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EA199800702A1 - Хиноксалиндионы - Google Patents

Хиноксалиндионы

Info

Publication number
EA199800702A1
EA199800702A1 EA199800702A EA199800702A EA199800702A1 EA 199800702 A1 EA199800702 A1 EA 199800702A1 EA 199800702 A EA199800702 A EA 199800702A EA 199800702 A EA199800702 A EA 199800702A EA 199800702 A1 EA199800702 A1 EA 199800702A1
Authority
EA
Eurasian Patent Office
Prior art keywords
aryl
compounds
alkoxy
ring
halogen
Prior art date
Application number
EA199800702A
Other languages
English (en)
Other versions
EA001730B1 (ru
Inventor
Дэйвид Джон Булл
Кристофер Ли Карр
Майкл Джонатан Фрэй
Элизабет Колетт Луиз Готье
Чарльз Эрик Моубрэй
Алан Стоуби
Original Assignee
Пфайзер Рисёрч Энд Дивелопмент Компани Н.В./С.А.
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 Пфайзер Рисёрч Энд Дивелопмент Компани Н.В./С.А. filed Critical Пфайзер Рисёрч Энд Дивелопмент Компани Н.В./С.А.
Publication of EA199800702A1 publication Critical patent/EA199800702A1/ru
Publication of EA001730B1 publication Critical patent/EA001730B1/ru

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • 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
    • A61P25/14Drugs 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Luminescent Compositions (AREA)
  • Polymers With Sulfur, Phosphorus Or Metals In The Main Chain (AREA)

Abstract

В изобретении предложены соединения формулы (I):и их фармацевтически приемлемые соли, где R представляет собой гетероарильную группу с 5 членами в кольце, содержащую 3 или 4 гетероатома азота, которая связана с кольцом хиноксалиндиона через кольцевой атом углерода или азота, или представляет собой гетероарильную группу с 6 членами в кольце, содержащую от 1 до 3 гетероатомов азота, которая связана с кольцом хиноксалиндиона через кольцевой атом углерода, причем любая из указанных групп является возможно бензоконденсированной и возможно замещенной, в том числе в бензоконденсированной части, 1 или 2 заместителями, каждый из которых произвольно выбран из С-Салкила, С-Салкенила, С-Сциклоалкила, галогена, гидрокси, С-Салкокси, С-Сциклоалкилокси, -СООН, С-Салкоксикарбонила, -CONRR, -NRR, -S(O)р(С-Салкила), -SONRR, арила, арилокси, арил(С-С)алкокси и гет, причем указанный С-Салкил возможно замещен С-Сциклоалкилом, галогеном, гидрокси, С-Салкокси, галоген(С-С)алкокси, С-Сциклоалкилокси, С-Сциклоалкил(С-С)алкоксигруппой, -СООН, С-Салкоксикарбонилом, -CONRR, -NRR-S(O)р(С-Салкилом), -SO(арилом), -SONRR, морфолино, арилом, арилокси, арил(С-С)алкокси или гет, причем указанный C-Салкенил возможно замещен арилом; Rи Rкаждый независимо выбран из Н, фтор-, хлор-, бром-, С-Салкила и галоген(С-С)алкила; Rи Rкаждый независимо выбран из Н, С-Салкила или, взятые вместе, они представляют собой C-Салкилен; р равно 0, 1 или 2; вместе с получением таких соединений, композициями, содержащими такие соединения, применениями таких соединений и промежуточными соединениями, применяемыми в синтезе таких соединений. Соединения полезны в качестве антагонистов NMDA рецептора при лечении острых нейродегенеративных и хронических неврологических
EA199800702A 1996-03-09 1997-02-27 Хиноксалиндионы EA001730B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9605027.3A GB9605027D0 (en) 1996-03-09 1996-03-09 Quinoxalinediones
PCT/EP1997/000995 WO1997032873A1 (en) 1996-03-09 1997-02-27 Quinoxalinediones

Publications (2)

Publication Number Publication Date
EA199800702A1 true EA199800702A1 (ru) 1999-04-29
EA001730B1 EA001730B1 (ru) 2001-08-27

Family

ID=10790134

Family Applications (1)

Application Number Title Priority Date Filing Date
EA199800702A EA001730B1 (ru) 1996-03-09 1997-02-27 Хиноксалиндионы

Country Status (42)

Country Link
US (1) US6376490B1 (ru)
EP (1) EP0885212B1 (ru)
JP (1) JP3110467B2 (ru)
KR (1) KR100288099B1 (ru)
CN (1) CN1103770C (ru)
AP (1) AP767A (ru)
AR (1) AR006119A1 (ru)
AT (1) ATE208773T1 (ru)
AU (1) AU717972B2 (ru)
BG (1) BG63340B1 (ru)
BR (1) BR9707851A (ru)
CA (1) CA2248366C (ru)
CO (1) CO4770976A1 (ru)
CZ (1) CZ292792B6 (ru)
DE (1) DE69708269T2 (ru)
DK (1) DK0885212T3 (ru)
DZ (1) DZ2188A1 (ru)
EA (1) EA001730B1 (ru)
ES (1) ES2163742T3 (ru)
GB (1) GB9605027D0 (ru)
HN (1) HN1998000034A (ru)
HR (1) HRP970132A2 (ru)
HU (1) HUP9900975A3 (ru)
ID (1) ID18112A (ru)
IL (1) IL125491A (ru)
IS (1) IS4811A (ru)
MA (1) MA26422A1 (ru)
NO (1) NO984058L (ru)
NZ (1) NZ331060A (ru)
OA (1) OA10850A (ru)
PE (2) PE43398A1 (ru)
PL (1) PL329032A1 (ru)
PT (1) PT885212E (ru)
SI (1) SI0885212T1 (ru)
SK (1) SK283467B6 (ru)
TN (1) TNSN97044A1 (ru)
TR (1) TR199801782T2 (ru)
TW (1) TW454004B (ru)
UY (1) UY24482A1 (ru)
WO (1) WO1997032873A1 (ru)
YU (2) YU39698A (ru)
ZA (1) ZA971987B (ru)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUP0003612A3 (en) * 1997-02-27 2003-04-28 Pfizer Quinoxalinediones and pharmaceutical compositions containing them
AP982A (en) * 1997-02-27 2001-07-16 Pfizer Quinoxalinediones.
US6340758B1 (en) * 1997-05-16 2002-01-22 Warner-Lambert Company Conformationally semi-constrained quinoxaline 2,3-diones as neuroprotective agents
DE10005150A1 (de) 2000-02-07 2001-08-09 Merck Patent Gmbh Verfahren zur Herstellung von 5-Arylnicotinaldehyden
RU2002133666A (ru) * 2000-05-19 2007-05-10 Мерк Патент ГмбХ (DE) Производные триазола
US7732162B2 (en) 2003-05-05 2010-06-08 Probiodrug Ag Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases
WO2005006945A2 (en) * 2003-07-03 2005-01-27 The Salk Institute For Biological Studies Methods for treating neural disorders and compounds useful therefor
MY145368A (en) 2004-01-13 2012-01-31 Nissan Chemical Ind Ltd Aminoquinoxaline compounds and polyaminoquinoxaline compounds, and use thereof
KR101170995B1 (ko) 2004-02-06 2012-08-08 닛산 가가쿠 고교 가부시키 가이샤 에너지 저장 디바이스용 전극 및 그 제조 방법
JP2007223901A (ja) * 2004-03-24 2007-09-06 Takeda Chem Ind Ltd 複素環化合物およびその用途
US20060211739A1 (en) * 2005-02-08 2006-09-21 Arturo Perez-Medrano Use of selective P2X7 receptor antagonists
WO2007112347A1 (en) * 2006-03-28 2007-10-04 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
JP5379692B2 (ja) 2006-11-09 2013-12-25 プロビオドルグ エージー 潰瘍、癌及び他の疾患の治療のためのグルタミニルシクラーゼの阻害薬としての3−ヒドロキシ−1,5−ジヒドロ−ピロール−2−オン誘導体
DK2091948T3 (da) 2006-11-30 2012-07-23 Probiodrug Ag Nye inhibitorer af glutaminylcyclase
US8603980B2 (en) 2007-01-16 2013-12-10 The Johns Hopkins University Glutamate receptor antagonists and methods of use
AU2008220785B2 (en) 2007-03-01 2013-02-21 Vivoryon Therapeutics N.V. New use of glutaminyl cyclase inhibitors
EP2865670B1 (en) 2007-04-18 2017-01-11 Probiodrug AG Thiourea derivatives as glutaminyl cyclase inhibitors
CN101679383B (zh) * 2007-05-17 2014-10-29 株式会社半导体能源研究所 三唑衍生物,和使用三唑衍生物的发光元件、发光器件和电子器件
EA022007B1 (ru) 2009-09-11 2015-10-30 Пробиодруг Аг Гетероциклические производные в качестве ингибиторов глутаминилциклазы
WO2011107530A2 (en) 2010-03-03 2011-09-09 Probiodrug Ag Novel inhibitors
NZ602312A (en) 2010-03-10 2014-02-28 Probiodrug Ag Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5)
JP5945532B2 (ja) 2010-04-21 2016-07-05 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤としてのベンゾイミダゾール誘導体
EP2686313B1 (en) 2011-03-16 2016-02-03 Probiodrug AG Benzimidazole derivatives as inhibitors of glutaminyl cyclase
CN104955809B (zh) * 2013-02-07 2018-12-11 普雷斯特威克化学公司 取代的乙炔衍生物及其作为mGluR4的正变构调节剂的用途
EP3461819B1 (en) 2017-09-29 2020-05-27 Probiodrug AG Inhibitors of glutaminyl cyclase
CN111548320B (zh) * 2019-10-09 2023-03-24 贵州大学 一类1,3,4-噁二唑酰肼类化合物及其制备方法和应用

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ES2150417T3 (es) * 1990-11-06 2000-12-01 Yamanouchi Pharma Co Ltd Derivados de pirazina fusionados.
DE4217952A1 (de) * 1992-05-30 1993-12-02 Basf Ag Chinoxalin-2,3(1H,4H)-dione
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HUP0003612A3 (en) * 1997-02-27 2003-04-28 Pfizer Quinoxalinediones and pharmaceutical compositions containing them

Also Published As

Publication number Publication date
JPH11506123A (ja) 1999-06-02
TR199801782T2 (xx) 1998-12-21
BG63340B1 (bg) 2001-10-31
NO984058D0 (no) 1998-09-03
ID18112A (id) 1998-03-05
CO4770976A1 (es) 1999-04-30
GB9605027D0 (en) 1996-05-08
HUP9900975A2 (hu) 1999-07-28
IS4811A (is) 1998-07-27
NO984058L (no) 1998-11-06
IL125491A0 (en) 1999-03-12
ZA971987B (en) 1998-09-07
PT885212E (pt) 2002-02-28
IL125491A (en) 2003-07-06
DK0885212T3 (da) 2002-03-25
PE58199A1 (es) 1999-06-11
EA001730B1 (ru) 2001-08-27
CA2248366C (en) 2002-06-04
DZ2188A1 (fr) 2002-12-02
OA10850A (en) 2001-08-16
AU2023197A (en) 1997-09-22
US6376490B1 (en) 2002-04-23
DE69708269T2 (de) 2002-07-25
YU41199A (sh) 2001-09-28
AR006119A1 (es) 1999-08-11
TW454004B (en) 2001-09-11
EP0885212B1 (en) 2001-11-14
BR9707851A (pt) 1999-07-27
UY24482A1 (es) 2000-09-29
AU717972B2 (en) 2000-04-06
TNSN97044A1 (fr) 2005-03-15
PL329032A1 (en) 1999-03-01
AP9700947A0 (en) 1997-04-30
KR100288099B1 (ko) 2001-05-02
SK121498A3 (en) 2000-10-09
SI0885212T1 (en) 2002-02-28
CN1103770C (zh) 2003-03-26
DE69708269D1 (de) 2001-12-20
CN1213369A (zh) 1999-04-07
JP3110467B2 (ja) 2000-11-20
MA26422A1 (fr) 2004-12-20
YU39698A (sh) 1999-03-04
CZ292792B6 (cs) 2003-12-17
CZ286498A3 (cs) 1999-07-14
ATE208773T1 (de) 2001-11-15
HUP9900975A3 (en) 2001-12-28
NZ331060A (en) 2000-01-28
CA2248366A1 (en) 1997-09-12
PE43398A1 (es) 1998-08-29
ES2163742T3 (es) 2002-02-01
HN1998000034A (es) 1999-02-09
SK283467B6 (sk) 2003-08-05
BG102760A (en) 1999-09-30
EP0885212A1 (en) 1998-12-23
KR19990087614A (ko) 1999-12-27
HRP970132A2 (en) 1998-06-30
WO1997032873A1 (en) 1997-09-12
AP767A (en) 1999-09-29

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