Patent · US Expired

Tri-substituted (aryl or heteroaryl) derivatives and pharmaceutical compositions containing the same

US5622977A · kind A · utility

62Cited by
16References
29Claims
0Family size

Assignee

Inventors

Key dates

Filing dateJun 7, 1995
Grant dateApr 22, 1997
Priority date
Expiry dateJun 7, 2015

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07C59/72
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

Compounds of the general formula (1) ##STR1## are described wherein Y is halogen or --OR.sup.1, where R.sup.1 is a substituted or unsubstituted alkyl; X is --O--, --S-- or --N(R.sup.8)--, where R.sup.8 is hydrogen or alkyl; R.sup.2 is substituted or unsubstituted alkyl, alkenyl, cycloalkyl or cycloalkenyl; R.sup.3 is hydrogen, halogen or --OR.sup.9, where R.sup.9 is hydrogen or substituted or unsubstituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl, or formyl, carboxamido or thiocarboxamido; R.sup.4 and R.sup.5, which may be the same or different, are each --(CH.sub.2).sub.n Ar, where Ar is a monocyclic or bicyclic aryl group or monocyclic or bicyclic heteroaryl and n is integer of 0 to 3; R.sup.6 is hydrogen or substituted or unsubstituted alkyl; R.sup.7 is hydrogen or substituted or unsubstituted alkyl; and the salts, solvates, hydrates and N-oxides thereof. Compounds according to the invention are potent, selective and orally active PDE IV inhibitors and are useful in the prophylaxis and treatment of asthma and other diseases.

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