PE20151794A1 - Compuestos de 1,3-oxazin-2-amina fusionados con ciclopropilo perfluorado como inhibidores de beta-secretasa y metodos de uso - Google Patents

Compuestos de 1,3-oxazin-2-amina fusionados con ciclopropilo perfluorado como inhibidores de beta-secretasa y metodos de uso

Info

Publication number
PE20151794A1
PE20151794A1 PE2015001879A PE2015001879A PE20151794A1 PE 20151794 A1 PE20151794 A1 PE 20151794A1 PE 2015001879 A PE2015001879 A PE 2015001879A PE 2015001879 A PE2015001879 A PE 2015001879A PE 20151794 A1 PE20151794 A1 PE 20151794A1
Authority
PE
Peru
Prior art keywords
beta
perfluorated
oxazin
cyclopropyl
methods
Prior art date
Application number
PE2015001879A
Other languages
English (en)
Inventor
Ana Elena Minatti
Jonathan D Low
Jennifer R Allen
Albert Amegadzie
James Brown
Michael J Frohn
Angel Guzman-Perez
Paul E Harrington
Patricia Lopez
Vu Van Ma
Nobuko Nishimura
Wenyuan Qian
Shannon Rumfelt
Robert M Rzasa
Kelvin Sham
Adrian L Smith
Ryan White
Qiufen Xue
Original Assignee
Amgen Inc
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
Application filed by Amgen Inc filed Critical Amgen Inc
Publication of PE20151794A1 publication Critical patent/PE20151794A1/es

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    • 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
    • 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
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D265/12—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D413/10—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 carbon chain containing aromatic rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Epidemiology (AREA)

Abstract

La presente invencion proporciona una nueva clase de compuestos utiles para modular la actividad de la enzima beta-secretasa (BACE). Los compuestos tienen una formula general I, donde A4, A5, A6 y A8 son N, etc.; Ra y Rb son H,F, etc.; R1 y R2 son H,F, etc.; R3 es alquilo C1-C6; R7 es -NH-R9, etc.; R9 es acetilo, etc. Compuestos preferidos son: N-(3-((1R,5S,6R)-3-amino-5-(difluorometil)-2-oxa-4-azabiciclo[4.1.0]hept-3-en-5-il)-4-fluorofenil)-5-cloro-3-metilpicolinamida; N-(3-((1R,5S,6R)-3-amino-5-(difluorometil)-2-oxa-4-azabiciclo[4.1.0]hept-3-en-5-il)-4-fluorofenil)-5-ciano-3-metilpicolinamida
PE2015001879A 2013-03-08 2014-03-06 Compuestos de 1,3-oxazin-2-amina fusionados con ciclopropilo perfluorado como inhibidores de beta-secretasa y metodos de uso PE20151794A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361775380P 2013-03-08 2013-03-08
US201461939580P 2014-02-13 2014-02-13

Publications (1)

Publication Number Publication Date
PE20151794A1 true PE20151794A1 (es) 2015-12-03

Family

ID=50478936

Family Applications (1)

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PE2015001879A PE20151794A1 (es) 2013-03-08 2014-03-06 Compuestos de 1,3-oxazin-2-amina fusionados con ciclopropilo perfluorado como inhibidores de beta-secretasa y metodos de uso

Country Status (22)

Country Link
US (3) US9085576B2 (es)
EP (1) EP2964644B1 (es)
JP (1) JP6374889B2 (es)
KR (1) KR20150124985A (es)
CN (1) CN105164121A (es)
AP (1) AP2015008716A0 (es)
AU (1) AU2014225604B2 (es)
BR (1) BR112015021336A2 (es)
CA (1) CA2903215C (es)
CL (1) CL2015002516A1 (es)
CR (1) CR20150519A (es)
EA (1) EA201591614A1 (es)
HK (1) HK1217486A1 (es)
IL (1) IL240829A0 (es)
MX (1) MX2015011618A (es)
PE (1) PE20151794A1 (es)
PH (1) PH12015502001A1 (es)
SG (1) SG11201507196WA (es)
TN (1) TN2015000382A1 (es)
TW (1) TW201446760A (es)
UY (1) UY35377A (es)
WO (1) WO2014138484A1 (es)

Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ589590A (en) 2008-06-13 2012-05-25 Shionogi & Co Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity
US8999980B2 (en) 2009-12-11 2015-04-07 Shionogi & Co., Ltd. Oxazine derivatives
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
MX2015011618A (es) 2013-03-08 2015-12-17 Amgen Inc Compuestos de 1,3-oxazin-2-amina fusionados con ciclopropilo perfluorado como inhibidores de beta-secretasa y metodos de uso.
CA2905606C (en) 2013-03-13 2021-03-09 Astellas Pharma Inc. Guanidino benzoic acid esters useful in treating renal disorders
US9428470B2 (en) 2014-02-13 2016-08-30 Takeda Pharmaceutical Company Limited Heterocyclic compound
US9346776B2 (en) 2014-02-13 2016-05-24 Takeda Pharmaceutical Company Limited Fused heterocyclic compound
CA2957544C (en) 2014-08-08 2023-01-24 Amgen Inc. Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
US9868738B2 (en) * 2014-09-19 2018-01-16 Merck Sharp & Dohme Corp. Diazine-fused amidines as BACE inhibitors, compositions, and their use
EP3261442B1 (en) * 2015-01-20 2020-04-01 Merck Sharp & Dohme Corp. Iminothiadiazine dioxides bearing an amine-linked substituent as bace inhibitors, compositions, and their use
KR102114536B1 (ko) 2015-05-07 2020-05-22 브리스톨-마이어스 스큅 컴퍼니 RORγ 조정제로서의 트리시클릭 술폰
AR105607A1 (es) 2015-08-07 2017-10-18 Bayer Cropscience Ag Derivados heterocíclicos condensados sustituidos por 2-(het)arilo como pesticidas
MA52119A (fr) 2015-10-19 2018-08-29 Ncyte Corp Composés hétérocycliques utilisés comme immunomodulateurs
EP3165093A1 (en) 2015-11-05 2017-05-10 Basf Se Substituted oxadiazoles for combating phytopathogenic fungi
SG10202004618TA (en) 2015-11-19 2020-06-29 Incyte Corp Heterocyclic compounds as immunomodulators
ES2916874T3 (es) * 2015-12-17 2022-07-06 Incyte Corp Derivados de N-fenil-piridina-2-carboxamida y su uso como moduladores de la interacción proteína/proteína PD-1/PD-L1
US20170174679A1 (en) * 2015-12-22 2017-06-22 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2017192961A1 (en) 2016-05-06 2017-11-09 Incyte Corporation Heterocyclic compounds as immunomodulators
TW201808902A (zh) 2016-05-26 2018-03-16 美商英塞特公司 作為免疫調節劑之雜環化合物
MD3472167T2 (ro) 2016-06-20 2023-02-28 Incyte Corp Compuși heterociclici ca imunomodulatori
ES2930092T3 (es) 2016-07-14 2022-12-07 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
ES2941716T3 (es) 2016-08-29 2023-05-25 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
CN106432071B (zh) * 2016-09-05 2019-04-02 河北正朗制药有限公司 5-氰基-4-甲氧基-2-吡啶甲酸的盐酸盐的制备及其应用
WO2018071314A1 (en) 2016-10-10 2018-04-19 Bristol-Myers Squibb Company Tricyclic sulfones as ror gamma modulators
EP3555084B1 (en) 2016-12-15 2022-03-16 Amgen Inc. Thiazine derivatives as beta-secretase inhibitors and methods of use
JP7159161B2 (ja) 2016-12-15 2022-10-24 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シクロプロピル縮合チアジン誘導体および使用方法
CA3047286A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Oxazine derivatives as beta-secretase inhibitors and methods of use
US11021493B2 (en) 2016-12-15 2021-06-01 Amgen Inc. 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use
MX2019007100A (es) 2016-12-15 2019-12-16 Amgen Inc Derivados de tiazina y oxazina biciclicos como inhibidores de beta-secretasa y metodos de uso.
ES2874756T3 (es) 2016-12-22 2021-11-05 Incyte Corp Derivados de triazolo[1,5-A]piridina como inmunomoduladores
ES2899402T3 (es) 2016-12-22 2022-03-11 Incyte Corp Derivados de piridina como inmunomoduladores
MX2019007416A (es) 2016-12-22 2019-12-11 Incyte Corp Derivados de benzooxazol como inmunomoduladores.
CA3047980A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Tetrahydro imidazo[4,5-c]pyridine derivatives as pd-l1 internalization inducers
JP7372255B2 (ja) 2018-03-30 2023-10-31 インサイト・コーポレイション 免疫調節剤としての複素環式化合物
JP7353708B2 (ja) 2018-04-27 2023-10-02 塩野義製薬株式会社 選択的ｂａｃｅ１阻害活性を有するテトラヒドロピラノオキサジン誘導体
HRP20230306T1 (hr) 2018-05-11 2023-05-12 Incyte Corporation Derivati tetrahidro-imidazo[4,5-c]piridina kao pd-l1 imunomodulatori
CN110759860B (zh) * 2018-07-27 2022-10-14 江苏瑞科医药科技有限公司 一种3-甲酸甲酯-4-甲氧基-5-氰基吡啶的制备方法
CN110183392B (zh) * 2019-06-14 2023-03-28 河北医科大学 一种3-取代苯基-4，5-二氢异噁唑衍生物的制备方法及其用途和中间体
US11753406B2 (en) 2019-08-09 2023-09-12 Incyte Corporation Salts of a PD-1/PD-L1 inhibitor
CA3155852A1 (en) 2019-09-30 2021-04-08 Incyte Corporation PYRIDO[3,2-D]PYRIMIDINE COMPOUNDS AS IMMUNOMODULATORS
WO2021096849A1 (en) 2019-11-11 2021-05-20 Incyte Corporation Salts and crystalline forms of a pd-1/pd-l1 inhibitor
CN113087669B (zh) * 2019-12-23 2023-11-17 南京药石科技股份有限公司 一种4-氰基-5-溴嘧啶的制备方法
EP4146657A1 (en) 2020-05-05 2023-03-15 Basf Se Condensed isoxazoline derivatives and their use as herbicides
US11760756B2 (en) 2020-11-06 2023-09-19 Incyte Corporation Crystalline form of a PD-1/PD-L1 inhibitor
WO2022099018A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Process of preparing a pd-1/pd-l1 inhibitor
US11866434B2 (en) 2020-11-06 2024-01-09 Incyte Corporation Process for making a PD-1/PD-L1 inhibitor and salts and crystalline forms thereof
TW202237119A (zh) 2020-12-10 2022-10-01 美商住友製藥腫瘤公司 Ａｌｋ﹘５抑制劑和彼之用途

Family Cites Families (81)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5441870A (en) 1992-04-15 1995-08-15 Athena Neurosciences, Inc. Methods for monitoring cellular processing of β-amyloid precursor protein
SI9300303A (en) 1993-06-08 1994-12-31 Krka Tovarna Zdravil Process for isolation of hypolipemic effective substance
AU6383396A (en) 1995-06-07 1996-12-30 Athena Neurosciences, Inc. Beta-secretase, antibodies to beta-secretase, and assays for detecting beta-secretase inhibition
TR200200662T2 (tr) 1998-09-24 2002-06-21 Pharmacia & Upjohn Company Alzheimer hastalığı sekretazı
US20040234976A1 (en) 1998-09-24 2004-11-25 Gurney Mark E. Alzheimer's disease secretase, app substrates therefor, and uses therefor
EP2153832B1 (en) 2003-12-15 2016-03-09 Merck Sharp & Dohme Corp. Heterocyclic aspartyl protease inhibitors
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7700603B2 (en) 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
EP2612854B1 (en) 2005-10-25 2015-04-29 Shionogi&Co., Ltd. Aminothiazolidine and aminotetrahydrothiazepine derivatives as BACE 1 inhibitors
WO2008062739A1 (fr) 2006-11-20 2008-05-29 Japan Tobacco Inc. Pyrazoles et leur utilisation en tant que médicaments
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
TW200902526A (en) 2007-04-24 2009-01-16 Shionogi & Amp Co Ltd Aminodihydrothiazin derivative substituted with a cyclic group
NZ581614A (en) 2007-05-03 2011-06-30 Pfizer Ltd 2-pyridine carboxamide derivatives as sodium channel modulators
CN101910143B (zh) 2008-01-18 2013-08-21 卫材R&D管理有限公司 稠合的氨基二氢噻嗪衍生物
TWI431004B (zh) 2008-05-02 2014-03-21 Lilly Co Eli Ｂａｃｅ抑制劑
NZ589590A (en) 2008-06-13 2012-05-25 Shionogi & Co Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity
WO2010013794A1 (en) 2008-07-28 2010-02-04 Eisai R&D Management Co., Ltd. Spiroaminodihydrothiazine derivatives
WO2010013302A1 (ja) 2008-07-28 2010-02-04 エーザイ・アール・アンド・ディー・マネジメント株式会社 スピロアミノジヒドロチアジン誘導体
US8461160B2 (en) 2009-05-08 2013-06-11 Hoffmann-La Roche, Inc. Dihydropyrimidinones
AR077277A1 (es) 2009-07-09 2011-08-17 Lilly Co Eli Compuestos de biciclo (1,3)tiazin-2-amina formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de la enfermedad de alzheimer
GB0912778D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydro-oxazine derivatives
US8188079B2 (en) 2009-08-19 2012-05-29 Hoffman-La Roche Inc. 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines
US20110065695A1 (en) 2009-09-11 2011-03-17 Jeremy Beauchamp Use of aminodihydrothiazines for the treatment or prevention of diabetes
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
WO2011058763A1 (ja) 2009-11-13 2011-05-19 塩野義製薬株式会社 アミノリンカーを有するアミノチアジンまたはアミノオキサジン誘導体
WO2011071057A1 (ja) 2009-12-09 2011-06-16 塩野義製薬株式会社 含硫黄複素環誘導体を含有するアルツハイマー症の治療用または予防用医薬組成物
US20120245154A1 (en) 2009-12-09 2012-09-27 Shionogi & Co., Ltd. Substituted aminothiazine derivative
US7964594B1 (en) 2009-12-10 2011-06-21 Hoffmann-La Roche Inc. Amino oxazine derivatives
EP2511269A4 (en) 2009-12-11 2013-04-24 Shionogi & Co FUSED HETEROCYCLIC COMPOUND HAVING AN AMINO GROUP
US8999980B2 (en) * 2009-12-11 2015-04-07 Shionogi & Co., Ltd. Oxazine derivatives
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
US8673894B2 (en) * 2010-05-07 2014-03-18 Hoffmann-La Roche Inc. 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds
MX2013008111A (es) 2011-01-12 2013-10-30 Novartis Ag Derivados de oxazina y su uso en el tratamiento de transtornos neurologicos.
US20140128385A1 (en) 2011-01-13 2014-05-08 Novartis Ag Bace-2 inhibitors for the treatment of metabolic disorders
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
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
US8754075B2 (en) 2011-04-11 2014-06-17 Hoffmann-La Roche Inc. 1,3-oxazines as BACE1 and/or BACE2 inhibitors
BR112013026341A2 (pt) 2011-04-13 2019-09-24 Merck Sharp & Dohe Corp composto, composição farmacêutica, e, método para tratar, prevenir e/ou atrasar o início de uma doença ou patologia
US20140235626A1 (en) 2011-04-26 2014-08-21 Shionogi & Co., Ltd. Pyridine derivatives and a pharmaceutical composition for inhibiting bace1 containing them
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
US8604024B2 (en) 2011-05-24 2013-12-10 Bristol-Myers Squibb Company Compounds for the reduction of beta-amyloid production
TW201302763A (zh) 2011-05-24 2013-01-16 必治妥美雅史谷比公司 用於減少β－類澱粉產生之化合物
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
AR086653A1 (es) 2011-06-03 2014-01-15 Bristol Myers Squibb Co COMPUESTOS PARA LA REDUCCION DE PRODUCCION DE b-AMILOIDE
JP2012250933A (ja) 2011-06-03 2012-12-20 Shionogi & Co Ltd オキサジン誘導体を含有するアルツハイマー症治療用または予防用医薬組成物
CN103717592A (zh) 2011-06-07 2014-04-09 霍夫曼-拉罗奇有限公司 作为bace1和/或bace2抑制剂的卤代-烷基-1,3噁嗪类
RU2599256C2 (ru) 2011-06-07 2016-10-10 Ф. Хоффманн-Ля Рош Аг [1,3]оксазины
US8927535B2 (en) * 2011-07-06 2015-01-06 Hoffman-La Roche Inc. Cyclopropyl-fused-1,3-thiazepines as BACE1 and/or BACE2 inhibitors
BR112014004181A2 (pt) 2011-08-22 2017-06-13 Merck Sharp & Dohme composto, composição farmacêutica, e, método de tratamento, prevenção, e / ou retardo do início de uma doença ou patologia
UY34278A (es) 2011-08-25 2013-04-05 Novartis Ag Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades
WO2013030713A1 (en) 2011-08-31 2013-03-07 Pfizer Inc. Hexahydropyrano [3,4-d][1,3] thiazin-2-amine compounds
US20130073953A1 (en) 2011-09-21 2013-03-21 Timothy Onyenobi News headline screenshot viewing system
EA201490774A1 (ru) 2011-10-13 2014-08-29 Новартис Аг Новые производные оксазина и их применение при лечении заболевания
US9133129B2 (en) 2011-10-24 2015-09-15 Takeda Pharmaceutical Company Limited Bicyclic compound
MX354173B (es) 2012-01-26 2018-02-16 Hoffmann La Roche Fluorometil-5,6-dihidro-4h-[1,3]oxazinas.
EP2827857A4 (en) 2012-03-20 2016-03-30 Elan Pharm Inc SPIROCYCLIC DIHYDRO-THIAZINE AND INHIBITORS OF BACE DIHYDRO-OXAZINE AND COMPOSITIONS AND USES THEREOF
CA2872154C (en) 2012-05-04 2016-08-23 Pfizer Inc. Heterocyclic substituted hexahydropyrano [3,4-d] [1,3] thiazin-2-amine compounds as inhibitors of app, bace1 and bace2
WO2013182638A1 (en) 2012-06-08 2013-12-12 H. Lundbeck A/S 2 -aminothiazinylheteroaryls as bace1 inhibitors for the treatment alzheimer's disease
CA2872181A1 (en) 2012-06-26 2014-01-03 F. Hoffmann-La Roche Ag Difluoro-hexahydro-cyclopentaoxazinyls and difluoro-hexahydro-benzooxazinyls as bace1 inhibitors
GB201212871D0 (en) 2012-07-20 2012-09-05 Eisai Ltd Novel compounds
CA2882389A1 (en) 2012-09-20 2014-03-27 Pfizer Inc. Alkyl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
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
EP2908824B1 (en) 2012-10-17 2018-05-02 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2908825B1 (en) 2012-10-17 2018-04-18 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
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
CN104755484B (zh) 2012-10-26 2016-02-17 伊莱利利公司 Bace抑制剂
EP2931284B1 (en) 2012-12-14 2017-08-23 Merck Sharp & Dohme Corp. Bace inhibitors of iminothiadiazine dioxides
EP2935282A1 (en) 2012-12-19 2015-10-28 Pfizer Inc. CARBOCYCLIC- AND HETEROCYCLIC-SUBSTITUTED HEXAHYDROPYRANO[3,4-d][1,3]THIAZIN-2-AMINE COMPOUNDS
US9475784B2 (en) 2012-12-19 2016-10-25 Bristol-Myers Squibb Company 4,6-diarylaminothiazines as BACE1 inhibitors and their use for the reduction of beta-amyloid production
EP2934539B1 (en) 2012-12-20 2019-03-27 Merck Sharp & Dohme Corp. C5, c6 oxacyclic-fused iminothiazine dioxide compounds as bace inhibitors
EP2934534B1 (en) 2012-12-21 2017-12-13 Merck Sharp & Dohme Corp. C5-spiro iminothiadiazine dioxides as bace inhibitors
EP2948446A1 (en) 2013-01-22 2015-12-02 F. Hoffmann-La Roche AG Fluoro-[1,3]oxazines as bace1 inhibitors
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
MX2015011618A (es) 2013-03-08 2015-12-17 Amgen Inc Compuestos de 1,3-oxazin-2-amina fusionados con ciclopropilo perfluorado como inhibidores de beta-secretasa y metodos de uso.
MX349262B (es) 2013-03-15 2017-07-20 Univ Brigham Young Material compuesto usado como un medidor de deformacion.
CN105431430B (zh) 2013-04-11 2019-05-28 豪夫迈·罗氏有限公司 Bace1抑制剂
WO2014173917A1 (en) 2013-04-26 2014-10-30 F. Hoffmann-La Roche Ag Synthesis of bace1 inhibitors
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
CA2957544C (en) 2014-08-08 2023-01-24 Amgen Inc. Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use

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