Organic compounds -- part of the class 532-570 series – Organic compounds – Carboxylic acid esters
Patent
1990-12-12
1992-11-10
Dees, Jose G.
Organic compounds -- part of the class 532-570 series
Organic compounds
Carboxylic acid esters
562451, C07C22938
Patent
active
051625695
ABSTRACT:
A class of substituted phenylacetonitrilealkylaminoalkyl-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: 4681970 (1987-07-01), Liang
G. Walz et al., Transplantation, 47, 331-334 (1989).
A. Nel et al., Scand. J. Immunology, 24, 283-290 (1986).
W. R. Chen et al., Acta. Pharmacologica Sinica, 11(3) 281-285 (1990).
Farah, Jr. John M.
Liang Chi-Dean
McKearn John P.
Mueller Richard A.
Dees Jos,e G.
Frazier B.
G. D. Searle & Co.
Keane J. Timothy
Matukaitis Paul D.
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