C07D249/16

Bicyclic sulfones and sulfoxides and methods of use thereof

The invention provides novel compounds having the general formula I: ##STR00001##
wherein R.sup.1, R.sup.B1, R.sup.B2, n, p, q, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds, and methods of using the compounds.

Bicyclic sulfones and sulfoxides and methods of use thereof

The invention provides novel compounds having the general formula I: ##STR00001##
wherein R.sup.1, R.sup.B1, R.sup.B2, n, p, q, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds, and methods of using the compounds.

Hydantoin containing deoxyuridine triphosphatase inhibitors

Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.

Thioether triazolopyridine and triazolopyrimidine inhibitors of myeloperoxidase

The present invention provides compounds of Formula (I): ##STR00001##
wherein A, X and Y are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, which may be used as medicaments.

Thioether triazolopyridine and triazolopyrimidine inhibitors of myeloperoxidase

The present invention provides compounds of Formula (I): ##STR00001##
wherein A, X and Y are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, which may be used as medicaments.

COMPOSITIONS AND METHODS FOR MODIFICATION OF BIOMOLECULES

The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

COMPOSITIONS AND METHODS FOR MODIFICATION OF BIOMOLECULES

The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

Monomers and oligonucleotides comprising cycloaddition adduct(s)

The invention features compounds of formula V or XII: ##STR00001## In one embodiment, the invention relates compounds and processes for conjugating ligand to oligonucleotide. The invention further relates to methods for treating various disorders and diseases such as viral infections, bacterial infections, parasitic infections, cancers, allergies, autoimmune diseases, immunodeficiencies and immunosuppression.

Monomers and oligonucleotides comprising cycloaddition adduct(s)

The invention features compounds of formula V or XII: ##STR00001## In one embodiment, the invention relates compounds and processes for conjugating ligand to oligonucleotide. The invention further relates to methods for treating various disorders and diseases such as viral infections, bacterial infections, parasitic infections, cancers, allergies, autoimmune diseases, immunodeficiencies and immunosuppression.

Methods for Synthesis of an Advantageous N-Heterocyclic Carbene Catalyst
20240059701 · 2024-02-22 ·

The present invention concerns the synthesis of the salts of a Triazolium N-Heterocyclic Carbene (NHC) catalyst in various salt forms prepared from 2-methylaniline, 2-methylphenylhydrazine hydrochloride or 2-methylphenylhydrazine. The molecules so prepared are useful in catalysis of carbene reactions and are advantageous due to their lack of chlorinated or fluorinated intermediates and lack of chlorine or fluorine in the final structure.