EA200400598A1 - Производные никотин- или изоникотинбензотиазола - Google Patents

Производные никотин- или изоникотинбензотиазола

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Publication number
EA200400598A1
EA200400598A1 EA200400598A EA200400598A EA200400598A1 EA 200400598 A1 EA200400598 A1 EA 200400598A1 EA 200400598 A EA200400598 A EA 200400598A EA 200400598 A EA200400598 A EA 200400598A EA 200400598 A1 EA200400598 A1 EA 200400598A1
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EA
Eurasian Patent Office
Prior art keywords
alkyl
ness
group
morpholinyl
cycloalkyl
Prior art date
Application number
EA200400598A
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English (en)
Other versions
EA007502B1 (ru
Inventor
Александер Флор
Роланд Якоб-Рётне
Роже Давид Норкросс
Клаус Ример
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Ф.Хоффманн-Ля Рош Аг
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Publication of EA200400598A1 publication Critical patent/EA200400598A1/ru
Publication of EA007502B1 publication Critical patent/EA007502B1/ru

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    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • A61P25/22—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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
    • 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
    • A61P25/36—Opioid-abuse
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P37/08—Antiallergic agents
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

В заявке описаны соединения общей формулы I, где Rозначает фенил, пиперидин-1-ил или морфолинил, A означает -O-, а R означает -(CH)-N(R")-C(O)-(низш.)алкил, -(CH)-O-(низш.)алкил, -(CH)-O-(CH)-O-(низш.)алкил, (низш.)алкил, -(CH)-морфолинил, -(CH)-фенил, -(CH)-N(R"), -(CH)-пиридинил, -(CH)-CF, -(CH)-2-оксопирролидинил или C-C-циклоалкил, R" означает водород или (низш.)алкил, а n равно 1 или 2, или A означает -N(R')-, а R означает (низш.)алкил, C-C-циклоалкил, -(CH)-O-(низш.)алкил, -(CH)-пиридинил, -(CH)-пиперидинил, -(CH)-фенил, -(CH)-N(R")-C(O)-(низш.)алкил, -(CH)-морфолинил или -(CH)-N(R"), R' и R" независимо друг от друга означают водород или (низш.)алкил, а n равно 1 или 2, или A означает -CH-, а R означает -N(R")-(CH)-O-(низш.)алкил, -N(R"), -S-(низш.)алкил, или R означает азетидинил, пирролидинил или пиперидинил, которые необязательно замещены гидроксигруппой или (низш.)алкокси, или R означает морфолинил, -N(R")-(CH)-(C-C)циклоалкил, -N(R")-(CH)-C(O)O-(низш.)алкил, -N(R")-(CH)-C(O)OH, -2-оксопирролидинил, -N(R")-C(O)O-(низш.)алкил, -O(CH)-O-(низш.)алкил или алкокси, R" означает водород или (низш.)алкил, а m равно 1, 2 или 3; A означает -S-, а R означает (низш.)алкил или A-R вместе означают пиперазинил, замещенный (низш.)алкилом, -C(O)- (низш.)алкилом или оксогруппой, или группа A-R означает пиперидинил, замещенный (низш.)алкокси или гидроксигруппой, или группа A-R означает морфолинил, замещенный (низш.)алкилом, или группа A-R означает C-C-циклоалкил, азетидин-1-ил, необязательно замещенный гидроксигруппой или (низш.)алкокси, или группа A-R означает тиоморфолин-1,1-диоксо, тетрагидропиран или 2-окса-5-азабицикло[2.2.1]гепт-5-ил, и их фармацевтически приемлемые кислотно-аддитивные соли. Установлено, что соединения общей формулы I являются лигандами рецептора аденозина. Соединения по настоящему изобретению прежде всего обладают высоким сродством к рецептору аденозина Aи могут применяться для лечения заболеваний, опосредованных указанным рецептором.Международная заявка была опубликована
EA200400598A 2001-11-19 2002-11-11 Производные никотин- или изоникотинбензотиазола EA007502B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP01127312 2001-11-19
PCT/EP2002/012562 WO2003043636A1 (en) 2001-11-19 2002-11-11 Nicotin-or isonicotin benzothiazole derivatives

Publications (2)

Publication Number Publication Date
EA200400598A1 true EA200400598A1 (ru) 2005-02-24
EA007502B1 EA007502B1 (ru) 2006-10-27

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ID=8179263

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EA200400598A EA007502B1 (ru) 2001-11-19 2002-11-11 Производные никотин- или изоникотинбензотиазола

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US (1) US6620811B2 (ru)
EP (1) EP1448198B1 (ru)
JP (1) JP4226474B2 (ru)
KR (1) KR100577110B1 (ru)
CN (1) CN100546580C (ru)
AR (1) AR039367A1 (ru)
AT (1) ATE376831T1 (ru)
AU (1) AU2002351955B2 (ru)
BR (1) BR0214245A (ru)
CA (1) CA2467552C (ru)
DE (1) DE60223278T2 (ru)
DK (1) DK1448198T3 (ru)
EA (1) EA007502B1 (ru)
EC (1) ECSP045109A (ru)
ES (1) ES2294187T3 (ru)
GT (1) GT200200232A (ru)
HR (1) HRP20040396A2 (ru)
HU (1) HUP0402161A3 (ru)
IL (2) IL161623A0 (ru)
JO (1) JO2290B1 (ru)
MA (1) MA27083A1 (ru)
MX (1) MXPA04004684A (ru)
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NO (1) NO20042576L (ru)
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PE (1) PE20030713A1 (ru)
PL (1) PL369517A1 (ru)
PT (1) PT1448198E (ru)
RS (1) RS39904A (ru)
RU (1) RU2294933C2 (ru)
SI (1) SI1448198T1 (ru)
TN (1) TNSN04087A1 (ru)
TW (1) TW200407134A (ru)
UA (1) UA77462C2 (ru)
UY (1) UY27542A1 (ru)
WO (1) WO2003043636A1 (ru)
ZA (1) ZA200403817B (ru)

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UA110097C2 (uk) 2009-09-02 2015-11-25 Терапевтичний агент для лікування розладів настрою
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TNSN04087A1 (en) 2006-06-01
SI1448198T1 (sl) 2008-02-29
EA007502B1 (ru) 2006-10-27
RU2004118425A (ru) 2006-01-10
CN100546580C (zh) 2009-10-07
IL161623A (en) 2010-11-30
CA2467552A1 (en) 2003-05-30
HRP20040396A2 (en) 2005-04-30
HUP0402161A3 (en) 2010-06-28
GT200200232A (es) 2003-06-17
TW200407134A (en) 2004-05-16
ECSP045109A (es) 2004-06-28
DE60223278T2 (de) 2008-08-14
MA27083A1 (fr) 2004-12-20
UY27542A1 (es) 2003-05-30
RU2294933C2 (ru) 2007-03-10
JP2005522413A (ja) 2005-07-28
JP4226474B2 (ja) 2009-02-18
RS39904A (en) 2006-10-27
PT1448198E (pt) 2007-12-11
CA2467552C (en) 2011-05-24
AU2002351955A1 (en) 2003-06-10
JO2290B1 (en) 2005-09-12
PE20030713A1 (es) 2003-08-23
KR20050044535A (ko) 2005-05-12
NZ532802A (en) 2005-07-29
ZA200403817B (en) 2005-05-23
MY126176A (en) 2006-09-29
UA77462C2 (en) 2006-12-15
DK1448198T3 (da) 2008-01-07
ATE376831T1 (de) 2007-11-15
US20030134854A1 (en) 2003-07-17
AR039367A1 (es) 2005-02-16
MXPA04004684A (es) 2004-08-12
WO2003043636A1 (en) 2003-05-30
CN1617722A (zh) 2005-05-18
PL369517A1 (en) 2005-04-18
US6620811B2 (en) 2003-09-16
DE60223278D1 (de) 2007-12-13
IL161623A0 (en) 2004-09-27
ES2294187T3 (es) 2008-04-01
EP1448198B1 (en) 2007-10-31
KR100577110B1 (ko) 2006-05-10
PA8558001A1 (es) 2003-07-28
EP1448198A1 (en) 2004-08-25
BR0214245A (pt) 2004-12-14
AU2002351955B2 (en) 2007-03-15
HUP0402161A2 (hu) 2005-02-28
NO20042576L (no) 2004-06-18

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