IP Library › Granted Patent US 8,618,141
Granted Patent B2
US 8,618,141 · App. 13/551,884 · Granted Dec 31, 2013

Aryl ureas with angiogenesis inhibiting activity

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Quick Facts
Patent No.
US 8,618,141
App. No.
13/551,884
Granted
Dec 31, 2013
Kind
B2
Abstract

This invention relates to methods of using aryl ureas to treat diseases mediated by the VEGF induced signal transduction pathway characterized by abnormal angiogenesis or hyperpermeability processes.

Claims (11)

1. A method of blocking tumor angiogenesis in a human or other mammal comprising administering to a human or other mammal with a tumor of the breast, gastrointestinal tract, kidney, ovary or cervix, an effective amount of the compound N-(4-chloro-3-(trifluoromethyl)phenyl)-N′-(4-(2-(N-methylcarbamoyl)-4-pyridyloxy)phenyl)urea of the formula below or a pharmaceutically acceptable salt thereof

2. A method as in claim 1 wherein the compound N-(4-chloro-3-(trifluoromethyl)phenyl)-N′-(4-(2-(N-methylcarbamoyl)-4-pyridyloxy)phenyl)urea or a pharmaceutically acceptable salt thereof is administered simultaneously with another angiogenesis inhibiting agent to a human or other mammal with a tumor of the breast, gastrointestinal tract, kidney, ovary or cervix in the same formulation or in separate formulations.

3. A method as in claim 1 wherein the tumor that is treated is characterized by abnormal angiogenesis or hyperpermiability processes, which are mediated by KDR (VEGFR-2).

4. A method as in claim 1 wherein the tumor that is treated is characterized by abnormal angiogenesis or hyperpermiability processes, which are not raf-mediated.

5. A method as in claim 4 wherein the tumor that is treated is characterized by abnormal angiogenesis or hyperpermiability processes, which are not p38-mediated.

6. A method of blocking tumor angiogenesis in a human or other mammal comprising administering to a human or other mammal with a tumor of the breast, gastrointestinal tract, kidney, ovary or cervix, an effective amount of the compound N-(4-chloro-3-(trifluoromethyl)phenyl)-N′-(4-(2-(N-methylcarbamoyl)-4-pyridyloxy)phenyl)urea tosylate.

7. A method of blocking angiogenesis in a tumor of the kidney comprising administering to a human or other mammal with a tumor of the kidney an effective amount of the tosylate salt of N-(4-chloro-3-(trifluoromethyl)phenyl)-N′-(4-(2-(N-methylcarbamoyl)-4-pyridyloxy)phenyl)urea of the formula below

8. A method as in claim 7 wherein the tumor of the kidney that is treated is characterized by abnormal angiogenesis or hyperpermiability processes, which are not raf-mediated nor p38-mediated.

9. A method as in claim 8 wherein the tumor of the kidney that is treated is characterized by abnormal angiogenesis or hyperpermiability processes, which are mediated by KDR (VEGFR-2).

10. The method of claim 6 , wherein the effective amount of the compound N-(4-chloro-3-(trifluoromethyl)phenyl)-N′-(4-(2-(N-methylcarbamoyl)-4-pyridyloxy)phenyl)urea tosylate is between 0.01 to 200 mg/Kg of total body weight.

11. The method of claim 7 , wherein the effective amount of the compound N-(4-chloro-3-(trifluoromethyl)phenyl)-N′-(4-(2-(N-methylcarbamoyl)-4-pyridyloxy)phenyl)urea of the formula below is between 0.01 to 200 mg/Kg of total body weight