C07D239/54

AN IMPROVED PROCESS FOR THE PREPARATION OF 4-({(1 R)-2-[5-(2-FLUORO-3METHOXYPHENYL)-3-{[2-FLUORO-6-(TRIFLUORO METHYL) PHENYL]METHYL}-4-METHYL-2,6-DIOXO-3,6DIHYDROPYRIMIDIN-1(2 H)-YL]-1-PHENYLETHYL}AMINO)BUTANOIC ACID OR ITS PHARMACEUTICALLY ACCEPTABLE SALTS

The present invention relates to an improved process for the preparation of 4-({(1R)-2-[5-(2-fluoro-3-methoxy phenyl)-3-{[2-fluoro-6-(trifluoro methyl) phenyl] methyl}-4-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl]-1-phenylethyl}amino) butanoic acid of formula (I) or its pharmaceutically acceptable salts. The compound of formula (I) is represented by the following structural formula:

##STR00001##

AN IMPROVED PROCESS FOR THE PREPARATION OF 4-({(1 R)-2-[5-(2-FLUORO-3METHOXYPHENYL)-3-{[2-FLUORO-6-(TRIFLUORO METHYL) PHENYL]METHYL}-4-METHYL-2,6-DIOXO-3,6DIHYDROPYRIMIDIN-1(2 H)-YL]-1-PHENYLETHYL}AMINO)BUTANOIC ACID OR ITS PHARMACEUTICALLY ACCEPTABLE SALTS

The present invention relates to an improved process for the preparation of 4-({(1R)-2-[5-(2-fluoro-3-methoxy phenyl)-3-{[2-fluoro-6-(trifluoro methyl) phenyl] methyl}-4-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl]-1-phenylethyl}amino) butanoic acid of formula (I) or its pharmaceutically acceptable salts. The compound of formula (I) is represented by the following structural formula:

##STR00001##

BROMODOMAIN INHIBITORS
20220315601 · 2022-10-06 · ·

The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.

BROMODOMAIN INHIBITORS
20220315601 · 2022-10-06 · ·

The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.

GONADOTROPIN RELEASING HORMONE RECEPTOR ANTAGONIST AND USE THEREOF

The present invention provides a compound or a pharmaceutically acceptable salt, isomer, prodrug, polymorph or solvate thereof, and a preparation method therefor and use thereof. The compound provided in the present invention has comparable or superior activity to Elagolix as a GnRHR antagonist in calcium flux assays and have better pharmacokinetic properties.

GONADOTROPIN RELEASING HORMONE RECEPTOR ANTAGONIST AND USE THEREOF

The present invention provides a compound or a pharmaceutically acceptable salt, isomer, prodrug, polymorph or solvate thereof, and a preparation method therefor and use thereof. The compound provided in the present invention has comparable or superior activity to Elagolix as a GnRHR antagonist in calcium flux assays and have better pharmacokinetic properties.

PYRIMIDINE COMPOUND

The present invention provides a novel pyrimidine compound represented by Formula [I] and a salt thereof:

##STR00001##

[in the formula, the symbols are as defined in the specification], which is useful for treating, preventing and/or diagnosing seizure and the like in disease involving epileptic seizure or convulsive seizure (including multiple drug resistant seizure, refractory seizure, acute symptomatic seizure, febrile seizure and status epilepticus), as well as a medical use therefor.

PYRIMIDINE CYCLOHEXENYL GLUCOCORTICOID RECEPTOR MODULATORS

The present invention provides a class of pyrimidinedione cyclohekenyl compounds and methods of using these compounds as glucocorticoid receptor modulators.

PYRIMIDINE CYCLOHEXENYL GLUCOCORTICOID RECEPTOR MODULATORS

The present invention provides a class of pyrimidinedione cyclohekenyl compounds and methods of using these compounds as glucocorticoid receptor modulators.

NANO-TO-NANO FE/PPM Pd CATALYSIS OF CROSS-COUPLING REACTIONS IN WATER
20170341069 · 2017-11-30 ·

In one embodiment, the present application discloses a catalyst composition comprising: a) a reaction solvent or a reaction medium; b) organometallic nanoparticles comprising: i) a nanoparticle (NP) catalyst, prepared by a reduction of an iron salt in an organic solvent, wherein the catalyst comprises at least one other metal selected from the group consisting of Pd, Pt, Au, Ni, Co, Cu, Mn, Rh, Ir, Ru and Os or mixtures thereof; c) a ligand; and d) a surfactant; wherein the metal or mixtures thereof is present in less than or equal to 50,000 ppm relative to the iron salt.