Global Patent Index - EP 0817630 A1

EP 0817630 A1 19980114 - INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE

Title (en)

INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE

Title (de)

INHIBITOREN DER FARNESYL-PROTEIN TRANSFERASE

Title (fr)

INHIBITEURS DE FARNESYL-PROTEINE TRANSFERASE

Publication

EP 0817630 A1 19980114 (EN)

Application

EP 96910528 A 19960325

Priority

  • US 9603980 W 19960325
  • US 41313795 A 19950329
  • US 41283095 A 19950329

Abstract (en)

[origin: WO9630015A1] The present invention comprises peptidomimetic compounds which comprise a suitably substituted aminoalkylbenzamide moiety. The instant compounds inhibit the farnesyl protein transferase enzyme and the farnesylation of certain proteins. Furthermore, the instant farnesyl protein transferase inhibitors differ from those previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.

IPC 1-7

A61K 31/415; C07C 321/02; C07D 233/56

IPC 8 full level

C07D 233/64 (2006.01); A61K 31/195 (2006.01); A61K 31/215 (2006.01); A61K 31/415 (2006.01); A61P 35/00 (2006.01); A61P 43/00 (2006.01); C07C 323/59 (2006.01); C07D 233/54 (2006.01); C07D 233/56 (2006.01); C07D 521/00 (2006.01)

CPC (source: EP)

A61P 35/00 (2017.12); A61P 43/00 (2017.12); C07C 323/59 (2013.01); C07D 233/64 (2013.01)

Designated contracting state (EPC)

AT BE CH DE DK ES FI FR GB GR IE IT LI LU NL PT SE

DOCDB simple family (publication)

WO 9630015 A1 19961003; AU 5370196 A 19961016; AU 706008 B2 19990603; CA 2216564 A1 19961003; EP 0817630 A1 19980114; EP 0817630 A4 19990127; JP H11503419 A 19990326

DOCDB simple family (application)

US 9603980 W 19960325; AU 5370196 A 19960325; CA 2216564 A 19960325; EP 96910528 A 19960325; JP 52954796 A 19960325