CA2693032A1 - Antagonistes des recepteurs nmda pour la neuroprotection - Google Patents

Antagonistes des recepteurs nmda pour la neuroprotection Download PDF

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Publication number
CA2693032A1
CA2693032A1 CA 2693032 CA2693032A CA2693032A1 CA 2693032 A1 CA2693032 A1 CA 2693032A1 CA 2693032 CA2693032 CA 2693032 CA 2693032 A CA2693032 A CA 2693032A CA 2693032 A1 CA2693032 A1 CA 2693032A1
Authority
CA
Canada
Prior art keywords
alkyl
compound
phenyl
piperazin
hydroxy
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
CA 2693032
Other languages
English (en)
Inventor
Dennis C. Liotta
James P. Snyder
Stephen F. Traynelis
Lawrence Wilson
Cara Mosley
Raymond J. Dingledine
Scott Myers
Yesim Altas Tahirovic
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
NeurOp Inc
Original Assignee
Emory University
Dennis C. Liotta
James P. Snyder
Stephen F. Traynelis
Lawrence Wilson
Cara Mosley
Raymond J. Dingledine
Scott Myers
Yesim Altas Tahirovic
Neurop, 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
Application filed by Emory University, Dennis C. Liotta, James P. Snyder, Stephen F. Traynelis, Lawrence Wilson, Cara Mosley, Raymond J. Dingledine, Scott Myers, Yesim Altas Tahirovic, Neurop, Inc. filed Critical Emory University
Publication of CA2693032A1 publication Critical patent/CA2693032A1/fr
Abandoned legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/32—Oxygen atoms
    • C07D209/34—Oxygen atoms in position 2
    • 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
    • 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
    • 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
    • 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
    • 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
    • C07C217/06—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 only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted
    • C07C217/14—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 only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring
    • C07C217/18—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 only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being 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
    • C07C217/20—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 only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C235/18—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides
    • C07C235/20—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D211/40—Oxygen atoms
    • C07D211/44—Oxygen atoms attached in position 4
    • C07D211/52—Oxygen atoms attached in position 4 having an aryl radical as the second substituent in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole 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
    • C07D233/30—Oxygen or sulfur atoms
    • C07D233/32—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole 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
    • C07D233/30—Oxygen or sulfur atoms
    • C07D233/32—One oxygen atom
    • C07D233/34—Ethylene-urea
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/26—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58—Benzoxazoles; Hydrogenated benzoxazoles 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 in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/088—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
CA 2693032 2007-06-29 2008-06-30 Antagonistes des recepteurs nmda pour la neuroprotection Abandoned CA2693032A1 (fr)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US94727607P 2007-06-29 2007-06-29
US60/947,276 2007-06-29
US94912007P 2007-07-11 2007-07-11
US60/949,120 2007-07-11
US98508207P 2007-11-02 2007-11-02
US60/985,082 2007-11-02
US12710508P 2008-05-09 2008-05-09
US61/127,105 2008-05-09
PCT/US2008/068843 WO2009006437A1 (fr) 2007-06-29 2008-06-30 Antagonistes des récepteurs nmda pour la neuroprotection

Publications (1)

Publication Number Publication Date
CA2693032A1 true CA2693032A1 (fr) 2009-01-08

Family

ID=40226514

Family Applications (1)

Application Number Title Priority Date Filing Date
CA 2693032 Abandoned CA2693032A1 (fr) 2007-06-29 2008-06-30 Antagonistes des recepteurs nmda pour la neuroprotection

Country Status (16)

Country Link
US (2) US8420680B2 (fr)
EP (1) EP2170334B1 (fr)
JP (1) JP2010532382A (fr)
KR (1) KR20100045983A (fr)
CN (3) CN101815518B (fr)
AU (1) AU2008272964A1 (fr)
BR (1) BRPI0813001A2 (fr)
CA (1) CA2693032A1 (fr)
CO (1) CO6290666A2 (fr)
EA (1) EA201070077A1 (fr)
HK (1) HK1146902A1 (fr)
MX (1) MX2009014216A (fr)
NZ (1) NZ582917A (fr)
SG (1) SG182964A1 (fr)
WO (1) WO2009006437A1 (fr)
ZA (1) ZA201001874B (fr)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2833209C (fr) 2007-04-27 2016-06-28 Purdue Pharma L.P. Composes de piperidine et piperazine en tant qu'antagonistes de trpv1
EP2296658A4 (fr) * 2008-05-09 2014-01-15 Univ Emory Antagonistes des récepteurs nmda utilisables pour le traitement de troubles neuropsychiatriques
US7964605B2 (en) * 2008-05-29 2011-06-21 Sk Holdings Co., Ltd. Phenyl piperazine compounds, pharmaceutical composition comprising the same, and use thereof
IN2012DN06631A (fr) 2010-02-16 2015-10-23 Pfizer
UA113288C2 (xx) 2011-06-22 2017-01-10 Trpv1 антагоністи, що містять дигідроксизамісник, і їх застосування
US8841301B2 (en) 2011-09-26 2014-09-23 Bristol-Myers Squibb Company Selective NR2B antagonists
WO2013049119A1 (fr) 2011-09-30 2013-04-04 Bristol-Myers Squibb Company Antagonistes sélectifs du nr2b
US9951088B2 (en) * 2012-05-09 2018-04-24 Sunovion Pharmaceuticals Inc. D2 receptor modulators and methods of use thereof in the treatment of diseases and disorders
US20160368897A1 (en) 2013-06-28 2016-12-22 Emory University Pyrazoline Dihydroquinolones, Pharmaceutical Compositions, and Uses
US20160293956A1 (en) * 2013-11-05 2016-10-06 The Regents Of The University Of California Hybrid carbon nanotube and graphene nanostructures
US9340504B2 (en) * 2013-11-21 2016-05-17 Purdue Pharma L.P. Pyridine and piperidine derivatives as novel sodium channel blockers
US9187506B2 (en) 2014-01-09 2015-11-17 Bristol-Myers Squibb Company (R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one and its prodrugs for the treatment of psychiatric disorders
US9221796B2 (en) * 2014-01-09 2015-12-29 Bristol-Myers Squibb Company Selective NR2B antagonists
CN105085433B (zh) * 2014-05-19 2019-06-25 中国科学院上海药物研究所 取代酰胺苯酚类化合物及其制备方法、药物组合物和用途
US10537552B2 (en) 2015-05-05 2020-01-21 Carafe Drug Innovation, Llc Substituted 5-hydroxyoxindoles and their use as analgesics and fever reducers
WO2017066368A1 (fr) 2015-10-14 2017-04-20 Bristol-Myers Squibb Company Antagonistes sélectifs de nr2b
CA3001890A1 (fr) 2015-10-14 2017-04-20 Bristol-Myers Squibb Company Antagonistes selectifs de nr2b
EP3383429B1 (fr) 2015-11-30 2020-10-14 INSERM - Institut National de la Santé et de la Recherche Médicale Antagonistes du recepteur au nmda pour le traitement de l'angiogenèse tumorale
JP2021509398A (ja) * 2017-08-21 2021-03-25 プレックス ファーマスーティカルズ，インク 二重作用ｆｋｂｐ１２およびｆｋｂｐ５２阻害剤
WO2019157014A1 (fr) 2018-02-06 2019-08-15 Emory University Modulateurs des récepteurs de l'acide n-méthyl-d-aspartique
CN114539129B (zh) * 2020-11-18 2023-06-09 上海中医药大学附属龙华医院 烯丙胺类双功能化合物及其用途
CA3230601A1 (fr) * 2021-09-02 2023-03-09 Dennis Liotta Antagonistes selectifs de la sous-unite glun2b des recepteurs du n-methyl-d-aspartate presentant une puissance amelioree a ph acide

Family Cites Families (117)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1325876A (en) * 1969-08-15 1973-08-08 Pfizer Ltd Piperazine derivatives their preparation and pharmaceutical compositions containing them
GB1361863A (en) * 1972-09-25 1974-07-30 Pfizer Ltd Piperazine derivatives their preparation and pharmaceutical compositions containing them
US4210753A (en) * 1976-03-17 1980-07-01 Otsuka Pharmaceutical Co., Ltd. Carbostyril compounds
JPS56164186A (en) * 1980-05-21 1981-12-17 Otsuka Pharmaceut Co Ltd Carbostyril derivative
DE3023369A1 (de) * 1980-06-23 1982-01-14 Boehringer Mannheim Gmbh, 6800 Mannheim Aryloxypropanolamine, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel
JPS579769A (en) * 1980-06-23 1982-01-19 Otsuka Pharmaceut Co Ltd 2-benzimidazolinone derivative
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
DE3442570A1 (de) * 1984-11-22 1986-05-22 Hoechst Ag, 6230 Frankfurt Neue substituierte phenylpiperazinderivate, verfahren zu deren herstellung und die verwendung substituierter phenylpiperazinderivate als aggressionshemmer fuer tiere
EG18188A (en) * 1986-05-01 1992-09-30 Pfizer Ltd Process for preparation anti-arhythmia agents
GB8610668D0 (en) * 1986-05-01 1986-06-04 Pfizer Ltd Anti-arrhythmia agents
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
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
US5179085A (en) * 1989-03-15 1993-01-12 Warner-Lambert Company N-substituted α-amino acids and derivatives thereof having pharmaceutical activity
US4924008A (en) * 1989-05-04 1990-05-08 American Home Products Corporation Benzobicycloalkane derivatives as anticonvulsant neuroprotective agents
US4957909A (en) * 1989-05-04 1990-09-18 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
US5095009A (en) * 1990-04-11 1992-03-10 Merrell Dow Pharmaceuticals Inc. NMDA 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
EP0424179A3 (en) 1989-10-20 1991-12-27 John William Olney Use of combined excitatory amino acid and cholinergic antagonists to prevent neurological deterioration
US5629307A (en) * 1989-10-20 1997-05-13 Olney; John W. Use of ibogaine in reducing excitotoxic brain damage
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
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
US4994459A (en) * 1989-12-11 1991-02-19 American Home Products Corporation Aryloxypropane substituted piperazine derivatives with antiarrhythmic and antifibrillatory activity
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
US5262568A (en) 1990-03-02 1993-11-16 State Of Oregon Tri- and tetra-substituted guanidines and their use as excitatory amino acid antagonists
DE69133065T2 (de) * 1990-03-02 2003-02-27 Oregon State Tri- und tetra-substituierte guanidine und deren verwendung als antagonisten von exzitatorischen aminosäuren
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
ES2088011T3 (es) * 1990-07-16 1996-08-01 Merrell Pharma Inc Antagonistas de aminoacidos excitadores.
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
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 (fr) * 1993-01-15 1994-07-16 Thierry Godel Derives de l'octahydrophenanthrene
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
CA2115792C (fr) * 1993-03-05 2005-11-01 David J. Mayer Methode de traitement de la douleur
US5834479A (en) 1993-03-05 1998-11-10 Mayer; David J. Method and composition for alleviating 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 (fr) * 1994-06-02 1995-12-06 Ciba-Geigy Ag Dérivés de 3-hétéroaliphatyle- et 3-(hétéro)-(aryle)-aliphatyle-2(1H)-quinolone
DE4422517A1 (de) * 1994-06-28 1996-01-04 Dresden Arzneimittel Neue (2-(3,4-Dimethoxy-phenyl)-ethyl)-(2-phenoxy-ethyl)-amine, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
CN1134410C (zh) * 1994-08-04 2004-01-14 C&C新药研究所 胺衍生物,制备它们的方法和它们作为抗心律失常药的应用
KR960007560A (ko) * 1994-08-16 1996-03-22 김정규 신규한 아민 유도체, 그의 제조방법 및 항부정맥제로서의 용도
GB9418443D0 (en) * 1994-09-13 1994-11-02 Pfizer Ltd Therapeutic agents
US6096743A (en) * 1994-09-27 2000-08-01 Yamanouchi Pharmaceuticals Co., Ltd. 1,2,3,4-tetrahydroquinoxalinedione derivative
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
JPH08143557A (ja) * 1994-11-24 1996-06-04 Toyobo Co Ltd 新規なフェニルピペラジン誘導体、その塩及びその溶媒和物
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)
US5768130A (en) * 1995-05-15 1998-06-16 Lsi Logic Corporation Method of calculating macrocell power and delay values
RU2176145C2 (ru) * 1995-05-26 2001-11-27 Пфайзер Инк. Синергическое лечение паркинсонизма
WO1997003677A1 (fr) * 1995-07-24 1997-02-06 Trustees Of Boston University Inhibition de l'activite des recepteurs du n-methyl-d-aspartate au moyen de derives de sulfate de pregnenolone
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
AU717140B2 (en) * 1996-03-08 2000-03-16 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
AU4078897A (en) * 1996-08-23 1998-03-06 Algos Pharmaceutical Corporation Anticonvulsant containing composition for treating neuropathic pain
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
EP0972766A4 (fr) * 1997-01-30 2000-05-03 Senju Pharma Co Derives d'hydroquinone
EP0869122B1 (fr) 1997-03-31 2002-12-04 Korea Research Institute Of Chemical Technology Dérivés de sulfures quinoliniques antagonistes des récepteurs NMDA et procédé pour leur préparation
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
US6071966A (en) * 1997-06-30 2000-06-06 Merz + Co. Gmbh & Co. 1-amino-alkylcyclohexane NMDA receptor antagonists
CA2292558C (fr) * 1997-06-30 2006-09-19 Merz + Co. Gmbh & Co. 1-aminoalkylcyclohexanes antagonistes du recepteur de nmda
US5783700A (en) * 1997-07-03 1998-07-21 Nichols; Alfred C. Quinolic acid derivatives
IL125658A0 (en) * 1997-08-18 1999-04-11 Hoffmann La Roche Ccr-3 receptor antagonists
NZ502785A (en) * 1997-10-24 2003-03-28 Warner Lambert Co Use of NR1A/2B site-selective NMDA receptor antagonist compounds for treating disease-related or drug-induced dyskinesias
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
AU2981099A (en) * 1998-03-09 1999-09-27 Trustees Of Tufts College Treatment of compulsive behaviours in man and animals
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
ATE326219T1 (de) * 1998-08-18 2006-06-15 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
WO2001002406A1 (fr) 1999-06-29 2001-01-11 Neurosearch A/S Agents bloquant les canaux potassiques
DE60007697T2 (de) * 1999-07-21 2004-12-09 F. Hoffmann-La Roche Ag Triazolderivate
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
WO2002028814A2 (fr) * 2000-10-06 2002-04-11 Regents Of The University Of California Bloqueur de canal de recepteur nmda a activite neuroprotectrice
US7375136B2 (en) * 2001-03-08 2008-05-20 Emory University pH-dependent NMDA receptor antagonists
DE10248925A1 (de) * 2002-10-15 2004-04-29 Proteosys Ag Neue Verbindungen mit dopaminerger und/oder serotoninerger Aktivität
WO2004100956A1 (fr) * 2003-05-16 2004-11-25 Pfizer Products Inc. Procede pour ameliorer les fonctions cognitives en administrant du ziprasidone
HUP0401526A2 (en) * 2004-07-29 2006-04-28 Richter Gedeon Vegyeszet Aryloxy acetic acid amide derivatives, pharmaceutical compositions comprising thereof, methods for their preparation and their use
CA2578217A1 (fr) * 2004-08-23 2006-03-02 Emory University Selection amelioree de composes dependant du ph pour therapie in vivo
CA2588457A1 (fr) * 2004-12-02 2006-06-08 Abbott Gmbh & Co. Kg Composes de type triazole adaptes au traitement de troubles dependant de la regulation du recepteur de dopamine d3
NZ555320A (en) 2004-12-03 2010-11-26 Schering Corp Substituted piperazines as CB1 antagonists
TWI329641B (en) * 2005-08-31 2010-09-01 Otsuka Pharma Co Ltd (benzo[b]thiophen-4-yl)piperazine compounds, pharmaceutical compositions comprising the same, uses of the same and processes for preparing the same
GB0521320D0 (en) * 2005-10-20 2005-11-30 Univ Reading The Beta adrenergic receptor pharmacophore
EP1988077A4 (fr) 2006-02-23 2009-09-02 Shionogi & Co Derives heterocycliques azotes substitues par des groupes cycliques
CN103429296A (zh) 2010-12-13 2013-12-04 内诺斯蒂姆股份有限公司 递送导管系统和方法

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CN103058957A (zh) 2013-04-24
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US20090253710A1 (en) 2009-10-08
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US9079852B2 (en) 2015-07-14
ZA201001874B (en) 2010-11-24
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