AU2012206555A1 - Oxazine derivatives and their use in the treatment of neurological disorders - Google Patents

Oxazine derivatives and their use in the treatment of neurological disorders Download PDF

Info

Publication number
AU2012206555A1
AU2012206555A1 AU2012206555A AU2012206555A AU2012206555A1 AU 2012206555 A1 AU2012206555 A1 AU 2012206555A1 AU 2012206555 A AU2012206555 A AU 2012206555A AU 2012206555 A AU2012206555 A AU 2012206555A AU 2012206555 A1 AU2012206555 A1 AU 2012206555A1
Authority
AU
Australia
Prior art keywords
amino
phenyl
fluoro
oxazin
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.)
Abandoned
Application number
AU2012206555A
Other languages
English (en)
Inventor
Konstanze Hurth
Rainer Martin Lueoend
Rainer Machauer
Ulf Neumann
Heinrich Rueeger
Michael Schaefer
Marina Tintelnot-Blomley
Siem Jacob Veenstra
Markus Voegtle
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
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
Application filed by Novartis AG filed Critical Novartis AG
Publication of AU2012206555A1 publication Critical patent/AU2012206555A1/en
Abandoned 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)
AU2012206555A 2011-01-12 2012-01-11 Oxazine derivatives and their use in the treatment of neurological disorders Abandoned AU2012206555A1 (en)

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
AU2012206555A1 true AU2012206555A1 (en) 2013-08-01

Family

ID=45476523

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2012206555A Abandoned AU2012206555A1 (en) 2011-01-12 2012-01-11 Oxazine derivatives and their use in the treatment of neurological disorders

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
US8637504B2 (en) 2008-06-13 2014-01-28 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity
UY32799A (es) 2009-07-24 2011-02-28 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurológicos
WO2011044185A2 (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
RU2012129168A (ru) 2009-12-11 2014-01-20 Сионоги Энд Ко. Лтд. Производные оксазина
AR081587A1 (es) 2010-06-09 2012-10-03 Janssen Pharmaceutica Nv DERIVADOS DE 5,6-DIHIDRO-2H-[1,4]OXAZIN-3-IL-AMINA UTILES COMO INHIBIDORES DE LA b-SECRETASA (BACE)
ES2648143T3 (es) 2010-12-22 2017-12-28 Janssen Pharmaceutica Nv Derivados de 5,6-dihidro-imidazo[1,2-a]pirazin-8-ilamina útiles como inhibidores de la beta-secretasa (BACE)
KR101569260B1 (ko) 2011-01-13 2015-11-13 노파르티스 아게 신규 헤테로시클릭 유도체 및 신경계 장애의 치료에서의 그의 용도
JP5853035B2 (ja) 2011-03-09 2016-02-09 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３，４−ジヒドロ−ピロロ［１，２−ａ］ピラジン−１−イルアミン誘導体
US9284284B2 (en) 2011-10-13 2016-03-15 Novartis Ag 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
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
AU2014223334C1 (en) 2013-03-01 2018-10-18 Amgen Inc. Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
EP2964644B1 (en) 2013-03-08 2018-12-26 Amgen, Inc. Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
EP3008067B1 (en) 2013-06-12 2017-03-29 Janssen Pharmaceutica N.V. 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace)
BR112015030597A2 (pt) 2013-06-12 2017-07-25 Janssen Pharmaceutica Nv derivados 4-amino-6-fenil-6,7-di-hidro[1,2,3]triazolo[1,5-a]pirazina como inibidores de beta-secretase (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
MX381482B (es) 2014-08-08 2025-03-12 Amgen Inc Compuestos de tiazin-2-amina fusionados con ciclopropilo como inhibidores de beta-secretasa y metodos de uso.
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
JP2017538753A (ja) 2014-12-18 2017-12-28 ヤンセン ファーマシューティカ エヌ．ベー． ２，３，４，５−テトラヒドロピリジン−６−アミンおよび３，４−ジヒドロ−２Ｈ−ピロール−５−アミンの化合物のβセクレターゼ阻害剤
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
RU2018104868A (ru) 2015-08-12 2019-09-13 Х. Лундбекк А/С 2-амино-3-фтор-3-(фторметил)-6-метил-6-фенил-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1
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
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.
AU2017376445B2 (en) 2016-12-15 2021-09-30 Amgen Inc. Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use
MX387729B (es) 2016-12-15 2025-03-18 Amgen Inc Derivados de dióxido de 1,4-tiazina y dióxido 1,2,4-tiadiazina como inhibidores de beta-secretasa y métodos de uso.
MX388697B (es) 2016-12-15 2025-03-20 Amgen Inc Derivados de tiazina como inhibidores de beta-secretasa y metodos de uso.
AU2017376441B2 (en) * 2016-12-15 2021-10-14 Amgen Inc. Oxazine 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
WO2004078163A2 (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
US7728025B2 (en) 2003-12-29 2010-06-01 Banyu Pharmaceutical Co., Ltd. 2-heteroaryl-substituted benzimidazole derivative
ES2537898T3 (es) * 2005-10-25 2015-06-15 Shionogi & Co., Ltd. Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1
BRPI0906962B8 (pt) 2008-01-18 2021-05-25 Eisai R&D Man Co Ltd composto de aminodiidrotiazina fundido
WO2010047372A1 (ja) 2008-10-22 2010-04-29 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
CN102666507B (zh) * 2010-07-13 2014-09-17 诺华股份有限公司 噁嗪衍生物及其在治疗神经病症中的用途

Also Published As

Publication number Publication date
US20130281449A1 (en) 2013-10-24
KR20140051822A (ko) 2014-05-02
EP2663559A1 (en) 2013-11-20
JP2014505688A (ja) 2014-03-06
BR112013017779A2 (pt) 2016-10-11
WO2012095463A1 (en) 2012-07-19
MX2013008111A (es) 2013-10-30
CN103429589A (zh) 2013-12-04
EP2663559B1 (en) 2015-07-01
EA201391029A1 (ru) 2014-01-30
CA2824097A1 (en) 2012-07-19

Similar Documents

Publication Publication Date Title
EP2663559B1 (en) Oxazine derivatives and their use in the treatment of neurological disorders
AU2011278825B2 (en) Oxazine derivatives and their use in the treatment of neurological disorders
AU2010274913B2 (en) Oxazine derivatives and their use as BACE inhibitors for the treatment of neurological disorders
AU2012206561B2 (en) Novel heterocyclic derivatives and their use in the treatment of neurological disorders
AU2010338365B2 (en) Pyrazine derivatives and their use in the treatment of neurological disorders
US8338413B1 (en) Oxazine 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
HK1188453B (en) Novel heterocyclic derivatives and their use in the treatment of neurological disorders
HK1166314B (en) Oxazine derivatives and their use as bace inhibitors for the treatment of neurological disorders
NZ612990B2 (en) Novel heterocyclic derivatives and their use in the treatment of neurological disorders

Legal Events

Date Code Title Description
MK4 Application lapsed section 142(2)(d) - no continuation fee paid for the application