Fluoro taxols
US5294637A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | May 20, 1993 |
| Grant date | Mar 15, 1994 |
| Priority date | — |
| Expiry date | May 20, 2013 |
Classification
- Technology area (CPC H)Electricity
- CPC primaryH05K3/403
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
This invention relates to a fluorinated taxol of formula I ##STR1## in which R.sup.1 is --COR.sup.z in which R.sup.z is RO-- or R; PA0 R.sup.g is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or a radical of the formula --W--R.sup.x in which W is a bond, C.sub.2-6 alkenediyl, or --(CH.sub.2).sub.t --, in which t is one to six; and R.sup.x is naphthyl, furyl, thienyl or phenyl, and furthermore R.sup.x can be optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups; PA0 R.sup.2 is --OCOR, H, OH, --OR, --OSO.sub.2 R, --OCONR.sup.o R, --OCONHR, --OCOO(CH.sub.2).sub.t R, or --OCOOR; and PA0 R and R.sup.o are independently C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl, C.sub.2-6 alkynyl, or phenyl, optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups. Further provided by this invention are pharmaceutical formulations and useful intermediates for the fluorinated taxols of formula I. A method of treating mammalian tumors using a compound of formula I is also provided.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.