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US 6,472,435 B1Granted
Anti-tumor agents
AssigneeAstraZeneca AB
InventorFrancis T Boyle
Life of this patent
Estimating the term…
Abstract
The invention concerns anti-tumor agents of formula (I), wherein each of R1, R2 and R3 has the meanings defined in the specification including hydrogen, (1-4C)alkyl, (3-4C)alkynyl and (1-4C)alkoxyl; each of R4 and R5 is (1-4C) alkyl; each of R6 and R7 is hydrogen or (1-4C)alkyl; X is N-(1-4C)alkylimino, N-(3-4C)alkenylimino, or (3-4C)alkynylimino; m is 1 or 2 and each R8 is as defined in the specification; each Y′ and Y2 is halogen, (1-4C)alkanesulphonyloxy, benzensulphonyloxy or phenyl-(1-4C)alkanesulfonyloxy; or a pharmaceutical acceptable salt thereof; provided that at least one of R1, R2 and R3 is other than hydrogen; a process for their preparation, pharmaceutical composition containing them and their use for producing an anti-proliferative effect in a warm-blooded animal.
Claims10
An anti-tumour agent of the formula I
- wherein
- R1 is hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, hydroxy-(1-4C)alkyl, (1-4C)alkoxy-(1-4C)alkyl, amino-(1-4C)alkyl, (1-4C)alkylamino-(1-4C)alkyl, di-[(1-4C)alkyl]amino-(1-4C)alkyl, pyrrolidin-1-yl-(1-4C)alkyl, piperidino-(1-4C)alkyl, morpholino-(1-4C)alkyl, piperazin-1-yl-(1-4C)alkyl, 4-(1-4C)alkylpiperazin-1-yl-(1-4)alkyl, carboxy-(1-4C)alkyl, (1-4C)alkoxycarbonyl-(1-4C)alkyl, carbamoyl-(1-4C)alkyl, N-(1-4C)alkylcarbamoyl-(1-4C)alkyl, N,N-di-[(1-4C)alkyl]carbamoyl-(1-4C)alkyl, hydroxy, (1-4C)alkoxy, hydroxy-(2-4C)alkoxy, (1-4C)alkoxy-(2-4C)alkoxy, amino-(2-4C)alkoxy, (1-4C)alkylamino-(2-4C)alkoxy, di-[(1-4C)alkyl]amino-(2-4C)alkoxy, pyrrolidin-1-yl-(2-4C)alkoxy, piperidino-(2-4C)alkoxy, morpholino-(2-4C)alkoxy, piperazin-1-yl-(2-4C)alkoxy, 4-(1-4C)alkylpiperazin-1-yl-(2-4C)alkoxy, (1-4C)alkylthio, (1-4C)alkylsulphinyl or (1-4C)alkylsulphonyl;
- R2 is hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, hydroxy-(1-4C)alkyl, (1-4C)alkoxy-(1-4C)alkyl, amino-(1-4C)alkyl, (1-4C)alkylamino-(1-4C)alkyl, di-[(1-4C)alkyl]amino-(1-4C)alkyl, pyrrolidin-1-yl-(1-4C)alkyl, piperidino-(1-4C)alkyl, morpholino-(1-4C)alkyl, piperazin-1-yl-(1-4C)alkyl, 4-(1-4C)alkylpiperazin-1-yl(1-4C)alkyl, carboxy-(1-4C)alkyl, (1-4C)alkoxycarbonyl-(1-4C)alkyl, carbamoyl-(1-4C)alkyl, N-(1-4C)alkylcarbamoyl-(1-4C)alkyl, N,N-di-[(1-4C)alkyl]carbamoyl-(1-4C)alkyl, hydroxy, (1-4C)alkoxy, hydroxy-(2-4C)alkoxy, (1-4C)alkoxy-(2-4C)alkoxy, amino-(2-4C)alkoxy, (1-4C)alkylamino-(2-4C)alkoxy, di-[(1-4C)alkyl]amino-(2-4C)alkoxy, pyrrolidin-1-yl-(2-4C)alkoxy, piperidino-(2-4C)alkoxy, morpholino-(2-4C)alkoxy, piperazin-1-yl-(2-4C)alkoxy or 4-(1-4C)alkylpiperazin-1-yl-(2-4C)alkoxy;
- R3 is hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, hydroxy-(1-4C)alkyl, (1-4C)alkoxy-(1-4C)alkyl, amino-(1-4C)alkyl, (1-4C)alkylamino-(1-4C)alkyl, di-[(1-4C)alkyl]amino-(1-4C)alkyl, pyrrolidin-1-yl-(1-4C)alkyl, piperidino-(1-4C)alkyl, morpholino-(1-4C)alkyl, piperazin-1-yl-(1-4C)alkyl, 4-(1-4C)alkylpiperazin-1-yl-(1-4C)alkyl, carboxy-(1-4C)alkyl, (1-4C)alkoxycarbonyl-(1-4C)alkyl, carbamoyl-(1-4C)alkyl, N-(1-4C)alkylcarbamoyl-(1-4C)alkyl, N,N-di-[(1-4C)alkyl]carbamoyl-(1-4C)alkyl, hydroxy, (1-4C)alkoxy, hydroxy-(2-4C)alkoxy, (1-4C)alkoxy-(2-4C)alkoxy, amino-(2-4C)alkoxy, (1-4C)alkylamino-(2-4C)alkoxy, di-[(1-4C)alkyl]amino-(2-4C)alkoxy, pyrrolidin-1-yl-(2-4C)alkoxy, piperidino-(2-4C)alkoxy, morpholino- (2-4C)alkoxy, piperazin-1-yl-(2-4C)alkoxy, piperazin-1-yl-(2-4C)alkoxy or 4-(1-4C)alkylpiperazin-1-yl-(2-4C)alkoxy;
- R4 is (1-4C)alkyl;
- R5 is (1-4C)alkyl;
- R6 is hydrogen or (1-4C)alkyl;
- R7 is hydrogen or (1-4C)alkyl;
- X is N-(1-4C)alkylimino, N-(3-4C)alkenylimino or N-(3-4C)alkynylimino;
- m is 1 or 2 and each R8 is independently hydrogen, halogeno, hydroxy, (1-4C)alkoxy, (2-4C)alkenyloxy, (2-4C)alkynyloxy, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, amino, (1-4C)alkylamino, di-[(1-4C)alkyl]amino, cyano, (2-4C)alkanoylamino, carboxy, (1-4C)alkoxycarbonyl, carbamoyl, N-(-4C)alkylcarbamoyl or N,N-di-[(1-4C)alkyl]carbamoyl;
- Y1 is halogeno, (1-4C)alkanesulphonyloxy, benzenesulphonyloxy or phenyl-(1-4C)alkanesulphonyloxy;
- and
- Y2 is halogeno, (1-4C)alkanesulphonyloxy, benzenesulphonyloxy or phenyl-(1-4C)alkanesulphonyloxy;
- and wherein any heterocyclic group in R1, R2 or R3 is optionally substituted with 1, 2 or 3 (1-4C)alkyl substituents, and wherein any phenyl group in Y1 or Y2 when Y1 and Y2 is benzenesulphonyloxy or phenyl-(1-4C)alkanesulphonyloxy is optionally substituted with 1, 2 or 3 substituents selected from halogeno, nitro, cyano, trifluoromethyl, hydroxy, amino, (1-4C)alkyl, (1-4C)alkoxy, (1-4C)alkylamino and di-[(1-4C)alkyl]amino;
- or a pharmaceutically-acceptable salt thereof;
- provided that at least one of R1, R2 and R3 is other than hydrogen.
13 more elements
Dependencies are inferred from the claim text.