Therapeutic quinazoline derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C544S284000

Reexamination Certificate

active

10088856

ABSTRACT:
A compound of formula (I) or a salt, ester, amide or prodrug thereof; where X is O, or S, S(O), S(O)2or NR6where R6is hydrogen of C1-6alkyl; R5is an optionally substituted 6-membered aromatic ring containing at least one nitrogen atom, and R1, R2, R3, R4are independently selected from halogeno, cyano, nitro, C1-3alkylsulphanyl, —N(OH)R7— (wherein R7is hydrogen, or C1-3alkyl), or R9X1— (wherein X1represents a direct bond, —O—, —CH2—, —OC(O), —C(O)—, —S—, —SO—, —SO2—, —NR10C(O)—, —C(O)NR11—, —SO2NR12—, —NR13SO2— or NR14— (wherein R10, R11, R12, R13and R14each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl), and R9is hydrogen, optionally substituted hydrocarbyl, optionally substituted heterocyclyl or optionally substituted alkoxy; provided that at least one of R2or R3is other than hydrogen. These compounds inhibit aurora 2 kinase and are useful in the preparation of medicaments for the treatment of proliferative disease such as cancer.

REFERENCES:
patent: 5721237 (1998-02-01), Myers et al.
patent: 6258820 (2001-07-01), Uckun et al.
patent: WO 95/15758 (1995-06-01), None
patent: WO 99/35132 (1999-07-01), None

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