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US 7,253,285 B2Granted
Thiazolinone 4-monosubstituted quinolines
AssigneeHoffmann-La Roche Inc.
InventorsLi Chen, Shaoqing Chen, Jianping Lou, Achyutharao Sidduri
Life of this patent
Estimating the term…
Abstract
Thiazolinone monosubstituted quinoline derivatives where the quinoline ring is mono-substituted at the 4 positions which derivatives demonstrates CDK1 antiproliferative activity and are useful as anti-cancer agents.
Claims80
A compound of the formula:
- wherein
- R1 is hydrogen, lower alkyl, aryloxy-lower alkyl, lower alkoxy-lower alkyl or;
- or R2—(X)n—
- X is lower alkylene, hydroxyloweralkylene, cycloloweralkylene, aryl lower alkylene, carboxyloweralkylene, hydroxy lower alkylene, amido lower alkylene, mono- or di-halo lower alkylene, amino lower alkylene, mono- or di-lower alkyl amino lower alkylene or imido lower alkylene;
- R2 is
- is an aryl ring, cyclolower alkyl ring containing from 3 to 6 carbon atoms, a 4 to 6 membered heterocycloalkyl ring containing from 3 to 5 carbon atoms and from 1 to 2 hetero atoms selected from the group consisting of oxygen, nitrogen and sulfur, or a 5 or 6 membered heteroaromatic ring containing from 1 to 2 hetero atoms selected from the group consisting of oxygen, sulfur and nitrogen;
- R5, R6 and R7 are independently selected from the group consisting of hydroxy, lower alkyl sulfone, hydroxy-lower alkyl, hydrogen, lower alkyl, halogen, perfluro lower alkyl, lower alkoxy, amino, mono- or di-lower alkyl amino, or when two of the substituents R5, R6 and R7 are substituted on adjacent carbon atoms on ring
- these two substituents can be taken together with their adjacent, attached carbon atoms to form an aryl ring, a 3 to 6 membered cyclolower alkyl ring, a 4 to 6 membered heterocycloalkyl ring or a 4 to 6 membered heteroaromatic ring, said heterocycloalkyl ring and said heteroaromatic ring containing from 1 to 2 hetero atoms selected from the group consisting of oxygen, nitrogen or sulfur;
- R4 is halo,
- is an aryl ring, a cycloalkyl ring containing from 2 to 6 carbon atoms, a 4 to 6 membered heterocyclic alkyl ring containing from 3 to 5 carbon atoms and from 1 to 2 hetero atoms selected from the group consisting of a oxygen, sulfur and nitrogen or a 5 to 6 numbered heteroaromatic right containing from 1 to 2 hetro atoms selected from the group consisting of oxygen sulfur and nitrogen;
- R8, R9, R11, R15 and R16 are independently hydrogen or lower alkyl;
- R10 and R12, are lower alkyl;
- R14 is perfluro lower alkyl or —N R15R16;
- R17 and R18 are independently hydrogen, lower alkyl, or
- n and k are integers from 0 to 1;
- m, w, y and z are integers from 0 to 3;
- p is an integer from 0 to 6 and v and t are integers from 1 to 6;
- or pharmaceutically acceptable salts thereof.
15 more elements
Dependencies are inferred from the claim text.