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)
Spanish (es)
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

    • 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
    • A61K31/40—Heterocyclic 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
    • A61K31/403—Heterocyclic 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
    • A61K31/4035—Isoindoles, e.g. phthalimide
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4433—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/10—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/10—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic 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
    • C07D513/02—Heterocyclic 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
    • C07D513/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (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)
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 (enExample)
EP (1) EP2035378A4 (enExample)
JP (1) JP2009541311A (enExample)
KR (1) KR20090031585A (enExample)
AR (1) AR061564A1 (enExample)
AU (1) AU2007261749B2 (enExample)
CA (1) CA2656625A1 (enExample)
CL (1) CL2007001830A1 (enExample)
EC (1) ECSP088972A (enExample)
IL (1) IL195670A0 (enExample)
MX (1) MX2008015719A (enExample)
MY (1) MY147390A (enExample)
NO (1) NO20090246L (enExample)
NZ (1) NZ574262A (enExample)
TW (1) TW200815349A (enExample)
UY (1) UY30426A1 (enExample)
WO (1) WO2007149033A1 (enExample)

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
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
CA2575340A1 (en) 2004-07-28 2006-02-09 Schering Corporation Macrocyclic beta-secretase inhibitors
WO2006138264A2 (en) 2005-06-14 2006-12-28 Schering Corporation Aspartyl protease inhibitors
US8722708B2 (en) 2005-06-14 2014-05-13 Merck Sharp & Dohme Inc. Substituted isoindolines as aspartyl protease inhibitors
CA2653650A1 (en) 2006-06-12 2007-12-21 Schering Corporation Heterocyclic 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
MX2011002705A (es) 2008-09-11 2011-09-09 Amgen Inc Compuestos con anillos espiro-triciclicos como moduladores de beta-secretasas y metodos de uso.
MX2011004680A (es) * 2008-11-06 2011-05-25 Astrazeneca Ab Moduladores de beta amiloide.
WO2010056195A1 (en) * 2008-11-14 2010-05-20 Astrazeneca Ab New compounds 575
TW201020244A (en) * 2008-11-14 2010-06-01 Astrazeneca Ab New compounds
WO2010056194A1 (en) * 2008-11-14 2010-05-20 Astrazeneca Ab 5h-pyrrolo [ 3, 4-b] pyridin derivatives and their use
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
WO2011044184A1 (en) 2009-10-08 2011-04-14 Schering Corporation Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
WO2011044185A2 (en) 2009-10-08 2011-04-14 Schering Corporation 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
WO2011044187A1 (en) 2009-10-08 2011-04-14 Schering Corporation Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
MX2012010658A (es) 2010-03-15 2012-12-05 Amgen Inc Compuestos de anillo espiro tetraciclico como moduladores de beta-secretasa.
US8497264B2 (en) 2010-03-15 2013-07-30 Amgen Inc. Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
US20110281894A1 (en) * 2010-05-12 2011-11-17 Astrazeneca Ab Hemifumarate salt
WO2012019056A1 (en) 2010-08-05 2012-02-09 Amgen Inc. Amino-iso-indole, amino-aza-iso-indole, amino-dihydroisoquinoline and amino-benzoxazine compounds as beta-secretase modulators and methods of use
US9284296B2 (en) 2010-11-22 2016-03-15 Aubergine Pharmaceuticals Llc 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
WO2012138734A1 (en) 2011-04-07 2012-10-11 Merck Sharp & Dohme Corp. C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
RU2014111055A (ru) 2011-08-22 2015-09-27 Мерк Шарп И Доум Корп. 2-спирозамещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов bace, композиции и их применение
WO2013044092A1 (en) 2011-09-21 2013-03-28 Amgen Inc. Amino-oxazines and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
ES2745539T3 (es) 2012-03-19 2020-03-02 Buck Inst Res Aging Inhibidores de BACE específicos de APP (ASBI) y uso de los mismos
WO2014062553A1 (en) 2012-10-17 2014-04-24 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2908825B1 (en) 2012-10-17 2018-04-18 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
US9725469B2 (en) 2012-11-15 2017-08-08 Amgen, Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
EP3653609B1 (en) 2013-02-12 2024-04-03 Buck Institute for Research on Aging Hydantoins that modulate bace-mediated app processing
US20240383891A1 (en) * 2023-05-16 2024-11-21 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
AU702293B2 (en) 1993-10-27 1999-02-18 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
ES2135062T3 (es) 1994-06-16 1999-10-16 Pfizer Pirazolo y pirrolopiridinas.
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
WO1999011643A1 (en) 1997-09-02 1999-03-11 Du Pont Pharmaceuticals Company Heterocyclyl-substituted ring-fused pyridines and pyrimidines as corticotropin releasing hormone (crh) antagonists, useful for treating cns and stress-related disorders
US5981168A (en) 1998-05-15 1999-11-09 The University Of British Columbia Method and composition for modulating amyloidosis
ES2318902T3 (es) 1998-09-24 2009-05-01 PHARMACIA & UPJOHN COMPANY LLC Secretasa en la enfermedad del alzheimer.
US6245884B1 (en) 1998-10-16 2001-06-12 Vivian Y. H. Hook Secretases related to alzheimer's dementia
US6313268B1 (en) * 1998-10-16 2001-11-06 Vivian Y. H. Hook Secretases related to Alzheimer's dementia
WO2000047618A2 (en) 1999-02-10 2000-08-17 Elan Pharmaceuticals, Inc. HUMAN β-SECRETASE ENZYME, INHIBITORS AND THEIR COMPOSITIONS AND USES
WO2000058479A1 (en) 1999-03-26 2000-10-05 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
JP2003502342A (ja) 1999-06-15 2003-01-21 エラン ファーマスーティカルズ インコーポレイテッド ベータ−セクレターゼのスタチン誘導テトラペプチド阻害剤
EP1194449B1 (en) 1999-06-28 2010-09-22 Oklahoma Medical Research Foundation Inhibitors of memapsin 2 and use thereof
DK1224297T3 (da) 1999-09-23 2009-09-07 Pharmacia & Upjohn Co Llc Alzheimers sygdom -sekretase, APP-substrater derfor og anvendelser deraf
GB9924957D0 (en) 1999-10-21 1999-12-22 Smithkline Beecham Plc Novel treatment
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
US6846813B2 (en) 2000-06-30 2005-01-25 Pharmacia & Upjohn Company Compounds to treat alzheimer's disease
CA2410680A1 (en) 2000-06-30 2002-01-10 Elan Pharmaceuticals, Inc. Compounds to treat alzheimer's disease
US6696488B2 (en) 2000-08-11 2004-02-24 The Brigham And Women's Hospital, Inc. (Hydroxyethyl)ureas as inhibitors of alzheimer's β-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
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
CA2548388A1 (en) 2003-12-15 2005-06-30 Schering Corporation Heterocyclic aspartyl protease inhibitors
JP2007530696A (ja) 2004-03-30 2007-11-01 メルク　エンド　カムパニー　インコーポレーテッド アスパラギン酸プロテアーゼ阻害剤として有用な２−アミノチアゾール化合物
AU2005244770A1 (en) * 2004-04-26 2005-12-01 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
CA2579724A1 (en) 2004-06-16 2006-01-26 Wyeth Amino-5,5-diphenylimidazolone derivatives for the inhibition of beta-secretase
CA2578600A1 (en) 2004-06-16 2006-01-26 Wyeth Diphenylimidazopyrimidine and -imidazole amines as inhibitors of b-secretase
JPWO2006006520A1 (ja) 2004-07-09 2008-04-24 株式会社ジェノファンクション 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
BRPI0515532A (pt) 2004-09-21 2008-07-29 Athersys Inc composto, composição farmacêutica, métodos de inibir a ligação de ligandos endógenos ao receptor de crth-2 em uma célula, de tratar, melhorar ou prevenir um distúrbio responsivo à inibição da ligação de ligandos endógenos ao receptor de crt-2 e de preparar um composto, e, kit
CN101084198A (zh) 2004-10-15 2007-12-05 阿斯利康(瑞典)有限公司 取代的氨基－嘧啶酮及其用途
US20090221579A1 (en) 2004-10-15 2009-09-03 Jeffrey Scott Albert Substituted Amino-Compounds and Uses Thereof
EP1831170A4 (en) 2004-12-14 2009-10-14 Astrazeneca Ab SUBSTITUTED AMINOPYRIDINES AND THEIR USE
CN101103034A (zh) 2005-01-14 2008-01-09 惠氏公司 抑制β-分泌酶的氨基-咪唑酮
US20060223849A1 (en) 2005-03-14 2006-10-05 Mjalli Adnan M Benzazole derivatives, compositions, and methods of use as beta-secretase inhibitors
EP1896406A2 (en) 2005-06-14 2008-03-12 Shering Corporation The preparation and use of compounds as protease inhibitors
WO2006138264A2 (en) 2005-06-14 2006-12-28 Schering Corporation Aspartyl protease inhibitors
CA2609562A1 (en) 2005-06-14 2006-12-28 Schering Corporation Macrocyclic heterocyclic aspartyl protease inhibitors
US8722708B2 (en) 2005-06-14 2014-05-13 Merck Sharp & Dohme Inc. Substituted isoindolines as aspartyl protease inhibitors
US7759353B2 (en) 2005-06-14 2010-07-20 Schering Corporation Substituted spiro iminopyrimidinones as aspartyl protease inhibitors, compositions, and methods of treatment
ATE489370T1 (de) 2005-06-14 2010-12-15 Schering Corp Herstellung und verwendung von verbindungen als aspartylproteasehemmer
TW200738683A (en) 2005-06-30 2007-10-16 Wyeth Corp Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation
BRPI0613578A2 (pt) 2005-06-30 2012-01-17 Wyeth Corp composito da fórmula i; uso de um composto de fórmula i; e composição farmacêutica
CA2615656A1 (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
ES2537898T3 (es) * 2005-10-25 2015-06-15 Shionogi & Co., Ltd. Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1
CN101296926A (zh) 2005-10-27 2008-10-29 先灵公司 天冬氨酰蛋白酶抑制剂
CN101351460A (zh) 2005-10-31 2009-01-21 先灵公司 天冬氨酰蛋白酶抑制剂
WO2007058580A1 (en) 2005-11-15 2007-05-24 Astrazeneca Ab Novel 2-aminopyrimidinone derivatives and their use
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
JP2009515950A (ja) 2005-11-15 2009-04-16 アストラゼネカ・アクチエボラーグ 新規な２−アミノピリミジン誘導体およびその使用
TW200804290A (en) 2005-11-15 2008-01-16 Astrazeneca Ab Compounds and uses thereof
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
TW200734311A (en) 2005-11-21 2007-09-16 Astrazeneca Ab New compounds
AR058381A1 (es) 2005-12-19 2008-01-30 Astrazeneca Ab Compuestos derivados de 2-aminopiridin-4-onas y una composicion farmaceutica
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
CA2653650A1 (en) 2006-06-12 2007-12-21 Schering Corporation Heterocyclic aspartyl protease inhibitors
TW200815443A (en) 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds I
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
TW200815449A (en) 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds II
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
WO2008076043A1 (en) 2006-12-20 2008-06-26 Astrazeneca Ab Novel 2-amino-5,5-diaryl-imidazol-4-ones
TW200831484A (en) 2006-12-20 2008-08-01 Astrazeneca Ab New compounds
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
WO2010056194A1 (en) 2008-11-14 2010-05-20 Astrazeneca Ab 5h-pyrrolo [ 3, 4-b] pyridin derivatives and their use
WO2010056195A1 (en) 2008-11-14 2010-05-20 Astrazeneca Ab New compounds 575
TW201020244A (en) 2008-11-14 2010-06-01 Astrazeneca Ab New compounds

Also Published As

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

Similar Documents

Publication Publication Date Title
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
MY147390A (en) Substituted isoindoles as bace inhibitors and their use
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
MX2008013196A (es) 5-amido-2-carboxiamida-indoles.
DOP2011000076A (es) Derivados de heteroaril amidas y su uso como activadores de glucoquinasa
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
DE602007011434D1 (de) 1h-indol-5-ylpiperazin-1-ylmethanonderivate
DE602006010738D1 (de) Pyrroloä2,3-cüpyridinderivate