摘要 |
The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I wherein A is a carbocycle or heterocycle; X is alkylene, NR<SUB>4</SUB>C(O), NR<SUB>4</SUB>C(S), NR<SUB>4</SUB>C(NH), NR<SUB>4</SUB>SO, NR<SUB>4</SUB>SO<SUB>2</SUB>, NR<SUB>4</SUB>C(O)NH, NR<SUB>4</SUB>C(S)NH, C(O)NR<SUB>4</SUB>, C(S)NR<SUB>4</SUB>, C(NH)NR<SUB>4</SUB>, NR<SUB>4</SUB>PO or NR<SUB>4</SUB>PO(OH) wherein R<SUB>4</SUB> is H or alkyl; R<SUB>1</SUB> is selected from the group consisting of alkyl, cycloalkyl, aryl or a heterocycle each of which is optionally substituted with hydroxyl, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; R<SUB>2</SUB> is halogen, hydroxyl, alkyl, acyl or alkoxy each optionally substituted with hydroxyl, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; R<SUB>3</SUB> is halogen, hydroxyl, alkyl, acyl or alkoxy each optionally substituted with hydroxyl, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; m is 0-3; n is 0-3; and salts and solvates thereof. |
申请人 |
GENENTECH, INC.;KOEHLER, MICHAEL F. T.;GOLDSMITH, RICHARD;SUTHERLIN, DANIEL P. |
发明人 |
KOEHLER, MICHAEL F. T.;GOLDSMITH, RICHARD;SUTHERLIN, DANIEL P. |