KR20140051822A - 옥사진 유도체 및 신경계 장애의 치료에서의 그의 용도 - Google Patents

옥사진 유도체 및 신경계 장애의 치료에서의 그의 용도 Download PDF

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Publication number
KR20140051822A
KR20140051822A KR20137021073A KR20137021073A KR20140051822A KR 20140051822 A KR20140051822 A KR 20140051822A KR 20137021073 A KR20137021073 A KR 20137021073A KR 20137021073 A KR20137021073 A KR 20137021073A KR 20140051822 A KR20140051822 A KR 20140051822A
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KR
South Korea
Prior art keywords
phenyl
fluoro
amino
carboxylic acid
dihydro
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
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KR20137021073A
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English (en)
Korean (ko)
Inventor
콘스탄체 후르트
라이너 마르틴 뤼왼드
라이너 마하우어
울프 노이만
하인리히 루이거
미하엘 섀퍼
마리나 틴텔노트-블로믈레이
짐 야콥 빈스트라
마르쿠스 푀그틀레
Original Assignee
노파르티스 아게
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Application filed by 노파르티스 아게 filed Critical 노파르티스 아게
Publication of KR20140051822A publication Critical patent/KR20140051822A/ko
Withdrawn legal-status Critical Current

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Classifications

    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P25/28—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
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR20137021073A 2011-01-12 2012-01-11 옥사진 유도체 및 신경계 장애의 치료에서의 그의 용도 Withdrawn KR20140051822A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161432037P 2011-01-12 2011-01-12
US61/432,037 2011-01-12
PCT/EP2012/050387 WO2012095463A1 (en) 2011-01-12 2012-01-11 Oxazine derivatives and their use in the treatment of neurological disorders

Publications (1)

Publication Number Publication Date
KR20140051822A true KR20140051822A (ko) 2014-05-02

Family

ID=45476523

Family Applications (1)

Application Number Title Priority Date Filing Date
KR20137021073A Withdrawn KR20140051822A (ko) 2011-01-12 2012-01-11 옥사진 유도체 및 신경계 장애의 치료에서의 그의 용도

Country Status (11)

Country Link
US (1) US20130281449A1 (cg-RX-API-DMAC7.html)
EP (1) EP2663559B1 (cg-RX-API-DMAC7.html)
JP (1) JP2014505688A (cg-RX-API-DMAC7.html)
KR (1) KR20140051822A (cg-RX-API-DMAC7.html)
CN (1) CN103429589A (cg-RX-API-DMAC7.html)
AU (1) AU2012206555A1 (cg-RX-API-DMAC7.html)
BR (1) BR112013017779A2 (cg-RX-API-DMAC7.html)
CA (1) CA2824097A1 (cg-RX-API-DMAC7.html)
EA (1) EA201391029A1 (cg-RX-API-DMAC7.html)
MX (1) MX2013008111A (cg-RX-API-DMAC7.html)
WO (1) WO2012095463A1 (cg-RX-API-DMAC7.html)

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JP5490692B2 (ja) 2008-06-13 2014-05-14 塩野義製薬株式会社 βセクレターゼ阻害作用を有する含硫黄複素環誘導体
AR077328A1 (es) 2009-07-24 2011-08-17 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos
WO2011044187A1 (en) 2009-10-08 2011-04-14 Schering Corporation Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
WO2011044185A2 (en) 2009-10-08 2011-04-14 Schering Corporation Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
UA110467C2 (uk) 2009-12-11 2016-01-12 Шионогі Енд Ко., Лтд. Похідні оксазину
JP5711813B2 (ja) 2010-06-09 2015-05-07 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプＪａｎｓｓｅｎ Ｐｈａｒｍａｃｅｕｔｉｃａ Ｎａａｍｌｏｚｅ Ｖｅｎｎｏｏｔｓｃｈａｐ βセクレターゼ（ＢＡＣＥ）の阻害剤として有用な５，６−ジヒドロ−２Ｈ−［１，４］オキサジン−３−イル−アミン誘導体
WO2012085038A1 (en) 2010-12-22 2012-06-28 Janssen Pharmaceutica Nv 5,6-DIHYDRO-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
KR101569260B1 (ko) 2011-01-13 2015-11-13 노파르티스 아게 신규 헤테로시클릭 유도체 및 신경계 장애의 치료에서의 그의 용도
EA023824B1 (ru) 2011-03-09 2016-07-29 Янссен Фармацевтика Нв ПРОИЗВОДНЫЕ 3,4-ДИГИДРОПИРРОЛО[1,2-a]ПИРАЗИН-1-ИЛАМИНА, ПРИГОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (BACE)
WO2013054291A1 (en) 2011-10-13 2013-04-18 Novartis Ag Novel oxazine derivatives and their use in the treatment of disease
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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
MX366855B (es) 2013-03-01 2019-07-26 Amgen Inc Compuestos perfluorados de 5,6-dihidro-4h-1,3-oxazin-2-amina como inhibidores de beta-secretasa y metodos de uso.
CN105164121A (zh) 2013-03-08 2015-12-16 美国安进公司 作为β分泌酶抑制剂的全氟化环丙基稠合的1,3-噁嗪-2-胺化合物以及其使用方法
CN105324383B (zh) 2013-06-12 2017-10-31 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‑6,7‑二氢[1,2,3]三唑并[1,5‑A]吡嗪衍生物
EA032662B1 (ru) 2013-06-12 2019-06-28 Янссен Фармацевтика Нв ПРОИЗВОДНЫЕ 4-АМИНО-6-ФЕНИЛ-5,6-ДИГИДРОИМИДАЗО[1,5-а]ПИРАЗИН-3(2H)-ОНА В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (BACE)
US20170066741A1 (en) 2014-02-19 2017-03-09 H. Lundbeck A/S 2-Amino-3,5,5-Trifluoro-3,4,5,6-Tetrahydropyridines as BACE1 Inhibitors for Treatment of Alzheimer's Disease
EP3177618A1 (en) 2014-08-08 2017-06-14 Amgen Inc. Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
JO3458B1 (ar) 2014-11-10 2020-07-05 H Lundbeck As 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1
MA40941A (fr) 2014-11-10 2017-09-19 H Lundbeck As 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1
CR20170187A (es) 2014-11-10 2018-02-01 H Lundbeck As 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer
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
TW201717948A (zh) 2015-08-10 2017-06-01 Ｈ 朗德貝克公司 包括給予２－胺基－３，５，５－三氟－３，４，５，６－四氫吡啶的聯合治療
CN107849011A (zh) 2015-08-12 2018-03-27 H.隆德贝克有限公司 作为bace1抑制剂的2‑氨基‑3‑氟‑3‑(氟甲基)‑6‑甲基‑6‑苯基‑3,4,5,6‑四氢吡啶
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
AU2017376441B2 (en) 2016-12-15 2021-10-14 Amgen Inc. Oxazine derivatives as beta-secretase inhibitors and methods of use
CA3047288A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Thiazine derivatives as beta-secretase inhibitors and methods of use
JP7148518B2 (ja) 2016-12-15 2022-10-05 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二環式チアジンおよびオキサジン誘導体ならびに使用方法
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
AU2017378316B2 (en) 2016-12-15 2021-04-01 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
KR102093540B1 (ko) * 2017-08-11 2020-03-25 주식회사 엘지화학 할로겐 치환된 스티렌 모노머의 제조방법
CN111675708A (zh) * 2020-06-10 2020-09-18 南京合巨药业有限公司 一种6-氰基-7-氮杂吲哚及其衍生物的制备方法
CN111943947B (zh) * 2020-07-24 2021-04-30 重庆文理学院 1H-吡咯[2,3-b]吡啶衍生物及其合成方法与应用

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Also Published As

Publication number Publication date
CN103429589A (zh) 2013-12-04
CA2824097A1 (en) 2012-07-19
MX2013008111A (es) 2013-10-30
WO2012095463A1 (en) 2012-07-19
EA201391029A1 (ru) 2014-01-30
US20130281449A1 (en) 2013-10-24
AU2012206555A1 (en) 2013-08-01
EP2663559B1 (en) 2015-07-01
JP2014505688A (ja) 2014-03-06
EP2663559A1 (en) 2013-11-20
BR112013017779A2 (pt) 2016-10-11

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Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20130809

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
PC1203 Withdrawal of no request for examination
WITN Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid