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21. 发明专利

BR0317113A 未知
公开(公告)号：BR0317113A
公开(公告)日：2005-10-25
申请号：BR0317113
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： A61K31/505 , 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.

22. 发明专利

ES2221164T3 SINTESIS Y ACTIVIDAD DE LA INMUNODEFICIENCIA HUMANA Y ANTIVIRUS DE LA HEPATITIS B DE NUCLEOSIDOS DE 1,3-OXASELENOLANO. 未知
公开(公告)号：ES2221164T3
公开(公告)日：2004-12-16
申请号：ES98914266
申请日：1998-03-19
申请人： UNIV EMORY , UNIV GEORGIA RES FOUND
发明人： SCHINAZI RAYMOND F , CHU CHUNG K , DU JINFA
IPC分类号： C07D421/04 , C07D473/00 , C07D473/18 , C07F9/6558 , C07F9/6561 , C07D473/30 , A61K31/505 , A61K31/52
摘要： Se describe un procedimiento y una composición para el tratamiento de infección por VIH, infección por VHB, o proliferación celular anormal en humanos y otros animales huésped, que incluye la administración de una cantidad eficaz de un nucleósido de 1,3- oxaselenolano o una sal farmacéuticamente aceptable de éste, opcionalmente en un vehículo farmacéuticamente aceptable.

23. 发明专利

AU2003244569A1 2'-Fluoronucleosides 未知
公开(公告)号：AU2003244569A1
公开(公告)日：2003-10-02
申请号：AU2003244569
申请日：2003-09-05
申请人： UNIV EMORY , UNIV GEORGIA RES FOUND
发明人： CHOI YONGSCOK , SHI JUNXING , MCATEE JEFFREY J , CHU CHUNG K , LIOTTA DENNIS C , SCHINAZI RAYMOND F , HONG JOON H , LEE KYEONG
IPC分类号： C07D239/47 , A61K31/505 , A61K31/506 , A61K31/52 , A61K31/522 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61P31/20 , A61P35/00 , C07D405/04 , C07D473/00 , C07D473/18 , C07D473/34 , C07F7/18 , C07F9/547 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H19/207 , A61K31/70
摘要： 2'-Fluoronucleoside compounds are disclosed which are useful in the treatment of hepatitis B infection, hepatitis C infection, HIV and abnormal cellular proliferation, including tumors and cancer. The compounds have general formulae (I), (II), (III), (IV) wherein Base is a purine or pyrimidine base; R 1 is OH, H, OR 3 , N 3 , CN, halogen, including F, or CF 3 , lower alkyl, amino, loweralkylamino, di(lower)alkylamino, or alkoxy, and base refers to a purine or pyrimidine base; R 2 is H, phosphate, including monophosphate, diphosphate, triphosphate, or a stabilized phosphate prodrug; acyl, or other pharmaceutically acceptable leaving group which when administered in vivo, is capable of providing a compound wherein R 2 is H or phosphate; sulfonate ester including alkyl or arylalkyl sulfonyl including methanesulfonyl, benzyl, wherein the phenyl group is optionally substituted with one or more substituents as described in the definition of aryl given above, a lipid, an amino acid, peptide, or cholesterol; and R 3 is acyl, alkyl, phosphate, or other pharmaceutically acceptable leaving group which when administered in vivo, is capable of being cleaved to the parent compound, or a pharmaceutically acceptable salt thereof.

24. 发明专利

GR3036393T3 ENANTIOMERICALLY PURE -g(b)-D-DIOXOLANE-NUCLEOSIDES. 未知
公开(公告)号：GR3036393T3
公开(公告)日：2001-11-30
申请号：GR20010401249
申请日：2001-08-14
申请人： UNIV GEORGIA RES FOUND , 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

25. 发明专利

AU739240B2 Synthesis, anti-human immunodeficiency virus and anti-hepatitis B virus activities of 1,3-oxaselenolane nucleosides 未知
公开(公告)号：AU739240B2
公开(公告)日：2001-10-04
申请号：AU6866598
申请日：1998-03-19
申请人： UNIV EMORY , UNIV GEORGIA RES FOUND
发明人： SCHINAZI RAYMOND F , CHU CHUNG K , DU JINFA
IPC分类号： C07D421/04 , C07D473/00 , C07D473/18 , C07F9/6558 , C07F9/6561 , C07D473/30 , A61K31/505 , A61K31/52
摘要： A method and composition for the treatment of HIV infection, HBV infection, or abnormal cellular proliferation in humans and other host animals is disclosed that includes the administration of an effective amount of a 1,3-oxaselenolane nucleoside or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.

26. 发明专利

AT201599T 未知
公开(公告)号：AT201599T
公开(公告)日：2001-06-15
申请号：AT93920366
申请日：1993-08-25
申请人： UNIV GEORGIA RES FOUND , 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

27. 发明专利

BR9610120A 未知
公开(公告)号：BR9610120A
公开(公告)日：1999-12-21
申请号：BR9610120
申请日：1996-09-06
申请人： UNIV GEORGIA RES FOUND , UNIV EMORY
发明人： CHU CHUNG K , MANOUILOV KONSTANTIN , DU JINFA
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
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.

28. 发明专利

AU709345B2 Therapeutic azide compounds 未知
公开(公告)号：AU709345B2
公开(公告)日：1999-08-26
申请号：AU7107696
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
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.

29. 发明专利

DE3851187D1 未知
公开(公告)号：DE3851187D1
公开(公告)日：1994-09-29
申请号：DE3851187
申请日：1988-01-13
申请人： UNIV GEORGIA RES FOUND , UNIV EMORY
发明人： CHU CHUNG K , SCHINAZI RAYMOND F
IPC分类号： C07H1/00 , A61K20060101 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7072 , A61P31/12 , C07H19/06 , C07H19/073 , C07H19/10
摘要： Compositions for the treatment of AIDS and ARC having the following compound as an active ingredient: where R1 is OH, monophosphate, diphosphate, or triphosphate; or a pharmacologically acceptable salt thereof. The primary advantage of this compound is its highly selective anti-retroviral activity, i.e., it significantly decreases viral replication as measured as reverse transcriptase activity while demonstrating orders of magnitude less cytotoxicity than other anti-viral compounds such as AZT. In a preferred embodiment, the compound is present in an amount sufficient to inhibit the HIV reverse transcriptase activity but not significantly inhibit human DNA polymerase activity. Also included within the scope of this invention are 3'-azido-2',3'-dideoxyuridine mono-, di-, and triphosphate and compositions containing these compounds as the active agent.

30. 发明专利

ES2291268T3 PROCESO PARA LA PREPARACION DE NUCLEOSIDOS BETA-D-(-)-DIOXOLANO ENANTIOMERICAMENTE PUROS. 未知
公开(公告)号：ES2291268T3
公开(公告)日：2008-03-01
申请号：ES01203571
申请日：1991-12-05
申请人： UNIV GEORGIA RES FOUND , UNIV EMORY
发明人： CHU CHUNG K , SCHINAZI RAYMOND F
IPC分类号： C07D405/04 , 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 , C07D411/04 , C07D473/00 , C07D473/30 , C07D473/34 , C07D473/40 , C07D497/08
摘要： Un proceso para la preparación de un nucleósido enantioméricamente puro Beta-D-[(2Beta,4Beta)-2-(hidroximetil)-4-dioxolanil] a partir de 1,6-anhidromanosa que comprende los siguientes pasos: (i) convertir 1-6-anhidromanosa a su derivado (2,3)-isopropilideno; (ii) preparar (2R,4R) y (2R,4S)-4-acetoxi-2-(oximetil protegido)-dioxolano del derivado (2,3)-isopropilideno; y (iii) condensar el (2R,4R) y (2R,4R)-4-acetoxi-2-(oximetil protegido)-dioxolano del paso (i) con una base heterocíclica en la presencia de SnCl 4, otro ácido Lewis, o triflato trimetilsilil para formar un nucleósido enantioméricamente puro Beta-D-[(2Beta,4Beta)-2-(hydroxymethil)-4-dioxolanil].

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