C07D213/74

METHODS AND COMPOUNDS FOR RESTORING MUTANT p53 FUNCTION
20230046427 · 2023-02-16 ·

Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods that restore DNA binding affinity of p53 mutants. The compounds of the present disclosure can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.

MODULATORS OF CIRCADIAN RHYTHMS AND USES THEREOF

Disclosed herein are, inter alia, compounds modulating MT.sub.1 and MT.sub.2 receptors' activity and methods of use thereof for treating MT.sub.1 and MT.sub.2 receptor-related conditions.

2-(HET)ARYL-SUBSTITUTED FUSED BICYCLIC HETEROCYCLE DERIVATIVES AS PESTICIDES

The invention relates to novel compounds of the formula (I)

##STR00001## in which the R.sup.1, R.sup.2a, R.sup.2b, R.sup.3, A.sup.1, A.sup.2, A.sup.3, A.sup.4 and n radicals are each as defined above, to their use as acaricides and/or insecticides for controlling animal pests and to processes and intermediates for their preparation.

2-(HET)ARYL-SUBSTITUTED FUSED BICYCLIC HETEROCYCLE DERIVATIVES AS PESTICIDES

The invention relates to novel compounds of the formula (I)

##STR00001## in which the R.sup.1, R.sup.2a, R.sup.2b, R.sup.3, A.sup.1, A.sup.2, A.sup.3, A.sup.4 and n radicals are each as defined above, to their use as acaricides and/or insecticides for controlling animal pests and to processes and intermediates for their preparation.

ANTHELMINTIC COMPOUNDS, COMPOSITIONS AND METHOD OF USING THEREOF
20180009754 · 2018-01-11 · ·

The present invention relates to novel anthelmintic compounds of formula (IA) below:

##STR00001## wherein, Y is selected from the group consisting of —H, aryl, cycloalkyl, cycloalkenyl, heteroaryl, heterocyclyl, alkyl, haloalkyl, and alkoxyalkyl; and Z is selected from the group consisting of aryl, cycloalkyl, cycloalkenyl, heteroaryl, heterocyclyl, alkyl, haloalkyl, and alkoxyalkyl. Variables Ring A, Ring B, Ring C, X.sub.1, X.sub.6, and X.sub.8 are as defined herein. The invention also relates to parasiticidal compositions comprising the compounds, and methods and uses of the compounds for treating and preventing parasitic infections and infestations in animals.

ANTHELMINTIC COMPOUNDS, COMPOSITIONS AND METHOD OF USING THEREOF
20180009754 · 2018-01-11 · ·

The present invention relates to novel anthelmintic compounds of formula (IA) below:

##STR00001## wherein, Y is selected from the group consisting of —H, aryl, cycloalkyl, cycloalkenyl, heteroaryl, heterocyclyl, alkyl, haloalkyl, and alkoxyalkyl; and Z is selected from the group consisting of aryl, cycloalkyl, cycloalkenyl, heteroaryl, heterocyclyl, alkyl, haloalkyl, and alkoxyalkyl. Variables Ring A, Ring B, Ring C, X.sub.1, X.sub.6, and X.sub.8 are as defined herein. The invention also relates to parasiticidal compositions comprising the compounds, and methods and uses of the compounds for treating and preventing parasitic infections and infestations in animals.

KINASE INHIBITOR COMPOUNDS AND COMPOSITIONS AND METHODS OF USE

Disclosed herein are kinase inhibitor compounds having the structure (I) or a stereoisomer, pharmaceutically acceptable salt, oxide, or solvate thereof, where R.sup.1, R.sup.2, X, L, Q, and Y are as defined herein. Also disclosed are compositions containing the kinase inhibitor compounds, methods of inhibiting activity of a kinase in a cell, methods of increasing cell proliferation in a population of pancreatic beta cells, methods of treating a subject for a condition associated with insufficient insulin secretion, and methods of treating a subject for a neurological disorder.

##STR00001##

KINASE INHIBITOR COMPOUNDS AND COMPOSITIONS AND METHODS OF USE

Disclosed herein are kinase inhibitor compounds having the structure (I) or a stereoisomer, pharmaceutically acceptable salt, oxide, or solvate thereof, where R.sup.1, R.sup.2, X, L, Q, and Y are as defined herein. Also disclosed are compositions containing the kinase inhibitor compounds, methods of inhibiting activity of a kinase in a cell, methods of increasing cell proliferation in a population of pancreatic beta cells, methods of treating a subject for a condition associated with insufficient insulin secretion, and methods of treating a subject for a neurological disorder.

##STR00001##

APTAMER NUCLEIC ACID MOLECULE, AND COMPLEX AND APPLICATION THEREOF
20230002769 · 2023-01-05 ·

The present application relates to an aptamer nucleic acid molecule, a complex containing the aptamer nucleic acid molecules, a method of detecting intracellular or extracellular RNA, DNA or other target molecules, and a kit containing the aptamer. The aptamer of the present application is capable of specifically binding a kind of fluorophore micromolecules, and can significantly enhance fluorescence intensity under excitation light of appropriate wavelength.

APTAMER NUCLEIC ACID MOLECULE, AND COMPLEX AND APPLICATION THEREOF
20230002769 · 2023-01-05 ·

The present application relates to an aptamer nucleic acid molecule, a complex containing the aptamer nucleic acid molecules, a method of detecting intracellular or extracellular RNA, DNA or other target molecules, and a kit containing the aptamer. The aptamer of the present application is capable of specifically binding a kind of fluorophore micromolecules, and can significantly enhance fluorescence intensity under excitation light of appropriate wavelength.