CO6491058A2 - 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
CO6491058A2
CO6491058A2 CO12007858A CO12007858A CO6491058A2 CO 6491058 A2 CO6491058 A2 CO 6491058A2 CO 12007858 A CO12007858 A CO 12007858A CO 12007858 A CO12007858 A CO 12007858A CO 6491058 A2 CO6491058 A2 CO 6491058A2
Authority
CO
Colombia
Prior art keywords
treatment
oxazine
derivatives
neurological disorders
bace inhibitors
Prior art date
Application number
CO12007858A
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
Markuis 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=CO6491058(A2) "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 CO6491058A2 publication Critical patent/CO6491058A2/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)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (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)
CO12007858A 2009-07-24 2012-01-19 Derivados de oxazina y su uso como inhibidores de bace para el tratamiento de trastornos neurológicos CO6491058A2 (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
CO6491058A2 true CO6491058A2 (es) 2012-07-31

Family

ID=42629546

Family Applications (1)

Application Number Title Priority Date Filing Date
CO12007858A CO6491058A2 (es) 2009-07-24 2012-01-19 Derivados de oxazina y su uso como inhibidores de bace para el tratamiento de trastornos neurológicos

Country Status (26)

Country Link
US (5) US8207164B2 (cg-RX-API-DMAC7.html)
EP (1) EP2456763B1 (cg-RX-API-DMAC7.html)
JP (1) JP5767214B2 (cg-RX-API-DMAC7.html)
KR (2) KR20140004810A (cg-RX-API-DMAC7.html)
CN (1) CN102471293B (cg-RX-API-DMAC7.html)
AR (1) AR077328A1 (cg-RX-API-DMAC7.html)
AU (1) AU2010274913B2 (cg-RX-API-DMAC7.html)
CA (1) CA2768980A1 (cg-RX-API-DMAC7.html)
CL (1) CL2012000185A1 (cg-RX-API-DMAC7.html)
CO (1) CO6491058A2 (cg-RX-API-DMAC7.html)
CR (1) CR20120002A (cg-RX-API-DMAC7.html)
CU (1) CU24083B1 (cg-RX-API-DMAC7.html)
EA (1) EA201200174A1 (cg-RX-API-DMAC7.html)
EC (1) ECSP12011622A (cg-RX-API-DMAC7.html)
ES (1) ES2534315T3 (cg-RX-API-DMAC7.html)
GT (1) GT201200016A (cg-RX-API-DMAC7.html)
IL (1) IL217378A (cg-RX-API-DMAC7.html)
MA (1) MA33450B1 (cg-RX-API-DMAC7.html)
MX (1) MX2012001070A (cg-RX-API-DMAC7.html)
NZ (1) NZ597529A (cg-RX-API-DMAC7.html)
PE (1) PE20121440A1 (cg-RX-API-DMAC7.html)
SG (1) SG177397A1 (cg-RX-API-DMAC7.html)
TW (1) TW201107316A (cg-RX-API-DMAC7.html)
UY (1) UY32799A (cg-RX-API-DMAC7.html)
WO (1) WO2011009943A1 (cg-RX-API-DMAC7.html)
ZA (1) ZA201200155B (cg-RX-API-DMAC7.html)

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
WO2008133273A1 (ja) 2007-04-24 2008-11-06 Shionogi & Co., Ltd. アルツハイマー症治療用医薬組成物
MX2009011498A (es) 2007-04-24 2009-11-10 Shionogi & Co Derivados de aminodihidrotiazina sustituida con un grupo ciclico.
AU2009258496B8 (en) 2008-06-13 2014-06-26 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting 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
UY32799A (es) 2009-07-24 2011-02-28 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
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
US8569310B2 (en) 2009-10-08 2013-10-29 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
EP2485590B1 (en) 2009-10-08 2015-01-07 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as bace-1 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
US8999980B2 (en) 2009-12-11 2015-04-07 Shionogi & Co., Ltd. Oxazine derivatives
WO2011080176A1 (en) * 2009-12-31 2011-07-07 Novartis Ag Pyrazine derivatives and their use in the treatment of neurological disorders
AU2011227501B9 (en) 2010-03-15 2013-08-22 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
EP2580200B1 (en) 2010-06-09 2016-09-14 Janssen Pharmaceutica, N.V. 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace)
EP2483255B1 (en) * 2010-07-13 2013-10-16 Novartis AG Oxazine derivatives and their use in the treatment of neurological disorders
US8927721B2 (en) 2010-10-29 2015-01-06 Shionogi & Co., Ltd. Naphthyridine derivative
WO2012057247A1 (ja) 2010-10-29 2012-05-03 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
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
EA201391029A1 (ru) * 2011-01-12 2014-01-30 Новартис Аг Производные оксазина и их применение при лечении неврологических нарушений
MX2013008192A (es) * 2011-01-13 2013-12-16 Novartis Ag Inhibidores de bace-2 para tratamiento de transtornos metabolicos.
KR101569260B1 (ko) * 2011-01-13 2015-11-13 노파르티스 아게 신규 헤테로시클릭 유도체 및 신경계 장애의 치료에서의 그의 용도
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
WO2012117027A1 (en) * 2011-03-01 2012-09-07 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
CN103415521B (zh) 2011-03-09 2016-01-06 詹森药业有限公司 用作β分泌酶(BACE)抑制剂的3,4-二氢-吡咯并[1,2-a]吡嗪-1-基胺衍生物
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
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
US9499502B2 (en) 2011-04-13 2016-11-22 Merck Sharp & Dohme Corp. 5-substituted iminothiazines and their mono- and dioxides as BACE inhibitors, compositions, and their use
US8883779B2 (en) 2011-04-26 2014-11-11 Shinogi & Co., Ltd. Oxazine derivatives and a pharmaceutical composition for inhibiting BACE1 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
KR20140041687A (ko) * 2011-06-07 2014-04-04 에프. 호프만-라 로슈 아게 Bace1 및/또는 bace2 억제제로서의 할로겐-알킬-1,3-옥사진
BR112013031510A2 (pt) * 2011-06-07 2016-12-27 Hoffmann La Roche [1,3]oxazinas
US8927535B2 (en) * 2011-07-06 2015-01-06 Hoffman-La Roche Inc. Cyclopropyl-fused-1,3-thiazepines as BACE1 and/or BACE2 inhibitors
AU2012298983A1 (en) 2011-08-22 2014-02-27 Merck Sharp & Dohme Corp. 2-spiro-substituted iminothiazines and their mono-and dioxides as BACE inhibitors, compositions and their use
WO2013044092A1 (en) 2011-09-21 2013-03-28 Amgen Inc. Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
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
WO2013083556A1 (en) 2011-12-06 2013-06-13 Janssen Pharmaceutica Nv 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives
SG11201403956VA (en) 2012-01-26 2014-10-30 Hoffmann La Roche 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
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
US9725469B2 (en) 2012-11-15 2017-08-08 Amgen, Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
CN104870000A (zh) 2012-12-20 2015-08-26 默沙东公司 作为bace抑制剂的c5,c6氧杂环稠合的亚胺基噻嗪二氧化物化合物,组合物及其用途
TW201512171A (zh) 2013-04-19 2015-04-01 Pfizer Ltd 化學化合物
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)
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)
FR3025591B1 (fr) * 2014-09-05 2016-10-14 Technofan Dispositif de ventilation, aeronef comportant un tel dispositif de ventilation et procede de surveillance associe
US10106524B2 (en) 2014-12-18 2018-10-23 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
JP2019524825A (ja) 2016-08-26 2019-09-05 イーライ リリー アンド カンパニー 選択的bace1阻害剤として有用な1,4−オキサジン
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 (cg-RX-API-DMAC7.html) 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
IL112778A0 (en) 1994-03-04 1995-05-26 Merck & Co Inc Substituted heterocycles, their preparation and pharmaceutical compositions containing them
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
TW200505902A (en) 2003-03-20 2005-02-16 Schering Corp Cannabinoid receptor ligands
RU2329261C2 (ru) 2003-12-29 2008-07-20 Баниу Фармасьютикал Ко., Лтд. Новое 2-гетероарил-замещенное производное бензимидазола
EP1715867A4 (en) 2004-02-12 2009-04-15 Merck & Co Inc BIPYRIDYLAMIDE AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR-5
TW200624426A (en) 2004-09-21 2006-07-16 Lilly Co Eli BACE inhibitors
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
CA2679659C (en) 2007-03-01 2016-01-19 Novartis Ag Pim kinase inhibitors and methods of their use
MX2009011498A (es) 2007-04-24 2009-11-10 Shionogi & Co Derivados de aminodihidrotiazina sustituida con un grupo ciclico.
WO2008133273A1 (ja) * 2007-04-24 2008-11-06 Shionogi & Co., Ltd. アルツハイマー症治療用医薬組成物
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
AU2009258496B8 (en) 2008-06-13 2014-06-26 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity
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
UY32799A (es) 2009-07-24 2011-02-28 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
US8188079B2 (en) 2009-08-19 2012-05-29 Hoffman-La Roche Inc. 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines
US20120238557A1 (en) 2009-11-13 2012-09-20 Shionogi & Co., Ltd. Aminothiazine or aminooxazine derivative having amino linker
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
US8999980B2 (en) 2009-12-11 2015-04-07 Shionogi & Co., Ltd. Oxazine derivatives
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
PH12012502379A1 (en) 2010-06-09 2013-02-18 Janssen Pharmaceutica Nv 5-amino-3,6-dihydro-1h-pyrazin-2-one derivatives useful as inhibitors of beta-secretase (bace)
EP2580200B1 (en) 2010-06-09 2016-09-14 Janssen Pharmaceutica, N.V. 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace)
EP2483255B1 (en) * 2010-07-13 2013-10-16 Novartis AG Oxazine derivatives and their use in the treatment of neurological disorders
EA201391029A1 (ru) 2011-01-12 2014-01-30 Новартис Аг Производные оксазина и их применение при лечении неврологических нарушений
US8524897B2 (en) 2011-01-12 2013-09-03 Novartis Ag Crystalline oxazine derivative
MX2013008192A (es) 2011-01-13 2013-12-16 Novartis Ag Inhibidores de bace-2 para tratamiento de transtornos metabolicos.
KR101569260B1 (ko) 2011-01-13 2015-11-13 노파르티스 아게 신규 헤테로시클릭 유도체 및 신경계 장애의 치료에서의 그의 용도
KR20140084146A (ko) 2011-10-13 2014-07-04 노파르티스 아게 신규 옥사진 유도체 및 질환의 치료에서의 그의 용도

Also Published As

Publication number Publication date
CN102471293B (zh) 2014-10-01
MX2012001070A (es) 2012-03-16
US8207164B2 (en) 2012-06-26
HK1166314A1 (en) 2012-10-26
NZ597529A (en) 2013-11-29
US8846658B2 (en) 2014-09-30
ZA201200155B (en) 2012-09-26
US20110021520A1 (en) 2011-01-27
AU2010274913A1 (en) 2012-02-02
MA33450B1 (fr) 2012-07-03
CR20120002A (es) 2012-02-15
US20140113894A1 (en) 2014-04-24
CA2768980A1 (en) 2011-01-27
EA201200174A1 (ru) 2012-08-30
IL217378A (en) 2015-02-26
US20150018338A1 (en) 2015-01-15
KR101422965B1 (ko) 2014-07-23
JP5767214B2 (ja) 2015-08-19
TW201107316A (en) 2011-03-01
SG177397A1 (en) 2012-02-28
CU24083B1 (es) 2015-03-30
WO2011009943A1 (en) 2011-01-27
GT201200016A (es) 2013-09-23
KR20140004810A (ko) 2014-01-13
UY32799A (es) 2011-02-28
KR20120039655A (ko) 2012-04-25
CN102471293A (zh) 2012-05-23
IL217378A0 (en) 2012-03-01
AU2010274913B2 (en) 2013-09-19
EP2456763A1 (en) 2012-05-30
US20140088084A1 (en) 2014-03-27
CU20120013A7 (es) 2012-04-15
ECSP12011622A (es) 2012-02-29
AR077328A1 (es) 2011-08-17
ES2534315T3 (es) 2015-04-21
US20120238560A1 (en) 2012-09-20
CL2012000185A1 (es) 2012-10-12
EP2456763B1 (en) 2015-01-21
PE20121440A1 (es) 2012-11-06
JP2013500247A (ja) 2013-01-07

Similar Documents

Publication Publication Date Title
CO6491058A2 (es) Derivados de oxazina y su uso como inhibidores de bace para el tratamiento de trastornos neurológicos
CU20120099A7 (es) Derivados de pirazina y su uso en el tratamiento de trastornos neurológicos
GT201300179A (es) Derivados heterociclicos novedosos y su uso en el tratamiento de trastornos neurologicos
ECSP12011692A (es) Derivados de oxazina y su uso en el tratamiento de los trastornos neurológicos
EA201391029A1 (ru) Производные оксазина и их применение при лечении неврологических нарушений
GT201400031A (es) Derivados de 2-amino-4-(piridin-2-il)-5,6-dihidro-4h-1,3-oxazina y su uso como inhibidores de bace-1 y/o bace-2
GT200900095A (es) Dihidropirazolonas sustituidas para el tratamiento de enfermedades cardiovasculares y hermatologicas.
ECSP13012611A (es) Derivados de pirazol-aminopirimidina como moduladores de la lrrk2
CO6612267A2 (es) Nuevos derivados de 1,1 dióxido- 5 fenil- 2,3,4-5tetrahidro- 1,4-benzotiazepina y composiciones farmaceúticas que los comprenden
ECSP10010582A (es) Derivados de aminodihidrotiazina como inhibidores de bace para el tratamiento de la enfermedad de alzheimer
UY30282A1 (es) Compuestos quimicos
ATE530524T1 (de) Substituierte sulfonamid-derivate
CO6470845A2 (es) Derivados de pirimidina novedosos y su uso en el tratamiento del cancer y enfermedades adicionales
UY33883A (es) Novedosos derivados heterocíclicos
UY31651A1 (es) Nuevos derivados de fluoroglicósidos aromáticos, medicamentos que comprenden estos compuestos y uso de los mismos.
UY34955A (es) 4-metil-2,3,5,9,9b-pentaaza-ciclopenta[a]naftalenos
ECSP11010992A (es) Derivados de anilina-pirimidina sustituidos con sulfoximina como inhibidores de quinasas dependientes de ciclina (cdk), producción y uso de los mismos como productos medicinales
ECSP11010956A (es) Compuestos enlazados con azufre para el tratamiento de enfermedades y trastornos oftalmicos
UY31133A1 (es) "oxazolidinonas sustituidas y su uso"
UY33181A (es) Derivados de oxazolopirimidina 2,5-sustituidos.
CR20150092A (es) Derivados de diazepinona útiles para el tratamiento del síndrome x frágil, enfermedad de parkinson o enfermedad del reflujo
HN2012000132A (es) Derivados de oxazina y su uso como inhibidores de bace para el tratamiento de trastornos neurologicos
CU24047B1 (es) Derivados de oxazina útiles en el tratamiento de los trastornos neurológicos
CR20120083A (es) Derivados de oxazina y su uso en el tratamiento de los trastornos neurologicos
UA107356C2 (en) Oxazine derivatives and their use as bace inhibitors for the treatment of neurological disorders

Legal Events

Date Code Title Description
FG Application granted