CR20120002A - Derivados de oxazina y su uso como inhibidores de bace para el tratamiento de trastornos neurológicos - Google Patents

Derivados de oxazina y su uso como inhibidores de bace para el tratamiento de trastornos neurológicos

Info

Publication number
CR20120002A
CR20120002A CR20120002A CR20120002A CR20120002A CR 20120002 A CR20120002 A CR 20120002A CR 20120002 A CR20120002 A CR 20120002A CR 20120002 A CR20120002 A CR 20120002A CR 20120002 A CR20120002 A CR 20120002A
Authority
CR
Costa Rica
Prior art keywords
treatment
oxazine
derivatives
neurological disorders
bace inhibitors
Prior art date
Application number
CR20120002A
Other languages
English (en)
Spanish (es)
Inventor
Sangamesh Badiger
Murali Chebrolu
Mathias Frederiksen
Philipp Holzer
Konstanze Hurth
Rainer Martin Lueoend
Rainer Machauer
Henrik Moebitz
Ulf Neumann
Rita Ramos
Heinrich Rueeger
Michael Schaefer
Marina Tintelnot-Blomley
Siem Jacob Veenstra
Markus Voegtle
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=42629546&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CR20120002(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 CR20120002A publication Critical patent/CR20120002A/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/301,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D267/00Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02Seven-membered rings
    • C07D267/08Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/10Seven-membered rings having the hetero atoms in positions 1 and 4 not condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CR20120002A 2009-07-24 2012-01-09 Derivados de oxazina y su uso como inhibidores de bace para el tratamiento de trastornos neurológicos CR20120002A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US22847209P 2009-07-24 2009-07-24
US25891109P 2009-11-06 2009-11-06
US36370210P 2010-07-13 2010-07-13

Publications (1)

Publication Number Publication Date
CR20120002A true CR20120002A (es) 2012-02-15

Family

ID=42629546

Family Applications (1)

Application Number Title Priority Date Filing Date
CR20120002A CR20120002A (es) 2009-07-24 2012-01-09 Derivados de oxazina y su uso como inhibidores de bace para el tratamiento de trastornos neurológicos

Country Status (26)

Country Link
US (5) US8207164B2 (enExample)
EP (1) EP2456763B1 (enExample)
JP (1) JP5767214B2 (enExample)
KR (2) KR101422965B1 (enExample)
CN (1) CN102471293B (enExample)
AR (1) AR077328A1 (enExample)
AU (1) AU2010274913B2 (enExample)
CA (1) CA2768980A1 (enExample)
CL (1) CL2012000185A1 (enExample)
CO (1) CO6491058A2 (enExample)
CR (1) CR20120002A (enExample)
CU (1) CU24083B1 (enExample)
EA (1) EA201200174A1 (enExample)
EC (1) ECSP12011622A (enExample)
ES (1) ES2534315T3 (enExample)
GT (1) GT201200016A (enExample)
IL (1) IL217378A (enExample)
MA (1) MA33450B1 (enExample)
MX (1) MX2012001070A (enExample)
NZ (1) NZ597529A (enExample)
PE (1) PE20121440A1 (enExample)
SG (1) SG177397A1 (enExample)
TW (1) TW201107316A (enExample)
UY (1) UY32799A (enExample)
WO (1) WO2011009943A1 (enExample)
ZA (1) ZA201200155B (enExample)

Families Citing this family (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
KR101052122B1 (ko) 2005-10-25 2011-07-26 시오노기세야쿠 가부시키가이샤 아미노디히드로티아진 유도체
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
MX2010013256A (es) 2008-06-13 2010-12-21 Shionogi & Co Derivado heterociclico que contiene azufre que tiene actividad inhibitoria de beta-secretasa.
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
AR077328A1 (es) * 2009-07-24 2011-08-17 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos
US8188079B2 (en) 2009-08-19 2012-05-29 Hoffman-La Roche Inc. 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
WO2011044185A2 (en) 2009-10-08 2011-04-14 Schering Corporation Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
WO2011044184A1 (en) 2009-10-08 2011-04-14 Schering Corporation 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
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
JPWO2011071135A1 (ja) 2009-12-11 2013-04-22 塩野義製薬株式会社 オキサジン誘導体
BR112012015916A2 (pt) * 2009-12-31 2017-04-25 Novartis Ag derivados de pirazina e seu uso no tratamento de distúrbios neurológicos
EP2547686B1 (en) 2010-03-15 2014-01-22 Amgen Inc. Amino-dihydrooxazine and amino-dihydrothiazine spiro compounds as beta-secretase modulators and their medical use
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
EA021240B1 (ru) 2010-06-09 2015-05-29 Янссен Фармацевтика Нв Производные 5,6-дигидро-2h-[1,4]оксазин-3-иламина в качестве ингибиторов бета-секретазы (bace)
MA33509B1 (fr) * 2010-07-13 2012-08-01 Novartis Ag Dérivés de l'oxazine et leur utilisation dans le traitement de troubles neurologiques
CA2816285A1 (en) 2010-10-29 2012-05-03 Shionogi & Co., Ltd. Naphthyridine derivative
EP2634188A4 (en) 2010-10-29 2014-05-07 Shionogi & Co FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE
US9840507B2 (en) 2010-12-22 2017-12-12 Janssen Pharmaceutica, Nv 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives useful as inhibitors of beta-secretase (BACE)
JP2014505688A (ja) * 2011-01-12 2014-03-06 ノバルティス アーゲー オキサジン誘導体および神経障害の処置におけるその使用
US8524897B2 (en) 2011-01-12 2013-09-03 Novartis Ag Crystalline oxazine derivative
EP2663308A1 (en) * 2011-01-13 2013-11-20 Novartis AG Bace-2 inhibitors for the treatment of metabolic disorders
CN106117193B (zh) 2011-01-13 2019-09-13 诺华股份有限公司 新的杂环衍生物及其在神经性疾病治疗中的应用
US9242943B2 (en) * 2011-01-18 2016-01-26 Siena Biotech S.P.A. 1,4 oxazines as BACE1 and/or BACE2 inhibitors
US8399459B2 (en) * 2011-02-02 2013-03-19 Hoffmann-La Roche Inc. 1,4 oxazines 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
HUE026338T2 (en) 2011-03-01 2016-05-30 Janssen Pharmaceutica Nv 6,7-dihydro-pyrazolo[1,5-a]pyrazin-4-ylamine derivatives useful as inhibitors of beta-secretase (bace)
US9067924B2 (en) 2011-03-04 2015-06-30 Hoffmann-La Roche Inc. 1,4 thiazepines/sulfones as BACE1 and/or BACE2 inhibitors
MX340031B (es) * 2011-03-09 2016-06-21 Janssen Pharmaceutica Nv Derivados de 3,4-dihidropirrolo[1,2-a]pirazin-1-ilamina utiles como inhibidores de beta-secretasa (bace).
US8748418B2 (en) 2011-03-18 2014-06-10 Hoffmann-La Roche Inc. 1,4-oxazepines as BACE1 and/or BACE2 inhibitors
US8877744B2 (en) 2011-04-04 2014-11-04 Hoffmann-La Roche Inc. 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors
US9221839B2 (en) 2011-04-07 2015-12-29 Merck Sharp & Dohme Corp. C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
US9145426B2 (en) 2011-04-07 2015-09-29 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
MX2013011947A (es) 2011-04-13 2014-01-16 Merck Sharp & Dohme Iminotiazinas 5-sustituidas y sus monoxidos y dioxidos como inhibidores de la enzima que encinde la proteina precursora amiloide en el sitio beta, composiciones y su uso.
TW201247635A (en) 2011-04-26 2012-12-01 Shionogi & Co Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them
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
WO2012168175A1 (en) * 2011-06-07 2012-12-13 F. Hoffmann-La Roche Ag [1,3]oxazines
EA023261B1 (ru) * 2011-06-07 2016-05-31 Ф.Хоффманн-Ля Рош Аг Галоген-алкил-1,3-оксазины в качестве ингибиторов bace1 и(или) bace2
US8927535B2 (en) * 2011-07-06 2015-01-06 Hoffman-La Roche Inc. Cyclopropyl-fused-1,3-thiazepines as BACE1 and/or BACE2 inhibitors
EP2747769B1 (en) 2011-08-22 2017-08-02 Merck Sharp & Dohme Corp. 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use
JP2014526560A (ja) 2011-09-21 2014-10-06 アムジエン・インコーポレーテツド β‐セクレターゼ調節因子としてのアミノオキサジン化合物およびアミノジヒドロチアジン化合物および使用方法
KR20140084146A (ko) * 2011-10-13 2014-07-04 노파르티스 아게 신규 옥사진 유도체 및 질환의 치료에서의 그의 용도
UA111749C2 (uk) * 2011-12-05 2016-06-10 Янссен Фармацевтика Нв Похідні 6-дифторметил-5,6-дигідро-2h-[1,4]оксазин-3-аміну
EP2788335B1 (en) * 2011-12-06 2016-04-13 Janssen Pharmaceutica, N.V. 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives for the treatment of disorders in which beta-secretase is involved
JP5869151B2 (ja) * 2012-01-26 2016-02-24 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft フルオロメチル−5,6−ジヒドロ−4h−[1,3]オキサジン
US8338413B1 (en) 2012-03-07 2012-12-25 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
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
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
US9725469B2 (en) 2012-11-15 2017-08-08 Amgen, Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
EP2934539B1 (en) 2012-12-20 2019-03-27 Merck Sharp & Dohme Corp. C5, c6 oxacyclic-fused iminothiazine dioxide compounds as bace inhibitors
TW201512171A (zh) 2013-04-19 2015-04-01 Pfizer Ltd 化學化合物
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).
CA2911690C (en) 2013-06-12 2021-08-24 Janssen Pharmaceutica Nv 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace)
ES2721073T3 (es) 2013-06-12 2019-07-26 Janssen Pharmaceutica Nv Derivados de 4-amino-6-fenil-6,7-dihidro[1,2,3]triazolo[1,5 a]pirazina como inhibidores de beta-secretasa (BACE)
FR3025591B1 (fr) * 2014-09-05 2016-10-14 Technofan Dispositif de ventilation, aeronef comportant un tel dispositif de ventilation et procede de surveillance associe
AU2015367594C1 (en) 2014-12-18 2019-10-31 Janssen Pharmaceutica Nv 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2H-pyrrol-5-amine compound inhibitors of beta-secretase
TW201726651A (zh) 2015-09-23 2017-08-01 健生藥品公司 2,3,4,5-四氫吡啶-6-胺衍生物
CN109661397A (zh) * 2016-08-26 2019-04-19 伊莱利利公司 用作选择性bace1抑制剂的1,4-噁嗪类化合物
US10159191B2 (en) 2016-09-23 2018-12-25 Deere & Company Harvester grain unloader
CN110018266B (zh) * 2019-02-15 2022-03-04 广州市妇女儿童医疗中心 一种快速定量分析48种氨基酸的方法
CN112250580A (zh) * 2020-10-28 2021-01-22 上海昂卓新材料科技有限公司 一种2-硝基-2-取代苯基丙烷-1,3-二醇的制备方法

Family Cites Families (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL6911868A (enExample) 1968-08-31 1970-03-03
PT72878B (en) 1980-04-24 1983-03-29 Merck & Co Inc Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
TW385308B (en) * 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists
TW200502221A (en) * 2002-10-03 2005-01-16 Astrazeneca Ab Novel lactams and uses thereof
JP2007524596A (ja) 2003-02-28 2007-08-30 トランスフォーム・ファーマシューティカルズ・インコーポレイテッド 共結晶医薬組成物
AR043633A1 (es) * 2003-03-20 2005-08-03 Schering Corp Ligandos de receptores de canabinoides
EP1702919B1 (en) 2003-12-29 2012-05-30 Msd K.K. Novel 2-heteroaryl-substituted benzimidazole derivative
JP2007524682A (ja) 2004-02-12 2007-08-30 メルク エンド カムパニー インコーポレーテッド 代謝調節型グルタミン酸受容体−5の調節物質としてのビピリジルアミド
SV2006002232A (es) 2004-09-21 2006-05-25 Lilly Co Eli Inhibidores bace ref. x-16940
US7888374B2 (en) * 2005-01-28 2011-02-15 Abbott Laboratories Inhibitors of c-jun N-terminal kinases
KR101052122B1 (ko) * 2005-10-25 2011-07-26 시오노기세야쿠 가부시키가이샤 아미노디히드로티아진 유도체
US8822497B2 (en) 2007-03-01 2014-09-02 Novartis Ag PIM kinase inhibitors and methods of their use
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
GB0713686D0 (en) 2007-07-13 2007-08-22 Addex Pharmaceuticals Sa New compounds 2
US20100317850A1 (en) 2008-01-18 2010-12-16 Yuichi Suzuki Condensed aminodihydrothiazine derivative
US20100197688A1 (en) * 2008-05-29 2010-08-05 Nantermet Philippe G Epha4 rtk inhibitors for treatment of neurological and neurodegenerative disorders and cancer
MX2010013256A (es) 2008-06-13 2010-12-21 Shionogi & Co Derivado heterociclico que contiene azufre que tiene actividad inhibitoria de beta-secretasa.
TW201028381A (en) 2008-07-14 2010-08-01 Shionogi & Co Pyridine derivative having ttk inhibition activity
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
US9237972B2 (en) 2008-12-16 2016-01-19 Kimberly-Clark Worldwide, Inc. Liquid surfactant compositions that adhere to surfaces and solidify and swell in the presence of water and articles using the same
US8461160B2 (en) 2009-05-08 2013-06-11 Hoffmann-La Roche, Inc. Dihydropyrimidinones
AR077328A1 (es) 2009-07-24 2011-08-17 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos
US8188079B2 (en) 2009-08-19 2012-05-29 Hoffman-La Roche Inc. 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines
JPWO2011058763A1 (ja) 2009-11-13 2013-03-28 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
US7964594B1 (en) 2009-12-10 2011-06-21 Hoffmann-La Roche Inc. Amino 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
JPWO2011071135A1 (ja) 2009-12-11 2013-04-22 塩野義製薬株式会社 オキサジン誘導体
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
EA021240B1 (ru) 2010-06-09 2015-05-29 Янссен Фармацевтика Нв Производные 5,6-дигидро-2h-[1,4]оксазин-3-иламина в качестве ингибиторов бета-секретазы (bace)
EA201291366A1 (ru) 2010-06-09 2013-04-30 Янссен Фармацевтика Нв Производные 5-амино-3,6-дигидро-1h-пиразин-2-она в качестве ингибиторов бета-секретазы (bace)
MA33509B1 (fr) * 2010-07-13 2012-08-01 Novartis Ag Dérivés de l'oxazine et leur utilisation dans le traitement de troubles neurologiques
US8524897B2 (en) 2011-01-12 2013-09-03 Novartis Ag Crystalline oxazine derivative
JP2014505688A (ja) 2011-01-12 2014-03-06 ノバルティス アーゲー オキサジン誘導体および神経障害の処置におけるその使用
CN106117193B (zh) 2011-01-13 2019-09-13 诺华股份有限公司 新的杂环衍生物及其在神经性疾病治疗中的应用
EP2663308A1 (en) 2011-01-13 2013-11-20 Novartis AG Bace-2 inhibitors for the treatment of metabolic disorders
KR20140084146A (ko) 2011-10-13 2014-07-04 노파르티스 아게 신규 옥사진 유도체 및 질환의 치료에서의 그의 용도

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