IP Library › Granted Patent US 7,528,255
Granted Patent B2
US 7,528,255 · App. 10/071,248 · Granted May 5, 2009

Hydroxy, ω-carboxyaryl substituted diphenyl ureas and dirivatives thereof as raf kinase inhibitors

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Quick Facts
Patent No.
US 7,528,255
App. No.
10/071,248
Granted
May 5, 2009
Kind
B2
Abstract

The invention relates to the use of a group of aryl ureas in treating raf mediated diseases and pharmaceutical compositions for use in such therapy of the formula wherein, Y is NHR Hal is chlorine or bromine, R is H, CH 3 or CH 2 OH, and X 1 to X 7 are each, independently, H, OH or —OC(O)C 1 -C 4 alkyl, or a salt purified stereoisomer thereof, wherein at least one of X 1 to X 7 is OH or —OC(O)C 1 -C 4 alkyl.

Claims (34)

1. A compound of formula (Ia)

wherein,

Y is NHR,

Hal is chlorine or bromine,

R is H, CH 3 or CH 2 OH, and

X 1 to X 7 are each, independently, H, OH or —OC(O)C 1 -C 4 alkyl,

or a salt or purified stereoisomer thereof,

with the proviso that at least one of X 1 to X 7 is OH or —OC(O)C 1 -C 4 alkyl.

2. A compound of claim 1 wherein X 1 is OH or —OC(O)C 1 -C 4 alkyl.

3. A compound of claim 1 wherein X 2 is OH or —OC(O)C 1 -C 4 alkyl.

4. A compound of claim 1 wherein X 3 is OH or —OC(O)C 1 -C 4 alkyl.

5. A compound of claim 1 wherein X 4 is OH or —OC(O)C 1 -C 4 alkyl.

6. A compound of claim 1 wherein X 5 is OH or —OC(O)C 1 -C 4 alkyl.

7. A compound of claim 1 wherein X 6 is OH or —OC(O)C 1 -C 4 alkyl.

8. A compound of claim 1 wherein X 7 is OH or —OC(O)C 1 -C 4 alkyl.

9. A compound of claim 1 wherein Hal is chlorine.

10. A compound of claim 1 which is 4-{4-[({[4-chloro-3-(trifluoromethyl) phenyl]amino}carbonyl)amino]2-(hydroxy)phenoxy}-2-pyridine carboxamide.

11. A compound of claim 1 which is 4-{4-[({[4-chloro-3-(trifluoromethyl)phenyl]amino}carbonyl)amino]3-(hydroxy)phenoxy}-2-pyridine carboxamide.

12. A compound of claim 1 which is 4-{4-[({[4-chloro-3-(trifluoromethyl) phenyl]amino}carbonyl)amino]5-(hydroxy)phenoxy}-2-pyridine carboxamide.

13. A compound of claim 1 which is 4-{4-[({[4-chloro-3-(trifluoromethyl) phenyl]amino}carbonyl)amino]6-(hydroxy)phenoxy}-2-pyridine carboxamide.

14. A compound of formula (Ib)

wherein,

Y is NHR,

Hal is chlorine or bromine,

R is H, CH 3 or CH 2 OH, and

X 4 to X 7 are each, independently, H, OH or —OC(O)C 1 -C 4 alkyl,

or a salt or purified stereoisomer thereof,

with the proviso that at least one of X 4 to X 7 is OH or —OC(O)C 1 -C 4 alkyl.

15. A compound of formula (Ic)

wherein,

Hal is chlorine or bromine, and

X 1 to X 7 are each, independently, H, OH or —OC(O)C 1 -C 4 alkyl,

or a salt or purified stereoisomer thereof,

with the proviso that at least one of X 1 to X 7 is OH or —OC(O)C 1 -C 4 alkyl.