Abstract: Optically active compounds of the formula ##STR1## wherein n is 1 or 2 and m is 0, 1, 2 or 3 have antiviral activity. Compounds of the formula wherein at least one of the internecleotide phosphorothioate linkages is of the Sp configuration possess increased antiviral activity and/or metabolic stability.

Abstract: A method for the synthesis of a plurality of oligonucleotides comprising the steps of(i) forming a first oligonucleotide on a first cleavable link attached to a solid support;(ii) attaching to the first oligonucleotide a cleavable linker moiety;(iii) forming a second oligonucleotide on the cleavable linker moiety; and(iv) cleaving the first cleavable link and the cleavable linker moiety to give a plurality of oligonucleotides; wherein the cleavable linker moiety is of the Formula (1): ##STR1## in which A.sup.1, A.sup.2 and E are as defined herein, and novel compounds which may be used in the operation of the method.

Abstract: There are provided compounds of formula (I) ##STR1## wherein each group B is, independently, a naturally occurring or modified heterocyclic base linked through a nitrogen or a carbon atom of the ring to the sugar moiety;each group X is a, independently, hydrogen, fluorine, hydroxy, or a C.sub.1 -C.sub.6 alkoxy group;each group Y is, independently, hydrogen, sulphidryl or hydroxy; and the pharmaceutically acceptable salts thereof.A process for their preparation and pharmaceutical compositions comprising them are also described. The compounds of this invention can be useful as antivirals, particularly as anti-HIV (Human Immunodeficiency Virus) agents, namely as drugs to be used against AIDS (Acquired Immunodeficiency Syndrome) therapeutically and/or prophylatically.

Abstract: A method is provided for the high fidelity, rapid and economical in vitro synthesis of oligonucleotides. Nucleoside H-phosphonates are condensed in seriatim using a dehydrating agent to produce a poly (nucleoside H-phosphonate). The product is oxidized to yield the desired oligonucleotide. A novel reagent is provided for multiple nucleoside additions in single cycles.

Abstract: The invention describes complexes between VB.sub.12 analogues and either GCSF or EPO that retain both significant affinity for intrinsic factor (IF) in the VB.sub.12 portion of the complex and significant bioactivity of the GCSF or EPO portion of the complex. The invention also concerns a process for the synthesis of these complexes. This is achieved at least in part, by using a spacer compound, which is linked covalantly between the VB.sub.12 portion and the GCSF or EPO. The complexes preferably have the formulaV--X--A--Y--ZwhereinV is vitamin B.sub.12 or a vitamin B.sub.12 analogue, or derivative, bonded to X either through a carboxylate group pendant to the corrin nucleus of VB.sub.12 or through the central cobalt atom or to a functional group introduced onto the VB.sub.12 molecule, X is selected from: --NHNH--, --NH--, --O--, --S--, --SS--or --CH.sub.2 --, and A is an optionally substituted, saturated or unsaturated, branched or linear, C.sub.

Abstract: Substantially pure single-stranded oligonucleotides having a preselected sequence of not more than about 200 nucleotides, at least one of which is at a preselected position in the sequence and includes a base with a covalently attached linker arm containing or capable of binding at least one reporter group or solid support. A process for the chemical synthesis of the substantially pure single-stranded oligonucleotide and modified nucleosides useful in such synthesis are provided.

Abstract: Novel adenine derivatives whose structures are represented by Formula I, are disclosed, as are methods of using those compounds and others of Formula II to treat monocyte-mediated disorders such as rheumatoid arthritis and multiple sclerosis.

Abstract: A versatile polymeric support system for the synthesis of oligonucleotides is provided featuring a universal primer which allows chain elongation, in either the 3' or 5' direction, with any currently available DNA or RNA synthesis method, by a process which utilizes oxidatively cleaved primers to facilitate chain elongation and release. The support system is capable of withstanding mildly basic and acidic reaction conditions, while still permitting a convenient and quantitative release, either before or after removal of protecting groups from reactive groups, of synthesized oligonucleotides from a single polymeric support. Removal of the protecting groups before cleavage of the oligomer from the support permits the use of the immobilized oligomer as an affinity hybridization support for both isolating and detecting complementary polynucleic acids.

Abstract: Adenosines derivatives of the formula ##STR1## wherein R.sub.1 is allyl, methallyl, straight or branched chain (C.sub.3-7)alkynyl, (C.sub.3-8)cycloalkyl, or phenyl mono- or independently of one another di-substituted by halogen having an atomic number of from 9 to 35, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, or CF.sub.3 ; R.sub.2 is hydrogen or C(.sub.1-4)alkyl, and R.sub.3 is (C.sub.1-4)alkyl, are useful for protecting vascular endothelium, for lowering blood lipid levels, and for treating raised blood pressure.

Abstract: This invention is concerned with the use of adenosine as an agent for the treatment of human beings. More particularly, this invention is concerned with the administration of adenosine to human patients by continuous intravenous infusion for, inter alia, control of blood pressure, use as a selective vasodilator, decreasing pulmonary vascular resistance, treating acute pulmonary hypertension in conjunction with idiopathic respiratory distress syndrome, in diagnosing pulmonary hypertension in conjunction with cardiac septum defects, in percutaneous transluminal angioplasty (PTCA), in coronary thrombolysis (CTL) and in radionucleide scintography.

Abstract: The present invention provides a compound having the structure: ##STR1## wherein R.sup.1 is hydrogen, benzyl or a substituted benzyl group;X is hydrogen, a flouro, an amino or a substituted amino group;Y is hydrogen, a methoxy, a methylthio, a benzylthio, a methylethyl, a chloro, an amino or a substituted amino group; andY' is an oxo or a thio group; andZ is hydrogen, a hydroxy, a methoxy, a halogen, an amino or a substituted amino group.The present invention also provides a method of synthesizing a compound having the above-identified structure as well as the intermediate compounds produced according to that method.

Abstract: This invention is directed to processes for producing high purity N-protected-2'-O-methyl-5'-dimethoxytrityl-3' ribonucleoside methoxy, N,N-diisopropyl phosphoramidites (group 1), and N-protected-2'-O-methyl-5'-dimethoxytrityl-3'-ribonucleoside ethoxy, N,N-diisopropyl phosphoramidites (group 2). This invention is further directed to the process for producing high purity 2'-O-methyl-5'-dimethoxytrityl-inosine (structure IX; group 3), and 2'-O-methyl-5'-dimethoxytrityl-inosine-3'-cyanoethyl, N,N-diisopropyl phosphoramidite (structure Xa; group 3). This invention is also directed to the process for producing high purity N-protected-3'-O-methyl-5'-dimethoxytrityl ribonucleosides (group 6), and N-protected-3'-O-methyl-5'-dimethoxytrityl-2'-ribonucleoside cyanoethyl, N,N-diisopropyl phosporamidites (group 7).

Abstract: A method and composition for inhibiting the spread of a retrovirus such as HIV in a human cell population in which a retrovirus such as HIV is present has been found. The spread of the retrovirus is inhibited by treatment of the cells with a synergistic combination mixture of a dideoxy-ribonucleoside excluding AZT and hydroxycarbamide.

Abstract: This invention provides novel 1-alkylsulfonyl-2,2-difluoro-3-carbamoyl ribose intermediates and intermediate nucleosides derived therefrom. The compounds are particularly useful in the preparation of 2'-deoxy-2',2'-difluoro-beta-cytidine and other beta anomer nucleosides which are antiviral and anticancer agents.

Abstract: This invention relates to certain aristeromycin/adenosine derivatives which are useful in inhibiting AdoMet-dependent transmethylation and in the treatment of patients afflicted with neoplastic or viral disease states.

Abstract: Methods and compounds are provided for solid phase synthesis of oligonucleotides and related polymers by condensing protected monomer-O- 1,3,2-dichalcogen-substituted-phospholane! synthons in the presence of a catalytic base. Compounds of the invention include 2-N-substituted-1,3,2-dichalcogen-substituted-phospholane precursors of the above synthons, the protected monomer-O- 1,3,2-dichalcogen-substituted-phospholane! synthons, and P-chiral oligonucleotides and related P-chiral polymers.

Abstract: An improved method for treating Class I histiocytosis, Langerhans cell histiocytosis, is disclosed. In accordance with that method, a therapeutically effective amount of a 2-halo-2'-deoxyadenosine is administered to a host mammal such as a human patient having histiocytosis in an amount of about 0.5 to 0.9 mg/kg of body weight over a course of about 5 to 9 days for up to two courses.

Abstract: Novel lyxose derivatives which selectively inhibit adenosine kinase and methods of preparing these compounds are provided. These compounds are useful in treating certain conditions in vivo which may be ameliorated by increased local concentrations of adenosine.

Abstract: Novel adenine derivatives whose structures are represented by Formula I, are disclosed, as are methods of using those compounds and others of Formula II to treat monocyte-mediated disorders such as rheumatoid arthritis and multiple sclerosis.

Abstract: A compound which exhibits antiviral activity having the formula: ##STR1## wherein; R.sub.1 is selected from the group consisting of alkyls and alkenyls containing from 8 to 22 carbon atoms;A is selected from the group consisting of O and S atoms;R.sub.2 is selected from the group consisting of alkyls and alkenyls containing from 8 to 22 carbon atoms; and theNucleoside is selected from the group consisting of 2',3'-dideoxynucleosides, 3'-azido-2',3'-dideoxynucleosides, and 2',3'-didehydro-2',3'-dideoxynucleosides.