ES2768823T3 - Derivados de 2,3,4,5-tetrahidropiridin-6-amina y 3,4-dihidro-2H-pirrol-5-amina útiles como inhibidores de beta-secretasa - Google Patents

Derivados de 2,3,4,5-tetrahidropiridin-6-amina y 3,4-dihidro-2H-pirrol-5-amina útiles como inhibidores de beta-secretasa Download PDF

Info

Publication number
ES2768823T3
ES2768823T3 ES15820456T ES15820456T ES2768823T3 ES 2768823 T3 ES2768823 T3 ES 2768823T3 ES 15820456 T ES15820456 T ES 15820456T ES 15820456 T ES15820456 T ES 15820456T ES 2768823 T3 ES2768823 T3 ES 2768823T3
Authority
ES
Spain
Prior art keywords
compound
formula
acid
reaction
mixture
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.)
Active
Application number
ES15820456T
Other languages
English (en)
Spanish (es)
Inventor
Andrés Trabanco-Suarez
Oscar Delgado-Gonzalez
Henricus Gijsen
Gool Michiel Van
Brandt Sven Van
CLEYN Michel DE
Lardies Santos Fustero
Sanchis Natalia Mateu
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.)
Janssen Pharmaceutica NV
Original Assignee
Janssen Pharmaceutica NV
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 Janssen Pharmaceutica NV filed Critical Janssen Pharmaceutica NV
Application granted granted Critical
Publication of ES2768823T3 publication Critical patent/ES2768823T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
ES15820456T 2014-12-18 2015-12-16 Derivados de 2,3,4,5-tetrahidropiridin-6-amina y 3,4-dihidro-2H-pirrol-5-amina útiles como inhibidores de beta-secretasa Active ES2768823T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14198977 2014-12-18
EP15164704 2015-04-22
PCT/EP2015/079981 WO2016096979A1 (en) 2014-12-18 2015-12-16 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2h-pyrrol-5-amine compound inhibitors of beta-secretase

Publications (1)

Publication Number Publication Date
ES2768823T3 true ES2768823T3 (es) 2020-06-23

Family

ID=55070992

Family Applications (1)

Application Number Title Priority Date Filing Date
ES15820456T Active ES2768823T3 (es) 2014-12-18 2015-12-16 Derivados de 2,3,4,5-tetrahidropiridin-6-amina y 3,4-dihidro-2H-pirrol-5-amina útiles como inhibidores de beta-secretasa

Country Status (13)

Country Link
US (1) US10106524B2 (enExample)
EP (1) EP3233834B1 (enExample)
JP (1) JP2017538753A (enExample)
KR (1) KR20170095881A (enExample)
CN (1) CN107108582B (enExample)
AU (1) AU2015367594C1 (enExample)
CA (1) CA2967164A1 (enExample)
EA (1) EA031041B1 (enExample)
ES (1) ES2768823T3 (enExample)
IL (1) IL252863A0 (enExample)
MX (1) MX2017008083A (enExample)
WO (1) WO2016096979A1 (enExample)
ZA (1) ZA201704116B (enExample)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2011263797B2 (en) 2010-06-09 2014-06-05 Janssen Pharmaceutica Nv 5,6-dihydro-2H-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (BACE)
JP5834091B2 (ja) 2010-12-22 2015-12-16 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 ベータ−セクレターゼ（ＢＡＣＥ）の阻害剤として有用な５，６−ジヒドロ−イミダゾ［１，２−ａ］ピラジン−８−イルアミン誘導体
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
CA2912156C (en) 2013-06-12 2021-07-20 Janssen Pharmaceutica Nv 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace)
CA2911693C (en) 2013-06-12 2021-08-24 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)
CA2967164A1 (en) 2014-12-18 2016-06-23 Janssen Pharmaceutica Nv 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2h-pyrrol-5-amine compound inhibitors of beta-secretase
KR20190075072A (ko) 2016-11-04 2019-06-28 얀센 파마슈티카 엔.브이. 4,4a,5,7-테트라히드로-3H-푸로[3,4-b]피리디닐 화합물
CN116059192B (zh) 2019-11-13 2024-10-29 润佳（苏州）医药科技有限公司 同位素富集的3-氨基-1-丙磺酸及其衍生物的用途
CN113549007B (zh) * 2021-07-23 2023-07-18 清华大学 一种哌啶乙酸酯类化合物的制备方法

Family Cites Families (56)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4188389A (en) 1978-11-03 1980-02-12 Ayerst Mckenna & Harrison, Inc. 1,2,3,4-Tetrahydropyrrolo(1,2-A)pyrazines
TW224974B (enExample) 1991-07-02 1994-06-11 Hoffmann La Roche
WO1998057641A1 (en) 1997-06-18 1998-12-23 Merck & Co., Inc. ALPHA 1a ADRENERGIC RECEPTOR ANTAGONISTS
CA2482991A1 (en) 2002-04-19 2003-10-30 Cellular Genomics, Inc. Imidazo[1,2-a]pyrazin-8-ylamines method of making and method of use thereof
DE60317353T2 (de) 2002-09-23 2008-08-28 Schering Corp. Imidazopyrazine als cdk-inhibitoren
AU2003297431A1 (en) 2002-12-20 2004-07-22 Pharmacia Corporation Mitogen activated protein kinase-activated protein kinase-2 inhibiting compounds
EP1678172B1 (en) 2003-10-15 2009-12-09 Targacept, Inc. Azabicyclic compounds for relieving pain and treating central nervous system disorders
US7618978B2 (en) 2004-04-22 2009-11-17 Eli Lilly And Company Amides as BACE inhibitors
ES2332659T3 (es) 2004-06-16 2010-02-10 Wyeth Derivados de amino-5,5-difenilimidazolona para la inhibicion de beta-secretasa.
TW200624426A (en) 2004-09-21 2006-07-16 Lilly Co Eli BACE inhibitors
CN101103034A (zh) 2005-01-14 2008-01-09 惠氏公司 抑制β-分泌酶的氨基-咪唑酮
US20070005404A1 (en) 2005-06-09 2007-01-04 Drive Diagnostics Ltd. System and method for providing driving insurance
CA2610828A1 (en) 2005-06-14 2006-12-28 Schering Corporation Heterocyclic aspartyl protease inhibitors, preparation and use thereof
EP1896448A1 (en) 2005-06-30 2008-03-12 Wyeth AMINO-5-(6-MEMBERED)HETEROARYLIMIDAZOLONE COMPOUNDS AND THE USE THEREOF FOR ß-SECRETASE MODULATION
EP2612854B1 (en) 2005-10-25 2015-04-29 Shionogi&Co., Ltd. Aminothiazolidine and aminotetrahydrothiazepine derivatives as BACE 1 inhibitors
TW200804290A (en) 2005-11-15 2008-01-16 Astrazeneca Ab Compounds and uses thereof
JP2009532464A (ja) 2006-04-05 2009-09-10 アストラゼネカ・アクチエボラーグ ２−アミノピリミジン−４−オン及びＡβ−関連の病理を治療又は予防するためのその使用
US20080051420A1 (en) 2006-06-14 2008-02-28 Astrazeneca Ab New Compounds 317
TW200902526A (en) 2007-04-24 2009-01-16 Shionogi & Amp Co Ltd Aminodihydrothiazin derivative substituted with a cyclic group
TW200902499A (en) 2007-05-15 2009-01-16 Astrazeneca Ab New compounds
WO2009058300A1 (en) 2007-10-30 2009-05-07 Arena Pharmaceuticals, Inc. Biphenyl derivatives as modulators of the histamine-h3 receptor useful for the treatment of disorders related thereto
NZ586831A (en) 2008-01-28 2012-02-24 Janssen Pharmaceutica Nv 6-substituted-thio-2-amino-quinoline derivatives useful as inhibitors of beta-secretase (bace)
NZ587039A (en) 2008-02-13 2013-01-25 Gilead Connecticut Inc 6-aryl-imidazo[1, 2-a]pyrazine derivatives, method of making, and method of use thereof
TWI431004B (zh) 2008-05-02 2014-03-21 Lilly Co Eli Ｂａｃｅ抑制劑
PA8854101A1 (es) 2008-12-18 2010-07-27 Ortho Mcneil Janssen Pharm Derivados de imidazol bicíclicos sustituidos como moduladores de gamma secretasa
WO2011002409A1 (en) 2009-07-02 2011-01-06 Astrazeneca Ab 5h-pyrrolo[3,4-£>]pyrazin-7-amine derivatives inhibitors of beta-secretase
AR077277A1 (es) 2009-07-09 2011-08-17 Lilly Co Eli Compuestos de biciclo (1,3)tiazin-2-amina formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de la enfermedad de alzheimer
AR077328A1 (es) 2009-07-24 2011-08-17 Novartis Ag Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos
US8188079B2 (en) 2009-08-19 2012-05-29 Hoffman-La Roche Inc. 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines
WO2011058763A1 (ja) 2009-11-13 2011-05-19 塩野義製薬株式会社 アミノリンカーを有するアミノチアジンまたはアミノオキサジン誘導体
UA110467C2 (uk) 2009-12-11 2016-01-12 Шионогі Енд Ко., Лтд. Похідні оксазину
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
JPWO2011077726A1 (ja) * 2009-12-24 2013-05-02 塩野義製薬株式会社 ４−アミノ−１，３−チアジンまたはオキサジン誘導体
CN102712621B (zh) 2009-12-31 2015-03-11 诺华股份有限公司 吡嗪衍生物及其在治疗神经学障碍中的用途
CN102918036A (zh) 2010-06-09 2013-02-06 詹森药业有限公司 用作β-分泌酶(BACE)抑制剂的5-氨基-3,6-二氢-1H-吡嗪-2-酮衍生物
AU2011263797B2 (en) 2010-06-09 2014-06-05 Janssen Pharmaceutica Nv 5,6-dihydro-2H-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (BACE)
JP2013529664A (ja) 2010-06-28 2013-07-22 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 アルツハイマー病および他の型の認知症の処置に有用な３−アミノ−５，６−ジヒドロ−１ｈ−ピラジン−２−オン誘導体
NZ606848A (en) 2010-09-22 2015-01-30 Janssen Pharmaceutica Nv 4,7-dihydro-pyrazolo[1,5-a]pyrazin-6-ylamine derivatives useful as inhibitors of beta-secretase (bace)
EP2634188A4 (en) 2010-10-29 2014-05-07 Shionogi & Co FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE
JP5834091B2 (ja) 2010-12-22 2015-12-16 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 ベータ−セクレターゼ（ＢＡＣＥ）の阻害剤として有用な５，６−ジヒドロ−イミダゾ［１，２−ａ］ピラジン−８−イルアミン誘導体
EA201391029A1 (ru) 2011-01-12 2014-01-30 Новартис Аг Производные оксазина и их применение при лечении неврологических нарушений
EA201391033A1 (ru) 2011-01-13 2014-01-30 Новартис Аг Ингибиторы bace-2 для лечения метаболических расстройств
JP2012147763A (ja) 2011-01-17 2012-08-09 Toshitaka Kobayashi 乾物穿孔具
US9242943B2 (en) 2011-01-18 2016-01-26 Siena Biotech S.P.A. 1,4 oxazines as BACE1 and/or BACE2 inhibitors
ES2558779T3 (es) 2011-03-01 2016-02-08 Janssen Pharmaceutica, N.V. Derivados de 6,7-dihidro-pirazolo[1,5-a]piracin-4-ilamina útiles como inhibidores de ß-secretasa (BACE)
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
WO2012147763A1 (ja) 2011-04-26 2012-11-01 塩野義製薬株式会社 オキサジン誘導体およびそれを含有するｂａｃｅ１阻害剤
EA201490774A1 (ru) 2011-10-13 2014-08-29 Новартис Аг Новые производные оксазина и их применение при лечении заболевания
UA111749C2 (uk) 2011-12-05 2016-06-10 Янссен Фармацевтика Нв Похідні 6-дифторметил-5,6-дигідро-2h-[1,4]оксазин-3-аміну
US20140364428A1 (en) 2011-12-06 2014-12-11 Janssen Pharmaceutica Nv 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives
EP2807155B1 (en) * 2012-01-26 2017-04-12 F. Hoffmann-La Roche AG Fluoromethyl-5,6-dihydro-4h-[1,3]oxazines
CA2894919A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. C5,c6 oxacyclic-fused iminothiazine dioxide compounds as bace inhibitors, compositions, and their use
AU2014280124B2 (en) 2013-06-12 2018-11-01 Janssen Pharmaceutica Nv 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (BACE)
CA2911693C (en) 2013-06-12 2021-08-24 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)
CA2912156C (en) 2013-06-12 2021-07-20 Janssen Pharmaceutica Nv 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace)
CA2967164A1 (en) 2014-12-18 2016-06-23 Janssen Pharmaceutica Nv 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2h-pyrrol-5-amine compound inhibitors of beta-secretase

Also Published As

Publication number Publication date
ZA201704116B (en) 2019-12-18
CA2967164A1 (en) 2016-06-23
JP2017538753A (ja) 2017-12-28
US20170362198A1 (en) 2017-12-21
MX2017008083A (es) 2017-10-31
EA201791367A1 (ru) 2017-10-31
CN107108582B (zh) 2019-10-18
WO2016096979A1 (en) 2016-06-23
AU2015367594C1 (en) 2019-10-31
AU2015367594A1 (en) 2017-06-01
AU2015367594B2 (en) 2019-07-18
EP3233834B1 (en) 2019-11-13
US10106524B2 (en) 2018-10-23
CN107108582A (zh) 2017-08-29
KR20170095881A (ko) 2017-08-23
EA031041B1 (ru) 2018-11-30
IL252863A0 (en) 2017-08-31
EP3233834A1 (en) 2017-10-25

Similar Documents

Publication Publication Date Title
JP5711813B2 (ja) 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
ES2582473T3 (es) Derivados de 5-(3-aminofenil)-5-alquil-5,6-dihidro-2H-[1,4]oxazin-3-amina para el tratamiento de trastornos en que está implicada la beta-secretasa
EP2588466B1 (en) 5-Amino-3,6-dihydro-1H-pyrazin-2-one derivatives useful as inhibitors of beta-secretase (BACE)
CN104703983B (zh) N2,n4‑双(4‑(哌嗪‑1‑基)苯基)嘧啶‑2,4‑二胺衍生物或其药学上可接受的盐，及以其作为活性成分用于预防或治疗癌症的组合物
ES2534973T3 (es) Derivados de 3,4-dihidro-pirrolo[1,2-a]pirazin-1-ilamina útiles como inhibidores de beta-secretasa (BACE)
JP2008526761A (ja) 多環式ビス−アミドｍｍｐ阻害剤
SG186408A1 (en) 3-amino-5, 6-dihydro-1h-pyrazin-2-one derivatives useful for the treatment of alzheimer's disease and other forms of dementia
CN107108582B (zh) β-分泌酶的2，3，4，5-四氢吡啶-6-胺化合物抑制剂
JP2011518142A (ja) Ｆａａｈ阻害剤として有用なエーテルベンジリデンピペリジン５員アリールカルボキサミド化合物
JP2011518143A (ja) Ｆａａｈ阻害剤として有用なエーテルベンジリデンピペリジンアリールカルボキサミド化合物
ES2358445T3 (es) Derivados de azabiciclo (3.1.0) hexano útiles como moduladores de los receptores d3 de dopamina.
JP2011518144A (ja) Ｆａａｈ阻害剤として有用な４−ベンジリデン−３−メチルピペリジンアリールカルボキサミド化合物
AU2011263836A1 (en) 5-amino-3,6-dihydro-1H-pyrazin-2-one derivatives useful as inhibitors of beta-secretase (BACE)
NZ612990B2 (en) Novel heterocyclic derivatives and their use in the treatment of neurological disorders
NZ623858B2 (en) 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives