Patent · US Expired

Method of using phenylacetonitrilealkylaminoalkyl-ortho-substituted aryl compounds as immunosuppressives

US5486539A · kind A · utility

6Cited by
5References
3Claims
0Family size

Assignee

Inventors

Key dates

Filing dateMar 1, 1994
Grant dateJan 23, 1996
Priority date
Expiry dateMar 1, 2014

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07C255/43
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

A class of substituted phenylacetonitrile-alkylaminoalkyl-ortho-substituted aryl compounds having immunosuppressive properties is described. Compounds of this class would be useful in reducing recipient rejection of transplanted organs and for treatment of autoimmune or inflammatory diseases. Compounds of particular interest are of the formula ##STR1## wherein m is one or two; wherein n is a number selected from one to five, inclusive; wherein R.sup.1 is selected from hydrido, alkyl, hydroxyalkyl, cycloalkyl, cycloalkylalkyl, alkoxyalkyl, alkenyl and alkynyl; wherein R.sup.6 is selected from loweralkyl; wherein each of R.sup.8, R.sup.9, R.sup.10 and R.sup.12 through R.sup.16 is independently selected from hydrido, hydroxy, alkyl, hydroxyalkyl, alkoxy, alkenyl, alkynyl, alkylcarbonyl, alkoxycarbonyl, alkylcarbonylalkenyl, alkylaminocarbonyl and alkoxyalkyl; with the proviso that at least one of R.sup.12 and R.sup.16 must be selected from hydroxy, alkyl, hydroxyalkyl, alkoxy, alkenyl, alkynyl, alkylcarbonyl, alkoxycarbonyl, alkylcarbonylalkenyl, alkylaminocarbonyl and alkoxyalkyl; or a tautomer thereof or a pharmaceutically-acceptable salt thereof.

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