C07D229/02

Photoreactive ligands and uses thereof

Disclosed herein are methods for identifying proteins as targets for interaction with a small molecule ligand. Also disclosed herein are small molecule ligands and compositions for use in profiling druggable proteins.

Photoreactive ligands and uses thereof

Disclosed herein are methods for identifying proteins as targets for interaction with a small molecule ligand. Also disclosed herein are small molecule ligands and compositions for use in profiling druggable proteins.

SULFUR AND AMIDE TROPOLONE INHIBITORS OF NUCLEOTIDYL TRANSFERASES AND USES THEREFOR

The present disclosure provides inhibitors of microorganisms including viruses and fungi of the formula (I) or (II) wherein the variables are defined herein. Also provided are methods of treatment using these agents in the treatment of infections of microorganisms such as viruses and fungi.

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SULFUR AND AMIDE TROPOLONE INHIBITORS OF NUCLEOTIDYL TRANSFERASES AND USES THEREFOR

The present disclosure provides inhibitors of microorganisms including viruses and fungi of the formula (I) or (II) wherein the variables are defined herein. Also provided are methods of treatment using these agents in the treatment of infections of microorganisms such as viruses and fungi.

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SMALL MOLECULES TARGETING MUTANT MAMMALIAN PROTEINS

Disclosed are compounds, compositions, and methods useful for treating or preventing a disease or disorder associated with a mutation in a protein.

SMALL MOLECULES TARGETING MUTANT MAMMALIAN PROTEINS

Disclosed are compounds, compositions, and methods useful for treating or preventing a disease or disorder associated with a mutation in a protein.

NOVEL SULFONAMIDEUREA COMPOUNDS

The present invention relates to compounds of formula (I): wherein Q is selected from O or S; R.sup.1 and R.sup.3 are each independently hydrogen or an optionally substituted hydrocarbyl group, or R.sup.1 and R.sup.3 together with the nitrogen atom to which they are attached may form a 3- to 12-membered optionally substituted cyclic group; and R.sup.2 is a cyclic group substituted at the position, wherein R.sup.2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

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COMPOSITIONS AND METHODS RELATED TO TETHERED KETHOXAL DERIVATIVES
20220143198 · 2022-05-12 · ·

Embodiments are directed to therapeutic, diagnostic, or functional complexes comprising a kethoxal derivative.

COMPOUNDS FOR TREATMENT OF HEPACI VIRUS INFECTION AND METHOD FOR DETERMINING THERAPY OF HEPACI VIRUS INFECTION, IN PARTICULAR, HCV INFECTION
20220024879 · 2022-01-27 ·

In a first aspect, the present invention relates to new compounds based on diphenylpiperazine and diphenylpiperidine structures. In particular, the present invention provides new flunarizine derivatives having improved hepaci virus infection inhibitory activity. In a further aspect, the present invention relates to a pharmaceutical composition containing said compound as well as the use of said pharmaceutical composition and the compounds according to the present invention in preventing or treating hepaci virus infection, in particular, HCV virus infection, like HCV of genotype 2. Moreover, a method for determining effectiveness of prophylactic or therapeutic treatment of hepaci virus, like HCV infection as well as a method for determining the therapy regimen of an individual afflicted with hepaci vims infection including HCV infection is provided. Said method is based on determining the sequence or interfacial hydrophobicity of the hepaci virus E1 protein. This may include determining the presence of mutations at predetermined positions of the E1 sequence. Based on determining the interfacial hydrophobicity of the E1 protein, the sensitivity to a diphenylpiperazine or diphenylpiperidine based hepaci virus inhibitor as well as a phenothiazine and cycloheptenepiperidine based hepaci virus inhibitor can be determined. When the central hydrophobicity region is disrupted or the hydrophobicity is below zero applying the Wimley-White hydropathy plot, or the mutations at positions 290, 299, 301 and 310 of SEQ ID No. 1 are present, it is submitted that the sensitivity against said compounds is reduced. Hence, it is possible to determine the therapy regimen of an individual afflicted with hepaci virus infection or being a risk of being afflicted with hepaci vims infection, in particular HCV infection like HCV genotype 2 infection.

FUNCTIONALITY INDEPENDENT LABELING OF ORGANIC COMPOUNDS
20220017471 · 2022-01-20 ·

Disclosed herein are methods of labeling organic compounds without depending on any functional group of the compound. In some embodiments, provided are bifunctional linkers useful in the methods.