Patent classifications
C07D249/04
FUNCTIONALIZED 1,3-BENZENE DIOLS AND THEIR METHOD OF USE FOR THE TREATMENT OF RADIATION DERMATITIS AND OTHER SKIN DISORDERS
Methods, compounds and compositions for treating and preventing dermatological disorders and ocular irritancy are disclosed. The compounds and compositions comprise a functionalized 1,3-benzene diol, such as 5-(2-(1H-1,2,3-triazol-1-yl)ethyl)-2-((1R,6R)-3-methyl-6-(prop-1-en-2-yl)cyclohex-2-enyl)benzene-1,3-diol and ethyl 3-(3,5-dihydroxy-4-((1R,6R)-3-methyl-6-(prop-1-en-2-yl)cyclohex-2-enyl)benzyl)azetidine-1-carboxylate.
SUBSTITUTED HETEROCYCLIC COMPOUNDS
There are disclosed compounds of the following formula I:
##STR00001##
or a stereoisomer or pharmaceutically acceptable salt thereof, wherein all substituents are as defined herein, which are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition. The compounds of the invention may be useful for treating neurodegenerative diseases or disorders.
SUBSTITUTED HETEROCYCLIC COMPOUNDS
There are disclosed compounds of the following formula I:
##STR00001##
or a stereoisomer or pharmaceutically acceptable salt thereof, wherein all substituents are as defined herein, which are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition. The compounds of the invention may be useful for treating neurodegenerative diseases or disorders.
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 α,α′-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##
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 α,α′-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##
Analogs of proxisome proliferator activated receptor (PPAR) agonists and methods of using the same
Peroxisome proliferator activated receptor (PPAR) compounds, and methods of using the same for treating bone fractures, treating osteoporosis and/or metabolic bone diseases, and inducing osteogenesis and/or chondrogenesis, are disclosed.
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##
Sulphonyl urea derivatives as NLRP3 inflammasome modulators
The present disclosure relates to compounds of Formula (I): ##STR00001##
and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.
Sulphonyl urea derivatives as NLRP3 inflammasome modulators
The present disclosure relates to compounds of Formula (I): ##STR00001##
and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.
PROCESS FOR PREPARING A COT INHIBITOR COMPOUND
Disclosed are syntheses of a Cot (cancer Osaka thyroid) inhibitor, which has the following formula:
##STR00001##