WO2004009062A3 - NMDA RECEPTOR ANTAGONISTS AND THEIR USE IN INHIBITING ABNORMAL HYPERPHOSPHORYLATION OF MICROTUBULE ASSOCIATED PROTEIN tau - Google Patents

NMDA RECEPTOR ANTAGONISTS AND THEIR USE IN INHIBITING ABNORMAL HYPERPHOSPHORYLATION OF MICROTUBULE ASSOCIATED PROTEIN tau Download PDF

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Publication number
WO2004009062A3
WO2004009062A3 PCT/US2003/022362 US0322362W WO2004009062A3 WO 2004009062 A3 WO2004009062 A3 WO 2004009062A3 US 0322362 W US0322362 W US 0322362W WO 2004009062 A3 WO2004009062 A3 WO 2004009062A3
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Prior art keywords
associated protein
protein tau
receptor antagonists
nmda receptor
microtubule associated
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Ceased
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PCT/US2003/022362
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French (fr)
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WO2004009062A2 (en
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Khalid Iqbal
Inge Grundke-Iqbal
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Priority to AU2003251993A priority Critical patent/AU2003251993A1/en
Priority to EP03765660A priority patent/EP1523309A2/en
Publication of WO2004009062A2 publication Critical patent/WO2004009062A2/en
Publication of WO2004009062A3 publication Critical patent/WO2004009062A3/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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • 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
    • A61K31/13—Amines
    • A61K31/132—Amines having two or more amino groups, e.g. spermidine, putrescine
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Virology (AREA)
  • Psychology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Hospice & Palliative Care (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Oncology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Aminocyclohexane and aminoalkylcyclohexane compounds, which are systemically-active as NMDA receptor antagonists, are effective in inhibiting abnormal hyperphosphorylation of microtubule associated protein tau, method of treating disorders resulting from or associated with abnormal hyperphosphorylation of microtubule associated protein tau such as various neurodegeneratives diseases, and pharmaceutical compositions comprising the same.
PCT/US2003/022362 2002-07-19 2003-07-17 NMDA RECEPTOR ANTAGONISTS AND THEIR USE IN INHIBITING ABNORMAL HYPERPHOSPHORYLATION OF MICROTUBULE ASSOCIATED PROTEIN tau Ceased WO2004009062A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU2003251993A AU2003251993A1 (en) 2002-07-19 2003-07-17 NMDA RECEPTOR ANTAGONISTS AND THEIR USE IN INHIBITING ABNORMAL HYPERPHOSPHORYLATION OF MICROTUBULE ASSOCIATED PROTEIN tau
EP03765660A EP1523309A2 (en) 2002-07-19 2003-07-17 Nmda receptor antagonists and their use in inhibiting abnormal hyperphosphorylation of microtubule associated protein tau

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US39743402P 2002-07-19 2002-07-19
US60/397,434 2002-07-19

Publications (2)

Publication Number Publication Date
WO2004009062A2 WO2004009062A2 (en) 2004-01-29
WO2004009062A3 true WO2004009062A3 (en) 2004-12-23

Family

ID=30771058

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2003/022362 Ceased WO2004009062A2 (en) 2002-07-19 2003-07-17 NMDA RECEPTOR ANTAGONISTS AND THEIR USE IN INHIBITING ABNORMAL HYPERPHOSPHORYLATION OF MICROTUBULE ASSOCIATED PROTEIN tau

Country Status (7)

Country Link
US (3) US20040019118A1 (en)
EP (1) EP1523309A2 (en)
AR (1) AR040604A1 (en)
AU (1) AU2003251993A1 (en)
TW (1) TW200410672A (en)
WO (1) WO2004009062A2 (en)
ZA (1) ZA200501430B (en)

Families Citing this family (31)

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US8557855B2 (en) * 2002-07-03 2013-10-15 Allergan, Inc. Methods of using ryanodine antagonists in treating neural injury
US20050113458A1 (en) * 2003-10-22 2005-05-26 Forest Laboratories, Inc. Use of 1-aminocyclohexane derivatives to modify deposition of fibrillogenic a-beta peptides in amyloidopathies
AR046314A1 (en) * 2003-11-05 2005-11-30 Merz Pharma Gmbh & Co Kgaa COMPOSITIONS THAT INCLUDE CYCLHEXILAMINES AND AMINOADAMANTANS
TW200531680A (en) * 2004-03-03 2005-10-01 Merz Pharma Gmbh & Co Kgaa Therapy using 1-aminocyclohexane derivatives for the treatment of behavioral disorders associated with alzheimer's disease
US7456224B2 (en) 2004-04-05 2008-11-25 Forest Laboratories Holdings, Ltd. Method for treating autism
CA2578953A1 (en) * 2004-09-23 2006-03-30 Merz Pharma Gmbh & Co. Kgaa Memantine for the treatment of childhood behavioral disorders
US20060205822A1 (en) * 2004-12-22 2006-09-14 Forest Laboratories, Inc. 1-Aminocyclohexane derivatives for the treatment of multiple sclerosis, emotional lability and pseudobulbar affect
US20070049630A1 (en) * 2005-08-24 2007-03-01 Allergan, Inc. Method of using ryanodine receptor antagonists to treat amyotrophic lateral sclerosis
US20070066638A1 (en) * 2005-09-16 2007-03-22 Cun-Jian Dong Ryanodine receptor blockers for treating pain
ES2321996B1 (en) * 2006-01-26 2010-03-05 Consejo Superior Investig. Cientificas USE OF COMPOUNDS THAT JOIN THE DOMAIN OF UNION TO TAU MICROTUBLES IN THE DEVELOPMENT OF PHARMACEUTICAL COMPOSITIONS, SUCH PHARMACEUTICAL COMPOSITIONS AND THEIR APPLICATION IN THE TREATMENT OF TAUOPATIAS.
US20070196856A1 (en) * 2006-02-23 2007-08-23 Allergan, Inc. Methods of determining activity of ryanodine receptor modulators
US20080108643A1 (en) * 2006-11-03 2008-05-08 Forest Laboratories Holdings Limited Method for treating autism
US8278345B2 (en) 2006-11-09 2012-10-02 Probiodrug Ag Inhibitors of glutaminyl cyclase
JP5523107B2 (en) 2006-11-30 2014-06-18 プロビオドルグ エージー Novel inhibitors of glutaminyl cyclase
JP2010515026A (en) * 2006-12-21 2010-05-06 コグノッシ， インコーポレイテッド Method for adjusting SET and use thereof
EP2481408A3 (en) 2007-03-01 2013-01-09 Probiodrug AG New use of glutaminyl cyclase inhibitors
WO2008128985A1 (en) 2007-04-18 2008-10-30 Probiodrug Ag Thiourea derivatives as glutaminyl cyclase inhibitors
WO2009033151A1 (en) * 2007-09-07 2009-03-12 The Trustees Of Columbia University In The City Of New York Tau protein screening assay
US8506933B2 (en) * 2007-11-30 2013-08-13 Msdx, Inc. Methods of detecting a neurological condition via analysis of circulating phagocytes
EP2111858A1 (en) * 2008-04-25 2009-10-28 EPFL Ecole Polytechnique Fédérale de Lausanne Novel treatment for alzheimer's disease
JP5993303B2 (en) * 2009-04-30 2016-09-14 グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング Use of 1-phenyl-3-dimethylaminopropane compounds for the treatment of rheumatic pain
MX2012002993A (en) 2009-09-11 2012-04-19 Probiodrug Ag Heterocylcic derivatives as inhibitors of glutaminyl cyclase.
WO2011066460A1 (en) * 2009-11-27 2011-06-03 Msdx, Inc. Methods of detecting or monitoring activity of an inflammatory or neurodegenerative condition
JP6026284B2 (en) 2010-03-03 2016-11-16 プロビオドルグ エージー Inhibitors of glutaminyl cyclase
US8269019B2 (en) 2010-03-10 2012-09-18 Probiodrug Ag Inhibitors
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
DE102010024105A1 (en) 2010-06-17 2011-12-22 Grünenthal GmbH Transdermal administration of memantine
US8673309B2 (en) 2011-02-11 2014-03-18 Msdx, Inc. Methods for measuring high molecular weight complexes of fibrinogen with fibronectin and fibulin-1
ES2570167T3 (en) 2011-03-16 2016-05-17 Probiodrug Ag Benzimidazole derivatives as glutaminyl cyclase inhibitors
US20190110972A1 (en) * 2013-11-20 2019-04-18 Lg Household & Health Care Ltd. Oral composition for tooth whitening product, and kit comprising same
PL3461819T3 (en) 2017-09-29 2020-11-30 Probiodrug Ag Inhibitors of glutaminyl cyclase

Citations (5)

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US5061703A (en) * 1989-04-14 1991-10-29 Merz + Co. Gmbh & Co. Adamantane derivatives in the prevention and treatment of cerebral ischemia
WO1992017168A1 (en) * 1991-04-04 1992-10-15 The Children's Medical Center Corporation Method of preventing nmda receptor-mediated neuronal damage
US5614560A (en) * 1991-04-04 1997-03-25 Children's Medical Center Corporation Method of preventing NMDA receptor-mediated neuronal damage
WO1999001416A2 (en) * 1997-06-30 1999-01-14 Merz + Co. Gmbh & Co. 1-amino-alkylcyclohexane nmda receptor antagonists
WO2001089448A2 (en) * 2000-03-28 2001-11-29 Olney John W Combination of adrenergic agonist and nmda antagonist for relieving chronic pain without adverse side effects

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Patent Citations (5)

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US5061703A (en) * 1989-04-14 1991-10-29 Merz + Co. Gmbh & Co. Adamantane derivatives in the prevention and treatment of cerebral ischemia
WO1992017168A1 (en) * 1991-04-04 1992-10-15 The Children's Medical Center Corporation Method of preventing nmda receptor-mediated neuronal damage
US5614560A (en) * 1991-04-04 1997-03-25 Children's Medical Center Corporation Method of preventing NMDA receptor-mediated neuronal damage
WO1999001416A2 (en) * 1997-06-30 1999-01-14 Merz + Co. Gmbh & Co. 1-amino-alkylcyclohexane nmda receptor antagonists
WO2001089448A2 (en) * 2000-03-28 2001-11-29 Olney John W Combination of adrenergic agonist and nmda antagonist for relieving chronic pain without adverse side effects

Non-Patent Citations (5)

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Title
NAISH HYWEL J ET AL: "Effect of low-affinity NMDA receptor antagonists on electrical activity in mouse cortical slices", EUROPEAN JOURNAL OF PHARMACOLOGY, vol. 443, no. 1-3, 17 May 2002 (2002-05-17), pages 79 - 83, XP002292644, ISSN: 0014-2999 *
NASKAR RITA ET AL: "Phenytoin blocks retinal ganglion cell death after partial optic nerve crush", EXPERIMENTAL EYE RESEARCH, vol. 74, no. 6, June 2002 (2002-06-01), pages 747 - 752, XP002271138, ISSN: 0014-4835 *
PARSONS C G ET AL: "Memantine and the amino-alkyl-cyclohexane MRZ 2/579 are moderate affinity uncompetitive NMDA receptor antagonists: In vitro characterisation", AMINO ACIDS (VIENNA), vol. 19, no. 1, 2000, pages 157 - 166, XP002292645, ISSN: 0939-4451 *
SCHUETTAUF FRANK ET AL: "Effects of anti-glaucoma medications on gangion cell survival: The DBA/2J mouse model.", VISION RESEARCH, vol. 42, no. 20, September 2002 (2002-09-01), pages 2333 - 2337, XP002271127, ISSN: 0042-6989 *
WENK ET AL: "Neuroprotection by novel antagonists at the NMDA receptor channel and glycineB sites", EUROPEAN JOURNAL OF PHARMACOLOGY, AMSTERDAM, NL, vol. 347, 1998, pages 183 - 187, XP002104884, ISSN: 0014-2999 *

Also Published As

Publication number Publication date
TW200410672A (en) 2004-07-01
AU2003251993A1 (en) 2004-02-09
AU2003251993A8 (en) 2004-02-09
EP1523309A2 (en) 2005-04-20
ZA200501430B (en) 2006-07-26
US20120157537A1 (en) 2012-06-21
WO2004009062A2 (en) 2004-01-29
US20040019118A1 (en) 2004-01-29
AR040604A1 (en) 2005-04-13
US20090005459A1 (en) 2009-01-01

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