ZA200302918B - Combination use of acetylcholinesterase inhibitors and gabaa inverse agonists for the treatment of cognitive disorders. - Google Patents

Combination use of acetylcholinesterase inhibitors and gabaa inverse agonists for the treatment of cognitive disorders. Download PDF

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Publication number
ZA200302918B
ZA200302918B ZA200302918A ZA200302918A ZA200302918B ZA 200302918 B ZA200302918 B ZA 200302918B ZA 200302918 A ZA200302918 A ZA 200302918A ZA 200302918 A ZA200302918 A ZA 200302918A ZA 200302918 B ZA200302918 B ZA 200302918B
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ZA
South Africa
Prior art keywords
tetrahydro
naphthyridine
carboxamide
oxo
ethoxy
Prior art date
Application number
ZA200302918A
Other languages
English (en)
Inventor
Anabella Villalobos
James Vincent Cassella
Lavanya Rajachandran
Original Assignee
Pfizer Prod Inc
Neurogen 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 Pfizer Prod Inc, Neurogen Corp filed Critical Pfizer Prod Inc
Publication of ZA200302918B publication Critical patent/ZA200302918B/en

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    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • 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
    • 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
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K31/47Quinolines; Isoquinolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
ZA200302918A 2000-10-17 2003-04-11 Combination use of acetylcholinesterase inhibitors and gabaa inverse agonists for the treatment of cognitive disorders. ZA200302918B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US24114500P 2000-10-17 2000-10-17

Publications (1)

Publication Number Publication Date
ZA200302918B true ZA200302918B (en) 2004-04-13

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Family Applications (1)

Application Number Title Priority Date Filing Date
ZA200302918A ZA200302918B (en) 2000-10-17 2003-04-11 Combination use of acetylcholinesterase inhibitors and gabaa inverse agonists for the treatment of cognitive disorders.

Country Status (14)

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US (2) US20020151591A1 (es)
EP (1) EP1328294A2 (es)
JP (1) JP2004511512A (es)
KR (1) KR20030046509A (es)
AR (1) AR030893A1 (es)
AU (2) AU9411701A (es)
CA (1) CA2426120A1 (es)
HU (1) HUP0302476A3 (es)
IL (1) IL155225A0 (es)
NZ (1) NZ525103A (es)
PE (1) PE20020473A1 (es)
UY (1) UY26970A1 (es)
WO (1) WO2002032412A2 (es)
ZA (1) ZA200302918B (es)

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MXPA05006940A (es) * 2002-12-24 2006-02-22 Neurochem Int Ltd Formulaciones terapeuticas para el tratamiento de enfermedades relacionadas con beta - amiloide.
US8299062B2 (en) * 2003-09-17 2012-10-30 Franklin Volvovitz Pharmaceutical compositions and methods for preventing, treating, or reversing neuronal dysfunction
WO2005027968A1 (ja) * 2003-09-19 2005-03-31 Eisai Co., Ltd. ダウン症候群治療剤
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CA2566204A1 (en) * 2004-05-14 2005-12-01 The Johns Hopkins University Method for improving cognitive function by co-administration of a gabab receptor antagonist and an acetylcholinesterase inhibitor
PA8640801A1 (es) * 2004-08-09 2006-08-03 Warner Lambert Co Nuevos inhibidores de la recaptacion de norepinefrina de quinoxalinona para el tratamiento de trastornos del sistema nervioso central
CN100382802C (zh) * 2005-08-08 2008-04-23 赵德禄 治疗自主神经系统功能紊乱的药物
EP2032987B1 (en) 2006-05-22 2016-02-24 The Board of Trustees of The Leland Stanford Junior University Pharmacological treatment of cognitive impairment
DK2074123T3 (da) * 2006-10-16 2013-01-14 Bionomics Ltd Nye anxiolytiske forbindelser
US10954231B2 (en) 2006-10-16 2021-03-23 Bionomics Limited Anxiolytic compounds
EP2089383B1 (en) 2006-11-09 2015-09-16 Probiodrug AG 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
ATE554085T1 (de) 2006-11-30 2012-05-15 Probiodrug Ag Neue inhibitoren von glutaminylcyclase
MX2009009234A (es) 2007-03-01 2009-12-01 Probiodrug Ag Uso nuevo de inhibidores de ciclasa de glutaminilo.
WO2008128985A1 (en) 2007-04-18 2008-10-30 Probiodrug Ag Thiourea derivatives as glutaminyl cyclase inhibitors
KR101755737B1 (ko) 2009-09-11 2017-07-07 프로비오드룩 아게 글루타미닐 사이클라제의 억제제로서 헤테로사이클릭 유도체
EA037187B1 (ru) 2010-02-09 2021-02-17 Дзе Джонс Хопкинс Юниверсити Способ и композиция для лечения когнитивного расстройства
US9181233B2 (en) 2010-03-03 2015-11-10 Probiodrug Ag Inhibitors of glutaminyl cyclase
CA2789440C (en) 2010-03-10 2020-03-24 Probiodrug Ag Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5)
JP5945532B2 (ja) 2010-04-21 2016-07-05 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤としてのベンゾイミダゾール誘導体
AU2011328993B2 (en) 2010-11-15 2017-03-02 Agenebio, Inc. Pyridazine derivatives, compositions and methods for treating cognitive impairment
WO2012116415A1 (en) 2011-03-02 2012-09-07 Bionomics Limited Novel small-molecules as therapeutics
ES2570167T3 (es) 2011-03-16 2016-05-17 Probiodrug Ag Derivados de benzimidazol como inhibidores de glutaminil ciclasa
JP6055817B2 (ja) 2011-05-12 2016-12-27 バイオノミックス リミテッド ナフチリジンの調製方法
US10154988B2 (en) 2012-11-14 2018-12-18 The Johns Hopkins University Methods and compositions for treating schizophrenia
WO2014144663A1 (en) 2013-03-15 2014-09-18 The Johns Hopkins University Methods and compositions for improving cognitive function
WO2014144801A1 (en) 2013-03-15 2014-09-18 Agenebio Inc. Methods and compositions for improving cognitive function
JP6883988B2 (ja) 2013-12-20 2021-06-09 エージンバイオ, インコーポレイテッド ベンゾジアゼピン誘導体、組成物、および認知障害を処置するための方法
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Also Published As

Publication number Publication date
JP2004511512A (ja) 2004-04-15
UY26970A1 (es) 2002-06-20
AR030893A1 (es) 2003-09-03
HUP0302476A3 (en) 2005-05-30
HUP0302476A2 (hu) 2003-11-28
IL155225A0 (en) 2003-11-23
PE20020473A1 (es) 2002-06-14
EP1328294A2 (en) 2003-07-23
KR20030046509A (ko) 2003-06-12
CA2426120A1 (en) 2002-04-25
WO2002032412A3 (en) 2003-03-20
US20050009861A1 (en) 2005-01-13
AU2001294117B2 (en) 2006-07-27
US20020151591A1 (en) 2002-10-17
WO2002032412A2 (en) 2002-04-25
AU9411701A (en) 2002-04-29
NZ525103A (en) 2004-12-24

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