Patent classifications
C07C57/42
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.n—CH.sub.3 or CH(OH)—(CH.sub.2).sub.n—CH.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.2—OH; 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.2—C(O)OH, or 6) C(O)—C(O)OH.
A METHOD FOR DIRECTLY CONSTRUCTING HIGHLY OPTICALLY ACTIVE TETRASUBSTITUTED ALLENIC ACID COMPOUNDS
The present invention discloses a method for directly constructing highly optically active tetrasubstituted allenic acid compounds, i.e., a one-step process for directly constructing highly optically active axially chiral tetrasubstituted allenic acid compounds by using tertiary propargyl alcohol, carbon monoxide and water as reactants in an organic solvent in the presence of palladium catalyst, chiral diphosphine ligand, monophosphine ligand and organic phosphoric acid. The method of the present invention has the following advantages: operations are simple, raw materials and reagents are readily available, the reaction conditions are mild, the substrate has high universality, the functional group has good compatibility, and the reaction has high enantioselectivity (90%˜>99% ee). The highly optically active allenic acid compounds obtained by the present invention can be used as an important intermediate to construct γ-butyrolactone compounds containing tetrasubstituted chiral quaternary carbon centers, tetrasubstituted allenic alcohol and other compounds.
A METHOD FOR DIRECTLY CONSTRUCTING HIGHLY OPTICALLY ACTIVE TETRASUBSTITUTED ALLENIC ACID COMPOUNDS
The present invention discloses a method for directly constructing highly optically active tetrasubstituted allenic acid compounds, i.e., a one-step process for directly constructing highly optically active axially chiral tetrasubstituted allenic acid compounds by using tertiary propargyl alcohol, carbon monoxide and water as reactants in an organic solvent in the presence of palladium catalyst, chiral diphosphine ligand, monophosphine ligand and organic phosphoric acid. The method of the present invention has the following advantages: operations are simple, raw materials and reagents are readily available, the reaction conditions are mild, the substrate has high universality, the functional group has good compatibility, and the reaction has high enantioselectivity (90%˜>99% ee). The highly optically active allenic acid compounds obtained by the present invention can be used as an important intermediate to construct γ-butyrolactone compounds containing tetrasubstituted chiral quaternary carbon centers, tetrasubstituted allenic alcohol and other compounds.
COMPOSITIONS AND METHODS OF USING ITACONIC ACID DERIVATIVES
The present invention is directed to itaconic acid derivatives, compounds comprising the derivatives and methods of using the derivatives in the treatment of cancer, inflammation, and autoimmune diseases.
COMPOSITIONS AND METHODS OF USING ITACONIC ACID DERIVATIVES
The present invention is directed to itaconic acid derivatives, compounds comprising the derivatives and methods of using the derivatives in the treatment of cancer, inflammation, and autoimmune diseases.
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.
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.
Organic ligand and preparation method thereof, quantum dot structure material, quantum-dot-containing layer, and light emitting diode
The present disclosure provides quantum dot organic ligand and preparation method thereof, quantum dot structure material, quantum-dot-containing layer, and quantum-dot-containing light emitting diode. The quantum dot organic ligand have the following structure R1-(R2).sub.n-R3, wherein R1 is a chelating group capable of chelating with a metal; R2 is a group having a conjugated electron pair, and n is a positive integer; and R3 is organic group. The conjugated electron pair structure of R2 facilitates delocalization of electrons, which can improve the transport and conduction of electrons and/or holes, thereby improving the efficiency of quantum dots and lowering the turn-on voltage.
Organic ligand and preparation method thereof, quantum dot structure material, quantum-dot-containing layer, and light emitting diode
The present disclosure provides quantum dot organic ligand and preparation method thereof, quantum dot structure material, quantum-dot-containing layer, and quantum-dot-containing light emitting diode. The quantum dot organic ligand have the following structure R1-(R2).sub.n-R3, wherein R1 is a chelating group capable of chelating with a metal; R2 is a group having a conjugated electron pair, and n is a positive integer; and R3 is organic group. The conjugated electron pair structure of R2 facilitates delocalization of electrons, which can improve the transport and conduction of electrons and/or holes, thereby improving the efficiency of quantum dots and lowering the turn-on voltage.
Substituted Aromatic Compounds and Pharmaceutical Uses Thereof
The present invention relates to substituted aromatic compounds of Formula I and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds in the prevention and/or treatment of various diseases and conditions in subjects, including the prevention or treatment of (i) blood disorders, (ii) renal disorders, a nephropathies, or renal disorder complications; (iii) inflammatory-related diseases; and/or (iv) oxidative stress related disorders.