C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 215/48 (2006.01) A61K 31/47 (2006.01) A61K 31/4709 (2006.01) A61K 31/5355 (2006.01) A61K 31/55 (2006.01) A61P 35/00 (2006.01) C07D 401/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01)
Patent
CA 2720552
To provide an antitumor agent which exhibits excellent c-Met inhibitory effect and mitigates side effects by virtue of selectively affecting to tumor cells in which c-Met is specifically expressed. The invention provides an acylthiourea compound represented by formula (I): Image (wherein each of R1 and R2, which may be the same or different, represents a hydrogen atom, an optionally substituted C1-6 alkyl group, an optionally substituted C3-10 cycloalkyl group, an optionally substituted C6-14 aromatic hydrocarbon group, or an optionally substituted saturated or unsaturated heterocyclic group, or R1 and R2 may form, together with the nitrogen atom to which they are attached, an optionally substituted nitrogen-containing heterocyclic ring; R3 represents a C1-6 alkyl group; and each of R4, R5, and R6, which may be identical to or different from one another, represents a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 alkylamino group, an optionally substituted aromatic hydrocarbon group, or an optionally substituted saturated or 101 unsaturated heterocyclic group, or R5 and R6 may form a ring together with the phenyl ring to which they are attached) or a salt thereof. 102
L'invention concerne un agent anti-tumoral qui présente une excellente activité inhibitrice sur c-Met, peut sélectivement agir sur une cellule tumorale dans laquelle c-Met est exprimé spécifiquement, et qui présente des effets secondaires indésirables réduits. L'invention concerne spécifiquement un composé d'acylthiourée représenté par la formule générale (I) [dans laquelle R1 et R2 représentent indépendamment un hydrogène, un groupe alkyle, un groupe cycloalkyle, un groupe hydrocarboné aromatique ou un cycle hétérocyclique saturé ou insaturé, ou R1 et R2 peuvent former ensemble un cycle; R3 représente un groupe alkyle en C1-6; et R4, R5 et R6 représentent indépendamment un hydrogène, un groupe alkyle, un groupe alcoxy, un groupe alkylamino, un groupe hydrocarboné aromatique, un cycle hétérocyclique saturé ou insaturé ou analogue] ou un de ses sels.
Egami Kosuke
Fujita Hidenori
Suda Yoshimitsu
Smart & Biggar
Taiho Pharmaceutical Co. Ltd.
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