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

옥사진 유도체 및 신경계 장애의 치료에서의 그의 용도 Download PDF

Info

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
Authority
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Withdrawn
Application number
KR20137021073A
Other languages
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
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 노파르티스 아게 filed Critical 노파르티스 아게
Publication of KR20140051822A publication Critical patent/KR20140051822A/ko
Withdrawn legal-status Critical Current

Links

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 (enExample)
EP (1) EP2663559B1 (enExample)
JP (1) JP2014505688A (enExample)
KR (1) KR20140051822A (enExample)
CN (1) CN103429589A (enExample)
AU (1) AU2012206555A1 (enExample)
BR (1) BR112013017779A2 (enExample)
CA (1) CA2824097A1 (enExample)
EA (1) EA201391029A1 (enExample)
MX (1) MX2013008111A (enExample)
WO (1) WO2012095463A1 (enExample)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101324426B1 (ko) 2008-06-13 2013-10-31 시오노기세야쿠 가부시키가이샤 β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체
UY32799A (es) 2009-07-24 2011-02-28 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
EP2485591B1 (en) 2009-10-08 2016-03-23 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2485920B1 (en) 2009-10-08 2016-04-27 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
KR20120104570A (ko) 2009-12-11 2012-09-21 시오노기세야쿠 가부시키가이샤 옥사진 유도체
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
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)
DK2663561T3 (en) 2011-01-13 2016-06-06 Novartis Ag New heterocyclic derivatives and their use in treating neurological disorders
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)
EP2766358B1 (en) 2011-10-13 2016-06-22 Novartis AG Novel oxazine derivatives and their use in the treatment of disease
UA111749C2 (uk) * 2011-12-05 2016-06-10 Янссен Фармацевтика Нв Похідні 6-дифторметил-5,6-дигідро-2h-[1,4]оксазин-3-аміну
WO2014065434A1 (en) 2012-10-24 2014-05-01 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity
JP6389830B2 (ja) 2013-03-01 2018-09-12 アムジエン・インコーポレーテツド ベータ−セクレターゼ阻害剤としてのパーフルオロ化５，６−ジヒドロ−４ｈ−１，３−オキサジン−２−アミン化合物および使用方法
JP6374889B2 (ja) 2013-03-08 2018-08-15 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過フッ素化シクロプロピル縮合１，３−オキサジン−２−アミン化合物、及び使用方法
WO2014198851A1 (en) 2013-06-12 2014-12-18 Janssen Pharmaceutica Nv 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace)
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)
GEAP201814248A (en) * 2014-02-19 2018-04-10 H Lundbeck As 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease
US9550762B2 (en) 2014-08-08 2017-01-24 Amgen, Inc. Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
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
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
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
JP2018531889A (ja) 2015-08-12 2018-11-01 ハー・ルンドベック・アクチエゼルスカベット Ｂａｃｅ１阻害剤としての２−アミノ−３−フルオロ−３−（フルオロメチル）−６−メチル−６−フェニル−３，４，５，６−テトラヒドロピリジン
US10399995B2 (en) 2016-08-26 2019-09-03 Eli Lilly And Company 1,4-Oxazines useful as selective BACE1 inhibitors
MX388697B (es) 2016-12-15 2025-03-20 Amgen Inc Derivados de tiazina como inhibidores de beta-secretasa y metodos de uso.
MA52722A (fr) 2016-12-15 2021-04-14 Amgen Inc Dérivés d'oxazine en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation
MX386618B (es) 2016-12-15 2025-03-19 Amgen Inc Derivados de tiazina condensados con ciclopropilo como inhibidores de beta-secretasa y métodos de uso.
MA54101A (fr) 2016-12-15 2021-10-27 Amgen Inc Dérivés de thiazine et d'oxazine bicycliques en tant qu'inhibiteurs de bêta-sécrétase et procédés d'utilisation
EP3555086B1 (en) 2016-12-15 2021-09-01 Amgen Inc. 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide 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

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL6911868A (enExample) 1968-08-31 1970-03-03
DE19725802A1 (de) 1996-07-10 1998-01-15 Lonza Ag Verfahren zur Herstellung von (S)- oder (R)-3,3,3-trifluor-2-hydroxy-2-methylpropionsäure
CA2514733A1 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
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
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
BRPI0906962B8 (pt) 2008-01-18 2021-05-25 Eisai R&D Man Co Ltd composto de aminodiidrotiazina fundido
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
BR112012004154A2 (pt) * 2010-07-13 2017-05-30 Novartis Ag "derivados de oxazina e seu uso no tratamento de distúrbios neurológicos"

Also Published As

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

Similar Documents

Publication Publication Date Title
KR20140051822A (ko) 옥사진 유도체 및 신경계 장애의 치료에서의 그의 용도
KR101422965B1 (ko) 옥사진 유도체, 및 신경계 장애의 치료를 위한 ｂａｃｅ 억제제로서의 그의 용도
KR101391041B1 (ko) 옥사진 유도체, 및 신경계 장애의 치료에 있어서의 그의 용도
KR101569260B1 (ko) 신규 헤테로시클릭 유도체 및 신경계 장애의 치료에서의 그의 용도
KR101419157B1 (ko) 피라진 유도체 및 신경계 장애의 치료에서의 그의 용도
US8338413B1 (en) Oxazine derivatives and their use in the treatment of neurological disorders
HK1188453B (en) Novel heterocyclic derivatives and their use in the treatment of neurological disorders
AU2013273640A1 (en) Oxazine derivatives and their use as BACE inhibitors for the treatment of neurological disorders

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