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1. WO2011006903 - SUBSTITUTED TRIAZOLE AND IMIDAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS

Publication Number WO/2011/006903
Publication Date 20.01.2011
International Application No. PCT/EP2010/060083
International Filing Date 13.07.2010
IPC
C07D 233/60 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
233Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54having two double bonds between ring members or between ring members and non-ring members
56with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
60with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
C07D 401/14 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
14containing three or more hetero rings
C07D 403/10 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02containing two hetero rings
10linked by a carbon chain containing aromatic rings
C07D 487/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/4178 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
41641,3-Diazoles
4178not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
A61K 31/4196 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
41961,2,4-Triazoles
CPC
A61K 31/4196
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
41961,2,4-Triazoles
A61P 25/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
A61P 25/16
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
14for treating abnormal movements, e.g. chorea, dyskinesia
16Anti-Parkinson drugs
A61P 25/28
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
C07D 233/60
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
233Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54having two double bonds between ring members or between ring members and non-ring members
56with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
60with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
Applicants
  • JANSSEN PHARMACEUTICALS, INC [US]/[US] (AllExceptUS)
  • WU, Tongfei [BE]/[BE] (UsOnly)
  • GIJSEN, Henricus, Jacobus, Maria [NL]/[NL] (UsOnly)
  • ROMBOUTS, Frederik, Jan, Rita [BE]/[BE] (UsOnly)
  • BISCHOFF, François, Paul [FR]/[BE] (UsOnly)
  • BERTHELOT, Didier, Jean-Claude [FR]/[BE] (UsOnly)
  • OEHLRICH, Daniel [GB]/[BE] (UsOnly)
  • DE CLEYN, Michel, Anna, Jozef [BE]/[BE] (UsOnly)
  • PIETERS, Serge, Maria, Aloysius [NL]/[NL] (UsOnly)
  • MINNE, Garrett, Berlond [BE]/[BE] (UsOnly)
  • VELTER, Adriana, Ingrid [RO]/[BE] (UsOnly)
  • VAN BRANDT, Sven, Franciscus, Anna [BE]/[BE] (UsOnly)
  • SURKYN, Michel [BE]/[BE] (UsOnly)
Inventors
  • WU, Tongfei
  • GIJSEN, Henricus, Jacobus, Maria
  • ROMBOUTS, Frederik, Jan, Rita
  • BISCHOFF, François, Paul
  • BERTHELOT, Didier, Jean-Claude
  • OEHLRICH, Daniel
  • DE CLEYN, Michel, Anna, Jozef
  • PIETERS, Serge, Maria, Aloysius
  • MINNE, Garrett, Berlond
  • VELTER, Adriana, Ingrid
  • VAN BRANDT, Sven, Franciscus, Anna
  • SURKYN, Michel
Agents
  • QUAGHEBEUR, Luc
Priority Data
09165585.215.07.2009EP
10164625.501.06.2010EP
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) SUBSTITUTED TRIAZOLE AND IMIDAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS
(FR) DÉRIVÉS DE TRIAZOLE ET D'IMIDAZOLE SUBSTITUÉS EN TANT QUE MODULATEURS DE GAMMA SECRÉTASE
Abstract
(EN)
The present invention is concerned with novel substituted triazole and imidazole derivatives of Formula (I) wherein R1, R2, A1, A2, A3, A4, X, and Het1 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
(FR)
La présente invention porte sur de nouveaux dérivés de triazole et d'imidazole substitués de Formule (I) dans laquelle R1, R2, A1, A2, A3, A4, X, et Het1 ont la signification définie dans les revendications. Les composés selon la présente invention sont utiles en tant que modulateurs de gamma secrétase. La présente invention porte en outre sur des procédés pour préparer de tels nouveaux composés, sur des compositions pharmaceutiques comprenant lesdits composés en tant qu'ingrédient actif ainsi que sur l'utilisation desdits composés comme médicament.
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