Pharmaceutical preparation for inhibiting undesirable cell growth - contains new and known 2,4-di:hydroxy-2H-1,4-benzoxazin-3(4H)-ones derivs., esp. useful for treating cancer

摘要

Pharmaceutical preparation for inhibiting undesirable cell growth in vertebrates comprises a 2,4-dihydroxy-2H-1,4-benzoxazin-3(4H)-one deriv. of formula (I), or a salt of (I), as active agent. R1 = H, 1-6C alkyl (opt. substd. by 1-3 halo, OH, 1-6C alkoxy, phenoxy, opt. esterified carboxy, or phenyl), or phenyl (opt. substd. by 1-3 1-6C alkyl, OH, alkoxy, acyloxy, halo or opt. esterified carboxy); R2 = H, COR1, a glycosidically linked sugar, 1-6C alkyl (opt. substd. by 1-3 halo, OH, 1-6C alkoxy, phenoxy, phenyl or opt. esterified carboxy), or phenyl (opt. substd. by 1-3, 1-6C alkyl, OH, alkoxy, acyloxy, halo or opt. esterified carboxy); R3 = H or COR1; n = 0-4; each R4 = 1-6C alkyl (opt. substd. by OH, alkoxy, phenyl or phenoxy), OR11, OCOR11; and R11 = R1, opt. esterified carboxy, or a glycosidically linked sugar; or two neighbouring R4 gps. form a gp. OCH2O or OCH2CH2O. Also new are cpds. (I), provided that when n is 0 or 1, R4 is 1-6C alkyl, 1-6C alkoxy, halo or opt. substd. phenyl, R3 is H and R2 is H, 1-6C alkyl or a glycosidically linked sugar, then R1 is not H. The most preferred cpds. of formula (I) are of formula (IA) where Q = H, or a sugar gp. (esp. a glucose or mannose residue). USE/ADVANTAGE - The preparations are esp. useful in treatment of cancers. Admin. is esp. oral. Dosage is, e.g. 0.2-20 (esp. 0.4-0.6) mg/kg/day. (I) are of low toxicity to healthy cells.