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WO2010087981A3 - Bicyclic amide derivatives for enhancing glutamatergic synaptic responses - Google Patents

Bicyclic amide derivatives for enhancing glutamatergic synaptic responses Download PDF

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Publication number
WO2010087981A3
WO2010087981A3 PCT/US2010/000255 US2010000255W WO2010087981A3 WO 2010087981 A3 WO2010087981 A3 WO 2010087981A3 US 2010000255 W US2010000255 W US 2010000255W WO 2010087981 A3 WO2010087981 A3 WO 2010087981A3
Authority
WO
WIPO (PCT)
Prior art keywords
syndrome
treatment
disorders
compounds
brain
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/US2010/000255
Other languages
French (fr)
Other versions
WO2010087981A2 (en
Inventor
Rudolf Mueller
Leslie J. Street
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Cortex Pharmaceuticals Inc
Original Assignee
Cortex Pharmaceuticals Inc
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
Priority to JP2011547981A priority Critical patent/JP2012516845A/en
Priority to AU2010208646A priority patent/AU2010208646A1/en
Priority to BRPI1005316A priority patent/BRPI1005316A2/en
Priority to CA2751285A priority patent/CA2751285A1/en
Priority to EA201101162A priority patent/EA018994B1/en
Priority to SG2011054376A priority patent/SG173168A1/en
Priority to CN2010800154033A priority patent/CN102369201A/en
Priority to MX2011008060A priority patent/MX2011008060A/en
Application filed by Cortex Pharmaceuticals Inc filed Critical Cortex Pharmaceuticals Inc
Priority to EP10736150A priority patent/EP2391621A4/en
Publication of WO2010087981A2 publication Critical patent/WO2010087981A2/en
Publication of WO2010087981A3 publication Critical patent/WO2010087981A3/en
Priority to IL214392A priority patent/IL214392A0/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/5381,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/05Phenols
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/537Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53831,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/16Central respiratory analeptics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08Bridged systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors. These brain networks, which are involved in cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, and in disorders wherein a deficiency in neurotrophic factors is implicated, as well as conditions such as stroke-induced central sleep apnea, obstructive sleep apnea, congenital hypoventilation syndrome, obesity hypoventilation syndrome, sudden infant death syndrome, Rett syndrome, spinal cord injury, traumatic brain injury, Cheney-Stokes respiration, Ondines curse, Prader-Willi's syndrome and drowning. In a particular aspect, the invention relates to bicyclic amide compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.
PCT/US2010/000255 2009-02-02 2010-01-29 Bicyclic amide derivatives for enhancing glutamatergic synaptic responses Ceased WO2010087981A2 (en)

Priority Applications (10)

Application Number Priority Date Filing Date Title
CN2010800154033A CN102369201A (en) 2009-02-02 2010-01-29 Bicyclic amide derivatives for the treatment of respiratory depression
BRPI1005316A BRPI1005316A2 (en) 2009-02-02 2010-01-29 compound, pharmaceutical composition, methods for treating and using a compound
CA2751285A CA2751285A1 (en) 2009-02-02 2010-01-29 Bicyclic amide derivatives for enhancing glutamatergic synaptic responses
EA201101162A EA018994B1 (en) 2009-02-02 2010-01-29 Bicyclic amide derivatives for enhancing glutamatergic synaptic responses
SG2011054376A SG173168A1 (en) 2009-02-02 2010-01-29 Bicyclic amide derivatives for enhancing glutamatergic synaptic responses
JP2011547981A JP2012516845A (en) 2009-02-02 2010-01-29 Bicyclic amide derivatives for enhancing glutamatergic synaptic responses
AU2010208646A AU2010208646A1 (en) 2009-02-02 2010-01-29 Bicyclic amide derivatives for enhancing glutamatergic synaptic responses
MX2011008060A MX2011008060A (en) 2009-02-02 2010-01-29 Bicyclic amide derivatives for enhancing glutamatergic synaptic responses.
EP10736150A EP2391621A4 (en) 2009-02-02 2010-01-29 Bicyclic amide derivatives for enhancing glutamatergic synaptic responses
IL214392A IL214392A0 (en) 2009-02-02 2011-08-01 Bicyclic amide derivatives for enhancing glutamatergic synaptic responses

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US20664209P 2009-02-02 2009-02-02
US61/206,642 2009-02-02

Publications (2)

Publication Number Publication Date
WO2010087981A2 WO2010087981A2 (en) 2010-08-05
WO2010087981A3 true WO2010087981A3 (en) 2011-03-24

Family

ID=42396261

Family Applications (2)

Application Number Title Priority Date Filing Date
PCT/US2010/000255 Ceased WO2010087981A2 (en) 2009-02-02 2010-01-29 Bicyclic amide derivatives for enhancing glutamatergic synaptic responses
PCT/US2010/000254 Ceased WO2010087980A2 (en) 2009-02-02 2010-01-29 Bicyclic amide derivatives for the treatment of respiratory depression

Family Applications After (1)

Application Number Title Priority Date Filing Date
PCT/US2010/000254 Ceased WO2010087980A2 (en) 2009-02-02 2010-01-29 Bicyclic amide derivatives for the treatment of respiratory depression

Country Status (12)

Country Link
EP (1) EP2391621A4 (en)
JP (1) JP2012516845A (en)
KR (1) KR20110115139A (en)
CN (1) CN102369201A (en)
AU (1) AU2010208646A1 (en)
BR (1) BRPI1005316A2 (en)
CA (1) CA2751285A1 (en)
EA (1) EA018994B1 (en)
IL (1) IL214392A0 (en)
MX (1) MX2011008060A (en)
SG (1) SG173168A1 (en)
WO (2) WO2010087981A2 (en)

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998035950A1 (en) * 1997-02-13 1998-08-20 Cortex Pharmaceuticals, Inc. Benzofurazan compounds which enhance ampa receptor activity
WO1999021422A1 (en) * 1997-10-27 1999-05-06 Cortex Pharmaceuticals, Inc. Treatment of schizophrenia with ampakines and neuroleptics
WO2008143963A1 (en) * 2007-05-17 2008-11-27 Cortex Pharmaceuticals, Inc. Di-substituted amides for enhancing glutamatergic synaptic responses

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK0651746T3 (en) * 1992-07-24 2002-07-29 Univ California Drugs that enhance synaptic responses mediated by AMPA receptors
US20020099050A1 (en) * 1993-07-23 2002-07-25 Lynch Gary S. Drugs that enhance synaptic responses mediated by AMPA receptors
BRPI0823262A2 (en) * 2007-08-10 2013-09-24 Cortex Pharma Inc Respiratory depression treatment method and use of a compound in the manufacture of a medicament for the treatment of respiratory depression

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998035950A1 (en) * 1997-02-13 1998-08-20 Cortex Pharmaceuticals, Inc. Benzofurazan compounds which enhance ampa receptor activity
WO1999021422A1 (en) * 1997-10-27 1999-05-06 Cortex Pharmaceuticals, Inc. Treatment of schizophrenia with ampakines and neuroleptics
WO2008143963A1 (en) * 2007-05-17 2008-11-27 Cortex Pharmaceuticals, Inc. Di-substituted amides for enhancing glutamatergic synaptic responses

Also Published As

Publication number Publication date
SG173168A1 (en) 2011-08-29
JP2012516845A (en) 2012-07-26
CA2751285A1 (en) 2010-08-05
EP2391621A4 (en) 2012-07-25
EA201101162A1 (en) 2012-01-30
EP2391621A2 (en) 2011-12-07
IL214392A0 (en) 2011-09-27
KR20110115139A (en) 2011-10-20
WO2010087980A3 (en) 2011-02-24
WO2010087981A2 (en) 2010-08-05
EA018994B1 (en) 2013-12-30
AU2010208646A1 (en) 2011-09-01
CN102369201A (en) 2012-03-07
MX2011008060A (en) 2011-09-09
WO2010087980A2 (en) 2010-08-05
BRPI1005316A2 (en) 2019-09-24

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