Described herein are compounds of Formula I and pharmaceutically acceptable salts, solvates, or stereoisomers thereof, as well as their uses as STAT5 and/or STAT6 inhibitors.

Amine substituted morpholino oligonucleotides, other than the classical N,N-dimethylamino PMO analogue, and methods of efficiently synthesizing these oligonucleotides with high yield are provided. Morpholino oligonucleotides having thiophosphoramidate, phosphoramidate, and alkyl phosphoramidate linkers. Chimeras containing unmodified DNA/RNA and other analogs of DNA/RNA can be prepared. These oligonucleotides form duplexes with complementary DNA or RNA that are more stable than natural DNA or DNA/RNA complexes, are active with RNAse H1, and may be transfected into cells using standard lipid reagents. These analogues are therefore useful for numerous applications.

Disclosed herein, inter alia, are prodrug compositions and methods of using the same for treatment and detection of disease. Specifically, disclosed herein is a compound of formula (I) having spiro-fused 1,2,4-trioxolane and piperidine rings, namely, 1,2,4-trioxa-8-azaspiro[4.5] decane. Also disclosed is a pharmaceutical composition containing the compound and a pharmaceutically acceptable carrier.

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The disclosure relates to compounds that act as covalent inhibitors of epidermal growth factor receptor (EGFR); pharmaceutical compositions comprising the compounds; and methods of treating or preventing kinase-mediated disorders, including cancer and other proliferation diseases.

The present invention pertains to a method for synthesizing a ribonucleic acid H-phosphonate monomer, and a method for performing oligonucleotide synthesis in which said monomer is used. The present invention pertains to a method for manufacturing an inexpensively manufacturable H-phosphonate nucleoside derivative in which selective protection is provided to position 2′ of a ribonucleoside monomer required in RNA oligonucleotide synthesis. The present invention is characterized in that: hydroxyl groups in position 2′ and position 3′, which have slightly different reactivity, are caused to react with an aromatic acyl halide at low temperature to selectively esterify position 2′; and subsequently the hydroxyl group at position 3′ in one pot is captured by a phosphityl group to prevent position 2′ and position 3′ transfer of the acyl group.

This disclosure relates to uridine diphosphate (UDP) derivatives, compositions comprising therapeutically effective amounts of those UDP derivatives and methods of using those derivatives or compositions in treating disorders that are responsive to ligands, such as agonists, of P.sub.2Y.sub.6 receptor, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease) and traumatic CNS injury, as well as pain.

The present invention relates to itraconazole prodrugs, pharmaceutical compositions comprising the prodrugs, and methods for treatment and/or prophylaxis of lung fibrosis, renal fibrosis, or liver fibrosis using the pharmaceutical compositions.

Phosphoramidate derivatives of 5-fluoro-2′-deoxyuridine are disclosed for use in the treatment of cancer, especially in the treatment of cancer where the patient shows resistance, for example, in a patient with cells with a lowered level of nucleoside transporter proteins and/or with nucleoside kinase-deficient cells and/or with Mycoplasma-infected cells and/or with cells with a raised level of thymidylate synthase.

Compounds useful as fluorescent or colored dyes are disclosed. The compounds have the following structure (I):

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or a stereoisomer, tautomer or salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, L.sup.l, L.sup.2, L.sup.3, L.sup.4, M.sup.1, M.sup.2, m and n are as defined herein. Methods associated with preparation and use of such compounds is also provided.

The present invention provides aryl phosphorous oxide compounds with kinase inhibitory activity. The compounds are capable of effectively inhibiting activity of various types of EGFR drug-resistant mutants (such as EGFR.sup.del19, EGFRdel.sup.19/T790M, EGFR.sup.del19/C797S, EGFR.sup.T790M/L858R, EGFR.sup.L858/C797S, EGFR.sup.del19/T790M/C797S, and EGFR.sup.L858R/T790M/C797S, and also have significant inhibitory effect on ALK fusion genes and mutants (such as L1196M), and are capable of being used for the treatment, combined treatment or prevention of various types of cancers.