C07C311/20

OPIOID RECEPTOR AGONIST, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USE THEREOF
20230027752 · 2023-01-26 ·

The invention belongs to the field of pharmacy, and relates to a class of opioid receptor agonists, their preparation method and the pharmaceutical use thereof, in particular to 3-(dimethylaminomethyl) cyclohex-4-ol derivatives or salts thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivatives or salts thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivatives or salts thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivative or salt thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivative or salt thereof and preparation method thereof, and relate to the use of said compounds in the treatment of opioid receptor-mediated diseases. The use of the compound or pharmaceutically acceptable salt, solvate or hydrate thereof in the preparation of a medicament for treating indications related to opioid receptors. The opioid receptor-related indications are pain, irritable bowel syndrome, pruritus, addiction and depression.

OPIOID RECEPTOR AGONIST, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USE THEREOF
20230027752 · 2023-01-26 ·

The invention belongs to the field of pharmacy, and relates to a class of opioid receptor agonists, their preparation method and the pharmaceutical use thereof, in particular to 3-(dimethylaminomethyl) cyclohex-4-ol derivatives or salts thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivatives or salts thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivatives or salts thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivative or salt thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivative or salt thereof and preparation method thereof, and relate to the use of said compounds in the treatment of opioid receptor-mediated diseases. The use of the compound or pharmaceutically acceptable salt, solvate or hydrate thereof in the preparation of a medicament for treating indications related to opioid receptors. The opioid receptor-related indications are pain, irritable bowel syndrome, pruritus, addiction and depression.

Highly enantioselective access to cyclic beta-amino acids

Disclosed herein is a method of forming a compound of formula I: ##STR00001##
wherein the substituents are defined in the specification. In particular, the compounds of formula I can be converted to amino acids bearing quaternary stereocenters with exceptional optical purities.

Highly enantioselective access to cyclic beta-amino acids

Disclosed herein is a method of forming a compound of formula I: ##STR00001##
wherein the substituents are defined in the specification. In particular, the compounds of formula I can be converted to amino acids bearing quaternary stereocenters with exceptional optical purities.

Method for producing optically active substance, optically active substance, method for producing chiral molecule, and chiral molecule

Provided is a method for producing an optically active substance, the method including an asymmetric induction, wherein an asymmetry inducer is allowed to act on a chiral molecule having a half-life of enantiomeric excess of shorter than 10 hours, thereby increasing abundance of one enantiomer of the chiral molecule. According to this method, one enantiomer of a chiral molecule that is susceptible to racemization can be selectively and efficiently obtained.

Method for producing optically active substance, optically active substance, method for producing chiral molecule, and chiral molecule

Provided is a method for producing an optically active substance, the method including an asymmetric induction, wherein an asymmetry inducer is allowed to act on a chiral molecule having a half-life of enantiomeric excess of shorter than 10 hours, thereby increasing abundance of one enantiomer of the chiral molecule. According to this method, one enantiomer of a chiral molecule that is susceptible to racemization can be selectively and efficiently obtained.

FERROPTOSIS INDUCING COMPOUND, COMPOSITIONS COMPRISING THE SAME, AND METHODS OF INDUCING FERROPTOSIS
20220324798 · 2022-10-13 ·

Provided is a compound according to Formula 1

##STR00001##

wherein X, R, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are as defined herein. The compound of Formula 1 can be useful in a composition and in a method for inducing ferroptosis in a cell.

FERROPTOSIS INDUCING COMPOUND, COMPOSITIONS COMPRISING THE SAME, AND METHODS OF INDUCING FERROPTOSIS
20220324798 · 2022-10-13 ·

Provided is a compound according to Formula 1

##STR00001##

wherein X, R, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are as defined herein. The compound of Formula 1 can be useful in a composition and in a method for inducing ferroptosis in a cell.

Tetrahydronaphthalene derivatives useful as Nrf2 activators

Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, and methods for their use as Nrf2 activators and for their production. ##STR00001##