Patent classifications
C07C233/87
PPAR AGONISTS AND METHODS OF USE THEREOF
Provided herein are deuterated compounds and compositions useful in increasing PPAR activity. The compounds have a formula
##STR00001##
where L.sup.5 comprises at least one deuterium. Exemplary species include
##STR00002##
The compounds and compositions provided herein are useful for the treatment of PPAR related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).
3-Phenylisoserine derivative production method
A method produces a 3-phenylisoserine derivative by protecting an amino group of a compound represented by General Formula (1) (wherein R.sup.1 represents a phenyl group, or a phenyl group having a substituent; R.sup.2 represents an alkali metal, alkaline earth metal, or nitrogen base; and R.sup.3 represents a hydrogen atom, methyl group, benzyl group, p-methoxybenzyl group, tert-butyl group, methoxymethyl group, 2-tetrahydropyranyl group, ethoxyethyl group, acetyl group, pivaloyl group, benzoyl group, trimethylsilyl group, triethylsilyl group, or tert-butyldimethylsilyl group) in water or a mixed solvent containing water to obtain a particular compound; extracting with a C.sub.4 ether-based solvent; replacing at least part of the C.sub.4 ether-based solvent with a C.sub.1-C.sub.4 aliphatic alcohol while removing the C.sub.4 ether-based solvent and water to perform esterification reaction; and isolating at 0 to 30 C. to obtain a 3-phenylisoserine derivative represented by General Formula (2). ##STR00001##
3-Phenylisoserine derivative production method
A method produces a 3-phenylisoserine derivative by protecting an amino group of a compound represented by General Formula (1) (wherein R.sup.1 represents a phenyl group, or a phenyl group having a substituent; R.sup.2 represents an alkali metal, alkaline earth metal, or nitrogen base; and R.sup.3 represents a hydrogen atom, methyl group, benzyl group, p-methoxybenzyl group, tert-butyl group, methoxymethyl group, 2-tetrahydropyranyl group, ethoxyethyl group, acetyl group, pivaloyl group, benzoyl group, trimethylsilyl group, triethylsilyl group, or tert-butyldimethylsilyl group) in water or a mixed solvent containing water to obtain a particular compound; extracting with a C.sub.4 ether-based solvent; replacing at least part of the C.sub.4 ether-based solvent with a C.sub.1-C.sub.4 aliphatic alcohol while removing the C.sub.4 ether-based solvent and water to perform esterification reaction; and isolating at 0 to 30 C. to obtain a 3-phenylisoserine derivative represented by General Formula (2). ##STR00001##
FARNESOID X RECEPTOR AGONISTS AND USES THEREOF
Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.
3-PHENYLISOSERINE DERIVATIVE PRODUCTION METHOD
A method produces a 3-phenylisoserine derivative by protecting an amino group of a compound represented by General Formula (1) (wherein R.sup.1 represents a phenyl group, or a phenyl group having a substituent; R.sup.2 represents an alkali metal, alkaline earth metal, or nitrogen base; and R.sup.3 represents a hydrogen atom, methyl group, benzyl group, p-methoxybenzyl group, tert-butyl group, methoxymethyl group, 2-tetrahydropyranyl group, ethoxyethyl group, acetyl group, pivaloyl group, benzoyl group, trimethylsilyl group, triethylsilyl group, or tert-butyldimethylsilyl group) in water or a mixed solvent containing water to obtain a particular compound; extracting with a C.sub.4 ether-based solvent; replacing at least part of the C.sub.4 ether-based solvent with a C.sub.1-C.sub.4 aliphatic alcohol while removing the C.sub.4 ether-based solvent and water to perform esterification reaction; and isolating at 0 to 30 C. to obtain a 3-phenylisoserine derivative represented by General Formula (2).
##STR00001##
3-PHENYLISOSERINE DERIVATIVE PRODUCTION METHOD
A method produces a 3-phenylisoserine derivative by protecting an amino group of a compound represented by General Formula (1) (wherein R.sup.1 represents a phenyl group, or a phenyl group having a substituent; R.sup.2 represents an alkali metal, alkaline earth metal, or nitrogen base; and R.sup.3 represents a hydrogen atom, methyl group, benzyl group, p-methoxybenzyl group, tert-butyl group, methoxymethyl group, 2-tetrahydropyranyl group, ethoxyethyl group, acetyl group, pivaloyl group, benzoyl group, trimethylsilyl group, triethylsilyl group, or tert-butyldimethylsilyl group) in water or a mixed solvent containing water to obtain a particular compound; extracting with a C.sub.4 ether-based solvent; replacing at least part of the C.sub.4 ether-based solvent with a C.sub.1-C.sub.4 aliphatic alcohol while removing the C.sub.4 ether-based solvent and water to perform esterification reaction; and isolating at 0 to 30 C. to obtain a 3-phenylisoserine derivative represented by General Formula (2).
##STR00001##
PPAR AGONISTS
Provided herein are compounds and compositions useful in increasing PPAR activity. The compounds and compositions provided herein are useful for the treatment of PPAR related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).
PPAR AGONISTS
Provided herein are compounds and compositions useful in increasing PPAR activity. The compounds and compositions provided herein are useful for the treatment of PPAR related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).
Inhibitors of Mcl-1 as Drugs to Overcome Resistance to BRAF Inhibitors and MEK Inhibitors
The present invention includes compositions and methods for inhibiting MCL-1, including novel inhibitors of MCL-1, and compositions and methods for treating a subject with cancer that is refractory to one or more MAPK pathway protein inhibitors.
PPAR agonists
Provided herein are compounds and compositions useful in increasing PPAR activity. The compounds and compositions provided herein are useful for the treatment of PPAR related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).