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Details for Patent: 5,543,520

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Details for Patent: 5,543,520

Title: Pyrimidine derivatives
Abstract:There are disclosed N-(fluoroalkoxyphenyl)-2-pyrimidine-amine derivatives of formula I ##STR1## wherein R.sub.1 is isoquinolinyl, thienyl or 1H-pyrrolyl, and R.sub.2 is fluoro-substituted alkoxy containing up to 2 carbon atoms. These compounds can be used, inter alia, for the therapy of tumoral diseases.
Inventor(s): Zimmermann; J urg (Wallbach, CH)
Assignee: Ciba-Geigy Corporation (Tarrytown, NY)
Filing Date:Sep 15, 1994
Application Number:08/306,333
Claims:1. A N-(fluoroalkoxyphenyl)-2-pyrimidine-amine derivative of formula I ##STR7## wherein R.sub.1 is isoquinolinyl or 1H-pyrrolyl, it being possible for each of these two radicals to be bonded to the pyrimidine moiety via any one of its ring atoms, or R.sub.1 is 2-thienyl or 3-thienyl, and R.sub.2 is fluoro-substituted alkoxy containing up to 2 carbon atoms, or a salt of such a compound containing a salt-forming group.

2. A compound of formula I according to claim 1, wherein R.sub.2 is trifluoromethoxy or 1,1,2,2-tetrafluoroethoxy, or a salt of such a compound containing a salt-forming group.

3. A compound of formula I according to claim 1, wherein R.sub.1 is 4-isoquinolinyl, 2- or 3-thienyl or 1H-pyrrol-2-yl, and R.sub.2 is trifluoromethoxy or 1,1,2,2-tetrafluoroethoxy, or a salt of such a compound containing a salt-forming group.

4. A compound of formula I according to claim 1, wherein R.sub.2 is 1,1,2,2-tetrafluoroethoxy, or a pharmaceutically acceptable salt thereof containing a salt-forming group.

5. A compound of formula I according to claim 3, wherein R.sub.2 is 1,1,2,2-tetrafluoroethoxy, or a pharmaceutically acceptable salt thereof containing a salt-forming group.

6. N-[3-(1,1,2,2-tetrafluoroethox y)phenyl]-4-(4-isoquinolyl)-2-pyrimidine-amine or a pharmaceutically acceptable salt thereof as claimed in claim 1.

7. A compound of formula I according to claim 1 selected from N-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-(1H-pyrrol-2-yl)-2-pyrimidine-amin e, N-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-4-(2-thienyl)-2-pyrimidine-amine, N-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-4-(3-thienyl)-2-pyrimidine-amine.
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