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US 2002/0119981 A1Published application
Novel N-substituted urea inhibitors of farnesyl-protein transferase
AssigneeSchering Corporation
InventorsStacy W. Remiszewski, Alan K. Mallams
Life of this patent
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Abstract
Novel halo-N-substituted urea compounds and pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel halo-N-substituted urea compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammals such as a human.
Claims15
A compound of the formula:
- 64
- or a pharmaceutically acceptable salt or solvate thereof, wherein:
- A represents N or N-oxide;
- X represents N, CH or C, such that when X is N or CH, there is a single bond to carbon atom 11 as represented by the solid line;
- or when X is C, there is a double bond to carbon atom 11, as represented by the solid and dotted lines;
- X1 and X2 are independently selected from bromo or chloro, and X3 and X4 are independently selected from hydrogen, bromo or chloro provided that at least one of X3 and X4 is hydrogen;
- Y1 and Y2 are independently selected from hydrogen or alkyl;
- Z is ═O or ═S;
- R5, R6, R7 and R8 each independently represents hydrogen, —CF3, —COR10, alkyl or aryl, and further wherein R5 may be combined with R6 to represent ═O or ═S and/or R7 may be combined with R8 to represent ═O or ═S;
- R10, R19 and R20 independently represent hydrogen, alkyl, alkoxy, aryl, aralkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl and heterocycloalkylalkyl, with the proviso that R19 and R20 are not both hydrogen;
- v is zero, 1, 2 or 3;
- and
- w is zero or 1.
10 more elements
Dependencies are inferred from the claim text.