ECSP078003A - Inhibidores de aspartil proteasas - Google Patents

Inhibidores de aspartil proteasas

Info

Publication number
ECSP078003A
ECSP078003A EC2007008003A ECSP078003A ECSP078003A EC SP078003 A ECSP078003 A EC SP078003A EC 2007008003 A EC2007008003 A EC 2007008003A EC SP078003 A ECSP078003 A EC SP078003A EC SP078003 A ECSP078003 A EC SP078003A
Authority
EC
Ecuador
Prior art keywords
proteasas
aspartil
inhibitors
compounds
formula
Prior art date
Application number
EC2007008003A
Other languages
English (en)
Inventor
Zhaoning Zhu
Andrew Stamford
Brian Mckittrick
Johannes H Voigt
Corey Strickland
William Greenlee
Xiaoxiang Liu
Mihirbaran Mandal
Original Assignee
Schering Corp
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 Schering Corp filed Critical Schering Corp
Publication of ECSP078003A publication Critical patent/ECSP078003A/es

Links

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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Virology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Molecular Biology (AREA)
  • Hospice & Palliative Care (AREA)
  • AIDS & HIV (AREA)
  • Oncology (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Se revelan compuestos de fórmula I o su estereoisómero, tautómero o sal aceptable para uso farmacéutico, donde j, k, U, W, R, R1, R2, R3, R4, R6, R7 y R7a son según se describieron anteriormente en la memoria descriptiva.Además se revela el método para inhibir la aspartil proteasa, y en particular, los métodos para tratar enfermedades cardiovasculares, enfermedades cognitivas y neurodegenerativas. Además se revelan métodos para tratar enfermedades cognitivas y neurodegenerativas utilizando los compuestos de fórmula I en combinación con un inhibidor de colinesterasa o un agonista m1 o antagonista m2 muscarínico.
EC2007008003A 2005-06-14 2007-12-12 Inhibidores de aspartil proteasas ECSP078003A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US69053705P 2005-06-14 2005-06-14

Publications (1)

Publication Number Publication Date
ECSP078003A true ECSP078003A (es) 2008-01-23

Family

ID=37114557

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2007008003A ECSP078003A (es) 2005-06-14 2007-12-12 Inhibidores de aspartil proteasas

Country Status (18)

Country Link
US (1) US7868000B2 (es)
EP (1) EP1896478B1 (es)
JP (2) JP2008543849A (es)
KR (1) KR20080029965A (es)
CN (1) CN101228163A (es)
AR (1) AR054617A1 (es)
AU (1) AU2006259572A1 (es)
BR (1) BRPI0612072A2 (es)
CA (1) CA2609582A1 (es)
EC (1) ECSP078003A (es)
IL (1) IL187814A0 (es)
MX (1) MX2007016180A (es)
NO (1) NO20080187L (es)
PE (1) PE20070135A1 (es)
RU (1) RU2008100165A (es)
SG (1) SG162790A1 (es)
TW (2) TW201004961A (es)
WO (1) WO2006138264A2 (es)

Families Citing this family (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0220581D0 (en) 2002-09-04 2002-10-09 Novartis Ag Organic Compound
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7700603B2 (en) 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
AR049401A1 (es) * 2004-06-18 2006-07-26 Novartis Ag Aza-biciclononanos
GB0415746D0 (en) * 2004-07-14 2004-08-18 Novartis Ag Organic compounds
PE20070135A1 (es) 2005-06-14 2007-03-09 Schering Corp Compuestos heterociclicos como inhibidores de aspartil proteasas
WO2006138265A2 (en) 2005-06-14 2006-12-28 Schering Corporation Heterocyclic aspartyl protease inhibitors, preparation and use thereof
AU2006259675A1 (en) * 2005-06-14 2006-12-28 Schering Corporation Aspartyl protease inhibitors
GB0521508D0 (en) * 2005-10-21 2005-11-30 Novartis Ag Organic compounds
ATE478070T1 (de) 2005-10-27 2010-09-15 Schering Corp Heterozyklische aspartyl-proteasehemmer
GB0525673D0 (en) * 2005-12-16 2006-01-25 Novartis Ag Organic compounds
GB0525672D0 (en) * 2005-12-16 2006-01-25 Novartis Ag Organic compounds
PE20080155A1 (es) 2006-06-12 2008-03-10 Schering Corp Compuestos heterociclicos como inhibidores de aspartil-proteasa
TW200815349A (en) 2006-06-22 2008-04-01 Astrazeneca Ab New compounds
JP2010512389A (ja) 2006-12-12 2010-04-22 シェーリング コーポレイション アスパルチルプロテアーゼ阻害剤
US20100016341A1 (en) * 2006-12-12 2010-01-21 Zhaoning Zhu Aspartyl protease inhibitors containing a tricyclic ring system
TW200902499A (en) 2007-05-15 2009-01-16 Astrazeneca Ab New compounds
US8518975B2 (en) 2007-09-06 2013-08-27 Merck Sharp + Dohme Corp. Gamma secretase modulators
MX2010005028A (es) 2007-11-05 2010-05-27 Schering Corp Moduladores de gamma secretasa.
EP2227471A1 (en) * 2007-12-11 2010-09-15 Schering Corporation Gamma secretase modulators
CA2723222C (en) * 2008-04-22 2013-04-02 Schering Corporation Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as bace-1 inhibitors, compositions, and their use
MX2011005046A (es) 2008-11-13 2011-06-01 Schering Corp Moduladores de gamma secretasa.
TW201020244A (en) 2008-11-14 2010-06-01 Astrazeneca Ab New compounds
WO2010075204A2 (en) 2008-12-22 2010-07-01 Schering Corporation Gamma secretase modulators
EP2379563B1 (en) 2008-12-22 2014-07-16 Merck Sharp & Dohme Corp. Gamma secretase modulators
FR2944011B1 (fr) * 2009-04-03 2011-05-20 Pf Medicament Derives d'aminocyclobutane ou d'aminocyclobutene, leur procede de preparation et leur utilisation a titre de medicaments.
WO2010147973A1 (en) 2009-06-16 2010-12-23 Schering Corporation Gamma secretase modulators
WO2010147975A1 (en) 2009-06-16 2010-12-23 Schering Corporation Gamma secretase modulators
WO2010147969A2 (en) 2009-06-16 2010-12-23 Schering Corporation Gamma secretase modulators
GB0912777D0 (en) * 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydropyrimidone derivatives
GB0912778D0 (en) 2009-07-22 2009-08-26 Eisai London Res Lab Ltd Fused aminodihydro-oxazine derivatives
EP2281824A1 (en) 2009-08-07 2011-02-09 Noscira, S.A. Furan-imidazolone derivatives, for the treatment of cognitive, neurodegenerative or neuronal diseases or disorders
EP2485920B1 (en) 2009-10-08 2016-04-27 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
EP2485590B1 (en) 2009-10-08 2015-01-07 Merck Sharp & Dohme Corp. 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
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
JPWO2011071109A1 (ja) * 2009-12-11 2013-04-22 塩野義製薬株式会社 アミノ基を有する縮合ヘテロ環化合物
EP2643299B1 (en) 2010-11-22 2016-06-22 Noscira, S.A. Bipyridine sulfonamide derivatives for the treatment of neurodegenerative diseases or conditions
US8415483B2 (en) 2010-12-22 2013-04-09 Astrazeneca Ab Compounds and their use as BACE inhibitors
GB201100181D0 (en) 2011-01-06 2011-02-23 Eisai Ltd Fused aminodihydrothiazine derivatives
ES2624288T3 (es) 2011-01-21 2017-07-13 Eisai R&D Management Co., Ltd. Métodos y compuestos útiles en la síntesis de derivados de aminodihidrotiazina condensados
GB201101140D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
GB201101139D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
EP2694489B1 (en) 2011-04-07 2017-09-06 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
CN103874496A (zh) 2011-08-22 2014-06-18 默沙东公司 作为bace抑制剂的2-螺-取代的亚氨基噻嗪类及其单和二氧化物、组合物及其用途
US9650336B2 (en) 2011-10-10 2017-05-16 Astrazeneca Ab Mono-fluoro beta-secretase inhibitors
CN104270945B (zh) 2012-03-19 2017-03-29 巴克老龄化研究所 App特异性bace抑制剂(asbi)及其用途
JO3143B1 (ar) 2012-04-03 2017-09-20 Lilly Co Eli مركبات تتراهيدرو بيرولو ثيازين
US9371320B2 (en) 2012-06-01 2016-06-21 Takeda Pharmaceutical Company Limited Heterocyclic compound
US9000185B2 (en) 2012-06-20 2015-04-07 Astrazeneca Ab Cycloalkyl ether 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
US9000182B2 (en) 2012-06-20 2015-04-07 Astrazeneca Ab 2H-imidazol-4-amine 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
US9422277B2 (en) 2012-10-17 2016-08-23 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use
EP2908824B1 (en) 2012-10-17 2018-05-02 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
SI2912041T1 (sl) * 2012-10-26 2017-02-28 Eli Lilly And Company Derivati tetrahidropirolotiazina kot inhibitorji beta sekretaze (bace)
WO2014099788A1 (en) 2012-12-21 2014-06-26 Merck Sharp & Dohme Corp. C5-spiro iminothiadiazine dioxides as bace inhibitors
CA2899938C (en) 2013-02-12 2021-10-19 Buck Institute For Research On Aging Hydantoins that modulate bace-mediated app processing
TWI593692B (zh) 2013-03-12 2017-08-01 美國禮來大藥廠 四氫吡咯并噻嗪化合物
JO3318B1 (ar) 2013-06-18 2019-03-13 Lilly Co Eli مثبطات bace
WO2015095104A1 (en) 2013-12-18 2015-06-25 Merck Sharp & Dohme Corp. Iminothiadiazepane dioxide compounds as bace inhibitors, compositions, and their use
AR103680A1 (es) 2015-02-23 2017-05-24 Lilly Co Eli Inhibidores selectivos de bace1
CN104761557B (zh) * 2015-04-08 2017-02-22 河南师范大学 六氢‑1H‑吡咯并[3,4‑d]嘧啶类化合物及其制备方法
AR104241A1 (es) 2015-04-29 2017-07-05 Lilly Co Eli Derivados de tetrahidrofuro tiazina como inhibidores de bace1 selectivos
EP3414253B1 (en) * 2016-02-11 2021-07-21 Merck Sharp & Dohme Corp. C5-c6-oxacylic fused iminothiazine dioxide compounds bearing an ether linker as bace inhibitors, compositions, and their use
CN107892697B (zh) * 2016-12-26 2020-11-03 郑州泰基鸿诺医药股份有限公司 一种[1,3]噻嗪-2-胺类化合物及应用，药物组合物
PE20210447A1 (es) 2018-02-28 2021-03-08 Japan Tobacco Inc Compuestos de dihidropirimidinona o dihidrotriazinona fusionados con anillos saturados y su uso farmaceutico

Family Cites Families (100)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL92011A0 (en) 1988-10-19 1990-07-12 Abbott Lab Heterocyclic peptide renin inhibitors
AU2436792A (en) * 1991-08-16 1993-03-16 Merck & Co., Inc. Quinazoline derivatives as inhibitors of hiv reverse transcriptase
US5610294A (en) * 1991-10-11 1997-03-11 The Du Pont Merck Pharmaceutical Company Substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors
IT1270008B (it) * 1994-09-23 1997-04-16 Ist Superiore Sanita Derivati purinici ed 8-azapurinici atti al trattamento terapeutico dell'aids
US5889006A (en) 1995-02-23 1999-03-30 Schering Corporation Muscarinic antagonists
IL117149A0 (en) 1995-02-23 1996-06-18 Schering Corp Muscarinic antagonists
US5935958A (en) 1996-07-01 1999-08-10 Schering Corporation Muscarinic antagonists
US5952349A (en) 1996-07-10 1999-09-14 Schering Corporation Muscarinic antagonists for treating memory loss
US5977138A (en) 1996-08-15 1999-11-02 Schering Corporation Ether muscarinic antagonists
PT1086076E (pt) * 1998-06-19 2005-05-31 Vertex Pharma Inibidores de sulfonamida de aspartil protease
US6066636A (en) 1998-06-30 2000-05-23 Schering Corporation Muscarinic antagonists
US6492408B1 (en) 1999-07-21 2002-12-10 Boehringer Ingelheim Pharmaceuticals, Inc. Small molecules useful in the treatment of inflammatory disease
US6294554B1 (en) 1999-09-22 2001-09-25 Schering Corporation Muscarinic antagonists
WO2002012243A2 (en) 2000-08-09 2002-02-14 Boehringer Ingelheim Pharmaceuticals, Inc. SYNTHESIS OF (R)-3-(4-BROMOBENZYL)-1-(3,5-DICHLOROPHENYL)-5-IODO-3-METHYL-1-H-IMIDAZO[1,2-a]IMIDAZOL-2-ONE
ATE439344T1 (de) 2000-12-22 2009-08-15 Schering Corp Muscarin-antagonisten
WO2002074719A2 (en) 2001-03-15 2002-09-26 The Johns Hopkins University Inhibitors of plasmepsins
JP2005506339A (ja) 2001-10-10 2005-03-03 シェーリング　コーポレイション ムスカリン性アンタゴニストとしてのピペリジン化合物
AR045219A1 (es) 2003-08-08 2005-10-19 Pharmacopeia Inc Aminas ciclicas inhibidoras de base - 1 que poseen un sustiuyente heterociclico
WO2005016876A2 (en) 2003-08-08 2005-02-24 Schering Corporation Cyclic amine bace-1 inhibitors having a benzamide substituent
US20050171112A1 (en) 2003-11-03 2005-08-04 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
EP2335701B1 (en) * 2003-12-15 2012-07-11 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7700603B2 (en) 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7618978B2 (en) 2004-04-22 2009-11-17 Eli Lilly And Company Amides as BACE inhibitors
BRPI0512213A (pt) * 2004-06-16 2008-02-19 Wyeth Corp método para tratamento, prevenção ou melhora de uma doença ou distúrbio; composição farmacêutica; processo para a preparação de um composto; e uso de um composto
RU2006144075A (ru) 2004-06-16 2008-07-27 Вайет (Us) ДИФЕНИЛИМИДАЗОПИРИМИДИН И -ИМИДАЗОЛАМИНЫ КАК ИНГИБИТОРЫ β-СЕКРЕТАЗЫ
CA2574218A1 (en) 2004-07-22 2006-02-09 Schering Corporation Substituted amide beta secretase inhibitors
CA2575340A1 (en) 2004-07-28 2006-02-09 Schering Corporation Macrocyclic beta-secretase inhibitors
DE602005023887D1 (de) 2004-08-06 2010-11-11 Janssen Pharmaceutica Nv Als b-sekretase (bace)-hemmer nützliche 2-amino-chinazolinderivate
EP1776350B1 (en) 2004-08-06 2013-01-23 Janssen Pharmaceutica NV NOVEL 2-AMINO-QUINAZOLINE DERIVATIVES USEFUL AS INHIBITORS OF ß-SECRETASE ( BACE )
US8436006B2 (en) 2004-08-06 2013-05-07 Jansssen Pharmaceutica N.V. 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE)
WO2006044492A2 (en) 2004-10-14 2006-04-27 Ingenious Targeting Laboratory, Inc. Methods for generating rat embryo-derived cell lines and genetic modification of rat genome
JP2008516945A (ja) * 2004-10-15 2008-05-22 アストラゼネカ・アクチエボラーグ 置換されたアミノ化合物およびそれらの使用
EP1802588A4 (en) 2004-10-15 2010-02-17 Astrazeneca Ab SUBSTITUTED AMINOPYRIMIDONE AND APPLICATIONS THEREOF
CA2593515A1 (en) 2005-01-14 2006-07-20 Wyeth Amino-imidazolones for the inhibition of beta-secretase
KR20080025079A (ko) 2005-06-14 2008-03-19 쉐링 코포레이션 아스파르틸 프로테아제 억제제
PE20070135A1 (es) 2005-06-14 2007-03-09 Schering Corp Compuestos heterociclicos como inhibidores de aspartil proteasas
ATE489370T1 (de) 2005-06-14 2010-12-15 Schering Corp Herstellung und verwendung von verbindungen als aspartylproteasehemmer
EP1896406A2 (en) 2005-06-14 2008-03-12 Shering Corporation The preparation and use of compounds as protease inhibitors
AU2006259675A1 (en) 2005-06-14 2006-12-28 Schering Corporation Aspartyl protease inhibitors
WO2006138265A2 (en) 2005-06-14 2006-12-28 Schering Corporation Heterocyclic aspartyl protease inhibitors, preparation and use thereof
AR053902A1 (es) 2005-06-14 2007-05-23 Schering Corp Inhibidores de aspartil proteasa heterociclicos macrociclicos
TW200738683A (en) 2005-06-30 2007-10-16 Wyeth Corp Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation
AU2006266167A1 (en) * 2005-06-30 2007-01-11 Wyeth Amino-5-(6-membered)heteroarylimidazolone compounds and the use thereof for beta-secretase modulation
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
EP1966198B1 (en) 2005-10-25 2011-03-16 Janssen Pharmaceutica NV 2-amino-3,4-dihydro-pyrido[3,4-d]pyrimidine derivatives useful as inhibitors of beta-secretase (bace)
CA2628074C (en) 2005-10-25 2014-01-14 Shionogi & Co., Ltd. Aminodihydrothiazine derivative
ATE478070T1 (de) 2005-10-27 2010-09-15 Schering Corp Heterozyklische aspartyl-proteasehemmer
JP2009513670A (ja) * 2005-10-31 2009-04-02 シェーリング コーポレイション アスパルチルプロテアーゼインヒビター
EP1951680A4 (en) 2005-11-15 2011-08-10 Astrazeneca Ab NOVEL 2-AMINOPYRIMIDINONE DERIVATIVES AND THEIR USE
TW200804290A (en) 2005-11-15 2008-01-16 Astrazeneca Ab Compounds and uses thereof
CN101360721A (zh) 2005-11-15 2009-02-04 阿斯利康(瑞典)有限公司 新颖的2-氨基嘧啶酮衍生物或2-氨基吡啶酮衍生物及其用途
TW200734311A (en) 2005-11-21 2007-09-16 Astrazeneca Ab New compounds
WO2007058601A1 (en) 2005-11-21 2007-05-24 Astrazeneca Ab Novel 2-amino-imidazole-4-one compounds and their use in the manufacture of a medicament to be used in the treatment of cognitive impairment, alzheimer’s disease, neurodegeneration and dementia
AU2006333049A1 (en) 2005-12-19 2007-07-12 Wyeth 2-amino-5-piperidinylimidazolone compounds and use thereof for beta-secretase modulation
AR058381A1 (es) 2005-12-19 2008-01-30 Astrazeneca Ab Compuestos derivados de 2-aminopiridin-4-onas y una composicion farmaceutica
US7776882B2 (en) * 2006-02-06 2010-08-17 Baxter Ellen W 2-amino-3,4-dihydro-quinoline derivatives useful as inhibitors of β-secretase (BACE)
US7932261B2 (en) 2006-02-06 2011-04-26 Janssen Pharmaceutica Nv Macrocycle derivatives useful as inhibitors of β-secretase (BACE)
US7868022B2 (en) 2006-02-06 2011-01-11 Janssen Pharmaceutica Nv 2-amino-quinoline derivatives useful as inhibitors of β-secretase (BACE)
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
CN101460480A (zh) 2006-04-05 2009-06-17 阿斯利康(瑞典)有限公司 2-氨基嘧啶-4-酮类化合物及其用于治疗或预防Aβ相关病理的用途
PE20080155A1 (es) * 2006-06-12 2008-03-10 Schering Corp Compuestos heterociclicos como inhibidores de aspartil-proteasa
TW200815443A (en) 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds I
US20080051420A1 (en) * 2006-06-14 2008-02-28 Astrazeneca Ab New Compounds 317
TW200815449A (en) * 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds II
TW200808796A (en) 2006-06-14 2008-02-16 Astrazeneca Ab New compounds III
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
TW200817406A (en) 2006-08-17 2008-04-16 Wyeth Corp Imidazole amines as inhibitors of β-secretase
WO2008063114A1 (en) 2006-11-20 2008-05-29 Astrazeneca Ab Amino- imidazolones and their use as medicament for treating cognitive impairment alzheimer disease, neurodegeneration and dementia
JP2010512389A (ja) * 2006-12-12 2010-04-22 シェーリング コーポレイション アスパルチルプロテアーゼ阻害剤
US20100016341A1 (en) * 2006-12-12 2010-01-21 Zhaoning Zhu Aspartyl protease inhibitors containing a tricyclic ring system
TW200831091A (en) 2006-12-20 2008-08-01 Astrazeneca Ab New compounds
TW200831484A (en) * 2006-12-20 2008-08-01 Astrazeneca Ab New compounds
WO2008076044A1 (en) 2006-12-20 2008-06-26 Astrazeneca Ab Novel 2-amino-5, 5-diaryl-imidazol-4-ones
CL2008000784A1 (es) 2007-03-20 2008-05-30 Wyeth Corp Compuestos amino-5-[-4-(diflourometoxi) fenil sustituido]-5-fenilmidazolona, inhibidores de b-secretasa; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar alzheimer, deterioro cognitivo, sindrome de down, disminucion co
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
JP5383484B2 (ja) 2007-04-24 2014-01-08 塩野義製薬株式会社 環式基で置換されたアミノジヒドロチアジン誘導体
US8653067B2 (en) 2007-04-24 2014-02-18 Shionogi & Co., Ltd. Pharmaceutical composition for treating Alzheimer's disease
TW200902499A (en) 2007-05-15 2009-01-16 Astrazeneca Ab New compounds
TW200902503A (en) * 2007-05-15 2009-01-16 Astrazeneca Ab New compounds
WO2009005471A1 (en) 2007-07-05 2009-01-08 Astrazeneca Ab Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors
WO2009005470A1 (en) 2007-07-05 2009-01-08 Astrazeneca Ab Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors
US8222264B2 (en) 2007-07-06 2012-07-17 Boehringer Ingelheim International Gmbh Substituted amino-quinazolinones, medicaments comprising said compound, their use and their method of manufacture
PL2233474T3 (pl) 2008-01-18 2015-12-31 Eisai R&D Man Co Ltd Skondensowana pochodna aminodihydrotiazyny
WO2009092566A1 (en) 2008-01-22 2009-07-30 Boehringer Ingelheim International Gmbh Substituted amino-benzimidazoles, medicaments comprising said compound, their use and their method of manufacture
WO2009097278A1 (en) 2008-01-28 2009-08-06 Janssen Pharmaceutica N.V. 6-SUBSTITUTED-THIO-2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE)
EP2240472B1 (en) 2008-01-29 2012-11-21 Janssen Pharmaceutica NV 2-amino-quinoline derivatives useful as inhibitors of beta-secretase (bace)
EP2245019B1 (en) * 2008-02-18 2012-11-14 F. Hoffmann-La Roche AG 4, 5-dihydro-oxazol-2-yl amine derivatives
CA2723222C (en) 2008-04-22 2013-04-02 Schering Corporation Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as bace-1 inhibitors, compositions, and their use
TWI431004B (zh) 2008-05-02 2014-03-21 Lilly Co Eli Ｂａｃｅ抑制劑
KR101324426B1 (ko) 2008-06-13 2013-10-31 시오노기세야쿠 가부시키가이샤 β 세크레타제 저해 작용을 갖는 황 함유 복소환 유도체
CN102105475B (zh) 2008-07-28 2014-04-09 卫材R&D管理有限公司 螺氨基二氢噻嗪衍生物
WO2010013302A1 (ja) 2008-07-28 2010-02-04 エーザイ・アール・アンド・ディー・マネジメント株式会社 スピロアミノジヒドロチアジン誘導体
JP5666304B2 (ja) 2008-09-30 2015-02-12 エーザイ・アール・アンド・ディー・マネジメント株式会社 新規な縮合アミノジヒドロチアジン誘導体
CN102186841A (zh) 2008-10-22 2011-09-14 盐野义制药株式会社 具有bace1抑制活性的2-氨基嘧啶-4-酮及2-氨基吡啶衍生物
US20100125081A1 (en) 2008-11-14 2010-05-20 Astrazeneca Ab New compounds 574
US8394807B2 (en) 2008-11-20 2013-03-12 Purdue Research Foundation Quinazoline inhibitors of BACE 1 and methods of using

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