Patent classifications
C07D239/557
3-((R)-2-(AMINO-2-PHENYLETHYL)-1-(2-FLUORO-6 TRIFLUOROMETHYL BENZYL)-5-IODO-6-METHYL-1H-PYRIMIDINE-2,4-DIONE OR A SALT THEREOF, PROCESS FOR ITS PREPARATION, AND ITS USE IN THE SYNTHESIS OF ELAGOLIX
A new intermediate is useful in the synthesis of elagolix. A process for obtaining the intermediate includes reacting a precursor with iodine monochloride in the presence of an organic solvent. A process for preparing elagolix makes use of the intermediate. The intermediate can be 3-((R)-2-(amino-2-phenylethyl)-1-(2-fluoro-6-trifluoromethylbenzyl)-5-iodo-6-methyl-1H-pyrimidine-2,4-dione or a salt thereof, such as a hydrochloride.
3-((R)-2-(AMINO-2-PHENYLETHYL)-1-(2-FLUORO-6 TRIFLUOROMETHYL BENZYL)-5-IODO-6-METHYL-1H-PYRIMIDINE-2,4-DIONE OR A SALT THEREOF, PROCESS FOR ITS PREPARATION, AND ITS USE IN THE SYNTHESIS OF ELAGOLIX
A new intermediate is useful in the synthesis of elagolix. A process for obtaining the intermediate includes reacting a precursor with iodine monochloride in the presence of an organic solvent. A process for preparing elagolix makes use of the intermediate. The intermediate can be 3-((R)-2-(amino-2-phenylethyl)-1-(2-fluoro-6-trifluoromethylbenzyl)-5-iodo-6-methyl-1H-pyrimidine-2,4-dione or a salt thereof, such as a hydrochloride.
TRIARYL COMPOUNDS FOR TREATMENT OF PD-L1 DISEASES
Compounds are provided that are useful as immunomodulators. The compounds have the Formula (I)
##STR00001##
including stereoisomers and pharmaceutically acceptable salts thereof, wherein R.sup.1a, R.sup.1b, R.sup.1c, R.sup.1d, R.sup.2a, R.sup.2b, R.sup.3, R.sup.3a, R.sup.4, R.sup.6, R.sup.7, R.sup.8, A, Z, X.sup.1 and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
NOVEL ULK1 INHIBITORS AND METHODS USING SAME
In certain aspects, the invention provides a method for treating a disease or condition in a subject, the method comprising co-administering to a subject in need thereof a therapeutically effective amount of at least one ULK1-inhibiting pyrimidine, and a therapeutically effective amount of an mTOR inhibitor.
AN IMPROVED PROCESS FOR THE PREPARATION OF RALTEGRAVIR
The present invention provides a process for the preparation of crystalline anhydrous compound of Formula (X), Further, the present invention relates to the use of compound of Formula (X) preparation of Raltegravir (I) or its pharmaceutically acceptable salt thereof.
##STR00001##
Six-membered C-N-linked aryl sulfide derivatives and aryl sulfoxide derivatives as pest conrol agents
The present invention relates to novel heterocyclic compounds, to processes for preparation thereof and to the use thereof for controlling animal pests, which include arthropods and especially insects and acarids.
Six-membered C-N-linked aryl sulfide derivatives and aryl sulfoxide derivatives as pest conrol agents
The present invention relates to novel heterocyclic compounds, to processes for preparation thereof and to the use thereof for controlling animal pests, which include arthropods and especially insects and acarids.
6-HYDROXY-4-OXO-1,4-DIHYDROPYRIMIDINE-5-CARBOXAMIDES AS APJ AGONISTS
The present invention provides compounds of Formula (I):
##STR00001##
wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments.
Method for producing orotic acid derivative
Provided is a method for producing an orotic acid derivative, the method comprising a condensation step of performing, under a basic condition, a condensation reaction between an orotic acid halide represented by General Formula (I) and a compound represented by General Formula (II) to generate an orotic acid derivative represented by General Formula (III); and a neutralization crystallization step of precipitating crystals of orotic acid by neutralization crystallization to separate a liquid containing the orotic acid derivative from the crystals of orotic acid, after the condensation step. In General Formula (I), (II), or (III), X is a halogen atom, and A is a group represented by General Formula (A-1) or (A-2). In General Formula (A-1) or (A-2), R.sup.1 is a hydrogen atom or an organic group, and R.sup.2 and R.sup.3 are each independently an organic group. In a case where R.sup.1 is an organic group, R.sup.1 and R.sup.2 may be bonded to each other to form a ring. ##STR00001##
Method for producing orotic acid derivative
Provided is a method for producing an orotic acid derivative, the method comprising a condensation step of performing, under a basic condition, a condensation reaction between an orotic acid halide represented by General Formula (I) and a compound represented by General Formula (II) to generate an orotic acid derivative represented by General Formula (III); and a neutralization crystallization step of precipitating crystals of orotic acid by neutralization crystallization to separate a liquid containing the orotic acid derivative from the crystals of orotic acid, after the condensation step. In General Formula (I), (II), or (III), X is a halogen atom, and A is a group represented by General Formula (A-1) or (A-2). In General Formula (A-1) or (A-2), R.sup.1 is a hydrogen atom or an organic group, and R.sup.2 and R.sup.3 are each independently an organic group. In a case where R.sup.1 is an organic group, R.sup.1 and R.sup.2 may be bonded to each other to form a ring. ##STR00001##