Patent classifications
C07D239/553
PROCESS FOR THE SYNTHESIS OF THE SODIUM SALT OF 4-[[(1R)-2-[5-(2-FLUORO-3-METHOXYPHENYL)-3-[[2-FLUORO-6-(TRIFLUOROMETHYL)-PHENYL]METHYL]-3,6-DIHYDRO-4-METHYL-2,6- DIOXO-1(2H)-PYRIMIDINYL]-1- PHENYLETHYL]AMINO]-BUTANOIC ACID (ELAGOLIX SODIUM SALT) AND INTERMEDIATES OF SAID PROCESS
The present invention to a process for the preparation of the sodium salt of 4-[[(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-1(2H)-pyrimidinyl]-1-phenylethyl]-amino]-butanoic acid, compound also known as Elagolix sodium salt, having the formula (I) reported below:
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ENHANCING THE ANTIVIRAL EFFICACY OF RNA VIRUS INHIBITION BY COMBINATION WITH MODULATORS OF PYRIMIDINE METABOLISM
Compounds and methods are provided for the treatment of pathogenic virus infections. Compositions and methods are provided for inhibiting RNA viruses.
IMPROVED PROCESS FOR THE PREPARATION OF ELAGOLIX AND ITS INTERMEDIATES
The present invention provides an improved process for the preparation of Elagolix sodium of formula (I) and its intermediates. The present invention also provides a compounds of formula (V) and (VI), (X), (Xa) and (Xb). The present invention further provides the use of compounds of formula (V), (VI), (X), (Xa) and (Xb) in the preparation of Elagolix sodium of formula (I). The present invention provides a process for the preparation of Elagolix sodium of formula (I) and its intermediates.
IMPROVED PROCESS FOR THE PREPARATION OF ELAGOLIX AND ITS INTERMEDIATES
The present invention provides an improved process for the preparation of Elagolix sodium of formula (I) and its intermediates. The present invention also provides a compounds of formula (V) and (VI), (X), (Xa) and (Xb). The present invention further provides the use of compounds of formula (V), (VI), (X), (Xa) and (Xb) in the preparation of Elagolix sodium of formula (I). The present invention provides a process for the preparation of Elagolix sodium of formula (I) and its intermediates.
DEUTERATED BENZYLAMINOPYRIMIDINEDIONE DERIVATIVES AND USE THEREOF
The present invention discloses deuterated benzylaminopyrimidinedione derivatives, the use thereof and the pharmaceutical composition containing the same. They may be used for suppressing the activities of myosin. The present invention also relates to the method of preparing this type of compounds and the pharmaceutical composition, and their use in treatment of hypertrophic cardiomyopathy and related heart diseases.
5-fluorouracil derivatives, preparation methods and uses thereof
Disclosed is a 5-fluorouracil derivative having the molecular structure shown in general formula VI, in which Ra and Rb groups are an alkoxy group or a fluorine-substituted alkoxy group having 1, 2, 3, or 4 carbon atoms, and are mono-, bis-, tri-, tetra- or penta-substituted on a phenyl group; a linking group L1 is an alkyl or alkenyl group having 1, 2, 3, or 4 carbon atoms, a linking group L2 is oxygen, or an alkyl or alkoxy group having 1, 2, 3, or 4 carbon atoms, or an amino acid, or an alkyl group having 1, 2, 3, or 4 carbon atoms containing an amino moiety, or a furyl group, and an X group is O or —NH—. Further disclosed is a method for preparing such a derivative and a use of the same in the treatment of cancer, tumor diseases, and diseases caused by abnormal neovascularization in a human or non-human mammal, and a medicament or a composition containing the 5-fluorouracil derivative.
5-fluorouracil derivatives, preparation methods and uses thereof
Disclosed is a 5-fluorouracil derivative having the molecular structure shown in general formula VI, in which Ra and Rb groups are an alkoxy group or a fluorine-substituted alkoxy group having 1, 2, 3, or 4 carbon atoms, and are mono-, bis-, tri-, tetra- or penta-substituted on a phenyl group; a linking group L1 is an alkyl or alkenyl group having 1, 2, 3, or 4 carbon atoms, a linking group L2 is oxygen, or an alkyl or alkoxy group having 1, 2, 3, or 4 carbon atoms, or an amino acid, or an alkyl group having 1, 2, 3, or 4 carbon atoms containing an amino moiety, or a furyl group, and an X group is O or —NH—. Further disclosed is a method for preparing such a derivative and a use of the same in the treatment of cancer, tumor diseases, and diseases caused by abnormal neovascularization in a human or non-human mammal, and a medicament or a composition containing the 5-fluorouracil derivative.
PRODRUGS FOR SUSTAINED RELEASING THERAPEUTIC AGENTS AND USES THEREOF
Provided are prodrugs for sustained releasing therapeutic agents, and methods for using such prodrugs for the treatment of diseases.
PRODRUGS FOR SUSTAINED RELEASING THERAPEUTIC AGENTS AND USES THEREOF
Provided are prodrugs for sustained releasing therapeutic agents, and methods for using such prodrugs for the treatment of diseases.
5-FLUOROURACIL DERIVATIVES, PREPARATION METHODS AND USES THEREOF
Disclosed is a 5-fluorouracil derivative having the molecular structure shown in general formula VI, in which Ra and Rb groups are an alkoxy group or a fluorine-substituted alkoxy group having 1, 2, 3, or 4 carbon atoms, and are mono-, bis-, tri-, tetra- or penta-substituted on a phenyl group; a linking group L1 is an alkyl or alkenyl group having 1, 2, 3, or 4 carbon atoms, a linking group L2 is oxygen, or an alkyl or alkoxy group having 1, 2, 3, or 4 carbon atoms, or an amino acid, or an alkyl group having 1, 2, 3, or 4 carbon atoms containing an amino moiety, or a furyl group, and an X group is O or —NH—. Further disclosed is a method for preparing such a derivative and a use of the same in the treatment of cancer, tumor diseases, and diseases caused by abnormal neovascularization in a human or non-human mammal, and a medicament or a composition containing the 5-fluorouracil derivative.