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 β-L- or β-D-2′,3′-dideoxynucleoside or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable diluent or excipient.
摘要:
A method for the treatment of a host, and in particular, a human, infected with hepatitis B virus (HBV) is provided that includes administering an effective amount of a β-L-thymine nucleotide, or a phosphate prodrug thereof, optionally in combination therapy with other drugs for the treatment of HBV.
摘要:
A method and composition for the treatment, prevention and/or prophylaxis of a host, and in particular, a human, infected with Epstein-Barr virus (EBV), is provided that includes administering an effective amount of a 5-substituted uracil nucleoside or its pharmaceutically acceptable salt or prodrug, optionally in a pharmaceutically acceptable diluent or excipient.
摘要:
The present invention discloses a method for treating HIV that includes administering β-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 β-D-D4FC as “salvage therapy” to patients which exhibit drug resistance to other anti-HIV agents. β-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:
A method and composition for the treatment of HIV and HBV infections in humans is disclosed that includes administering an effective amount of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, a pharmaceutically acceptable derivative thereof, including a 5′ or N4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier. A process for the resolution of a racemic mixture of nucleoside enantiomers is also disclosed that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers.
摘要翻译:公开了用于治疗人体中HIV和HBV感染的方法和组合物,其包括给予有效量的2-羟甲基-5-(5-氟胞嘧啶-1-基)-1,3-氧硫杂环戊烷,其药学上可接受的衍生物 ,包括在药学上可接受的载体中的5'或N 4 S 4烷基化或酰化衍生物或其药学上可接受的盐。 还公开了一种用于拆分核苷对映异构体外消旋混合物的方法,其包括将外消旋混合物暴露于优先催化其中一种对映异构体中的反应的酶的步骤。
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:
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.
摘要:
A method of treatment of: i) HIV-1 infections in mammals, including humans; or ii) HBV infections in mammals, including humans; which method comprises the administration to the human in need of such treatment, an effective amount of the (R)-enantiomer of the triphosphate of a compound of formula (A) or a pharmaceutically acceptable salt thereof; and compounds for use in the method.
摘要:
Method for the sterospecific preparation of 2′ or 3′ deoxy and 2′,3′-dideoxy-β-L-pentafuranonucleoside compounds. 2′ or 3′ deoxy and 2′,3′-dideoxy-β-L-pentofuranonucleoside compounds are also described. Finally, the invention concerns the use of these compounds, and particularly 2′,3′dideoxy-β-L-fluorocytidine, as drugs, and especially as anti-viral agents.
摘要:
A method and composition for the treatment of HIV and HBV infections in humans is disclosed that includes administering an effective amount of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, a pharmaceutically acceptable derivative thereof, including a 5′ or N4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier. A process for the resolution of a racemic mixture of nucleoside enantiomers is also disclosed that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers.
摘要翻译:公开了用于治疗人体中HIV和HBV感染的方法和组合物,其包括给予有效量的2-羟甲基-5-(5-氟胞嘧啶-1-基)-1,3-氧硫杂环戊烷,其药学上可接受的衍生物 ,包括在药学上可接受的载体中的5'或N 4 S 4烷基化或酰化衍生物或其药学上可接受的盐。 还公开了一种用于拆分核苷对映异构体外消旋混合物的方法,其包括将外消旋混合物暴露于优先催化其中一种对映异构体中的反应的酶的步骤。