The disclosure relates to compounds that are, e.g., PAP Associated Domain Containing 5 (PAPD5) inhibitors and methods of use thereof.

Toll-like receptor 8 (TLR8)-specific inhibitors and methods of using the same in individuals having an autoimmune disease or an inflammatory disorder.

The present invention relates to a method for solubilizing 5-amino-2,3-dihydro-1,4-phthalazinedione or salts thereof, to the solubilisate produced by this method and respective uses in pharmaceutical dosage forms. A phosphatidylcholine-based solubilization method is disclosed.

The present invention relates to a method for solubilizing 5-amino-2,3-dihydro-1,4-phthalazinedione or salts thereof, to the solubilisate produced by this method and respective uses in pharmaceutical dosage forms. A phosphatidylcholine-based solubilization method is disclosed.

A compound of formula (Ia), (Ib) or (Ic) wherein: n is 1 or 2; R.sup.N is H or Me; R.sup.1 is optionally one or more halo or methyl groups; R.sup.2a and R.sup.2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH.sub.2OH; R.sup.2c and R.sup.2d (if present) are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH.sub.2OH; R.sup.3a and R.sup.3b are independently selected from H and Me; R.sup.4a is selected from OH, NH.sub.2, C(O)NH.sub.2, and CH.sub.2OH; R.sup.4b is either H or Me; X is either N or CH; R.sup.7 is selected from H and C.sub.1-4 alkyl; (a) one of R.sup.8a, R.sup.8b, R.sup.8c and R.sup.8d is selected from H, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, NHC.sub.1-4 alkyl; (b) another of R.sup.8a, R.sup.8b, R.sup.8c and R.sup.8d is selected from H, C.sub.1-4 alkyl, C.sub.1-4 fluoroalkyl, C.sub.3-6 cycloalkyl, C.sub.5-6 heteroaryl, C.sub.5-6 heteroaryl methyl, C.sub.4-6 heterocyclyl, C.sub.4-6 heterocyclyl methyl, phenyl, benzyl, halo, amido, amidomethyl, acylamido, acylamidomethyl, C.sub.1-4 alkyl ester, C.sub.1-4 alkyl ester methyl, C.sub.1-4 alkyl carbamoyl, C.sub.1-4 alkyl carbamoyl methyl, C.sub.1-4 alkylacyl, C.sub.1-4 alkylacyl methyl, phenylcarbonyl, carboxy, carboxymethyl, ether, amino, amino methyl, sulfonamido, sulfonamino, sulfone, sulfoxide, nitrile and nitrilemethyl; (c) the others of R.sup.8a, R.sup.8b, R.sup.8c and R.sup.8d are H. ##STR00001##

A compound of formula (Ia), (Ib) or (Ic) wherein: n is 1 or 2; R.sup.N is H or Me; R.sup.1 is optionally one or more halo or methyl groups; R.sup.2a and R.sup.2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH.sub.2OH; R.sup.2c and R.sup.2d (if present) are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH.sub.2OH; R.sup.3a and R.sup.3b are independently selected from H and Me; R.sup.4a is selected from OH, NH.sub.2, C(O)NH.sub.2, and CH.sub.2OH; R.sup.4b is either H or Me; X is either N or CH; R.sup.7 is selected from H and C.sub.1-4 alkyl; (a) one of R.sup.8a, R.sup.8b, R.sup.8c and R.sup.8d is selected from H, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, NHC.sub.1-4 alkyl; (b) another of R.sup.8a, R.sup.8b, R.sup.8c and R.sup.8d is selected from H, C.sub.1-4 alkyl, C.sub.1-4 fluoroalkyl, C.sub.3-6 cycloalkyl, C.sub.5-6 heteroaryl, C.sub.5-6 heteroaryl methyl, C.sub.4-6 heterocyclyl, C.sub.4-6 heterocyclyl methyl, phenyl, benzyl, halo, amido, amidomethyl, acylamido, acylamidomethyl, C.sub.1-4 alkyl ester, C.sub.1-4 alkyl ester methyl, C.sub.1-4 alkyl carbamoyl, C.sub.1-4 alkyl carbamoyl methyl, C.sub.1-4 alkylacyl, C.sub.1-4 alkylacyl methyl, phenylcarbonyl, carboxy, carboxymethyl, ether, amino, amino methyl, sulfonamido, sulfonamino, sulfone, sulfoxide, nitrile and nitrilemethyl; (c) the others of R.sup.8a, R.sup.8b, R.sup.8c and R.sup.8d are H. ##STR00001##

The present invention relates to compounds that inhibit Protein Arginine N-Methyl Transferase 5 (PRMT5) activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.

The present invention relates to compounds that inhibit Protein Arginine N-Methyl Transferase 5 (PRMT5) activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.

The present invention relates to compounds that inhibit Protein Arginine N-Methyl Transferase 5 (PRMT5) activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.

The present invention relates to compounds that inhibit Protein Arginine N-Methyl Transferase 5 (PRMT5) activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.