Selective angiotensin ii receptor ligands
AssigneeVicore Pharma AB
InventorsTomas Fex, Bengt Ohlsson, Anders Hallberg, Mats Larhed
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.
Claims22
A compound of formula I,
- wherein:
- R1 represents C1-2 alkyl (optionally substituted by one or more fluorine atoms), OR7 or a fluorine atom;
- 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 C1-6 alkyl, C1-6 alkoxy, C1-6 alkoxy-CA-6 alkyl, the alkyl part of which are optionally substituted by one or more halogen atoms, or
- R4 represents aryl, C1-6 alkylaryl, C1-3 alkenylaryl, heteroaryl, C1-6 alkylheteroaryl or C1-3 alkenylheteroaryl, each of which are optionally substituted by one or more substituents selected from halogen, —CF3, CF3O—, C1-6 alkyl, and C1-6 alkoxy;
- R5 represents H or C1-6 alkyl, each of which is optionally substituted by one or more halogen atoms;
- R6 represents C2-4 alkyl, optionally substituted by one or more halogens;
- 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 R2 and R3 both represent H.
A compound as claimed in any one of the preceding claims, wherein R4 represents C1-4 alkyl or C1-4 alkoxy-C1-4 alkyl group, phenyl;
- C1-3 alkylaryl;
- or C1-3 alkylheteroaryl, each of which is optionally substituted by one or more halogen atoms.
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 or methyl.
A compound as claimed in any one of the preceding claims, wherein Y1 represents —CF— or —CH and Y2, Y3 and Y4 all represent —CH—.
A compound as claimed in any one of the preceding claims, which is:
- furan-2-ylmethyl-3-[[5-isobutyl-3-[4-[(2-tert-butyl-imidazol-1-yl)methyl]phenyl]-2-thienyl]sulfonyl]urea,
- thiophen-2-ylmethyl-3-[[5-isobutyl-3-[4-[(2-tert-butyl-imidazol-1-yl)methyl]phenyl]-2-thienyl]sulfonylurea,
- 2-methoxyethyl-3-[[5-isobutyl-3-[4-[(2-tert-butyl-imidazol-1-yl)methyl]phenyl]-2-thienyl]sulfonylurea,
- pyridin-2-ylmethyl-3-[[5-isobutyl-3-[4-[(2-tert-butyl-imidazol-1-yl)methyl]phenyl]-2-thienyl]sulfonylurea,
- 1-[[3-[4-[(2-tert-butylimidazol-1-yl)methyl]-3-fluoro-phenyl]-5-isobutyl-2-thienyl]sulfonyl]-3-(2-pyridylmethyl)urea,
- 1-[[3-[4-[(2-tert-butylimidazol-1-yl)methyl]-3-fluoro-phenyl]-5-isobutyl-2-thienyl]sulfonyl]-3-ethyl-urea, or
- 1-[[3-[4-[(2-tert-butylimidazol-1-yl)methyl]-3-fluoro-phenyl]-5-isobutyl-2-thienyl]sulfonyl]-3-(2-thienylmethyl)urea.
A compound as defined in any one of the preceding claims, for use as a pharmaceutical.
Dependencies are inferred from the claim text.