Patent classifications
C07D239/49
CARBOXYLIC ACID COMPOUNDS
The present disclosure concerns at least one entity chosen from compounds of Formula (I) and pharmaceutically acceptable salts thereof:
##STR00001##
wherein the variable groups X, R.sup.1, R.sup.2, R.sup.3 m, n and p are as defined herein. The present disclosure also relates to methods for the preparation of at least one such entity, and intermediates useful in the preparation thereof, to pharmaceutical compositions containing at least one such entity, to the use of at least one such entity in the preparation of medicaments, and to the use of at least one such entity in the treatment of conditions such as, for example, allergic diseases, autoimmune diseases, viral diseases, and cancer.
CARBOXYLIC ACID COMPOUNDS
The present disclosure concerns at least one entity chosen from compounds of Formula (I) and pharmaceutically acceptable salts thereof:
##STR00001##
wherein the variable groups X, R.sup.1, R.sup.2, R.sup.3 m, n and p are as defined herein. The present disclosure also relates to methods for the preparation of at least one such entity, and intermediates useful in the preparation thereof, to pharmaceutical compositions containing at least one such entity, to the use of at least one such entity in the preparation of medicaments, and to the use of at least one such entity in the treatment of conditions such as, for example, allergic diseases, autoimmune diseases, viral diseases, and cancer.
Ligand-Directed Covalent Modification of Protein
The present invention relates to enzyme inhibitors. More specifically, the present invention relates to ligand-directed covalent modification of proteins; method of designing same; pharmaceutical formulation of same; and method of use.
Flagellar and needle complex (injectosome) loop as anti bacterial drug target
The present invention relates to a method for screening a compound that inhibits secretion of toxins into host-cell cytoplasm by virulent bacteria using a needle type III secretion system. The compound of the invention is selected by screening for a compound which interacts with a loop region of the cytoplasmic domain of the membrane protein FlhB from Salmonella typhimurium or a paralog thereof. Compositions including the compound of the invention, use of the compound, and methods of treating disorders caused by virulent bacteria are also provided.
Flagellar and needle complex (injectosome) loop as anti bacterial drug target
The present invention relates to a method for screening a compound that inhibits secretion of toxins into host-cell cytoplasm by virulent bacteria using a needle type III secretion system. The compound of the invention is selected by screening for a compound which interacts with a loop region of the cytoplasmic domain of the membrane protein FlhB from Salmonella typhimurium or a paralog thereof. Compositions including the compound of the invention, use of the compound, and methods of treating disorders caused by virulent bacteria are also provided.
Small-molecule-targeted protein degradation
Certain aspects of the invention relate to compounds, compositions and methods that are useful for treating or preventing a disease in a subject by enhancing the degradation of a protein. In other aspects, said compounds can be useful research tools for investigating protein degradation. In other aspects, said compounds are useful research tools for investigating protein function. In certain embodiments, the degraded protein is implicated in a disease or disorder whose pathology is related at least in part to the excessive expression of the protein or the expression of a mutant form of the protein.
Small-molecule-targeted protein degradation
Certain aspects of the invention relate to compounds, compositions and methods that are useful for treating or preventing a disease in a subject by enhancing the degradation of a protein. In other aspects, said compounds can be useful research tools for investigating protein degradation. In other aspects, said compounds are useful research tools for investigating protein function. In certain embodiments, the degraded protein is implicated in a disease or disorder whose pathology is related at least in part to the excessive expression of the protein or the expression of a mutant form of the protein.
ACID ADDITION SALT OF PYRIMETHAMINE
Acid addition salt of pyrimethamine (5-4-chlorophenyl)-6-ethyl-2,4-pyrimidinediamine) and methane sulfonic acid, process for its preparation and pharmaceutical compositions comprising the acid addition salt are disclosed.
ACID ADDITION SALT OF PYRIMETHAMINE
Acid addition salt of pyrimethamine (5-4-chlorophenyl)-6-ethyl-2,4-pyrimidinediamine) and methane sulfonic acid, process for its preparation and pharmaceutical compositions comprising the acid addition salt are disclosed.
Heteroaryl compounds and their use
The application is directed to compounds of formula (I): and their salts and solvates, wherein R.sup.1, R.sup.2, R.sup.3, A.sup.1, A.sup.2, A.sup.3, and n are as set forth in the specification, as well as to a method for their preparation, pharmaceutical compositions comprising the same, and use thereof for the treatment and/or prevention of a lysosomal storage disease, such as Gaucher's, and other diseases or disorders that are synucleinopathies. ##STR00001##