Global Patent Index - EP 0986539 A1

EP 0986539 A1 2000-03-22 - DNA-BINDING PYRROLE AND IMIDAZOLE POLYAMIDE DERIVATIVES

Title (en)

DNA-BINDING PYRROLE AND IMIDAZOLE POLYAMIDE DERIVATIVES

Title (de)

DNA-BINDENDE PYRROL- UND IMIDAZOLPOLYAMIDDERIVATE

Title (fr)

DERIVES DE POLYAMIDES PYRROLE-IMIDAZOLE LIANT L'ADN

Publication

EP 0986539 A1 (EN)

Application

EP 98918047 A

Priority

  • US 9806997 W
  • US 4344497 P
  • US 4344697 P
  • US 4202297 P
  • US 83752497 A
  • US 85352297 A
  • US 9712722 W

Abstract (en)

[origin: WO9849142A1] Novel small molecule polyamides of Formula (I) that specifically bind with subnanomolar affinity to any predetermined sequence in the human genome with potential use in molecular biology and human medicine are described. Further, the designed compounds which target the minor groove of B-form double helical DNA offer a general approach for the control of gene-expression. Simple rules are disclosed which provide for rational control of the DNA-binding sequence specificity of synthetic polyamides containing N-methylpyrrole and N-methylimidazole amino acids. A series of molecular templates for polyamide design are disclosed which provide for small molecules which recognize predetermined DNA sequences with affinities and specificities comparable to sequence specific DNA-binding proteins such as transcription factors.

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

C07D 207/34; A61K 31/415; C07D 233/90; C07D 403/14

IPC 8 full level (invention and additional information)

C07D 233/90 (2006.01); A61K 31/415 (2006.01); A61K 31/4164 (2006.01); A61K 47/48 (2006.01); A61P 43/00 (2006.01); C07D 207/34 (2006.01); C07D 403/14 (2006.01); C07D 413/14 (2006.01); C07K 5/078 (2006.01); C07K 7/04 (2006.01); C08G 69/00 (2006.01); C12Q 1/68 (2006.01)

CPC (invention and additional information)

C07D 403/14 (2013.01); A61K 47/48315 (2013.01); C07D 207/34 (2013.01); C07D 233/90 (2013.01); C07K 5/06139 (2013.01); C07K 5/06182 (2013.01); C07K 7/04 (2013.01); C08G 69/00 (2013.01); C12Q 1/6839 (2013.01)

Citation (search report)

See references of WO 9849142A1

Designated contracting state (EPC)

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

EPO simple patent family

WO 9849142 A1 19981105; CA 2286232 A1 19981105; EP 0986539 A1 20000322; JP 2002515063 A 20020521

INPADOC legal status


2008-03-19 [18R] REFUSED

- Effective date: 20071108

2001-07-18 [17Q] FIRST EXAMINATION REPORT

- Effective date: 20010605

2000-03-22 [17P] REQUEST FOR EXAMINATION FILED

- Effective date: 19991011

2000-03-22 [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 MC NL PT SE