Method of using phenylacetonitrilealkylaminoalkyl-ortho-substitu

Details Method of using phenylacetonitrilealkylaminoalkyl-ortho-substitu Method of using phenylacetonitrilealkylaminoalkyl-ortho-substitu

1994-03-01

1996-01-23

Brust, Joseph Paul

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ester doai

558390, A61K 31275

Patent

active

054865395

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.

REFERENCES:
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patent: 4593042 (1986-06-01), Liang
patent: 4681970 (1987-07-01), Liang
patent: 5162569 (1992-11-01), Liang et al.
Walz et al, Transplantation, 47; pp. 331-334 (1989).
Nel et al, Scand. J. Immunology, 24; pp. 283-290 (1986).
Chen et al, Acta. Pharmacologica Sinica, 11(3); pp. 281-285 (1989).

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