C07F9/65522

Method of biotransformation of benzopyrone compounds into the corresponding phosphate-conjugated derivatives

The present invention is related to a biotransformation process, effected by means of an isolated polypeptide possessing benzopyrone phosphate synthetase activity, and also a microorganism comprising a nucleic acid sequence that encodes the polypeptide, for the preparation of phosphate-conjugated derivatives of benzopyrone compounds. The hydrophilic property of the benzopyrone compounds is enhanced after catalyzed by the benzopyrone phosphate synthetase of the present invention.

PRODRUGS OF TETRAHYDROCANNABINOL, COMPOSITIONS COMPRISING PRODRUGS OF TETRAHYDROCANNABINOL AND METHODS OF USING THE SAME

Described herein are .sup.9-THC prodrugs, methods of making .sup.9-THC prodrugs, formulations comprising .sup.9-THC prodrugs and methods of using .sup.9-THC. One embodiment described herein relates to the transdermal administration of a .sup.9-THC prodrug for treating and preventing diseases and/or disorders.

P-CHIRAL PHOSPHINE LIGANDS AND USE THEREOF FOR ASYMMETRIC SYNTHESIS
20190211040 · 2019-07-11 ·

The present invention relates to chiral compounds with two optically active phosphorus atoms, chiral transition metal catalysts which comprise these compounds as ligands, a process for preparing the P-chiral compounds and processes for asymmetric synthesis using the chiral transition metal catalysts. The present invention specifically relates to a process for preparing an optically active carbonyl compound by asymmetric hydrogenation of a prochiral ,-unsaturated carbonyl compound with hydrogen in the presence of an optically active transition metal catalyst according to the invention. Yet more specifically, the present invention relates to a process for the asymmetric hydrogenation of citral, and also a process for preparing optically active menthol.

Heteroaryl compounds useful as inhibitors of sumo activating enzyme

Disclosed are chemical entities which are compounds of formula (I): ##STR00001##
or pharmaceutically acceptable salts thereof; wherein Y, R.sup.a, R.sup.a, R.sup.b, R.sup.c, X.sub.1, X.sub.2, X.sub.3, R.sup.d, Z.sub.1, and Z.sub.2 have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry. Chemical entities according to the disclosure can be useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular, and neurodegenerative diseases or disorders.

HETEROAROMATIC PHOSPHONIUM SALTS FOR TREATING CANCER
20240209011 · 2024-06-27 ·

The present invention relates to chromen-4-one derivatives comprising a phosphonium quaternary group, and to associated multi-salts, solvates, prodrugs and pharmaceutical compositions. The present invention also relates to the use of such compounds and compositions in the treatment and prevention of cancer.

##STR00001##

SYNERGISTIC CANNABINOID ESTERS, THEIR SALTS AND USES THEREOF
20240189327 · 2024-06-13 ·

Cannabinoid esters and their soluble salts with synergistic or additive therapeutic counterparts and stable formulations thereof, as well as their edible, beverage and medicinal applications. The synergistic or additive cannabinoid esters may be used as drugs or prodrugs for treating various conditions related to the modulation or biased modulation of cannabinoid receptors, including but not limited to, pain and inflammation, arthritis, cancer, glaucoma, neurodegenerative disorders, multiple sclerosis, renal fibrosis, fibrotic disorder, mental health disorders, addiction, motor function disorders and gastrointestinal and metabolic disorders.

PRODRUGS OF TETRAHYDROCANNABINOL COMPOSITIONS COMPRISING PRODRUGS OF TETRAHYDROCANNABINOL AND METHODS OF USING THE SAME

Described herein are ?.sup.9-THC prodrugs, methods of making ?.sup.9-THC prodrugs, formulations comprising ?.sup.9-THC prodrugs and methods of using ?.sup.9-THC. One embodiment described herein relates to the transdermal administration of a ?.sup.9-THC prodrug for treating and preventing diseases and/or disorders.

COMPOSITIONS COMPRISING A POLYMERIC DYE AND A CYCLODEXTRIN AND USES THEREOF
20190136065 · 2019-05-09 ·

Compositions comprising a polymeric dye and a cyclodextrin are provided. Methods associated with preparation and use of such compounds, for example in methods for detection of any analyte molecule, are also provided.

Mitochondrially delivered anti-cancer compounds
RE047300 · 2019-03-19 · ·

This invention relates to anti-cancer compounds and to methods for treating or preventing cancer. In one aspect the invention concerns mitochondrially delivered pro-oxidant anti-cancer compounds that generate reactive oxygen species and induce apoptosis of cancerous cells. The delivery moiety can be a lipophilic cation and the pro-oxidant moiety can be a pro-oxidant vitamin E analogue, such as -tocopheryl succinate, -tocopheryl maleate, -tocopheryl maleyl amide, or 2,5,7,8-tetramethyl-2R-(4R,8R,12-trimethyltridecyl)-chroman-6-yloxyacetic acid (-tocopheryloxyacetic acid).

SUBSTITUTED BICYCLIC COMPOUNDS

Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V):

##STR00001##

and/or a salt thereof, wherein R.sub.1 is OH or OP(O)(OH).sub.2, and X.sub.1, X.sub.2, X.sub.3, R.sub.2, R.sub.2a, R.sub.a, R.sub.b, and R.sub.c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.