US 10,703,723 B2Granted

Prodrugs of sulfasalazine, pharmaceutical compositions thereof and their use in the treatment of autoimmune disease

AssigneeTruly Translational Sweden AB

InventorsMarguérite Mascha Mensonides-Harsema, Charlott Brunmark, Karin von Wachenfeldt

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Abstract

The present invention relates to new compounds of formula I and pharmaceutically acceptable salts and/or co-crystals thereof. The present invention also relates to pharmaceutical compositions comprising these compounds and to their use as medicaments for the prevention, prophylaxis of progression, and/or treatment of a disease in which modulation of extracellular (chemotactic) cytokines and/or TNF-alpha and or nuclear factor kappa B (NFKB) and/or inflammatory cells is beneficial, such as autoimmune diseases, like rheumatoid arthritis, oligoarthritis, spondyloarthropathy, psoriatic arthritis, psoriasis and inflammatory bowel diseases, such as Crohns' disease and ulcerative colitis.

Claims20

Dependent claims

A compound of formula I, a pharmaceutically acceptable salt, crystals and/or co-crystal thereof, diastereomer, enantiomer, or mixture thereof, wherein:

R1 and R2 are independently chosen from hydrogen and C1-6alkyl, R3 and R4 are independently chosen from hydrogen, C1-6alkyl, C1-6heteroalkyl, C3-12cycloalkyl, C3-12heterocycloalkyl, C5-13aryl, C5-13heteroraryl, C3-12cycloalkylC1-6alkyl, C3-12heterocycloalkylC1-6alkyl, C5-13arylC1-6alkyl and C5-13heteroarylC1-6alkyl, or R3 and R4 together with the nitrogen to which they are attached form a ring chosen from C3-12heterocycloalkyl and C5-13heteroaryl, and wherein R1, R2, R3 and R4 are optionally substituted with one or more R, and R is independently chosen from halogen, —OH, —SH, —CN, —CF3, ═O, —NO2, —C(O)NR5R6, —R5, —OR5, —SR5, —C(O)R5, —COOR5 and —NR5R6, wherein R5 and R6 are independently chosen from hydrogen, C1-4alkyl and C1-4cycloalkyl, and optionally substituted with one or more R7, wherein R7 is chosen from halogen, —OH, —SH, —CN, —CF3, ═O, —NO2, —C(O)NR8R9, —R8, —OR8, —SR8, —C(O)R8, —COOR8 and —NR8R9, wherein R8 and R9 are independently chosen from hydrogen, C1-4alkyl and C1-4cycloalkyl.

Dependencies are inferred from the claim text.