C07D231/18

HALOGEN SUBSTITUTED DIKETONES, PYRAZOLE COMPOUNDS AND PROCESSES FOR THE MANUFACTURE OF PYRAZOLE COMPOUNDS
20210040043 · 2021-02-11 ·

The present invention concerns new halogen substituted diketone compounds, new pyrazole compounds, processes for the manufacture of pyrazole compounds and processes for the manufacture of agrochemical or pharmaceutical compounds.

HALOGEN SUBSTITUTED DIKETONES, PYRAZOLE COMPOUNDS AND PROCESSES FOR THE MANUFACTURE OF PYRAZOLE COMPOUNDS
20210040043 · 2021-02-11 ·

The present invention concerns new halogen substituted diketone compounds, new pyrazole compounds, processes for the manufacture of pyrazole compounds and processes for the manufacture of agrochemical or pharmaceutical compounds.

Method for producing a polymorphic form of 3-[5-amino-4-(3- cyanobenzoyl)-pyrazol-1-yl]-N-cyclopropyl-4-methylbenzamide

This invention relates to a process for the preparation of Form A of 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol-1-yl]-N-cyclopropyl-4-methylbenzamide. Also disclosed herein is Form A of 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol-1-yl]-N-cyclopropyl-4-methylbenzamide, or pharmaceutical compositions thereof, obtainable by the process described herein.

Method for producing a polymorphic form of 3-[5-amino-4-(3- cyanobenzoyl)-pyrazol-1-yl]-N-cyclopropyl-4-methylbenzamide

This invention relates to a process for the preparation of Form A of 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol-1-yl]-N-cyclopropyl-4-methylbenzamide. Also disclosed herein is Form A of 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol-1-yl]-N-cyclopropyl-4-methylbenzamide, or pharmaceutical compositions thereof, obtainable by the process described herein.

NOVEL COMPOUNDS

The present invention relates to compounds of formula (I), wherein Q is selected from O or S; R.sup.1 is a 5- or 6-membered heteroaryl group consisting of one or more carbon atoms, and one or more nitrogen and/or oxygen atoms, and substituted with a monovalent, optionally substituted cycloalkyl, cycloalkenyl or heterocyclic group, wherein the 5- or 6-membered heteroaryl group of R.sup.1 may optionally be further substituted; R.sup.2 is an ,-substituted cyclic group which may optionally be further substituted; R.sup.3 and R.sup.4 are each independently hydrogen, halogen, OH, NH.sub.2, CN, R.sup.5, OR.sup.5, NHR.sup.5 or N(R.sup.5).sub.2; or R.sup.3 and R.sup.4 together with the carbon atom to which they are attached may form a 3- to 7-membered saturated or unsaturated, optionally substituted cyclic group; and R.sup.5 is independently an optionally substituted C.sub.1-C.sub.4 alkyl group. 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 NLRP3.

##STR00001##

NOVEL COMPOUNDS
20210040065 · 2021-02-11 ·

The present invention relates to compounds of formula (I): comprising a 5-membered nitrogen-containing heteroaryl ring A, wherein the heteroaryl ring A is substituted with at least one group containing an oxygen atom, and wherein said oxygen atom is attached to the heteroaryl ring A via at least two other atoms. 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 NLRP3.

##STR00001##

NOVEL COMPOUNDS
20210040065 · 2021-02-11 ·

The present invention relates to compounds of formula (I): comprising a 5-membered nitrogen-containing heteroaryl ring A, wherein the heteroaryl ring A is substituted with at least one group containing an oxygen atom, and wherein said oxygen atom is attached to the heteroaryl ring A via at least two other atoms. 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 NLRP3.

##STR00001##

PYRAZOLE COMPOUNDS AND PREPARATION THEREOF

The present invention provides processes for preparation of substituted pyrazole compounds of formula II, that can be used as intermediates for preparation of substituted piperidine urea compounds useful for the treatment of dilated cardiomyopathy (DCM). R.sup.2 is independently selected from F, C1-C4 alkyl, C1-C4 haloalkyl, R.sup.3 is independently selected from H, F, C1-C4 alkyl, C1-C4 haloalkyl, R.sup.4 is C1-C4 alkyl, R.sup.6 is H or a protecting group and R.sup.7 is selected from H, CI or trialkylsilyl.

##STR00001##

PYRAZOLE COMPOUNDS AND PREPARATION THEREOF

The present invention provides processes for preparation of substituted pyrazole compounds of formula II, that can be used as intermediates for preparation of substituted piperidine urea compounds useful for the treatment of dilated cardiomyopathy (DCM). R.sup.2 is independently selected from F, C1-C4 alkyl, C1-C4 haloalkyl, R.sup.3 is independently selected from H, F, C1-C4 alkyl, C1-C4 haloalkyl, R.sup.4 is C1-C4 alkyl, R.sup.6 is H or a protecting group and R.sup.7 is selected from H, CI or trialkylsilyl.

##STR00001##

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.