Title:
The macro ring compound by which conformation restrictions were carried out and by which total synthesis was carried out
Document Type and Number:
Japanese Patent JP6111276
Kind Code:
B2
Abstract:
The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.
Inventors:
Daniel Obrecht
Philip Airmelt
Se Umche
Arnaud Pietre
Jean-Francois Gosalves
Marc Tomen
Philip Airmelt
Se Umche
Arnaud Pietre
Jean-Francois Gosalves
Marc Tomen
Application Number:
JP2014561464A
Publication Date:
April 05, 2017
Filing Date:
March 15, 2013
Export Citation:
Assignee:
POLYPHOR AG
International Classes:
C07D273/02; A61K31/395; A61K31/397; A61K31/407; A61K31/4162; A61K31/4178; A61K31/424; A61K31/437; A61K31/439; A61K31/4427; A61K31/529; A61K31/5377; A61P1/00; A61P1/04; A61P3/04; A61P3/10; A61P5/14; A61P7/04; A61P9/00; A61P9/10; A61P9/12; A61P11/00; A61P11/02; A61P11/06; A61P13/08; A61P13/12; A61P15/00; A61P17/00; A61P17/02; A61P17/06; A61P19/00; A61P19/02; A61P21/04; A61P25/00; A61P25/24; A61P25/28; A61P27/02; A61P29/00; A61P31/04; A61P35/00; A61P37/06; A61P37/08; A61P43/00; C07D291/02; C07D413/00; C07D413/12; C07D419/12; C07D498/04; C07D498/14; C07D498/18; C07D498/22; C07D515/08; C07D515/14
Domestic Patent References:
| JP54073194A | ||||
| JP54039087A | ||||
| JP2008531473A |
Foreign References:
| WO2008105526A1 | ||||
| WO2010132163A1 | ||||
| WO2011015241A1 | ||||
| US20080262055 |
Attorney, Agent or Firm:
Samejima Mutsumi
Masahiro Nitta
Kure Hidenori
Nobuhiko Akiyama
Masahiro Nitta
Kure Hidenori
Nobuhiko Akiyama