C07C69/28

BISPHENOL DERIVATIVES AND THEIR USE AS ANDROGEN RECEPTOR ACTIVITY MODULATORS

Compounds having a structure of Formula I:

##STR00001##

or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.11a, R.sup.11b, R.sup.11c, R.sup.11d, and X, are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.

EPOXY ESTER COMPOUND, CELLULOSE ESTER RESIN COMPOSITION, OPTICAL FILM, AND LIQUID-CRYSTAL DISPLAY DEVICE
20170292009 · 2017-10-12 ·

The present invention has an object to provide a compound which has excellent compatibility even with a cellulose ester resin having a low acetylation degree, is capable of providing an optical film having a high Rth value and high bleed resistance, and can be suitably used as a retardation enhancer; a cellulose ester resin composition including the compound; an optical film including the resin composition; and a liquid-crystal display device including the optical film. The present invention provides an epoxy ester compound represented by the following Formula (1) (in the formula, R.sup.1 to R.sup.4 each independently represent an alkyl group having 1 to 3 carbon atoms; and A's each represent an aromatic group (a1) or an aliphatic group (a2) having 1 to 4 carbon atoms, and the average presence ratio [(a1)/(a2)] of the aromatic groups (a1) to the aliphatic groups (a2) is 99.9/0.1 to 80/20 in terms of a molar ratio).

EPOXY ESTER COMPOUND, CELLULOSE ESTER RESIN COMPOSITION, OPTICAL FILM, AND LIQUID-CRYSTAL DISPLAY DEVICE
20170292009 · 2017-10-12 ·

The present invention has an object to provide a compound which has excellent compatibility even with a cellulose ester resin having a low acetylation degree, is capable of providing an optical film having a high Rth value and high bleed resistance, and can be suitably used as a retardation enhancer; a cellulose ester resin composition including the compound; an optical film including the resin composition; and a liquid-crystal display device including the optical film. The present invention provides an epoxy ester compound represented by the following Formula (1) (in the formula, R.sup.1 to R.sup.4 each independently represent an alkyl group having 1 to 3 carbon atoms; and A's each represent an aromatic group (a1) or an aliphatic group (a2) having 1 to 4 carbon atoms, and the average presence ratio [(a1)/(a2)] of the aromatic groups (a1) to the aliphatic groups (a2) is 99.9/0.1 to 80/20 in terms of a molar ratio).

CANNABINOID DERIVATIVES
20220267239 · 2022-08-25 ·

The present invention provides cannabinoid derivatives, a pharmaceutical composition comprising said derivative and a method of using said derivatives in treating or preventing a disease associated with cannabinoid receptors. The claimed cannabinoid derivatives are described by formula (I) or an enantiomer, diastereomer, racemate, tautomer, or metabolite thereof, or a pharmaceutically acceptable salt, solvate or hydrate of the compound.

CANNABINOID DERIVATIVES
20220267239 · 2022-08-25 ·

The present invention provides cannabinoid derivatives, a pharmaceutical composition comprising said derivative and a method of using said derivatives in treating or preventing a disease associated with cannabinoid receptors. The claimed cannabinoid derivatives are described by formula (I) or an enantiomer, diastereomer, racemate, tautomer, or metabolite thereof, or a pharmaceutically acceptable salt, solvate or hydrate of the compound.

KINETIC RESOLUTION REACTION OF A (1RS,2SR)-(2-HYDROXY-3,5,5-TRIMETHYL-3-CYCLOPENTENYL)METHYL CARBOXYLATE COMPOUND, A PROCESS FOR PREPARING OPTICALLY ACTIVE TRANS-alpha-NECRODYL ISOBUTYRATE, AND A PROCESS FOR PREPARING OPTICALLY ACTIVE gamma-NECRODYL ISOBUTYRATE

The present invention relates to a process for preparing a (1S,2R)-(2-hydroxy-3,5,5-trimethyl-3-cyclopentenyl)methyl carboxylate compound of the following general formula (S,R)-(2), wherein R.sup.1 represents a monovalent hydrocarbon group having 1 to 6 carbon atoms, and a bold wedged bond represents the absolute configuration, and a (1R,2S)-(2-acetoxy-3,5,5-trimethyl-3-cyclopentenyl)methyl carboxylate compound of the following general formula (R,S)-(3), wherein R.sup.1 is as defined above, a hashed wedged bond represents the absolute configuration, and Ac represents an acetyl group, the process comprising: subjecting a (1RS,2SR)-(2-hydroxy-3,5,5-trimethyl-3-cyclopentenyl)methyl carboxylate compound of the following general formula (RS,SR)-(2), wherein R.sup.1 is as defined above, and a hashed unwedged bond represents a relative configuration, to a kinetic resolution reaction with a lipase in the presence of vinyl acetate to obtain the (1S,2R)-(2-hydroxy-3,5,5-trimethyl-3-cyclopentenyl)methyl carboxylate compound ((S,R)-(2)) and the (1R,2S)-(2-acetoxy-3,5,5-trimethyl-3-cyclopentenyl)methyl carboxylate compound ((R,S)-(3)).

##STR00001##

KINETIC RESOLUTION REACTION OF A (1RS,2SR)-(2-HYDROXY-3,5,5-TRIMETHYL-3-CYCLOPENTENYL)METHYL CARBOXYLATE COMPOUND, A PROCESS FOR PREPARING OPTICALLY ACTIVE TRANS-alpha-NECRODYL ISOBUTYRATE, AND A PROCESS FOR PREPARING OPTICALLY ACTIVE gamma-NECRODYL ISOBUTYRATE

The present invention relates to a process for preparing a (1S,2R)-(2-hydroxy-3,5,5-trimethyl-3-cyclopentenyl)methyl carboxylate compound of the following general formula (S,R)-(2), wherein R.sup.1 represents a monovalent hydrocarbon group having 1 to 6 carbon atoms, and a bold wedged bond represents the absolute configuration, and a (1R,2S)-(2-acetoxy-3,5,5-trimethyl-3-cyclopentenyl)methyl carboxylate compound of the following general formula (R,S)-(3), wherein R.sup.1 is as defined above, a hashed wedged bond represents the absolute configuration, and Ac represents an acetyl group, the process comprising: subjecting a (1RS,2SR)-(2-hydroxy-3,5,5-trimethyl-3-cyclopentenyl)methyl carboxylate compound of the following general formula (RS,SR)-(2), wherein R.sup.1 is as defined above, and a hashed unwedged bond represents a relative configuration, to a kinetic resolution reaction with a lipase in the presence of vinyl acetate to obtain the (1S,2R)-(2-hydroxy-3,5,5-trimethyl-3-cyclopentenyl)methyl carboxylate compound ((S,R)-(2)) and the (1R,2S)-(2-acetoxy-3,5,5-trimethyl-3-cyclopentenyl)methyl carboxylate compound ((R,S)-(3)).

##STR00001##

BISPHENOL DERIVATIVES AND THEIR USE AS ANDROGEN RECEPTOR ACTIVITY MODULATORS

Compounds having a structure of Formula I:

##STR00001##

or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.11a, R.sup.11b, R.sup.11c, R.sup.11d, and X, are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.

BISPHENOL DERIVATIVES AND THEIR USE AS ANDROGEN RECEPTOR ACTIVITY MODULATORS

Compounds having a structure of Formula I:

##STR00001##

or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.11a, R.sup.11b, R.sup.11c, R.sup.11d, and X, are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.

Ophthalmic composition containing compounds found in Harderian gland secretions
11339114 · 2022-05-24 · ·

The present invention is directed to pharmaceutical compositions comprising compounds found in Harderian gland secretions, a method of treating dry eye in a human comprising ophthalmically administering an effective amount of a compound, e.g. a lipid compound, found in Harderian gland secretions, pharmaceutical compositions comprising said lipid compounds, as identified by characteristic chemical data and mass spectra of said lipid compounds, said lipid compound in essentially pure form, and an ophthalmic vehicle comprising a therapeutic agent and a compound present in the secretions of the Harderian gland, e.g. a lipid compound, found in the secretions of the Harderian gland, e.g. a rabbit Harderian gland.