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1. 发明申请

WO0026225A3 NUCLEOSIDES WITH ANTI-HEPATITIS B VIRUS ACTIVITY 审中-公开
标题翻译：具有抗乙型肝炎病毒活性的核苷
公开(公告)号：WO0026225A3
公开(公告)日：2000-10-05
申请号：PCT/US9926157
申请日：1999-11-05
申请人： CENTRE NAT RECH SCIENT , UAB RESEARCH FOUNDATION , UNIV EMORY , GOSSELIN GILLES , IMBACH JEAN LOUIS , SOMMADOSSI JEAN PIERRE , SCHINAZI RAYMOND F
发明人： GOSSELIN GILLES , IMBACH JEAN-LOUIS , SOMMADOSSI JEAN-PIERRE , SCHINAZI RAYMOND F
IPC分类号： A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61P31/20 , C07H19/06 , C07H19/10 , A61K31/70 , A61P31/12
CPC分类号： C07H19/06 , C07H19/10
摘要： Compounds and pharmaceutical compositions active against hepatitis B virus are provided, as is a method for the treatment of hepatitis B virus infection in humans and other host animals is provided comprising administering an effective amount of a beta -L-(2' or 3'- azido)-2',3'-dideoxy-5-fluorocytosine of formula (I) wherein R is H, acyl, monophosphate, diphosphate, or triphosphate, or a stabilized phosphate derivative (to form a stabilized nucleotide prodrug), and R' is H, acyl, or alkyl.
摘要翻译：提供了对乙型肝炎病毒具有活性的化合物和药物组合物，以及治疗人和其他宿主动物的乙型肝炎病毒感染的方法，包括给予有效量的β-L-（2'或3'- （其中R是H，酰基，单磷酸酯，二磷酸酯或三磷酸酯）或稳定的磷酸酯衍生物（以形成稳定化的核苷酸前体药物）的式（I）的叠氮基）-2'，3'-二脱氧-5-氟胞嘧啶，是H，酰基或烷基。

2. 发明申请

WO2010091386A3 PURINE NUCLEOSIDE MONOPHOSPHATE PRODRUGS FOR TREATMENT OF CANCER AND VIRAL INFECTIONS 审中-公开
标题翻译：嘌呤核苷单磷酸酯前体治疗癌症和病毒感染
公开(公告)号：WO2010091386A3
公开(公告)日：2010-12-09
申请号：PCT/US2010023563
申请日：2010-02-09
申请人： RFS PHARMA LLC , UNIV EMORY , CHO JONG HYUN , COATS STEVEN J , SCHINAZI RAYMOND F , ZHANG HONGWANG , ZHOU LONGHU
发明人： CHO JONG HYUN , COATS STEVEN J , SCHINAZI RAYMOND F , ZHANG HONGWANG , ZHOU LONGHU
IPC分类号： C07D487/04 , A61K31/7028 , A61P31/12 , A61P35/00 , C07D405/04
CPC分类号： A61K31/7076 , A61K31/675 , A61K31/7028 , A61K31/7042 , A61K31/7052 , A61K31/706 , A61K31/7064 , A61K31/7068 , A61K31/708 , A61K45/06 , C07D473/16 , C07H19/173 , C07H19/20 , A61K2300/00
摘要： The present invention is directed to compounds, compositions and methods for treating or preventing cancer and viral infections, in particular, HIV, HCV, Norovirus, Saporo virus, HSV-I, HSV-2, Dengue virus, Yellow fever, and HBV in human patients or other animal hosts. The compounds are certain 6-substituted purine monophosphates, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof. In particular, the compounds show potent antiviral activity against HIV-I, HIV-2, HCV, Norovirus, Saporovirus, HSV-I, HSV-2, Dengue virus, Yellow fever, and HBV.
摘要翻译：本发明涉及用于治疗或预防人体内癌症和病毒感染，特别是HIV，HCV，诺如病毒，Saporo病毒，HSV-1，HSV-2，登革病毒，黄热病和HBV的化合物，组合物和方法患者或其他动物宿主。这些化合物是某些6-取代的单磷酸嘌呤及其药学上可接受的盐，前药和其它衍生物。特别是，这些化合物显示出对HIV-1，HIV-2，HCV，诺如病毒，Saporovirus，HSV-1，HSV-2，登革热病毒，黄热病和HBV有效的抗病毒活性。

3. 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。

4. 发明申请

WO2012078416A2 MONOPHOSPHATE PRODRUGS OF DAPD AND ANALOGS THEREOF 审中-公开
标题翻译： DAPD及其类似物的单磷酸酯产物
公开(公告)号：WO2012078416A2
公开(公告)日：2012-06-14
申请号：PCT/US2011062484
申请日：2011-11-29
申请人： RFS PHARMA LLC , UNIV EMORY , SCHINAZI RAYMOND F , COATS STEVEN J
发明人： SCHINAZI RAYMOND F , COATS STEVEN J
IPC分类号： C07H19/16 , A61K31/7076 , A61P31/18 , A61P31/20 , C07H19/20 , C07H21/00
CPC分类号： A61K31/7072 , A61K31/675 , A61K45/06 , C07F9/65616 , A61K2300/00
摘要： The present invention is directed to compounds, compositions and methods for treating or preventing cancer and viral infections, in particular, HIV and HBV, in human patients or other animal hosts. The compounds are certain 6-substituted-2- amino-purine dioxolane monophosphates or phosphonates, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof.
摘要翻译：本发明涉及在人类患者或其他动物宿主中治疗或预防癌症和病毒感染，特别是HIV和HBV的化合物，组合物和方法。这些化合物是某些6-取代-2-氨基 - 嘌呤二氧戊环单磷酸酯或膦酸酯及其药学上可接受的盐，前药和其它衍生物。

5. 发明申请

WO2004013298A3 2',3'-DIDEOXYNUCLEOSIDE ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVITRIDAE INFECTIONS 审中-公开
标题翻译：用于治疗或预防黄病毒感染的2'，3'-二脱氧核苷类似物
公开(公告)号：WO2004013298A3
公开(公告)日：2004-04-01
申请号：PCT/US0324288
申请日：2003-08-01
申请人： PHARMASSET LTD , UNIV EMORY , UNIV LELAND STANFORD JUNIOR , SHI JUNXING , SCHINAZI RAYMOND F , STRIKER ROBERT
发明人： SHI JUNXING , SCHINAZI RAYMOND F , STRIKER ROBERT
IPC分类号： A61K31/513 , A61K31/553 , A61K31/58 , A61K31/7056 , A61K31/7068 , A61K31/7072 , A61K38/20 , A61K38/21 , C07H19/06
CPC分类号： C07H19/06 , A61K31/513 , A61K31/553 , A61K31/58 , A61K31/7056 , A61K31/7068 , A61K31/7072 , A61K38/2066 , A61K38/21 , A61K2300/00
摘要： A method for the treatment or prevention of Flaviviridae infections, in particular, hepatitis C virus infection, in a host, and in particular, a human, is provided that includes administering an effective amount of a R-L- or (3-D-2',3'-dideoxynucleoside or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable diluent or excipient.
摘要翻译：提供了用于治疗或预防宿主特别是人类中黄病毒科感染，特别是丙型肝炎病毒感染的方法，其包括施用有效量的RL-或（3-D-2' ，3'-双脱氧核苷或其药学上可接受的盐或前药，任选地在药学上可接受的稀释剂或赋形剂中。

6. 发明申请

WO0043014A3 BETA-D-2',3'-DIDEHYDRO-2',3'-DIDEOXY-5-FLUOROCYTIDINE FOR USE IN THE TREATMENT OF HIV INFECTIONS 审中-公开
标题翻译：用于治疗艾滋病毒感染的β-D-2'，3'-DIDEHYDRO-2'，3'-DIDEOXY-5-FLUOROCYTIDINE
公开(公告)号：WO0043014A3
公开(公告)日：2000-11-30
申请号：PCT/US0001738
申请日：2000-01-21
申请人： UNIV EMORY , SCHINAZI RAYMOND F , HAMMOND JENNIFER , MELLORS JOHN W , LIOTTA DENNIS C
发明人： SCHINAZI RAYMOND F , HAMMOND JENNIFER , MELLORS JOHN W , LIOTTA DENNIS C
IPC分类号： C12N15/01 , A61K31/513 , A61K31/70 , A61K31/7068 , A61K45/00 , A61K45/06 , A61P31/18
CPC分类号： A61K31/7068 , A61K31/513 , A61K31/52 , A61K31/70 , A61K45/06 , A61K31/535 , A61K2300/00
摘要： The present invention discloses a method for treating HIV that includes administering beta -D-D4FC or its pharmaceutically acceptable salt or prodrug to a human in need of therapy in combination or alternation with a drug that induces a mutation in HIV-1 at a location other than the 70(K to N), 90 or the 172 codons of the reverse transcriptase region. Also disclosed is a method for using beta -D-D4FC as "salvage therapy" to patients which exhibit drug resistance to other anti-HIV agents. beta -D-D4FC can be used generally as salvage therapy for any patient which exhibits resistance to a drug that induces a mutation at other than the 70(K to N), 90 or the 172 codons.
摘要翻译：本发明公开了一种治疗HIV的方法，其包括向与需要治疗的人组合或交替使用β-D-D4FC或其药学上可接受的盐或前药，在其它位置诱导HIV-1突变的药物比70（K至N），90或反转录酶区域的172个密码子。还公开了使用β-D-D4FC作为对其他抗HIV药物具有耐药性的患者的“补救疗法”的方法。一般来说，β-D-D4FC可用于任何对在70（K至N），90或172个密码子以外诱导突变的药物具有抗性的患者的补救疗法。

7. 发明申请

WO2012158811A3 PURINE MONOPHOSPHATE PRODRUGS FOR TREATMENT OF VIRAL INFECTIONS 审中-公开
标题翻译：用于治疗病毒感染的嘌呤一磷酸酯制剂
公开(公告)号：WO2012158811A3
公开(公告)日：2013-02-28
申请号：PCT/US2012038165
申请日：2012-05-16
申请人： RFS PHARMA LLC , SCHINAZI RAYMOND F , CHO JONG HYUN , ZHOU LONGHU , ZHANG HONGWANG , PRADERE UGO , COATS STEVEN J , UNIV EMORY
发明人： SCHINAZI RAYMOND F , CHO JONG HYUN , ZHOU LONGHU , ZHANG HONGWANG , PRADERE UGO , COATS STEVEN J
IPC分类号： C07H19/20 , A61K31/7028 , A61K31/7072 , A61K31/7076 , A61P31/12 , C07D405/04 , C07D487/04 , C07H19/10 , C07H19/173
CPC分类号： C07F9/65586 , A61K31/7076 , A61K45/06 , C07D473/16 , C07F9/65742 , C07H19/20 , C07H19/207 , C07H19/213
摘要： The present invention is directed to compounds, compositions and methods for treating or preventing viral infections using nucleoside analog monophosphate prodrugs. More specifically, HCV, Norovirus, Saporovirus, Dengue virus, Chikungunya virus and Yellow fever in human patients or other animal hosts. The compounds are certain 2,6-diamino 2-C-methyl purine nucleoside monophosphate prodrugs and modified prodrug analogs, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof. In particular, the compounds show potent antiviral activity against HCV, Norovirus, Saporovirus, Dengue virus, Chikungunya virus and Yellow fever. This invention teaches how to modify the metabolic pathway of 2,6-diamino 2'-C-methyl purine and deliver nucleotide triphosphate(s) to polymerases at heretofore unobtainable therapeutically-relevant concentrations.
摘要翻译：本发明涉及使用核苷类似物单磷酸酯前药治疗或预防病毒感染的化合物，组合物和方法。更具体地，在人类患者或其他动物宿主中，HCV，诺如病毒，Saporovirus，登革热病毒，基孔肯雅病毒和黄热病。这些化合物是某些2,6-二氨基2-C-甲基嘌呤核苷单磷酸前体药物和修饰的前药类似物及其药学上可接受的盐，前药和其它衍生物。特别地，这些化合物显示针对HCV，诺如病毒，Saporovirus，登革热病毒，基孔肯雅病毒和黄热病的有效的抗病毒活性。本发明教导了如何修饰2,6-二氨基2'-C-甲基嘌呤的代谢途径，并将迄今为止无法获得的治疗相关浓度的核苷酸三磷酸转移至聚合酶。

8. 发明申请

WO2010068708A2 3'-AZIDO PURINE NUCLEOTIDE PRODRUGS FOR TREATMENT OF VIRAL INFECTIONS 审中-公开
标题翻译：用于治疗病毒感染的3'-AZIDO PURINE NUCLEOTIDE PRODRUGS
公开(公告)号：WO2010068708A2
公开(公告)日：2010-06-17
申请号：PCT/US2009067400
申请日：2009-12-09
申请人： RFS PHARMA LLC , SCHINAZI RAYMOND F , MELLORS JOHN W , SLUIS-CREMER NICOLAS PAUL , AMBLARD FRANK , COATS STEVEN J , SHI JUNXING , WHITAKER RICHARD ANTHONY , UNIV EMORY , UNIV PITTSBURGH
发明人： SCHINAZI RAYMOND F , MELLORS JOHN W , SLUIS-CREMER NICOLAS PAUL , AMBLARD FRANK , COATS STEVEN J , SHI JUNXING , WHITAKER RICHARD ANTHONY
IPC分类号： C07D487/04 , A61K31/437 , A61P31/12 , C07D491/048
CPC分类号： C07D473/34 , A61K31/437 , C07D473/16 , C07D473/18 , C07H19/173 , C07H19/20 , C07H19/207
摘要： The present invention is directed to compounds, compositions and methods for treating or preventing viral infections, in particular, HIV, and HBV, in human patients or other animal hosts. The compounds are 3'-azido-2',3'-dideoxy purine monophosphates, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof. In particular, the compounds show potent antiviral activity against HIV-1 and HBV.
摘要翻译：本发明涉及用于在人类患者或其他动物宿主中治疗或预防病毒感染，特别是HIV和HBV的化合物，组合物和方法。化合物是3'-叠氮基-2'，3'-二脱氧嘌呤单磷酸酯及其药学上可接受的盐，前药和其它衍生物。特别地，这些化合物对HIV-1和HBV显示有效的抗病毒活性。

9. 发明申请

WO2012027712A2 POTENT AND SELECTIVE INHIBITORS OF HEPATITIS C VIRUS 审中-公开
标题翻译：丙型肝炎病毒潜伏和选择性抑制剂
公开(公告)号：WO2012027712A2
公开(公告)日：2012-03-01
申请号：PCT/US2011049426
申请日：2011-08-26
申请人： RFS PHARMA LLC , UNIV EMORY , COATS STEVEN J , AMBLARD FRANCK , ZHANG HONGWANG , ZHOU LONGHU , WHITAKER RICHARD ANTHONY , MCBRAYER TAMARA ROSARIO , SCHINAZI RAYMOND F , SHI JUNXING
发明人： COATS STEVEN J , AMBLARD FRANCK , ZHANG HONGWANG , ZHOU LONGHU , WHITAKER RICHARD ANTHONY , MCBRAYER TAMARA ROSARIO , SCHINAZI RAYMOND F , SHI JUNXING
IPC分类号： C07D403/04 , A61K31/4178 , A61P31/14 , C07D403/14 , C07D405/14 , C07D413/14
CPC分类号： C07D403/14 , A61K31/4178 , A61K31/4192 , A61K31/444 , A61K31/506 , A61K31/5377 , A61K31/655 , A61K45/06 , C07D401/14 , C07D403/04 , C07D405/14 , C07D407/14 , C07D413/14
摘要： The present invention is directed to compounds, compositions and methods for treating or preventing hepatitis C virus (HCV) infection in human subjects or other animal hosts. The compounds are as also pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof as pharmaceutical compositions and methods for treatment or prevention of HCV infection.
摘要翻译：本发明涉及用于治疗或预防人受试者或其他动物宿主中丙型肝炎病毒（HCV）感染的化合物，组合物和方法。这些化合物也是药学上可接受的，盐，前药和其它衍生物，作为用于治疗或预防HCV感染的药物组合物和方法。

10. 发明申请

WO2011041512A3 COMPOSITIONS AND METHODS FOR TREATING MLV-INFECTION, AND PREVENTING AND TREATING MLV-INITIATED DISEASES 审中-公开
标题翻译：治疗MLV感染的组合物和方法，以及预防和治疗MLV引发的疾病
公开(公告)号：WO2011041512A3
公开(公告)日：2011-09-29
申请号：PCT/US2010050864
申请日：2010-09-30
申请人： UNIV EMORY , UNIV UTAH , SCHINAZI RAYMOND F , SINGH ILA
发明人： SCHINAZI RAYMOND F , SINGH ILA
IPC分类号： A61K31/475 , A61K31/4738 , A61K31/4745 , A61P35/00
CPC分类号： A61K31/4738 , A61K31/4745 , A61K31/475 , A61K45/06 , A61K2300/00
摘要： Compositions and methods for inhibiting infection by XMRV or other MLV are disclosed. Also disclosed are methods for treating cancers resulting from infection by XMRV or other MLV, and for preventing such cancers. The anti- XMRV/anti-MLV compounds are predominantly integrase inhibitors, such as globoidnan A, L-000870812, S/GSK1349572, S/GSK1265744, Raltegravir and Elvitegravir, and also reverse transcriptase inhibitors AZT, tenofovir, and tenofovir DF. The compounds are also useful for treating chronic fatigue syndrome or other diseases with neuroimmune symptoms resulting from an infection by XMRV or other MLV. The compositions can also include other therapeutic agents known for treating prostate cancer, breast cancer, lymphomas, and leukemias, such as anti-androgenic agents, radioisotopes, and conventional anti-cancer compounds.
摘要翻译：公开了用于抑制XMRV或其他MLV感染的组合物和方法。还公开了治疗由XMRV或其他MLV感染引起的癌症和用于预防这些癌症的方法。抗XMRV /抗MLV化合物主要是整合酶抑制剂，例如globoidnan A，L-000870812，S / GSK1349572，S / GSK1265744，Raltegravir和Elvitegravir，以及逆转录酶抑制剂AZT，替诺福韦和替诺福韦DF。该化合物还可用于治疗由XMRV或其他MLV感染引起的神经免疫症状的慢性疲劳综合征或其他疾病。组合物还可以包含已知用于治疗前列腺癌，乳腺癌，淋巴瘤和白血病的其他治疗剂，例如抗雄激素药，放射性同位素和常规抗癌化合物。

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