MA38457A1 - Compounds based on 1,3-oxazin-2-amine fused with perfluorinated cyclopropyl for use as beta-secretase inhibitors and methods of use thereof - Google Patents

Compounds based on 1,3-oxazin-2-amine fused with perfluorinated cyclopropyl for use as beta-secretase inhibitors and methods of use thereof

Info

Publication number
MA38457A1
MA38457A1 MA38457A MA38457A MA38457A1 MA 38457 A1 MA38457 A1 MA 38457A1 MA 38457 A MA38457 A MA 38457A MA 38457 A MA38457 A MA 38457A MA 38457 A1 MA38457 A1 MA 38457A1
Authority
MA
Morocco
Prior art keywords
compounds
beta
relates
bace
oxazin
Prior art date
Application number
MA38457A
Other languages
French (fr)
Inventor
Wenyuan Qian
Ana Elena Minatti
Jonathan D Low
Jennifer R Allen
Albert Amegadzie
James Brown
Michael J Frohn
Angel Guzman-Perez
Paul E Harrington
Patricia Lopez
Vu Van Ma
Nobuko Nishimura
Shannon Rumfelt
Robert M Rzasa
Kelvin Sham
Adrian L Smith
Ryan White
Qiufen Xue
Original Assignee
Amgen Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Amgen Inc filed Critical Amgen Inc
Priority claimed from PCT/US2014/021412 external-priority patent/WO2014138484A1/en
Publication of MA38457A1 publication Critical patent/MA38457A1/en

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

La présente invention concerne des composés de 1,3-oxazin-2-amine fusionnée avec du cyclopropyle perfluoré, utilisables en tant qu'inhibiteurs de la bêta-sécrétase et leurs procédés d'utilisation. La présente invention concerne donc une classe inédite de composés pouvant être utilisés en vue de la modulation de l'activité d'une enzyme, la bêta-sécrétase (bace). Lesdits composés sont représentés par la formule générale i : [formule a inserer ici], dans laquelle les variables a4, a5, a6, a8, chacun des ra, rb, r1, r2, r3 et r7 de la formule i sont chacun tels que définis ici. L'invention concerne également des compositions pharmaceutiques contenant lesdits composés et l'utilisation desdits composés et compositions en vue du traitement d'affections et/ou d'états pathologiques associés à la formation et au dépôt de plaques bêta-amyloïde, résultant de l'activité biologique de la bace. Lesdites affections à médiation par la bace comprennent, par exemple, la maladie d'alzheimer, les déficits cognitifs, les troubles cognitifs, la schizophrénie et d'autres affections touchant le système nerveux central. L'invention concerne, en outre, des composés de formule ii et iii et leurs modes de réalisation avec leurs sous-formules, des intermédiaires et des procédés de préparation des composés selon l'invention.The present invention relates to 1,3-oxazin-2-amine compounds fused with perfluorinated cyclopropyl, useful as beta-secretase inhibitors and methods of use thereof. The present invention thus relates to an unprecedented class of compounds that can be used to modulate the activity of an enzyme, beta-secretase (bace). Said compounds are represented by the general formula i: [formula to be inserted here], in which the variables a4, a5, a6, a8, each of the ra, rb, r1, r2, r3 and r7 of the formula i are each such that defined here. The invention also relates to pharmaceutical compositions containing said compounds and the use of said compounds and compositions for the treatment of conditions and / or pathological conditions associated with the formation and deposition of beta-amyloid plaques resulting from the biological activity of the bace. Such bace-mediated conditions include, for example, Alzheimer's disease, cognitive deficits, cognitive disorders, schizophrenia, and other diseases affecting the central nervous system. The invention further relates to compounds of formulas ii and iii and their embodiments with their sub-formulas, intermediates and processes for the preparation of the compounds according to the invention.

MA38457A 2013-03-08 2014-03-06 Compounds based on 1,3-oxazin-2-amine fused with perfluorinated cyclopropyl for use as beta-secretase inhibitors and methods of use thereof MA38457A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361775380P 2013-03-08 2013-03-08
PCT/US2014/021412 WO2014138484A1 (en) 2013-03-08 2014-03-06 Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use

Publications (1)

Publication Number Publication Date
MA38457A1 true MA38457A1 (en) 2017-02-28

Family

ID=56119031

Family Applications (1)

Application Number Title Priority Date Filing Date
MA38457A MA38457A1 (en) 2013-03-08 2014-03-06 Compounds based on 1,3-oxazin-2-amine fused with perfluorinated cyclopropyl for use as beta-secretase inhibitors and methods of use thereof

Country Status (2)

Country Link
AR (1) AR095207A1 (en)
MA (1) MA38457A1 (en)

Also Published As

Publication number Publication date
AR095207A1 (en) 2015-09-30

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