CA2440284A1 - Ph-dependent nmda receptor antagonists - Google Patents

Ph-dependent nmda receptor antagonists Download PDF

Info

Publication number
CA2440284A1
CA2440284A1 CA002440284A CA2440284A CA2440284A1 CA 2440284 A1 CA2440284 A1 CA 2440284A1 CA 002440284 A CA002440284 A CA 002440284A CA 2440284 A CA2440284 A CA 2440284A CA 2440284 A1 CA2440284 A1 CA 2440284A1
Authority
CA
Canada
Prior art keywords
lower alkyl
group
alkyl
aryl
independently
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.)
Abandoned
Application number
CA002440284A
Other languages
English (en)
French (fr)
Inventor
Raymond J. Dingledine
Dennis C. Liotta
Stephen F. Traynelis
James P. Snyder
Yesmin Altas
David D. Mott
James J. Doherty
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.)
Emory University
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA2440284A1 publication Critical patent/CA2440284A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/02—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C217/04—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C217/28—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having one amino group and at least two singly-bound oxygen atoms, with at least one being part of an etherified hydroxy group, bound to the carbon skeleton, e.g. ethers of polyhydroxy amines
    • C07C217/30—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having one amino group and at least two singly-bound oxygen atoms, with at least one being part of an etherified hydroxy group, bound to the carbon skeleton, e.g. ethers of polyhydroxy amines having the oxygen atom of at least one of the etherified hydroxy groups further bound to a carbon atom of a six-membered aromatic ring
    • C07C217/32—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having one amino group and at least two singly-bound oxygen atoms, with at least one being part of an etherified hydroxy group, bound to the carbon skeleton, e.g. ethers of polyhydroxy amines having the oxygen atom of at least one of the etherified hydroxy groups further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted
    • C07C217/34—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having one amino group and at least two singly-bound oxygen atoms, with at least one being part of an etherified hydroxy group, bound to the carbon skeleton, e.g. ethers of polyhydroxy amines having the oxygen atom of at least one of the etherified hydroxy groups further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted by halogen atoms, by trihalomethyl, nitro or nitroso groups, or by singly-bound oxygen atoms
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/28—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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/08—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/21—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D263/18—Oxygen atoms
    • C07D263/20—Oxygen atoms attached in position 2
    • C07D263/24—Oxygen atoms attached in position 2 with hydrocarbon radicals, substituted by oxygen atoms, attached to other ring carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CA002440284A 2001-03-08 2002-03-08 Ph-dependent nmda receptor antagonists Abandoned CA2440284A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US27420501P 2001-03-08 2001-03-08
US60/274,205 2001-03-08
PCT/US2002/007033 WO2002072542A2 (en) 2001-03-08 2002-03-08 Ph-dependent nmda receptor antagonists

Publications (1)

Publication Number Publication Date
CA2440284A1 true CA2440284A1 (en) 2002-09-19

Family

ID=23047230

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002440284A Abandoned CA2440284A1 (en) 2001-03-08 2002-03-08 Ph-dependent nmda receptor antagonists

Country Status (6)

Country Link
US (2) US7375136B2 (cg-RX-API-DMAC7.html)
EP (1) EP1436258A4 (cg-RX-API-DMAC7.html)
JP (1) JP2005506292A (cg-RX-API-DMAC7.html)
AU (1) AU2002250256B2 (cg-RX-API-DMAC7.html)
CA (1) CA2440284A1 (cg-RX-API-DMAC7.html)
WO (1) WO2002072542A2 (cg-RX-API-DMAC7.html)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7375136B2 (en) * 2001-03-08 2008-05-20 Emory University pH-dependent NMDA receptor antagonists
ES2686625T3 (es) * 2001-12-06 2018-10-18 Fibrogen, Inc. Métodos para el tratamiento o prevención de la anemia
JP2004123562A (ja) * 2002-09-30 2004-04-22 Japan Science & Technology Corp 神経細胞死抑制作用を有する化合物を用いた医薬
US7732162B2 (en) * 2003-05-05 2010-06-08 Probiodrug Ag Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases
WO2005089430A2 (en) * 2004-03-17 2005-09-29 Neurorecovery, Inc. System and method for neurological injury detection, classification and subsequent injury amelioration
EP1791569A4 (en) * 2004-08-23 2009-12-16 Univ Emory Improved selection of-ph dependent compounds for in vivo therapy
EP1976495A2 (en) * 2006-01-06 2008-10-08 Aarhus Universitet Compounds acting on the serotonin transporter
WO2008055945A1 (en) 2006-11-09 2008-05-15 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
DK2091948T3 (da) 2006-11-30 2012-07-23 Probiodrug Ag Nye inhibitorer af glutaminylcyclase
EP2481408A3 (en) 2007-03-01 2013-01-09 Probiodrug AG New use of glutaminyl cyclase inhibitors
US8609649B2 (en) 2007-03-20 2013-12-17 Brandeis University Compositions and methods for the diagnosis, treatment, and prevention of amyotrophic lateral sclerosis and related neurological diseases
WO2008120655A1 (ja) 2007-03-30 2008-10-09 Institute Of Medicinal Molecular Design, Inc. Ｉ型１１βヒドロキシステロイド脱水素酵素阻害活性を有するオキサゾリジノン誘導体
DK2142514T3 (da) 2007-04-18 2015-03-23 Probiodrug Ag Thioureaderivater som glutaminylcyclase-inhibitorer
CN103058957A (zh) * 2007-06-29 2013-04-24 埃莫里大学 用于神经保护的nmda受体拮抗剂
BRPI0820406A2 (pt) * 2007-11-06 2015-05-19 Univ Emory Métodos para identificar aumento de antagonistas do receptor nmda
KR20110016891A (ko) * 2008-05-09 2011-02-18 에모리 유니버시티 신경정신 장애의 치료를 위한 ｎｍｄａ 수용체 길항물질
US8486940B2 (en) 2009-09-11 2013-07-16 Probiodrug Ag Inhibitors
WO2011101774A1 (en) 2010-02-16 2011-08-25 Pfizer Inc. (r)-4-((4-((4-(tetrahydrofuran-3-yloxy)benzo[d]isoxazol-3-yloxy)methyl)piperidin-1-yl)methyl)tetrahydro-2h-pyran-4-ol, a partial agonist of 5-ht4 receptors
WO2011107530A2 (en) 2010-03-03 2011-09-09 Probiodrug Ag Novel inhibitors
ES2481823T3 (es) 2010-03-10 2014-07-31 Probiodrug Ag Inhibidores heterocíclicos de glutaminil ciclasa (QC, EC 2.3.2.5)
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
US8530670B2 (en) 2011-03-16 2013-09-10 Probiodrug Ag Inhibitors
CN104490872A (zh) * 2014-12-11 2015-04-08 温州医科大学附属第一医院 2-(2-苯并呋喃基)-2-咪唑啉治疗神经系统线粒体损伤疾病中的用途
EP3383429B1 (en) 2015-11-30 2020-10-14 INSERM - Institut National de la Santé et de la Recherche Médicale Nmdar antagonists for the treatment of tumor angiogenesis
PL3461819T3 (pl) 2017-09-29 2020-11-30 Probiodrug Ag Inhibitory cyklazy glutaminylowej
WO2021019375A1 (en) * 2019-07-31 2021-02-04 Sea4Us - Biotecnologia E Recursos Marinhos, Lda. Kv1.3 antagonists for use in the treatment of chronic and acute pain
CA3149175A1 (en) 2019-07-31 2021-02-04 Sea4Us - Biotecnologia E Recursos Marinhos, Lda. Nitenin analogue compounds and their use in the treatment of chronic and acute pain
AU2022339672B2 (en) 2021-09-02 2025-10-16 Emory University Glun2b-subunit selective antagonists of the n-methyl-d-aspartate receptors with enhanced potency at acidic ph

Family Cites Families (92)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US509009A (en) * 1893-11-21 Hermann wecker
EG18188A (en) * 1986-05-01 1992-09-30 Pfizer Ltd Process for preparation anti-arhythmia agents
US4906779A (en) 1986-07-10 1990-03-06 State Of Oregon, Acting By And Through The Oregon State Board Of Higher Education, Acting For And On Behalf Of The Oregon Health Sciences University N,N'-disubstituted guanidines and their use as excitatory amino acid antagonists
US5093525A (en) 1986-07-10 1992-03-03 State Of Oregon, Acting By And Through The Oregon State Board Of Higher Education, Acting For And On Behalf Of The Oregon Health Sciences University N,N'-disubstituted guanidines and their use as excitatory amino acid antagonists
US5190976A (en) 1986-07-10 1993-03-02 State Of Oregon, Acting By And Through The Oregon State Board Of Higher Education, Acting For And On Behalf Of The Oregon Health Sciences University And University Of Oregon N,N'-disubstituted guanidines and their use as excitatory amino acid antagonists
US5179085A (en) 1989-03-15 1993-01-12 Warner-Lambert Company N-substituted α-amino acids and derivatives thereof having pharmaceutical activity
US4957909A (en) 1989-05-04 1990-09-18 American Home Products Corporation Benzobicycloalkane derivatives as anticonvulsant neuroprotective agents
US4924008A (en) 1989-05-04 1990-05-08 American Home Products Corporation Benzobicycloalkane derivatives as anticonvulsant neuroprotective agents
US4994467A (en) 1989-05-31 1991-02-19 Zimmerman Andrew W Treating autism and other developmental disorders in children with NMDA receptor antagonists
US5500419A (en) 1989-09-19 1996-03-19 Merrell Dow Pharmaceuticals Inc. NMDA antagonists
US5326756A (en) 1989-09-19 1994-07-05 Merrell Dow Pharmaceuticals Inc. R-4-oxo-5 phosphononorvaline used as NMDA antagonists
US5095009A (en) 1990-04-11 1992-03-10 Merrell Dow Pharmaceuticals Inc. NMDA antagonists
US5474990A (en) 1989-10-20 1995-12-12 Olney; John W. Barbiturates as safening agents in conjunction with NMDA antagonists
US5767130A (en) 1989-10-20 1998-06-16 Olney; John W. Use of kainic acid antagonists to prevent toxic side effects of NMDA antagonists
US5629307A (en) 1989-10-20 1997-05-13 Olney; John W. Use of ibogaine in reducing excitotoxic brain damage
EP0424179A3 (en) 1989-10-20 1991-12-27 John William Olney Use of combined excitatory amino acid and cholinergic antagonists to prevent neurological deterioration
US5034400A (en) 1989-10-20 1991-07-23 Olney John W Method for preventing neurotoxic side effects of NMDA antagonists
US5132313A (en) 1989-10-26 1992-07-21 University Of Pittsburgh Non-competitive NMDA receptor antagonists and methods for their use
US5013540A (en) 1989-11-30 1991-05-07 Board Of Regents, The University Of Texas System Using NMDA receptor antagonists to reduce damage due to laser treatment
US5039528A (en) 1989-12-11 1991-08-13 Olney John W EAA antagonists as anti-emetic drugs
US5336689A (en) 1990-03-02 1994-08-09 State Of Oregon, Acting By And Through The Oregon State Board Of Higher Education, Acting For And On Behalf Of The Oregon Health Sciences University And The University Of Oregon Tri- and tetra-substituted guanidines and their use as excitatory amino acid antagonists
IE910719A1 (en) 1990-03-02 1991-09-11 Oregon State Tri- and tetra-substituted guanidines and their use as¹excitatory amino acid and antagonists
US5262568A (en) 1990-03-02 1993-11-16 State Of Oregon Tri- and tetra-substituted guanidines and their use as excitatory amino acid antagonists
GB9005318D0 (en) * 1990-03-09 1990-05-02 Isis Innovation Antiarrhythmic agents
US5194430A (en) 1990-05-17 1993-03-16 Merrell Dow Pharmaceuticals Inc. Heterocyclic-nmda antagonists
DE69118539T2 (de) 1990-07-16 1996-09-19 Merrell Dow Pharmaceuticals Inc., Cincinnati, Ohio Exzitatorische Aminosäureantagonisten
ATE154010T1 (de) 1990-10-15 1997-06-15 Astra Ab 2-phenyl- und 2-thienyl-(2)-piperidinderivate mit neuroprotektiven eigenschaften
US5189054A (en) 1990-11-02 1993-02-23 Merrell Dow Pharmaceuticals Inc. 3-amidoindolyl derivatives and pharmaceutical compositions thereof
US5118675A (en) 1991-02-15 1992-06-02 American Home Products Corporation Quinoxaline phosphono-amino acids
US5606063A (en) 1991-02-27 1997-02-25 Merrell Pharmaceuticals Inc. NMDA antagonists
WO1992015931A2 (fr) * 1991-02-28 1992-09-17 Thomson-Lcd Registres a decalage redondants pour dispositifs de balayage
US5594007A (en) 1991-04-18 1997-01-14 Pfizer Inc. Method for treating spinal cord trauma with phenolic 2-piperidino-1-alkanols
DE4123106A1 (de) 1991-07-09 1993-01-14 Schering Ag Arzneimittel zur behandlung von entzugssymptomen
US5124319A (en) 1991-10-11 1992-06-23 American Home Products Corporation Benzimidazole phosphono-amino acids
US5710168A (en) 1991-10-23 1998-01-20 Pfizer Inc. 2-piperidino-1-alkanol derivatives as neuroprotective agents
US5318985A (en) 1991-12-20 1994-06-07 Merrell Dow Pharmaceuticals Inc. Potentiation of NMDA antagonists
US5441963A (en) 1991-12-20 1995-08-15 Merrell Dow Pharmaceuticals Potentiation of NMDA antagonists
DE4222826A1 (de) 1992-07-09 1994-01-13 Schering Ag Arzneimittel zur Verhinderung der Toleranzentwicklung während der Behandlung mit Benzodiazepin-Rezeptor-Bindenen Wirkstoffen
US5192751A (en) 1992-07-24 1993-03-09 Eli Lilly And Company Use of competitive NMDA receptor antagonists in the treatment of urinary incontinence
US5498610A (en) 1992-11-06 1996-03-12 Pfizer Inc. Neuroprotective indolone and related derivatives
CA2111138A1 (en) 1993-01-15 1994-07-16 Thierry Godel Octahydrophenanthrene derivatives
US5321012A (en) 1993-01-28 1994-06-14 Virginia Commonwealth University Medical College Inhibiting the development of tolerance to and/or dependence on a narcotic addictive substance
US5834479A (en) 1993-03-05 1998-11-10 Mayer; David J. Method and composition for alleviating pain
CA2115792C (en) 1993-03-05 2005-11-01 David J. Mayer Method for the treatment of pain
US5519048A (en) 1993-05-27 1996-05-21 Merrell Pharmaceuticals Inc. 3-(indol-3-yl)-propenoic acid derivatives and pharmaceutical compositions thereof
FR2707643B1 (fr) 1993-07-16 1995-08-11 Rhone Poulenc Rorer Sa Dérivés d'imidazo[1,2-a]pyrazine-4-one, leur préparation et les médicaments les contenant.
US5395822A (en) 1993-09-20 1995-03-07 Izumi; Yukitoshi Use of pyruvate to prevent neuronal degeneration associated with ischemia
IS4233A (is) 1993-12-22 1995-06-23 Astra Aktiebolag Misleit hringtengd efnasambönd
US5587384A (en) 1994-02-04 1996-12-24 The Johns Hopkins University Inhibitors of poly(ADP-ribose) synthetase and use thereof to treat NMDA neurotoxicity
FR2717805B1 (fr) 1994-03-28 1996-05-10 Rhone Poulenc Rorer Sa Dérivés de 5H-indeno[1,2-b]pyrazine-2,3-dione, leur préparation et les médicaments les contenant .
EP0685466A1 (de) 1994-06-02 1995-12-06 Ciba-Geigy Ag 3-Heteroaliphatyl- und 3-Hetero-(aryl)aliphatyl-2(1H)-chinolonderivate
DE69531691T2 (de) * 1994-08-04 2004-07-08 C & C Research Labs Neues amin-derivat, verfahren zur herstellung und dessen verwendung als anti-arrhythmisches mittel
GB9418443D0 (en) 1994-09-13 1994-11-02 Pfizer Ltd Therapeutic agents
PL181532B1 (pl) 1994-09-27 2001-08-31 Yamanouchi Pharma Co Ltd Pochodne 1,2,3,4-tetrahydrochinoksalinodionu PL PL PL PL PL PL PL PL PL
US5563157B1 (en) 1994-10-31 1999-02-02 Hoecst Marion Roussel Inc Heterocycle substituted propenoic acid derivatives and pharmaceutical compositions thereof
FR2726275B1 (fr) 1994-11-02 1996-12-06 Rhone Poulenc Rorer Sa Spiro heterocycle-imidazo(1,2-a)indeno(1,2-e)pyrazine)-4'- ones, leur preparation et les medicaments les contenants
US5605911A (en) 1995-01-31 1997-02-25 Washington University Use of alpha-2 adrenergic drugs to prevent adverse effects of NMDA receptor hypofunction (NRH)
PT828513E (pt) 1995-05-26 2004-05-31 Pfizer Combinacoes contendo antagonistas selectivos de nmda para o tratamento do parkinsonismo
WO1997003677A1 (en) 1995-07-24 1997-02-06 Trustees Of Boston University Inhibition of nmda receptor activity by pregnenolone sulfate derivatives
US5888996A (en) 1995-07-26 1999-03-30 Trustees Of Boston University Inhibition of NMDA receptor activity and modulation of glutamate-mediated synaptic activity
US5840731A (en) 1995-08-02 1998-11-24 Virginia Commonwealth University Pain-alleviating drug composition and method for alleviating pain
MY132385A (en) 1995-08-31 2007-10-31 Novartis Ag 2,3-dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives
AUPN605795A0 (en) 1995-10-19 1995-11-09 F.H. Faulding & Co. Limited Analgesic pharmaceutical composition
TW427978B (en) 1996-02-03 2001-04-01 Hoffmann La Roche Tetrahydroisoquinoline derivatives
WO1997032581A1 (en) * 1996-03-08 1997-09-12 F. Hoffmann-La Roche Ag Use of 4-phenyl-3,6-dihydro-2h-pyridyl derivatives as nmda receptor subtype blockers
US6025369A (en) 1996-05-03 2000-02-15 The Board Of Regents Of The University Nebraska N-methyl-D-aspartate (NMDA) receptor blockers for the prevention of atherosclerosis
TW498067B (en) 1996-07-19 2002-08-11 Hoffmann La Roche 4-hydroxy-piperidine derivatives
ES2241055T3 (es) 1996-08-23 2005-10-16 Endo Pharmaceuticals Inc Composicion que contiene un anticonvulsionante para tratar el dolor neuropatico.
US5902815A (en) 1996-09-03 1999-05-11 Washington University Use of 5HT-2A serotonin agonists to prevent adverse effects of NMDA receptor hypofunction
US5958919A (en) 1996-09-20 1999-09-28 Washington University Treatment of presymptomatic alzheimer's disease to prevent neuronal degeneration
US5919826A (en) 1996-10-24 1999-07-06 Algos Pharmaceutical Corporation Method of alleviating pain
ATE229004T1 (de) 1997-03-31 2002-12-15 Korea Res Inst Chem Tech Chinolinische sulfid-derivate als nmda rezeptor- antagonisten und verfahren zu ihrer herstellung
US6057373A (en) 1997-05-22 2000-05-02 Synchroneuron, Llc Methods of treating tardive dyskinesia and other movement disorders using NMDA receptor antagonists
US5866585A (en) 1997-05-22 1999-02-02 Synchroneuron, Llc Methods of treating tardive dyskinesia using NMDA receptor antagonists
IL133235A (en) 1997-06-30 2004-02-19 Merz Pharma Gmbh & Co Kgaa 1-amino-alkylcyclohexane nmda receptor antagonists and pharmaceutical compositions comprising them
US6071966A (en) 1997-06-30 2000-06-06 Merz + Co. Gmbh & Co. 1-amino-alkylcyclohexane NMDA receptor antagonists
US5783700A (en) 1997-07-03 1998-07-21 Nichols; Alfred C. Quinolic acid derivatives
BR9814867A (pt) 1997-10-24 2000-10-03 Warner Lambert Co Método para tratar discinesias relacionadas a doenças ou induzidas por drogas
US6177434B1 (en) 1997-12-16 2001-01-23 The United States Of America As Represented By The Secretary Of The Navy Prevention or reversal of sensorineural hearing loss (SNHL) through biologic mechanisms
US6294583B1 (en) 1998-01-13 2001-09-25 Synchroneuron, Llc Methods of treating tardive dyskinesia and other movement disorders
US6242456B1 (en) 1998-03-09 2001-06-05 Trustees Of Tufts College Treatment of stereotypic, self-injurious and compulsive behaviors in man and animals using antagonists of NMDA receptors
US6007841A (en) 1998-03-13 1999-12-28 Algos Pharmaceutical Corporation Analgesic composition and method for treating pain
US6197820B1 (en) 1998-04-06 2001-03-06 Uab Research Foundation Use of phenylglycine derivatives to decrease neuronal death caused by brain tumors and brain lesions
US6054451A (en) 1998-04-21 2000-04-25 Algos Pharmaceutical Corporation Analgesic composition and method for alleviating pain
PE20000728A1 (es) 1998-06-26 2000-08-21 Cocensys Inc Heterociclos 4-bencil piperidina alquilsulfoxido y su uso como antagonistas receptores subtipo-selectivo nmda
DE69931316D1 (de) * 1998-08-18 2006-06-22 Hoffmann La Roche Verwendung von Aryl-Cyclohexylamine Derivaten zur Herstellung von NMDA-Rezeptorblockern
US6200990B1 (en) 1998-12-21 2001-03-13 Alcon Laboratories, Inc. Neuroprotective agents having antioxidant and NMDA antagonist activity
DE60005517T2 (de) * 1999-06-29 2004-07-01 Neurosearch A/S Kaliumkanal-blockierende mittel
EP1070708B1 (en) 1999-07-21 2004-01-14 F. Hoffmann-La Roche Ag Triazole derivatives
GB9917822D0 (en) 1999-07-29 1999-09-29 Imperial College Nmda antagonist
US6339093B1 (en) 1999-10-08 2002-01-15 Hoffmann-La Roche Inc. Isoquinoline derivatives
US7375136B2 (en) * 2001-03-08 2008-05-20 Emory University pH-dependent NMDA receptor antagonists

Also Published As

Publication number Publication date
EP1436258A2 (en) 2004-07-14
US20040138502A1 (en) 2004-07-15
EP1436258A4 (en) 2005-03-23
JP2005506292A (ja) 2005-03-03
WO2002072542A3 (en) 2003-02-27
AU2002250256B2 (en) 2008-04-03
WO2002072542A2 (en) 2002-09-19
US20090023791A1 (en) 2009-01-22
US7375136B2 (en) 2008-05-20

Similar Documents

Publication Publication Date Title
US7375136B2 (en) pH-dependent NMDA receptor antagonists
AU2002250256A1 (en) pH-dependent NMDA receptor antagonists
JP2005506292A5 (cg-RX-API-DMAC7.html)
JP4568113B2 (ja) Ｍｃｈ調節作用を有するジアリール置換環状尿素誘導体
HUT56543A (en) Process for producing aromatic amines and pharmaceutical compositions comprising such compounds
CA2806664A1 (en) Arylsulfonamide derivatives, compositions, and methods of use
US12391664B2 (en) GluN2C/D subunit selective antagonists of the N-methyl-D-aspartate receptor
US12258308B2 (en) Benzene derivative
RU2655919C2 (ru) Производные аминоциклобутана, способ их получения и их применение в качестве лекарственных средств
JP2006515618A (ja) 置換アルキルアミドピペリジン類
AU2012317457A1 (en) Phenyl derivative
EP1753725B1 (fr) Derives de tetrahydroisoquinolilsulfonamides, leur preparation et leur utilisation en therapeutique
US7576129B2 (en) Carboxylic acid compounds
AU2009244536A1 (en) Alpha2B and alpha2C agonists
EP0426804B1 (en) 2-(2-hydroxy-3-phenoxypropylamino)-ethoxybenzene derivatives
AU2008201372A1 (en) Ph-Dependent NMDA receptor antagonists
CA2925846A1 (en) Chromene derivatives substituted by alkoxide as inhibitors of the tcr-nck interaction
WO2022129047A2 (en) Novel modulators of the nmda receptor
JP2002363163A (ja) ベンズアゼピン誘導体
IE66056B1 (en) Phenylacetonitrilealkylaminoalkyl-ortho-substituted aryl compounds as immunosuppressives
JPH0699306B2 (ja) 抗けいれん剤および抗てんかん剤としての３‐アリルオキシアゼチジンカルボキサミド
PT93725A (pt) Processo para a preparacao de derivados de benzopirano anti-hipertensivos
BR112021001853B1 (pt) Compostos derivado de benzeno, sais dos mesmos, uso dos mesmos para prevenir ou tratar neuropatia, composição farmacêutica e agentes profiláctico e/ou terapêutico e para a promoção da diferenciação de células de schwann
HK1212968B (en) Aminocyclobutane derivatives, method for preparing same and the use thereof as drugs
HK1240927A1 (en) Aminocyclobutane derivatives, method for preparing same and the use thereof as drugs

Legal Events

Date Code Title Description
EEER Examination request
FZDE Dead