Title:
BENZIMIDAZOLE DERIVATIVES AS INHIBITORS OF GLUTAMINYL CYCLASE
Document Type and Number:
WIPO Patent Application WO/2011/131748
Kind Code:
A3
Abstract:
The invention relates to novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
Inventors:
HEISER ULRICH (DE)
RAMSBECK DANIEL (DE)
HOFFMANN TORSTEN (DE)
BOEHME LIVIA (DE)
RAMSBECK DANIEL (DE)
HOFFMANN TORSTEN (DE)
BOEHME LIVIA (DE)
Application Number:
PCT/EP2011/056396
Publication Date:
March 15, 2012
Filing Date:
April 21, 2011
Export Citation:
Assignee:
PROBIODRUG AG (DE)
HEISER ULRICH (DE)
RAMSBECK DANIEL (DE)
HOFFMANN TORSTEN (DE)
BOEHME LIVIA (DE)
HEISER ULRICH (DE)
RAMSBECK DANIEL (DE)
HOFFMANN TORSTEN (DE)
BOEHME LIVIA (DE)
International Classes:
C07D209/08; A61K31/4184; A61P25/00; C07D401/12; C07D405/04; C07D405/12; C07D409/04; C07D409/12; C07D417/12; C07D417/14
Domestic Patent References:
| WO2008055950A1 | 2008-05-15 | |||
| WO2001005770A1 | 2001-01-25 | |||
| WO2008128985A1 | 2008-10-30 |
Foreign References:
| JPS6224244A | 1987-02-02 | |||
| JPS63250385A | 1988-10-18 |
Other References:
SYED ABUZAR ET AL: "Synthesis of N-Aryl- & N-Heteroaryl-benzimidazoles as Potential Anthelmintics", INDIAN JOURNAL OF CHEMISTRY. SECTION B: ORGANIC AND MEDICINAL CHEMISTRY, COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH (C S I R), IN, vol. 19B, 1 July 1980 (1980-07-01), pages 599 - 600, XP009137828, ISSN: 0376-4699
PETER T. GALLAGHER, BRIAN IDDON, HANS SUSCHITZKY, J. CHEM. SOC., PERKIN TRANS. 1, 1980, pages 2362 - 2370, XP009150380
DATABASE REGISTRY [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; 21 April 2009 (2009-04-21), XP002651033, retrieved from STN Database accession no. 1137428-36-4
DATABASE REGISTRY [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; 2 November 2008 (2008-11-02), XP002651034, retrieved from STN Database accession no. 1069857-25-5
ISTVAN MOLNAR: "In 4,5-Stellung ungleich substituierteo-Nitraniline", HELVETICA CHIMICA ACTA, vol. 46, no. 5, 1 January 1963 (1963-01-01), pages 1779 - 1783, XP055002977, ISSN: 0018-019X, DOI: 10.1002/hlca.19630460537
PETER T. GALLAGHER, BRIAN IDDON, HANS SUSCHITZKY, J. CHEM. SOC., PERKIN TRANS. 1, 1980, pages 2362 - 2370, XP009150380
DATABASE REGISTRY [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; 21 April 2009 (2009-04-21), XP002651033, retrieved from STN Database accession no. 1137428-36-4
DATABASE REGISTRY [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; 2 November 2008 (2008-11-02), XP002651034, retrieved from STN Database accession no. 1069857-25-5
ISTVAN MOLNAR: "In 4,5-Stellung ungleich substituierteo-Nitraniline", HELVETICA CHIMICA ACTA, vol. 46, no. 5, 1 January 1963 (1963-01-01), pages 1779 - 1783, XP055002977, ISSN: 0018-019X, DOI: 10.1002/hlca.19630460537
Attorney, Agent or Firm:
HOFFMANN, Matthias (Weinbergweg 22, Halle / Saale, DE)
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