C07D211/96

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.

Sulfonyl piperidine derivatives and their use for treating prokineticin mediated diseases

The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof ##STR00001##
in which q, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 are as defined in the specification, for use in therapy.

Sulfonyl piperidine derivatives and their use for treating prokineticin mediated diseases

The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof ##STR00001##
in which q, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 are as defined in the specification, for use in therapy.

SMALL MOLECULES THAT SENSITIZE HIV-1 INFECTED CELLS TO ANTIBODY DEPENDENT CELLULAR CYTOTOXICITY

Compounds and methods of treating HIV-1 in a human infected with HIV-1 or preventing HIV-1 infection in a human susceptible to infection with HIV-1 are provided. The compounds are of formula (I), (II), and (IA), wherein R.sup.1-R.sup.7, X, X′, Y, Y′, Z, and n are defined herein, and the methods comprises administering therapeutically effective amounts of these compounds to the human.

##STR00001##

SMALL MOLECULES THAT SENSITIZE HIV-1 INFECTED CELLS TO ANTIBODY DEPENDENT CELLULAR CYTOTOXICITY

Compounds and methods of treating HIV-1 in a human infected with HIV-1 or preventing HIV-1 infection in a human susceptible to infection with HIV-1 are provided. The compounds are of formula (I), (II), and (IA), wherein R.sup.1-R.sup.7, X, X′, Y, Y′, Z, and n are defined herein, and the methods comprises administering therapeutically effective amounts of these compounds to the human.

##STR00001##

ACLY inhibitors and uses thereof

The present invention provides compounds useful as inhibitors of ATP citrate lyase (ACLY), compositions thereof, and methods of using the same.

ACLY inhibitors and uses thereof

The present invention provides compounds useful as inhibitors of ATP citrate lyase (ACLY), compositions thereof, and methods of using the same.

QUATERNARY HETEROATOM CONTAINING COMPOUNDS

The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II):

##STR00001##

comprising treating a compound of Formula (I):

##STR00002##

with a transition metal catalyst and under alkylation conditions as valence and stability permit.

QUATERNARY HETEROATOM CONTAINING COMPOUNDS

The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II):

##STR00001##

comprising treating a compound of Formula (I):

##STR00002##

with a transition metal catalyst and under alkylation conditions as valence and stability permit.

NOVEL SULFONAMIDE CARBOXAMIDE COMPOUNDS

The present invention relates to compounds of formula (I) wherein Q is selected from O or S; R.sup.1 is a non-aromatic heterocyclic group comprising at least one ring nitrogen atom, wherein R.sup.1 is attached to the sulfur atom of the sulfonylurea group by a ring carbon atom, and wherein R.sup.1 may optionally be substituted; and R.sup.2 is a cyclic group substituted at the α-position, wherein R.sup.2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP.sub.3.

##STR00001##