BRPI0410440A - derivados de benzotiazol como ligandos de receptor de adenosina - Google Patents

derivados de benzotiazol como ligandos de receptor de adenosina

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Publication number
BRPI0410440A
BRPI0410440A BRPI0410440-4A BRPI0410440A BRPI0410440A BR PI0410440 A BRPI0410440 A BR PI0410440A BR PI0410440 A BRPI0410440 A BR PI0410440A BR PI0410440 A BRPI0410440 A BR PI0410440A
Authority
BR
Brazil
Prior art keywords
optionally substituted
lower alkyl
oxa
aromatic heterocycle
alkyl
Prior art date
Application number
BRPI0410440-4A
Other languages
English (en)
Inventor
Alexandre Flohr
Roland Jakob-Roetne
Roger David Norcross
Claus Riemer
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of BRPI0410440A publication Critical patent/BRPI0410440A/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34Tobacco-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Anesthesiology (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

"DERIVADOS DE BENZOTIAZOL COMO LIGANDOS DE RECEPTOR DE ADENOSINA". A invenção diz respeito aos compostos da fórmula geral I em que R¬ 1¬ é 1,4-dioxepanila ou tetraidropiran-4-ila; R¬ 2¬ é N(R)-(CH~ 2~)~ n~-heterociclo não-aromático de 5 ou 6 membros, opcionalmente substituído por um ou mais substituintes, selecionados do grupo que consiste em alquila inferior ou NR¬ 2¬, ou -(CH~ 2~)~ n~-heterociclo não aromático de 5 ou 6 membros, opcionalmente substituído por -(CH~ 2~)~ n~-OH, alquila inferior, alcóxi inferior, ou é (CH~ 2~)~ n~-heterociclo aromático de 5 ou 6 membros, opcionalmente substituído por alquila inferior, alcóxi inferior, halógeno, halógeno-alquila inferior, - CH~ 2~N(R)(CH~ 2~)~ 2~0CH~ 3~, -N(R)(CH~ 2~)~ 2~0CH~ 3~,-CH~ 2~-morfolinila ou -CH~ 2~-Pirrolidinila ou é (CH~ 2)~ n~-cicloalquila, opcionalmente substituída por hidróxi, ou é -N(R)cicloalquila, opcionalmente substituída por hidróxi ou alquila inferior, ou é fenila, opcionalmente substituída por alcóxi inferior, halógeno, halógenoalquila inferior, alquila inferior, -CH~ 2~-Pirrolidin-l-ila, -CH~ 2~-Morfolinila, CH~ 2~N(R)(CH~ 2~)~ 2~0CH~ 3~ ou -CH~ 2~-N(R)C(O)-alquila inferior, ou é 1,4-dioxa-8-aza-espiro¢4.5!decano, ou é 2-oxa-5-aza-biciclo¢2.2.1!heptano, ou é l-oxa-8aza-espiro¢4.5!decano, ou é -N(R)-7-oxa-biciclo¢2.2.1!hept-2-ila, ou é 2-azabiciclo¢2.2.2!decano; R é hidrogênio ou alquila inferior; n é O ou 1; e sais de adição de ácido farmaceuticamente aceitáveis destes para o tratamento de doenças, que relacionam ao receptor A2A.
BRPI0410440-4A 2003-05-19 2004-05-14 derivados de benzotiazol como ligandos de receptor de adenosina BRPI0410440A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP03011039 2003-05-19
PCT/EP2004/005178 WO2005000842A1 (en) 2003-05-19 2004-05-14 Benzothiazole derivatives as adenosine receptor ligands

Publications (1)

Publication Number Publication Date
BRPI0410440A true BRPI0410440A (pt) 2006-06-06

Family

ID=33442729

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0410440-4A BRPI0410440A (pt) 2003-05-19 2004-05-14 derivados de benzotiazol como ligandos de receptor de adenosina

Country Status (28)

Country Link
US (1) US7371748B2 (pt)
EP (1) EP1636223B1 (pt)
JP (1) JP4444290B2 (pt)
KR (1) KR100859886B1 (pt)
CN (1) CN100528871C (pt)
AR (1) AR044362A1 (pt)
AT (1) ATE389652T1 (pt)
AU (1) AU2004251814B2 (pt)
BR (1) BRPI0410440A (pt)
CA (1) CA2524366C (pt)
CL (1) CL2004001067A1 (pt)
CO (1) CO5630031A2 (pt)
DE (1) DE602004012555T2 (pt)
DK (1) DK1636223T3 (pt)
ES (1) ES2301991T3 (pt)
HK (1) HK1092469A1 (pt)
HR (1) HRP20080207T3 (pt)
IL (1) IL171686A (pt)
MX (1) MXPA05012360A (pt)
NO (1) NO20055150L (pt)
NZ (1) NZ543074A (pt)
PL (1) PL1636223T3 (pt)
PT (1) PT1636223E (pt)
RU (1) RU2351597C2 (pt)
SI (1) SI1636223T1 (pt)
TW (1) TW200505882A (pt)
WO (1) WO2005000842A1 (pt)
ZA (1) ZA200509294B (pt)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008052930A2 (en) * 2006-11-03 2008-05-08 F. Hoffmann-La Roche Ag Preparation of 4-alk0xy-7- (tetrahydropyran-4-yl) benzothiazol-2-amine derivatives
IL272284B2 (en) 2017-08-01 2024-01-01 Merck Patent Gmbh History of thiazolopyridines, their preparation and pharmaceutical preparations containing them
JP7287952B2 (ja) 2017-08-21 2023-06-06 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング アデノシン受容体アンタゴニストとしてのベンズイミダゾール誘導体
WO2019038214A1 (en) 2017-08-21 2019-02-28 Merck Patent Gmbh QUINOXALINE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS
WO2019141096A1 (zh) * 2018-01-19 2019-07-25 四川科伦博泰生物医药股份有限公司 取代脲类化合物及其制备方法和用途
CN112867715B (zh) 2018-10-25 2024-03-05 默克专利股份公司 作为腺苷受体拮抗剂的5-氮杂吲唑衍生物
KR20210083293A (ko) 2018-10-25 2021-07-06 메르크 파텐트 게엠베하 아데노신 수용체 안타고니스트로서의 5-아자인다졸 유도체
AR117844A1 (es) 2019-01-22 2021-09-01 Merck Patent Gmbh Derivados de tiazolopiridina como antagonistas del receptor de adenosina

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1234358C (zh) * 2000-06-21 2006-01-04 弗·哈夫曼-拉罗切有限公司 苯并噻唑衍生物
EP1450796B1 (en) * 2001-11-27 2008-04-09 F. Hoffmann-La Roche Ag Benzothiazole derivatives
US6727247B2 (en) * 2001-12-10 2004-04-27 Hoffman-La Roche Inc. Substituted benzothiazole amide derivatives
US6734179B2 (en) * 2001-12-12 2004-05-11 Hoffmann-La Roche Inc. Benzothiazoles
PL378343A1 (pl) * 2003-01-13 2006-03-20 F. Hoffmann-La Roche Ag Pochodne benzoksazolu i ich zastosowanie jako ligandów receptora adenozyny

Also Published As

Publication number Publication date
CL2004001067A1 (es) 2005-04-15
PT1636223E (pt) 2008-05-06
DK1636223T3 (da) 2008-06-23
AU2004251814B2 (en) 2009-07-23
CA2524366A1 (en) 2005-01-06
JP4444290B2 (ja) 2010-03-31
RU2005139527A (ru) 2006-07-27
IL171686A (en) 2011-11-30
AR044362A1 (es) 2005-09-07
KR20060013406A (ko) 2006-02-09
CN100528871C (zh) 2009-08-19
NO20055150L (no) 2005-11-04
HRP20080207T3 (en) 2008-06-30
ATE389652T1 (de) 2008-04-15
RU2351597C2 (ru) 2009-04-10
ZA200509294B (en) 2006-10-25
US20040235915A1 (en) 2004-11-25
CA2524366C (en) 2012-03-13
AU2004251814A1 (en) 2005-01-06
MXPA05012360A (es) 2006-02-02
WO2005000842A1 (en) 2005-01-06
US7371748B2 (en) 2008-05-13
KR100859886B1 (ko) 2008-09-23
DE602004012555T2 (de) 2009-04-16
EP1636223A1 (en) 2006-03-22
DE602004012555D1 (de) 2008-04-30
CO5630031A2 (es) 2006-04-28
HK1092469A1 (en) 2007-02-09
EP1636223B1 (en) 2008-03-19
SI1636223T1 (sl) 2008-06-30
ES2301991T3 (es) 2008-07-01
PL1636223T3 (pl) 2008-07-31
NZ543074A (en) 2009-01-31
TW200505882A (en) 2005-02-16
CN1791600A (zh) 2006-06-21
JP2006528220A (ja) 2006-12-14

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Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B09B Patent application refused [chapter 9.2 patent gazette]
B09B Patent application refused [chapter 9.2 patent gazette]

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