AU2001294117B2 - 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
AU2001294117B2
AU2001294117B2 AU2001294117A AU2001294117A AU2001294117B2 AU 2001294117 B2 AU2001294117 B2 AU 2001294117B2 AU 2001294117 A AU2001294117 A AU 2001294117A AU 2001294117 A AU2001294117 A AU 2001294117A AU 2001294117 B2 AU2001294117 B2 AU 2001294117B2
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Australia
Prior art keywords
dihydro
naphthyridine
oxo
carboxamide
ethoxy
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Ceased
Application number
AU2001294117A
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AU2001294117A1 (en
Inventor
James Vincent Cassella
Lavanya Rajachandran
Anabella Villalobos
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Neurogen Corp
Pfizer Products Inc
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Neurogen Corp
Pfizer Products Inc
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Publication of AU2001294117A1 publication Critical patent/AU2001294117A1/en
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Publication of AU2001294117B2 publication Critical patent/AU2001294117B2/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • 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
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 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
    • 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
    • A61K31/13—Amines
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • 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
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • 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
    • A61K31/66—Phosphorus compounds
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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)
AU2001294117A 2000-10-17 2001-10-15 Combination use of acetylcholinesterase inhibitors and GABAA inverse agonists for the treatment of cognitive disorders Ceased AU2001294117B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US24114500P 2000-10-17 2000-10-17
US60/241,145 2000-10-17
PCT/IB2001/001934 WO2002032412A2 (en) 2000-10-17 2001-10-15 Combination use of acetylcholinesterase inhibitors and gabaa inverse agonists for the treatment of cognitive disorders

Publications (2)

Publication Number Publication Date
AU2001294117A1 AU2001294117A1 (en) 2002-07-04
AU2001294117B2 true AU2001294117B2 (en) 2006-07-27

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AU2001294117A Ceased AU2001294117B2 (en) 2000-10-17 2001-10-15 Combination use of acetylcholinesterase inhibitors and GABAA inverse agonists for the treatment of cognitive disorders
AU9411701A Pending AU9411701A (en) 2000-10-17 2001-10-15 Combination use of acetylcholinesterase inhibitors and gaba<sub>A</sub> inverse agonists for the treatment of cognitive disorders

Family Applications After (1)

Application Number Title Priority Date Filing Date
AU9411701A Pending AU9411701A (en) 2000-10-17 2001-10-15 Combination use of acetylcholinesterase inhibitors and gaba<sub>A</sub> inverse agonists for the treatment of cognitive disorders

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US (2) US20020151591A1 (https=)
EP (1) EP1328294A2 (https=)
JP (1) JP2004511512A (https=)
KR (1) KR20030046509A (https=)
AR (1) AR030893A1 (https=)
AU (2) AU2001294117B2 (https=)
CA (1) CA2426120A1 (https=)
HU (1) HUP0302476A3 (https=)
IL (1) IL155225A0 (https=)
NZ (1) NZ525103A (https=)
PE (1) PE20020473A1 (https=)
UY (1) UY26970A1 (https=)
WO (1) WO2002032412A2 (https=)
ZA (1) ZA200302918B (https=)

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AU2003292936A1 (en) * 2002-12-24 2004-07-22 Neurochem (International) Limited Therapeutic formulations for the treatment of beta-amyloid related diseases
US8299062B2 (en) * 2003-09-17 2012-10-30 Franklin Volvovitz Pharmaceutical compositions and methods for preventing, treating, or reversing neuronal dysfunction
EP1666066A4 (en) * 2003-09-19 2007-03-28 Eisai R&D Man Co Ltd DRUG AGAINST THE DOWN SYNDROME
TW200533371A (en) * 2004-04-15 2005-10-16 Dainippon Pharmaceutical Co Medicament comprising a combination of an acetylcholinesterase inhibitor and a 5-substituted-3-oxadiazolyl-1,6-naphthyridin-2(1h)-one derivative
WO2005112946A1 (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
JP2008509212A (ja) * 2004-08-09 2008-03-27 ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー 中枢神経系障害の治療のための新規なキノキサリノンノルエピネフリン再吸収阻害剤
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
US10954231B2 (en) 2006-10-16 2021-03-23 Bionomics Limited Anxiolytic compounds
NZ576036A (en) 2006-10-16 2010-10-29 Bionomics Ltd Naphthyridine containing compounds for treating anxiety disorders
US8278345B2 (en) 2006-11-09 2012-10-02 Probiodrug Ag Inhibitors of glutaminyl cyclase
ATE554085T1 (de) 2006-11-30 2012-05-15 Probiodrug Ag Neue inhibitoren von glutaminylcyclase
JP5930573B2 (ja) 2007-03-01 2016-06-15 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤の新規使用
EP2142514B1 (en) 2007-04-18 2014-12-24 Probiodrug AG Thiourea derivatives as glutaminyl cyclase inhibitors
JP5934645B2 (ja) 2009-09-11 2016-06-15 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのヘテロ環式誘導体
AU2011215870B2 (en) 2010-02-09 2016-01-28 The Johns Hopkins University Methods and compositions for improving cognitive function
JP6026284B2 (ja) 2010-03-03 2016-11-16 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
NZ602312A (en) 2010-03-10 2014-02-28 Probiodrug Ag Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5)
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
EP3034079B1 (en) 2010-11-15 2018-01-10 Agenebio, Inc. Pyridazine derivatives, compositions and methods for treating cognitive impairment
US9023848B2 (en) 2011-03-02 2015-05-05 Bionomics Limited Small-molecules as therapeutics
EP2686313B1 (en) 2011-03-16 2016-02-03 Probiodrug AG Benzimidazole derivatives as inhibitors of glutaminyl cyclase
EP2707367B1 (en) 2011-05-12 2019-10-09 Bionomics Limited Methods for preparing naphthyridines
US20140206667A1 (en) 2012-11-14 2014-07-24 Michela Gallagher 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
JP6433482B2 (ja) 2013-03-15 2018-12-05 エージンバイオ， インコーポレイテッド 認知機能を改善するための方法および組成物
NZ760341A (en) 2013-12-20 2021-12-24 Agenebio Inc Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment
WO2016191288A1 (en) 2015-05-22 2016-12-01 Agenebio, Inc. Extended release pharmaceutical compositions of levetiracetam
MX392119B (es) 2015-06-19 2025-03-11 Agenebio Inc Derivados de benzodiazepina, composiciones y metodos para tratar deterioro cognitivo
US20180170941A1 (en) 2016-12-19 2018-06-21 Agenebio, Inc. Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment
US11505555B2 (en) 2016-12-19 2022-11-22 Agenebio, Inc. Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment
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CN120584115A (zh) 2022-08-19 2025-09-02 艾吉因生物股份有限公司 苯并氮杂䓬衍生物、组合物和用于治疗认知损害的方法

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Also Published As

Publication number Publication date
US20020151591A1 (en) 2002-10-17
IL155225A0 (en) 2003-11-23
WO2002032412A2 (en) 2002-04-25
WO2002032412A3 (en) 2003-03-20
CA2426120A1 (en) 2002-04-25
HUP0302476A3 (en) 2005-05-30
PE20020473A1 (es) 2002-06-14
HUP0302476A2 (hu) 2003-11-28
JP2004511512A (ja) 2004-04-15
AU9411701A (en) 2002-04-29
EP1328294A2 (en) 2003-07-23
KR20030046509A (ko) 2003-06-12
US20050009861A1 (en) 2005-01-13
AR030893A1 (es) 2003-09-03
UY26970A1 (es) 2002-06-20
NZ525103A (en) 2004-12-24
ZA200302918B (en) 2004-04-13

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