HUP0402161A2 - Nikotin- vagy izonikotin-benzotiazol-származékok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények - Google Patents

Nikotin- vagy izonikotin-benzotiazol-származékok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények

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Publication number
HUP0402161A2
HUP0402161A2 HU0402161A HUP0402161A HUP0402161A2 HU P0402161 A2 HUP0402161 A2 HU P0402161A2 HU 0402161 A HU0402161 A HU 0402161A HU P0402161 A HUP0402161 A HU P0402161A HU P0402161 A2 HUP0402161 A2 HU P0402161A2
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HU
Hungary
Prior art keywords
lower alkyl
group
morpholinyl
cycloalkyl
carbon
Prior art date
Application number
HU0402161A
Other languages
English (en)
Inventor
Alexander Flohr
Roland Jakob-Roetne
Roger David Norcross
Claus Riemer
Original Assignee
F. Hoffmann-La Roche Ag
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.)
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Publication date
Application filed by F. Hoffmann-La Roche Ag filed Critical F. Hoffmann-La Roche Ag
Publication of HUP0402161A2 publication Critical patent/HUP0402161A2/hu
Publication of HUP0402161A3 publication Critical patent/HUP0402161A3/hu

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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
    • C07D417/14—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
    • 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
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
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    • 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
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    • 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
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    • 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
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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (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)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

A találmány (IA) vagy (IB) általános képletű vegyületekre ésgyógyászatilag alkalmas savaddíciós sóikra vonatkozik. A képletben Rljelentése fenil-, piperidin-l-il- vagy morfolinil-csoport; A jelentése-O- ; és R jelentése -(CH2)n-N(R")-C(O)-kis szénatomszámú alkil-, -(CH2)n-O- kis szénatomszámú alkil-, -(CH2)n-O-(CH2)n-O- kis szén-atomszámú alkil-, kis szénatomszámú alkil-, -(CH2)n-morfolinil-, -(CH2)n-fenil-, -(CH2)n-N(R")2, -(CH2)n-piridinil-, -(CH2)n-CF3, -(CH2)n-2-oxo-pirrolidinil- vagy 4-6 szénatomos cikloalkil-csoport; R"jelentése egymástól függetlenül hidrogénatom vagy kis szénatomszámúalkilcsoport és n értéke 1 vagy 2; vagy A jelentése -N(R')- és Rjelentése kis szénatomszámú alkil-, 4-6 szénatomos cikloalkil-, -(CH2)n-O-kis szénatomszámú alkil-, -(CH2)n-piridinil-, -(CH2)n- -piperidinil-, -(CH2)n-fenil-, -(CH2)n-N(R")-C(O)-kis szénatomszámúalkil-, -(CH2)n-morfolinil- vagy -(CH2)n-N(R")2; R' és R" jelentéseegymástól függetlenül hidrogénatom vagy kis szénatomszámú alkilcsoportés n értéke 1 vagy 2; vagy A jelentése -CH2- és R jelentése -N(R")-(CH2)m,-O-kis szénatomszámú alkil-, -N(R")2, S-kis szénatomszámúalkil- vagy acetidinil-, pirrolidinil- vagy piperidinilcsoport, amelycsoportok adott esetben hidroxi- vagy kis szénatomszámúalkoxicsoporttal helyettesítve lehetnek; vagy jelentése morfolinil-, -N(R")-(CH2)m-C4-6-cikloalkil-, -N(R")-(CH2)m-C(O)O-kis szénatomszámúalkil-, -N(R")-(CH2)m-C(O)OH, -2-oxo-pirrolidinil-, -N(R")-C(O)O-kisszénatomszámú alkil-, -O(CH2)m-O-kis szénatomszámú alkil- vagyalkoxicsoport; R" egymástól függetlenül hidrogénatom vagy kisszénatomszámú alkilcsoport és m értéke 1, 2 vagy 3; vagy A jelentése -S- és R jelentése kis szénatomszámú alkilcsoport; vagy A-R együtt kisszénatomszámú alkil-, -C(O)-kis szénatomszámú alkil- vagyoxocsoporttal helyettesített piperazinilcsoportot; kis szénatomszámúalkoxi- vagy hidroxilcsoporttal helyettesített piperidinilcsoportot;kis szénatomszámú alkilcsoporttal helyettesített morfolinilcsoportot;4-6 szénatomos cikloalkilcsoportot; adott esetben hidroxi- vagy kisszénatomszámú alkoxicsoporttal helyettesített azetidin-l-il-csoportot;tiomorfolin-l,l-dioxo-, tetrahidropirano- vagy 2-oxa-5-aza-biciklo[2.2.1]hept-5-il-csoportot képez. Azt találták, hogy az (I)általános képletű vegyületek adenozin receptor ligandok; specifikusana találmány szerinti vegyületek az A2A receptorhoz jó affinitástmutatnak és ezért ezzel a receptorral kapcsolatos betegségekkezelésére alkalmazhatók. A találmány kiterjed a vegyületekelőállítására és ezeket tartalmazó gyógyszerkészítményekre. Ó
HU0402161A 2001-11-19 2002-11-11 Nicotin-or isonicotin benzothiazole derivatives, process for their preparation and pharmaceutical compositions containing them HUP0402161A3 (en)

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
HUP0402161A2 true HUP0402161A2 (hu) 2005-02-28
HUP0402161A3 HUP0402161A3 (en) 2010-06-28

Family

ID=8179263

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HU0402161A HUP0402161A3 (en) 2001-11-19 2002-11-11 Nicotin-or isonicotin benzothiazole derivatives, process for their preparation and pharmaceutical compositions containing them

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US (1) US6620811B2 (hu)
EP (1) EP1448198B1 (hu)
JP (1) JP4226474B2 (hu)
KR (1) KR100577110B1 (hu)
CN (1) CN100546580C (hu)
AR (1) AR039367A1 (hu)
AT (1) ATE376831T1 (hu)
AU (1) AU2002351955B2 (hu)
BR (1) BR0214245A (hu)
CA (1) CA2467552C (hu)
DE (1) DE60223278T2 (hu)
DK (1) DK1448198T3 (hu)
EA (1) EA007502B1 (hu)
EC (1) ECSP045109A (hu)
ES (1) ES2294187T3 (hu)
GT (1) GT200200232A (hu)
HR (1) HRP20040396A2 (hu)
HU (1) HUP0402161A3 (hu)
IL (2) IL161623A0 (hu)
JO (1) JO2290B1 (hu)
MA (1) MA27083A1 (hu)
MX (1) MXPA04004684A (hu)
MY (1) MY126176A (hu)
NO (1) NO20042576L (hu)
NZ (1) NZ532802A (hu)
PA (1) PA8558001A1 (hu)
PE (1) PE20030713A1 (hu)
PL (1) PL369517A1 (hu)
PT (1) PT1448198E (hu)
RS (1) RS39904A (hu)
RU (1) RU2294933C2 (hu)
SI (1) SI1448198T1 (hu)
TN (1) TNSN04087A1 (hu)
TW (1) TW200407134A (hu)
UA (1) UA77462C2 (hu)
UY (1) UY27542A1 (hu)
WO (1) WO2003043636A1 (hu)
ZA (1) ZA200403817B (hu)

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Also Published As

Publication number Publication date
EA200400598A1 (ru) 2005-02-24
IL161623A0 (en) 2004-09-27
PA8558001A1 (es) 2003-07-28
EP1448198B1 (en) 2007-10-31
DE60223278T2 (de) 2008-08-14
WO2003043636A1 (en) 2003-05-30
HUP0402161A3 (en) 2010-06-28
HRP20040396A2 (en) 2005-04-30
PT1448198E (pt) 2007-12-11
GT200200232A (es) 2003-06-17
ECSP045109A (es) 2004-06-28
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AU2002351955A1 (en) 2003-06-10
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PL369517A1 (en) 2005-04-18
MA27083A1 (fr) 2004-12-20
CN100546580C (zh) 2009-10-07
RU2004118425A (ru) 2006-01-10
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US6620811B2 (en) 2003-09-16
ES2294187T3 (es) 2008-04-01
RS39904A (en) 2006-10-27
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US20030134854A1 (en) 2003-07-17
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SI1448198T1 (sl) 2008-02-29
DE60223278D1 (de) 2007-12-13
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MXPA04004684A (es) 2004-08-12
UA77462C2 (en) 2006-12-15
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