AP2014007507A0 - 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 - Google Patents

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

Info

Publication number: AP2014007507A0
Authority: AP; ARIPO
Prior art keywords: bace; pyridin; dihydro; inhibitors; amino
Prior art date: 2011-08-25

Application number

AP2014007507A

Other languages

English (en)

Inventor

Heinrich Rueeger

Rainer Machauer

Rainer Martin Lueoend

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.)

2011-08-25

Filing date

2012-08-23

Publication date

2014-03-31

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=AP2014007507(A0) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2012-08-23 Application filed by Novartis Ag filed Critical Novartis Ag

2014-03-31 Publication of AP2014007507A0 publication Critical patent/AP2014007507A0/xx

Links

SWOJGEXAJRUTCJ-UHFFFAOYSA-N 4-pyridin-2-yl-5,6-dihydro-4h-1,3-oxazin-2-amine Chemical class C1COC(N)=NC1C1=CC=CC=N1 SWOJGEXAJRUTCJ-UHFFFAOYSA-N 0.000 title 1
101150058765 BACE1 gene Proteins 0.000 title 1
239000003112 inhibitor Substances 0.000 title 1

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

AP2014007507A 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 AP2014007507A0 (en)

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 (1)

Publication Number	Publication Date
AP2014007507A0 true AP2014007507A0 (en)	2014-03-31

Family

ID=47018309

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
AP2014007507A AP2014007507A0 (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

Country Status (28)

Country	Link
US (2)	US9163011B2 (es)
EP (2)	EP3023423B1 (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)
IL (1)	IL230975A0 (es)
MA (1)	MA35356B1 (es)
MX (1)	MX339303B (es)
PE (1)	PE20141540A1 (es)
PH (1)	PH12014500356A1 (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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UA110467C2 (uk) †	2009-12-11	2016-01-12	Шионогі Енд Ко., Лтд.	Похідні оксазину
CA2824220C (en)	2011-01-13	2020-09-01	Novartis Ag	Novel heterocyclic derivatives and their use in the treatment of neurological disorders
EP2912035A4 (en)	2012-10-24	2016-06-15	Shionogi & Co	DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY
CA2902212C (en) *	2013-03-01	2020-10-13	Amgen Inc.	Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
AU2014225604B2 (en)	2013-03-08	2018-05-17	Amgen Inc.	Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
PE20151748A1 (es) *	2013-04-11	2015-12-02	Hoffmann La Roche	Inhibidores de bace1
TWI639607B (zh)	2013-06-18	2018-11-01	美國禮來大藥廠	Ｂａｃｅ抑制劑
TW201609700A (zh)	2014-02-19	2016-03-16	Ｈ朗德貝克公司	２－胺基－３，５，５－三氟－３，４，５，６－四氫吡啶作爲ｂａｃｅ１抑制劑用於治療阿茲海默症
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
AU2015301028B2 (en)	2014-08-08	2019-09-26	Amgen Inc.	Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
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
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
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
US10603311B2 (en)	2015-02-25	2020-03-31	Prilenia Neurotherapeutics Ltd.	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
US20180244645A1 (en)	2015-08-12	2018-08-30	H. Lundbeck A/S	2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors
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
CA3047285A1 (en)	2016-12-15	2018-06-21	Amgen Inc.	Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use
MA54100A (fr)	2016-12-15	2021-10-20	Amgen Inc	Dérivés de thiazine en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation
MX387729B (es)	2016-12-15	2025-03-18	Amgen Inc	Derivados de dióxido de 1,4-tiazina y dióxido 1,2,4-tiadiazina como inhibidores de beta-secretasa y métodos de uso.
AU2017378316B2 (en)	2016-12-15	2021-04-01	Amgen Inc.	Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
US10947223B2 (en)	2016-12-15	2021-03-16	Amgen Inc.	Substituted oxazines as beta-secretase inhibitors
US11629154B2 (en)	2018-04-27	2023-04-18	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
US12042492B2 (en)	2020-10-09	2024-07-23	Texas Tech University System	BACE1 inhibitory ligand molecules against amyloid beta-induced synaptic and mitochondrial toxicities
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EA201391033A1 (ru)	2011-01-13	2014-01-30	Новартис Аг	Ингибиторы bace-2 для лечения метаболических расстройств
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WO2012147763A1 (ja)	2011-04-26	2012-11-01	塩野義製薬株式会社	オキサジン誘導体およびそれを含有するｂａｃｅ１阻害剤
US8785436B2 (en)	2011-05-16	2014-07-22	Hoffmann-La Roche Inc.	1,3-oxazines as BACE 1 and/or BACE2 inhibitors
US8987255B2 (en)	2011-06-07	2015-03-24	Hoffmann-La Roche Inc.	Halogen-alkyl-1,3 oxazines as BACE1 and/or BACE2 inhibitors
MX2013014007A (es)	2011-06-07	2014-03-12	Hoffmann La Roche	[1,3] oxazinas.

2012
- 2012-08-20 UY UY0001034278A patent/UY34278A/es not_active Application Discontinuation
- 2012-08-23 ES ES12772462.3T patent/ES2565229T3/es active Active
- 2012-08-23 CN CN201280052486.2A patent/CN103906748B/zh not_active Expired - Fee Related
- 2012-08-23 AP AP2014007507A patent/AP2014007507A0/xx unknown
- 2012-08-23 AU AU2012298177A patent/AU2012298177B2/en not_active Ceased
- 2012-08-23 KR KR1020147007405A patent/KR101601571B1/ko not_active Expired - Fee Related
- 2012-08-23 PE PE2014000256A patent/PE20141540A1/es not_active Application Discontinuation
- 2012-08-23 EA EA201490491A patent/EA024580B1/ru not_active IP Right Cessation
- 2012-08-23 SG SG2014012108A patent/SG2014012108A/en unknown
- 2012-08-23 US US13/592,580 patent/US9163011B2/en active Active
- 2012-08-23 ES ES15197854.1T patent/ES2638832T3/es active Active
- 2012-08-23 EP EP15197854.1A patent/EP3023423B1/en active Active
- 2012-08-23 WO PCT/IB2012/054269 patent/WO2013027188A1/en not_active Ceased
- 2012-08-23 PH PH1/2014/500356A patent/PH12014500356A1/en unknown
- 2012-08-23 PL PL12772462T patent/PL2748162T3/pl unknown
- 2012-08-23 CA CA2845093A patent/CA2845093A1/en not_active Abandoned
- 2012-08-23 BR BR112014004131A patent/BR112014004131A2/pt unknown
- 2012-08-23 EP EP12772462.3A patent/EP2748162B1/en active Active
- 2012-08-23 JP JP2014526591A patent/JP5816369B2/ja not_active Expired - Fee Related
- 2012-08-23 MX MX2014002230A patent/MX339303B/es active IP Right Grant
- 2012-08-24 AR ARP120103130A patent/AR087668A1/es unknown
- 2012-08-24 TW TW101130894A patent/TW201313706A/zh unknown
2014
- 2014-02-11 TN TNP2014000062A patent/TN2014000062A1/en unknown
- 2014-02-13 IL IL230975A patent/IL230975A0/en unknown
- 2014-02-14 ZA ZA2014/01139A patent/ZA201401139B/en unknown
- 2014-02-20 MA MA36766A patent/MA35356B1/fr unknown
- 2014-02-21 CO CO14037398A patent/CO6890097A2/es active IP Right Grant
- 2014-02-24 GT GT201400031A patent/GT201400031A/es unknown
- 2014-02-24 CR CR20140084A patent/CR20140084A/es unknown
- 2014-02-25 CL CL2014000458A patent/CL2014000458A1/es unknown
2015
- 2015-02-05 US US14/615,418 patent/US20150150877A1/en not_active Abandoned

Also Published As

Publication number	Publication date
PH12014500356A1 (en)	2014-04-07
CR20140084A (es)	2014-05-02
ES2565229T3 (es)	2016-04-01
WO2013027188A1 (en)	2013-02-28
EA201490491A1 (ru)	2014-06-30
BR112014004131A2 (pt)	2017-06-13
AU2012298177A1 (en)	2014-03-06
EP3023423A1 (en)	2016-05-25
ES2638832T3 (es)	2017-10-24
KR20140054313A (ko)	2014-05-08
PL2748162T3 (pl)	2016-06-30
EP2748162A1 (en)	2014-07-02
AR087668A1 (es)	2014-04-09
CN103906748A (zh)	2014-07-02
CN103906748B (zh)	2017-06-16
MX2014002230A (es)	2014-04-25
SG2014012108A (en)	2014-05-29
US9163011B2 (en)	2015-10-20
TW201313706A (zh)	2013-04-01
AU2012298177B2 (en)	2015-10-29
CO6890097A2 (es)	2014-03-10
US20150150877A1 (en)	2015-06-04
EA024580B1 (ru)	2016-09-30
US20130172331A1 (en)	2013-07-04
KR101601571B1 (ko)	2016-03-08
MX339303B (es)	2016-05-19
EP2748162B1 (en)	2015-12-16
NZ621093A (en)	2015-05-29
CA2845093A1 (en)	2013-02-28
TN2014000062A1 (en)	2015-07-01
CL2014000458A1 (es)	2014-09-05
EP3023423B1 (en)	2017-05-31
ZA201401139B (en)	2014-12-23
PE20141540A1 (es)	2014-10-31
HK1195903A1 (en)	2014-11-28
MA35356B1 (fr)	2014-08-01
JP2014524463A (ja)	2014-09-22
IL230975A0 (en)	2014-03-31
JP5816369B2 (ja)	2015-11-18
UY34278A (es)	2013-04-05
GT201400031A (es)	2015-02-19

Publication	Publication Date	Title
IL230975A0 (en)	2014-03-31	Derivatives of 2-amino-4 (pyridine-2-yl)-6, 5-dihydro-h4, 1, 3-oxazine and their use as inhibitors of 1-bace and/or 2-bace
ZA201308400B (en)	2014-07-30	1,3-oxazines as bace1 and/or bace2 inhibitors
IL229686A0 (en)	2014-01-30	Halogen -alkyl-1,3 oxazines as bace1 and/or bace2 inhibitors
BR112013016360A2 (pt)	2018-06-26	1,4 oxazinas como inibidores de bace1 e/ou bace2
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