CR20140084A - 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
CR20140084A
CR20140084A CR20140084A CR20140084A CR20140084A CR 20140084 A CR20140084 A CR 20140084A CR 20140084 A CR20140084 A CR 20140084A CR 20140084 A CR20140084 A CR 20140084A CR 20140084 A CR20140084 A CR 20140084A
Authority
CR
Costa Rica
Prior art keywords
bace
derivatives
piridin
dihidro
oxazine
Prior art date
Application number
CR20140084A
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=CR20140084(A) "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 CR20140084A publication Critical patent/CR20140084A/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)
  • 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)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (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)

Abstract

La invención se refiere a novedosos derivados de oxazina de lafórmula (I), y a las sales farmacéuticamente aceptables de losmismos.
CR20140084A 2011-08-25 2014-02-24 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 CR20140084A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161527172P 2011-08-25 2011-08-25
US201261665395P 2012-06-28 2012-06-28

Publications (1)

Publication Number Publication Date
CR20140084A true CR20140084A (es) 2014-05-02

Family

ID=47018309

Family Applications (1)

Application Number Title Priority Date Filing Date
CR20140084A CR20140084A (es) 2011-08-25 2014-02-24 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) ES2638832T3 (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)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101324426B1 (ko) 2008-06-13 2013-10-31 시오노기세야쿠 가부시키가이샤 β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체
KR20120104570A (ko) 2009-12-11 2012-09-21 시오노기세야쿠 가부시키가이샤 옥사진 유도체
DK2663561T3 (en) 2011-01-13 2016-06-06 Novartis Ag New heterocyclic derivatives and their use in treating neurological disorders
WO2014065434A1 (en) * 2012-10-24 2014-05-01 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity
JP6389830B2 (ja) * 2013-03-01 2018-09-12 アムジエン・インコーポレーテツド ベータ−セクレターゼ阻害剤としてのパーフルオロ化５，６−ジヒドロ−４ｈ−１，３−オキサジン−２−アミン化合物および使用方法
JP6374889B2 (ja) 2013-03-08 2018-08-15 アムジエン・インコーポレーテツド β−セクレターゼ阻害剤としての過フッ素化シクロプロピル縮合１，３−オキサジン−２−アミン化合物、及び使用方法
AU2014253275B2 (en) 2013-04-11 2018-10-18 F. Hoffmann-La Roche Ag BACE1 inhibitors
JO3318B1 (ar) 2013-06-18 2019-03-13 Lilly Co Eli مثبطات bace
GEAP201814248A (en) * 2014-02-19 2018-04-10 H Lundbeck As 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
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
US11471449B2 (en) 2015-02-25 2022-10-18 Prilenia Neurotherapeutics Ltd. Use of pridopidine to improve cognitive function and for treating Alzheimer's disease
MX378579B (es) * 2015-02-25 2025-03-11 Prilenia Neurotherapeutics Ltd Uso de pridopidina para mejorar la funcion cognitiva y para tratamiento de enfermedad de alzheimer.
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
JP2018531889A (ja) 2015-08-12 2018-11-01 ハー・ルンドベック・アクチエゼルスカベット Ｂａｃｅ１阻害剤としての２−アミノ−３−フルオロ−３−（フルオロメチル）−６−メチル−６−フェニル−３，４，５，６−テトラヒドロピリジン
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
EP3555086B1 (en) 2016-12-15 2021-09-01 Amgen Inc. 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide 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.
MA54101A (fr) 2016-12-15 2021-10-27 Amgen Inc Dérivés de thiazine et d'oxazine bicycliques en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation
MA52722A (fr) 2016-12-15 2021-04-14 Amgen Inc Dérivés d'oxazine en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation
CA3098430A1 (en) 2018-04-27 2019-10-31 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
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

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL6911868A (es) 1968-08-31 1970-03-03
WO2003006426A1 (en) * 2001-07-13 2003-01-23 Axxima Pharmaceuticals Ag Aromatic guanylhydrazones as effective compounds against neurodiseases
TW200303742A (en) 2001-11-21 2003-09-16 Novartis Ag Organic compounds
CA2514733A1 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
KR100909918B1 (ko) 2003-05-20 2009-07-29 노파르티스 아게 과산화소체 증식체-활성화 수용체의 리간드로서의 ｎ-아실질소 헤테로환
CN101346357B (zh) 2005-10-25 2014-04-02 盐野义制药株式会社 氨基二氢噻嗪衍生物
EP2689780A1 (en) * 2007-04-24 2014-01-29 Shionogi & Co., Ltd. Intermediates for aminodihydrothiazine derivatives substituted with a cyclic group
JP5383483B2 (ja) 2007-04-24 2014-01-08 塩野義製薬株式会社 アルツハイマー症治療用医薬組成物
CN102186841A (zh) * 2008-10-22 2011-09-14 盐野义制药株式会社 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物
WO2010063718A1 (en) 2008-12-02 2010-06-10 ETH Zürich Screening assay for metabolic disease therapeuticals
US8461160B2 (en) * 2009-05-08 2013-06-11 Hoffmann-La Roche, Inc. Dihydropyrimidinones
GB0912778D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydro-oxazine derivatives
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
US7964594B1 (en) 2009-12-10 2011-06-21 Hoffmann-La Roche Inc. Amino oxazine derivatives
KR20120104570A (ko) 2009-12-11 2012-09-21 시오노기세야쿠 가부시키가이샤 옥사진 유도체
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
CN103596569A (zh) 2011-01-13 2014-02-19 诺瓦提斯公司 用于治疗代谢障碍的bace-2抑制剂
SG191710A1 (en) 2011-01-21 2013-08-30 Eisai R&D Man Co Ltd Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives
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
US8754075B2 (en) 2011-04-11 2014-06-17 Hoffmann-La Roche Inc. 1,3-oxazines as BACE1 and/or BACE2 inhibitors
CN103608345A (zh) 2011-04-26 2014-02-26 盐野义制药株式会社 噁嗪衍生物和含有该噁嗪衍生物的bace1抑制剂
US8785436B2 (en) 2011-05-16 2014-07-22 Hoffmann-La Roche Inc. 1,3-oxazines as BACE 1 and/or BACE2 inhibitors
AU2012266544A1 (en) 2011-06-07 2013-11-21 F. Hoffmann-La Roche Ag 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.

Also Published As

Publication number Publication date
AU2012298177B2 (en) 2015-10-29
ES2565229T3 (es) 2016-04-01
GT201400031A (es) 2015-02-19
US9163011B2 (en) 2015-10-20
JP5816369B2 (ja) 2015-11-18
EA024580B1 (ru) 2016-09-30
ES2638832T3 (es) 2017-10-24
MA35356B1 (fr) 2014-08-01
TN2014000062A1 (en) 2015-07-01
UY34278A (es) 2013-04-05
US20150150877A1 (en) 2015-06-04
MX2014002230A (es) 2014-04-25
KR101601571B1 (ko) 2016-03-08
SG2014012108A (en) 2014-05-29
CA2845093A1 (en) 2013-02-28
EA201490491A1 (ru) 2014-06-30
MX339303B (es) 2016-05-19
EP3023423A1 (en) 2016-05-25
AP2014007507A0 (en) 2014-03-31
PE20141540A1 (es) 2014-10-31
US20130172331A1 (en) 2013-07-04
AU2012298177A1 (en) 2014-03-06
EP2748162A1 (en) 2014-07-02
AR087668A1 (es) 2014-04-09
CN103906748A (zh) 2014-07-02
TW201313706A (zh) 2013-04-01
BR112014004131A2 (pt) 2017-06-13
ZA201401139B (en) 2014-12-23
PH12014500356A1 (en) 2014-04-07
EP3023423B1 (en) 2017-05-31
PL2748162T3 (pl) 2016-06-30
JP2014524463A (ja) 2014-09-22
KR20140054313A (ko) 2014-05-08
IL230975A0 (en) 2014-03-31
CL2014000458A1 (es) 2014-09-05
WO2013027188A1 (en) 2013-02-28
CN103906748B (zh) 2017-06-16
CO6890097A2 (es) 2014-03-10
EP2748162B1 (en) 2015-12-16
HK1195903A1 (en) 2014-11-28
NZ621093A (en) 2015-05-29

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