MA35356B1 - Dérivés de 2-amino-4-(pyridine-2-yl)-5,6-dihydro-4h-1,3-oxazine, et leur utilisation comme inhibiteurs de bace1 et bace2 - Google Patents

Dérivés de 2-amino-4-(pyridine-2-yl)-5,6-dihydro-4h-1,3-oxazine, et leur utilisation comme inhibiteurs de bace1 et bace2

Info

Publication number
MA35356B1
MA35356B1 MA36766A MA36766A MA35356B1 MA 35356 B1 MA35356 B1 MA 35356B1 MA 36766 A MA36766 A MA 36766A MA 36766 A MA36766 A MA 36766A MA 35356 B1 MA35356 B1 MA 35356B1
Authority
MA
Morocco
Prior art keywords
bace2
bace1
oxazine
pyridin
dihydro
Prior art date
Application number
MA36766A
Other languages
English (en)
Inventor
Rainer Martin Lueoend
Rainer Machauer
Heinrich Rueeger
Siem 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=MA35356(B1) "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 MA35356B1 publication Critical patent/MA35356B1/fr

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)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Child & Adolescent Psychology (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)

Abstract

La présente invention concerne de nouveaux dérivés d'oxazine représentés par la formule (i) et certains de leurs sels pharmaceutiquement admis, formule dans laquelle les variables sont telles que définies dans la spécification. L'invention concerne également certaines de leurs compositions pharmaceutiques, de leurs combinaisons, et leur utilisation comme médicaments, en particulier pour le traitement de la maladie d'alzheimer ou du diabète par inhibition de bace1 ou bace2.
MA36766A 2011-08-25 2014-02-20 Dérivés de 2-amino-4-(pyridine-2-yl)-5,6-dihydro-4h-1,3-oxazine, et leur utilisation comme inhibiteurs de bace1 et bace2 MA35356B1 (fr)

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 (fr) 2011-08-25 2012-08-23 Dérivés de 2-amino-4-(pyridine-2-yl)-5,6-dihydro-4h-1,3-oxazine, et leur utilisation comme inhibiteurs de bace1 et bace2

Publications (1)

Publication Number Publication Date
MA35356B1 true MA35356B1 (fr) 2014-08-01

Family

ID=47018309

Family Applications (1)

Application Number Title Priority Date Filing Date
MA36766A MA35356B1 (fr) 2011-08-25 2014-02-20 Dérivés de 2-amino-4-(pyridine-2-yl)-5,6-dihydro-4h-1,3-oxazine, et leur utilisation comme inhibiteurs de bace1 et bace2

Country Status (28)

Country Link
US (2) US9163011B2 (fr)
EP (2) EP3023423B1 (fr)
JP (1) JP5816369B2 (fr)
KR (1) KR101601571B1 (fr)
CN (1) CN103906748B (fr)
AP (1) AP2014007507A0 (fr)
AR (1) AR087668A1 (fr)
AU (1) AU2012298177B2 (fr)
BR (1) BR112014004131A2 (fr)
CA (1) CA2845093A1 (fr)
CL (1) CL2014000458A1 (fr)
CO (1) CO6890097A2 (fr)
CR (1) CR20140084A (fr)
EA (1) EA024580B1 (fr)
ES (2) ES2565229T3 (fr)
GT (1) GT201400031A (fr)
IL (1) IL230975A0 (fr)
MA (1) MA35356B1 (fr)
MX (1) MX339303B (fr)
PE (1) PE20141540A1 (fr)
PH (1) PH12014500356A1 (fr)
PL (1) PL2748162T3 (fr)
SG (1) SG2014012108A (fr)
TN (1) TN2014000062A1 (fr)
TW (1) TW201313706A (fr)
UY (1) UY34278A (fr)
WO (1) WO2013027188A1 (fr)
ZA (1) ZA201401139B (fr)

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KR101569260B1 (ko) 2011-01-13 2015-11-13 노파르티스 아게 신규 헤테로시클릭 유도체 및 신경계 장애의 치료에서의 그의 용도
JP2016501827A (ja) * 2012-10-24 2016-01-21 塩野義製薬株式会社 Ｂａｃｅ１阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体
AU2014223334C1 (en) * 2013-03-01 2018-10-18 Amgen Inc. Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
EP2964644B1 (fr) 2013-03-08 2018-12-26 Amgen, Inc. Composés perfluorés à base de 1,3-oxazin-2-amine condensée avec un cyclopropyle en tant qu'inhibiteurs de la bêta-secrétase et leurs procédés d'utilisation
MY174747A (en) 2013-04-11 2020-05-13 Hoffmann La Roche Bace1 inhibitors
TWI639607B (zh) 2013-06-18 2018-11-01 美國禮來大藥廠 Ｂａｃｅ抑制劑
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
MX381482B (es) 2014-08-08 2025-03-12 Amgen Inc Compuestos de tiazin-2-amina fusionados con ciclopropilo como inhibidores de beta-secretasa y metodos de uso.
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
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US11471449B2 (en) 2015-02-25 2022-10-18 Prilenia Neurotherapeutics Ltd. Use of pridopidine to improve cognitive function and for treating Alzheimer's disease
EP3854785A1 (fr) 2015-02-25 2021-07-28 Prilenia Neurotherapeutics Ltd. Utilisation de pridopidine pour traiter la dépression ou l'anxiété
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
RU2018104868A (ru) 2015-08-12 2019-09-13 Х. Лундбекк А/С 2-амино-3-фтор-3-(фторметил)-6-метил-6-фенил-3,4,5,6-тетрагидропиридины в качестве ингибиторов 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
AU2017376441B2 (en) * 2016-12-15 2021-10-14 Amgen Inc. Oxazine derivatives as beta-secretase inhibitors and methods of use
MX386618B (es) 2016-12-15 2025-03-19 Amgen Inc Derivados de tiazina condensados con ciclopropilo como inhibidores de beta-secretasa y métodos de uso.
MX388697B (es) 2016-12-15 2025-03-20 Amgen Inc Derivados de tiazina como inhibidores de beta-secretasa y metodos de uso.
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.
AU2017376445B2 (en) 2016-12-15 2021-09-30 Amgen Inc. Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use
BR112020021728A2 (pt) 2018-04-27 2021-01-26 Shionogi & Co., Ltd. derivados de tetra-hidropiranooxazina tendo atividade inibitória de bace1 seletiva
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Also Published As

Publication number Publication date
WO2013027188A1 (fr) 2013-02-28
US9163011B2 (en) 2015-10-20
SG2014012108A (en) 2014-05-29
CL2014000458A1 (es) 2014-09-05
EP2748162B1 (fr) 2015-12-16
EP2748162A1 (fr) 2014-07-02
CN103906748B (zh) 2017-06-16
ES2565229T3 (es) 2016-04-01
EA024580B1 (ru) 2016-09-30
AP2014007507A0 (en) 2014-03-31
AR087668A1 (es) 2014-04-09
UY34278A (es) 2013-04-05
BR112014004131A2 (pt) 2017-06-13
TW201313706A (zh) 2013-04-01
AU2012298177A1 (en) 2014-03-06
CR20140084A (es) 2014-05-02
EP3023423A1 (fr) 2016-05-25
CO6890097A2 (es) 2014-03-10
ZA201401139B (en) 2014-12-23
PL2748162T3 (pl) 2016-06-30
JP2014524463A (ja) 2014-09-22
CA2845093A1 (fr) 2013-02-28
AU2012298177B2 (en) 2015-10-29
CN103906748A (zh) 2014-07-02
PH12014500356A1 (en) 2014-04-07
MX2014002230A (es) 2014-04-25
TN2014000062A1 (en) 2015-07-01
IL230975A0 (en) 2014-03-31
EP3023423B1 (fr) 2017-05-31
HK1195903A1 (en) 2014-11-28
KR20140054313A (ko) 2014-05-08
EA201490491A1 (ru) 2014-06-30
MX339303B (es) 2016-05-19
ES2638832T3 (es) 2017-10-24
US20130172331A1 (en) 2013-07-04
NZ621093A (en) 2015-05-29
KR101601571B1 (ko) 2016-03-08
PE20141540A1 (es) 2014-10-31
US20150150877A1 (en) 2015-06-04
JP5816369B2 (ja) 2015-11-18
GT201400031A (es) 2015-02-19

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