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1. WO2009012205 - INHIBITORS OF BETA AMYLOID PRODUCTION

Publication Number WO/2009/012205
Publication Date 22.01.2009
International Application No. PCT/US2008/069942
International Filing Date 14.07.2008
IPC
C07C 311/17 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
311Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
15Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
16having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
17to an acyclic carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
C07D 333/34 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
333Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
02not condensed with other rings
04not substituted on the ring sulfur atom
26with 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
30Hetero atoms other than halogen
34Sulfur atoms
A61K 31/18 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
16Amides, e.g. hydroxamic acids
18Sulfonamides
A61K 31/381 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
38having sulfur as a ring hetero atom
381having five-membered rings
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
C07C 311/17
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
311Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
15Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
16having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
17to an acyclic carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
C07D 333/34
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
333Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
02not condensed with other rings
04not substituted on the ring sulfur
26with 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
30Hetero atoms other than halogen
34Sulfur atoms
Applicants
  • WYETH [US]/[US] (AllExceptUS)
  • CAGGIANO, Thomas, J. [US]/[US] (UsOnly)
  • MORRIS, Koi, M. [US]/[US] (UsOnly)
  • HARRISON, Boyd, L. [US]/[US] (UsOnly)
  • KREFT, Anthony, F., III [US]/[US] (UsOnly)
  • KUBRAK, Dennis, M. [US]/[US] (UsOnly)
  • SPRINGER, Dane, M. [US]/[US] (UsOnly)
Inventors
  • CAGGIANO, Thomas, J.
  • MORRIS, Koi, M.
  • HARRISON, Boyd, L.
  • KREFT, Anthony, F., III
  • KUBRAK, Dennis, M.
  • SPRINGER, Dane, M.
Agents
  • KODROFF, Cathy A.
Priority Data
60/959,67516.07.2007US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) INHIBITORS OF BETA AMYLOID PRODUCTION
(FR) INHIBITEURS DE PRODUCTION DE BÊTA AMYLOÏDE
Abstract
(EN)
Novel sulfonamide compounds useful in the treatment of conditions related to the production of beta-amyloid are described, as are routes to their preparation. The sulfonamide compounds are of the following structure, wherein R4-R3 are defined herein. Also provided are pharmaceutical compositions containing these compounds and/or prodrugs of these compounds and a physiologically compatible carrier. These compounds are specifically useful for inhibiting beta amyloid production, and treating Alzheimer's Disease, amyloid angiopathy, cerebral amyloid angiopathy, systemic amyloidosis, hereditary cerebral hemorrhage with amyloidosis of the Dutch type, inclusion body myositis, mild cognitive impairment (MCI) and Down's syndrome.
(FR)
L'invention concerne de nouveaux composés sulfonamide utiles dans le traitement d'affections liées à la production de bêta amyloïde, ainsi que des voies pour leur préparation. Les composés sulfonamide ont la structure suivante, dans laquelle R4 et R3 sont définis ici. Sont également proposés des compositions pharmaceutiques contenant ces composés et/ou des promédicaments de ces composés et un support physiologiquement compatible. Ces composés sont spécialement utiles pour inhiber la production de bêta amyloïde et traiter la maladie d'Alzheimer, une angiopathie d'amyloïde, une angiopathie amyloïde cérébrale, une amyloïdose systémique, une hémorragie cérébrale héréditaire avec amyloïdose du type Dutch, y compris myosite corporelle, trouble cognitif léger (MCI) et syndrome de Down.
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