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1. WO2011000915 - ISOFORM-SELECTIVE HCN BLOCKERS

Publication Number WO/2011/000915
Publication Date 06.01.2011
International Application No. PCT/EP2010/059369
International Filing Date 01.07.2010
IPC
C07D 223/16 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
223Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
14condensed with carbocyclic rings or ring systems
16Benzazepines; Hydrogenated benzazepines
C07D 401/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/55 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
55having seven-membered rings, e.g. azelastine, pentylenetetrazole
CPC
C07D 223/16
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
223Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
14condensed with carbocyclic rings or ring systems
16Benzazepines; Hydrogenated benzazepines
C07D 401/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
Applicants
  • UNIVERSITA' DEGLI STUDI DI FIRENZE [IT]/[IT] (AllExceptUS)
  • ROMANELLI, Maria Novella [IT]/[IT] (UsOnly)
  • MUGELLI, Alessandro [IT]/[IT] (UsOnly)
  • CERBAI, Elisabetta [IT]/[IT] (UsOnly)
  • SARTIANI, Laura [IT]/[IT] (UsOnly)
  • DEL LUNGO, Martina [IT]/[IT] (UsOnly)
  • MELCHIORRE, Michele [IT]/[IT] (UsOnly)
Inventors
  • ROMANELLI, Maria Novella
  • MUGELLI, Alessandro
  • CERBAI, Elisabetta
  • SARTIANI, Laura
  • DEL LUNGO, Martina
  • MELCHIORRE, Michele
Agents
  • GERVASI, Gemma
Priority Data
FI2009A00014101.07.2009IT
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) ISOFORM-SELECTIVE HCN BLOCKERS
(FR) BLOQUEURS SÉLECTIFS D'ISOFORMES DE HCN
Abstract
(EN)
The present invention relates to compounds of formula (I) as isoform-selective HCN blockers. In particular said compounds showed diverse capabilities of blocking selectively isoforms HCN1, HCN2 and HCN4 expressed in HEK cells. The invention further relates to the medical use of said compounds or as pharmacological or drug-development tools.
(FR)
La présente invention a pour objet des composés de formule (I) en tant que bloqueurs sélectifs d'isoformes de HCN. En particulier, lesdits composés ont présenté diverses capacités de blocage sélectif des isoformes HCNl, HCN2 et HCN4 exprimées dans les cellules HEK. La présente invention concerne en outre l'utilisation médicale desdits composés ou en tant qu'outils pharmacologiques ou de développement de médicaments.
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