BRPI0414266A - derivados de tiazolopiridina como ligandos receptores da adenosina - Google Patents

derivados de tiazolopiridina como ligandos receptores da adenosina

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Publication number
BRPI0414266A
BRPI0414266A BRPI0414266-7A BRPI0414266A BRPI0414266A BR PI0414266 A BRPI0414266 A BR PI0414266A BR PI0414266 A BRPI0414266 A BR PI0414266A BR PI0414266 A BRPI0414266 A BR PI0414266A
Authority
BR
Brazil
Prior art keywords
lower alkyl
disease
heterocyclyl
compounds
substituents selected
Prior art date
Application number
BRPI0414266-7A
Other languages
English (en)
Inventor
Roger David Norcross
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 BRPI0414266A publication Critical patent/BRPI0414266A/pt

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    • 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
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • 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
    • A61P25/36—Opioid-abuse
    • 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
    • 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
    • A61P9/10—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)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

"DERIVADOS DE TIAZOLOPIRIDINA COMO LIGANDOS RECEPTORES DA ADENOSINA". A presente invenção diz respeito aos compostos da fórmula geral (I) em que R¬ 1¬ é morfolin-4-ila, fenila ou tetraidropiran-4-ila; R¬ 2¬ é -(CH~ 2~)~ n~-arila, não substituída ou substituída por um ou mais substituintes, selecionados do grupo consistindo de halogeno, alcóxi inferior, alquila inferior, -(CH~ 2~)~ n~NR<39>R<39><39>, -O(CH~ 2~)~ n~-O-alquila inferior, ou -(CH~ 2~)~ n~-heterociclila, ou é heteroarila, não substituída ou substituída por um ou mais substituintes, selecionados do grupo consistindo de alquila inferior, alcóxi inferior, -(CH~ 2~)~ n~ NR<39>R<39><39>, -(CH~ 2~)~ n~heterociclila, que é opcionalmente substituída por hidróxi ou alcóxi inferior, ou é -(CH~ 2~)~ n~-heterociclila, opcionalmente substituída por um ou mais substituintes selecionados do grupo consistindo de -(CH~ 2~)~ n~-OH, -(CH~ 2~)~ n~-O-alquila inferior ou alquila inferior, ou é -(CH~ 2~)~ n~-cicloalquila, ou é -(CH~ 2~)~ n~-O-alquila inferior, ou é NR<39>R<39><39>, ou é benzo¢1,3!dioxol, 2-metil-1-oxo-2,8-diaza-espiro ¢4,5!decano, 2-oxa-5-aza-biciclo¢2,2,1!heptano ou 1-oxa-8-aza-espiro ¢4,5! decano; R<39>,R<39><39> são independentemente um do outro alquila inferior, -(CH~ 2~)~ n~O-alquila inferior ou cicloalquila, opcionalmente substituída por hidróxi; n é 0, 1 ou 2; e aos sais de adição de ácido farmaceuticamente aceitáveis destes. Estes compostos podem ser utilizados no controle ou prevenção de enfermidades que se baseiam na modulação do sistema de adenosina, tal como doença de Alzheimer, doença de Parkinson, doença de Huntington, neuro-proteção, esquizofrenia, ansiedade, dor, déficit da respiração, depressão, vício de drogas, tais como anfetamina, cocaína, opióides, etanol, nicotina, canabinóides, ou contra asma, respostas alérgicas, hipoxia, isquemia, ataque apoplético e abuso de substâncias. Além disso, os compostos da presente invenção podem ser úteis como sedativos, relaxantes musculares, antipsicóticos, antiepilépticos, anticonvulsivantes e agentes cardioprotetores para os distúrbios tais como doença da artéria coronária e insuficiência cardíaca. As indicações mais preferíveis de acordo com a presente invenção são aquelas que incluem os distúrbios do sistema nervoso central, por exemplo, o tratamento ou prevenção da doença de Alzheimer, certos distúrbios depressivos, vício de drogas, neuroproteção e doença de Parkinson assim como ADHD.
BRPI0414266-7A 2003-09-19 2004-09-11 derivados de tiazolopiridina como ligandos receptores da adenosina BRPI0414266A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP03021119 2003-09-19
PCT/EP2004/010179 WO2005028484A1 (en) 2003-09-19 2004-09-11 Thiazolopyridine derivatives as adenosine receptor ligands

Publications (1)

Publication Number Publication Date
BRPI0414266A true BRPI0414266A (pt) 2006-11-07

Family

ID=34306777

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0414266-7A BRPI0414266A (pt) 2003-09-19 2004-09-11 derivados de tiazolopiridina como ligandos receptores da adenosina

Country Status (13)

Country Link
US (1) US7273865B2 (pt)
EP (1) EP1670805A1 (pt)
JP (1) JP2007505851A (pt)
KR (1) KR20060058132A (pt)
CN (1) CN1871244A (pt)
AR (1) AR045659A1 (pt)
AU (1) AU2004274154A1 (pt)
BR (1) BRPI0414266A (pt)
CA (1) CA2539314A1 (pt)
MX (1) MXPA06002943A (pt)
RU (1) RU2006112847A (pt)
TW (1) TWI297339B (pt)
WO (1) WO2005028484A1 (pt)

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SE521512C2 (sv) 2001-06-25 2003-11-11 Niconovum Ab Anordning för administrering av en substans till främre delen av en individs munhåla
SI1578422T1 (sl) 2002-12-20 2007-12-31 Niconovum Ab Fizikalno in kemiäśno stabilni nikotin in mikrokristal na celulozo vsebujoäś material iz trdnih delcev
EP1853610A1 (en) * 2005-03-03 2007-11-14 Sirtris Pharmaceuticals, Inc. N-phenyl benzamide derivatives as sirtuin modulators
US8088928B2 (en) * 2005-08-04 2012-01-03 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
US8093401B2 (en) * 2005-08-04 2012-01-10 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
AU2006278397B2 (en) 2005-08-04 2013-01-17 Sirtris Pharmaceuticals, Inc. Oxazolopyridine derivatives as sirtuin modulators
US7855289B2 (en) 2005-08-04 2010-12-21 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
WO2007101270A1 (en) * 2006-03-02 2007-09-07 Incyte Corporation MODULATORS OF 11-β HYDROXYL STEROID DEHYDROGENASE TYPE 1, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USING THE SAME
AU2007224584A1 (en) 2006-03-16 2007-09-20 Niconovum Ab Improved snuff composition
CA2649677A1 (en) * 2006-05-01 2007-11-15 Incyte Corporation Tetrasubstituted ureas as modulators of 11-.beta. hydroxyl steroid dehydrogenase type 1
CN101448844B (zh) * 2006-05-18 2012-07-25 霍夫曼-拉罗奇有限公司 作为腺苷a2b受体拮抗剂的噻唑并嘧啶/吡啶脲衍生物
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BRPI0819093A2 (pt) * 2007-11-01 2017-05-02 Sirtris Pharmaceuticals Inc compostos moduladores de sirtuína
EP2217606A1 (en) * 2007-11-08 2010-08-18 Sirtris Pharmaceuticals, Inc. Solubilized thiazolopyridines
SG171835A1 (en) 2008-12-19 2011-07-28 Sirtris Pharmaceuticals Inc Thiazolopyridine sirtuin modulating compounds
AU2014347027A1 (en) 2013-11-06 2016-06-23 Bristol-Myers Squibb Company GSK -3 inhibitors
AU2014347026A1 (en) 2013-11-06 2016-06-23 Bristol-Myers Squibb Company Substituted pyridine derivatives useful as GSK-3 inhibitors
WO2015091584A1 (en) * 2013-12-18 2015-06-25 F. Hoffmann-La Roche Ag Thiazolopyridine compounds, compositions and their use as tyk2 kinase inhibitors
CN103720703A (zh) * 2013-12-24 2014-04-16 新乡医学院第一附属医院 腺苷a2a受体特异性阻断剂对延髓呼吸中枢的作用
IT201600070952A1 (it) * 2016-07-07 2018-01-07 Univ Degli Studi Di Ferrara NUOVI TIAZOLO[5,4-d]PIRIMIDIN DERIVATI QUALI AGONISTI INVERSI DEI RECETTORI A2A DELL’ADENOSINA
PL3661941T3 (pl) * 2017-08-01 2023-05-08 Merck Patent Gmbh Pochodne tiazolopirydynowe jako antagoniści receptora adenozynowego
IL272637B2 (en) 2017-08-21 2024-03-01 Merck Patent Gmbh History of benzaimidazole, their preparation and medicines containing them
US11192899B2 (en) 2017-08-21 2021-12-07 Merck Patent Gmbh Quinoxaline derivatives as adenosine receptor antagonists
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
WO2020083856A1 (en) 2018-10-25 2020-04-30 Merck Patent Gmbh 5-azaindazole derivatives as adenosine receptor antagonists
CN111205244B (zh) * 2018-11-22 2023-08-18 上海科技大学 噻唑并环类化合物、其制备方法、中间体和应用
AR117844A1 (es) * 2019-01-22 2021-09-01 Merck Patent Gmbh Derivados de tiazolopiridina como antagonistas del receptor de adenosina

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CA2413086C (en) * 2000-06-21 2011-06-28 Alexander Alanine Benzothiazole derivatives
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US6713499B2 (en) * 2001-12-12 2004-03-30 Hoffman-La Roche Inc. 7-Amino-benzothiazole derivatives

Also Published As

Publication number Publication date
EP1670805A1 (en) 2006-06-21
US7273865B2 (en) 2007-09-25
AU2004274154A1 (en) 2005-03-31
KR20060058132A (ko) 2006-05-29
TWI297339B (en) 2008-06-01
RU2006112847A (ru) 2007-11-10
CA2539314A1 (en) 2005-03-31
WO2005028484A1 (en) 2005-03-31
JP2007505851A (ja) 2007-03-15
TW200526670A (en) 2005-08-16
MXPA06002943A (es) 2006-05-31
CN1871244A (zh) 2006-11-29
AR045659A1 (es) 2005-11-02
US20050065151A1 (en) 2005-03-24

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B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

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