Anti-androgenic amide derivative
US4386080A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | May 21, 1981 |
| Grant date | May 31, 1983 |
| Priority date | — |
| Expiry date | May 21, 2001 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D303/48
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Novel 3,4-disubstituted-N-acylanilines of the formula: ##STR1## wherein R.sup.1, R.sup.2 and ring A are defined in claim 1; wherein R.sup.3 is hydrogen or alkyl of up to 4 carbon atoms, or is joined to R.sup.5 as stated below; PA1 wherein R.sup.4 is alkyl of 2 to 4 carbon atoms, or has the formula --CX.sup.1 X.sup.2 X.sup.3 wherein X.sup.1, X.sup.2 and X.sup.3, which may be the same or different, each is hydrogen, fluorine or chlorine; wherein R.sup.5 is hydrogen, hydroxy or alkoxy or acyloxy each of up to 15 carbon atoms, or is joined to R.sup.3 to form an oxycarbonyl group such that together with the ##STR2## part of the molecule it forms an oxazolidinedione group; and wherein R.sup.6 is hydrogen or halogen. These compounds possess antiandrogenic activity and are useful for the treatment of androgen dependent or prostatic diseases. Representative of the compounds is 3,4-dichloro-N-(2-hydroxy-2-p-nitrophenylpropionyl)aniline. Also disclosed are processes for the manufacture of the compounds and pharmaceutical and veterinary compositions containing them.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.