AU2007271469B2 - Pyrazolealkanamide substituted thiophenes as AMPA potentiators - Google Patents

Pyrazolealkanamide substituted thiophenes as AMPA potentiators Download PDF

Info

Publication number
AU2007271469B2
AU2007271469B2 AU2007271469A AU2007271469A AU2007271469B2 AU 2007271469 B2 AU2007271469 B2 AU 2007271469B2 AU 2007271469 A AU2007271469 A AU 2007271469A AU 2007271469 A AU2007271469 A AU 2007271469A AU 2007271469 B2 AU2007271469 B2 AU 2007271469B2
Authority
AU
Australia
Prior art keywords
mmol
trifluoromethyl
carboxamide
thiophene
tetrahydrobenzo
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
AU2007271469A
Other languages
English (en)
Other versions
AU2007271469A1 (en
Inventor
Kevin James Gillen
Craig Jamieson
John Kinnaird Ferguson Maclean
Elizabeth Margaret Moir
Zoran Rankovic
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp & Dohme BV
Original Assignee
Merck Sharp and Dohme Ltd
Merck Sharp & Dohme BV
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 Merck Sharp and Dohme Ltd, Merck Sharp & Dohme BV filed Critical Merck Sharp and Dohme Ltd
Publication of AU2007271469A1 publication Critical patent/AU2007271469A1/en
Assigned to MSD OSS B.V. reassignment MSD OSS B.V. Amend patent request/document other than specification (104) Assignors: N.V ORGANON
Application granted granted Critical
Publication of AU2007271469B2 publication Critical patent/AU2007271469B2/en
Assigned to MERCK SHARP & DOHME B.V. reassignment MERCK SHARP & DOHME B.V. Request to Amend Deed and Register Assignors: MSD OSS B.V.
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • 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)
AU2007271469A 2006-07-04 2007-07-02 Pyrazolealkanamide substituted thiophenes as AMPA potentiators Ceased AU2007271469B2 (en)

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

Publications (2)

Publication Number Publication Date
AU2007271469A1 AU2007271469A1 (en) 2008-01-10
AU2007271469B2 true AU2007271469B2 (en) 2012-05-31

Family

ID=37226676

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2007271469A Ceased AU2007271469B2 (en) 2006-07-04 2007-07-02 Pyrazolealkanamide substituted thiophenes as AMPA potentiators

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
WO2005040110A1 (en) * 2003-10-08 2005-05-06 Eli Lilly And Company Pyrrole and pyrazole derivatives as potentiators of glutamate receptors

Family Cites Families (8)

* Cited by examiner, † Cited by third party
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
CN1255413C (zh) * 2001-06-14 2006-05-10 阿克佐诺贝尔公司 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
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
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
WO2005040110A1 (en) * 2003-10-08 2005-05-06 Eli Lilly And Company Pyrrole and pyrazole derivatives as potentiators of glutamate receptors

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
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
CN101484448B (zh) 2012-03-14

Similar Documents

Publication Publication Date Title
EP2041124B1 (en) Pyrazolealkanamide substituted thiophenes as ampa potentiators
CN105829307B (zh) 用作tnf活性调节剂的四氢咪唑并吡啶衍生物
US8648084B2 (en) Selective substituted pyrazine ligands for neuronal nicotinic receptors
CN105814056B (zh) 用作tnf活性调节剂的嘌呤衍生物
AU2011340685A1 (en) Triazolopyridine compounds
CN101855227B (zh) 杂环衍生物
RU2734959C2 (ru) Трициклические конденсированные производные пиридин-2-она и их применение в качестве ингибиторов brd4
CN105814065B (zh) 用作tnf活性调节剂的咪唑并噻唑衍生物
WO2009119088A1 (ja) 複素環化合物
JP2013544277A (ja) Ｋａｔｉｉ阻害剤
CA3120037A1 (en) Heteroaromatic compounds as vanin inhibitors
US20130090327A1 (en) Inhibitors of Protein Tyrosine Kinase Activity
JP7414820B2 (ja) ヒストンデアセチラーゼの阻害剤
AU2005321903A1 (en) Thienopyrimidine derivatives as phosphodiesterase 10 inhibitors
EP0900799A1 (en) Novel atropisomers of 2,3-disubstituted-(5,6)-heteroarylfused-pyrimidin-4-ones
CN107903208A (zh) 一类联芳吡啶类去泛素化酶抑制剂、其制备方法及应用
JP2009544668A (ja) ピリミジノンの誘導体及びそれらの医薬としての利用
CN120435469A (zh) Ahr激动剂
AU2006232945B2 (en) Tetrahydrothiopyrano pyrazole cannabinoid modulators cross reference to related applications

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired