EA201070077A1 - Антагонисты nmda-рецепторов с нейропротективным действием - Google Patents

Антагонисты nmda-рецепторов с нейропротективным действием

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Publication number
EA201070077A1
EA201070077A1 EA201070077A EA201070077A EA201070077A1 EA 201070077 A1 EA201070077 A1 EA 201070077A1 EA 201070077 A EA201070077 A EA 201070077A EA 201070077 A EA201070077 A EA 201070077A EA 201070077 A1 EA201070077 A1 EA 201070077A1
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Eurasian Patent Office
Prior art keywords
alkyl
bond
nrc
nrr
alkenyl
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EA201070077A
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English (en)
Inventor
Деннис К. Лиотта
Джеймс П. Снайдер
Стефен Ф. Трейнелис
Лоуренс Уилсон
Кара Мозли
Рэймонд Дж. Дингледин
Скотт Майерс
Йесим Алтас Тахировик
Original Assignee
Эмори Юниверсити
Ньюроп, Инк.
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Publication of EA201070077A1 publication Critical patent/EA201070077A1/ru

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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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

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  • Organic Chemistry (AREA)
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  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
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  • 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)
  • Quinoline Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)

Abstract

Предложены соединения, фармацевтические композиции и способы лечения или профилактики нарушений, связанных с активностью NMDA-рецепторов, включая невропатическую боль, инсульт, травму головного мозга, эпилепсию и связанные неврологические состояния или нейродегенерацию. Предложены соединения, имеющие общую формулу I, или их фармацевтически приемлемая соль, сложный эфир, пролекарство или производноегде каждый (L)-Arявляется замещенным или незамещенньм, моно- или бициклическим арилом или гетероарилом; W - связь, алкил или алкенил; Х - связь, NRили О, и каждый из Rи Rнезависимо представляет собой Н, алкил, алкенил или аралкил, или Rи Rвместе образуют 5-8-членное кольцо; R-Rвыбраны из определенных заместителей или карбонила; Y – связь, О, S, SO, SO, CH, NH, N(алкил) или NHC(=O); и Z представляет собой ОН, NRR, NRSO(алкил), NRC(О)NRR, NRC(О)О(алкил), NR-дигидротиазол или NR-дигидроимидазол, или где Z может сливаться с Arс образованием выбранных гетероциклов.
EA201070077A 2007-06-29 2008-06-30 Антагонисты nmda-рецепторов с нейропротективным действием EA201070077A1 (ru)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US94727607P 2007-06-29 2007-06-29
US94912007P 2007-07-11 2007-07-11
US98508207P 2007-11-02 2007-11-02
US12710508P 2008-05-09 2008-05-09
PCT/US2008/068843 WO2009006437A1 (en) 2007-06-29 2008-06-30 Nmda receptor antagonists for neuroprotection

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EA201070077A1 true EA201070077A1 (ru) 2010-08-30

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US (2) US8420680B2 (ru)
EP (1) EP2170334B1 (ru)
JP (1) JP2010532382A (ru)
KR (1) KR20100045983A (ru)
CN (3) CN103058957A (ru)
AU (1) AU2008272964A1 (ru)
BR (1) BRPI0813001A2 (ru)
CA (1) CA2693032A1 (ru)
CO (1) CO6290666A2 (ru)
EA (1) EA201070077A1 (ru)
MX (1) MX2009014216A (ru)
NZ (1) NZ582917A (ru)
SG (1) SG182964A1 (ru)
WO (1) WO2009006437A1 (ru)
ZA (1) ZA201001874B (ru)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090170867A1 (en) 2007-04-27 2009-07-02 Shionogi & Co., Ltd. Trpv1 antagonists including sulfonamide substituent and uses thereof
MX2010012186A (es) * 2008-05-09 2011-02-22 Univ Emory Antagonistas del receptor nmda para el tratamiento de transtornos neuropsiquitricos.
US7964605B2 (en) * 2008-05-29 2011-06-21 Sk Holdings Co., Ltd. Phenyl piperazine compounds, pharmaceutical composition comprising the same, and use thereof
IN2012DN06631A (ru) 2010-02-16 2015-10-23 Pfizer
RU2621708C2 (ru) 2011-06-22 2017-06-07 ПУРДЬЮ ФАРМА Эл. Пи. Антагонисты trpv1, включающие дигидроксигруппу в качестве заместителя, и их применение
EP2760843B1 (en) 2011-09-26 2016-03-02 Bristol-Myers Squibb Company Selective nr2b antagonists
EP2760856B1 (en) 2011-09-30 2016-09-14 Bristol-Myers Squibb Company Selective nr2b antagonists
JP6345651B2 (ja) * 2012-05-09 2018-06-20 サノビオン ファーマシューティカルズ インクＳｕｎｏｖｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃ． ヘテロアリール化合物及びその使用方法
WO2014210456A1 (en) 2013-06-28 2014-12-31 Emory University Pyrazoline dihydroquinolones, pharmaceutical compositions, and uses
KR102146360B1 (ko) * 2013-11-05 2020-08-20 더 리전트 오브 더 유니버시티 오브 캘리포니아 하이브리드 탄소 나노튜브 및 그래핀 나노구조
US9340504B2 (en) * 2013-11-21 2016-05-17 Purdue Pharma L.P. Pyridine and piperidine derivatives as novel sodium channel blockers
US9221796B2 (en) * 2014-01-09 2015-12-29 Bristol-Myers Squibb Company Selective NR2B antagonists
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
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
WO2016179157A1 (en) 2015-05-05 2016-11-10 Carafe Drug Innovation, Llc Substituted 5-hydroxyoxindoles and their use as analgesics and fever reducers
US10344020B2 (en) 2015-10-14 2019-07-09 Bristol-Myers Squibb Company Selective NR2B antagonists
WO2017066368A1 (en) 2015-10-14 2017-04-20 Bristol-Myers Squibb Company Selective nr2b antagonists
US10583171B2 (en) 2015-11-30 2020-03-10 INSERM (Institut National de la Santé et de la Recherche Médicale) NMDAR antagonists for the treatment of diseases associated with angiogenesis
EP3672934A4 (en) 2017-08-21 2021-05-05 Plex Pharmaceuticals, Inc. DOUBLE ACTING FKBP12 AND FKBP52 INHIBITORS
EP4417596A1 (en) * 2017-11-06 2024-08-21 Acelot, Inc. Small molecule drugs and related methods for treatment of diseases related to a 42 oligomer formation
WO2019157014A1 (en) 2018-02-06 2019-08-15 Emory University N-methyl-d-aspartic acid receptor modulators
WO2019191424A1 (en) 2018-03-28 2019-10-03 Emory University Glun2c/d subunit selective antagonists of the n-methyl-d-aspartate receptor
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
JP2024533182A (ja) 2021-09-02 2024-09-12 エモリー ユニバーシティー 酸性ｐＨで増強された効力を有するＮ－メチル－Ｄ－アスパラギン酸受容体のＧｌｕＮ２Ｂサブユニット選択的アンタゴニスト
CN113861064B (zh) * 2021-10-14 2024-05-10 南京医科大学 一类神经保护剂及其药物用途
EP4493551A1 (en) 2022-03-14 2025-01-22 Slap Pharmaceuticals LLC Multicyclic compounds
GB202315614D0 (en) * 2023-10-12 2023-11-29 Veriulence Ltd Antibacterial

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
JPS579769A (en) * 1980-06-23 1982-01-19 Otsuka Pharmaceut Co Ltd 2-benzimidazolinone derivative
DE3023369A1 (de) * 1980-06-23 1982-01-14 Boehringer Mannheim Gmbh, 6800 Mannheim Aryloxypropanolamine, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel
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
GB8610668D0 (en) * 1986-05-01 1986-06-04 Pfizer Ltd Anti-arrhythmia agents
EG18188A (en) 1986-05-01 1992-09-30 Pfizer Ltd Process for preparation anti-arhythmia 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
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
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
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
US4994459A (en) * 1989-12-11 1991-02-19 American Home Products Corporation Aryloxypropane substituted piperazine derivatives with antiarrhythmic and antifibrillatory activity
SG73414A1 (en) 1990-03-02 2000-06-20 Oregon State Tri-and tetra-substituted guanidines and their use as excitatory amino acid antagonists
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
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
EP0539503B1 (en) 1990-07-16 1996-04-03 Merrell Dow Pharmaceuticals Inc. Excitatory amino acid antagonists
WO1992006957A1 (en) 1990-10-15 1992-04-30 Fisons Corporation 2-phenyl-and 2-thienyl-(2)-piperidine derivatives having neuroprotective properties
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 (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
CA2115792C (en) 1993-03-05 2005-11-01 David J. Mayer Method for the treatment of pain
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 (de) 1994-06-02 1995-12-06 Ciba-Geigy Ag 3-Heteroaliphatyl- und 3-Hetero-(aryl)aliphatyl-2(1H)-chinolonderivate
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
ES2206508T3 (es) * 1994-08-04 2004-05-16 C & C RESEARCH LABS. Nuevo derivado aminado, procedimiento de obtencion de este derivado y su utilizacion como antiarritmico.
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
FI974323A0 (fi) 1995-05-26 1997-11-25 Pfizer Selektiivisiä NMDA-antagonisteja sisältäviä yhdistelmiä parkinsonismin hoitoa varten
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
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
CA2278660A1 (en) * 1997-01-30 1998-08-06 Kazumi Ogata Hydroquinone derivatives
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
US6071966A (en) 1997-06-30 2000-06-06 Merz + Co. Gmbh & Co. 1-amino-alkylcyclohexane NMDA receptor antagonists
ATE240936T1 (de) 1997-06-30 2003-06-15 Merz & Co Gmbh & Co 1-amino-alkylcyclohexane als nmda-rezeptor- antagonisten
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
WO1999045906A1 (en) 1998-03-09 1999-09-16 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
US6184236B1 (en) 1998-08-18 2001-02-06 Hoffmann-La Roche Inc. Method of treating a neurodegenerative disease by administering an aryl-cyclohexylamine derivative
US6200990B1 (en) 1998-12-21 2001-03-13 Alcon Laboratories, Inc. Neuroprotective agents having antioxidant and NMDA antagonist activity
WO2001002406A1 (en) 1999-06-29 2001-01-11 Neurosearch A/S Potassium channel blocking agents
ATE257827T1 (de) 1999-07-21 2004-01-15 Hoffmann La Roche 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
AU2001296994A1 (en) * 2000-10-06 2002-04-15 Regents Of The University Of California Nmda receptor channel blocker with neuroprotective activity
JP2005506292A (ja) * 2001-03-08 2005-03-03 エモリー　ユニバーシティ ｐＨに依存するＮＭＤＡレセプターアンタゴニスト
DE10248925A1 (de) * 2002-10-15 2004-04-29 Proteosys Ag Neue Verbindungen mit dopaminerger und/oder serotoninerger Aktivität
BRPI0419067A (pt) * 2003-05-16 2007-12-11 Pfizer Prod Inc método para aumento da cognição utilizando ziprasidona
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
JP5015779B2 (ja) * 2004-08-23 2012-08-29 エモリー・ユニバーシテイ インビボ治療のためのｐＨ依存性化合物の改良選択法
WO2006058753A1 (en) * 2004-12-02 2006-06-08 Abbott Gmbh & Co. Kg Triazole compounds suitable for treating disorders that respond to modulaiont of the dopamine d3 receptor
KR101351209B1 (ko) * 2004-12-03 2014-02-06 머크 샤프 앤드 돔 코포레이션 Ｃｂ1 길항제로서 치환된 피페라진
AR055203A1 (es) * 2005-08-31 2007-08-08 Otsuka Pharma Co Ltd Derivados de benzotiofeno con propiedades antipsicoticas
GB0521320D0 (en) * 2005-10-20 2005-11-30 Univ Reading The Beta adrenergic receptor pharmacophore
EP2520567A3 (en) * 2006-02-23 2012-12-12 Shionogi & Co., Ltd. Nitrogen-containing heterocycle derivatives substituted with cyclic group
EP2651494B1 (en) 2010-12-13 2017-02-15 Pacesetter, Inc. Delivery catheter

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