6 results about "Methylthioadenosine phosphorylase" patented technology

The present invention relates to a compound, the compound is a compound represented by a formula (I), or an isomer, an isotope derivative, a polymorphic substance, a prodrug, a pharmaceutically acceptable salt or a solvate thereof, and the definitions of A1, B1 and L are the same as the definitions in the specification. Also provided are pharmaceutical compositions and compounds of formula (I) for use in methods of treating related diseases by inhibition of MAT2A, including some cancers in which a gene encoding a methylthioadenosine phosphorylase (MTAP) is deleted and / or not fully functioning.

This invention discloses the preparation and application of a substituted heteroaryl ketone compound. The structure of the substituted heteroaryl ketone compound is shown in Formula I, wherein the definitions of each substituent are as described in the specification and claims. The compound of this invention has MAT2A enzyme inhibitory activity and, as a MAT2A inhibitor, can be used to prepare drugs for treating or preventing diseases of MAT2A overexpression and diseases of gene deletion encoding methionine phosphorylase.

The present invention provides a 5'-methylthioadenosine phosphorylase mutant, the amino acid sequence of which is derived from a mutation of the sequence shown in SEQ ID No. 3 of the sequence table, wherein the mutation is selected from at least one of the following: H64A, P131D, W114N, L206S, E168Q, F217V, F217S, F217W, R219A, R219Q, R219F, V184A and V184T. The present invention also provides its application in the catalytic synthesis of 2'-fluoro-2'-deoxyadenosine. The mutant H64A / W114N / L206S of the present invention has an enzyme activity of 1.31 U / g, while the ApMTAP unmutated enzyme strain has an enzyme activity of 0.11 U / g, which is about 12 times higher than the enzyme activity, that is, the yield of 2'-fluoro-2'-deoxyadenosine has been greatly improved, and is suitable for the field of enzyme catalysis.

Amide prodrugs of alkylthio-DADMe-Immucillin A compounds as inhibitors of MTAP (5- methylthioadenosine phosphorylase) and their use as therapeutic agents against various cancers. The invention relates to compounds, pharmaceutical compositions, methods for inhibiting MTAP, and methods for treating cancer. The inhibitors are compounds of the general formula: (I).

Disclosed herein are certain 2-oxoquinazoline derivatives of Formula (IA):that are methionine adenosyltransferase 2A (MAT2A) inhibitors. Also disclosed are pharmaceutical compositions comprising such compounds and methods of treating diseases treatable by inhibition of MAT2A such as cancer, including cancers characterized by reduced or absence of methylthioadenosine phosphorylase (MTAP) activity.

The present disclosure provides compounds according to Formula I and their pharmaceutically acceptable salts, tautomers, and / or isotopologues as described in the disclosure. The compounds are inhibitors of methionine adenosyltransferase isoform 2A (MAT2A). Also provided are pharmaceutical compositions and methods of using the compounds for the treatment of cancers, including certain cancers in which the gene encoding the enzyme methylthioadenosine phosphorylase (MTAP) has been deleted.