C07C311/18

STAT3 dimerization inhibitors

The subject matter disclosed herein relates to compositions and methods of making and using the compositions. In a further aspect, the subject matter disclosed herein relates to inhibitors of STAT3 dimerization. Methods of making these compositions as well as compositions comprising these compositions are also disclosed. Also disclosed are methods of treating or preventing certain cancers by administering to an individual in need thereof and effective amount of the compounds disclosed herein. Still further, disclosed herein are methods of inhibiting STAT3 by contacting a cell with a compound or composition as disclosed herein.

Sulfamoyl-arylamides and the use thereof as medicaments for the treatment of hepatitis B

Inhibitors of HBV replication of Formula (I) ##STR00001##
including stereochemically isomeric forms, salts, hydrates and solvates thereof, wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.

Sulfamoyl-arylamides and the use thereof as medicaments for the treatment of hepatitis B

Inhibitors of HBV replication of Formula (I) ##STR00001##
including stereochemically isomeric forms, salts, hydrates and solvates thereof, wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.

Preparation of sulfonamide-containing antimicrobials and substrate treating compositions of sulfonamide-containing antimicrobials

A quaternary ammonium sulfonamide compound of formula (I): wherein R=(II), C.sub.1-C.sub.3 linear or branched alkyl, R.sub.1 and R.sub.2 are the same or different and selected from C.sub.1 to C.sub.18 linear or branched alkyl, R.sub.3 and R.sub.4 are the same or different and selected from C.sub.1 to C.sub.4 linear or branched alkyl, CF.sub.3, OR.sub.5 where R.sub.5 is C.sub.1 to C.sub.8 linear or branched alkyl or polyethylene oxide, l is 1, 2, 3, 4, 5, 6, 7 or 8, m is 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16 or 17, n is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17 or 18, wherein the aryl groups of R may be substituted or unsubstituted, X=halogen, and Y=(III) wherein R.sub.6, R.sub.7, R.sub.8, R.sub.9 and R.sub.10 are the same or different and selected from C.sub.1 to C.sub.6 linear or branched alkyl and the benzophenone is selected from the group consisting of substituted benzophenone and unsubstituted benzophenone, process for preparing the compound and antimicrobial surface coating compositions of the compound. ##STR00001##

Preparation of sulfonamide-containing antimicrobials and substrate treating compositions of sulfonamide-containing antimicrobials

A quaternary ammonium sulfonamide compound of formula (I): wherein R=(II), C.sub.1-C.sub.3 linear or branched alkyl, R.sub.1 and R.sub.2 are the same or different and selected from C.sub.1 to C.sub.18 linear or branched alkyl, R.sub.3 and R.sub.4 are the same or different and selected from C.sub.1 to C.sub.4 linear or branched alkyl, CF.sub.3, OR.sub.5 where R.sub.5 is C.sub.1 to C.sub.8 linear or branched alkyl or polyethylene oxide, l is 1, 2, 3, 4, 5, 6, 7 or 8, m is 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16 or 17, n is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17 or 18, wherein the aryl groups of R may be substituted or unsubstituted, X=halogen, and Y=(III) wherein R.sub.6, R.sub.7, R.sub.8, R.sub.9 and R.sub.10 are the same or different and selected from C.sub.1 to C.sub.6 linear or branched alkyl and the benzophenone is selected from the group consisting of substituted benzophenone and unsubstituted benzophenone, process for preparing the compound and antimicrobial surface coating compositions of the compound. ##STR00001##

Cannabinoid receptor CB2 ligand 4-(aminomethyl)-N, N-dialkylanilines

Disclosed herein are novel cannabionid receptor-2 (CB2) agonists and inverse agonists represented by Formula (I), and method of modulating the activity of CB2 by contacting the CB-2 receptor with a compound of Formula (I). Also, disclosed are methods for treating multiple myeloma or osteoporosis in a mammal in need thereof by modulating the activity of a cannabinoid receptor-2 (CB2).

Cannabinoid receptor CB2 ligand 4-(aminomethyl)-N, N-dialkylanilines

Disclosed herein are novel cannabionid receptor-2 (CB2) agonists and inverse agonists represented by Formula (I), and method of modulating the activity of CB2 by contacting the CB-2 receptor with a compound of Formula (I). Also, disclosed are methods for treating multiple myeloma or osteoporosis in a mammal in need thereof by modulating the activity of a cannabinoid receptor-2 (CB2).

IONIC METAL ALKYLIDENE COMPOUNDS AND USE THEREOF IN OLEFINIC METATHESIS REACTIONS

A compound of formula (I) wherein: M is selected from Mo or W; X is selected from O or NR.sup.5; R.sup.1 and R.sup.2 are independently selected from H, C.sub.1-6 alkyl, and aryl; C.sub.1-6 alkyl and aryl optionally being substituted with one or more of C.sub.1-6 alkyl, C.sub.1-6 alkoxy, and OC.sub.6H.sub.5; R.sup.3 is selected from a nitrogen-containing aromatic heterocycle being bound to M via said nitrogen; and from halogen; R.sup.4 is an aryl oxy group being bound to M via said oxygen of said aryl oxy group; wherein said aryl group Ar of said aryl oxy group is bound to a group Cat such to form a cationic ligand Cat.sup.+-ZArO, wherein Z is either a covalent bond or a linker; R.sup.5 is alkyl or aryl, optionally substituted.

##STR00001##

IONIC METAL ALKYLIDENE COMPOUNDS AND USE THEREOF IN OLEFINIC METATHESIS REACTIONS

A compound of formula (I) wherein: M is selected from Mo or W; X is selected from O or NR.sup.5; R.sup.1 and R.sup.2 are independently selected from H, C.sub.1-6 alkyl, and aryl; C.sub.1-6 alkyl and aryl optionally being substituted with one or more of C.sub.1-6 alkyl, C.sub.1-6 alkoxy, and OC.sub.6H.sub.5; R.sup.3 is selected from a nitrogen-containing aromatic heterocycle being bound to M via said nitrogen; and from halogen; R.sup.4 is an aryl oxy group being bound to M via said oxygen of said aryl oxy group; wherein said aryl group Ar of said aryl oxy group is bound to a group Cat such to form a cationic ligand Cat.sup.+-ZArO, wherein Z is either a covalent bond or a linker; R.sup.5 is alkyl or aryl, optionally substituted.

##STR00001##

BUMETANIDE DERIVATIVES FOR THE THERAPY OF HYPERHIDROSIS
20210022978 · 2021-01-28 ·

The present invention relates to bumetanide derivatives of formula (I) as well as pharmaceutical compositions comprising these compounds for use in the treatment or prevention of diseases/disorders involving Na.sup.+K.sup.+2Cl.sup.-cotransporters (NKCCs), and particularly for use in the treatment or prevention of hyperhidrosis.

##STR00001##