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1. WO2007140980 - PYRROLIDINE DERIVATIVES USEFUL AS BACE INHIBITORS

Publication Number WO/2007/140980
Publication Date 13.12.2007
International Application No. PCT/EP2007/004959
International Filing Date 04.06.2007
IPC
C07D 215/48 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
215Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
16with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
48Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
A61K 31/47 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
435having six-membered rings with one nitrogen as the only ring hetero atom
47Quinolines; Isoquinolines
A61P 25/28 2006.01
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
CPC
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 25/28
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 215/48
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
215Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
16with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
48Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
Applicants
  • NOVARTIS AG [CH]/[CH] (AllExceptUS)
  • ROGEL, Olivier [FR]/[FR] (UsOnly)
  • RONDEAU, Jean-Michel [FR]/[FR] (UsOnly)
  • RUEEGER, Heinrich [CH]/[CH] (UsOnly)
  • SIMIC, Oliver [DE]/[CH] (UsOnly)
  • SIROCKIN, Finton [FR]/[FR] (UsOnly)
  • TINTELNOT-BLOMLEY, Marina [DE]/[DE] (UsOnly)
Inventors
  • ROGEL, Olivier
  • RONDEAU, Jean-Michel
  • RUEEGER, Heinrich
  • SIMIC, Oliver
  • SIROCKIN, Finton
  • TINTELNOT-BLOMLEY, Marina
Agents
  • VOEGELI-LANGE, Regina
Priority Data
0611064.705.06.2006GB
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PYRROLIDINE DERIVATIVES USEFUL AS BACE INHIBITORS
(FR) DÉRIVÉS DE LA PYRROLIDINE UTILISABLES EN TANT QU'INHIBITEURS DE BACE
Abstract
(EN)
Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (= disorder) that depends on the activity of beta-secretase and/or the generation of beta-amyloid and the subsequent aggregation into oligomers and fibrils; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on the activity of beta-secretase and/or the generation of beta-amyloid and the subsequent aggregation into oligomers and fibrils; the use of a compound of that class in the treatment of a disease that depends on the activity of beta- secretase and/or the generation of beta-amyloid and the subsequent aggregation into oligomers and fibrils; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound. The substituted pyrrolidine compounds are especially of the formula (I), wherein the substituents are as defined in the specification.
(FR)
La présente invention concerne des nouveaux composés de pyrrolidine porteurs de 3-mono-, 3,4-di- ou 3,4,4-tri-substitutions, lesdits composés étant utilisables pour le diagnostic et le traitement thérapeutique d'un animal homéotherme, en particulier pour le traitement d'une maladie (= affection) qui dépend de l'activité de la bêta-secrétase et/ou de la génération de bêta-amyloïde et l'agrégation subséquente en oligomères et en fibrilles. L'invention concerne également l'utilisation d'un composé de cette classe pour la préparation d'une formulation pharmaceutique destinée au traitement d'une maladie qui dépend de l'activité de la bêta-secrétase et/ou de la génération de bêta-amyloïde et l'agrégation subséquente en oligomères et en fibrilles ; l'utilisation d'un composé de cette classe pour le traitement d'une maladie qui dépend de l'activité de la bêta-secrétase et/ou de la génération de bêta-amyloïde et l'agrégation subséquente en oligomères et en fibrilles ; des formulations pharmaceutiques comprenant un desdits composés de pyrrolidine porteurs de substitutions et/ou un procédé de traitement comprenant l'administration d'un desdits composés de pyrrolidine porteurs de substitutions. Les composés de pyrrolidine porteurs de substitutions répondent en particulier à la formule (I), dans laquelle les substituants sont tels que définis dans la spécification.
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