BR112015030498A2 - derivados 4-amino-6-fenil-5,6-di-hidroimidazo[1,5-a]pirazin-3(2h)-ona como inibidores de beta-secretase (bace) - Google Patents

derivados 4-amino-6-fenil-5,6-di-hidroimidazo[1,5-a]pirazin-3(2h)-ona como inibidores de beta-secretase (bace)

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Publication number
BR112015030498A2
BR112015030498A2 BR112015030498A BR112015030498A BR112015030498A2 BR 112015030498 A2 BR112015030498 A2 BR 112015030498A2 BR 112015030498 A BR112015030498 A BR 112015030498A BR 112015030498 A BR112015030498 A BR 112015030498A BR 112015030498 A2 BR112015030498 A2 BR 112015030498A2
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Prior art keywords
beta
dementia
dihydroimidazo
bace
pyrazin
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BR112015030498A
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English (en)
Inventor
Oehlrich Daniel
Jacobus Maria Gijsen Henricus
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Janssen Pharmaceutica Nv
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Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of BR112015030498A2 publication Critical patent/BR112015030498A2/pt

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    • C07D487/02—Heterocyclic 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
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Abstract

resumo patente de invenção: "derivados 4-amino-6-fenil-5,6-di-hidroimidazo[1,5-a]pirazin-3(2h)-ona como inibidores de beta-secretase (bace)". a presente invenção refere-se a novos derivados 5,6-di-hidroimidazo[1,5-a]pirazin-3(2h)-ona como inibidores de beta-secretase, também conhecida como enzima de clivagem de amiloide de local beta, bace, em particular bace1 e/ou bace2 (em que bace1 também é conhecida como asp2, ou memapsina2, e bace2 também é conhecida como asp1, memapsina 1 ou drap). a invenção também é dirigida a composições farmacêuticas compreendendo tais compostos, a processos para a preparação de tais compostos e composições, e ao uso de tais compostos e composições para a prevenção e tratamento de distúrbios nos quais está envolvida a beta-secretase, como doença de alzheimer (ad), defeito cognitivo ligeiro, senilidade, demência, demência com corpos de lewy, síndrome de down, demência associada a derrame cerebral, demência associada à doença de parkinson, demência do tipo alzheimer, demência associada a beta-amiloide, degeneração macular relacionada à idade, diabetes do tipo 2 e outros distúrbios metabólicos.
BR112015030498A 2013-06-12 2014-06-12 derivados 4-amino-6-fenil-5,6-di-hidroimidazo[1,5-a]pirazin-3(2h)-ona como inibidores de beta-secretase (bace) BR112015030498A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP13171723 2013-06-12
PCT/EP2014/062283 WO2014198851A1 (en) 2013-06-12 2014-06-12 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazin-3(2h)-one derivatives as inhibitors of beta-secretase (bace)

Publications (1)

Publication Number Publication Date
BR112015030498A2 true BR112015030498A2 (pt) 2017-07-25

Family

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BR112015030498A BR112015030498A2 (pt) 2013-06-12 2014-06-12 derivados 4-amino-6-fenil-5,6-di-hidroimidazo[1,5-a]pirazin-3(2h)-ona como inibidores de beta-secretase (bace)

Country Status (12)

Country Link
US (1) US9834559B2 (pt)
EP (1) EP3008067B1 (pt)
JP (1) JP6387402B2 (pt)
KR (1) KR102243135B1 (pt)
CN (1) CN105452251B (pt)
AU (1) AU2014280122B2 (pt)
BR (1) BR112015030498A2 (pt)
CA (1) CA2912156C (pt)
EA (1) EA032662B1 (pt)
ES (1) ES2627633T3 (pt)
MX (1) MX368326B (pt)
WO (1) WO2014198851A1 (pt)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011154431A1 (en) 2010-06-09 2011-12-15 Janssen Pharmaceutica Nv 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace)
AU2011347377B2 (en) 2010-12-22 2016-03-03 Janssen Pharmaceutica Nv 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives useful as inhibitors of beta-secretase (BACE)
ES2534973T3 (es) 2011-03-09 2015-04-30 Janssen Pharmaceutica N.V. Derivados de 3,4-dihidro-pirrolo[1,2-a]pirazin-1-ilamina útiles como inhibidores de beta-secretasa (BACE)
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
CN105452251B (zh) 2013-06-12 2017-12-26 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‑3(2H)‑酮衍生物
EP3008066B1 (en) 2013-06-12 2018-08-15 Janssen Pharmaceutica N.V. 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace)
EP3233834B1 (en) 2014-12-18 2019-11-13 Janssen Pharmaceutica NV 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2h-pyrrol-5-amine derivatives useful as inhibitors of beta-secretase
CN111484497B (zh) * 2019-01-25 2021-07-02 江苏恒瑞医药股份有限公司 咪唑并[1,5-a]吡嗪类衍生物的可药用盐、晶型及其制备方法

Family Cites Families (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA825620A (en) 1969-10-21 E. Mccown William Producing sheet glass
AU515569B2 (en) 1977-11-11 1981-04-09 Phillips Petroleum Company Coupled diene polymers
US4188389A (en) 1978-11-03 1980-02-12 Ayerst Mckenna & Harrison, Inc. 1,2,3,4-Tetrahydropyrrolo(1,2-A)pyrazines
TW224974B (pt) 1991-07-02 1994-06-11 Hoffmann La Roche
EP0998285A4 (en) 1997-06-18 2003-01-08 Merck & Co Inc ANTAGONISTS OF THE ALPHA 1a ADRENERIC RECEPTOR
IL164703A0 (en) 2002-04-19 2005-12-18 Cellular Genomics Inc ImidazoÄ1,2-AÜpyrazin-8-ylamines method of making and method of use thereof
DE10242984B4 (de) 2002-09-17 2010-09-23 Sanatis Gmbh Vorrichtung zum Herstellen von Gemischen aus zwei Komponenten
EP1543008B1 (en) 2002-09-23 2007-11-07 Schering Corporation Imidazopyrazines as cyclin dependent kinase inhibitors
BR0317525A (pt) 2002-12-20 2005-11-16 Pharmacia Corp Compostos pirazol acìclico, composição terapêutica e farmacêutica, kit, bem como respectivos usos
WO2005037832A2 (en) 2003-10-15 2005-04-28 Targacept, Inc. Azabicycyclic compounds for relieving pain and treating central nervous system disorders
JP2007533740A (ja) 2004-04-22 2007-11-22 イーライ リリー アンド カンパニー Ｂａｃｅ阻害剤としてのアミド
PE20060459A1 (es) 2004-06-16 2006-05-30 Wyeth Corp DERIVADOS DE AMINO-5,5-DIFENILIMIDAZOLONA COMO INHIBIDORES DE LA ß-SECRETASA
PE20060692A1 (es) 2004-09-21 2006-07-19 Lilly Co Eli Inhibidores bace
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
KR20080028881A (ko) 2005-06-14 2008-04-02 쉐링 코포레이션 헤테로사이클릭 아스파르틸 프로테아제 억제제, 이의제조방법 및 용도
WO2007005404A1 (en) 2005-06-30 2007-01-11 Wyeth AMINO-5-(6-MEMBERED)HETEROARYLIMIDAZOLONE COMPOUNDS AND THE USE THEREOF FOR ß-SECRETASE MODULATION
ES2476027T3 (es) 2005-10-25 2014-07-11 Shionogi & Co., Ltd. Derivados de aminodihidrotriazina
TW200804290A (en) 2005-11-15 2008-01-16 Astrazeneca Ab Compounds and uses thereof
WO2007114771A1 (en) 2006-04-05 2007-10-11 Astrazeneca Ab 2-AMINOPYRIMIDIN-4-ONES AND THEIR USE FOR TREATING OR PREVENTING Aβ-RELATED PATHOLOGIES
US20080051420A1 (en) 2006-06-14 2008-02-28 Astrazeneca Ab New Compounds 317
ES2476605T3 (es) 2007-04-24 2014-07-15 Shionogi & Co., Ltd. Derivados de aminohidrotiazina sustituidos con grupos cíclicos
TW200902499A (en) 2007-05-15 2009-01-16 Astrazeneca Ab New compounds
CN101910155A (zh) 2007-10-30 2010-12-08 艾尼纳制药公司 作为组胺-h3受体调节剂用于治疗与组胺-h3受体调节剂相关的障碍的联苯衍生物
CA2713998A1 (en) 2008-01-28 2009-08-06 Janssen Pharmaceutica N.V. 6-substituted-thio-2-amino-quinoline derivatives useful as inhibitors of.beta.-secretase (bace)
WO2009102468A1 (en) 2008-02-13 2009-08-20 Cgi Pharmaceuticals, Inc. 6-aryl-imidaz0[l, 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
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
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
US8999980B2 (en) 2009-12-11 2015-04-07 Shionogi & Co., Ltd. Oxazine derivatives
EP2518059A4 (en) 2009-12-24 2013-05-29 Shionogi & Co 4-AMINO-1,3-THIAZINE OR OXAZINE DERIVATIVE
US20120277244A1 (en) 2009-12-31 2012-11-01 Novartis Ag Pyrazine derivatives and their use in the treatment of neurological disorders
JP2013531644A (ja) 2010-06-09 2013-08-08 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 βセクレターゼ（ＢＡＣＥ）の阻害剤として有用な５−アミノ−３，６−ジヒドロ−１Ｈ−ピラジン−２−オン誘導体
WO2011154431A1 (en) 2010-06-09 2011-12-15 Janssen Pharmaceutica Nv 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace)
EP2585440A1 (en) 2010-06-28 2013-05-01 Janssen Pharmaceutica, N.V. 3-amino-5,6-dihydro-1h-pyrazin-2-one derivatives useful for the treatement of alzheimer's disease and other forms of dementia
SG188338A1 (en) 2010-09-22 2013-04-30 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
AU2011347377B2 (en) 2010-12-22 2016-03-03 Janssen Pharmaceutica Nv 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives useful as inhibitors of beta-secretase (BACE)
CN103429589A (zh) 2011-01-12 2013-12-04 诺瓦提斯公司 噁嗪衍生物及其在治疗神经障碍中的用途
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
SI2681219T1 (sl) * 2011-03-01 2016-02-29 Janssen Pharmaceutica, N.V. Derivati 6,7-dihidro-pirazolo(1,5-a)pirazin-4-ilamina uporabni kot inhibitorji beta-sekretaze (BACE)
ES2534973T3 (es) * 2011-03-09 2015-04-30 Janssen Pharmaceutica N.V. Derivados de 3,4-dihidro-pirrolo[1,2-a]pirazin-1-ilamina útiles como inhibidores de beta-secretasa (BACE)
TW201247635A (en) 2011-04-26 2012-12-01 Shionogi & Co Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them
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
WO2013083556A1 (en) 2011-12-06 2013-06-13 Janssen Pharmaceutica Nv 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives
WO2014099794A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. C5, c6 oxacyclic-fused iminothiazine dioxide compounds as bace inhibitors
CN105452251B (zh) 2013-06-12 2017-12-26 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‑3(2H)‑酮衍生物
EP3008066B1 (en) 2013-06-12 2018-08-15 Janssen Pharmaceutica N.V. 4-amino-6-phenyl-5,6-dihydroimidazo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace)
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
EP3233834B1 (en) 2014-12-18 2019-11-13 Janssen Pharmaceutica NV 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2h-pyrrol-5-amine derivatives useful as inhibitors of beta-secretase

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MX368326B (es) 2019-09-27
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