Abstract: The present invention provides novel phosphonic acid-based cationic lipids of the general structure: ##STR1## or a salt, or solvate, or enantiomers thereof wherein; (a) R.sub.1 is a lipophilic moiety; (b) R.sub.2 is a positively charged moiety; (c) R.sub.3 is a lipophilic moiety of 1 to about 24 carbon atoms, a positively charged moiety, or a negatively charged moiety; (d) n is an integer from 0 to 8; (e) X.sup.- is an anion or polyanion; (f) Y is N or O, and (g) m is an integer from 0 to a number equivalent to the positive charge(s) present on the lipid.The present invention further provides compositions of these lipids with polyanionic macromolecules, methods for interfering with protein expression in a cell utilizing these compositions and a kit for preparing the same.

Abstract: Oligomers having phosphonate internucleosidyl linkages which are enriched for phosphonate linkages of a preselected chirality which hybridize to an RNA target sequence and methods for their preparation are provided.

Abstract: New organophosphorus mononucleoside derivatives, methods of their synthesis and methods for the synthesis of organophosphorus dinucleotide derivatives utilizing the organophosphorus mononucleosides are provided.

Abstract: Compositions and methods of treating androgen-associated hair loss, in particular decreasing the progression of male pattern baldness using a nucleoside Oligomer or Oligomers useful in the described methods are provided.

Abstract: The present invention provides amide-based oligomeric cationic lipids. The present invention further provides compositions of these amide-based cationic lipids with anionic macromolecules, methods for interfering with protein expression in a cell utilizing these compositions and a kit for preparing the same.

Abstract: Methods of preparing N.sup.4 -alkanoyl, aroyl and aralkanoyl 2'-O-methylcytidine derivatives are provided. Also provided are cytidine derivatives and nucleoside monomers comprising these cytidine derivatives which are useful in the synthesis of Oligomers, including oligonucleotides and methylphosphonate Oligomers.

Abstract: Methods and compounds for selective cleavage of nucleic acid are described. The compounds generally contain three functionalities: (1) an oligonucleoside portion which is substantially complementary to at least a portion of the target nucleic acid, thereby providing selectivity to the compound; (2) a non-complementary portion which replaces one of the otherwise-complementary nucleoside bases in the oligonucleoside and which serves to place the target nucleic acid strand into a conformation that favors the cleavage of a phosphodiester linkage opposite the non-complementary portion; and (3) a cleavage moiety which possesses one or more and preferably two or more of the features of (a) proton donation, (b) proton acceptance, (c) hydrogen bonding, (d) charge neutralization and (e) Lewis acidity. These compounds may be used for the study and treatment of diseases involving foreign genetic materials or alterations to or inappropriate expression of genomic DNA.

Abstract: Oligomers having phosphonate internucleosidyl linkages which are enriched for phosphonate linkages of a preselected chirality which hybridize to an RNA target sequence and methods for their preparation are provided.

Abstract: Methods for purifying an oligomer by normal phase column chromatography on a support selected from polyhydroxyethyl aspartamide, hydrophilic silica and silica from an oligomer impurity having a different nucleoside sequence are described. These methods are based upon the different retention times of the oligomer and the impurity on the column.

Abstract: Oligomers having chirally pure phosphonate internucleosidyl linkages mixed with non-phosphonate internucleosidyl linkages which hybridize to RNA target sequences and methods for their preparation are provided.

Abstract: Processes for the stereospecific synthesis of 2',2"-bis(deoxy)di-nucleosides and for the stereoselective synthesis of 2',2"-bis(substituted) dinucleosides are provided. Also provided are activated 2'-substituted-nucleoside alkylphosphonate active esters useful in the synthesis of these dinucleosides.

Abstract: Methods of synthesizing oligomers using low water oxidizer reagents which result in high coupling efficiencies are provided. These methods are suitable for larger scale preparations of methylphosphonate oligomers.

Abstract: Polymeric reagents useful in the solid phase synthesis of oligomers are provided. These polymeric reagents are suitably loaded with nucleosidyl moieties and do not undergo non-specific chain elongation.

Abstract: A unit dose package has two chambers separated by a frangible seal. A liquid or solvent is provided in one of the chambers. An absorptive pad and powder are provided in the other chamber. The liquid and powder are stored separately, to avoid decomposition of the unstable mixture. In use, the first chamber is squeezed or rolled, bursting the seal, and driving the liquid into the second chamber, where it dissolves the powder and is absorbed by the pad. The package is peeled or torn open, and the pad is removed and applied to the skin.

Abstract: Methods of preparing N.sup.4 -alkanoyl, aroyl and aralkanoyl 2'-O-methylcytidine derivatives are provided. Also provided are novel cytidine derivatives and nucleoside monomers comprising these cytidine derivatives which are useful in the synthesis of Oligomers, including oligonucleotides and methylphosphonate Oligomers.