Patent classifications
C07D263/24
IMPROVED PROCESS FOR THE PREPARATION OF [[2(S)-[[4(R)-(3-HYDROXYPHENYL)-3(R),4-DIMETHYL-1-PIPERIDINYL]METHYL]-1-OXO-3-PHENYLPROPYL]AMINO]ACETIC ACID DIHYDRATE
The present invention relates to an improved process for the preparation of [[2(S)-[[4(R)-(3-hydroxyphenyl)-3(R),4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-phenylpropyl]amino]acetic acid dihydrate, represented by the following structural formula (I).
IMPROVED PROCESS FOR THE PREPARATION OF [[2(S)-[[4(R)-(3-HYDROXYPHENYL)-3(R),4-DIMETHYL-1-PIPERIDINYL]METHYL]-1-OXO-3-PHENYLPROPYL]AMINO]ACETIC ACID DIHYDRATE
The present invention relates to an improved process for the preparation of [[2(S)-[[4(R)-(3-hydroxyphenyl)-3(R),4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-phenylpropyl]amino]acetic acid dihydrate, represented by the following structural formula (I).
AGONISTS OF ROR GAMMAt
The present invention is directed to compounds of the formula (I) wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
##STR00001##
AGONISTS OF ROR GAMMAt
The present invention is directed to compounds of the formula (I) wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
##STR00001##
METHOD FOR SYNTHESIZING N-SUBSTITUTED PHENYL-5-HYDROXYMETHYL-2-OXAZOLIDINONE
The disclosure discloses a method for synthesizing N-substituted phenyl-5-hydroxymethyl-2-oxazolidinone, wherein the method comprises: reacting from raw materials, 3-R2-4-R1-aniline and epichlorohydrin, and allowing the resulting product to react under alkaline conditions in a CO.sub.2 atmosphere to obtain N-substituted phenyl-5-hydroxymethyl-2-oxazolidinone, wherein R.sub.1 is a morpholine group, a morpholin-3-one group or a piperazine group, and derivative groups thereof, and R.sub.2 is halogen, hydrogen or lower alkyl. The method provided by the disclosure has such advantages as few steps, simple operation, cheap and easily available raw materials, mild reaction conditions, and high product yield, and is especially suitable for industrial production of antibiotic linezolid intermediates and antithrombotic drug rivaroxaban intermediates.
METHOD FOR SYNTHESIZING N-SUBSTITUTED PHENYL-5-HYDROXYMETHYL-2-OXAZOLIDINONE
The disclosure discloses a method for synthesizing N-substituted phenyl-5-hydroxymethyl-2-oxazolidinone, wherein the method comprises: reacting from raw materials, 3-R2-4-R1-aniline and epichlorohydrin, and allowing the resulting product to react under alkaline conditions in a CO.sub.2 atmosphere to obtain N-substituted phenyl-5-hydroxymethyl-2-oxazolidinone, wherein R.sub.1 is a morpholine group, a morpholin-3-one group or a piperazine group, and derivative groups thereof, and R.sub.2 is halogen, hydrogen or lower alkyl. The method provided by the disclosure has such advantages as few steps, simple operation, cheap and easily available raw materials, mild reaction conditions, and high product yield, and is especially suitable for industrial production of antibiotic linezolid intermediates and antithrombotic drug rivaroxaban intermediates.
ALKENYLDIARYLMETHANES AS NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS FOR ANTI-HIV-1 CHEMOTHERAPY
The invention disclosed herein pertains to compounds of alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for the treatment of patients with acquired-immune deficiency syndrome (AIDS). Also described are methods for treating AIDS patients using the described alkenyldiarylmethane compounds.
ALKENYLDIARYLMETHANES AS NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS FOR ANTI-HIV-1 CHEMOTHERAPY
The invention disclosed herein pertains to compounds of alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for the treatment of patients with acquired-immune deficiency syndrome (AIDS). Also described are methods for treating AIDS patients using the described alkenyldiarylmethane compounds.
FORMULATION OF METAXALONE
Dosage forms of metaxalone containing submicron particles of metaxalone and uses thereof are described. The submicron dosage forms have improved bioavailability compared to certain conventional metaxalone dosage forms.
FORMULATION OF METAXALONE
Dosage forms of metaxalone containing submicron particles of metaxalone and uses thereof are described. The submicron dosage forms have improved bioavailability compared to certain conventional metaxalone dosage forms.