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Last Updated: October 23, 2021

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Claims for Patent: 6,958,335


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Summary for Patent: 6,958,335
Title: Treatment of gastrointestinal stromal tumors
Abstract:4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2- ylamino)phenyl]-benzamide of the formula I ##STR1## or a pharmaceutically acceptable salt thereof can be used in the treatment of gastrointestinal stromal tumours.
Inventor(s): Buchdunger; Elisabeth (Neuenburg, DE), Capdeville; Renaud (Riedesheim, FR), Demetri; George Daniel (Brookline, MA), Dimitrijevic; Sasa (Habsheim, FR), Druker; Brian Jay (Portland, OR), Fletcher; Jonathan A. (Brookline, MA), Heinrich; Michael C. (Lake Oswego, OR), Joensuu; Heikki (Helsinki, FI), Silberman; Sandra Leta (Randolph, NJ), Tuveson; David (Berwyn, PA)
Assignee: Novartis AG (Basel, CH) Dana-Farber Cancer Institute, Inc. (Boston, MA) Oregon Health & Science University (Portland, OR)
Application Number:10/415,015
Patent Claims: 1. A method of treating gastrointestinal stromal tumours which comprises administering to a human in need of such treatment a dose, effective against gastrointestinal stromal tumours, of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2 -ylamino)phenyl]-benzamide of the formula I ##STR3##

or a pharmaceutically acceptable salt thereof.

2. The method according to claim 1 wherein a pharmaceutically acceptable acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2 -yl-amino)phenyl]-benzamide of the formula I is administered.

3. The method according to claim 1 wherein a methanesulfonate salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2 -ylamino)phenyl]-benzamide of the formula I is administered.

4. The method according to claim 1 wherein a daily dose of 200 to 600 mg of a monomethanesulfonate salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2 -ylamino)phenyl]-benzamide of the formula I is administered to an adult human.

5. A method for administering to a human subject having gastrointestinal stromal tumours 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyrimidin-3-yl)pyrimidin -2-ylamino)phenyl]-benzamide of the formula I ##STR4##

or a pharmaceutically acceptable salt thereof, which comprises administering a pharmaceutically effective amount of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2 -ylamino)phenyl]-benzamide of the formula I or a pharmaceutically acceptable salt thereof to the human subject once daily for a period exceeding 3 months.

6. A method according to claim 5 wherein a daily dose of 200 to 600 mg of monomethanesulfonate salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2 -ylamino)phenyl]-benzamide of the formula I is administered.

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