Patent · US Expired

Antivirally active heterocyclic azahexane derivatives

US5849911A · kind A · utility

41Cited by
3References
11Claims
0Family size

Assignee

Inventors

Key dates

Filing dateApr 9, 1997
Grant dateDec 15, 1998
Priority date
Expiry dateApr 9, 2017

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D333/20
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

There are described compounds of formula I*, ##STR1## wherein R.sub.1 is lower alkoxycarbonyl, PA1 R.sub.2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl, PA1 R.sub.3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C.sub.4 -C.sub.8 cycloalkyl, PA1 R.sub.4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, sulfinyl (--SO--) and sulfonyl (--SO.sub.2 --) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl, PA1 R.sub.5, independently of R.sub.2, has one of the meanings mentioned for R.sub.2, and PA1 R.sub.6, independently of R.sub.1, is lower alkoxycarbonyl, or salts thereof, provided that at least one salt-forming group is present. The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS. They exhibit outstanding pharmacodynamic properties.

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