CN101484448B - 作为ampa增强剂的吡唑烷烃基酰胺取代的噻吩 - Google Patents

作为ampa增强剂的吡唑烷烃基酰胺取代的噻吩 Download PDF

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Publication number
CN101484448B
CN101484448B CN2007800248081A CN200780024808A CN101484448B CN 101484448 B CN101484448 B CN 101484448B CN 2007800248081 A CN2007800248081 A CN 2007800248081A CN 200780024808 A CN200780024808 A CN 200780024808A CN 101484448 B CN101484448 B CN 101484448B
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mmol
thiophene
trifluoromethyl
carboxamide
tetrahydro
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CN101484448A (zh
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K·J·吉伦
C·贾米森
J·K·F·麦克林
E·M·莫伊尔
Z·兰科维克
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Organon NV
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00—Drugs for disorders of the nervous system
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    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
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  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CN2007800248081A 2006-07-04 2007-07-02 作为ampa增强剂的吡唑烷烃基酰胺取代的噻吩 Expired - Fee Related CN101484448B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP06116592 2006-07-04
EP06116592.4 2006-07-04
PCT/EP2007/005851 WO2008003452A1 (en) 2006-07-04 2007-07-02 Pyrazolealkanamide substituted thiophenes as ampa potentiators

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CN101484448A CN101484448A (zh) 2009-07-15
CN101484448B true CN101484448B (zh) 2012-03-14

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CN2007800248081A Expired - Fee Related CN101484448B (zh) 2006-07-04 2007-07-02 作为ampa增强剂的吡唑烷烃基酰胺取代的噻吩

Country Status (15)

Country Link
US (1) US7820707B2 (enExample)
EP (1) EP2041124B1 (enExample)
JP (1) JP2009541404A (enExample)
KR (1) KR20090027672A (enExample)
CN (1) CN101484448B (enExample)
AR (1) AR061792A1 (enExample)
AU (1) AU2007271469B2 (enExample)
CA (1) CA2655680A1 (enExample)
IL (1) IL196302A0 (enExample)
MX (1) MX2008016494A (enExample)
NZ (1) NZ573325A (enExample)
PE (1) PE20080378A1 (enExample)
TW (1) TW200817385A (enExample)
WO (1) WO2008003452A1 (enExample)
ZA (1) ZA200810165B (enExample)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2718727A1 (en) * 2008-03-25 2009-10-01 Takeda Pharmaceutical Company Limited Heterocyclic compound
TW201012803A (en) * 2008-06-06 2010-04-01 Organon Nv Heterocyclic derivatives
WO2011036885A1 (ja) * 2009-09-25 2011-03-31 武田薬品工業株式会社 複素環化合物
WO2011036889A1 (ja) * 2009-09-25 2011-03-31 武田薬品工業株式会社 複素環化合物
CA2806436C (en) 2010-08-10 2019-09-10 Syngenta Participations Ag Process for the preparation of 3-haloalkylpyrazoles
JO3225B1 (ar) * 2012-11-27 2018-03-08 Lilly Co Eli 6-((s)-1-{1-[5-(2-هيدروكسي-إيثوكسي)-بيريدين-2-يل]-1h-بيرازول-3-يل}إيثيل)-3h-1 ، 3-بنزو ثيازول-2- أون باعتباره مضاد مستقبل ampa يعتمد على tarp- جاما 8
AU2014304562B8 (en) 2013-08-08 2018-07-05 Galapagos Nv Thieno[2,3-c]pyrans as CFTR modulators
CN103772282B (zh) * 2014-02-26 2015-09-23 上海毕得医药科技有限公司 一种3-叔丁基-1h-吡唑-4-甲醛的制备方法
TW201609719A (zh) * 2014-05-28 2016-03-16 美國禮來大藥廠 作為ＴＡＲＰ－γ８依賴性ＡＭＰＡ受體拮抗劑之６－經取代－３Ｈ－１，３－苯并噻唑－２－酮化合物
CN107286114B (zh) * 2016-04-13 2020-08-18 中国人民解放军军事医学科学院毒物药物研究所 Ampa受体增效剂的脑靶向前药及其医药用途
GB201702221D0 (en) * 2017-02-10 2017-03-29 Univ Of Sussex Compounds
GB201803340D0 (en) 2018-03-01 2018-04-18 Univ Of Sussex Compounds

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1516701A (zh) * 2001-06-14 2004-07-28 ��˹��ŵ�� 作为AMPA受体正性调节剂的(吡啶并/噻吩并)-[f]-氧杂吖庚因-5-酮衍生物

Family Cites Families (8)

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Publication number Priority date Publication date Assignee Title
AU771358B2 (en) * 1997-11-21 2004-03-18 Astrazeneca Ab Metabotropic glutamate receptor antagonists for treating central nervous system diseases
CH1196397H1 (de) * 1999-06-02 2007-05-31 Nps Pharma Inc Metabotrope Glutamatrezeptorantagonisten zur Behandlung von Krankheiten des zentralen Nervensystems.
US6414013B1 (en) * 2000-06-19 2002-07-02 Pharmacia & Upjohn S.P.A. Thiophene compounds, process for preparing the same, and pharmaceutical compositions containing the same background of the invention
US20040171603A1 (en) 2001-05-18 2004-09-02 Janos Pato Novel therapeutic targets for the treatment of mycobacterial infections and compounds useful therefor
US20050085531A1 (en) 2003-10-03 2005-04-21 Hodge Carl N. Thiophene-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions, and uses thereof
WO2005040110A1 (en) 2003-10-08 2005-05-06 Eli Lilly And Company Pyrrole and pyrazole derivatives as potentiators of glutamate receptors
WO2005070916A1 (en) 2004-01-09 2005-08-04 Eli Lilly And Company Thiophene and furan compounds
EP1802634A2 (en) 2004-10-20 2007-07-04 Compass Pharmaceuticals LLC Thiophens and their use as anti-tumor agents

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1516701A (zh) * 2001-06-14 2004-07-28 ��˹��ŵ�� 作为AMPA受体正性调节剂的(吡啶并/噻吩并)-[f]-氧杂吖庚因-5-酮衍生物

Also Published As

Publication number Publication date
ZA200810165B (en) 2009-09-30
KR20090027672A (ko) 2009-03-17
IL196302A0 (en) 2009-09-22
NZ573325A (en) 2011-05-27
AU2007271469A1 (en) 2008-01-10
US20080255086A1 (en) 2008-10-16
MX2008016494A (es) 2009-01-21
EP2041124B1 (en) 2013-06-26
AU2007271469B2 (en) 2012-05-31
WO2008003452A1 (en) 2008-01-10
US7820707B2 (en) 2010-10-26
JP2009541404A (ja) 2009-11-26
CN101484448A (zh) 2009-07-15
TW200817385A (en) 2008-04-16
AR061792A1 (es) 2008-09-24
CA2655680A1 (en) 2008-01-10
EP2041124A1 (en) 2009-04-01
PE20080378A1 (es) 2008-04-25

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