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US 6,387,912 B1Granted
Utilization of pyrimidine derivatives for preventing and treating cerebral ischaemia
AssigneeBASF SE
InventorsGerd Steiner, Kurt Schellhaas, Wilfried Lubisch, Uta Holzenkamp, Dorothea Starck, Monika Knopp, Laszlo Szabo, Franz Emling, Francisco Javier Garcia-Ladona, Hans-Peter Hofmann, Liliane Unger
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Abstract
Use of pyrimidine derivatives of the formula I where the substituents are as defined in the description, and of their physiologically tolerated salts for producing medicaments for the prophylaxis and treatment of cerebral ischemia and strokes.
Claims1
A method of preventing or treating cerebral ischemia or strokes in a mammal in need of such treatment comprising administering to said mammal an effective amount of pyrimidine derivatives of the formula I
- where
- A is NH or oxygen,
- B is hydrogen or methyl,
- C is hydrogen, methyl or hydroxyl,
- D is methyl,
- E is
- D and E are together —CH2—CH2—NR1—CH2—, —CH2—NR1—CH2— or —CH2—NR1—CH2—CH2—,
- X is nitrogen,
- Y is CH2, CH2—CH2, CH2—CH2CH2 or CH2—CH,
- Z is nitrogen, carbon or CH, with it also being possible for the bond between Y and Z to be a double bond, n is the number 2, 3, or 4,
- R1 is hydrogen, a C1-C4-alkyl group, an acetyl or benzoyl group, a phenylalkyl C1-C4 radical or phenylalkoxy C2-C5 radical, with the aromatic moiety optionally being substituted by halogen, or C1-C4-alkyl, trifluoromethyl, hydroxyl, C1-C4-alkoxy, amino, cyano or nitro groups, a naphthylalkyl C1-C3 radical, a phenylalkanone C2-C4 radical or a phenyl- or pyridylcarbamoylalkyl C2 radical, with it being possible for the phenyl or pyridyl group to be substituted by halogen, a C1-C3-alkyl group, a methoxy group and by a nitro or amino group,
- R2 is a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which is optionally monosubstituted, disubstituted or trisubstituted by halogen atoms, C1-C4-alkyl or trifluoromethyl, trifluoromethoxy, hydroxyl, C1-C4-alkoxy, amino, monomethylamino, dimethylamino, cyano, thiomethyl or nitro groups and which can optionally be fused to a benzene nucleus which can optionally be monosubstituted or disubstituted by halogen atoms, C1-C4-alkyl or hydroxyl, trifluoromethyl, C1-C4-alkoxy, amino, cyano or nitro groups and which can optionally contain 1 nitrogen atom, or to a 5- or 6-membered ring which can contain 1-2 oxygen atoms, or can be substituted by a phenyl-C1-C2-alkyl- or -alkoxy group, with it being possible for the phenyl radical to be substituted by halogen, or a methyl, trifluoromethyl or methoxy group,
- R3 and R4 are, independently of each other, hydrogen or a C1-C4-alkyl group, or their physiologically tolerated salts.
10 more elements
Dependencies are inferred from the claim text.