C07D231/18

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

In one aspect, compounds of Formula A, or a pharmaceutically acceptable salt thereof, are featured (Formula A) or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.

##STR00001##

BETA-AMINO ACID DERIVATIVE, KINASE INHIBITOR AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME, AND METHOD FOR PERFORMING AN IN VIVO RELATED APPLICATION THAT BENEFITS FROM THE INHIBITION OF A KINASE

A compound represented by Formula (I), a pharmaceutically acceptable salt or ester, hydrate, solvate or crystalline form thereof is provided:

##STR00001##

The compound represented by Formula (I) is a β-amino acid derivative, and in Formula (I) X is a single bond or O; Y is NH or C═O; Z is C═O, C═S, NH,

##STR00002##

W is C or N; A is a single bond, O, OH, OCH.sub.2, a heterocycle or N.sub.3; R.sub.1 is H or F; R.sub.2 is H, F, OH, CF.sub.3, CH.sub.2OH, CHO or

##STR00003##

R.sub.3 is H; n is 0 or 1; and m is 0 or 1.

Sulfonylureas and sulfonylthioureas as NLRP.SUB.3 .inhibitors

The present invention relates to sulfonylureas and sulfonylthioureas comprising a 5-membered nitrogen-containing heteroaryl ring attached to the sulfonyl group, wherein the heteroaryl ring is substituted with a nitrogen-containing group R.sup.1′ wherein R.sup.1 contains from 1 to 7 atoms other than hydrogen or halogen. 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.

Sulfonylureas and sulfonylthioureas as NLRP.SUB.3 .inhibitors

The present invention relates to sulfonylureas and sulfonylthioureas comprising a 5-membered nitrogen-containing heteroaryl ring attached to the sulfonyl group, wherein the heteroaryl ring is substituted with a nitrogen-containing group R.sup.1′ wherein R.sup.1 contains from 1 to 7 atoms other than hydrogen or halogen. 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.

Beta-amino acid derivative, kinase inhibitor and pharmaceutical composition containing the same, and method for performing an in vivo related application that benefits from the inhibition of a kinase

A compound represented by Formula (I), a pharmaceutically acceptable salt or ester, hydrate, solvate or crystalline form thereof is provided: ##STR00001##
The compound represented by Formula (I) is a β-amino acid derivative, and in Formula (I) X is a single bond or O; Y is NH or C═O; Z is C═O, C═S, NH, ##STR00002##
W is C or N; A is a single bond, O, OH, OCH.sub.2, a heterocycle or N.sub.3; R.sub.1 is H or F; R.sub.2 is H, F, OH, CF.sub.3, CH.sub.2OH, CHO or ##STR00003##
R.sub.3 is H; n is 0 or 1; and m is 0 or 1.

[(1,4,5-TRISUBSTITUTED-1H-PYRAZOL-3-YL)SULFANYL]ACETIC ACID DERIVATIVES, SALTS THEREOF, AND USE THEREOF AS ACTIVE HERBICIDAL INGREDIENTS

The present invention relates to the technical field of crop protection products, especially that of herbicides for control of broad-leaved weeds and weed grasses in crops of useful plants.

Specifically, this invention relates to novel substituted [(1,4,5-trisubstituted 1H-pyrazol yl)sulfanyl]acetic acid derivatives of the formula (I) or an agrochemically acceptable salt thereof, to processes for preparation thereof and to the use thereof as herbicides.

[(1,4,5-TRISUBSTITUTED-1H-PYRAZOL-3-YL)SULFANYL]ACETIC ACID DERIVATIVES, SALTS THEREOF, AND USE THEREOF AS ACTIVE HERBICIDAL INGREDIENTS

The present invention relates to the technical field of crop protection products, especially that of herbicides for control of broad-leaved weeds and weed grasses in crops of useful plants.

Specifically, this invention relates to novel substituted [(1,4,5-trisubstituted 1H-pyrazol yl)sulfanyl]acetic acid derivatives of the formula (I) or an agrochemically acceptable salt thereof, to processes for preparation thereof and to the use thereof as herbicides.

SYNTHESIS OF NOVEL EP4 ANTAGONIST AND USE IN CANCER AND INFLAMMATION

The present disclosure provides a novel compound effective in antagonizing EP4, which is a compound represented by Formula I, or a tautomer, stereoisomer, hydrate, solvate, pharmaceutically acceptable salt or prodrug of the compound represented by Formula I:

##STR00001## wherein: R.sup.1 is selected from —CH.sub.3, —CHF.sub.2, and —CF.sub.3; R.sup.2 is selected from C.sub.2-C.sub.6 alkyl, C.sub.3-C.sub.6 cycloalkyl, C.sub.2-C.sub.6 halogen-substituted alkyl, C.sub.3-C.sub.6 halogen-substituted cycloalkyl; R.sup.3 is selected from hydrogen, halogen, C.sub.1-C.sub.2 alkyl, C.sub.1-C.sub.2 fluorine- or chlorine-substituted alkyl; R.sup.4 is selected from hydrogen, halogen, C.sub.1-C.sub.6 alkyl, C.sub.1-C.sub.6 alkoxyl, C.sub.1-C.sub.6 halogen-substituted alkyl, C.sub.1-C.sub.6 halogen-substituted alkoxyl.

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured:

##STR00001## or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured:

##STR00001## or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.