BR112012013175A2 - 2-amino-5,5-diflúor-5,6-di-hidro-4h-oxazinas como inibidores de bace 1 e/ou bace 2 - Google Patents

2-amino-5,5-diflúor-5,6-di-hidro-4h-oxazinas como inibidores de bace 1 e/ou bace 2

Info

Publication number
BR112012013175A2
BR112012013175A2 BR112012013175A BR112012013175A BR112012013175A2 BR 112012013175 A2 BR112012013175 A2 BR 112012013175A2 BR 112012013175 A BR112012013175 A BR 112012013175A BR 112012013175 A BR112012013175 A BR 112012013175A BR 112012013175 A2 BR112012013175 A2 BR 112012013175A2
Authority
BR
Brazil
Prior art keywords
bace
oxazines
difluoro
dihydro
inhibitors
Prior art date
Application number
BR112012013175A
Other languages
English (en)
Portuguese (pt)
Inventor
V Mayweg Alexander
Banner David
Pinard Emmanuel
Power Eoin
Hilpert Hans
Mauser Harald
Rogers-Evans Mark
Narquizian Robert
Woltering Thomas
Guba Wolfgang
Wostl Wolfgang
Original Assignee
F Hoffmann La Rocha Ag
Siena Biotech Spa
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=43585547&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BR112012013175(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by F Hoffmann La Rocha Ag, Siena Biotech Spa filed Critical F Hoffmann La Rocha Ag
Publication of BR112012013175A2 publication Critical patent/BR112012013175A2/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/06—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings
    • C07D265/08—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Psychology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
BR112012013175A 2009-12-11 2010-12-06 2-amino-5,5-diflúor-5,6-di-hidro-4h-oxazinas como inibidores de bace 1 e/ou bace 2 BR112012013175A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP09178983 2009-12-11
PCT/EP2010/068912 WO2011069934A1 (en) 2009-12-11 2010-12-06 2-amino-5, 5-difluoro-5, 6-dihydro-4h-oxazines as bace 1 and/or bace 2 inhibitors

Publications (1)

Publication Number Publication Date
BR112012013175A2 true BR112012013175A2 (pt) 2019-09-24

Family

ID=43585547

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112012013175A BR112012013175A2 (pt) 2009-12-11 2010-12-06 2-amino-5,5-diflúor-5,6-di-hidro-4h-oxazinas como inibidores de bace 1 e/ou bace 2

Country Status (26)

Country Link
US (1) US8389513B2 (https=)
EP (1) EP2509965A1 (https=)
JP (1) JP5584778B2 (https=)
KR (1) KR101506773B1 (https=)
CN (1) CN102712609A (https=)
AR (1) AR079327A1 (https=)
AU (1) AU2010330031B2 (https=)
BR (1) BR112012013175A2 (https=)
CA (1) CA2776727C (https=)
CL (1) CL2012001464A1 (https=)
CO (1) CO6541656A2 (https=)
CR (1) CR20120262A (https=)
EC (1) ECSP12011961A (https=)
IL (1) IL219107A (https=)
IN (1) IN2012DN03043A (https=)
MA (1) MA34779B1 (https=)
MX (1) MX2012006493A (https=)
MY (1) MY169962A (https=)
NZ (1) NZ599008A (https=)
PE (1) PE20121500A1 (https=)
PH (1) PH12012500619A1 (https=)
RU (1) RU2515221C2 (https=)
SG (1) SG181610A1 (https=)
TW (1) TWI487704B (https=)
UA (1) UA103272C2 (https=)
WO (1) WO2011069934A1 (https=)

Families Citing this family (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2416603C9 (ru) 2005-10-25 2012-06-20 Сионоги Энд Ко., Лтд. Производные аминодигидротиазина
EP2147914B1 (en) 2007-04-24 2014-06-04 Shionogi&Co., Ltd. Aminodihydrothiazine derivatives substituted with cyclic groups
EP2151435A4 (en) 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
WO2009151098A1 (ja) 2008-06-13 2009-12-17 塩野義製薬株式会社 βセクレターゼ阻害作用を有する含硫黄複素環誘導体
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
UY32799A (es) 2009-07-24 2011-02-28 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
EP2485920B1 (en) 2009-10-08 2016-04-27 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
EP2485590B1 (en) 2009-10-08 2015-01-07 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
US8563543B2 (en) 2009-10-08 2013-10-22 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
TWI488852B (zh) 2009-12-11 2015-06-21 Shionogi & Co 衍生物
KR101730937B1 (ko) 2010-06-09 2017-04-27 얀센 파마슈티카 엔.브이. 베타-세크레타아제(ｂａｃｅ) 저해제로 유용한 5,6-디하이드로-2ｈ-[1,4]옥사진-3-일-아민 유도체
JP5766198B2 (ja) 2010-10-29 2015-08-19 塩野義製薬株式会社 縮合アミノジヒドロピリミジン誘導体
JP5816630B2 (ja) 2010-10-29 2015-11-18 塩野義製薬株式会社 ナフチリジン誘導体
EP2643325A1 (en) 2010-11-23 2013-10-02 Amgen Inc. Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use
SG191097A1 (en) 2010-12-22 2013-08-30 Janssen Pharmaceutica Nv 5,6-DIHYDRO-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
US8524897B2 (en) 2011-01-12 2013-09-03 Novartis Ag Crystalline oxazine derivative
PT2663561E (pt) 2011-01-13 2016-06-07 Novartis Ag Derivados heterocíclicos novos e sua utilização no tratamento de distúrbios neurológicos
TWI547482B (zh) 2011-01-25 2016-09-01 陶氏農業科學公司 增加可回收之3-氯-4,5,6-三氟-2-氰吡啶之量的改良方法
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
EP2683721B1 (en) 2011-03-09 2015-01-28 Janssen Pharmaceutica N.V. 3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
EP2694489B1 (en) 2011-04-07 2017-09-06 Merck Sharp & Dohme Corp. C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2694521B1 (en) 2011-04-07 2015-11-25 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
US8754075B2 (en) * 2011-04-11 2014-06-17 Hoffmann-La Roche Inc. 1,3-oxazines as BACE1 and/or BACE2 inhibitors
JP2014514302A (ja) 2011-04-13 2014-06-19 メルク・シャープ・アンド・ドーム・コーポレーション Ｂａｃｅ阻害薬としての５−置換されたイミノチアジン類およびそれのモノおよびジオキシド、組成物およびそれらの使用
TW201247635A (en) 2011-04-26 2012-12-01 Shionogi & Co Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them
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
CN103608344B (zh) * 2011-06-07 2016-11-23 霍夫曼-拉罗奇有限公司 [1,3]噁嗪类
BR112013031098A2 (pt) 2011-06-07 2016-12-06 Hoffmann La Roche halogeno-alquil-1,3 oxazinas como inibidores de bace1 e/ou bace2
RU2014111055A (ru) 2011-08-22 2015-09-27 Мерк Шарп И Доум Корп. 2-спирозамещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов bace, композиции и их применение
UY34278A (es) * 2011-08-25 2013-04-05 Novartis Ag Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades
US20130073953A1 (en) * 2011-09-21 2013-03-21 Timothy Onyenobi News headline screenshot viewing system
UA111749C2 (uk) * 2011-12-05 2016-06-10 Янссен Фармацевтика Нв Похідні 6-дифторметил-5,6-дигідро-2h-[1,4]оксазин-3-аміну
UA113538C2 (xx) * 2012-01-26 2017-02-10 Фторметил-5,6-дигідро-4h-$1,3]оксазини
US8338413B1 (en) 2012-03-07 2012-12-25 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
BR112014023384A8 (pt) 2012-03-20 2018-01-16 R Artis Dean inibidores de bace espirocíclicos de di-hidro-tiazina e di-hidro-oxazina, e composições e usos dos mesmos.
PE20150021A1 (es) 2012-05-24 2015-01-28 Hoffmann La Roche 5-amino[1,4]tiazinas como inhibidores de bace1
CA2872181A1 (en) * 2012-06-26 2014-01-03 F. Hoffmann-La Roche Ag Difluoro-hexahydro-cyclopentaoxazinyls and difluoro-hexahydro-benzooxazinyls as bace1 inhibitors
WO2014056816A1 (en) 2012-10-10 2014-04-17 F. Hoffmann-La Roche Ag COMBINATION OF AN Aβ ANTIBODY AND A BACE INHIBITOR
WO2014059185A1 (en) 2012-10-12 2014-04-17 Amgen Inc. Amino - dihydrothiazine and amino - dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use
EP2912035A4 (en) 2012-10-24 2016-06-15 Shionogi & Co DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY
WO2014120658A1 (en) 2013-01-29 2014-08-07 Amgen Inc. Fused multicyclic 3-amino-5,6-dihydro-2h-1,4-thiazine derivatives and their use as beta-secretase inhibitors
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
AP2015008716A0 (en) 2013-03-08 2015-09-30 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
US20160090360A1 (en) * 2013-04-26 2016-03-31 Hoffmann-La Roche Inc. Synthesis of bace inhibitors
WO2014198854A1 (en) 2013-06-12 2014-12-18 Janssen Pharmaceutica Nv 4-amino-6-phenyl-6,7-dihydro[1,2,3]triazolo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace)
CA2912156C (en) 2013-06-12 2021-07-20 Janssen Pharmaceutica Nv 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace)
JO3318B1 (ar) 2013-06-18 2019-03-13 Lilly Co Eli مثبطات bace
WO2015017407A1 (en) 2013-07-30 2015-02-05 Amgen Inc. Bridged bicyclic amino thiazine dioxide compounds as inhibitors of beta- secretase
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
MX2017008083A (es) 2014-12-18 2017-10-31 Janssen Pharmaceutica Nv Compuestos 2,3,4,5-tetrahidropiridin-6-amina y 3,4-dihidro-2h-pirrol-5-amina inhibidores de beta-secretasa.
CR20170426A (es) 2015-03-20 2017-10-23 Hoffmann La Roche Inhibidores de bace 1
WO2017024180A1 (en) 2015-08-06 2017-02-09 Amgen Inc. Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
WO2017061534A1 (en) 2015-10-08 2017-04-13 Shionogi & Co., Ltd. Dihydrothiazine derivatives
WO2018112084A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use
JP7149271B2 (ja) 2016-12-15 2022-10-06 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１，４－チアジンジオキシドおよび１，２，４－チアジアジンジオキシド誘導体ならびに使用方法
US10947223B2 (en) 2016-12-15 2021-03-16 Amgen Inc. Substituted oxazines as beta-secretase inhibitors
JP7149272B2 (ja) 2016-12-15 2022-10-06 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チアジン誘導体および使用方法
EP3555085B1 (en) 2016-12-15 2020-12-02 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
TW202014191A (zh) 2018-04-27 2020-04-16 日商鹽野義製藥股份有限公司 具有選擇性ｂａｃｅ１抑制活性的四氫哌喃并衍生物
CN110747276B (zh) * 2019-11-22 2020-06-30 山东大学齐鲁医院 Bace2作为胶质瘤预后/诊断/治疗标志物的应用

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1156798T3 (da) * 1999-02-09 2003-11-03 Univ Virginia Felbamat-afledte forbindelser
EP1537072A1 (en) * 2002-09-10 2005-06-08 Pharmacia & Upjohn Company LLC Substituted aminoethers for the treatment of alzheimer s disease
CA2505098A1 (en) * 2002-11-12 2004-05-27 Merck & Co., Inc. Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease
CA2526487A1 (en) * 2003-06-30 2005-01-06 Daiichi Pharmaceutical Co., Ltd. Heterocyclic methyl sulfone derivative
JP2008513426A (ja) 2004-09-20 2008-05-01 バイオリポックス エービー 炎症の治療に有用なピラゾール化合物
EP1802587A4 (en) * 2004-10-15 2010-02-17 Astrazeneca Ab SUBSTITUTED AMINO BINDINGS AND THEIR APPLICATIONS
RU2416603C9 (ru) 2005-10-25 2012-06-20 Сионоги Энд Ко., Лтд. Производные аминодигидротиазина
SA08290245B1 (ar) 2007-04-23 2012-02-12 استرازينيكا ايه بي مشتقات كربو كساميد جديدة من -n (8-اريل رباعي هيدرو نفثالين غير متجانس- 2- يل) أو -n (5-اريل كرومان غير متجانس -3-يل) لعلاج الألم
EP2151435A4 (en) 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
EP2147914B1 (en) 2007-04-24 2014-06-04 Shionogi&Co., Ltd. Aminodihydrothiazine derivatives substituted with cyclic groups
RU2476431C2 (ru) 2008-01-18 2013-02-27 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Конденсированное производное аминодигидротиазина
AU2009216825A1 (en) 2008-02-18 2009-08-27 F. Hoffmann-La Roche Ag 4, 5-dihydro-oxazol-2-yl amine derivatives
GB0912778D0 (en) * 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydro-oxazine derivatives
UY32799A (es) 2009-07-24 2011-02-28 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
EP2511269A4 (en) * 2009-12-11 2013-04-24 Shionogi & Co FUSED HETEROCYCLIC COMPOUND HAVING AN AMINO GROUP

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RU2012126989A (ru) 2014-01-20
AR079327A1 (es) 2012-01-18
US20110144097A1 (en) 2011-06-16
TWI487704B (zh) 2015-06-11
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AU2010330031B2 (en) 2013-06-20
IL219107A0 (en) 2012-06-28
CA2776727A1 (en) 2011-06-16
PH12012500619A1 (en) 2012-10-22
UA103272C2 (uk) 2013-09-25
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SG181610A1 (en) 2012-07-30
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