PE20150021A1 - 5-amino[1,4]tiazinas como inhibidores de bace1 - Google Patents

5-amino[1,4]tiazinas como inhibidores de bace1

Info

Publication number
PE20150021A1
PE20150021A1 PE2014002013A PE2014002013A PE20150021A1 PE 20150021 A1 PE20150021 A1 PE 20150021A1 PE 2014002013 A PE2014002013 A PE 2014002013A PE 2014002013 A PE2014002013 A PE 2014002013A PE 20150021 A1 PE20150021 A1 PE 20150021A1
Authority
PE
Peru
Prior art keywords
alkyl
amino
halogen
thiazines
thiazin
Prior art date
Application number
PE2014002013A
Other languages
English (en)
Inventor
Hans Hilpert
Thomas Woltering
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20150021A1 publication Critical patent/PE20150021A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for 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

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA L, DONDE R1 ES ARILO, HETEROARILO, ENTRE OTROS; R2 ES H, ALQUILO C1-C6 Y HALOGENO; R3 ES ALQUILO C1-C6, HALOGENO-ALQUILO C1-C6; R4 ES ALQUILO C1-C6, HALOGENO-ALQUILO C1-C6, H; R5 ES ALQUILO C1-C6, HALOGENO-ALQUILO C1-C6, H; X ES 0, 2. SON COMPUESTOS PREFERIDOS [3-(( R)-5-AMINO-3-METIL-3,6-DIHIDRO-2H-[1,4]TIAZIN-3-IL)-4-FLUORO-FENIL]-AMIDA DEL ACIDO 5-CIANO-PIRIDIN-2-CARBOXILICO; [3-(( R)-5-AMINO-3-METIL-1,1-DIOXO-1,2,3,6-TETRAHIDRO-1?6-[1,4] TIAZIN-3-IL)-4-FLUORO-FENIL]-AMIDA DEL ACIDO 5-DIFLUOROMETOXI-PIRIDIN-2-CARBOXILICO. DICHO COMPUESTO TIENE ACTIVIDAD INHIBIDORA DE BACE1 Y ES UTIL EN EL TRATAMIENTO TERAPEUTICO Y/O PROFILACTICO DE LA ENFERMEDAD DE ALZHEIMER
PE2014002013A 2012-05-24 2013-05-21 5-amino[1,4]tiazinas como inhibidores de bace1 PE20150021A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP12169353 2012-05-24

Publications (1)

Publication Number Publication Date
PE20150021A1 true PE20150021A1 (es) 2015-01-28

Family

ID=48534350

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2014002013A PE20150021A1 (es) 2012-05-24 2013-05-21 5-amino[1,4]tiazinas como inhibidores de bace1

Country Status (22)

Country Link
US (1) US9273042B2 (es)
EP (1) EP2855469B1 (es)
JP (1) JP6251249B2 (es)
KR (1) KR20150014934A (es)
CN (1) CN104334554B (es)
AU (1) AU2013265376B2 (es)
BR (1) BR112014028813A2 (es)
CA (1) CA2872179A1 (es)
CL (1) CL2014003123A1 (es)
CO (1) CO7131369A2 (es)
CR (1) CR20140495A (es)
EA (1) EA026004B1 (es)
HK (1) HK1201261A1 (es)
IL (1) IL235681A (es)
MA (1) MA37691B1 (es)
MX (1) MX2014013839A (es)
NZ (1) NZ702254A (es)
PE (1) PE20150021A1 (es)
PH (1) PH12014502541A1 (es)
SG (1) SG11201407575PA (es)
UA (1) UA113438C2 (es)
WO (1) WO2013174781A1 (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2012298983A1 (en) * 2011-08-22 2014-02-27 Merck Sharp & Dohme Corp. 2-spiro-substituted iminothiazines and their mono-and dioxides as BACE inhibitors, compositions and their use
WO2014059185A1 (en) 2012-10-12 2014-04-17 Amgen Inc. Amino - dihydrothiazine and amino - dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use
US9096615B2 (en) 2013-07-30 2015-08-04 Amgen Inc. Bridged bicyclic amino thiazine dioxide compounds as inhibitors of beta-secretase and methods of use thereof
US9725468B2 (en) 2013-09-13 2017-08-08 Merck Sharp & Dohme Corp. C5-spiro iminothiazine dioxides as BACE inhibitors, compositions, and their use
EP3215514B1 (en) * 2014-11-03 2018-11-21 F. Hoffmann-La Roche AG Bace1 inhibitors
PE20171349A1 (es) 2015-03-20 2017-09-13 Hoffmann La Roche Inhibidores de bace1
JP6895424B2 (ja) * 2015-08-12 2021-06-30 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft Bace1阻害剤
JP7353708B2 (ja) 2018-04-27 2023-10-02 塩野義製薬株式会社 選択的bace1阻害活性を有するテトラヒドロピラノオキサジン誘導体
CN110467611B (zh) * 2018-05-11 2022-09-27 广东东阳光药业有限公司 亚氨基噻二嗪二氧化物衍生物及其用途

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090221579A1 (en) * 2004-10-15 2009-09-03 Jeffrey Scott Albert Substituted Amino-Compounds and Uses Thereof
US8461160B2 (en) * 2009-05-08 2013-06-11 Hoffmann-La Roche, Inc. Dihydropyrimidinones
US8188079B2 (en) 2009-08-19 2012-05-29 Hoffman-La Roche Inc. 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines
US20110065695A1 (en) * 2009-09-11 2011-03-17 Jeremy Beauchamp Use of aminodihydrothiazines for the treatment or prevention of diabetes
UA103272C2 (uk) * 2009-12-11 2013-09-25 Ф. Хоффманн-Ля Рош Аг 2-аміно-5,5-дифтор-5,6-дигідро-4h-оксазини як інгібітори bace1 і/або bace2
MX2013011947A (es) * 2011-04-13 2014-01-16 Merck Sharp & Dohme Iminotiazinas 5-sustituidas y sus monoxidos y dioxidos como inhibidores de la enzima que encinde la proteina precursora amiloide en el sitio beta, composiciones y su uso.
AU2012298983A1 (en) * 2011-08-22 2014-02-27 Merck Sharp & Dohme Corp. 2-spiro-substituted iminothiazines and their mono-and dioxides as BACE inhibitors, compositions and their use

Also Published As

Publication number Publication date
NZ702254A (en) 2016-08-26
EP2855469B1 (en) 2019-06-19
US20150141413A1 (en) 2015-05-21
UA113438C2 (xx) 2017-01-25
PH12014502541B1 (en) 2015-01-21
IL235681A0 (en) 2015-02-01
CN104334554B (zh) 2017-10-31
EA026004B1 (ru) 2017-02-28
MA37691B1 (fr) 2016-11-30
CA2872179A1 (en) 2013-11-28
AU2013265376B2 (en) 2017-07-20
CL2014003123A1 (es) 2015-02-27
SG11201407575PA (en) 2014-12-30
BR112014028813A2 (pt) 2017-06-27
US9273042B2 (en) 2016-03-01
JP2015517548A (ja) 2015-06-22
EP2855469A1 (en) 2015-04-08
IL235681A (en) 2017-10-31
CN104334554A (zh) 2015-02-04
PH12014502541A1 (en) 2015-01-21
EA201492097A1 (ru) 2015-04-30
AU2013265376A1 (en) 2014-11-13
KR20150014934A (ko) 2015-02-09
HK1201261A1 (en) 2015-08-28
JP6251249B2 (ja) 2017-12-20
WO2013174781A1 (en) 2013-11-28
CR20140495A (es) 2014-12-01
CO7131369A2 (es) 2014-12-01
MX2014013839A (es) 2015-02-04
MA37691A1 (fr) 2016-03-31

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