BRPI0414266A - derivados de tiazolopiridina como ligandos receptores da adenosina - Google Patents
derivados de tiazolopiridina como ligandos receptores da adenosinaInfo
- 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
Links
Classifications
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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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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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
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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
- 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
Landscapes
- 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.
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) |
Families Citing this family (28)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
FR2913886B1 (fr) | 2007-03-22 | 2012-03-02 | Guerbet Sa | Utilisation de nanoparticules metalliques dans le diagnostique de la maladie d'alzheimer |
TW200916472A (en) * | 2007-06-20 | 2009-04-16 | Sirtris Pharmaceuticals Inc | Sirtuin modulating compounds |
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 |
Family Cites Families (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2413086C (en) * | 2000-06-21 | 2011-06-28 | Alexander Alanine | Benzothiazole derivatives |
US6620811B2 (en) * | 2001-11-19 | 2003-09-16 | Hoffmann-La Roche Inc. | Isonicotin- and nicotinamide derivatives of benzothiazoles |
US6599901B1 (en) * | 2001-11-19 | 2003-07-29 | Hoffman-La Roche Inc. | Pyridone substituted benzothiazole derivatives |
US6624163B2 (en) * | 2001-11-29 | 2003-09-23 | Hoffman-La Roche Inc. | Benzothiazole derivatives |
US6727247B2 (en) * | 2001-12-10 | 2004-04-27 | Hoffman-La Roche Inc. | Substituted benzothiazole amide derivatives |
PL370980A1 (en) * | 2001-12-12 | 2005-06-13 | F.Hoffmann-La Roche Ag | Benzothiophenes as adenosine receptor modulators |
US6734179B2 (en) * | 2001-12-12 | 2004-05-11 | Hoffmann-La Roche Inc. | Benzothiazoles |
US6713499B2 (en) * | 2001-12-12 | 2004-03-30 | Hoffman-La Roche Inc. | 7-Amino-benzothiazole derivatives |
-
2004
- 2004-09-11 MX MXPA06002943A patent/MXPA06002943A/es not_active Application Discontinuation
- 2004-09-11 EP EP04765102A patent/EP1670805A1/en not_active Ceased
- 2004-09-11 CA CA002539314A patent/CA2539314A1/en not_active Abandoned
- 2004-09-11 KR KR1020067005454A patent/KR20060058132A/ko not_active Application Discontinuation
- 2004-09-11 JP JP2006526568A patent/JP2007505851A/ja active Pending
- 2004-09-11 WO PCT/EP2004/010179 patent/WO2005028484A1/en active Application Filing
- 2004-09-11 AU AU2004274154A patent/AU2004274154A1/en not_active Abandoned
- 2004-09-11 CN CNA2004800309594A patent/CN1871244A/zh active Pending
- 2004-09-11 RU RU2006112847/04A patent/RU2006112847A/ru not_active Application Discontinuation
- 2004-09-11 BR BRPI0414266-7A patent/BRPI0414266A/pt not_active IP Right Cessation
- 2004-09-15 US US10/941,708 patent/US7273865B2/en not_active Expired - Fee Related
- 2004-09-16 TW TW093128066A patent/TWI297339B/zh not_active IP Right Cessation
- 2004-09-16 AR ARP040103313A patent/AR045659A1/es not_active Application Discontinuation
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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Legal Events
Date | Code | Title | Description |
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B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE AS 6A E 7A ANUIDADES. |
|
B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2159 DE 22/05/2012. |