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US 2012/0238575 A1Published application
Antiproliferative pyrimidyl, fused pyrimidyl and pyrimidyl hydrazones
AssigneeMerck Serono SA
InventorsBRIAN HEALEY, Zhong Zhao, Amanda Sutton, Matthias Schwarz
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Abstract
The present invention is related to a novel series of pyrimidyl or fused pyrimidyl hydrazones. Compounds of Formula (I) wherein A is selected from the group consisting of Formulas (A1), (A2), (A3), (A4), (A5) are useful for the treatment and/or prevention of a proliferative disease.
Claims13
A compound according to Formula (I)
- wherein
- A is selected from the group consisting of A1, A2, A3, A4 and A5:
- wherein each X is independently selected from the group consisting of CR6, N and NR6;
- and each Y is independently selected from the group consisting of CR6, N, NR6, S and O;
- L is either a bond or NR6;
- R1, R6 and R9 are independently either hydrogen or C1-C6-alkyl;
- each R2 is independently selected from the group consisting of hydrogen, halogen, cyano, thioamide, acyl, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, sulfonylamine, halo-C1-C6-alkyl, C1-C6-alkoxy, hydroxylamine, hydroxyl, C3-C8-cycloalkyl, C3-C8-heterocycloalkyl, aryl and heteroaryl;
- n is an integer selected from 1, 2, 3, 4 or 5;
- R3 and R7 are independently selected from the group consisting of hydrogen, halogen, cyano, thiourea, acylamine, carboxy, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C8-cycloalkyl, C3-C8-heterocycloalkyl, sulfonylamine, halo-C1-C6-alkyl, C1-C6-alkoxy, halo-C1-C6-alkoxy, hydroxylamine, hydroxyl, aryl and heteroaryl, wherein each of said C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C8-cycloalkyl, C3-C8-heterocycloalkyl, sulfonylamine, halo-C1-C6-alkyl, C1-C6-alkoxy, halo-C1-C6-alkoxy, hydroxylamine, hydroxyl, aryl and heteroaryl is optionally substituted with one or more substituents selected from the group consisting of halogen, amine, cyano, C1-C6-alkyl, C2-C6-alkenyl, C3-C8-cycloalkyl, C3-C8-heterocycloalkyl, sulfonylamine, halo-C1-C6-alkyl, C1-C6-alkoxy, halo-C1-C6-alkoxy, hydroxyl, acylamine, hydroxy-C1-C6-alkyl, aryl and heteroaryl;
- R5 is selected from the group consisting of hydrogen, halogen, cyano, thiourea, amino, acylamine, carboxy, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C8-cycloalkyl, C3-C8-heterocycloalkyl, sulfonylamine, halo-C1-C6-alkyl, C1-C6-alkoxy, halo-C1-C6-alkoxy, hydroxylamine, hydroxyl, aryl and heteroaryl, wherein each of said C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C8-cycloalkyl, C3-C8-heterocycloalkyl, sulfonylamine, halo-C1-C6-alkyl, C1-C6-alkoxy, halo-C1-C6-alkoxy, hydroxylamine, hydroxyl, aryl and heteroaryl is optionally substituted with one or more substituents selected from the group consisting of halogen, amine, cyano, C1-C6-alkyl, C2-C6-alkenyl, C3-C8-cycloalkyl, C3-C8-heterocycloalkyl, sulfonylamine, halo-C1-C6-alkyl, C1-C6-alkoxy, halo-C1-C6-alkoxy, hydroxyl, acylamine, hydroxy-C1-C6-alkyl, aryl and heteroaryl;
- R4 is selected from the group consisting of C3-C8-cycloalkyl, C3-C8-heterocycloalkyl, aryl and heteroaryl bonded through a ring carbon, wherein each of said C3-C8-cycloalkyl, C3-C8-heterocycloalkyl, aryl and heteroaryl bonded through a ring carbon is optionally substituted with one or more substituents selected from the group consisting of halogen, amine, cyano, C1-C6-alkyl, C2-C6-alkenyl, C3-C8-cycloalkyl, C3-C8-heterocycloalkyl, sulfonylamine, halo-C1-C6-alkyl, C1-C6-alkoxy, halo-C1-C6-alkoxy, hydroxyl, aminocarbonyl, acylamine, hydroxy-C1-C6-alkyl, aryl and heteroaryl;
- and
- and geometrical isomers, enantiomers, diastereomers, tautomers, racemates or pharmaceutically acceptable salts thereof.
10 more elements
Dependencies are inferred from the claim text.