Heterocycle-substituted Pyridyl Benzothiophenes as Kinase Inhibitors
AssigneeAllergan, Inc.
InventorsSougato Boral, Thomas C. Malone, Shimiao Wang, Sandhya Rao, Rong Yang
Life of this patent
Estimating the term…
Abstract
This invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and X are as defined herein. The compounds of Formula I are useful as receptor tyrosine kinase (RTK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders and metabolic diseases.
Claims9
A compound represented by Formula I, its enantiomers, diastereoisomers, or a pharmaceutically acceptable salt thereof:
- wherein:
- R1 is hydrogen;
- X is
- R2 is benzothiophene;
- R3 is phenyl, optionally substituted with methyl, trifluoromethyl, fluoro, or chloro;
- R4 is hydrogen or C1-C8 alkyl optionally substituted with hydroxyl;
- and.
-8. (canceled)
A compound selected from the group consisting of:
- 1-{2-[2-amino-5-(2H-tetrazol-5-yl)pyridin-3-yl]-1-benzothien-5-yl}-3-[4-chloro-3-(trifluoromethyl)phenyl]urea;
- 1-(2-{2-amino-5-[2-(3-hydroxypropyl)-2H-tetrazol-5-yl]pyridin-3-yl}-1-benzothien-5-yl)-3-[4-chloro-3-(trifluoromethyl)phenyl]urea;
- 1-(2-{2-amino-5-[2-(3-hydroxypropyl)-2H-tetrazol-5-yl]pyridin-3-yl}-1-benzothien-5-yl)-3-[4-fluoro-3-(trifluoromethyl)phenyl]urea;
- 1-(2-{2-amino-5-[2-(3-hydroxypropyl)-2H-tetrazol-5-yl]pyridin-3-yl}-1-benzothien-5-yl)-3-[3-fluoro-5-(trifluoromethyl)phenyl]urea;
- 1-(2-{2-amino-5-[2-(3-hydroxypropyl)-2H-tetrazol-5-yl]pyridin-3-yl}-1-benzothien-5-yl)-3-[3,5-bis(trifluoromethyl)phenyl]urea;
- and
- 1-(2-{2-amino-5-[2-(2-hydroxyethyl)-2H-tetrazol-5-yl]pyridin-3-yl}-1-benzothien-5-yl)-3-[4-chloro-3-(trifluoromethyl)phenyl]urea;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.