Abstract: (−)-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one, its pharmaceutically acceptable derivatives, pharmaceutical formulation thereof, methods for its preparation and its uses as an antiviral agent are described

Abstract: A novel compound which inhibits certain integrins, particularly &agr;v integrins. Additionally, the novel compound may be used in a method of treating tumors or cancer which comprises administering a pharmaceutically effective amount of the compound to a patient. Additionally, the novel compound may be used in a method of inhibiting angiogensis. Finally, a method of producing the novel compound is disclosed.

Abstract: The present invention relates to a novel nucleotide analogue having the general formula (I) and pharmaceutically acceptable salts, esters, or salt of such esters: wherein n, X, Q U R1′, R1, Z and R2 are defined here within. The compounds object of the present invention may be a single enantiomers or as mixtures of said enantiomers, the compounds may have a &agr;D, &agr;-L, &bgr;-D, &bgr;-L, R or S configuration at each chiral center or mixtures thereof. This invention also relates to pharmaceutical compositions containing them, alone or in combination with other therapeutic agents, and their use as antiviral agents, particularly against HIV and/or HBV infections in mammals.

Abstract: The present invention provides a novel method for treating leukemia and more particularly acute myelogenous leukemia (AML) in a host comprising administering to the host a therapeutically effective amount of a compound having the formula I: 1

Abstract: The present invention is concerned with novel [1,8] naphthyridine derivatives useful for the inhibition of the hepatitis virus, more specifically the hepatitis C virus.

Abstract: The present invention relates to methods and compositions for preparing biologically important nucleoside analogues containing 1,3-dioxolane sugar rings. In particular, this invention relates to the stereoselective synthesis of the beta (cis) isomer by glycosylating the base with an intermediate of formula (II) below a temperature of about −10° C.

Abstract: This invention relates to single enantiomers of novel cis-substituted 1,3-oxathiolanes, of the formula (I): wherein; R1 is hydrogen, and R2 is cytosine or 5-fluorocytosine; and pharmaceutically acceptable salts and esters thereof. This invention also relates to pharmaceutical compositions containing them and to the use of these compounds as antiviral agents, particularly in combination therapy.

Abstract: The current invention is down to (+) an (−) enantiomers, as well as racemic mixtures of nucleoside analogs, wherein the carbohydrate portion of the analog is a dioxolane moiety and the nucleobase moiety is N6-carbocyclic-alkylamino-substituted-2-amino-purine moiety attached via its N9 position to the dioxolane moiety. The compounds are useful for treating viral infections such as HBV and HIV infections, alone or in combination with other therapeutic agents.

Abstract: Nucleoside analogues containing a 1,3-dioxolane structure are suitable antiviral agents, particulary for the treatment of the HIV infections in mammals, especially humans. Examples of the nucleoside analogues include: cis-2-acetoxymethyl-4-(thymin-1′-yl)-1,3,-dioxolane, cis-2-hydroxymethyl-4-(thymin-1′-yl)-1,3-dioxolane, cis-2-benzoyloxymethyl-4-(cytosin-1′-yl)-1,3-dioxolane, and cis-2-hydroxymethyl-4-(cytosin-1′-yl)-1,3-dioxolane. These compounds can be in the form of their racemates or their separate enantiomers.

Abstract: In accordance with the present invention there is provided a nucleoside analogue of formula (I) or (Ia) which is useful as an antiviral agent.

Abstract: Disclosed are processes for preparing compounds of the formula (I) and pharmaceutically acceptable salts or esters thereof: 1

Abstract: The present invention relates to heterocyclic Compounds having antiviral activity.

Abstract: A highly conserved, immunologically accessible antigen at the surface of Neisseria meningitidis organisms. Immunotherapeutic, prophylactic and diagnostic compositions and methods useful in the treatment, prevention an diagnosis of Neisseria meningitidis diseases. A proteinase K resistant Neisseria meningitidis surface protein having an apparent molecular weight of 22 kDa, the corresponding nucleotide and derived amino acid sequences (SEQ ID NO: 1, NO:3, NO:5 and NO:7: SEQ ID NO: 2, NO:4, NO:6, and NO:8), recombinant DNA methods for the production of the Neisseria meningitidis 22 kDA surface protein, and antibodies that bind to the Neisseria meningitidis 22 kDA surface protein.

Abstract: The present invention comprises compounds that are effective inhibitors of integrins, particularly &agr;v&bgr;3 and &agr;v&bgr;5 integrins. Particularly, the compounds are of formula I and pharmaceutically acceptable salts thereof wherein X,Y1 W, R1 to R5, A and B are defined according to the disclosure herein.

Abstract: The present invention relates to heterocyclic Compounds having antiviral activity. In particular, Compounds of formula (I): wherein B, W, X, Y, Q, R1, R2, R3, R4 and n are as defined herein, are useful in the therapy and prophylaxis of viral infection in mammals.

Abstract: This invention relates to single enantiomers of novel cis-substituted 1,3-oxathiolanes, of the formula (I): wherein; R1 is hydrogen, and R2 is cytosine or 5-fluorocytosine, and pharmaceutically acceptable salts and esters thereof. This invention also relates to pharmaceutical compositions containing them and to the use of these compounds as antiviral agents, particularly in combination therapy.

Abstract: Nucleotide analogues having the general formula (I) and pharmaceutically acceptable derivatives: wherein n is 0 or an integer; X is O or S, CH2, CH-halogen, CH—N3, or C═CH2; Q and U are independently selected from: O, S, and CH(Ra) wherein Ra is hydrogen, OH, halogen, N3 ,NH2, SH, carboxyl, C1-6 alkyl or Ra is CH2(Rb) wherein Rb is hydrogen, OH, SH, NH2, C1-6 alkyl or carboxyl; or both Q and U are CH when Q and U are linked by a double bond; Z is selected from: O, a C1-6 alkoxy, a C1-6 thioalkyl, a C1-6 aminoalkyl, (CH2)m wherein m is 0 or an integer, and N(Rc)2 wherein both Rc are independently hydrogen or a C1-6 alkyl; and R2 is a purine or pyrimidine base or an analogue or derivative thereof. Members of this series of analogues possess anti-viral activity.

Abstract: (−)-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one, its pharmaceutically acceptable derivatives, pharmaceutical formulation thereof, methods for its preparation and its uses as an antiviral agent are described.

Abstract: Disclosed are processes for preparing compounds of the formula (I) and pharmaceutically acceptable salts or esters thereof: wherein R2 is a purine or pyrimidine base or an analogue or derivative thereof; and Z is S, S═O or SO2. The invention also relates to intermediates of use in the preparation of these compounds.

Abstract: The present invention is directed to a method of treating hepatitis B viral infections in mammals comprising the administration of .beta.-L-5-fluoro-2',3'-dideoxycytidine and pharmaceutically acceptable derivatives thereof.