C07C57/60

COMPOSITIONS AND METHODS FOR PREPARING BETA,GAMMA-UNSATURATED ACIDS
20180327343 · 2018-11-15 ·

The present disclosure provides methods for enantioselective synthesis of acyclic -quaternary carboxylic acid derivatives via iridium-catalyzed allylic alkylation.

NOVEL REXINOID COMPOUNDS AND METHODS OF USING REXINOID COMPOUNDS FOR TREATING METABOLIC DISORDERS AND CANCER

Novel rexinoid compounds are provided herein. Also provided herein are methods of using the compounds to treat disorders, such as metabolic disorders, diabetes, insulin resistance, glucose intolerance, obesity, steatosis, inflammation, and/or cancer.

SUBSTITUTED AROMATIC COMPOUNDS FOR THE TREATMENT OF PULMONARY FIBROSIS, LIVER FIBROSIS,SKIN FIBROSIS AND CARDIAC FIBROSIS

The present invention relates to substituted aromatic compounds for use in prevention or treatment of various fibrotic diseases and conditions in subjects, including pulmonary fibrosis, liver fibrosis, skin fibrosis and cardiac fibrosis, where the compound has the following formula:

##STR00001##

or a pharmaceutically acceptable salt thereof, wherein A is C.sub.5 alkyl, C.sub.6 alkyl, C.sub.5 alkenyl, C.sub.6 alkenyl, C(O)(CH.sub.2).sub.nCH.sub.3 or CH(OH)(CH.sub.2).sub.nCH.sub.3 wherein n is 3 or 4; R.sub.1 is H, OH or F; R.sub.2 is H, OH, F or CH.sub.2OH; R.sub.3 is H, OH, F or CH.sub.2Ph; R.sub.4 is H, OH or F; Q is 1) (CH.sub.2).sub.mC(O)OH wherein m is 1 or 2, 2) CH(CH.sub.3)C(O)OH, 3) C(CH.sub.3).sub.2C(O)OH, 4) CH(F)C(O)OH, 5) CF.sub.2C(O)OH, or 6) C(O)C(O)OH.

SUBSTITUTED AROMATIC COMPOUNDS FOR THE TREATMENT OF PULMONARY FIBROSIS, LIVER FIBROSIS,SKIN FIBROSIS AND CARDIAC FIBROSIS

The present invention relates to substituted aromatic compounds for use in prevention or treatment of various fibrotic diseases and conditions in subjects, including pulmonary fibrosis, liver fibrosis, skin fibrosis and cardiac fibrosis, where the compound has the following formula:

##STR00001##

or a pharmaceutically acceptable salt thereof, wherein A is C.sub.5 alkyl, C.sub.6 alkyl, C.sub.5 alkenyl, C.sub.6 alkenyl, C(O)(CH.sub.2).sub.nCH.sub.3 or CH(OH)(CH.sub.2).sub.nCH.sub.3 wherein n is 3 or 4; R.sub.1 is H, OH or F; R.sub.2 is H, OH, F or CH.sub.2OH; R.sub.3 is H, OH, F or CH.sub.2Ph; R.sub.4 is H, OH or F; Q is 1) (CH.sub.2).sub.mC(O)OH wherein m is 1 or 2, 2) CH(CH.sub.3)C(O)OH, 3) C(CH.sub.3).sub.2C(O)OH, 4) CH(F)C(O)OH, 5) CF.sub.2C(O)OH, or 6) C(O)C(O)OH.

Chiral oligomeric pentenoate amides as bio-oligomer mimetics

Chiral oligomeric pentenoate amides are bio-oligomer mimetics possessing a high degree of conformation rigidity. Conformational rigidity is desirable in the design of molecules with high affinities for biological receptors and enzymes. Libraries of such oligomeric mimetics, such as of chiral oligomeric pentenoate amides can be used to probe biological systems. The present invention provides a method for preparation of chiral oligomeric pentanoate amides comprising conversion of a chiral oxazolidinone (4) ##STR00001##
to a chiral monomer of formula (1) ##STR00002##
which can be oligomerized to a chiral compound of formula (12) ##STR00003##
and so forth.

Chiral oligomeric pentenoate amides as bio-oligomer mimetics

Chiral oligomeric pentenoate amides are bio-oligomer mimetics possessing a high degree of conformation rigidity. Conformational rigidity is desirable in the design of molecules with high affinities for biological receptors and enzymes. Libraries of such oligomeric mimetics, such as of chiral oligomeric pentenoate amides can be used to probe biological systems. The present invention provides a method for preparation of chiral oligomeric pentanoate amides comprising conversion of a chiral oxazolidinone (4) ##STR00001##
to a chiral monomer of formula (1) ##STR00002##
which can be oligomerized to a chiral compound of formula (12) ##STR00003##
and so forth.

Substituted aromatic compounds for the treatment pulmonary fibrosis, liver fibrosis, skin fibrosis and cardiac fibrosis

The present invention relates to substituted aromatic compounds for use in prevention or treatment of various fibrotic diseases and conditions in subjects, including pulmonary fibrosis, liver fibrosis, skin fibrosis and cardiac fibrosis, where the compound has the following formula: or a pharmaceutically acceptable salt thereof, wherein A is C.sub.5 alkyl, C.sub.6 alkyl, C.sub.5 alkenyl, C.sub.6 alkenyl, C(O)(CH.sub.2).sub.nCH.sub.3 or CH(OH)(CH.sub.2).sub.nCH.sub.3 wherein n is 3 or 4; R.sub.1 is H, OH or F; R.sub.2 is H, OH, F or CH.sub.2OH; R.sub.3 is H, OH, F or CH.sub.2Ph; R.sub.4 is H, OH or F; Q is 1) (CH.sub.2).sub.mC(O)OH wherein m is 1 or 2, 2) CH(CH.sub.3)C(O)OH, 3) C(CH.sub.3).sub.2C(O)OH, 4) CH(F)C(O)OH, 5) CF.sub.2C(O)OH, or 6) C(O)C(O)OH. ##STR00001##

Substituted aromatic compounds for the treatment pulmonary fibrosis, liver fibrosis, skin fibrosis and cardiac fibrosis

The present invention relates to substituted aromatic compounds for use in prevention or treatment of various fibrotic diseases and conditions in subjects, including pulmonary fibrosis, liver fibrosis, skin fibrosis and cardiac fibrosis, where the compound has the following formula: or a pharmaceutically acceptable salt thereof, wherein A is C.sub.5 alkyl, C.sub.6 alkyl, C.sub.5 alkenyl, C.sub.6 alkenyl, C(O)(CH.sub.2).sub.nCH.sub.3 or CH(OH)(CH.sub.2).sub.nCH.sub.3 wherein n is 3 or 4; R.sub.1 is H, OH or F; R.sub.2 is H, OH, F or CH.sub.2OH; R.sub.3 is H, OH, F or CH.sub.2Ph; R.sub.4 is H, OH or F; Q is 1) (CH.sub.2).sub.mC(O)OH wherein m is 1 or 2, 2) CH(CH.sub.3)C(O)OH, 3) C(CH.sub.3).sub.2C(O)OH, 4) CH(F)C(O)OH, 5) CF.sub.2C(O)OH, or 6) C(O)C(O)OH. ##STR00001##

Ligand-exchangeable janus nanoparticles and methods of making the same

The present disclosure relates to a nanocrystal that includes a nanocrystal core, a first ligand coordinated to a first portion of a surface of the nanocrystal core, and a second ligand coordinated to a second portion of the surface, where the second ligand includes a first functionalized aromatic molecule.

Ligand-exchangeable janus nanoparticles and methods of making the same

The present disclosure relates to a nanocrystal that includes a nanocrystal core, a first ligand coordinated to a first portion of a surface of the nanocrystal core, and a second ligand coordinated to a second portion of the surface, where the second ligand includes a first functionalized aromatic molecule.