Protein farnesyl transferase inhibitors
US5523430A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | May 23, 1994 |
| Grant date | Jun 4, 1996 |
| Priority date | — |
| Expiry date | May 23, 2014 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07F9/3826
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, and inhibition of cholesterol biosynthesis, are effected by compounds of the formula ##STR1## their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs, and solvates, wherein: PA1 X is --ONR.sup.1 C(O)--, --N(OR.sup.1)C(O)--, --NR.sup.1 C(O)--, --C(O)NR.sup.1 --, --NR.sup.1 S(O.sub.2)--, --C(O)O--, --OC(O)--, --O--, --NR.sup.1 -- or --(S)q; PA1 Y and Z are each independently --CO.sub.2 R.sup.2, --SO.sub.3 R.sup.2 or --P(O)(OR.sup.2)(OR.sup.3); PA1 R is alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkenylene or aryl; PA1 R.sup.1, R.sup.2 and R.sup.3 are each independently hydrogen, alkyl, aryl or aralkyl; PA1 m and n are each independently 0 or an integer from 1 to 5; PA1 p is 0 or 1; and PA1 q is an integer from 1 to 2.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.