| 摘要 |
The invention relates to derivatives of 4-amino-quinazoline, having general formula (I) wherein: A, B = C<SUB>1-4</SUB>-alkylene which is optionally substituted; L = a single bond, C<SUB>1-2</SUB>-alkylene, -CH=CH- or -C=C-; groups C<SUB>1-2</SUB>-alkylene and -CH=CH- which are optionally substituted, or L = cycloprop-1,2-diyl; R = H, C<SUB>1-5</SUB>-alkyl, C<SUB>1-3</SUB>-fluoroalkyl, C<SUB>3-6</SUB>-cycloalkyl, -C(O)C<SUB>1-3</SUB>-alkyl, C<SUB>1-3</SUB>-alkylene-C<SUB>3-6</SUB>-cycloalkyl, -CH<SUB>2</SUB>-C=CH, C<SUB>2-4</SUB>-alkylene-NR<SUB>a</SUB>R<SUB>b</SUB>, C<SUB>1-3</SUB>-alkylene-X-C<SUB>1-3</SUB>-alkyl, in which X = O, SO<SUB>2</SUB>; R<SUB>1</SUB> = aryl or heteroaryl which are optionally substituted; R<SUB>2</SUB> and R<SUB>3</SUB> = H, C<SUB>1-3</SUB>-alkyl or C<SUB>1-3</SUB>-fluoroalkyl, or R<SUB>2</SUB> and R<SUB>3</SUB> together form a cycloprop-1,1-diyl; R<SUB>4</SUB> = H, C<SUB>1-5</SUB>-alkyl, C<SUB>1-3</SUB>- fluoroalkyl, C<SUB>1-5</SUB>-alkoxy, -SF<SUB>5</SUB>, C<SUB>1-3</SUB>-alkylene-X-C<SUB>1-3</SUB>-alkyl, in which X = O or SO<SUB>2</SUB>, C<SUB>1-5</SUB>-alkylene- NR<SUB>a</SUB>R<SUB>b</SUB>, an aryl or a heteroaryl which are optionally substituted; R<SUB>5</SUB> = H, halogen, C<SUB>1-5</SUB>-alkyl, C<SUB>1-3</SUB>-fluoroalkyl, C<SUB>1-5</SUB>-alkoxy, C<SUB>3-6</SUB>-cycloalkyl, C<SUB>1-3</SUB>-alkylene-C<SUB>3-6</SUB>-cycloalkyl, C<SUB>1-3</SUB>-alkylene-O-C<SUB>1-3</SUB>-alkyl, C<SUB>1-3</SUB>-alkylene-(OH), C<SUB>1-3</SUB>-alkylene-X-C<SUB>1-3</SUB>-alkyl, in which X = S, SO or SO<SUB>2</SUB>, or R<SUB>5</SUB> = -NR<SUB>a</SUB>R<SUB>b</SUB>, C<SUB>1-3</SUB>-alkylene-NR<SUB>a</SUB>R<SUB>b</SUB>, aryl, C<SUB>1-3</SUB>-alkylene-aryl, -O-aryl, C<SUB>1-3</SUB>-alkylene-O-aryl, C<SUB>1-3</SUB>-alkylene-O-C<SUB>1-3</SUB>-alkylene-aryl, heteroaryl or C<SUB>1-3</SUB>-alkylene-heteroaryl which are optionally substituted, or R<SUB>5</SUB> = heterocycle which is optionally substituted by C<SUB>1-3</SUB>-alkyl, -C(O)C<SUB>1-3</SUB>-alkyl, -C(O)C<SUB>1-3</SUB>-fluoroalkyl, C<SUB>1-3</SUB>-alkylene-C<SUB>3-6</SUB>-cycloalkyl, C<SUB>1-3</SUB>-alkylene-aryl, C<SUB>1-3</SUB>-alkylene-heteroaryl which are optionally substituted; R<SUB>7</SUB> = H, halogen, C<SUB>1-5</SUB>-alkyl, C<SUB>1-13</SUB>-fluoroalkyl, C<SUB>1-5</SUB>-alkoxy, -COOH, -C(O)O-C<SUB>1-3</SUB>-alkyl, C<SUB>1-3</SUB>-fluoroalkoxy, C<SUB>1-3</SUB>-alkylene-(OH), -NO<SUB>2</SUB>, -CN, -X-C<SUB>1-3</SUB>-alkyl, in which X represents S, SO or SO<SUB>2</SUB>, or R<SUB>7</SUB> = -NR<SUB>a</SUB>R<SUB>b</SUB>, C<SUB>1-3</SUB>-alkylene-NR<SUB>a</SUB>R<SUB>b</SUB>, -C(O)-NR<SUB>a</SUB>R<SUB>b</SUB>, -C(O)-C<SUB>1-3</SUB>-alkyl, aryl, -O-aryl or heteroaryl which are optionally substituted; in the form of a base, an acid addition salt, a hydrate or a solvate. The invention also relates to the method of preparing said derivatives and to the use of same in therapeutics. |
| 申请人 |
SANOFIS-AVENTIS;AUGEREAU, JEAN-MICHEL;COURTEMANCHE, GILLES;DESPEYROUX, PIERRE;GESLIN, MICHEL;THOMAS, ANNE |
发明人 |
AUGEREAU, JEAN-MICHEL;COURTEMANCHE, GILLES;DESPEYROUX, PIERRE;GESLIN, MICHEL;THOMAS, ANNE |
