US 7,115,740 B2Granted

Pyrimido compounds having antiproliferative activity

AssigneeHoffmann-La Roche Inc.

InventorsYi Chen, Apostolos Dermatakis, Jin-Jun Liu, Kin-Chun Luk, Christophe Michoud, Pamela Loreen Rossman

Life of this patent

Estimating the term…

Abstract

Disclosed are novel pyrimido compounds that are selective inhibitors of both KDR and FGFR kinases. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer.

Claims30

Dependent claims

A compound of formula

wherein
R1 is selected from the group consisting of
—H,
—(CH2)n-heterocycle,
-lower alkyl substituted by up to three groups selected from —OR9, —COR10, —CO2R10, —CONR10R11, —SO2NR10R11, SO2R10 or —CN;
-alkyl,
-cycloalkyl,
-alkenyl, and
-alkynyl,
where n is 0, 1, 2, or 3, and the heterocycle, cycloalkyl, alkenyl, and alkynyl groups are each independently, optionally substituted by up to 3 groups selected from
—OR9,
—COR10,
—CO2R10,
—CONR10R11,
—SO2NR10R11,
—SO2R10, and
—CN;
R2 and R3 are independently selected from the group consisting of
—H,
—OR9,
-halogen,
—COR10,
—(CH2)n-heterocycle,
-alkyl,
-cycloalkyl,
-alkenyl, and
-alkynyl,
where n is 0, 1, 2, or 3, and the heterocycle, alkyl, cycloalkyl, alkenyl, and alkynyl groups are each independently, optionally substituted by up to 3 groups selected from
—OR9,
-halogen,
—COR10, and
—CO2R10;
R4, R5, R6, R7 and R8 are each independently selected from the group consisting of
—H,
-lower alkyl that optionally may be substituted by hydroxy or alkoxy,
—OR12,
-halogen,
—COR13, and
—CO2R13;
R9 is selected from the group consisting of
—H,
—COR10,
-lower alkyl that optionally may be substituted by hydroxy or alkoxy,
-cycloalkyl that optionally may be substituted by hydroxy, alkoxy, and lower alkyl, and
-heterocycle that optionally may be substituted by hydroxy, alkoxy or lower alkyl;
R10 and R11 are each independently selected from the group consisting of
—H,
-lower alkyl that optionally may be substituted by hydroxy or alkoxy,
-cycloalkyl that optionally may be substituted by hydroxy, alkoxy or lower alkyl, and
-heterocycle that optionally may be substituted by hydroxy, alkoxy or lower alkyl;
R12 is selected from the group consisting of —H, lower alkyl and —COR13;
and
R13 is selected from the group consisting of —H and lower alkyl;
or the pharmaceutically acceptable salts thereof.

51 more elements

Dependencies are inferred from the claim text.

patentgrep

Loading patent…

Abstract

A compound of formula

wherein
R1 is selected from the group consisting of
—H,
—(CH2)n-heterocycle,
-lower alkyl substituted by up to three groups selected from —OR9, —COR10, —CO2R10, —CONR10R11, —SO2NR10R11, SO2R10 or —CN;
-alkyl,
-cycloalkyl,
-alkenyl, and
-alkynyl,
where n is 0, 1, 2, or 3, and the heterocycle, cycloalkyl, alkenyl, and alkynyl groups are each independently, optionally substituted by up to 3 groups selected from
—OR9,
—COR10,
—CO2R10,
—CONR10R11,
—SO2NR10R11,
—SO2R10, and
—CN;
R2 and R3 are independently selected from the group consisting of
—H,
—OR9,
-halogen,
—COR10,
—(CH2)n-heterocycle,
-alkyl,
-cycloalkyl,
-alkenyl, and
-alkynyl,
where n is 0, 1, 2, or 3, and the heterocycle, alkyl, cycloalkyl, alkenyl, and alkynyl groups are each independently, optionally substituted by up to 3 groups selected from
—OR9,
-halogen,
—COR10, and
—CO2R10;
R4, R5, R6, R7 and R8 are each independently selected from the group consisting of
—H,
-lower alkyl that optionally may be substituted by hydroxy or alkoxy,
—OR12,
-halogen,
—COR13, and
—CO2R13;
R9 is selected from the group consisting of
—H,
—COR10,
-lower alkyl that optionally may be substituted by hydroxy or alkoxy,
-cycloalkyl that optionally may be substituted by hydroxy, alkoxy, and lower alkyl, and
-heterocycle that optionally may be substituted by hydroxy, alkoxy or lower alkyl;
R10 and R11 are each independently selected from the group consisting of
—H,
-lower alkyl that optionally may be substituted by hydroxy or alkoxy,
-cycloalkyl that optionally may be substituted by hydroxy, alkoxy or lower alkyl, and
-heterocycle that optionally may be substituted by hydroxy, alkoxy or lower alkyl;
R12 is selected from the group consisting of —H, lower alkyl and —COR13;
and
R13 is selected from the group consisting of —H and lower alkyl;
or the pharmaceutically acceptable salts thereof.

51 more elements