CA2440760C - Substituted pyrazolopyrimidines and thiazolopyrimidines used as analgesics - Google Patents

Substituted pyrazolopyrimidines and thiazolopyrimidines used as analgesics Download PDF

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Publication number
CA2440760C
CA2440760C CA2440760A CA2440760A CA2440760C CA 2440760 C CA2440760 C CA 2440760C CA 2440760 A CA2440760 A CA 2440760A CA 2440760 A CA2440760 A CA 2440760A CA 2440760 C CA2440760 C CA 2440760C
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CA
Canada
Prior art keywords
compound
denotes
alkyl
pyrimidine
compound according
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.)
Expired - Fee Related
Application number
CA2440760A
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English (en)
French (fr)
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CA2440760A1 (en
Inventor
Matthias Gerlach
Corinna Maul
Utz-Peter Jagusch
Bernd Sundermann
Martin Fuhr
Adriaan P. Ijzerman
Miriam Dissen-De Groote
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.)
Grünenthal GmbH
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Grünenthal GmbH
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
Priority claimed from DE2001112197 external-priority patent/DE10112197A1/de
Priority claimed from DE2001153344 external-priority patent/DE10153344A1/de
Application filed by Grünenthal GmbH filed Critical Grünenthal GmbH
Publication of CA2440760A1 publication Critical patent/CA2440760A1/en
Application granted granted Critical
Publication of CA2440760C publication Critical patent/CA2440760C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/20—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
    • A61P25/28—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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • 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
    • A61P9/06—Antiarrhythmics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA2440760A 2001-03-14 2002-03-13 Substituted pyrazolopyrimidines and thiazolopyrimidines used as analgesics Expired - Fee Related CA2440760C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
DE10112197.0 2001-03-14
DE2001112197 DE10112197A1 (de) 2001-03-14 2001-03-14 Substituierte Pyrazolo- und Thiazolopyrimidine
DE10153344.6 2001-10-29
DE2001153344 DE10153344A1 (de) 2001-10-29 2001-10-29 Verwendung von substituierten Pyrazolopyrimidinen als Liganden von Nucleosid-Transport-Proteinen und/oder von Purinorezeptoren
PCT/EP2002/002722 WO2002072585A2 (de) 2001-03-14 2002-03-13 Substituierte pyrazolo- und thiazolopyrimidine als analgetika

Publications (2)

Publication Number Publication Date
CA2440760A1 CA2440760A1 (en) 2002-09-19
CA2440760C true CA2440760C (en) 2010-02-09

Family

ID=26008763

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2440760A Expired - Fee Related CA2440760C (en) 2001-03-14 2002-03-13 Substituted pyrazolopyrimidines and thiazolopyrimidines used as analgesics

Country Status (24)

Country Link
US (1) US7135568B2 (enExample)
EP (2) EP1368355B1 (enExample)
JP (1) JP2004527508A (enExample)
KR (1) KR20030082982A (enExample)
CN (1) CN1318422C (enExample)
AT (2) ATE404568T1 (enExample)
AU (1) AU2002302419B2 (enExample)
BR (1) BR0208244A (enExample)
CA (1) CA2440760C (enExample)
CY (1) CY1105507T1 (enExample)
CZ (1) CZ20032474A3 (enExample)
DE (2) DE50212652D1 (enExample)
DK (1) DK1368355T3 (enExample)
ES (2) ES2311920T3 (enExample)
HU (1) HUP0401211A3 (enExample)
IL (2) IL157895A0 (enExample)
MX (1) MXPA03008291A (enExample)
NO (1) NO20034031L (enExample)
NZ (2) NZ528639A (enExample)
PL (1) PL364388A1 (enExample)
PT (1) PT1368355E (enExample)
RU (1) RU2003129060A (enExample)
SK (1) SK11542003A3 (enExample)
WO (1) WO2002072585A2 (enExample)

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PL382706A1 (pl) * 2002-08-26 2007-11-26 Takeda Pharmaceutical Company Limited Związek modulujący receptor wapnia i jego zastosowanie
UA81453C2 (en) * 2003-02-27 2008-01-10 Pyrazolopyridine derivates
GB0404434D0 (en) 2004-02-27 2004-03-31 Novartis Ag Organic compounds
WO2005112936A1 (en) * 2004-05-14 2005-12-01 The Regents Of The University Of Michigan Compositions and methods relating to protein kinase inhibitors
AR050188A1 (es) * 2004-08-03 2006-10-04 Uriach Y Compania S A J Compuestos heterociclicos condensados utiles en terapia como inhibidores de quinasas p38 y composiciones farmaceuticas que los contienen
EP1736475A1 (en) * 2005-06-21 2006-12-27 Ferrer Internacional, S.A. Halogenated pyrazolo[1,5-a]pyrimidines, processes, uses, compositions and intermediates
KR100838692B1 (ko) 2007-07-11 2008-06-16 한국화학연구원 7-(3′,4′-디알콕시페닐)-4,5,6,7-테트라히드로피라졸로[1,5-ａ]피리미딘 화합물, 이의 제조방법 및 이를 포함하는천식 및 만성폐쇄성 폐질환을 포함한 염증관련 질환,관절염, 아토피 피부염, 암 및 뇌질환의 치료 및 예방을위한 약제학적 조성물
RU2376291C1 (ru) * 2008-05-07 2009-12-20 Андрей Александрович Иващенко ЗАМЕЩЕННЫЕ 3,5-ДИАМИНО-4-СУЛЬФОНИЛ-ПИРАЗОЛЫ И 2-АМИНО-3-СУЛЬФОНИЛ-ПИРАЗОЛО[1,5-a]ПИРИМИДИНЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-HT6 РЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ
RU2374249C1 (ru) * 2008-09-17 2009-11-27 Андрей Александрович Иващенко ЗАМЕЩЕННЫЕ ЦИКЛОАЛКАНО[е ИЛИ d]ПИРАЗОЛО[1,5-а]ПИРИМИДИНЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-НТ6 РЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ
EA017805B1 (ru) * 2008-01-24 2013-03-29 Андрей Александрович ИВАЩЕНКО 2-АЛКИЛАМИНО-3-АРИЛСУЛЬФОНИЛЦИКЛОАЛКАНО[e ИЛИ d]ПИРАЗОЛО[1,5-a]ПИРИМИДИНЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-НТРЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ
RU2369600C1 (ru) * 2008-01-24 2009-10-10 Андрей Александрович Иващенко ЗАМЕЩЕННЫЕ 4-СУЛЬФОНИЛ-ПИРАЗОЛЫ И 3-СУЛЬФОНИЛ-ПИРАЗОЛО[1,5-a]ПИРИМИДИНЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ5-HT6 РЕЦЕПТОРОВ, АКТИВНЫЙ КОМПОНЕНТ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, ЛЕКАРСТВЕННОЕ СРЕДСТВО И СПОСОБЫ ИХ ПОЛУЧЕНИЯ
JP5584627B2 (ja) * 2008-01-24 2014-09-03 アンドレイ・アレクサンドロビッチ・イワシェンコ 置換されたシクロアルキル［ｅ又はｄ］ピラゾロ［１，５−ａ］ピリミジン−セロトニン５−ＨＴ６受容体のアンタゴニスト、その調製の方法及び使用
JP2012504663A (ja) * 2008-10-06 2012-02-23 アンドレイ・アレクサンドロビッチ・イワシェンコ 置換された３−アリールスルホニル−ピラゾロ［１，５−ａ］ピリミジン、セロトニン５−ＨＴ６受容体アンタゴニスト、その調製のための方法及び使用
EP2379566A2 (en) * 2008-12-22 2011-10-26 Schering Corporation Gamma secretase modulators
JO3407B1 (ar) * 2012-05-31 2019-10-20 Eisai R&D Man Co Ltd مركبات رباعي هيدرو بيرازولو بيريميدين
CN102775412B (zh) * 2012-08-21 2013-05-01 四川大学 一种镇静催眠的化合物及其制备方法和用途
CN102977106B (zh) * 2012-12-12 2014-12-10 中国药科大学 一类具有外周镇痛作用的κ阿片受体激动剂
US10179781B2 (en) * 2013-03-15 2019-01-15 Chromocell Corporation Sodium channel modulators for the treatment of pain
CN105611923B (zh) * 2013-09-10 2019-08-23 卓莫赛尔公司 用于治疗疼痛和糖尿病的钠通道调节剂
WO2016123629A1 (en) * 2015-01-30 2016-08-04 Vanderbilt University Indazole and azaindazole substituted compounds as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
CA3002144C (en) 2015-10-16 2024-01-23 Eisai R&D Management Co., Ltd. Ep4 antagonists
WO2018133835A1 (en) * 2017-01-20 2018-07-26 National Institute Of Biological Sciences, Beijing Nucleoside analogue regulating mammalian circadian rhythm
AU2018257332B2 (en) 2017-04-27 2021-11-04 Takeda Pharmaceutical Company Limited Heterocyclic compound
WO2018199235A1 (ja) * 2017-04-27 2018-11-01 武田薬品工業株式会社 複素環化合物
CN113354644B (zh) * 2020-03-04 2023-07-04 烟台药物研究所 一类用作dpp-iv抑制剂的吡唑并嘧啶结构的化合物及应用
IL297963A (en) 2020-05-07 2023-01-01 Adorx Therapeutics Ltd Antagonists of the adenosine a2a receptor
CN116023382B (zh) * 2023-02-22 2025-09-23 北京师范大学 一种合成手性四氢吡唑并[1,5-a]嘧啶的方法

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EP0264773A1 (en) 1986-10-16 1988-04-27 American Cyanamid Company 4,5-dihydro and 4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidines
NZ233641A (en) * 1989-05-16 1992-07-28 Merrell Dow Pharma Quinoline and thienopyridine derivatives and excitatory amino acid antagonistic pharmaceutical compositions
GB9206266D0 (en) * 1992-03-23 1992-05-06 Merck Sharp & Dohme Therapeutic agents
FR2717812B1 (fr) * 1994-03-28 1996-05-10 Rhone Poulenc Rorer Sa Indeno[1,2-e]pyrazine-4-ones, leur préparation et les médicaments les contenant.
FR2722786B1 (fr) * 1994-07-20 1996-08-23 Rhone Poulenc Rorer Sa Derives de 4-hydroxy-3-phenyl-indeno(1,2-b)pyridine-2(1h)- one, leur preparation et les medicaments les contenant
DE4444815A1 (de) * 1994-12-15 1996-06-20 Merck Patent Gmbh Thienopyridone
JP2003288537A (ja) 2000-09-25 2003-10-10 Everyd.Com:Kk 商品宅配システムおよび方法
DE10112197A1 (de) 2001-03-14 2002-09-19 Gruenenthal Gmbh Substituierte Pyrazolo- und Thiazolopyrimidine

Also Published As

Publication number Publication date
CY1105507T1 (el) 2010-04-28
NZ528639A (en) 2005-07-29
EP1368355A2 (de) 2003-12-10
JP2004527508A (ja) 2004-09-09
EP1637533A1 (de) 2006-03-22
DK1368355T3 (da) 2006-10-09
RU2003129060A (ru) 2005-04-10
ES2311920T3 (es) 2009-02-16
DE50212652D1 (de) 2008-09-25
CN1318422C (zh) 2007-05-30
US7135568B2 (en) 2006-11-14
PT1368355E (pt) 2006-09-29
NO20034031L (no) 2003-10-21
EP1368355B1 (de) 2006-06-07
ATE328886T1 (de) 2006-06-15
AU2002302419B2 (en) 2007-01-18
ES2263779T3 (es) 2006-12-16
KR20030082982A (ko) 2003-10-23
CA2440760A1 (en) 2002-09-19
HUP0401211A3 (en) 2008-03-28
NO20034031D0 (no) 2003-09-11
CN1507447A (zh) 2004-06-23
EP1637533B1 (de) 2008-08-13
IL157895A (en) 2009-12-24
US20040127508A1 (en) 2004-07-01
ATE404568T1 (de) 2008-08-15
WO2002072585A2 (de) 2002-09-19
DE50207103D1 (en) 2006-07-20
CZ20032474A3 (cs) 2003-12-17
IL157895A0 (en) 2004-03-28
MXPA03008291A (es) 2003-12-11
HK1061034A1 (en) 2004-09-03
BR0208244A (pt) 2004-03-02
NZ540574A (en) 2006-11-30
SK11542003A3 (sk) 2004-07-07
PL364388A1 (en) 2004-12-13
WO2002072585A3 (de) 2003-02-20
HUP0401211A2 (hu) 2004-10-28

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