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CO2017007691A2 - Inhibidores de la β-secretasa derivados de la 5-amino-3-(5-(3-isoxazol-5-il)-3-(fluorometil)-6,6-dimetil-1-(metilimino)-3,6-dihidro-2h-1,4-tiazina o 5-amino-3-(5-(1h-1,2,3-triazol-4-il)-2-fluorofenil)-6,6-dimetil-1-(metilimino)-3,6-dihidro-2h-1,4-tiazina composiciones que los comprenden y métodos de elaboración - Google Patents

Inhibidores de la β-secretasa derivados de la 5-amino-3-(5-(3-isoxazol-5-il)-3-(fluorometil)-6,6-dimetil-1-(metilimino)-3,6-dihidro-2h-1,4-tiazina o 5-amino-3-(5-(1h-1,2,3-triazol-4-il)-2-fluorofenil)-6,6-dimetil-1-(metilimino)-3,6-dihidro-2h-1,4-tiazina composiciones que los comprenden y métodos de elaboración

Info

Publication number
CO2017007691A2
CO2017007691A2 CONC2017/0007691A CO2017007691A CO2017007691A2 CO 2017007691 A2 CO2017007691 A2 CO 2017007691A2 CO 2017007691 A CO2017007691 A CO 2017007691A CO 2017007691 A2 CO2017007691 A2 CO 2017007691A2
Authority
CO
Colombia
Prior art keywords
methylimino
thiazine
dihydro
dimethyl
amino
Prior art date
Application number
CONC2017/0007691A
Other languages
English (en)
Inventor
Thomas Woltering
Wolfgang Haap
Jens-Uwe Peters
Wolfgang Guba
Cosimo Dolente
Bjoern Bartels
Sander Ulrike Obst
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 CO2017007691A2 publication Critical patent/CO2017007691A2/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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 three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

La presente invención proporciona un compuesto de fórmula I, que presenta una actividad inhibidora de BACE1, su preparación, composiciones farmacéuticas que los contienen y su utilización como sustancias terapéuticamente activas. Los compuestos activos de la presente invención resultan útiles en el tratamiento terapéutico y/o profiláctico de, por ejemplo, la enfermedad de Alzheimer.
CONC2017/0007691A 2015-03-20 2017-07-28 Inhibidores de la β-secretasa derivados de la 5-amino-3-(5-(3-isoxazol-5-il)-3-(fluorometil)-6,6-dimetil-1-(metilimino)-3,6-dihidro-2h-1,4-tiazina o 5-amino-3-(5-(1h-1,2,3-triazol-4-il)-2-fluorofenil)-6,6-dimetil-1-(metilimino)-3,6-dihidro-2h-1,4-tiazina composiciones que los comprenden y métodos de elaboración CO2017007691A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP15160101 2015-03-20
PCT/EP2016/055649 WO2016150785A1 (en) 2015-03-20 2016-03-16 Bace1 inhibitors

Publications (1)

Publication Number Publication Date
CO2017007691A2 true CO2017007691A2 (es) 2017-10-20

Family

ID=52780400

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2017/0007691A CO2017007691A2 (es) 2015-03-20 2017-07-28 Inhibidores de la β-secretasa derivados de la 5-amino-3-(5-(3-isoxazol-5-il)-3-(fluorometil)-6,6-dimetil-1-(metilimino)-3,6-dihidro-2h-1,4-tiazina o 5-amino-3-(5-(1h-1,2,3-triazol-4-il)-2-fluorofenil)-6,6-dimetil-1-(metilimino)-3,6-dihidro-2h-1,4-tiazina composiciones que los comprenden y métodos de elaboración

Country Status (19)

Country Link
US (4) US10047081B2 (es)
EP (1) EP3271355B1 (es)
JP (1) JP6674960B2 (es)
KR (1) KR20170129745A (es)
CN (1) CN107406440B (es)
AU (1) AU2016236402B2 (es)
BR (1) BR112017015474A2 (es)
CA (1) CA2979113A1 (es)
CL (1) CL2017002229A1 (es)
CO (1) CO2017007691A2 (es)
CR (1) CR20170426A (es)
HK (1) HK1244790A1 (es)
IL (1) IL253322A0 (es)
MX (1) MX2017012188A (es)
PE (1) PE20171349A1 (es)
PH (1) PH12017501668A1 (es)
RU (1) RU2712272C2 (es)
SG (1) SG11201707050VA (es)
WO (1) WO2016150785A1 (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2017012188A (es) 2015-03-20 2017-12-15 Hoffmann La Roche Inhibidores de beta-secretasa 1 (bace1).
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
AR115495A1 (es) 2018-06-06 2021-01-27 Syngenta Crop Protection Ag Derivados heterocíclicos con sustituyentes que contienen azufre activos como plaguicidas

Family Cites Families (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19962924A1 (de) 1999-12-24 2001-07-05 Bayer Ag Substituierte Oxazolidinone und ihre Verwendung
MX2010008347A (es) 2008-02-18 2010-11-12 Hoffmann La Roche Derivados de 4,5-dihidro-oxazol-2-ilamina.
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
US7964594B1 (en) 2009-12-10 2011-06-21 Hoffmann-La Roche Inc. Amino oxazine derivatives
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
US8673894B2 (en) 2010-05-07 2014-03-18 Hoffmann-La Roche Inc. 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds
US8815881B2 (en) 2010-08-09 2014-08-26 Hoffmann-La Roche Inc. 1,4,5,6-tetrahydro-pyrimidin-2-ylamine compounds
US20120053200A1 (en) 2010-09-01 2012-03-01 Harald Mauser Bace 2 inhibitors
US9242943B2 (en) 2011-01-18 2016-01-26 Siena Biotech S.P.A. 1,4 oxazines as BACE1 and/or BACE2 inhibitors
US8399459B2 (en) 2011-02-02 2013-03-19 Hoffmann-La Roche Inc. 1,4 oxazines as BACE1 and/or BACE2 inhibitors
US8404680B2 (en) 2011-02-08 2013-03-26 Hoffmann-La Roche Inc. N-[3-(5-amino-3,3a,7,7a-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)-phenyl]-amides as BACE1 and/or BACE2 inhibitors
US8815841B2 (en) 2011-02-18 2014-08-26 Hoffmann-La Roche Inc. 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors
US9067924B2 (en) 2011-03-04 2015-06-30 Hoffmann-La Roche Inc. 1,4 thiazepines/sulfones as BACE1 and/or BACE2 inhibitors
US8748418B2 (en) 2011-03-18 2014-06-10 Hoffmann-La Roche Inc. 1,4-oxazepines as BACE1 and/or BACE2 inhibitors
US8877744B2 (en) 2011-04-04 2014-11-04 Hoffmann-La Roche Inc. 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors
US8754075B2 (en) 2011-04-11 2014-06-17 Hoffmann-La Roche Inc. 1,3-oxazines as BACE1 and/or BACE2 inhibitors
WO2012139425A1 (en) 2011-04-13 2012-10-18 Schering Corporation 5-substituted iminothiazines and their mono-and dioxides as bace inhibitors,compositions,and their use
CN103596939A (zh) * 2011-04-13 2014-02-19 默沙东公司 作为bace抑制剂的5-取代的亚氨基噻嗪类及其单和二氧化物、组合物及其应用
US8785436B2 (en) 2011-05-16 2014-07-22 Hoffmann-La Roche Inc. 1,3-oxazines as BACE 1 and/or BACE2 inhibitors
US9079919B2 (en) 2011-05-27 2015-07-14 Hoffmann-La Roche Inc. Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as BACE1 and/or BACE2 inhibitors
MX2013014007A (es) 2011-06-07 2014-03-12 Hoffmann La Roche [1,3] oxazinas.
WO2012168164A1 (en) 2011-06-07 2012-12-13 F. Hoffmann-La Roche Ag Halogen-alkyl-1,3 oxazines as bace1 and/or bace2 inhibitors
US8927535B2 (en) 2011-07-06 2015-01-06 Hoffman-La Roche Inc. Cyclopropyl-fused-1,3-thiazepines as BACE1 and/or BACE2 inhibitors
US9181236B2 (en) * 2011-08-22 2015-11-10 Merck Sharp & Dohme Corp. 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use
US8476264B2 (en) 2011-09-21 2013-07-02 Hoffmann-La Roche Inc. N-(3-(2-amino-6,6-difluoro-4,4A,5,6,7,7A-hexahydro-cyclopenta[E][1,3]oxazin-4-yl)-phenylamides as BACE1 inhibitors
CN104066727B (zh) 2012-01-26 2019-04-26 霍夫曼-拉罗奇有限公司 氟甲基-5,6-二氢-4h-[1,3]噁嗪类
MX2014013839A (es) * 2012-05-24 2015-02-04 Hoffmann La Roche 5-amino[1,4]tiazinas como inhibidores de beta-secretasa 1 (bace 1).
US9181232B2 (en) 2012-06-26 2015-11-10 Hoffmann-La Roche Inc. Difluoro-hexahydro-cyclopentaoxazinyls and difluoro-hexahydro-benzooxazinyls as BACE1 inhibitors
EP2908825B1 (en) * 2012-10-17 2018-04-18 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
BR112015016315A2 (pt) 2013-01-22 2017-07-11 Hoffmann La Roche fluoro-[1,3]oxazinas como inibidores de bace1
EP2968356B1 (en) 2013-03-15 2018-03-07 Merck Sharp & Dohme Corp. S-imino-s-oxo iminothiadiazine compounds as bace inhibitors, compositions, and their use
WO2014150331A1 (en) * 2013-03-15 2014-09-25 Merck Sharp & Dohme Corp. S-imino-s-oxo iminothiazine compounds as bace inhibitors, compositions, and their use
EP2968353B1 (en) 2013-03-15 2018-12-19 Merck Sharp & Dohme Corp. C2-azaspiro iminothiazine dioxides as bace inhibitors
MX2017012188A (es) * 2015-03-20 2017-12-15 Hoffmann La Roche Inhibidores de beta-secretasa 1 (bace1).

Also Published As

Publication number Publication date
US20180319787A1 (en) 2018-11-08
CN107406440A (zh) 2017-11-28
RU2017134884A (ru) 2019-04-22
US10723729B2 (en) 2020-07-28
US11034687B2 (en) 2021-06-15
EP3271355B1 (en) 2020-07-29
US10047081B2 (en) 2018-08-14
JP6674960B2 (ja) 2020-04-01
IL253322A0 (en) 2017-09-28
US20190337936A1 (en) 2019-11-07
AU2016236402A1 (en) 2017-07-27
WO2016150785A1 (en) 2016-09-29
PH12017501668A1 (en) 2018-03-19
PE20171349A1 (es) 2017-09-13
CL2017002229A1 (es) 2018-04-13
BR112017015474A2 (pt) 2018-01-30
RU2712272C2 (ru) 2020-01-28
EP3271355A1 (en) 2018-01-24
KR20170129745A (ko) 2017-11-27
MX2017012188A (es) 2017-12-15
CR20170426A (es) 2017-10-23
CA2979113A1 (en) 2016-09-29
HK1244790A1 (zh) 2018-08-17
US20200308166A1 (en) 2020-10-01
AU2016236402B2 (en) 2019-08-01
JP2018507879A (ja) 2018-03-22
US20180057485A1 (en) 2018-03-01
RU2017134884A3 (es) 2019-07-17
SG11201707050VA (en) 2017-10-30
US10399969B2 (en) 2019-09-03
CN107406440B (zh) 2021-05-07

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