Global Patent Index - EP 1034154 A1

EP 1034154 A1 2000-09-13 - A SOLID-PHASE TECHNOLOGY FOR THE PREPARATION OF COMBINATORIAL LIBRARIES THROUGH AMIDE-BOND ANCHORING

Title (en)

A SOLID-PHASE TECHNOLOGY FOR THE PREPARATION OF COMBINATORIAL LIBRARIES THROUGH AMIDE-BOND ANCHORING

Title (de)

FESTPHASENTECHNOLOGIE ZUR HERSTELLUNG VON KOMBINATORISCHEN BIBLIOTHEKEN DURCH AMIDBINDUNGKNÜPFUNG

Title (fr)

TECHNOLOGIE EN PHASE SOLIDE POUR L'ELABORATION DE BIBLIOTHEQUES COMBINATOIRES PAR VIA ANCRAGE PAR LIAISON AMIDE

Publication

EP 1034154 A1 (EN)

Application

EP 98956988 A

Priority

  • GB 9803523 W
  • GB 9724853 A
  • GB 9808744 A

Abstract (en)

[origin: WO9926902A1] The present invention provides the means to suppress epimerisation of the C alpha terminal amino acid of a protected peptide sequence during coupling by using the protection moiety shown in (1) which is referred to as a "precursor linker". This moiety has a number of features; the functional group R and the 2-hydroxyl function lie in a para position relative to each other while the ether residue lies in a para position relative to the aldehyde residue. R1 is an electron donating alkyl group. The R group is a moiety that may readily be interconverted between electron-withdrawing and electron donating. This is based on the safety catch principle. The principle, that a stable bond is smoothly converted to a labile one at a convenient point during a synthesis, has been applied in peptide chemistry for the development of linkers and protecting groups. One approach has been to exploit the facile reductive conversion of a sulphoxide to sulphide. This approach when applied to the precursor linker (1) provides the functional protection moieties which are referred to as "linker compounds".

IPC 1-7 (main, further and additional classification)

C07B 61/00; C07C 59/74; C07K 1/04

IPC 8 full level (invention and additional information)

C07B 61/00 (2006.01); C07C 59/74 (2006.01); C07C 323/22 (2006.01); C07C 323/52 (2006.01); C07K 1/04 (2006.01); C08G 85/00 (2006.01); C40B 40/02 (2006.01); C40B 40/14 (2006.01); C40B 50/00 (2006.01); C40B 50/06 (2006.01)

CPC (invention and additional information)

C07K 1/047 (2013.01); C07C 59/74 (2013.01); C07K 1/042 (2013.01); C40B 40/00 (2013.01); Y02P 20/55 (2015.11)

Citation (search report)

See references of WO 9926902A1

Designated contracting state (EPC)

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

EPO simple patent family

WO 9926902 A1 19990603; AU 1342099 A 19990615; AU 734992 B2 20010628; CA 2311490 A1 19990603; EP 1034154 A1 20000913; JP 2001524457 A 20011204

INPADOC legal status


2002-12-11 [18W] WITHDRAWN

- Date of withdrawal: 20021018

2000-10-25 [RAP3] CORRECTION OF THE ADDRESS OR NAME OF APPLICANT (A DOCUMENT)

- Owner name: MEDIVIR UK LTD

2000-09-20 [RAP1] TRANSFER OF RIGHTS OF AN EP PUBLISHED APPLICATION

- Owner name: MEDIVIR UK LTD

2000-09-13 [17P] REQUEST FOR EXAMINATION FILED

- Effective date: 20000626

2000-09-13 [AK] DESIGNATED CONTRACTING STATES:

- Kind Code of Ref Document: A1

- Designated State(s): AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU NL PT SE