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US 6,642,232 B2Granted
3-[4-Substituted heterocyclyl)-pyrrol-2-ylmethylidene]-2- indolinone derivatives as kinase inhibitors
AssigneeSugen, Inc.
InventorsMatthew Mattson, Tomas Vojkovsky, Congxin Liang, Peng Cho Tang, Huiping Guan
Life of this patent
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Abstract
The present invention relates to certain 3-[4-(substituted heterocyclyl)-pyrrol-2-ylmethylidene]-2-indolinone derivatives that inhibit kinases, in particular VEGFR and/or PDGFR kinases. Pharmaceutical compositions comprising these compounds, methods of treating diseases mediated by kinases utilizing pharmaceutical compositions comprising these compounds, and methods of preparing them are also disclosed.
Claims25
A compound of Formula (IV):
- wherein:
- R is:
- (a) hydrogen;
- (b) —PO(OR5)2 where each R5 is independently hydrogen or alkyl;
- (c) —COR6 where R6 is alkyl;
- or
- (d) —CHR7NR8R9 where R7 is hydrogen or alkyl, and R8 and R9 are independently hydrogen or alkyl;
- or R8 and R9 together with the nitrogen atom to which they are attached form a heterocycloamino ring;
- R1 is hydrogen, alkyl, alkoxy, hydroxy, trifluoromethyl, trifluoromethoxy, F, Cl, Br, or I;
- R2 is hydrogen, alkyl, heteroaryl, alkoxy, hydroxy, F, Cl, Br, or I;
- R3 is hydrogen or alkyl;
- R4 is hydrogen or alkyl;
- ring A is optionally substituted heterocycloamino;
- Het is cycloalkylaminoalkyl, cycloalkylalkylaminoalkyl, heteroaryl, heterocycle, heterocyclylcarbonylalkyl, heterocyclylalkylcarbonyl, or heterocyclylalkyl;
- X is NR8R9 or OR8;
- and
- n is 0 or 1;
- or
- a pharmaceutically acceptable salt thereof.
16 more elements
A compound of Formula (I):
- wherein:
- R is:
- (a) hydrogen;
- (b) —PO(OR5)2 where each R5 is independently hydrogen or alkyl;
- (c) —COR6 where R6 is alkyl;
- or
- (d) —CHR7NR8R9 where R7 is hydrogen or alkyl, and R8 and R9 are independently hydrogen or alkyl;
- or R8 and R9 together with the nitrogen atom to which they are attached form a heterocycloamino ring;
- R1 is hydrogen, alkyl, alkoxy, hydroxy, trifluoromethyl, trifluoromethoxy, F, Cl, Br, or I;
- R2 is hydrogen, alkyl, heteroaryl, alkoxy, hydroxy, F, Cl, Br, or I;
- R3 is hydrogen or alkyl;
- R4 is hydrogen or alkyl;
- ring A is optionally substituted heterocycloamino;
- Het is cycloalkylaminoalkyl, cycloalkylalkylaminoalkyl, heteroaryl, heterocycle, or heterocyclylalkyl;
- or
- a pharmaceutically acceptable salt thereof.
13 more elements
A compound selected from the group consisting of:
- 1 434.5 2 452.5 3 469.0 4 436.5 5 495.6 6 424.5 7 440.9 8 452.5 9 469.0 10 436.53 11 436.53 12 13 14 15 16 17 18 19 20 21 22 23 24 25
Dependencies are inferred from the claim text.