IN2012DN03043A - - Google Patents

Download PDF

Info

Publication number
IN2012DN03043A
IN2012DN03043A IN3043DEN2012A IN2012DN03043A IN 2012DN03043 A IN2012DN03043 A IN 2012DN03043A IN 3043DEN2012 A IN3043DEN2012 A IN 3043DEN2012A IN 2012DN03043 A IN2012DN03043 A IN 2012DN03043A
Authority
IN
India
Prior art keywords
present
bace1
oxazin
difluoro
alzheimer
Prior art date
Application number
Other languages
English (en)
Inventor
David Banner
Wolfgang Guba
Hans Hilpert
Harald Mauser
Alexander V Mayweg
Robert Narquizian
Emmanuel Pinard
Eoin Power
Mark Rogers-Evans
Thomas Woltering
Wolfgang Wostl
Original Assignee
Hoffmann La Roche
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=IN2012DN03043(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche, Siena Biotech Spa filed Critical Hoffmann La Roche
Publication of IN2012DN03043A publication Critical patent/IN2012DN03043A/en

Links

Classifications

    • 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)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Psychology (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)
IN3043DEN2012 2009-12-11 2010-12-06 IN2012DN03043A (enrdf_load_stackoverflow)

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
IN2012DN03043A true IN2012DN03043A (enrdf_load_stackoverflow) 2015-07-31

Family

ID=43585547

Family Applications (1)

Application Number Title Priority Date Filing Date
IN3043DEN2012 IN2012DN03043A (enrdf_load_stackoverflow) 2009-12-11 2010-12-06

Country Status (26)

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

Families Citing this family (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2572263T3 (es) 2005-10-25 2016-05-31 Shionogi & Co Derivados de dihidrooxazina y tetrahidropirimidina como inhibidores de BACE 1
US8653067B2 (en) 2007-04-24 2014-02-18 Shionogi & Co., Ltd. Pharmaceutical composition for treating Alzheimer's disease
US8168630B2 (en) 2007-04-24 2012-05-01 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives substituted with a cyclic group
JP5490692B2 (ja) 2008-06-13 2014-05-14 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
JPWO2010047372A1 (ja) 2008-10-22 2012-03-22 塩野義製薬株式会社 Ｂａｃｅ１阻害活性を有する２−アミノピリミジン−４−オンおよび２−アミノピリジン誘導体
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
WO2011044187A1 (en) 2009-10-08 2011-04-14 Schering Corporation Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
AU2010328975B2 (en) 2009-12-11 2015-01-22 Shionogi & Co. Ltd. Oxazine derivative
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
EP2634186A4 (en) 2010-10-29 2014-03-26 Shionogi & Co naphthyridine
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
US8957083B2 (en) 2010-11-23 2015-02-17 Amgen Inc. Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use
EP2655376B1 (en) 2010-12-22 2017-08-23 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
DK2663561T3 (en) 2011-01-13 2016-06-06 Novartis Ag New heterocyclic derivatives and their use in treating neurological disorders
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
BR112013022917A2 (pt) 2011-03-09 2016-12-06 Janssen Pharmaceutica Nv derivados 3,4-dihidro-pirrolo[1,2-a]pirazino-1-ilamina úteis como inibidores de 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
WO2012139425A1 (en) 2011-04-13 2012-10-18 Schering Corporation 5-substituted iminothiazines and their mono-and dioxides as bace inhibitors,compositions,and their use
JPWO2012147763A1 (ja) * 2011-04-26 2014-07-28 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
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
CA2837252A1 (en) 2011-06-07 2012-12-13 F. Hoffmann-La Roche Ag Halogen-alkyl-1,3 oxazines as bace1 and/or bace2 inhibitors
RU2599256C2 (ru) * 2011-06-07 2016-10-10 Ф. Хоффманн-Ля Рош Аг [1,3]оксазины
CN103874496A (zh) 2011-08-22 2014-06-18 默沙东公司 作为bace抑制剂的2-螺-取代的亚氨基噻嗪类及其单和二氧化物、组合物及其用途
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
AU2013211646B2 (en) * 2012-01-26 2017-09-14 F. Hoffmann-La Roche Ag Fluoromethyl-5,6-dihydro-4h-[1,3]oxazines
US8338413B1 (en) 2012-03-07 2012-12-25 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
HK1206597A1 (en) 2012-03-20 2016-01-15 艾朗制药股份有限公司 Spirocyclic dihydro-thiazine and dihydro-oxazine bace inhibitors, and compositions and uses thereof
KR20150014934A (ko) * 2012-05-24 2015-02-09 에프. 호프만-라 로슈 아게 Bace1 억제제로서의 5-아미노[1,4]티아진
MA37763B1 (fr) * 2012-06-26 2017-05-31 Hoffmann La Roche Difluoro-hexahydro-cyclopentaoxazinyles et difluoro-hexahydro-benzooxazinyles en tant qu'inhibiteurs de bace1
WO2014056816A1 (en) 2012-10-10 2014-04-17 F. Hoffmann-La Roche Ag COMBINATION OF AN Aβ ANTIBODY AND A BACE INHIBITOR
US9556135B2 (en) 2012-10-12 2017-01-31 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
MX366855B (es) * 2013-03-01 2019-07-26 Amgen Inc Compuestos perfluorados de 5,6-dihidro-4h-1,3-oxazin-2-amina como inhibidores de beta-secretasa y metodos de uso.
EP2964644B1 (en) 2013-03-08 2018-12-26 Amgen, Inc. Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
KR102247765B1 (ko) 2013-04-11 2021-05-06 에프. 호프만-라 로슈 아게 Bace1 억제제
WO2014173917A1 (en) * 2013-04-26 2014-10-30 F. Hoffmann-La Roche Ag Synthesis of bace1 inhibitors
MX368326B (es) 2013-06-12 2019-09-27 Janssen Pharmaceutica Nv Derivados de 4-amino-6-fenil-5,6-dihidroimidazo[1,5-a]pirazin-3(2h )-ona como inhibidores de beta-secretasa (bace).
AU2014280125B2 (en) 2013-06-12 2018-03-15 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)
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
WO2016022724A1 (en) 2014-08-08 2016-02-11 Amgen Inc. Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
CN107108582B (zh) 2014-12-18 2019-10-18 詹森药业有限公司 β-分泌酶的2，3，4，5-四氢吡啶-6-胺化合物抑制剂
PE20171349A1 (es) 2015-03-20 2017-09-13 Hoffmann La Roche Inhibidores de bace1
US10246429B2 (en) 2015-08-06 2019-04-02 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
MX388696B (es) 2016-12-15 2025-03-20 Amgen Inc Derivados de oxazina como inhibidores de beta secretasa y metodos de uso.
US10889579B2 (en) 2016-12-15 2021-01-12 Amgen Inc. Thiazine derivatives as β-secretase inhibitors and methods of use
CA3047287A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Cyclopropyl fused thiazine 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
US11548903B2 (en) 2016-12-15 2023-01-10 Amgen Inc. Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use
WO2019208693A1 (en) 2018-04-27 2019-10-31 Shionogi & Co., Ltd. Tetrahydropyranooxazine derivatives having selective bace1 inhibitory activity
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
JP2002536409A (ja) * 1999-02-09 2002-10-29 ユニバーシティ オブ バージニア パテント ファウンデーション フェルバメートから誘導される化合物
MXPA05002705A (es) * 2002-09-10 2005-09-08 Pharmacia & Upjohn Co Llc Aminoeteres sustituidos para el tratamiento de la enfermedad de alzheimer.
CA2505098A1 (en) * 2002-11-12 2004-05-27 Merck & Co., Inc. Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease
RU2336270C2 (ru) * 2003-06-30 2008-10-20 Дайити Фармасьютикал Ко., Лтд. Гетероциклические метилсульфоновые производные
US20070225318A1 (en) 2004-09-20 2007-09-27 Biolipox Ab Pyrazole Compounds Useful In The Treatment Of Inflammation
JP2008516945A (ja) * 2004-10-15 2008-05-22 アストラゼネカ・アクチエボラーグ 置換されたアミノ化合物およびそれらの使用
ES2572263T3 (es) 2005-10-25 2016-05-31 Shionogi & Co Derivados de dihidrooxazina y tetrahidropirimidina como inhibidores de BACE 1
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
US8653067B2 (en) 2007-04-24 2014-02-18 Shionogi & Co., Ltd. Pharmaceutical composition for treating Alzheimer's disease
US8168630B2 (en) 2007-04-24 2012-05-01 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives substituted with a cyclic group
BRPI0906962B8 (pt) 2008-01-18 2021-05-25 Eisai R&D Man Co Ltd composto de aminodiidrotiazina fundido
JP5258904B2 (ja) 2008-02-18 2013-08-07 エフ．ホフマン−ラ ロシュ アーゲー ４，５−ジヒドロオキサゾール−２−イルアミン誘導体
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
JPWO2011071109A1 (ja) * 2009-12-11 2013-04-22 塩野義製薬株式会社 アミノ基を有する縮合ヘテロ環化合物

Also Published As

Publication number Publication date
BR112012013175A2 (pt) 2019-09-24
NZ599008A (en) 2013-08-30
RU2012126989A (ru) 2014-01-20
CA2776727C (en) 2016-05-31
JP2013513563A (ja) 2013-04-22
UA103272C2 (uk) 2013-09-25
SG181610A1 (en) 2012-07-30
JP5584778B2 (ja) 2014-09-03
KR20120104598A (ko) 2012-09-21
CO6541656A2 (es) 2012-10-16
TW201124408A (en) 2011-07-16
AR079327A1 (es) 2012-01-18
CR20120262A (es) 2012-07-27
WO2011069934A1 (en) 2011-06-16
RU2515221C2 (ru) 2014-05-10
ECSP12011961A (es) 2012-07-31
EP2509965A1 (en) 2012-10-17
CN102712609A (zh) 2012-10-03
CA2776727A1 (en) 2011-06-16
MY169962A (en) 2019-06-19
MX2012006493A (es) 2012-07-03
US8389513B2 (en) 2013-03-05
PE20121500A1 (es) 2012-11-05
AU2010330031A1 (en) 2012-06-07
MA34779B1 (fr) 2014-01-02
AU2010330031B2 (en) 2013-06-20
US20110144097A1 (en) 2011-06-16
CL2012001464A1 (es) 2014-03-07
TWI487704B (zh) 2015-06-11
IL219107A (en) 2015-10-29
IL219107A0 (en) 2012-06-28
KR101506773B1 (ko) 2015-03-27
PH12012500619A1 (en) 2012-10-22

Similar Documents

Publication Publication Date Title
IN2012DN03043A (enrdf_load_stackoverflow)
IN2012DN00766A (enrdf_load_stackoverflow)
PH12013502090A1 (en) 1,3 oxazines as bace1 and/or bace2 inhibitors
MX2013007558A (es) 1,4-oxazinas como inhibidores de los genes enzima de segmentacion de la proteina precursora del sitio 1 y/o 2 (bace1 y/o bace2).
PH12013502156A1 (en) 1,3-oxazines as bace1 and/or bace2 inhibitors
WO2012104263A3 (en) 1,4 oxazines as bace1 and/or bace2 inhibitors
MX2013008478A (es) 1, 4 riazepinas/sulfonas como inhibidores de beta secretasa 1 (base1) y/o beta secretasa 2 (bace2).
MX2013014007A (es) [1,3] oxazinas.
PH12013502316A1 (en) Halogen-alkyl-1,3 oxazines as bace1 and/or bace2 inhibitors
MX2013008213A (es) N-[3-(5-amino-3,3a,7,7a-tetrahidro-1h-2,4-dioxa-6-aza-inden-7-il) -fenil]-amidas como inhibidores de beta-secretasa 1 (bace1) y/o beta-secretasa 2 (bace2).
PH12013502262A1 (en) Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as bace1 and/or bace2 inhibitors
MX2013014194A (es) 1,3-tiazepinas fusionadas a ciclopropilo como inhibidores de beta-secretasa 1 (bace) y/o beta-secretasa 2 (bace 2).
MX2014003408A (es) N-(3-(2-amino-6,6-difluor-4,4a,5,6,7,7a-hexahidro-ciclopenta-[e][ 1,3]oxazin-4-il)-fenil)-amidas como inhibidores de la beta-secretasa 1 (bace1).
PH12014501334A1 (en) Fluoromethyl-5,6-dihydro-4h-[1,3]oxazines
MX2012012952A (es) Compuestos de 2, 5, 6, 7,-tetrahidro-[1, 4] oxazepin-3-ilamina o 2, 3, 6, 7-tetrahidro-[1, 4] oxazepin-5-ilamina.
NZ596579A (en) Bace inhibitors
MX2009007411A (es) Derivados de espiropiperidina-glicinamida.
MX2013008056A (es) 1,4-oxazepinas como inhibidores de beta-secretasa 1 (bace1) y/o beta-secretasa 2 (bace2).
PH12014502541A1 (en) 5-amino [1,4] thiazines as bace 1 inhibitors
MX2013002398A (es) Inhibidores de beta-secretasa (base) para su uso en tratamiento de diabetes.