Global Patent Index - EP 0880503 A1

EP 0880503 A1 19981202 - BALANOL ANALOGUES

Title (en)

BALANOL ANALOGUES

Title (de)

BALANOL ANALOGE

Title (fr)

ANALOGUES DE BALANOL

Publication

EP 0880503 A1 19981202 (EN)

Application

EP 97901527 A 19970210

Priority

  • DK 9700058 W 19970210
  • DK 13696 A 19960209

Abstract (en)

[origin: WO9729091A1] The present invention relates to a solid phase methodology for the preparation of a combinatorial library of structural analogues of the natural product balanol (ophiocordin, azepinostatin), which is a protein kinase C (PKC) and protein kinase A (PKA) inhibitor. The method comprises solid-phase synthesis of the analog variants of balanol whereby a high molecular diversity is introduced. The synthetic scheme is based on a retrosynthetic analysis of the native structure which revealed three main building blocks suitable as templates for modification. The dicarboxy-functional moiety can be immobilised to the polymer support either as the monoallyl ester or as the internal anhydride. The libraries produced by the method are especially suited for high throughput screening of potential drug candidates for the treatment of mammals, especially humans.

IPC 1-7

C07D 223/12; A61K 31/55; C07B 61/00

IPC 8 full level

C07D 223/12 (2006.01); C07B 61/00 (2006.01)

CPC (source: EP)

C07D 223/12 (2013.01); C40B 40/00 (2013.01)

Citation (search report)

See references of WO 9729091A1

Designated contracting state (EPC)

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

DOCDB simple family (publication)

WO 9729091 A1 19970814; AU 1540997 A 19970828; EP 0880503 A1 19981202; JP 2000504672 A 20000418

DOCDB simple family (application)

DK 9700058 W 19970210; AU 1540997 A 19970210; EP 97901527 A 19970210; JP 52807397 A 19970210