MA33450B1 - Dérivés d'oxazine et leur utilisation en tant qu'inhibiteurs de bace pour le traitement de troubles neurologiques - Google Patents

Dérivés d'oxazine et leur utilisation en tant qu'inhibiteurs de bace pour le traitement de troubles neurologiques

Info

Publication number
MA33450B1
MA33450B1 MA34558A MA34558A MA33450B1 MA 33450 B1 MA33450 B1 MA 33450B1 MA 34558 A MA34558 A MA 34558A MA 34558 A MA34558 A MA 34558A MA 33450 B1 MA33450 B1 MA 33450B1
Authority
MA
Morocco
Prior art keywords
treatment
neurological disorders
inhibitors
oxazin
derivatives
Prior art date
Application number
MA34558A
Other languages
Arabic (ar)
English (en)
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=MA33450(B1) "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 MA33450B1 publication Critical patent/MA33450B1/fr

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)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

L'invention concerne de nouveaux composés hétérocycliques de formule (I) dans lesquels toutes les variables sont telles que définies dans la spécification, sous forme libre ou sous forme de sel, leur préparation, leur utilisation médicale en tant qu'inhibiteurs de BACE pour le traitement de la maladie d'Alzheimer et des médicaments comprenant ceux-ci.
MA34558A 2009-07-24 2010-07-23 Dérivés d'oxazine et leur utilisation en tant qu'inhibiteurs de bace pour le traitement de troubles neurologiques MA33450B1 (fr)

Applications Claiming Priority (4)

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
PCT/EP2010/060718 WO2011009943A1 (fr) 2009-07-24 2010-07-23 Dérivés d’oxazine et leur utilisation en tant qu’inhibiteurs de bace pour le traitement de troubles neurologiques

Publications (1)

Publication Number Publication Date
MA33450B1 true MA33450B1 (fr) 2012-07-03

Family

ID=42629546

Family Applications (1)

Application Number Title Priority Date Filing Date
MA34558A MA33450B1 (fr) 2009-07-24 2010-07-23 Dérivés d'oxazine et leur utilisation en tant qu'inhibiteurs de bace pour le traitement de troubles neurologiques

Country Status (26)

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

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
CN101346357B (zh) 2005-10-25 2014-04-02 盐野义制药株式会社 氨基二氢噻嗪衍生物
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
EP2689780A1 (fr) 2007-04-24 2014-01-29 Shionogi & Co., Ltd. Intermédiaires de dérivés d'aminodihydrothiazine substitués avec un groupe cyclique
KR101324426B1 (ko) 2008-06-13 2013-10-31 시오노기세야쿠 가부시키가이샤 β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체
CN102186841A (zh) 2008-10-22 2011-09-14 盐野义制药株式会社 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物
UY32799A (es) 2009-07-24 2011-02-28 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
US8188079B2 (en) 2009-08-19 2012-05-29 Hoffman-La Roche Inc. 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines
EP2485920B1 (fr) 2009-10-08 2016-04-27 Merck Sharp & Dohme Corp. Composés hétérocycliques iminopentafluorosoufrés en tant qu'inhibiteurs de bace-1, compositions et leur utilisation
EP2485591B1 (fr) 2009-10-08 2016-03-23 Merck Sharp & Dohme Corp. Composés de type dioxyde d'imino-thiadiazine utilisés en tant qu'inhibiteurs de bace, compositions en contenant et leur utilisation
US8557826B2 (en) 2009-10-08 2013-10-15 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions, and their use
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
KR20120104570A (ko) 2009-12-11 2012-09-21 시오노기세야쿠 가부시키가이샤 옥사진 유도체
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
US20120277244A1 (en) * 2009-12-31 2012-11-01 Novartis Ag Pyrazine derivatives and their use in the treatment of neurological disorders
JP5584352B2 (ja) 2010-03-15 2014-09-03 アムジエン・インコーポレーテツド β−セクレターゼ調節剤としてのアミノ−ジヒドロオキサジン系およびアミノ−ジヒドロチアジン系スピロ化合物ならびにそれらの医学的用途
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
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
BR112012004154A2 (pt) * 2010-07-13 2017-05-30 Novartis Ag "derivados de oxazina e seu uso no tratamento de distúrbios neurológicos"
CN103261199A (zh) 2010-10-29 2013-08-21 盐野义制药株式会社 萘啶衍生物
EP2634188A4 (fr) 2010-10-29 2014-05-07 Shionogi & Co Dérivé d'aminodihydropyrimidine fusionnée
BR112013015430A2 (pt) 2010-12-22 2016-09-20 Janssen Pharmaceutica Nv derivados de 5,6-diidro-imidazo[1,2-a]pirazin-8-ilamina úteis como inibidores de beta-secretase (bace)
US8524897B2 (en) * 2011-01-12 2013-09-03 Novartis Ag Crystalline oxazine derivative
KR20140051822A (ko) * 2011-01-12 2014-05-02 노파르티스 아게 옥사진 유도체 및 신경계 장애의 치료에서의 그의 용도
CN103596569A (zh) * 2011-01-13 2014-02-19 诺瓦提斯公司 用于治疗代谢障碍的bace-2抑制剂
DK2663561T3 (en) 2011-01-13 2016-06-06 Novartis Ag New heterocyclic derivatives and their use in treating neurological disorders
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
CN103415519B (zh) * 2011-03-01 2016-03-02 詹森药业有限公司 作为β-分泌酶(BACE)抑制剂有用的6,7-二氢-吡唑[1,5-a]吡嗪-4-基胺衍生物
US9067924B2 (en) * 2011-03-04 2015-06-30 Hoffmann-La Roche Inc. 1,4 thiazepines/sulfones as BACE1 and/or BACE2 inhibitors
PH12013501805A1 (en) 2011-03-09 2013-11-18 Janssen Pharmaceutica Nv 3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (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
EP2694489B1 (fr) 2011-04-07 2017-09-06 Merck Sharp & Dohme Corp. Composés de dioxyde de thiadiazine condensés avec des dérivés oxacycliques en c5-c6 comme inhibiteurs de bace, compositions, et utilisation 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
RU2013150349A (ru) 2011-04-13 2015-05-20 Мерк Шарп И Доум Корп. 5-замещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов васе, содержащие их композиции и их применение
CN103608345A (zh) 2011-04-26 2014-02-26 盐野义制药株式会社 噁嗪衍生物和含有该噁嗪衍生物的bace1抑制剂
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
AU2012266544A1 (en) * 2011-06-07 2013-11-21 F. Hoffmann-La Roche Ag Halogen-alkyl-1,3 oxazines as BACE1 and/or BACE2 inhibitors
MX2013014007A (es) * 2011-06-07 2014-03-12 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
US9181236B2 (en) 2011-08-22 2015-11-10 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
EP2766358B1 (fr) * 2011-10-13 2016-06-22 Novartis AG Dérivés de l'oxazine et leur utilisation pour le traitement d'une maladie
UA111749C2 (uk) 2011-12-05 2016-06-10 Янссен Фармацевтика Нв Похідні 6-дифторметил-5,6-дигідро-2h-[1,4]оксазин-3-аміну
CA2853891C (fr) * 2011-12-06 2020-03-10 Janssen Pharmaceutica Nv Derives de 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2h-[1,4]oxazin-3-amine
PE20142376A1 (es) * 2012-01-26 2015-01-17 Hoffmann La Roche Fluormetil-5,6-dihidro-4h-[1,3]oxazinas
US8338413B1 (en) 2012-03-07 2012-12-25 Novartis Ag Oxazine derivatives and their use in the treatment of neurological disorders
WO2014059185A1 (fr) * 2012-10-12 2014-04-17 Amgen Inc. Composés amino-dihydrothiazine et amino-dioxydo dihydrothiazine en tant qu'antagonistes de bêta-sécrétase et procédés d'utilisation
WO2014065434A1 (fr) 2012-10-24 2014-05-01 Shionogi & Co., Ltd. Dérivés de dihydrooxazine ou d'oxazépine ayant une activité inhibitrice de bace1
WO2014078314A1 (fr) 2012-11-15 2014-05-22 Amgen Inc. Composés d'amino-oxazine et d'amino-dihydrothiazine jouant le rôle de modulateurs de bêta-sécrétase et procédés d'utilisation
AU2013363151A1 (en) 2012-12-20 2015-06-04 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
US9751886B2 (en) 2013-06-12 2017-09-05 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)
WO2014198851A1 (fr) 2013-06-12 2014-12-18 Janssen Pharmaceutica Nv Dérivés de 4-amino-6-phényl-5,6-dihydro-imidazo[1,5-a]pyrazin-3(2h)-one utilisés comme inhibiteurs de la bêta-sécrétase (bace)
CN105283457B (zh) 2013-06-12 2018-09-18 詹森药业有限公司 作为β-分泌酶(BACE)抑制剂的4-氨基-6-苯基-5,6-二氢咪唑并[1,5-A]吡嗪衍生物
FR3025591B1 (fr) * 2014-09-05 2016-10-14 Technofan Dispositif de ventilation, aeronef comportant un tel dispositif de ventilation et procede de surveillance associe
ES2768823T3 (es) 2014-12-18 2020-06-23 Janssen Pharmaceutica Nv Derivados de 2,3,4,5-tetrahidropiridin-6-amina y 3,4-dihidro-2H-pirrol-5-amina útiles como inhibidores de beta-secretasa
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
US10399995B2 (en) 2016-08-26 2019-09-03 Eli Lilly And Company 1,4-Oxazines useful as selective BACE1 inhibitors
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 (fr) 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
CA2514733A1 (fr) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Compositions pharmaceutiques a base d'un co-cristal
TW200505902A (en) * 2003-03-20 2005-02-16 Schering Corp Cannabinoid receptor ligands
JP4707560B2 (ja) 2003-12-29 2011-06-22 Msd株式会社 新規2−ヘテロアリール置換ベンズイミダゾール誘導体
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
CN101346357B (zh) * 2005-10-25 2014-04-02 盐野义制药株式会社 氨基二氢噻嗪衍生物
ES2431163T3 (es) 2007-03-01 2013-11-25 Novartis Ag Inhibidores de PIM quinasa y métodos para su uso
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
EP2689780A1 (fr) 2007-04-24 2014-01-29 Shionogi & Co., Ltd. Intermédiaires de dérivés d'aminodihydrothiazine substitués avec un groupe cyclique
GB0713686D0 (en) 2007-07-13 2007-08-22 Addex Pharmaceuticals Sa New compounds 2
BRPI0906962B8 (pt) 2008-01-18 2021-05-25 Eisai R&D Man Co Ltd composto de aminodiidrotiazina fundido
US20100197688A1 (en) * 2008-05-29 2010-08-05 Nantermet Philippe G Epha4 rtk inhibitors for treatment of neurological and neurodegenerative disorders and cancer
KR101324426B1 (ko) 2008-06-13 2013-10-31 시오노기세야쿠 가부시키가이샤 β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체
TW201028381A (en) 2008-07-14 2010-08-01 Shionogi & Co Pyridine derivative having ttk inhibition activity
CN102186841A (zh) 2008-10-22 2011-09-14 盐野义制药株式会社 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物
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
CN102686584A (zh) 2009-11-13 2012-09-19 盐野义制药株式会社 具有氨基连接基的氨基噻嗪或氨基噁嗪衍生物
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
KR20120104570A (ko) 2009-12-11 2012-09-21 시오노기세야쿠 가부시키가이샤 옥사진 유도체
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
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
ES2459593T3 (es) 2010-06-09 2014-05-09 Janssen Pharmaceutica, N.V. Derivados de 5-amino-3,6-dihidro-1H-pirazin-2-ona útiles como inhibidores de beta-secretasa (BACE)
BR112012004154A2 (pt) * 2010-07-13 2017-05-30 Novartis Ag "derivados de oxazina e seu uso no tratamento de distúrbios neurológicos"
US8524897B2 (en) 2011-01-12 2013-09-03 Novartis Ag Crystalline oxazine derivative
KR20140051822A (ko) 2011-01-12 2014-05-02 노파르티스 아게 옥사진 유도체 및 신경계 장애의 치료에서의 그의 용도
CN103596569A (zh) 2011-01-13 2014-02-19 诺瓦提斯公司 用于治疗代谢障碍的bace-2抑制剂
DK2663561T3 (en) 2011-01-13 2016-06-06 Novartis Ag New heterocyclic derivatives and their use in treating neurological disorders
EP2766358B1 (fr) 2011-10-13 2016-06-22 Novartis AG Dérivés de l'oxazine et leur utilisation pour le traitement d'une maladie

Also Published As

Publication number Publication date
CN102471293A (zh) 2012-05-23
ES2534315T3 (es) 2015-04-21
ZA201200155B (en) 2012-09-26
CU24083B1 (es) 2015-03-30
KR20120039655A (ko) 2012-04-25
MX2012001070A (es) 2012-03-16
EP2456763A1 (fr) 2012-05-30
HK1166314A1 (en) 2012-10-26
AU2010274913A1 (en) 2012-02-02
PE20121440A1 (es) 2012-11-06
US20110021520A1 (en) 2011-01-27
CL2012000185A1 (es) 2012-10-12
ECSP12011622A (es) 2012-02-29
UY32799A (es) 2011-02-28
US8846658B2 (en) 2014-09-30
US8207164B2 (en) 2012-06-26
NZ597529A (en) 2013-11-29
IL217378A (en) 2015-02-26
IL217378A0 (en) 2012-03-01
US20140113894A1 (en) 2014-04-24
EA201200174A1 (ru) 2012-08-30
CO6491058A2 (es) 2012-07-31
US20120238560A1 (en) 2012-09-20
WO2011009943A1 (fr) 2011-01-27
GT201200016A (es) 2013-09-23
JP5767214B2 (ja) 2015-08-19
CU20120013A7 (es) 2012-04-15
AR077328A1 (es) 2011-08-17
KR101422965B1 (ko) 2014-07-23
TW201107316A (en) 2011-03-01
CA2768980A1 (fr) 2011-01-27
JP2013500247A (ja) 2013-01-07
EP2456763B1 (fr) 2015-01-21
US20150018338A1 (en) 2015-01-15
US20140088084A1 (en) 2014-03-27
SG177397A1 (en) 2012-02-28
AU2010274913B2 (en) 2013-09-19
CN102471293B (zh) 2014-10-01
CR20120002A (es) 2012-02-15
KR20140004810A (ko) 2014-01-13

Similar Documents

Publication Publication Date Title
MA33450B1 (fr) Dérivés d'oxazine et leur utilisation en tant qu'inhibiteurs de bace pour le traitement de troubles neurologiques
MA34898B1 (fr) Nouveaux dérivés hétérocycliques et leur utilisation dans le traitement de troubles neurologiques
MA33509B1 (fr) Dérivés de l'oxazine et leur utilisation dans le traitement de troubles neurologiques
EP2091328A4 (fr) Composés de spiropipéridine inhibiteurs de la bêta-sécrétase pour le traitement de la maladie d'alzheimer
MA47079B1 (fr) Composés amino-triazolopyidines et leur utilisation pour traiter le cancer
MA35826B1 (fr) Triazolopyridines substituées et leur utilisation à titre d'inhibiteurs de ttk
EP1841426A4 (fr) Carbinamines tertiaires incluant des heterocycles substitues, agissant en tant qu'inhibiteurs de la beta-secretase et utilisees dans le traitement de la maladie d'alzheimer
MA31766B1 (fr) Composés organiques
TN2011000209A1 (en) Aryl methyl benzoquinazolinone m1 receptor positive allosteric modulators
MA31952B1 (fr) Pyrrolopyrimidines et pyrrolopyridines
TN2015000547A1 (fr) Composes heteroaromatiques et leur utilisation comme ligands de dopamine d1
MA32351B1 (fr) Derives d'aminodihydrothiazine a titre d'inhibiteurs de bace pour le traitement de la maladie d'alzheimer
TN2011000316A1 (fr) Derives de sulfonamides
MA27775A1 (fr) Composes organiques
EP1673078A4 (fr) Inhibiteurs de type benzylether et benzylamino de beta-secretase pour le traitement de la maladie d'alzheimer
MA38391B1 (fr) Dérivés de pyridinyl et triazolone pyridinyl de fusion
EA201290519A1 (ru) Положительные аллостерические модуляторы рецептора хинолин амида m1
MA30405B1 (fr) Derives de 4-benzylphtalazinone substitues en 2 en tant qu'antagonistes des histamines hl et h3
MA31158B1 (fr) Composes tricycliques et leur utilisation comme modulateurs du recepteur de glucocorticoïdes
MA34361B1 (fr) Dérivés de tétrahydro-pyrido-pyrimidine
MA40955A (fr) 2-amino-6-(difluorométhyl)-5,5-difluoro-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1
MX2012002583A (es) Moduladores de piranil aril metil benzoquinazolinona alostericos positivos del receptor m1.
MA39972B1 (fr) Composés et compositions d'induction de la chondrogenèse
MA30532B1 (fr) Sulfonamides tricycliques condenses inhibiteurs de gamma-secretase
MA38999A1 (fr) Nouveaux composés hétérocycliques