BR112015006218A2 - derivados de ariletinil - Google Patents
derivados de ariletinilInfo
- Publication number
- BR112015006218A2 BR112015006218A2 BR112015006218A BR112015006218A BR112015006218A2 BR 112015006218 A2 BR112015006218 A2 BR 112015006218A2 BR 112015006218 A BR112015006218 A BR 112015006218A BR 112015006218 A BR112015006218 A BR 112015006218A BR 112015006218 A2 BR112015006218 A2 BR 112015006218A2
- Authority
- BR
- Brazil
- Prior art keywords
- formula
- compounds
- derivatives
- fluorophenyl
- arylethynyl
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- 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
-
- 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
- A61P25/06—Antimigraine agents
-
- 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
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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
- A61P25/34—Tobacco-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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- 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
- 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)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Urology & Nephrology (AREA)
- Physical Education & Sports Medicine (AREA)
- Cardiology (AREA)
- Ophthalmology & Optometry (AREA)
- Heart & Thoracic Surgery (AREA)
- Otolaryngology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Epidemiology (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pyridine Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
resumo patente de invenção: "derivados de ariletinil". i a presente invenção se refere a derivados de etinil da fórmula (i), na qual r1 é fenil, 3-fluorofenil. 4-fluorofenil ou 2,5-di-fluorofenil; ou a um sal de adição ácido farmaceuticamente aceitável, em forma enantioméricamente pura com configuração absoluta como mostrado na fórmula (i). foi descoberto agora de forma surpreendente que os compostos da fórmula geral 1 são moduladores alostéricos do sub tipo 5 do modulador metabrotópico glutamato (mglur5), que são uteis para o tratamento da esquizofrenia, distúrbios cognitivos, síndrome x frágil ou autismo e que exibe propriedades bioquímicas, físico químicas e fármaco dinâmicas vantajosas, quando comparados com os compostos da técnica precedente.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12186265 | 2012-09-27 | ||
| PCT/EP2013/069674 WO2014056710A1 (en) | 2012-09-27 | 2013-09-23 | Arylethynyl derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112015006218A2 true BR112015006218A2 (pt) | 2017-07-04 |
Family
ID=47044829
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112015006218A BR112015006218A2 (pt) | 2012-09-27 | 2013-09-23 | derivados de ariletinil |
Country Status (30)
| Country | Link |
|---|---|
| US (1) | US9221802B2 (pt) |
| EP (1) | EP2900659B1 (pt) |
| JP (1) | JP6027251B2 (pt) |
| KR (1) | KR101737245B1 (pt) |
| CN (1) | CN104684911B (pt) |
| AR (1) | AR092673A1 (pt) |
| AU (1) | AU2013329739B2 (pt) |
| BR (1) | BR112015006218A2 (pt) |
| CA (1) | CA2885382A1 (pt) |
| CL (1) | CL2015000707A1 (pt) |
| CR (1) | CR20150139A (pt) |
| DK (1) | DK2900659T3 (pt) |
| EA (1) | EA025482B1 (pt) |
| ES (1) | ES2594031T3 (pt) |
| HK (1) | HK1207376A1 (pt) |
| HU (1) | HUE029636T2 (pt) |
| IL (1) | IL237596A (pt) |
| MA (1) | MA37941B1 (pt) |
| MX (1) | MX366136B (pt) |
| MY (1) | MY171743A (pt) |
| NZ (1) | NZ706283A (pt) |
| PE (1) | PE20150708A1 (pt) |
| PH (1) | PH12015500538B1 (pt) |
| PL (1) | PL2900659T3 (pt) |
| SG (1) | SG11201502449RA (pt) |
| SI (1) | SI2900659T1 (pt) |
| TW (1) | TWI476194B (pt) |
| UA (1) | UA113779C2 (pt) |
| WO (1) | WO2014056710A1 (pt) |
| ZA (1) | ZA201501678B (pt) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA113223C2 (xx) * | 2012-08-13 | 2016-12-26 | Арилетинілпіримідини | |
| CA2879489A1 (en) * | 2012-10-18 | 2014-04-24 | F.Hoffmann-La Roche Ag | Ethynyl derivatives as modulators of mglur5 receptor activity |
| AU2016273751B2 (en) | 2015-06-03 | 2020-04-02 | F. Hoffmann-La Roche Ag | Ethynyl derivatives |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0325956D0 (en) | 2003-11-06 | 2003-12-10 | Addex Pharmaceuticals Sa | Novel compounds |
| WO2006048771A1 (en) | 2004-11-04 | 2006-05-11 | Addex Pharmaceuticals Sa | Novel tetrazole derivatives as positive allosteric modulators of metabotropic glutamate receptors |
| GB0510139D0 (en) | 2005-05-18 | 2005-06-22 | Addex Pharmaceuticals Sa | Novel compounds B1 |
| TW200811157A (en) * | 2006-05-05 | 2008-03-01 | Astrazeneca Ab | mGluR5 modulators I |
| NZ581817A (en) | 2007-06-03 | 2012-05-25 | Univ Vanderbilt | Benzamide mglur5 positive allosteric modulators and methods of making and using same |
| US8034806B2 (en) * | 2007-11-02 | 2011-10-11 | Vanderbilt University | Bicyclic mGluR5 positive allosteric modulators and methods of making and using same |
| TW201116532A (en) * | 2009-08-05 | 2011-05-16 | Merz Pharma Gmbh & Co Kgaa | Metabotropic glutamate receptor modulators |
| US8586581B2 (en) * | 2009-12-17 | 2013-11-19 | Hoffmann-La Roche Inc | Ethynyl compounds useful for treatment of CNS disorders |
| US8420661B2 (en) * | 2010-04-13 | 2013-04-16 | Hoffmann-La Roche Inc. | Arylethynyl derivatives |
-
2013
- 2013-09-23 DK DK13766286.2T patent/DK2900659T3/en active
- 2013-09-23 EP EP13766286.2A patent/EP2900659B1/en active Active
- 2013-09-23 CA CA2885382A patent/CA2885382A1/en not_active Abandoned
- 2013-09-23 UA UAA201503791A patent/UA113779C2/uk unknown
- 2013-09-23 JP JP2015533547A patent/JP6027251B2/ja active Active
- 2013-09-23 WO PCT/EP2013/069674 patent/WO2014056710A1/en active Application Filing
- 2013-09-23 BR BR112015006218A patent/BR112015006218A2/pt not_active IP Right Cessation
- 2013-09-23 KR KR1020157010351A patent/KR101737245B1/ko active IP Right Grant
- 2013-09-23 SI SI201330373A patent/SI2900659T1/sl unknown
- 2013-09-23 HU HUE13766286A patent/HUE029636T2/en unknown
- 2013-09-23 MY MYPI2015000777A patent/MY171743A/en unknown
- 2013-09-23 EA EA201590557A patent/EA025482B1/ru not_active IP Right Cessation
- 2013-09-23 CN CN201380050037.9A patent/CN104684911B/zh active Active
- 2013-09-23 NZ NZ706283A patent/NZ706283A/en not_active IP Right Cessation
- 2013-09-23 PE PE2015000422A patent/PE20150708A1/es active IP Right Grant
- 2013-09-23 SG SG11201502449RA patent/SG11201502449RA/en unknown
- 2013-09-23 ES ES13766286.2T patent/ES2594031T3/es active Active
- 2013-09-23 MX MX2015003560A patent/MX366136B/es active IP Right Grant
- 2013-09-23 AU AU2013329739A patent/AU2013329739B2/en not_active Ceased
- 2013-09-23 PL PL13766286T patent/PL2900659T3/pl unknown
- 2013-09-25 AR ARP130103433A patent/AR092673A1/es unknown
- 2013-09-26 TW TW102134845A patent/TWI476194B/zh not_active IP Right Cessation
-
2015
- 2015-03-05 IL IL237596A patent/IL237596A/en active IP Right Grant
- 2015-03-11 ZA ZA2015/01678A patent/ZA201501678B/en unknown
- 2015-03-12 PH PH12015500538A patent/PH12015500538B1/en unknown
- 2015-03-16 CR CR20150139A patent/CR20150139A/es unknown
- 2015-03-20 CL CL2015000707A patent/CL2015000707A1/es unknown
- 2015-03-20 MA MA37941A patent/MA37941B1/fr unknown
- 2015-03-26 US US14/669,653 patent/US9221802B2/en active Active
- 2015-08-19 HK HK15108049.7A patent/HK1207376A1/xx unknown
Also Published As
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 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] |
Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI |
|
| B06U | Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette] | ||
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 8A ANUIDADE. |
|
| 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: EM VIRTUDE DO ARQUIVAMENTO PUBLICADO NA RPI 2640 DE 10-08-2021 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDO O ARQUIVAMENTO DO PEDIDO DE PATENTE, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013. |