ATE244018T1 - Herstellungb und verwendung eines spezifischen gaba-aalpha5 rezeptorligands zur behandlung der erkrankung von alzheimer - Google Patents

Herstellungb und verwendung eines spezifischen gaba-aalpha5 rezeptorligands zur behandlung der erkrankung von alzheimer

Info

Publication number
ATE244018T1
ATE244018T1 AT96903108T AT96903108T ATE244018T1 AT E244018 T1 ATE244018 T1 AT E244018T1 AT 96903108 T AT96903108 T AT 96903108T AT 96903108 T AT96903108 T AT 96903108T AT E244018 T1 ATE244018 T1 AT E244018T1
Authority
AT
Austria
Prior art keywords
treatment
alzheimer
disease
receptor ligand
aalpha5
Prior art date
Application number
AT96903108T
Other languages
English (en)
Inventor
Gerard Raphael Dawson
Original Assignee
Merck Sharp & Dohme
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 Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Application granted granted Critical
Publication of ATE244018T1 publication Critical patent/ATE244018T1/de

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Classifications

    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/94—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving narcotics or drugs or pharmaceuticals, neurotransmitters or associated receptors
    • G01N33/9406—Neurotransmitters
    • G01N33/9426—GABA, i.e. gamma-amino-butyrate
    • 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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/70571—Receptors; Cell surface antigens; Cell surface determinants for neuromediators, e.g. serotonin receptor, dopamine receptor
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/68—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
    • G01N33/6893—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids related to diseases not provided for elsewhere
    • G01N33/6896—Neurological disorders, e.g. Alzheimer's disease
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/46—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans from vertebrates
    • G01N2333/47—Assays involving proteins of known structure or function as defined in the subgroups
    • G01N2333/4701—Details
    • G01N2333/4709—Amyloid plaque core protein
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00—Detection or diagnosis of diseases
    • G01N2800/28—Neurological disorders
    • G01N2800/2814—Dementia; Cognitive disorders
    • G01N2800/2821—Alzheimer

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Molecular Biology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurology (AREA)
  • Cell Biology (AREA)
  • Biochemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Neurosurgery (AREA)
  • Microbiology (AREA)
  • Pathology (AREA)
  • Physics & Mathematics (AREA)
  • Biotechnology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Analytical Chemistry (AREA)
  • Food Science & Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Physics & Mathematics (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Toxicology (AREA)
  • Hospice & Palliative Care (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
AT96903108T 1995-02-23 1996-02-20 Herstellungb und verwendung eines spezifischen gaba-aalpha5 rezeptorligands zur behandlung der erkrankung von alzheimer ATE244018T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9503601.8A GB9503601D0 (en) 1995-02-23 1995-02-23 Method of treatment and method of manufacture of medicament
PCT/GB1996/000377 WO1996025948A1 (en) 1995-02-23 1996-02-20 PREPARATION AND USE OF A SPECIFIC GABA-Aα5 RECEPTOR LIGAND FOR TREATMENT OF ALZHEIMER'S DISEASE

Publications (1)

Publication Number Publication Date
ATE244018T1 true ATE244018T1 (de) 2003-07-15

Family

ID=10770108

Family Applications (1)

Application Number Title Priority Date Filing Date
AT96903108T ATE244018T1 (de) 1995-02-23 1996-02-20 Herstellungb und verwendung eines spezifischen gaba-aalpha5 rezeptorligands zur behandlung der erkrankung von alzheimer

Country Status (10)

Country Link
US (2) US6426343B1 (de)
EP (1) EP0810879B1 (de)
JP (1) JPH11501302A (de)
AT (1) ATE244018T1 (de)
AU (1) AU706515B2 (de)
CA (1) CA2212058C (de)
DE (1) DE69628912T2 (de)
ES (1) ES2201169T3 (de)
GB (1) GB9503601D0 (de)
WO (1) WO1996025948A1 (de)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2179490T3 (es) 1997-05-08 2003-01-16 Merck Sharp & Dohme Derivados de 1,2,4-triazolo(3,4-a)ftalazina sustituidos como ligandos de gaba alfa 5.
GB9716344D0 (en) * 1997-08-01 1997-10-08 Merck Sharp & Dohme Therapeutic compounds
KR20010041234A (ko) 1998-02-25 2001-05-15 더블유. 지. 콜 치환된 1,2,4-트리아졸로[3,4-ａ]피리다진
GB9805561D0 (en) * 1998-03-16 1998-05-13 Merck Sharp & Dohme A combination of therapeutic agents
GB9805557D0 (en) 1998-03-16 1998-05-13 Merck Sharp & Dohme A combination of therapeutic agents
GB9805559D0 (en) * 1998-03-16 1998-05-13 Merck Sharp & Dohme A combination of therapeutic agents
WO2000027849A2 (en) 1998-11-12 2000-05-18 Merck & Co., Inc. Therapeutic polymorphs of a gaba-a alpha-5 inverse agonist and pamoate formulations of the same
JP2002529406A (ja) * 1998-11-12 2002-09-10 メルク エンド カムパニー インコーポレーテッド ＧＡＢＡＡα５逆活性薬と、ＣＯＸ−２阻害剤、ＮＳＡＩＤ、エストロゲン、又はビタミンＥとの組合わせ
GB9824897D0 (en) * 1998-11-12 1999-01-06 Merck Sharp & Dohme Therapeutic compounds
US6737242B1 (en) 1999-05-07 2004-05-18 Neurogen Corporation Methods for screening GABA-modulatory compounds for specified pharmacological activities
ATE366934T1 (de) * 1999-05-07 2007-08-15 Neurogen Corp Screening-verfahren von gaba-modulierenden verbindungen für bestimmte pharmakologische wirkungen
GB9911802D0 (en) * 1999-05-20 1999-07-21 Merck Sharp & Dohme Therapeutic combination
GB9911803D0 (en) * 1999-05-20 1999-07-21 Merck Sharp & Dohme Therapeutic combination
GB9911804D0 (en) * 1999-05-20 1999-07-21 Merck Sharp & Dohme Therapeutic combination
IL145209A0 (en) 2000-09-06 2002-06-30 Pfizer Prod Inc Pharmaceutical combinations for the treatment of stroke and traumatic brain injury
GB0028583D0 (en) 2000-11-23 2001-01-10 Merck Sharp & Dohme Therapeutic compounds
US20040023952A1 (en) * 2001-06-20 2004-02-05 Leventhal Audie G. Enhanced brain function by gaba-ergic stimulation
GB0128499D0 (en) * 2001-11-28 2002-01-23 Merck Sharp & Dohme Therapeutic agents
EP2258359A3 (de) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenese durch Modulation des Muscarinrezeptors mit Sabcomelin
JP2009506069A (ja) 2005-08-26 2009-02-12 ブレインセルス，インコーポレイティド ムスカリン性受容体調節による神経発生
US7985756B2 (en) 2005-10-21 2011-07-26 Braincells Inc. Modulation of neurogenesis by PDE inhibition
WO2007053596A1 (en) 2005-10-31 2007-05-10 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
WO2007134077A2 (en) 2006-05-09 2007-11-22 Braincells, Inc. 5 ht receptor mediated neurogenesis
WO2007134136A2 (en) 2006-05-09 2007-11-22 Braincells, Inc. Neurogenesis by modulating angiotensin
WO2007139818A2 (en) 2006-05-22 2007-12-06 The Board Of Trustees Of The Leland Stanford Junior University Pharmacological treatment of cognitive impairment
EP2068872A1 (de) 2006-09-08 2009-06-17 Braincells, Inc. Kombinationen mit einem 4-acylaminopyridin-derivat
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
EP2298296A1 (de) 2009-08-25 2011-03-23 CNRS Centre National De La Recherche Scientifique Zusammensetzung und Behandlung kognitiver Beeinträchtigungen bei Personen mit Down-Syndrom
US8946206B2 (en) 2010-12-17 2015-02-03 The Board Of Trustees Of The Leland Stanford Junior University Methods for improving cognitive function
WO2012114342A1 (en) 2011-02-23 2012-08-30 Coeruleus Ltd. Flumazenil complexes, compositions comprising same and uses thereof
US20150374705A1 (en) 2012-02-14 2015-12-31 Shanghai Institues for Biological Sciences Substances for treatment or relief of pain
KR101743960B1 (ko) * 2015-07-06 2017-06-08 서울대학교산학협력단 G단백질 결합형 수용체19 작용제를 유효성분으로 함유하는 알츠하이머 질환 또는 치매를 예방, 치료 또는 지연하기 위한 약학적 조성물

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU587802B2 (en) * 1985-03-08 1989-08-31 Ferrosan A/S Novel oxadiazolyl imidazobenzodiazepine derivatives and methods of preparing such compounds
FR2672602B1 (fr) * 1991-02-12 1993-06-04 Centre Nat Rech Scient Composes derives des beta-carbolines ligands du recepteur des benzodiazepines ayant un effet agoniste inverse et antagoniste vis-a-vis des benzodiazepines et medicaments les contenant.
US5182290A (en) 1991-08-27 1993-01-26 Neurogen Corporation Certain oxazoloquinolinones; a new class of GABA brain receptor ligands
US5212310A (en) 1991-12-19 1993-05-18 Neurogen Corporation Certain aryl fused imidazopyrimidines; a new class of GABA brain receptor ligands
ES2296064T3 (es) * 1992-12-10 2008-04-16 MERCK SHARP & DOHME LIMITED Lineas celulares transfectadas de manera estable que expresan receptores gaba-a humanos con una combinacion de subunidades alfa-2, beta-3 y gamma-2.

Also Published As

Publication number Publication date
US6426343B1 (en) 2002-07-30
AU706515B2 (en) 1999-06-17
EP0810879B1 (de) 2003-07-02
CA2212058A1 (en) 1996-08-29
DE69628912D1 (de) 2003-08-07
JPH11501302A (ja) 1999-02-02
DE69628912T2 (de) 2004-06-03
WO1996025948A1 (en) 1996-08-29
ES2201169T3 (es) 2004-03-16
AU4725796A (en) 1996-09-11
CA2212058C (en) 2008-05-13
US6323198B1 (en) 2001-11-27
EP0810879A1 (de) 1997-12-10
GB9503601D0 (en) 1995-04-12

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