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 thereofInfo
- 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
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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.
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) |
-
2014
- 2014-03-06 MA MA38457A patent/MA38457A1/en unknown
- 2014-03-10 AR ARP140100815A patent/AR095207A1/en unknown
Also Published As
Publication number | Publication date |
---|---|
AR095207A1 (en) | 2015-09-30 |
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