MX339303B - Derivados de 2-amino-4- (piridin-2-il) -5,6-dihidro-4h-1,3-oxazina y su uso como inhibidores de bace-1 y/o bace-2. - Google Patents

Derivados de 2-amino-4- (piridin-2-il) -5,6-dihidro-4h-1,3-oxazina y su uso como inhibidores de bace-1 y/o bace-2.

Info

Publication number
MX339303B
MX339303B MX2014002230A MX2014002230A MX339303B MX 339303 B MX339303 B MX 339303B MX 2014002230 A MX2014002230 A MX 2014002230A MX 2014002230 A MX2014002230 A MX 2014002230A MX 339303 B MX339303 B MX 339303B
Authority
MX
Mexico
Prior art keywords
bace
pyridin
dihydro
inhibitors
amino
Prior art date
Application number
MX2014002230A
Other languages
English (en)
Other versions
MX2014002230A (es
Inventor
Rainer Martin Lueoend
Rainer Machauer
Heinrich Rueeger
Slem Jacob Veenstra
Original Assignee
Novartis Ag
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=47018309&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=MX339303(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of MX2014002230A publication Critical patent/MX2014002230A/es
Publication of MX339303B publication Critical patent/MX339303B/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
    • A61K31/535—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Obesity (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La invención se refiere a novedosos derivados de oxazina de la fórmula (I), y a las sales farmacéuticamente aceptables de los mismos: (ver Fórmula) en donde todas las variables son como se definen en la memoria descriptiva, a composiciones farmacéuticas de los mismos, a combinaciones de los mismos, y a su uso como medicamentos, en particular para el tratamiento de enfermedad de Alzheimer o de diabetes por medio de la inhibición de BACE-1 o BACE-2.
MX2014002230A 2011-08-25 2012-08-23 Derivados de 2-amino-4- (piridin-2-il) -5,6-dihidro-4h-1,3-oxazina y su uso como inhibidores de bace-1 y/o bace-2. MX339303B (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161527172P 2011-08-25 2011-08-25
US201261665395P 2012-06-28 2012-06-28
PCT/IB2012/054269 WO2013027188A1 (en) 2011-08-25 2012-08-23 2 -amino-4 - (pyridin- 2 -yl) - 5, 6 -dihydro-4h- 1, 3 -oxazine derivatives and their use as bace-1 and/or bace - 2 inhibitors

Publications (2)

Publication Number Publication Date
MX2014002230A MX2014002230A (es) 2014-04-25
MX339303B true MX339303B (es) 2016-05-19

Family

ID=47018309

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2014002230A MX339303B (es) 2011-08-25 2012-08-23 Derivados de 2-amino-4- (piridin-2-il) -5,6-dihidro-4h-1,3-oxazina y su uso como inhibidores de bace-1 y/o bace-2.

Country Status (28)

Country Link
US (2) US9163011B2 (es)
EP (2) EP2748162B1 (es)
JP (1) JP5816369B2 (es)
KR (1) KR101601571B1 (es)
CN (1) CN103906748B (es)
AP (1) AP2014007507A0 (es)
AR (1) AR087668A1 (es)
AU (1) AU2012298177B2 (es)
BR (1) BR112014004131A2 (es)
CA (1) CA2845093A1 (es)
CL (1) CL2014000458A1 (es)
CO (1) CO6890097A2 (es)
CR (1) CR20140084A (es)
EA (1) EA024580B1 (es)
ES (2) ES2565229T3 (es)
GT (1) GT201400031A (es)
HK (1) HK1195903A1 (es)
IL (1) IL230975A0 (es)
MA (1) MA35356B1 (es)
MX (1) MX339303B (es)
PE (1) PE20141540A1 (es)
PL (1) PL2748162T3 (es)
SG (1) SG2014012108A (es)
TN (1) TN2014000062A1 (es)
TW (1) TW201313706A (es)
UY (1) UY34278A (es)
WO (1) WO2013027188A1 (es)
ZA (1) ZA201401139B (es)

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EP2663561B1 (en) 2011-01-13 2016-03-16 Novartis AG Novel heterocyclic derivatives and their use in the treatment of neurological disorders
WO2014065434A1 (en) * 2012-10-24 2014-05-01 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity
EP2961749B1 (en) * 2013-03-01 2019-10-09 Amgen Inc. Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
CA2903215C (en) 2013-03-08 2021-07-20 Amgen Inc. Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
MA38556A1 (fr) * 2013-04-11 2017-09-29 Hoffmann La Roche Inhibiteurs de bace1
JO3318B1 (ar) 2013-06-18 2019-03-13 Lilly Co Eli مثبطات bace
US20170066741A1 (en) 2014-02-19 2017-03-09 H. Lundbeck A/S 2-Amino-3,5,5-Trifluoro-3,4,5,6-Tetrahydropyridines as BACE1 Inhibitors for Treatment of Alzheimer's Disease
TW201623295A (zh) 2014-04-11 2016-07-01 塩野義製藥股份有限公司 具有ｂａｃｅ１抑制活性之二氫噻及二氫衍生物
US9550762B2 (en) 2014-08-08 2017-01-24 Amgen, Inc. Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
JO3458B1 (ar) 2014-11-10 2020-07-05 H Lundbeck As 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1
MA40941A (fr) 2014-11-10 2017-09-19 H Lundbeck As 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1
CR20170187A (es) 2014-11-10 2018-02-01 H Lundbeck As 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer
CA2977264C (en) * 2015-02-25 2021-12-07 Teva Pharmaceuticals International Gmbh Use of pridopidine to improve cognitive function and for treating alzheimer's disease
US11471449B2 (en) 2015-02-25 2022-10-18 Prilenia Neurotherapeutics Ltd. Use of pridopidine to improve cognitive function and for treating Alzheimer's disease
TW201717948A (zh) 2015-08-10 2017-06-01 Ｈ 朗德貝克公司 包括給予２－胺基－３，５，５－三氟－３，４，５，６－四氫吡啶的聯合治療
PE20181015A1 (es) 2015-08-12 2018-06-26 H Lundbeck As 2-amino-3-fluoro-3-(fluorometil)-6-meti-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1
JP6616525B2 (ja) * 2016-03-01 2019-12-04 エフ．ホフマン−ラ ロシュ アーゲー Ｂａｃｅ１阻害剤
WO2018112081A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Oxazine derivatives as beta-secretase inhibitors and methods of use
EP3555106B1 (en) 2016-12-15 2022-03-09 Amgen Inc. Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use
EP3555085B1 (en) 2016-12-15 2020-12-02 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
CA3047288A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Thiazine derivatives as beta-secretase inhibitors and methods of use
US11021493B2 (en) 2016-12-15 2021-06-01 Amgen Inc. 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use
AU2019258575A1 (en) 2018-04-27 2020-10-29 Shionogi & Co., Ltd. Tetrahydropyranooxazine derivatives having selective BACE1 inhibitory activity
CN109725092A (zh) * 2019-03-19 2019-05-07 北京和合医学诊断技术股份有限公司 检测血液中齐拉西酮含量的液相色谱分析方法
CN113173852B (zh) * 2021-04-26 2022-07-12 深圳市华先医药科技有限公司 二氟丙二酸酯类化合物的制备方法

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Also Published As

Publication number Publication date
EP3023423B1 (en) 2017-05-31
TN2014000062A1 (en) 2015-07-01
JP2014524463A (ja) 2014-09-22
KR101601571B1 (ko) 2016-03-08
EA024580B1 (ru) 2016-09-30
IL230975A0 (en) 2014-03-31
MX2014002230A (es) 2014-04-25
GT201400031A (es) 2015-02-19
US20150150877A1 (en) 2015-06-04
SG2014012108A (en) 2014-05-29
AU2012298177B2 (en) 2015-10-29
KR20140054313A (ko) 2014-05-08
CR20140084A (es) 2014-05-02
US20130172331A1 (en) 2013-07-04
ES2638832T3 (es) 2017-10-24
AR087668A1 (es) 2014-04-09
UY34278A (es) 2013-04-05
US9163011B2 (en) 2015-10-20
JP5816369B2 (ja) 2015-11-18
CA2845093A1 (en) 2013-02-28
CO6890097A2 (es) 2014-03-10
CN103906748B (zh) 2017-06-16
PE20141540A1 (es) 2014-10-31
WO2013027188A1 (en) 2013-02-28
EA201490491A1 (ru) 2014-06-30
PL2748162T3 (pl) 2016-06-30
ZA201401139B (en) 2014-12-23
NZ621093A (en) 2015-05-29
BR112014004131A2 (pt) 2017-06-13
ES2565229T3 (es) 2016-04-01
EP2748162A1 (en) 2014-07-02
EP2748162B1 (en) 2015-12-16
TW201313706A (zh) 2013-04-01
CN103906748A (zh) 2014-07-02
EP3023423A1 (en) 2016-05-25
AP2014007507A0 (en) 2014-03-31
AU2012298177A1 (en) 2014-03-06
MA35356B1 (fr) 2014-08-01
CL2014000458A1 (es) 2014-09-05
HK1195903A1 (en) 2014-11-28

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