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Last Updated: April 25, 2024

Details for Patent: 9,040,548


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Title:Quinazoline derivatives as VEGF inhibitors
Abstract: The invention relates to quinazoline derivatives of formula (I), ##STR00001## wherein m is an integer from 1 to 3; R.sup.1 represents halogeno or C.sub.1-3alkyl; X.sup.1 represents --O--; R.sup.2 is selected from one of the following three groups: 1) C.sub.1-5alkylR.sup.3, wherein R.sup.3 is piperidinyl-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C.sub.1-4alkyl, C.sub.1-4hydroxyalkyl and C.sub.1-4alkoxy; 2) C.sub.2-5alkenylR.sup.3, wherein R.sup.3 is as defined herein; 3) C.sub.2-5alkynylR.sup.3, wherein R.sup.3 is as defined herein; and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof; processes for their preparation; pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.
Inventor(s): Thomas; Andrew Peter (Cheshire, GB), Stokes; Elaine Sophie Elizabeth (Cheshire, GB), Hennequin; Laurent Francois Andre (Reims Cedex 2, FR)
Assignee: AstraZeneca AB (Sodertalje, SE)
Filing Date:Jan 03, 2014
Application Number:14/146,954
Claims:1. A method of treating breast cancer in a warm-blooded animal in need of such treatment which comprises administering to the animal an effective amount of 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-yl- methoxy)quinazoline or a pharmaceutically acceptable salt thereof.

2. The method as claimed in claim 1, wherein the warm-blooded animal is a human.

3. A method of treating lung cancer in a warm-blooded animal in need of such treatment which comprises administering to the animal an effective amount of 1 to 50 mg/kg of 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)qu- inazoline or a pharmaceutically acceptable salt thereof.

4. The method as claimed in claim 3, wherein the warm-blooded animal is a human.

5. A method of treating prostate cancer in a warm-blooded animal in need of such treatment which comprises administering to the animal an effective amount of 1 to 50 mg/kg of 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)qu- inazoline or a pharmaceutically acceptable salt thereof.

6. The method as claimed in claim 5, wherein the warm-blooded animal is a human.

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