摘要 |
Quinazoline derivatives have the formula: or the pharmaceutically acceptable salts thereof; wherein each of Z<SUP>5</SUP>, Z<SUP>6</SUP>, Z<SUP>7 </SUP>and Z<SUP>8 </SUP>is N or CH and wherein one or two Z<SUP>5</SUP>, Z<SUP>6</SUP>, Z<SUP>7 </SUP>and Z<SUP>8 </SUP>are N and wherein two adjacent Z positions cannot be N; wherein m and n are each independently 0-3; wherein R<SUP>1 </SUP>is independently OH, SH, NH<SUB>2</SUB>, OR, SR, NHR, halo or R-halide; wherein two adjacent R<SUP>1 </SUP>groups may be joined to form an aliphatic hetero cycle ring of 5-6 members; wherein R<SUP>2 </SUP>is independently R, halo, R-halide, OR-halide, NH<SUB>2</SUB>, CONH<SUB>2 </SUB>or CONHR; wherein R is optionally substituted C<SUB>1</SUB>-C<SUB>12 </SUB>alkyl, C<SUB>1</SUB>-C<SUB>12 </SUB>alkenyl, C<SUB>1</SUB>-C<SUB>12 </SUB>alkynyl, or aryl C<SUB>1</SUB>-C<SUB>12 </SUB>alkyl, containing 0-4 heteroatoms in place of a carbon in the carbon backbone, where the optional substituents are -O, -N, or OH; and wherein R<SUP>3 </SUP>is H or CH<SUB>3</SUB>. Such compounds are useful in pharmaceutical compositions and methods of treating conditions characterized by enhanced TGFbeta activity.
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