ECSP088972A - Isoindoles sustituidos como inhibidores de bace y su uso - Google Patents

Isoindoles sustituidos como inhibidores de bace y su uso

Info

Publication number
ECSP088972A
ECSP088972A EC2008008972A ECSP088972A ECSP088972A EC SP088972 A ECSP088972 A EC SP088972A EC 2008008972 A EC2008008972 A EC 2008008972A EC SP088972 A ECSP088972 A EC SP088972A EC SP088972 A ECSP088972 A EC SP088972A
Authority
EC
Ecuador
Prior art keywords
isoindols
replaced
bace inhibitors
new compounds
bace
Prior art date
Application number
EC2008008972A
Other languages
English (en)
Inventor
James Arnold
Laszlo Rakos
Didier Rotticci
Stefan Berg
Christopher William Murray
Gianni Chessari
Miles Stuart Congreve
Karin Kolmodin
Sahil Patel
Joerg Holens
Phil Edwards
Annika Kers
Mark Sylvester
Liselotte Oehberg
Original Assignee
Astrazeneca Ab
Astex Therapeutics Ltd
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38833680&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ECSP088972(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Astrazeneca Ab, Astex Therapeutics Ltd filed Critical Astrazeneca Ab
Publication of ECSP088972A publication Critical patent/ECSP088972A/es

Links

Classifications

    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/4035Isoindoles, e.g. phthalimide
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4433Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44Iso-indoles; Hydrogenated iso-indoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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
    • C07D513/04Ortho-condensed systems

Landscapes

  • 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)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Indole Compounds (AREA)

Abstract

Esta invención se refiere a nuevos compuestos que tienen la estructura de fórmula I y sus sales farmacéuticamente aceptables, composiciones y métodos de uso. Estos nuevos compuestos proporcionan un tratamiento o profilaxis de deterioros cognitivos, enfermedad de Alzheimer, neurodegeneración y demencia.
EC2008008972A 2006-06-22 2008-12-12 Isoindoles sustituidos como inhibidores de bace y su uso ECSP088972A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US81580006P 2006-06-22 2006-06-22
US81855706P 2006-07-05 2006-07-05
US89124207P 2007-02-23 2007-02-23

Publications (1)

Publication Number Publication Date
ECSP088972A true ECSP088972A (es) 2009-01-30

Family

ID=38833680

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2008008972A ECSP088972A (es) 2006-06-22 2008-12-12 Isoindoles sustituidos como inhibidores de bace y su uso

Country Status (17)

Country Link
US (2) US7855213B2 (es)
EP (1) EP2035378A4 (es)
JP (1) JP2009541311A (es)
KR (1) KR20090031585A (es)
AR (1) AR061564A1 (es)
AU (1) AU2007261749B2 (es)
CA (1) CA2656625A1 (es)
CL (1) CL2007001830A1 (es)
EC (1) ECSP088972A (es)
IL (1) IL195670A0 (es)
MX (1) MX2008015719A (es)
MY (1) MY147390A (es)
NO (1) NO20090246L (es)
NZ (1) NZ574262A (es)
TW (1) TW200815349A (es)
UY (1) UY30426A1 (es)
WO (1) WO2007149033A1 (es)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
ATE396990T1 (de) 2004-07-28 2008-06-15 Schering Corp Makrocyclische inhibitoren der beta-sekretase
SG162790A1 (en) 2005-06-14 2010-07-29 Schering Corp Aspartyl protease inhibitors
EP1896032B1 (en) 2005-06-14 2012-10-31 Merck Sharp & Dohme Corp. The preparation and use of compounds as protease inhibitors
US8168641B2 (en) 2006-06-12 2012-05-01 Schering Corporation Aspartyl protease inhibitors
TW200815349A (en) * 2006-06-22 2008-04-01 Astrazeneca Ab New compounds
TW200902499A (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
AU2009239536C1 (en) 2008-04-22 2012-12-13 Merck Sharp & Dohme Corp. Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use
US8426447B2 (en) 2008-09-11 2013-04-23 Amgen Inc. Spiro-tricyclic ring compounds as beta-secretase modulators and methods of use
MX2011004680A (es) * 2008-11-06 2011-05-25 Astrazeneca Ab Moduladores de beta amiloide.
TW201020244A (en) * 2008-11-14 2010-06-01 Astrazeneca Ab New compounds
US20100125081A1 (en) * 2008-11-14 2010-05-20 Astrazeneca Ab New compounds 574
WO2010056195A1 (en) * 2008-11-14 2010-05-20 Astrazeneca Ab New compounds 575
WO2011002409A1 (en) * 2009-07-02 2011-01-06 Astrazeneca Ab 5h-pyrrolo[3,4-£>]pyrazin-7-amine derivatives inhibitors of beta-secretase
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
US8557826B2 (en) 2009-10-08 2013-10-15 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions, and their use
EP2485920B1 (en) 2009-10-08 2016-04-27 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as bace-1 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
EP2485591B1 (en) 2009-10-08 2016-03-23 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
US8883782B2 (en) 2010-03-15 2014-11-11 Amgen Inc. Spiro-tetracyclic ring compounds as beta-secretase modulators and methods of use
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
US20110281894A1 (en) * 2010-05-12 2011-11-17 Astrazeneca Ab Hemifumarate salt
EP2601197B1 (en) 2010-08-05 2014-06-25 Amgen Inc. Amino-iso-indole, amino-aza-iso-indole, amino-dihydroisoquinoline and amino-benzoxazine compounds as beta-secretase modulators and methods of use
EP2643299B1 (en) 2010-11-22 2016-06-22 Noscira, S.A. Bipyridine sulfonamide derivatives for the treatment of neurodegenerative diseases or conditions
US9346827B2 (en) 2011-02-07 2016-05-24 Amgen Inc. 5-amino-oxazepine and 5-amino-thiazepane compounds as beta secretase antagonists and methods of use
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
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
JP2014526560A (ja) 2011-09-21 2014-10-06 アムジエン・インコーポレーテツド β‐セクレターゼ調節因子としてのアミノオキサジン化合物およびアミノジヒドロチアジン化合物および使用方法
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
WO2014062549A1 (en) 2012-10-17 2014-04-24 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
WO2014078314A1 (en) 2012-11-15 2014-05-22 Amgen Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
CA2899938C (en) 2013-02-12 2021-10-19 Buck Institute For Research On Aging Hydantoins that modulate bace-mediated app processing
EP4712965A2 (en) * 2023-05-16 2026-03-25 Springworks Therapeutics, Inc. Benzimidazole and related analogs for inhibiting yap/taz-tead

Family Cites Families (85)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4605642A (en) 1984-02-23 1986-08-12 The Salk Institute For Biological Studies CRF antagonists
US5063245A (en) 1990-03-28 1991-11-05 Nova Pharmaceutical Corporation Corticotropin-releasing factor antagonism compounds
WO1995011968A1 (en) 1993-10-27 1995-05-04 Athena Neurosciences, Inc. Transgenic animals harboring app allele having swedish mutation
US5877399A (en) 1994-01-27 1999-03-02 Johns Hopkins University Transgenic mice expressing APP-Swedish mutation develop progressive neurologic disease
DE4419849A1 (de) 1994-06-07 1995-12-14 Hoechst Ag Isoindolinpigmente
NZ284846A (en) 1994-06-16 1998-12-23 Pfizer 1-substituted-pyrazolo[3,4-b]pyridin-5-carboxylic acid derivatives, preparation, use, intermediates and pharmaceutical compositions thereof
DE19516804A1 (de) 1995-05-08 1996-11-14 Hoechst Ag Isoindolinpigmente auf Basis von Aminochinoxalindionen
US5744346A (en) * 1995-06-07 1998-04-28 Athena Neurosciences, Inc. β-secretase
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
US6211235B1 (en) 1996-11-22 2001-04-03 Elan Pharmaceuticals, Inc. Compounds for inhibiting β-amyloid peptide release and/or its synthesis
GB9701684D0 (en) 1997-01-28 1997-03-19 Smithkline Beecham Plc Novel compounds
ATE221886T1 (de) 1997-09-02 2002-08-15 Bristol Myers Squibb Pharma Co Heterocyclyl-substituierte annellierte pyridine und pyrimidine als antagonisten des corticotropin freisetzenden hormons (crh), verwendbar für die behandlung von cns und stress
US5981168A (en) 1998-05-15 1999-11-09 The University Of British Columbia Method and composition for modulating amyloidosis
NZ510708A (en) 1998-09-24 2003-12-19 Upjohn Co Alzheimer's disease and Asp1 and Asp2 cleaving APP site (beta secretase)
US6313268B1 (en) * 1998-10-16 2001-11-06 Vivian Y. H. Hook Secretases related to Alzheimer's dementia
US6245884B1 (en) 1998-10-16 2001-06-12 Vivian Y. H. Hook Secretases related to alzheimer's dementia
HK1044545A1 (zh) 1999-02-10 2002-10-25 Elan Pharmaceuticals, Inc. 贝他分泌酶组合物及其方法
AU3770800A (en) 1999-03-26 2000-10-16 Amgen, Inc. Beta secretase genes and polypeptides
US6376530B1 (en) * 1999-05-10 2002-04-23 Merck & Co., Inc. Cyclic amidines useful as NMDA NR2B antagonists
WO2000077030A1 (en) 1999-06-15 2000-12-21 Elan Pharmaceuticals, Inc. Statine-derived tetrapeptide inhibitors of beta-secretase
EP1194449B1 (en) 1999-06-28 2010-09-22 Oklahoma Medical Research Foundation Inhibitors of memapsin 2 and use thereof
AU782312B2 (en) 1999-09-23 2005-07-21 Pharmacia & Upjohn Company Alzheimer's disease secretase, APP substrates therefor, and uses therefor
GB9924957D0 (en) 1999-10-21 1999-12-22 Smithkline Beecham Plc Novel treatment
US6846813B2 (en) 2000-06-30 2005-01-25 Pharmacia & Upjohn Company Compounds to treat alzheimer's disease
PE20020276A1 (es) 2000-06-30 2002-04-06 Elan Pharm Inc COMPUESTOS DE AMINA SUSTITUIDA COMO INHIBIDORES DE ß-SECRETASA PARA EL TRATAMIENTO DE ALZHEIMER
DE60116313T2 (de) 2000-06-30 2006-08-31 Elan Pharmaceuticals, Inc., San Francisco Verbindungen zur behandlung der alzheimerischen krankheit
WO2002014264A2 (en) 2000-08-11 2002-02-21 The Brigham And Women's Hospital, Inc. (hydroxyethyl)ureas as inhibitors of alzheimer's beta-amyloid production
WO2002025276A1 (en) 2000-09-22 2002-03-28 Wyeth Crystal structure of bace and uses thereof
JP2004149429A (ja) * 2002-10-29 2004-05-27 Takeda Chem Ind Ltd インドール化合物およびその用途
SG163508A1 (en) 2003-12-15 2010-08-30 Schering Corp Heterocyclic aspartyl protease inhibitors
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
WO2005097767A1 (en) 2004-03-30 2005-10-20 Merck & Co., Inc. 2-aminothiazole compounds useful as aspartyl protease inhibitors
US7491744B2 (en) * 2004-04-26 2009-02-17 Vanderbilt University Indoleacetic acid and indenacetic acid derivatives as therapeutic agents with reduced gastrointestinal toxicity
WO2005123672A2 (en) 2004-06-14 2005-12-29 Takeda San Diego, Inc. Kinase inhibitors
ATE444962T1 (de) 2004-06-16 2009-10-15 Wyeth Corp Amino-5,5-diphenylimidazolon-derivate zur beta- sekretase-hemmung
JP2008503460A (ja) 2004-06-16 2008-02-07 ワイス β−セクレターゼのインヒビターとしてのジフェニルイミダゾピリミジンおよびイミダゾールアミン
WO2006006520A1 (ja) 2004-07-09 2006-01-19 Genofunction, Inc. 新規創薬標的の探索方法
JPWO2006006527A1 (ja) 2004-07-12 2008-04-24 大日本印刷株式会社 電磁波シールドフィルタ
PT1789398E (pt) * 2004-08-06 2010-10-21 Janssen Pharmaceutica Nv Derivados de 2-amino- quinazolina úteis como inibidores de β-secretase (bace)
TW200613272A (en) 2004-08-13 2006-05-01 Astrazeneca Ab Isoindolone compounds and their use as metabotropic glutamate receptor potentiators
EP1805171A4 (en) 2004-09-21 2009-05-13 Wyeth Corp CRTH2 RECEPTOR ANTAGONISM DISPLAYING INDIGENOUS ACIDS AND APPLICATIONS THEREOF
EP1802587A4 (en) 2004-10-15 2010-02-17 Astrazeneca Ab SUBSTITUTED AMINO BINDINGS AND THEIR APPLICATIONS
WO2006041405A1 (en) 2004-10-15 2006-04-20 Astrazeneca Ab Substituted amino-pyrimidones and uses thereof
EP1831170A4 (en) 2004-12-14 2009-10-14 Astrazeneca Ab SUBSTITUTED AMINOPYRIDINES AND THEIR USE
EP2264036A1 (en) 2005-01-14 2010-12-22 Wyeth LLC (Formerly Known As Wyeth) Amino-imidazolones for the inhibition of beta-secretase
CA2600570C (en) 2005-03-14 2011-12-06 Transtech Pharma, Inc. Benzazole derivatives, compositions, and methods of use as .beta.-secretase inhibitors
SG162790A1 (en) 2005-06-14 2010-07-29 Schering Corp Aspartyl protease inhibitors
CA2609562A1 (en) 2005-06-14 2006-12-28 Schering Corporation Macrocyclic heterocyclic aspartyl protease inhibitors
AU2006259574A1 (en) 2005-06-14 2006-12-28 Schering Corporation The preparation and use of compounds as aspartyl protease inhibitors
EP1896032B1 (en) 2005-06-14 2012-10-31 Merck Sharp & Dohme Corp. The preparation and use of compounds as protease inhibitors
EP1896406A2 (en) 2005-06-14 2008-03-12 Shering Corporation The preparation and use of compounds as protease inhibitors
US7759353B2 (en) 2005-06-14 2010-07-20 Schering Corporation Substituted spiro iminopyrimidinones as aspartyl protease inhibitors, compositions, and methods of treatment
TW200738683A (en) 2005-06-30 2007-10-16 Wyeth Corp Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation
JP2009500329A (ja) 2005-06-30 2009-01-08 ワイス アミノ−5−(6員)ヘテロアリールイミダゾロン化合物およびβ−セレクターゼ調節のためのその使用
WO2007011810A1 (en) 2005-07-18 2007-01-25 Merck & Co., Inc. Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease
US7601751B2 (en) 2005-09-01 2009-10-13 Bristol-Myers Squibb Company Indole acetic acid acyl guanidines as β-secretase inhibitors
CN101346357B (zh) * 2005-10-25 2014-04-02 盐野义制药株式会社 氨基二氢噻嗪衍生物
ATE478070T1 (de) 2005-10-27 2010-09-15 Schering Corp Heterozyklische aspartyl-proteasehemmer
EP1943246A1 (en) 2005-10-31 2008-07-16 Schering Corporation Aspartyl protease inhibitors
EP1951682A4 (en) 2005-11-15 2011-06-15 Astrazeneca Ab NEW 2-AMINOPYRIMIDONE OR 2-AMINOPYRIDINONE DERIVATIVES AND THEIR USE
CN101360720A (zh) 2005-11-15 2009-02-04 阿斯利康(瑞典)有限公司 新颖的2-氨基嘧啶酮衍生物及其用途
TW200804290A (en) 2005-11-15 2008-01-16 Astrazeneca Ab Compounds and uses thereof
CN101360722A (zh) 2005-11-15 2009-02-04 阿斯利康(瑞典)有限公司 新颖的2-氨基嘧啶衍生物及其用途
TW200734311A (en) 2005-11-21 2007-09-16 Astrazeneca Ab New compounds
CN101360716A (zh) 2005-11-21 2009-02-04 阿斯利康(瑞典)有限公司 新颖的2-氨基-咪唑-4-酮化合物及其在制备用于治疗认知缺损、阿尔茨海默病、神经变性和痴呆的药物中的用途
AR058381A1 (es) 2005-12-19 2008-01-30 Astrazeneca Ab Compuestos derivados de 2-aminopiridin-4-onas y una composicion farmaceutica
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
TW200808751A (en) 2006-04-13 2008-02-16 Astrazeneca Ab New compounds
US8168641B2 (en) 2006-06-12 2012-05-01 Schering Corporation Aspartyl protease inhibitors
TW200815449A (en) 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds II
TW200815447A (en) 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds IV
TW200808796A (en) 2006-06-14 2008-02-16 Astrazeneca Ab New compounds III
TW200815443A (en) 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds I
TW200815349A (en) 2006-06-22 2008-04-01 Astrazeneca Ab New compounds
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
TW200831091A (en) 2006-12-20 2008-08-01 Astrazeneca Ab New compounds
TW200831484A (en) 2006-12-20 2008-08-01 Astrazeneca Ab New compounds
WO2008076043A1 (en) 2006-12-20 2008-06-26 Astrazeneca Ab Novel 2-amino-5,5-diaryl-imidazol-4-ones
TW200902503A (en) 2007-05-15 2009-01-16 Astrazeneca Ab New compounds
TW200902499A (en) 2007-05-15 2009-01-16 Astrazeneca Ab New compounds
WO2009005470A1 (en) 2007-07-05 2009-01-08 Astrazeneca Ab Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors
WO2009005471A1 (en) 2007-07-05 2009-01-08 Astrazeneca Ab Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors
TW201020244A (en) * 2008-11-14 2010-06-01 Astrazeneca Ab New compounds
WO2010056195A1 (en) 2008-11-14 2010-05-20 Astrazeneca Ab New compounds 575
US20100125081A1 (en) * 2008-11-14 2010-05-20 Astrazeneca Ab New compounds 574

Also Published As

Publication number Publication date
TW200815349A (en) 2008-04-01
CA2656625A1 (en) 2007-12-27
US20110059992A1 (en) 2011-03-10
WO2007149033A1 (en) 2007-12-27
NO20090246L (no) 2009-03-20
KR20090031585A (ko) 2009-03-26
EP2035378A1 (en) 2009-03-18
US7855213B2 (en) 2010-12-21
US20080171771A1 (en) 2008-07-17
AU2007261749A1 (en) 2007-12-27
JP2009541311A (ja) 2009-11-26
UY30426A1 (es) 2008-01-31
EP2035378A4 (en) 2012-01-25
IL195670A0 (en) 2009-09-01
AR061564A1 (es) 2008-09-03
MX2008015719A (es) 2009-01-09
NZ574262A (en) 2011-11-25
AU2007261749B2 (en) 2011-11-03
MY147390A (en) 2012-11-30
CL2007001830A1 (es) 2008-04-04

Similar Documents

Publication Publication Date Title
ECSP088972A (es) Isoindoles sustituidos como inhibidores de bace y su uso
ECSP099755A (es) Derivados de pirrolopiridina y su uso como inhibidores de bace
UY29927A1 (es) Derivados sustituidos de la 5-fenil-2-tioxo-imidazolin-4-ona y de la 5-fenil-2-amino-imidazolidin-4-ona y sus sales, composiciones y aplicaciones
UY31083A1 (es) Derivados de sulfoximinas para la inhibicion de b-secretasa
ECSP088969A (es) Amino-imidazolones y su uso como medicamento para tratar deficiencias cognitivas, enfermedad de alzheimer, neurodegeneración y demencia
ECSP088970A (es) Amino-imidazolonas y su uso como medicamento para el tratamiento de la deficiencia cognitiva, la enfermedad de alzheimer, la neurodegeneración y la demencia
UY29919A1 (es) Derivados sustituidos de 3,4-dihidroisoquinolin-1-amino-trifluoroacetato, sus composiciones farmacéuticas y aplicaciones
MX388468B (es) Compuestos multicíclicos y métodos de uso de los mismos.
UY30025A1 (es) Derivados sustituidos de las 2-amino-5,6-dihidro pirimidin-4(3h)-onas y sus sales farmacéuticamente aceptables, composiciones farmacéuticas conteniéndolos y aplicaciones.
UY30274A1 (es) Derivados sustituidos de la n-(4-metil-1,3-tiazol-2-il)guanidina, formulaciones farmacéuticas conteniéndolo y aplicaciones
UY30407A1 (es) Derivados de [2,3,4,8-tetrahidroimidazo-[1,5-a]-pirimidin-8-il]-fenil sulfonatos sustituidos, composiciones farmacéuticas y aplicaciones.
UY32730A (es) Inhibidores de cyp17
WO2008076046A8 (en) Novel 2-amino-5, 5-diaryl-imidazol-4-ones
CL2012000033A1 (es) Compuestos n-(3-(4as,7as)-2-amino-4a,5,7,7a-tetrahidro-4h-furo[3,4-d][1,3] tiazin-7a-il)-4- fluorofenilo) -5-fluoropiconilamida, inhibidor de bace; composicion farmaceutica que los comprende, uso del compuesto para el tratamiento de la enfermedad de alzheimer.
NO20081554L (no) Isoindollmidforbindelser og sammensetninger omfattende samme, og anvendelse derav
PT1940839E (pt) Inibidores de piridopirimidinona pi3k alfa
EA200900213A1 (ru) Ингибиторы обратной транскриптазы вич (варианты), фармацевтическая композиция на их основе, способ ингибирования репликации ретровируса с их помощью и названные ингибиторы для изготовления лекарственного средства для ингибирования обратной транскриптазы вич и для лечения или профилактики инфекционного вич
EA200800760A1 (ru) ПИРИДОПИРИМИДИНОНОВЫЕ ИНГИБИТОРЫ PI3Kα
TW200800958A (en) N-substituted-azacyclylamines as histamine-3 antagonists
MX2008013196A (es) 5-amido-2-carboxiamida-indoles.
MX2009003645A (es) Azaciclilaminas n-sustituidas como antagonistas de histamina-3.
CR11157A (es) Derivados de 7-alquinil-1,8-naftiridonas, su preparacion y su aplicacion en terapeutica
ATE466854T1 (de) 1h-indol-6-ylpiperazin-1-ylmethanonderivate zur verwendung als h3-rezeptormodulatoren
CL2008001990A1 (es) Compuestos derivados de amino-quinazolinas sustituidas; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento de alzheimer.
DE602007011434D1 (de) 1h-indol-5-ylpiperazin-1-ylmethanonderivate