Inventors:
Said M. Sebti - Tampa FL
Andrew D. Hamilton - Guilford CT
David J. Augeri - Kenosha WI
Kenneth J. Barr - Chicago IL
Greg B. Donner - Mundelein IL
Stephen A. Fakhoury - Mundelein IL
Stephen J. OConnor - Wilmette IL
Saul H. Rosenberg - Grayslake IL
Wang Shen - Gurnee IL
Bruce G. Szczepankiewicz - Lindenhurst IL
Indrani W. Gunawardana - Libertyville IL
Assignee:
University of Pittsburgh - Pittsburgh PA
International Classification:
A61K 3144
US Classification:
514357, 514352, 51425505, 514256, 544238, 544333, 544405, 546264, 546266, 548252, 549321
Abstract:
Compounds having the formula or a pharmaceutically acceptable salt thereof wherein R is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L â, and (i) heterocyclic-L is selected from (e) âC(O)NHâCH(R )-tetrazolyl, (f) âC(O)NH-heterocyclic, and (g) âC(O)NHâCH(R )âC(O)NR R ; R is heterocyclic, aryl, substituted or unsubstituted cycloalkyl; R is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; L is absent or is selected from (a) âL âN(R )âL â, (b) âL âOâL â, (c) âL âS(O) âL â (d) âL âL âC(W)âN(R )âL â, (e) âL âL âS(O) âN(R )âL â, (f) âL âN(R )âC(W)âL âL â, (g) âL âN(R )âS(O) âL âL â, (h) optionally substituted alkylene, (i) optionally substituted alkenylene, and (j) optionally substituted alkynylene are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases.