Patent · US Expired

Pyrazoloquinolones as anticancer agents

US5334595A · kind A · utility

6Cited by
5References
16Claims
0Family size

Assignee

Inventor

Key dates

Filing dateOct 23, 1992
Grant dateAug 2, 1994
Priority date
Expiry dateOct 23, 2012

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D471/04
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower-alkyl, or trifluoromethyl; PA0 R.sub.2 is lower-alkyl, trifluoromethyl or CH.sub.2 Y where Y is hydroxy, chloro, lower-alkylamino or dilower-alkylamino PA0 R.sub.3 and R.sub.4 are each independently hydrogen or fluoro; PA0 R.sub.5 is hydrogen, lower-alkyl or PA1 (a) phenyl, 2-pyridyl, 4-pyridyl, 1-naphthyl or such groups substituted with one or more, the same or different, lower-alkyl, fluoro, hydroxy, or lower-alkoxy; PA1 (b) cycloalkyl or cycloalkyl substituted with amino, lower-alkylamino, dilower-alkylamino, formamido, acetamido, lower-alkyl, hydroxy, lower-alkoxy, trifluoromethyl, carboxy, lower-alkoxycarbonyl or halo, or cycloalkyl having a phenyl ring fused thereto; PA1 (c) A saturated heterocyclic 5- or 6-membered ring containing oxygen and/or nitrogen or such ring substituted with lower-alkyl; or PA1 (d) (CH.sub.2).sub.n -Z wherein n is an integer from about one to four and Z is amino, dilower-alkylamino, bis(hydroxylower-alkyl)lower-alkylamino; or a pharmaceutically acceptable acid addition salt thereof are topoiosmerase II inhibitors and are useful in the treatment of cancer in mammalian hosts.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.