CN103415521B - 用作β分泌酶（BACE）抑制剂的3,4-二氢-吡咯并[1,2-a]吡嗪-1-基胺衍生物 - Google Patents

用作β分泌酶（BACE）抑制剂的3,4-二氢-吡咯并[1,2-a]吡嗪-1-基胺衍生物 Download PDF

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Publication number: CN103415521B
Authority: CN; China
Prior art keywords: group; mmol; mixture; vacuo; compound
Prior art date: 2011-03-09
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.): Expired - Fee Related

Application number

CN201280012485.5A

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English (en)

Chinese (zh)

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CN103415521A (zh

Inventor

A.A.特拉班科-苏亚亚雷滋

F.德加多-吉梅内滋

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.)

2011-03-09

Filing date

2012-03-07

Publication date

2016-01-06

2012-03-07 Application filed by Janssen Pharmaceutica NV filed Critical Janssen Pharmaceutica NV

2013-11-27 Publication of CN103415521A publication Critical patent/CN103415521A/zh

2016-01-06 Application granted granted Critical

2016-01-06 Publication of CN103415521B publication Critical patent/CN103415521B/zh

Status Expired - Fee Related legal-status Critical Current

2032-03-07 Anticipated expiration legal-status Critical

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0 CC(*=C)=*CC(*)(C[n]1c2c(*)c(*)c1*)*=C2[N-] Chemical compound CC(*=C)=*CC(*)(C[n]1c2c(*)c(*)c1*)*=C2[N-] 0.000 description 7
VVGWSGBWRBKKEU-UHFFFAOYSA-N CCC(CC(C=CCC=C1)=CC1Br)(C#N)N Chemical compound CCC(CC(C=CCC=C1)=CC1Br)(C#N)N VVGWSGBWRBKKEU-UHFFFAOYSA-N 0.000 description 1
VCSJGLABQPIRTG-MCQMVECXSA-N C[C@@H]1C=C(COC)N(CC2=CCC(CBr)C[C@H]2F)[C@@H]1C Chemical compound C[C@@H]1C=C(COC)N(CC2=CCC(CBr)C[C@H]2F)[C@@H]1C VCSJGLABQPIRTG-MCQMVECXSA-N 0.000 description 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- 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
- C07D487/04—Ortho-condensed systems
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
- 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
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
General Health & Medical Sciences (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
Medicinal Chemistry (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Biomedical Technology (AREA)
Neurology (AREA)
Neurosurgery (AREA)
Hospice & Palliative Care (AREA)
Psychiatry (AREA)
Epidemiology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Plural Heterocyclic Compounds (AREA)

CN201280012485.5A 2011-03-09 2012-03-07 用作β分泌酶（BACE）抑制剂的3,4-二氢-吡咯并[1,2-a]吡嗪-1-基胺衍生物 Expired - Fee Related CN103415521B (zh)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
EP11157418		2011-03-09
EP11157418.2		2011-03-09
PCT/EP2012/053863 WO2012120023A1 (en)	2011-03-09	2012-03-07	3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)

Publications (2)

Publication Number	Publication Date
CN103415521A CN103415521A (zh)	2013-11-27
CN103415521B true CN103415521B (zh)	2016-01-06

Family

ID=43833325

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
CN201280012485.5A Expired - Fee Related CN103415521B (zh)	2011-03-09	2012-03-07	用作β分泌酶（BACE）抑制剂的3,4-二氢-吡咯并[1,2-a]吡嗪-1-基胺衍生物

Country Status (20)

Country	Link
US (1)	US9845326B2 (2)
EP (1)	EP2683721B1 (2)
JP (1)	JP5853035B2 (2)
KR (1)	KR102012675B1 (2)
CN (1)	CN103415521B (2)
AU (1)	AU2012224632B2 (2)
BR (1)	BR112013022917A2 (2)
CA (1)	CA2825620C (2)
CL (1)	CL2013002511A1 (2)
CO (1)	CO6751283A2 (2)
EA (1)	EA023824B1 (2)
ES (1)	ES2534973T3 (2)
IL (1)	IL228239A (2)
MX (1)	MX340031B (2)
MY (1)	MY163346A (2)
PH (1)	PH12013501805A1 (2)
SG (1)	SG193342A1 (2)
UA (1)	UA109687C2 (2)
WO (1)	WO2012120023A1 (2)
ZA (1)	ZA201306719B (2)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
EP2612854B1 (en)	2005-10-25	2015-04-29	Shionogi&Co., Ltd.	Aminothiazolidine and aminotetrahydrothiazepine derivatives as BACE 1 inhibitors
TW200902526A (en)	2007-04-24	2009-01-16	Shionogi & Amp Co Ltd	Aminodihydrothiazin derivative substituted with a cyclic group
WO2008133273A1 (ja)	2007-04-24	2008-11-06	Shionogi & Co., Ltd.	アルツハイマー症治療用医薬組成物
WO2009151098A1 (ja)	2008-06-13	2009-12-17	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
JPWO2010047372A1 (ja)	2008-10-22	2012-03-22	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
UA110467C2 (uk)	2009-12-11	2016-01-12	Шионогі Енд Ко., Лтд.	Похідні оксазину
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)
EP2634188A4 (en)	2010-10-29	2014-05-07	Shionogi & Co	FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE
CN103261199A (zh)	2010-10-29	2013-08-21	盐野义制药株式会社	萘啶衍生物
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ＪａｎｓｓｅｎＰｈａｒｍａｃｅｕｔｉｃａＮａａｍｌｏｚｅＶｅｎｎｏｏｔｓｃｈａｐ	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
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ＪａｎｓｓｅｎＰｈａｒｍａｃｅｕｔｉｃａＮａａｍｌｏｚｅＶｅｎｎｏｏｔｓｃｈａｐ	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
EP2912035A4 (en)	2012-10-24	2016-06-15	Shionogi & Co	DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY
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)
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)
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)
RU2572076C2 (ru) *	2014-03-26	2015-12-27	Федеральное государственное бюджетное научное учреждение "Научно-исследовательский институт фармакологии имени В.В. Закусова"	1-арилпирроло[1,2-a]пиразин-3-карбоксамиды с нейропсихотропной активностью
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
WO2018165520A1 (en)	2017-03-10	2018-09-13	Vps-3, Inc.	Metalloenzyme inhibitor compounds
WO2021021979A2 (en)	2019-07-30	2021-02-04	Eikonizo Therapapeutics, Inc.	Hdac6 inhibitors and uses thereof
EP4504190A4 (en)	2022-04-08	2026-03-25	Eikonizo Therapeutics Inc	OXADIAZOLE HDAC6 INHIBITORS AND THEIR USES
CN117471007B (zh) *	2023-10-31	2024-08-09	广东省中医院（广州中医药大学第二附属医院、广州中医药大学第二临床医学院、广东省中医药科学院）	一种血浆β-淀粉样蛋白检测方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
WO2006076284A2 (en) *	2005-01-14	2006-07-20	Wyeth	AMINO-IMIDAZOLONES FOR THE INHIBITION OF ß-SECRETASE
WO2009022961A1 (en) *	2007-05-15	2009-02-19	Astrazeneca Ab	Pyrrolopyridine derivatives and their use as bace inhibitors
WO2011002409A1 (en) *	2009-07-02	2011-01-06	Astrazeneca Ab	5h-pyrrolo[3,4-£>]pyrazin-7-amine derivatives inhibitors of beta-secretase

Family Cites Families (52)

* 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 (2)	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
CN2781924Y (zh)	2005-01-21	2006-05-24	厦门革新塑胶制品有限公司	折叠床中部支脚
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
GB2443654A (en)	2006-05-30	2008-05-14	Matthew Emmerson Allen	System for detecting and testing drivers who show abnormal driving behaviour.
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
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
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
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)
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
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ＪａｎｓｓｅｎＰｈａｒｍａｃｅｕｔｉｃａＮａａｍｌｏｚｅＶｅｎｎｏｏｔｓｃｈａｐ	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
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ＪａｎｓｓｅｎＰｈａｒｍａｃｅｕｔｉｃａＮａａｍｌｏｚｅＶｅｎｎｏｏｔｓｃｈａｐ	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
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
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)
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)
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

2012
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Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
WO2006076284A2 (en) *	2005-01-14	2006-07-20	Wyeth	AMINO-IMIDAZOLONES FOR THE INHIBITION OF ß-SECRETASE
CN101103034A (zh) *	2005-01-14	2008-01-09	惠氏公司	抑制β-分泌酶的氨基-咪唑酮
WO2009022961A1 (en) *	2007-05-15	2009-02-19	Astrazeneca Ab	Pyrrolopyridine derivatives and their use as bace inhibitors
CN101796052A (zh) *	2007-05-15	2010-08-04	阿斯利康(瑞典)有限公司	吡咯并吡啶衍生物和它们作为bace抑制剂的用途
WO2011002409A1 (en) *	2009-07-02	2011-01-06	Astrazeneca Ab	5h-pyrrolo[3,4-£>]pyrazin-7-amine derivatives inhibitors of beta-secretase

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NZ615720A (en)	2014-08-29
MX2013010280A (es)	2013-10-01
PH12013501805A1 (en)	2013-11-18
CA2825620A1 (en)	2012-09-13
MY163346A (en)	2017-09-15
UA109687C2 (xx)	2015-09-25
SG193342A1 (en)	2013-10-30
JP2014507455A (ja)	2014-03-27
US20130345228A1 (en)	2013-12-26
AU2012224632A1 (en)	2013-08-01
EP2683721B1 (en)	2015-01-28
WO2012120023A1 (en)	2012-09-13
CN103415521A (zh)	2013-11-27
ZA201306719B (en)	2015-04-29
KR20140019332A (ko)	2014-02-14
EP2683721A1 (en)	2014-01-15
CL2013002511A1 (es)	2014-01-24
US9845326B2 (en)	2017-12-19
HK1189223A1 (zh)	2014-05-30
KR102012675B1 (ko)	2019-08-21
MX340031B (es)	2016-06-21
IL228239A (en)	2016-06-30
EA023824B1 (ru)	2016-07-29
CO6751283A2 (es)	2013-09-16
ES2534973T3 (es)	2015-04-30
EA201391296A1 (ru)	2014-01-30
AU2012224632B2 (en)	2016-06-16
CA2825620C (en)	2019-04-23
IL228239A0 (en)	2013-11-25
JP5853035B2 (ja)	2016-02-09
BR112013022917A2 (pt)	2016-12-06

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