Inhibitors of protein isoprenyl transferases

US6221865A · kind A · utility

Assignee

• UNIVERSITY OF PITTSBURGH · US

Inventors

• Said M. Sebti · Tampa, US
• Andrew D. Hamilton · Felton, GB
• Kenneth J. Barr · San Francisco, US
• Stephen A. Fakhoury · Mundelein, US
• Stephen O'Connor · Wilmette, US
• Saul H. Rosenberg · Grayslake, US
• Wang Shen · San Mateo, US
• Bryan K. Sorensen · Antioch, US
• Gerard M. Sullivan · Round Lake Beach, US
• James T. Wasicak · Waterford, US
• Kenneth J. Henry · Carmel, US
• Le Wang · Xi'an, CN

Key dates

• Filing date: May 7, 1998
• Grant date: Apr 24, 2001
• Expiry date: May 7, 2018

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2603/74
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sub.1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L.sub.2 --, and (i) heterocyclic-L.sub.2 --; R.sub.2 is selected from PA1 (a) ##STR2## PA1 (b) --C(O)NH--CH(R.sub.14)--C(O)OR.sub.15, ##STR3## PA1 (d) --C(O)NH--CH(R.sub.14)--C(O)NHSO.sub.2 R.sub.16, PA1 (e) --C(O)NH--CH(R.sub.14)-tetrazolyl, (f) --C(O)NH-heterocyclic, and PA1 (g) --C(O)NH--CH(R.sub.14)--C(O)NR.sub.17 R.sub.18 ; R.sub.3 is substituted or unsubstituted heterocyclic or aryl, substituted or unsubstituted cycloalkyl or cycloalkenyl, ##STR4## PA1 and --P(W)R.sup.R3 R.sup.R3 '; R.sub.4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; L.sub.1 is absent or is selected from (a) --L.sub.4 --N(R.sub.5)--L.sub.5 --, (b) --L.sub.4 --O--L.sub.5 --, (c) --L.sub.4 --S(O).sub.n --L.sub.5 --(d) --L.sub.4 --L.sub.6 --C(W)--N(R.sub.5)--L.sub.5 --, (e) --L.sub.4 --L.sub.6 --S(O).sub.m --N(R.sub.5)--L.sub.5 --, (f) --L.sub.4 --N(R.sub.5)--C(W)--L.sub.7 --L.sub.5 --, (g) --L.sub.4 --N(R.sub.5)--S(O).sub.p --L.sub.7 --L.sub.5 --, (h) …