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
Links
- 150000001875 compounds Chemical class 0.000 title abstract 7
- 238000000034 method Methods 0.000 title abstract 3
- RWRGWJAYHSYMIU-UHFFFAOYSA-N 2H-1,3-oxazin-2-amine Chemical compound NC1OC=CC=N1 RWRGWJAYHSYMIU-UHFFFAOYSA-N 0.000 title abstract 2
- 239000002439 beta secretase inhibitor Substances 0.000 title abstract 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 title abstract 2
- 101150058765 BACE1 gene Proteins 0.000 abstract 3
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000037259 Amyloid Plaque Diseases 0.000 abstract 1
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 abstract 1
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 abstract 1
- 102000013455 Amyloid beta-Peptides Human genes 0.000 abstract 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 230000004071 biological effect Effects 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 210000003169 central nervous system Anatomy 0.000 abstract 1
- 230000007278 cognition impairment Effects 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 230000008021 deposition Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
Landscapes
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (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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