EA201100461A1 - Спиро-трициклические соединения как модуляторы бета-секретазы и способы их использования - Google Patents

Спиро-трициклические соединения как модуляторы бета-секретазы и способы их использования

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Publication number
EA201100461A1
EA201100461A1 EA201100461A EA201100461A EA201100461A1 EA 201100461 A1 EA201100461 A1 EA 201100461A1 EA 201100461 A EA201100461 A EA 201100461A EA 201100461 A EA201100461 A EA 201100461A EA 201100461 A1 EA201100461 A1 EA 201100461A1
Authority
EA
Eurasian Patent Office
Prior art keywords
beta
compounds
secretase
diseases
present
Prior art date
Application number
EA201100461A
Other languages
English (en)
Inventor
Альберт Амегадзи
Мэриан С. Брайан
Цзянь Дж. Чэнь
Алан С. Чэн
Томас Динин
Олег Эпстейн
Виджей Кешав Гор
Цзыхао Хуа
Джейсон Б. Хьюмэн
Хунбин Хуан
Чарльз Креймэн
Дэниэл Ла
Цинъянь Лю
Ву Ван Ма
Исаак Маркс
Винод Ф. Пэтел
Вэньюань Цянь
Мэтью Вайсс
Райан Уайт
Честер С. Юань
Original Assignee
Амген Инк.
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 Амген Инк. filed Critical Амген Инк.
Publication of EA201100461A1 publication Critical patent/EA201100461A1/ru

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10Spiro-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/424Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/10Spiro-condensed systems

Abstract

Предметом настоящего изобретения является новый класс соединений, которые могут использоваться для модуляции ферментной активности бета-секретазы и для лечения заболеваний, в развитии которых принимает участие бета-секретаза, включая болезнь Альцгеймера и связанные с ней состояния. В одном из вариантов осуществления этого изобретения соединения имеют общую формулу Iв которой А, А, А, А, А, А, Т, Т, W, X, Y и Z определяются в этом описании изобретения. Предметом настоящего изобретения является также использование таких соединений в фармацевтических препаратах для лечения и профилактики заболеваний и состояний, связанных с активностью белка бета-секретазы. К таким заболеваниям относится, например, болезнь Альцгеймера, недостаточность когнитивной функции, когнитивные нарушения, шизофрения и другие заболевания центральной нервной системы, связанные и/или вызываемые образованием и/или отложением бляшек в головном мозге. Предметом настоящего изобретения являются также другие варианты воплощения соединений формулы I, промежуточных соединений и процессов, которые могут применяться для получения соединений формулы I.
EA201100461A 2008-09-11 2009-09-11 Спиро-трициклические соединения как модуляторы бета-секретазы и способы их использования EA201100461A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US9608208P 2008-09-11 2008-09-11
PCT/US2009/056748 WO2010030954A1 (en) 2008-09-11 2009-09-11 Spiro-tetracyclic ring compounds as betasecretase modulators and methods of use

Publications (1)

Publication Number Publication Date
EA201100461A1 true EA201100461A1 (ru) 2011-10-31

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Application Number Title Priority Date Filing Date
EA201100461A EA201100461A1 (ru) 2008-09-11 2009-09-11 Спиро-трициклические соединения как модуляторы бета-секретазы и способы их использования

Country Status (21)

Country Link
US (1) US8426447B2 (ru)
EP (1) EP2328903B1 (ru)
JP (1) JP5579720B2 (ru)
KR (1) KR20110073511A (ru)
CN (1) CN102209721A (ru)
AU (1) AU2009291602B2 (ru)
BR (1) BRPI0918449A2 (ru)
CA (1) CA2736130C (ru)
CL (1) CL2011000516A1 (ru)
CO (1) CO6362014A2 (ru)
CR (1) CR20110134A (ru)
EA (1) EA201100461A1 (ru)
ES (1) ES2459195T3 (ru)
IL (1) IL211440A0 (ru)
MA (1) MA32705B1 (ru)
MX (1) MX2011002705A (ru)
MY (1) MY148558A (ru)
PE (1) PE20110805A1 (ru)
TW (1) TWI385175B (ru)
WO (1) WO2010030954A1 (ru)
ZA (1) ZA201102674B (ru)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
AR075854A1 (es) 2009-03-13 2011-05-04 Vitae Pharmaceuticals Inc Inhibidores de beta- secretasa
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
CN102812005B (zh) 2010-02-24 2014-12-10 生命医药公司 β-分泌酶抑制剂
JP5584352B2 (ja) * 2010-03-15 2014-09-03 アムジエン・インコーポレーテツド β−セクレターゼ調節剤としてのアミノ−ジヒドロオキサジン系およびアミノ−ジヒドロチアジン系スピロ化合物ならびにそれらの医学的用途
US8883782B2 (en) * 2010-03-15 2014-11-11 Amgen Inc. Spiro-tetracyclic ring compounds as beta-secretase modulators and methods of use
WO2011130741A1 (en) * 2010-04-16 2011-10-20 Array Biopharma Inc. Compounds for treating neurodegenerative diseases
US8921363B2 (en) * 2010-08-05 2014-12-30 Amgen Inc. Derivatives of 1 H-isoindol-3-amine, 1 H-iso-aza-indol-3amine, 3,4-dihydroisoquinolin-1-amine, and 1,4-dihydroisoquinolin-3-amine as beta-secretase inhibitors
CA2808590A1 (en) 2010-08-23 2012-03-01 Amgen Inc. Sulfonylpiperazine derivatives that interact with glucokinase regulatory protein for the treatment of diabetes
TW201307357A (zh) * 2010-11-22 2013-02-16 Array Biopharma Inc 治療神經退化性疾病之化合物
KR20140032948A (ko) 2010-11-22 2014-03-17 이데미쓰 고산 가부시키가이샤 산소 함유 축합환 유도체 및 그것을 포함하여 이루어지는 유기 전계 발광 소자
EP2643325A1 (en) 2010-11-23 2013-10-02 Amgen Inc. Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use
US8415483B2 (en) 2010-12-22 2013-04-09 Astrazeneca Ab Compounds and their use as BACE inhibitors
EP2673279A1 (en) 2011-02-07 2013-12-18 Amgen Inc. 5-amino-oxazepine and 5-amino-thiazepane compounds as beta-secretase antagonists and methods of use
US8962859B2 (en) * 2011-02-15 2015-02-24 Amgen Inc. Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use
US9221839B2 (en) 2011-04-07 2015-12-29 Merck Sharp & Dohme Corp. C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
EP2694521B1 (en) 2011-04-07 2015-11-25 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
RU2599256C2 (ru) 2011-06-07 2016-10-10 Ф. Хоффманн-Ля Рош Аг [1,3]оксазины
US9181236B2 (en) 2011-08-22 2015-11-10 Merck Sharp & Dohme Corp. 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use
WO2013044092A1 (en) * 2011-09-21 2013-03-28 Amgen Inc. Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
US9650336B2 (en) 2011-10-10 2017-05-16 Astrazeneca Ab Mono-fluoro beta-secretase inhibitors
TWI557112B (zh) 2012-03-05 2016-11-11 百靈佳殷格翰國際股份有限公司 β-分泌酶抑制劑
EP2650284A1 (en) * 2012-04-10 2013-10-16 Merz Pharma GmbH & Co. KGaA Heterocyclic derivatives as metabotropic glutamate receptor modulators
EA026380B1 (ru) * 2012-05-30 2017-04-28 Коментис, Инк. Соединения хроманов
US9000185B2 (en) 2012-06-20 2015-04-07 Astrazeneca Ab Cycloalkyl ether compounds and their use as BACE inhibitors
US9000182B2 (en) 2012-06-20 2015-04-07 Astrazeneca Ab 2H-imidazol-4-amine compounds and their use as BACE inhibitors
US9000183B2 (en) 2012-06-20 2015-04-07 Astrazeneca Ab Cyclohexane-1,2′-indene-1′,2″-imidazol compounds and their use as BACE inhibitors
US9000184B2 (en) 2012-06-20 2015-04-07 Astrazeneca Ab Cyclohexane-1,2′-naphthalene-1′,2″-imidazol compounds and their use as BACE inhibitors
US10548882B2 (en) 2012-06-21 2020-02-04 Astrazeneca Ab Camsylate salt
TW201422592A (zh) 2012-08-27 2014-06-16 Boehringer Ingelheim Int β-分泌酶抑制劑
EP2900650A1 (en) 2012-09-28 2015-08-05 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
US9725469B2 (en) 2012-11-15 2017-08-08 Amgen, Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
MX2020003488A (es) 2015-02-02 2022-05-24 Forma Therapeutics Inc Acidos 3-alquil-4-amido-biciclico [4,5,0] hidroxamicos como inhibidores de histona desacetilasas (hdac).
AR103598A1 (es) 2015-02-02 2017-05-24 Forma Therapeutics Inc Ácidos bicíclicos[4,6,0]hidroxámicos como inhibidores de hdac
EP3472131B1 (en) 2016-06-17 2020-02-19 Forma Therapeutics, Inc. 2-spiro-5- and 6-hydroxamic acid indanes as hdac inhibitors

Family Cites Families (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2683718A (en) * 1952-01-11 1954-07-13 Searle & Co Spiro-[xanthene-9, 4'-imidazolidine]-2, 5-dione
US3185696A (en) * 1959-03-12 1965-05-25 Jack M Tien 3', 6'-diaminofluoran derivatives of gamma-lactam
FR2576178B1 (fr) 1985-01-24 1987-04-17 Furodet Philippe Procede de fabrication pour un enfumoir a chargement par-dessous
DE3601492A1 (de) 1986-01-20 1987-07-23 Vacuumschmelze Gmbh Verfahren zur herstellung eines stabilisierten filament-supraleiters mit hohem anteil an stabilisierungsmaterial
US5441870A (en) 1992-04-15 1995-08-15 Athena Neurosciences, Inc. Methods for monitoring cellular processing of β-amyloid precursor protein
SI9300303A (en) 1993-06-08 1994-12-31 Krka Tovarna Zdravil Process for isolation of hypolipemic effective substance
JPH11507538A (ja) 1995-06-07 1999-07-06 アテナ ニューロサイエンシズ インコーポレイティド β−セクレターゼ、β−セクレターゼに対する抗体、及びβ−セクレターゼ阻害を検出するためのアッセイ
SG113454A1 (en) 1998-09-24 2005-08-29 Upjohn Co Alzheimer's disease secretase
MY138097A (en) 2000-03-22 2009-04-30 Du Pont Insecticidal anthranilamides
CN1217920C (zh) 2000-06-30 2005-09-07 艾兰制药公司 治疗早老性痴呆的化合物
US7196163B2 (en) 2001-05-22 2007-03-27 Merk & Co., Inc. Assays using amyloid precursor proteins with modified β-secretase cleavage sites to monitor β-secretase activity
MXPA04000140A (es) 2001-06-27 2004-06-03 Elan Pharm Inc Derivados de beta-hidroxiamina utiles en el tratamiento de enfermedad de alzheimer.
KR100713137B1 (ko) 2001-06-28 2007-05-02 동화약품공업주식회사 신규의 2,4-디플루오로벤즈아미드 유도체
WO2003006021A1 (en) 2001-07-10 2003-01-23 Elan Pharmaceuticals, Inc. Alpha-hydroxyamide statine derivatives for the treatment of alzh eimer's disease
WO2003006013A1 (en) 2001-07-10 2003-01-23 Elan Pharmaceuticals, Inc. Diaminediols for the treatment of alzheimer's disease
US20030109559A1 (en) 2001-07-11 2003-06-12 Andrea Gailunas N-(3-amino-2-hydroxy-propyl)substituted alkylamide compounds
WO2003029169A2 (en) 2001-10-04 2003-04-10 Elan Pharmaceuticals, Inc. Hydroxypropylamines
WO2003030886A2 (en) 2001-10-05 2003-04-17 Elan Pharmaceuticals, Inc Allylamides useful in the treatment of alzheimer's disease
MXPA04004079A (es) 2001-10-29 2005-07-05 Pharmacia & Upjohn Co Llc Amidas hidroxi sustituidas para tratamiento de enfermedad de alzheimer.
AP2004003049A0 (en) 2001-11-08 2004-06-30 Elan Pharm Inc N,N' -substituted-1,3-diamino -2-hydroxypropane derivatives.
TW200304374A (en) 2001-11-30 2003-10-01 Smithkline Beecham Plc Novel compounds
BR0214736A (pt) 2001-12-06 2004-11-23 Elan Pharm Inc Composto e seus sais farmaceuticamente aceitáveis, composição farmacêutica e método de tratar seres humanos ou animais que sofrem de doenças ou condições
JP2005534614A (ja) 2002-01-04 2005-11-17 イーラン ファーマスーティカルズ、インコーポレイテッド アルツハイマー病治療のための置換アミノカルボキサミド
TW200406390A (en) 2002-01-17 2004-05-01 Neurogen Corp Substituted quinazolin-4-ylamine analogues
US7115652B2 (en) 2002-06-17 2006-10-03 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
AU2003276047A1 (en) 2002-06-17 2003-12-31 Sunesis Pharmaceuticals, Inc. Aspartyl protease inhibitors
CA2489988A1 (en) 2002-06-20 2003-12-31 Michael R. Reeder Process for preparing 5-(1,3-oxazol-2-yl) benzoic acid derivatives
UY27967A1 (es) 2002-09-10 2004-05-31 Pfizer Acetil 2-hindroxi-1,3-diaminoalcanos
DE60329316D1 (de) 2002-11-12 2009-10-29 Merck & Co Inc Phenylcarboxamide als beta-sekretase-hemmer zur behandlung von alzheimer
GB0228410D0 (en) 2002-12-05 2003-01-08 Glaxo Group Ltd Novel Compounds
AU2004204692B2 (en) 2003-01-07 2009-07-09 Merck & Co., Inc. Macrocyclic beta-secretase inhibitors for treatment of Alzheimer's disease
GB0305918D0 (en) 2003-03-14 2003-04-23 Glaxo Group Ltd Novel compounds
WO2004080459A1 (en) 2003-03-14 2004-09-23 Merck Sharp & Dohme Limited Method for treating mild cognitive impairment and for preventing or delaying alzheimer’s disease
CL2004000849A1 (es) 2003-04-21 2005-01-28 Elan Pharmaceuticals Inc Pharm Compuestos derivados de benzamidas-2-hidroxi-3-diaminoalcanos, utiles para el tratamiento o la prevencion de alzheimer, sindrome de down, hemorragia cerebral hereditaria, demencias degenerativas y otras.
CL2004000848A1 (es) 2003-04-21 2005-01-28 Elan Pharmaceuticals Inc Pharm Compuestos derivados de fenacil-2-hidroxi-3-diaminoalcanos, inhibidores de la enzima betasecretasa, utiles para preparar un medicamento para tratar alzheimer, sindrome de down, hemorragia cerebral hereditaria con amiloidosis de tipo holandes, y otras
CN100430377C (zh) 2003-06-30 2008-11-05 麦克公司 用于治疗阿尔茨海默病的N-烷基苯基甲酰胺β分泌酶抑制剂
WO2005004803A2 (en) 2003-07-01 2005-01-20 Merck & Co., Inc. Phenylcarboxylate beta-secretase inhibitors for the treatment of alzheimer's disease
EP1699455B1 (en) 2003-12-15 2013-05-08 Merck Sharp & Dohme Corp. Heterocyclic aspartyl protease inhibitors
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7700603B2 (en) 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
GB0402143D0 (en) 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
EP1732906A4 (en) 2004-03-30 2007-11-21 Merck & Co Inc 2-AMINOTHIAZOLE COMPOUNDS USEFUL AS ASPARTYLE-PROTEASE INHIBITORS
EP1756087B1 (en) 2004-06-16 2009-10-07 Wyeth Amino-5,5-diphenylimidazolone derivatives for the inhibition of beta-secretase
WO2006041404A1 (en) 2004-10-15 2006-04-20 Astrazeneca Ab Substituted amino-compounds and uses thereof
WO2006076284A2 (en) 2005-01-14 2006-07-20 Wyeth AMINO-IMIDAZOLONES FOR THE INHIBITION OF ß-SECRETASE
US7759337B2 (en) 2005-03-03 2010-07-20 Amgen Inc. Phthalazine compounds and methods of use
AR054618A1 (es) 2005-06-14 2007-07-04 Schering Corp Compuestos de azetidina y su uso como inhibidores de proteasas
ES2436795T3 (es) 2005-06-14 2014-01-07 Merck Sharp & Dohme Corp. Inhibidores heterocíclicos de aspartil proteasa, preparación y uso de los mismos
JP2008543866A (ja) * 2005-06-16 2008-12-04 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 三環式オピオイドモジュレーター
TW200738683A (en) 2005-06-30 2007-10-16 Wyeth Corp Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation
US20070020316A1 (en) * 2005-07-13 2007-01-25 Raviv Laor Personal topical disinfectant device
WO2007011810A1 (en) 2005-07-18 2007-01-25 Merck & Co., Inc. Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease
TW200730523A (en) 2005-07-29 2007-08-16 Wyeth Corp Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation
JP2009509957A (ja) 2005-09-26 2009-03-12 ワイス β−セクレターゼ阻害剤としてのアミノ−5−[4−(ジフルオロメトキシ)フェニル]−5−フェニルイミダゾロン化合物
CN103936690B (zh) 2005-10-25 2016-06-08 盐野义制药株式会社 氨基二氢噻嗪衍生物
WO2007100536A1 (en) 2006-02-24 2007-09-07 Wyeth DIHYDROSPIRO[DIBENZO[A,D][7]ANNULENE-5,4'-IMIDAZOL] COMPOUNDS FOR THE INHIBITION OF β-SECRETASE
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
TW200808751A (en) 2006-04-13 2008-02-16 Astrazeneca Ab New compounds
AR061264A1 (es) 2006-06-12 2008-08-13 Schering Corp Inhibidores de aspartil-proteasas derivados de pirimidina, composiciones farmaceuticas que los contienen y usos para tratar enfermedades cognitivas o neurodegenerativas, y como inhibidores del virus vih.
TW200815447A (en) 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds IV
TW200815349A (en) 2006-06-22 2008-04-01 Astrazeneca Ab New compounds
EP2091328B1 (en) 2006-10-30 2011-12-28 Merck Sharp & Dohme Corp. Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease
TW200831091A (en) 2006-12-20 2008-08-01 Astrazeneca Ab New compounds
TW200831484A (en) 2006-12-20 2008-08-01 Astrazeneca Ab New compounds
CA2675221C (en) 2007-02-02 2016-02-23 F. Hoffmann-La Roche Ag Novel 2-aminooxazolines as taar1 ligands
CL2008000791A1 (es) 2007-03-23 2008-05-30 Wyeth Corp Compuestos derivados de 2-amino-5-(4-difluorometoxi-fenil)-5-fenil-imidazolidin-4-ona; composicion farmaceutica que comprende a dichos compuestos; y su uso en el tratamiento de una enfermedad asociada con la actividad bace excesiva, tales como enferm
MX2009011498A (es) 2007-04-24 2009-11-10 Shionogi & Co Derivados de aminodihidrotiazina sustituida con un grupo ciclico.
EP2151435A4 (en) 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
UY31083A1 (es) 2007-05-15 2009-01-05 Astrazeneca Ab Derivados de sulfoximinas para la inhibicion de b-secretasa
RU2476431C2 (ru) 2008-01-18 2013-02-27 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Конденсированное производное аминодигидротиазина
BRPI0907563A2 (pt) 2008-02-18 2015-08-04 Hoffmann La Roche Derivados de 4,5-di-hidro-xazol-2-il amina
JP2011518225A (ja) 2008-04-22 2011-06-23 シェーリング コーポレイション Bace−1阻害剤としてのフェニル置換2−イミノ−3−メチルピロロピリミジノン化合物、組成物、およびそれらの使用
TWI431004B (zh) 2008-05-02 2014-03-21 Lilly Co Eli Bace抑制劑
KR101307007B1 (ko) 2008-07-24 2013-09-11 에프. 호프만-라 로슈 아게 4,5-다이하이드로-옥사졸-2-일 유도체
AU2009277485B2 (en) * 2008-07-28 2013-05-02 Eisai R&D Management Co., Ltd. Spiroaminodihydrothiazine derivatives

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JP2012502112A (ja) 2012-01-26
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EP2328903A1 (en) 2011-06-08
WO2010030954A1 (en) 2010-03-18
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US8426447B2 (en) 2013-04-23
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