日：2001-04-10
申请号：JP2000246125
申请日：2000-08-15
申请人： UNIV OF GEORGIA RES FOUNDATION , UNIV EMORY
发明人： CHU CHUNG K , SCHINAZI RAYMOND F
IPC分类号： C07D473/18 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/52 , A61K31/522 , A61K31/53 , A61K31/675 , A61K31/7076 , A61P31/12 , A61P31/18 , A61P37/04 , C07D327/04 , C07D405/04 , C07D411/04 , C07D473/00 , C07D473/30 , C07D473/34 , C07D473/40 , C07D497/08
摘要： PROBLEM TO BE SOLVED: To provide a method for producing a compound having high HIV activity. SOLUTION: A process for the preparation of enantiomerically pure β-D-(-)- dxoxolane-nucleosides (e.g. a compound represented by formula 2 when thymine is used as a base) comprises a step for preparing a dioxolane ring from 1,6- anhydromannose represented by formula 1. The base is selected from adenine, hypoxanthine, cytosine, uracil, etc., in addition to thymine.

4. 发明公开

EP1478322A4 Beta-2'-OR 3'-HALONUCLEOSIDES 审中-公开
标题翻译： β-2'-或3'-卤代核糖
公开(公告)号：EP1478322A4
公开(公告)日：2007-08-08
申请号：EP02756310
申请日：2002-06-24
申请人： PHARMASSET LTD , UNIV GEORGIA RES FOUND , UNIV EMORY
发明人： CHU CHUNG K , OTTO MICHAEL J , SHI JUNXING , SCHINAZI RAYMOND F , CHOI YONGSEOK , GUMINA GIUSEPPE , CHONG YOUHOON , STUYVER LIEVEN J
IPC分类号： A01N43/04 , A61K31/52 , A61K31/522 , A61K31/675 , A61K31/70 , A61K31/7064 , A61K31/7068 , A61K31/7076 , A61K45/00 , A61P31/14 , A61P31/18 , A61P35/00 , C07H9/04 , C07H19/06 , C07H19/16
CPC分类号： A61K31/70 , A61K31/52 , A61K31/522 , A61K31/675 , C07H9/04 , C07H19/06
摘要： The present invention includes compounds and compositions of β-halonucleosides, as well as methods to treat HIV, HBV or abnormal cellular proliferation comprising administering said compounds or compositions.
摘要翻译：本发明包括β-卤代核苷的化合物和组合物，以及治疗HIV，HBV或异常细胞增殖的方法，包括施用所述化合物或组合物。

5. 发明申请

WO9014831A3 3'-AZIDO-2',3'-DIDEOXY-5-METHYLCYTIDINE ANTI-VIRAL COMPOSITION 审中-公开
标题翻译： 3'-AZIDO-2'，3'-DIDEOXY-5-METHYLCYTIDINE ANTI-VIRAL COMPOSITION
公开(公告)号：WO9014831A3
公开(公告)日：1991-01-24
申请号：PCT/US9003207
申请日：1990-06-06
申请人： UNIV GEORGIA RES FOUND , UNIV EMORY
发明人： CHU CHUNG K , SCHINAZY RAYMOND F
IPC分类号： A61K31/70 , A61P31/12 , C07D405/04 , C07H19/06 , C07H19/10
CPC分类号： A61K31/70 , C07D405/04 , C07H19/06 , C07H19/10
摘要： A composition delivering an HIV-inhibitory amount of an active compound of general formula (I) wherein R is OH, monophosphate, diphosphate, or triphosphate, or a pharmacologically acceptable salt thereof; and wherein the means is a pharmaceutically acceptable carrier. In the preferred embodiment, an effective dose of 3'-azido-2',3'-dideoxy-5-methylcytidine, or its derivatives, is administered in a pharmaceutically acceptable carrier to a patient for the treatment of AIDS.

6. 发明公开

EP1569659A4 DIOXOLANE THYMINE AND COMBINATIONS FOR USE AGAINST 3TC/ AZT RESISTANT STRAINS OF HIV 审中-公开
标题翻译：二氧THYMINUND组合AGAINST 3TC / AZT耐药的HIV毒株
公开(公告)号：EP1569659A4
公开(公告)日：2009-03-25
申请号：EP03812874
申请日：2003-12-08
申请人： UNIV GEORGIA RES FOUND , UNIV EMORY
发明人： CHU CHUNG K , SCHINAZI RAYMOND F
IPC分类号： A61K31/70 , A61K31/505 , A61K31/513 , A61K31/52 , A61K31/65 , A61K31/675 , A61K45/06 , A61P31/18
CPC分类号： A61K45/06 , A61K31/505 , A61K31/513 , A61K31/52 , A61K31/65 , A61K31/675 , A61K31/70 , A61K2300/00
摘要： The present invention relates to the use of a dioxolane thymine compound according to the chemical structure of Formula (I): where R1 is H, an acyl group, a C1-C20 alkyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group, for use in the treatment of HIV infections which exhibit resistance to 3TC and/or AZT. Preferably, compounds according to the present invention are combined with at least one anti-HIV agent which inhibits HIV by a mechanism other than through the inhibition of thymidine kinase (TK). These agents include those selected from among nucleoside reverse transcriptase inhibitors (NRTI), non-nucloeoside reverse transcriptase inhibitors, protease inhibitors, fusion inhibitors, among others. These agents are generally selected from the group consisting of 3TC (Lamivudine), AZT (Zidovudine), (-)-FTC, ddI (Didanosine), ddC (zalcitabine), abacavir (ABC), tenofovir (PMPA), D-D4FC (Reverset), D4T (Stavudine), Racivir, L-D4FC, NVP (Nevirapine), DLV (Delavirdine), EFV (Efavirenz), SQVM (Saquinavir mesylate), RTV (Ritonavir), IDV (Indinavir), SQV (Saquinavir), NFV (Nelfinavir), APV (Amprenavir), LPV (Lopinavir), fuseon and mixtures thereof. The TK dependent agents, such as AZT and D4T, may be used in combination with one of the dioloxane thymine compounds according to the present invention, but the use of such agents may be less preferred. In preferred compositions according to the present invention, Rl is preferably H or a C2-C18 acyl group or a monophosphate group. Pharmaceutical compositions and methods of reducing the likelihood that a patient at risk for contract an HIV infection will contract the infection are other aspects of the present invention.

7. 发明公开

EP0852499A4 THERAPEUTIC AZIDE COMPOUNDS 失效
标题翻译：疗效叠氮化
公开(公告)号：EP0852499A4
公开(公告)日：2001-03-07
申请号：EP96932197
申请日：1996-09-06
申请人： UNIV GEORGIA RES FOUND , UNIV EMORY
发明人： CHU CHUNG K , KOTRA LAKSHIMI , MANOUILOV KOSTANTIN , DU JINFA , SCHINAZI RAYMOND
IPC分类号： C07D499/21 , A61K31/00 , A61K31/505 , A61K31/52 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/706 , A61K31/7064 , A61K31/7076 , A61K47/48 , A61P43/00 , C07D239/46 , C07D473/16 , C07D473/34 , C07D501/14 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/167 , C07H19/173 , C07H19/19 , C07H19/20
CPC分类号： A61K31/7076 , A61K47/52 , C07H19/04 , C07H19/10 , C07H19/16 , C07H19/20
摘要： Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and hydroxy substituents are converted in vivo to the corresponding drugs, increasing the half-life of the drugs. In addition azide prodrugs are often better able to penetrate the blood-brain barrier than the corresponding drugs. Especially useful are azide derivatives of cordycepin, 2'-F-ara-ddI, AraA, acyclovir, penciclovir and related drugs. Useful azide prodrugs are azide derivatives of therapeutic alicyclic amines, ketones, and hydroxy-substituted compounds, including aralkyl, heterocyclic aralkyl, and cyclic aliphatic compounds, where the amine or oxygen moiety is on the ring, or where the amine or oxygen moiety is on an aliphatic side chain, as well as therapeutic purines and pyrimidines, nucleoside analogs and phosphorylated nucleoside analogs.

8. 发明公开

EP0656778A4 ENANTIOMERICALLY PURE -g(b)-D-DIOXOLANE-NUCLEOSIDES. 失效
标题翻译：完全自由基β-D-DIOXOLAN-NUKLEOSIDE。
公开(公告)号：EP0656778A4
公开(公告)日：1995-08-02
申请号：EP93920366
申请日：1993-08-25
申请人： UNIV GEORGIA , UNIV EMORY
发明人： CHU CHUNG K , SCHINAZI RAYMOND F
IPC分类号： C07D473/18 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/52 , A61K31/522 , A61K31/53 , A61K31/675 , A61K31/7076 , A61K38/21 , A61P31/12 , A61P31/18 , A61P37/04 , C07D327/04 , C07D405/04 , C07D411/04 , C07D473/00 , C07D473/16 , C07D473/30 , C07D473/34 , C07D473/40 , C07D497/08 , C07F9/6561 , C07F5/02
CPC分类号： C07D473/00 , A61K31/675 , A61K31/70 , A61K31/704 , A61K31/7076 , A61K38/21 , C07B2200/07 , C07D327/04 , C07D411/04 , C07D497/08 , A61K2300/00

9. 发明申请

WO2004052296A2 DIOXOLANE THYMINE AND COMBINATIONS FOR USE AGAINST 3TC/ AZT RESISTANT STRAINS OF HIV 审中-公开
标题翻译：二氧六环三胺及其组合用于抗HIV 3TC / AZT抗性株
公开(公告)号：WO2004052296A2
公开(公告)日：2004-06-24
申请号：PCT/US0339029
申请日：2003-12-08
申请人： UNIV GEORGIA RES FOUND , UNIV EMORY , CHU CHUNG K , SCHINAZI RAYMOND F
发明人： CHU CHUNG K , SCHINAZI RAYMOND F
IPC分类号： A61K31/505 , A61K31/513 , A61K31/52 , A61K31/65 , A61K31/675 , A61K31/70 , A61K45/06 , A61K
CPC分类号： A61K45/06 , A61K31/505 , A61K31/513 , A61K31/52 , A61K31/65 , A61K31/675 , A61K31/70 , A61K2300/00
摘要： The present invention relates to the use of a dioxolane thymine compound according to the chemical structure of Formula (I): where R is H, an acyl group, a C1-C20 alkyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group, for use in the treatment of HIV infections which exhibit resistance to 3TC and/or AZT. Preferably, compounds according to the present invention are combined with at least one anti-HIV agent which inhibits HIV by a mechanism other than through the inhibition of thymidine kinase (TK). These agents include those selected from among nucleoside reverse transcriptase inhibitors (NRTI), non-nucloeoside reverse transcriptase inhibitors, protease inhibitors, fusion inhibitors, among others. These agents are generally selected from the group consisting of 3TC (Lamivudine), AZT (Zidovudine), (-)-FTC, ddI (Didanosine), ddC (zalcitabine), abacavir (ABC), tenofovir (PMPA), D-D4FC (Reverset), D4T (Stavudine), Racivir, L-D4FC, NVP (Nevirapine), DLV (Delavirdine), EFV (Efavirenz), SQVM (Saquinavir mesylate), RTV (Ritonavir), IDV (Indinavir), SQV (Saquinavir), NFV (Nelfinavir), APV (Amprenavir), LPV (Lopinavir), fuseon and mixtures thereof. The TK dependent agents, such as AZT and D4T, may be used in combination with one of the dioloxane thymine compounds according to the present invention, but the use of such agents may be less preferred. In preferred compositions according to the present invention, R is preferably H or a C2-C18 acyl group or a monophosphate group. Pharmaceutical compositions and methods of reducing the likelihood that a patient at risk for contract an HIV infection will contract the infection are other aspects of the present invention.
摘要翻译：本发明涉及根据式（I）的化学结构的二氧戊环胸腺嘧啶化合物的用途：其中R 1是H，酰基，C 1 -C 20烷基或醚基团，磷酸盐，二磷酸盐，三磷酸盐或磷酸二酯基团，用于治疗对3TC和/或AZT表现出抗性的HIV感染。优选地，根据本发明的化合物与至少一种通过除抑制胸苷激酶（TK）之外的机制抑制HIV的抗HIV剂组合。这些药剂包括选自核苷逆转录酶抑制剂（NRTI），非核苷逆转录酶抑制剂，蛋白酶抑制剂，融合抑制剂等等的那些。这些药物通常选自3TC（拉米夫定），AZT（齐多夫定），（ - ） - FTC，ddI（去甲肌苷），ddC（扎西他滨），abacavir（ABC），替诺福韦（PMPA），D-D4FC （NVR），DLV（Delavirdine），EFV（Efavirenz），SQVM（甲磺酸沙奎那韦），RTV（利托那韦），IDV（茚地那韦），SQV（沙奎那韦）， NFV（奈非那韦），APV（安普那韦），LPV（洛匹那韦），fuseon及其混合物。诸如AZT和D4T的TK依赖性试剂可以与根据本发明的二
恶烷胸腺嘧啶化合物之一组合使用，但是使用这种试剂可能不太优选。在根据本发明的优选组合物中，R 1优选为H或C 2 -C 18酰基或单磷酸酯基团。降低感染HIV感染风险的患者感染感染的可能性的药物组合物和方法是本发明的其他方面。

10. 发明申请

WO9014831A2 3'-AZIDO-2',3'-DIDEOXY-5-METHYLCYTIDINE ANTI-VIRAL COMPOSITION 审中-公开
标题翻译： 3'-AZIDO-2'，3'-DIDEOXY-5-METHYLCYTIDINE ANTI-VIRAL COMPOSITION
公开(公告)号：WO9014831A2
公开(公告)日：1990-12-13
申请号：PCT/US9003207
申请日：1990-06-06
申请人： UNIV GEORGIA , UNIV EMORY
发明人： CHU CHUNG K , SCHINAZY RAYMOND F
IPC分类号： A61K31/70 , A61P31/12 , C07D405/04 , C07H19/06 , C07H19/10
CPC分类号： A61K31/70 , C07D405/04 , C07H19/06 , C07H19/10
摘要： A composition delivering an HIV-inhibitory amount of an active compound of general formula (I) wherein R is OH, monophosphate, diphosphate, or triphosphate, or a pharmacologically acceptable salt thereof; and wherein the means is a pharmaceutically acceptable carrier. In the preferred embodiment, an effective dose of 3'-azido-2',3'-dideoxy-5-methylcytidine, or its derivatives, is administered in a pharmaceutically acceptable carrier to a patient for the treatment of AIDS.
摘要翻译：一种组合物，其输送HIV抑制量的通式（I）的活性化合物，其中R是OH，单磷酸酯，二磷酸酯或三磷酸酯，或其药理学上可接受的盐; 并且其中所述方法是药学上可接受的载体。在优选的实施方案中，将有效剂量的3'-叠氮基-2'，3'-二脱氧-5-甲基胞苷或其衍生物在药学上可接受的载体中施用于患者用于治疗AIDS。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式