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1. (WO1998050029) INHIBITORS OF PROTEIN ISOPRENYL TRANSFERASES

Pub. No.:    WO/1998/050029    International Application No.:    PCT/US1998/009296
Publication Date: Fri Nov 13 00:59:59 CET 1998 International Filing Date: Fri May 08 01:59:59 CEST 1998
IPC: C07C 237/36
C07C 239/20
C07C 271/22
C07C 317/50
C07C 323/59
C07C 323/60
C07C 327/42
C07D 205/04
C07D 207/08
C07D 207/09
C07D 207/10
C07D 207/12
C07D 207/26
C07D 207/267
C07D 209/48
C07D 211/14
C07D 211/42
C07D 211/52
C07D 211/58
C07D 213/30
C07D 213/32
C07D 213/38
C07D 213/56
C07D 213/64
C07D 213/65
C07D 213/68
C07D 213/70
C07D 213/71
C07D 213/74
C07D 213/75
C07D 213/76
C07D 233/54
C07D 235/06
C07D 237/14
C07D 239/26
C07D 239/42
C07D 241/04
C07D 241/12
C07D 241/18
C07D 253/06
C07D 257/04
C07D 261/02
C07D 263/22
C07D 263/32
C07D 265/30
C07D 277/20
C07D 277/30
C07D 277/36
C07D 277/48
C07D 277/50
C07D 279/12
C07D 295/084
C07D 295/13
C07D 295/155
C07D 295/185
C07D 307/54
C07D 307/81
C07D 317/30
C07D 317/60
C07D 333/18
C07D 333/20
C07D 333/24
C07D 487/08
C07F 9/53
Applicants: UNIVERSITY OF PITTSBURGH
Inventors: SEBTI, Said, M.
HAMILTON, Andrew, D.
AUGERI, David, J.
BARR, Kenneth, J.
DONNER, Bernard, G.
FAKHOURY, Stephen, A.
JANOWICK, David, A.
KALVIN, Douglas, M.
LARSEN, John, J.
LIU, Gang
O'CONNOR, Stephen, J.
ROSENBERG, Saul, H.
SHEN, Wang
SWENSON, Rolf, E.
SORENSEN, Bryan, K.
SULLIVAN, Gerard M.
SZCZEPANKIEWICZ, Bruce G.
TASKER, Andrew S.
WASICK, James I.
WINN, Martin
Title: INHIBITORS OF PROTEIN ISOPRENYL TRANSFERASES
Abstract:
Compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) lower alkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl -L2-, and (i) heterocyclic -L2-; R2 is selected from (a) formula (1), (b) -C(O)NH-CH(R14)-C(O)OR15, (c) formula (2), (d) -C(O)NH-CH(R14)-C(O)NHSO2R16, (e) -C(O)NH-CH(R14)-tetrazolyl, (f) -C(O)NH-heterocyclic, and (g) -C(O)NH-CH(R14)-C(O)NR17R18; R3 is substituted or unsubstituted heterocyclic or aryl, substituted or unsubstituted cycloalkyl or cycloalkenyl, formula (3), and -P(W)R?R3RR3'; R¿4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylalkyl, heterocyclic, or (heterocyclic)alkyl; L1 is absent or is selected from (a) -L4-N(R5)-L5-, (b) -L4-O-L5-, (c) -L4-S(O)n-L5-, (d) -L4-L6-C(W)-N(R5)-L5-, (e) -L4-L6-S(O)m-N(R5)-L5-, (f) -L4-N(R5)-C(W)-L7-L5-, (g) -L4-N(R5)-S(O)p-L7-L5-, (h) optionally substituted alkylene, (i) optionally substituted alkenylene, (j) optionally substituted alkynylene, (k) a covalent bond, (1) formula (4), and (m) formula (5) are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases.