Selective angiotensin ii receptor ligands
AssigneeVicore Pharma AB
InventorsTomas Fex, Bengt Ohlsson
Life of this patent
Estimating the term…
Abstract
There is provided pharmaceutical compounds of formula I, wherein R1, R2, R3, R4, R5, R6, Y1, Y2, Y3 and Y4 have meanings given in the description, which compounds are useful in the treatment of autoimmune and/or fibrotic diseases, including interstitial lung diseases, such as idiopathic pulmonary fibrosis and sarcoidosis.
Claims21
A compound of formula I,
- wherein:
- R1 represents C1-4 alkyl, optionally substituted by one or more fluorine atoms and/or with OR7;
- R2 and R3 each independently represent H or C1-6 alkyl, optionally substituted by one or more halogen atoms;
- Y1, Y2, Y3 and Y4 independently represent —CH—, —CF— or —N—;
- R4 represents C1-7 alkyl, C1-6 alkoxy, C1-6 alkoxy-C3-6 alkyl, each of which alkyl group is substituted, and/or terminated, by at least one —OH group, and which are optionally substituted with one or more halogen atoms;
- R5 represents H or C1-6 alkyl, optionally substituted by one or more halogen atoms;
- R6 represents C2-4 alkyl, optionally substituted by one or more halogen atoms;
- and
- R7 represents H, or methyl optionally substituted by one or more fluorine atoms,
- or a pharmaceutically-acceptable salt thereof.
A compound as claimed in any one of the preceding claims, wherein R4 represents ethyl, n-propyl, n-butyl, isobutyl or methylcyclohexyl, each of which is substituted and/or terminated by one —OH group.
A compound as claimed in any one of the preceding claims, wherein R5 represents H, methyl, ethyl, n-propyl, n-butyl or isobutyl.
A compound as claimed in any one of the preceding claims, wherein R6 represents n-propyl, n-butyl or isobutyl.
A compound as claimed in any one of the preceding claims, wherein R7 represents H.
A compound s claimed in any one of the preceding claims, wherein Y1 represents —CH— or —CF—;
- Y2 represents —CH or —CF—;
- Y3 represents —CH—;
- and Y4 represents —CH—.
A compound as claimed in any one of the preceding claims, which is:
- 1-[[3-[3-fluoro-4-[(2-methylimidazol-1-yi)methyl]phenyl]-5-isobutyl-2-thienyl]sulfonyl]-3-(2-hydroxyethyl)urea,
- 1-[[3-[3-fluoro-4-[(2-methylimidazol-1-yl)methyl]phenyl]-5-isobutyl-2-thienyl]sulfonyl]-3-(3-hydroxypropyl)urea,
- 1-[[3-[3-fluoro-4-[(2-methylimidazol-1-yl)methyl]phenyl]-5-isobutyl-2-thienyl]sulfonyl]-3-(2-hydroxy-2-methyl-propyl)urea,
- 1-[[3-[2-fluoro-4-[(2-methylimidazol-1-yl)methyl]phenyl]-5-isobutyl-2-thienyl]sulfonyl]-3-(2-hydroxyethyl)urea, or
- 1-[[3-[3,5-difluoro-4-[(2-methylimidazol-1-yl)methyl]phenyl]-5-isobutyl-2-thienyl]sulfonyl]-3-(2-hydroxyethyl)urea,
- 1-[[3-[4-[(2-tert-butylimidazol-1-yl)methy]-3-fluoro-phenyl]-5-isobutyl-2-thienyl]sulfonyl]-3-(2-hydroxyethylurea,
- 1-[[3-[4-[(2-tert-butylimidazol-1-yl)methyl]-3-fluoro-phenyl]-5-isobutyl-2-thienyl]sulfonyl]-3-(2-hydroxy-2-methyl-propyl)urea,
- 1-[[3-[4-[(2-ethylimidazol-1-yl)methyl]-3-fluoro-phenyl]-5-isobutyl-2-thienyl]sulfonyl]-3-(2-hydroxyethyl)urea,
- 1-[[3-[4-[(2-ethylimidazol-1-yl)methyl]-3-fluoro-phenyl]-5-isobutyl-2-thienyl]sulfonyl]-3-[(1-hydroxycyclohexyl)methyl]urea,
- 1-[[3-[3-fluoro-4-[(2-isopropylimidazol-1-yl)methyl]phenyl]-5-isobutyl-2-thienyl]sulfonyl]-3-(2-hydroxyethyl)urea.
Dependencies are inferred from the claim text.