C07D241/06

P2X7R ANTAGONISTS
20220380310 · 2022-12-01 ·

A compound has Formula I:

##STR00001##

R.sub.1 is hydrogen, hydroxy, halogen, nitro, amino, alkyl, alkoxy, alkylamino, cycloalkyl, cycloalkyamino, heterocyclyl, aryl, heteroaryl, —NR.sub.7R.sub.8, —CO—R.sub.10, or —NH—CO—R.sub.10; L is a bond, a heterocyclic bivalent group, a heteroaromatic bivalent group, or an aromatic bivalent group; M is a bond, alkyl, aryl, heterocyclic bivalent group, heteroaromatic bivalent group, or aromatic bivalent group; X is a bond, —O—, —S—, —SO.sub.2—, —CO—, —NR.sub.9—, —(CH.sub.2).sub.m—, or heterocyclic bivalent group, m is 1, 2, 3, 4, 5, or 6; Y is a bond, —NH—, heterocyclic bivalent group, heteroaromatic bivalent group, bivalent benzyl group, or aromatic bivalent group; and Z is hydrogen, halogen, alkyl, aryl, heterocyclyl, heteroaryl, —NR.sub.7R.sub.8, —CO—R.sub.10, or —NH—CO—R.sub.10; R.sub.7, R.sub.8, and R.sub.9 are independently hydrogen, hydroxy, halogen, nitro, amino, alkyl, alkoxy, alkylamino, cycloalkyl, cycloalkyamino, heterocyclyl, or heteroaryl; and R.sub.10 is —O-tert-butyl, —CH.sub.2CH.sub.2-phenyl, hydrogen, hydroxy, halogen, nitro, amino, alkyl, alkoxy, alkylamino, cycloalkyl, cycloalkyamino, heterocyclyl, or heteroaryl.

P2X7R ANTAGONISTS
20220380310 · 2022-12-01 ·

A compound has Formula I:

##STR00001##

R.sub.1 is hydrogen, hydroxy, halogen, nitro, amino, alkyl, alkoxy, alkylamino, cycloalkyl, cycloalkyamino, heterocyclyl, aryl, heteroaryl, —NR.sub.7R.sub.8, —CO—R.sub.10, or —NH—CO—R.sub.10; L is a bond, a heterocyclic bivalent group, a heteroaromatic bivalent group, or an aromatic bivalent group; M is a bond, alkyl, aryl, heterocyclic bivalent group, heteroaromatic bivalent group, or aromatic bivalent group; X is a bond, —O—, —S—, —SO.sub.2—, —CO—, —NR.sub.9—, —(CH.sub.2).sub.m—, or heterocyclic bivalent group, m is 1, 2, 3, 4, 5, or 6; Y is a bond, —NH—, heterocyclic bivalent group, heteroaromatic bivalent group, bivalent benzyl group, or aromatic bivalent group; and Z is hydrogen, halogen, alkyl, aryl, heterocyclyl, heteroaryl, —NR.sub.7R.sub.8, —CO—R.sub.10, or —NH—CO—R.sub.10; R.sub.7, R.sub.8, and R.sub.9 are independently hydrogen, hydroxy, halogen, nitro, amino, alkyl, alkoxy, alkylamino, cycloalkyl, cycloalkyamino, heterocyclyl, or heteroaryl; and R.sub.10 is —O-tert-butyl, —CH.sub.2CH.sub.2-phenyl, hydrogen, hydroxy, halogen, nitro, amino, alkyl, alkoxy, alkylamino, cycloalkyl, cycloalkyamino, heterocyclyl, or heteroaryl.

INHIBITORS OF ENCEPHALITIC ALPHAVIRUSES

Compounds of Formula I and Formula II:

##STR00001##

pharmaceutical compositions containing them, and use of the compounds as active ingredients to treat infection with alphavirus.

CRYSTAL FORM OF DIAZASPIROPYRAN COMPOUND
20230141887 · 2023-05-11 ·

Disclosed are a salt type and a crystal form (I) of a diazaspiropyran compound, and a preparation method therefor. Also disclosed is the use of the salt type and the crystal form in the preparation of drugs for treating related diseases.

##STR00001##

N-acyl amino acid compounds and methods of use

The invention relates to compounds of formula (I): ##STR00001##
or a salt thereof, wherein R.sup.1, A, L, and R.sup.2 and n are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are αvβ1 integrin inhibitors that are useful for treating tissue specific fibrosis.

N-acyl amino acid compounds and methods of use

The invention relates to compounds of formula (I): ##STR00001##
or a salt thereof, wherein R.sup.1, A, L, and R.sup.2 and n are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are αvβ1 integrin inhibitors that are useful for treating tissue specific fibrosis.

N-ACYL AMINO ACID COMPOUNDS AND METHODS OF USE

The invention relates to compounds of formula (I):

##STR00001##

or a salt thereof, wherein R.sup.1, A, L, and R.sup.2 and n are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are αvβ1 integrin inhibitors that are useful for treating tissue specific fibrosis.

N-ACYL AMINO ACID COMPOUNDS AND METHODS OF USE

The invention relates to compounds of formula (I):

##STR00001##

or a salt thereof, wherein R.sup.1, A, L, and R.sup.2 and n are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are αvβ1 integrin inhibitors that are useful for treating tissue specific fibrosis.

Perfluorinated Allyl Ethers and Perfluorinated Allyl Amines and Methods of Making and Using the Same

##STR00001##

##STR00002##

Described herein is a method to synthesize a perfluorinated allyl ether compound of formula (I) or a perfluorinated allyl amine compound of formula (II) Where R.sub.f.sup.1 and R.sub.f.sup.2 are (i) independently selected from a perfluorinated alkyl group comprising 1-7 carbon atoms, a perfluorinated aryl group comprising a 5- or 6-membered ring, or combinations thereof, and optionally comprising one or more catenated heteroatoms selected from N or O; or (ii) bonded together to form a perfluorinated ring structure having 4-8 ring carbon atoms, optionally comprising at least one catenated O or N atom; and R.sub.f.sup.3 is a perfluorinated alkyl group comprising 1-3 carbon atoms. The resulting perfluorinated allyl ether compounds disclosed herein may be used in polymer synthesis.

Perfluorinated Allyl Ethers and Perfluorinated Allyl Amines and Methods of Making and Using the Same

##STR00001##

##STR00002##

Described herein is a method to synthesize a perfluorinated allyl ether compound of formula (I) or a perfluorinated allyl amine compound of formula (II) Where R.sub.f.sup.1 and R.sub.f.sup.2 are (i) independently selected from a perfluorinated alkyl group comprising 1-7 carbon atoms, a perfluorinated aryl group comprising a 5- or 6-membered ring, or combinations thereof, and optionally comprising one or more catenated heteroatoms selected from N or O; or (ii) bonded together to form a perfluorinated ring structure having 4-8 ring carbon atoms, optionally comprising at least one catenated O or N atom; and R.sub.f.sup.3 is a perfluorinated alkyl group comprising 1-3 carbon atoms. The resulting perfluorinated allyl ether compounds disclosed herein may be used in polymer synthesis.