Abstract: Disclosed are processes for preparing compounds of the formula (I) and pharmaceutically acceptable salts or esters thereof: ##STR1## wherein R.sub.2 is a purine or pyrimidine base or an analogue or derivative thereof; and Z is S, S.dbd.O or SO.sub.2. The invention also relates to intermediates of use in the preparation of these compounds.

Abstract: The present invention relates to highly diastereoselective processes for production of cis-nucleosides and nucleoside analogues and derivatives in high optical purity and intermediates useful in those processes.

Abstract: The invention relates to 1,3-oxathiolane nucleoside analogues and their use in the treatment of viral infections. More specifically, this invention relates to (-)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidi n-2-one and pharmaceutically acceptable derivatives and pharmaceutical formulations thereof.

Abstract: This invention relates to a naphthoquinone derivatives, to processes and to intermediates for preparing these derivatives, to pharmaceutical composition and to the use of these derivatives as antitumor agents in mammals.

Abstract: Novel pyrano heterocyclic anthracycline derivatives are described, which are useful in the treatment of cancer and tumors, such as breast cancer, leukemia, lung cancer, colon cancer, ovarian cancer, renal cancer, and melanoma. As well, these compounds may be used ex vivo for the treatment of cancerous bone marrow before retransplanting said marrow in a patient. Pharmaceutical compositions and methods of preparing the compounds are also described.

Abstract: This invention relates to novel substituted 1,3-oxathiolanes and substituted 1,3-dithiolanes or pharmaceutically acceptable salts and esters thereof, of the formula: ##STR1## wherein X is S, S.dbd.O, or SO.sub.2 ;Y is O, S, S.dbd.O, or SO.sub.2 ;R.sub.1 is hydrogen, trisubstituted silyl, C.sub.1-6 alkyl, aralkyl, or C.sub.1-6 acyl, and R.sub.2 is a pyrimidine base or an analogue or derivative thereof.This invention also relates to processes for preparing these compounds, intermediates useful in their preparation, to pharmaceutical compositions containing them and to the use of these compounds as antiviral agents.

Abstract: The invention relates to 1,3-oxathiolane nucleoside analogues and their use in the treatment of viral infections. More specifically, this invention relates to (-)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidi n-2-one and pharmaceutically acceptable derivatives and pharmaceutical formulations thereof.

Abstract: Use of a compound of formula (I) or a pharmaceutically acceptable derivative thereof in the manufacture of a medicament for the treatment of hepatitis B is disclosed.

Abstract: Disclosed are processes for preparing compounds of the formula (I) and pharmaceutically acceptable salts or esters thereof: ##STR1## wherein R.sub.2 is a purine or pyrimidine base or an analogue or derivative thereof; and Z is S, S.dbd.O or SO.sub.2. The invention also relates to intermediates of use in the preparation of these compounds.

Abstract: The present invention provides methods for producing linear thiopeptides using an amino acid ortho amino thioanilide compound of formula (III) ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen or C.sub.1 -C.sub.4 branched or unbranched alkyl;R.sub.2 is selected from the group consisting of hydrogen, halo, amino, hydroxy, C.sub.1 -C.sub.4 branched or unbranched alkoxy, guanido, amido, acyl, carboxy, cyano, mercapto, nitro, azido, and C.sub.1 -C.sub.4 branched or unbranched alkyl optionally substituted by halo, amino, hydroxy, C.sub.1 -C.sub.4 branched or unbranched alkoxy, guanido, amido, acyl, carboxy, cyano, mercapto, nitro, azido;R.sub.3 is a decarboxylated amino acid residue or a decarboxylated amino acid chain comprising at least two amino acid residue.

Abstract: This invention relates to 1-amino thioacylbenzimidazoyl-2-one derivatives having the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are defined herein. These compounds are useful as thioacylating reagents. This invention also relates to a process for producing cyclic and linear thiopeptides using the thioacylating reagents of this invention. This invention further relates to intermediate anilide compounds, which are produced by reacting an ortho phenylene diamine with an amino acid chain or peptide. This invention also relates to intermediate thioanilide compounds, which are produced by thionating the intermediate anilide compounds. This invention further relates to a process for producing the thioacylating reagents of this invention by cyclizing the intermediate thioanilide compounds.

Abstract: Peptides are provided which are suitable for the treatment of pain and gastro-intestinal disorders, such as diarrhea, and are represented by the structure: ##STR1## where values for the substituents and n are disclosed herein. Methods for preparing these peptides by solution and solid phase syntheses are also provided. Pharmaceutical compositions utilizing these peptides in a pharmaceutically effective amount and methods of treatment using them are provided.

Abstract: There is provided novel 2-substituted-4-substituted-1,3-dioxolanes which are particularly useful as antiviral agents.

Abstract: There is provided cyclic peptides of the general formulae: ##STR1## wherein x represents an amino acid sequence from position 585 to 604 (gp41-HIV-1) such amino acid sequences being characterized by at least one of a lysine at position 586 or a lysine at both positions 585 and 586; x.sup.2 represents an amino acid sequence from position 585 to 604 (gp41-HIV-1); y represents an amino acid sequence from position 612 to 629 (gp41-HIV-1); e and f represent one or more epitopes; and a and b represent the amino and carboxy terminals, respectively, as well as substituents which are effective to make the peptide more useful as an immunodiagnositc reagent. Peptides of formula III have one or both of e and f present.There is also provided peptides of the general formulae: ##STR2## wherein x.sup.1 represents an amino acid sequence from position 577 to 596 (gp36-HIV-2) such amino acid sequences being characterized by at least one of a lysine at position 578 or a lysine at both positions 577 and 578; x.sup.

Abstract: Methods and compositions for preventing or treating human immunodeficiency virus (HIV) infections characterized by 2-substituted-5-substituted-1,3-oxathiolanes.

Abstract: Thioacylating reagents are provided for the introduction of thioamide bonds into growing peptides represented by the structure: ##STR1## where the substituents are disclosed herein. Intermediate precursors for preparing these thioacylating reagents are also provided. A process for preparing the thioacylating reagents and the intermediate precursors is further provided.