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

Антагонисты nmda-рецепторов с нейропротективным действием

Info

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
Authority
EA
Eurasian Patent Office
Prior art keywords
alkyl
bond
nrc
nrr
alkenyl
Prior art date
Application number
EA201070077A
Other languages
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.
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 Эмори Юниверсити, Ньюроп, Инк. filed Critical Эмори Юниверсити
Publication of EA201070077A1 publication Critical patent/EA201070077A1/ru

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; 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
    • C07D209/32Oxygen atoms
    • C07D209/34Oxygen atoms in position 2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/02Compounds 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
    • C07C217/04Compounds 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
    • C07C217/06Compounds 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
    • C07C217/14Compounds 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
    • C07C217/18Compounds 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
    • C07C217/20Compounds 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02Carboxylic 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
    • C07C235/04Carboxylic 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
    • C07C235/18Carboxylic 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
    • C07C235/20Carboxylic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides 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
    • C07C311/01Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/08Sulfonamides 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/36Heterocyclic 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
    • C07D211/40Oxygen atoms
    • C07D211/44Oxygen atoms attached in position 4
    • C07D211/52Oxygen atoms attached in position 4 having an aryl radical as the second substituent in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/72Nitrogen atoms
    • C07D213/74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/20Oxygen atoms
    • C07D215/22Oxygen atoms attached in position 2 or 4
    • C07D215/227Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04Heterocyclic 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
    • C07D233/28Heterocyclic 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
    • C07D233/30Oxygen or sulfur atoms
    • C07D233/32One oxygen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04Heterocyclic 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
    • C07D233/28Heterocyclic 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
    • C07D233/30Oxygen or sulfur atoms
    • C07D233/32One oxygen atom
    • C07D233/34Ethylene-urea
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24Benzimidazoles; 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
    • C07D235/26Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58Benzoxazoles; 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/04Heterocyclic 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
    • C07D295/08Heterocyclic 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
    • C07D295/084Heterocyclic 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
    • C07D295/088Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (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)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Quinoline Compounds (AREA)
  • Hydrogenated Pyridines (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

Publications (1)

Publication Number Publication Date
EA201070077A1 true EA201070077A1 (ru) 2010-08-30

Family

ID=40226514

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201070077A EA201070077A1 (ru) 2007-06-29 2008-06-30 Антагонисты nmda-рецепторов с нейропротективным действием

Country Status (15)

Country Link
US (2) US8420680B2 (ru)
EP (1) EP2170334B1 (ru)
JP (1) JP2010532382A (ru)
KR (1) KR20100045983A (ru)
CN (3) CN103497114A (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
CA2685266C (en) 2007-04-27 2014-01-28 Purdue Pharma L.P. Trpv1 antagonists and uses thereof for the treatment of prevention of pain, ui and ulcer, ibd, or ibs in an animal
JP2011520815A (ja) * 2008-05-09 2011-07-21 エモリー・ユニバーシテイ 精神神経障害治療のためのnmda受容体拮抗薬
US7964605B2 (en) * 2008-05-29 2011-06-21 Sk Holdings Co., Ltd. Phenyl piperazine compounds, pharmaceutical composition comprising the same, and use thereof
CA2788656A1 (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
PE20141531A1 (es) 2011-06-22 2014-10-23 Purdue Pharma Lp Antagonistas de trpv1 que incluyen sustituyentes dihidroxi y sus usos
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
JP6457510B2 (ja) * 2013-11-05 2019-01-23 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア カーボンナノチューブとグラフェンの複合的ナノ構造
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
US10537552B2 (en) 2015-05-05 2020-01-21 Carafe Drug Innovation, Llc Substituted 5-hydroxyoxindoles and their use as analgesics and fever reducers
BR112018007181A2 (pt) 2015-10-14 2018-10-16 Bristol-Myers Squibb Company antagonistas de nr2b seletivos
KR20180063306A (ko) 2015-10-14 2018-06-11 브리스톨-마이어스 스큅 컴퍼니 선택적 nr2b 길항제
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
US12065407B2 (en) 2017-08-21 2024-08-20 Plex Pharmaceuticals, Inc. Dual acting FKBP12 and FKBP52 inhibitors
EP4417596B1 (en) 2017-11-06 2026-04-29 Acelot, Inc. Small molecule drugs and related methods for treatment of diseases related to a-beta-42 oligomer formation
WO2019157014A1 (en) 2018-02-06 2019-08-15 Emory University N-methyl-d-aspartic acid receptor modulators
US11981652B2 (en) 2018-03-28 2024-05-14 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
CA3230601A1 (en) * 2021-09-02 2023-03-09 Dennis Liotta Glun2b-subunit selective antagonists of the n-methyl-d-aspartate receptors with enhanced potency at acidic ph
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
AU2023235233A1 (en) 2022-03-14 2024-09-12 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
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
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
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
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
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
US5629307A (en) 1989-10-20 1997-05-13 Olney; John W. Use of ibogaine in reducing excitotoxic brain damage
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
US5474990A (en) 1989-10-20 1995-12-12 Olney; John W. Barbiturates as safening agents in conjunction with 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
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
EP0517852B1 (en) 1990-03-02 2002-07-10 STATE OF OREGON, acting by and through THE OREGON STATE BOARD OF HIGHER EDUCATION, acting for and on behalf of 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
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
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
KR0178469B1 (ko) 1990-07-16 1999-03-20 메이나드 알. 존슨 흥분성 아미노산 길항제
DE69126438T2 (de) 1990-10-15 1997-10-02 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
US5441963A (en) 1991-12-20 1995-08-15 Merrell Dow Pharmaceuticals Potentiation of NMDA antagonists
US5318985A (en) 1991-12-20 1994-06-07 Merrell Dow Pharmaceuticals Inc. 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
AU2630095A (en) 1994-08-04 1996-03-04 C & C Research Laboratories Novel amine derivative, process for producing the same, and use thereof as antiarrhythmic
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
DK0784054T3 (da) 1994-09-27 2002-03-25 Yamanouchi Pharma Co Ltd 1,2,3,4-tetrahydroquinoxalinderivater og deres anvendelse som glutamatreceptorantagonister
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
ATE258067T1 (de) 1995-05-26 2004-02-15 Pfizer Kombinationspräparat zur behandlung der parkinsonschen krankheit, das selektive nmda- antagonisten enthält
US5888996A (en) 1995-07-26 1999-03-30 Trustees Of Boston University Inhibition of NMDA receptor activity and modulation of glutamate-mediated synaptic activity
EP0840612A1 (en) 1995-07-24 1998-05-13 Trustees Of Boston University Inhibition of nmda receptor activity by pregnenolone sulfate derivatives
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
CN1131031C (zh) 1996-03-08 2003-12-17 弗·哈夫曼-拉罗切有限公司 作为nmda受体亚型阻断剂的4-苯基3,6-二氢-2h-吡啶基衍生物的应用
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
WO1998007447A1 (en) 1996-08-23 1998-02-26 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
US6358515B2 (en) * 1997-01-30 2002-03-19 Senju Pharmaceutical Co., Ltd. Hydroquinone derivatives
DE69809827D1 (de) 1997-03-31 2003-01-16 Korea Res Inst Chem Tech Chinolinische Sulfid-Derivate als NMDA Rezeptor-Antagonisten und Verfahren zu ihrer Herstellung
US5866585A (en) 1997-05-22 1999-02-02 Synchroneuron, Llc Methods of treating tardive dyskinesia using NMDA receptor antagonists
US6057373A (en) 1997-05-22 2000-05-02 Synchroneuron, Llc Methods of treating tardive dyskinesia and other movement disorders using NMDA receptor antagonists
US6071966A (en) 1997-06-30 2000-06-06 Merz + Co. Gmbh & Co. 1-amino-alkylcyclohexane NMDA receptor antagonists
KR100630506B1 (ko) 1997-06-30 2006-09-29 메르츠 파마 게엠베하 운트 코. 카가아 Nmda 수용체 길항물질로서의 1-아미노-알킬시클로헥산 화합물, 이를 함유하는 제약학적 조성물 및 이것으로 치료하는 방법
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
EP1024799A1 (en) 1997-10-24 2000-08-09 Warner-Lambert Company Method 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
EP1061924A1 (en) 1998-03-09 2000-12-27 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
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
AU5390900A (en) 1999-06-29 2001-01-22 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
US7022882B2 (en) * 2000-10-06 2006-04-04 The Regents Of The University Of California NMDA receptor channel blocker with neuroprotective activity
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
MXPA05012325A (es) * 2003-05-16 2006-01-30 Pfizer Prod Inc Procedimiento para potenciar la cognicion usando zipirasidona.
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
WO2006023957A1 (en) 2004-08-23 2006-03-02 Emory University Improved selection of-ph dependent compounds for in vivo therapy
BRPI0518823A2 (pt) * 2004-12-02 2008-12-09 Abbott Gmbh & Co Kg compostos de triazol adequados para o tratamento de transtornos que respondam À modulaÇço do receptor d3 da dopamina
CN102633730A (zh) * 2004-12-03 2012-08-15 先灵公司 作为cb1拮抗剂的取代哌嗪
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

Also Published As

Publication number Publication date
MX2009014216A (es) 2010-07-05
US8420680B2 (en) 2013-04-16
HK1146902A1 (en) 2011-07-22
EP2170334B1 (en) 2021-03-17
CO6290666A2 (es) 2011-06-20
EP2170334A1 (en) 2010-04-07
JP2010532382A (ja) 2010-10-07
CN103497114A (zh) 2014-01-08
BRPI0813001A2 (pt) 2019-09-24
AU2008272964A1 (en) 2009-01-08
ZA201001874B (en) 2010-11-24
CA2693032A1 (en) 2009-01-08
KR20100045983A (ko) 2010-05-04
US20090253710A1 (en) 2009-10-08
US9079852B2 (en) 2015-07-14
CN103058957A (zh) 2013-04-24
EP2170334A4 (en) 2010-09-29
SG182964A1 (en) 2012-08-30
CN101815518B (zh) 2013-01-09
CN101815518A (zh) 2010-08-25
NZ582917A (en) 2013-01-25
WO2009006437A1 (en) 2009-01-08
US20140031363A1 (en) 2014-01-30

Similar Documents

Publication Publication Date Title
EA201070077A1 (ru) Антагонисты nmda-рецепторов с нейропротективным действием
ZA202409114B (en) MODULATORS OF THR-ß AND METHODS OF USE THEREOF
SA518391518B1 (ar) مشتقات n-] 2-(1- بنزيل ببريدين-4-يل) إيثيل[ -4-(بيرازين-2-يل)-ببرازين-1- كربوكساميد ومركبات متصلة بها كمضادات مستقبلة المسكارين 4 (m4) لمعالجة أمراض عصبية
AR046297A1 (es) Inhibidores de la dpp - iv metodos para prepararlos y composiciones farmaceuticas que los contienen como agente activo
EA200870117A1 (ru) Азаиндоловые ингибиторы аурора-киназ
JP4792974B2 (ja) アゼチジン環化合物およびその医薬
MY139399A (en) Crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist
EA200701745A1 (ru) Циклопропанкарбоксамидные производные
WO2007084914A3 (en) Phenoxy-substituted pyrimidines as adenosine receptor antagonists
EA200800886A1 (ru) Способ получения 1-н-имидазо[4,5-с]пиридинов и их аналогов
EA201370184A1 (ru) Гетероарильные производные
NZ631477A (en) Substituted pyrrolidine-2-carboxamides
WO2013058681A3 (ru) Замещенные феноксиуксусные кислоты их эфиры и амиды, включающие 2,6-диоксо-2,3,6,7-тетрагидро-1н-пурин-8-иловый фрагмент-антагонисты аденозинового а2а рецептора и их применение
JP2019532067A5 (ru)
PE20200756A1 (es) Compuestos de indazol como potenciadores alostericos mglur4, composiciones y metodos de tratamiento de la disfuncion neurologica
EA022994B1 (ru) Способ подавления толерантности к опиоидному анальгетику
ATE552246T1 (de) Substituierte aryloxy-n- bicyclomethylacetamidverbindungen als vr1- antagonisten
US20120190646A1 (en) Compositions Comprising Thalidomide and Artemisinin for the Treatment of Cancer
EA201590074A1 (ru) Производное бензодиоксола, способ его получения и его применение
EA200701035A1 (ru) Замещенные n-сульфониламинобензил-2-феноксиацетамидные соединения
AR078120A1 (es) Antagonistas de ccr3 de arilsulfonamida 2,5-disustituida y composiciones farmaceuticas
EA201290505A1 (ru) Соединения для лечения неврологических расстройств
RU2007128080A (ru) Производные пирролидиния в качестве мускариновых рецепторов мз
EP1698618A4 (en) benzamide derivatives
RU2012136457A (ru) Новые композиции для уменьшения аb 42 синтеза и их применение в лечении болезни альцгеймера (ad)