BR112015007991A2 - derivados de etinila como moduladores da atividade do receptor de mglur5 - Google Patents
derivados de etinila como moduladores da atividade do receptor de mglur5Info
- Publication number
- BR112015007991A2 BR112015007991A2 BR112015007991A BR112015007991A BR112015007991A2 BR 112015007991 A2 BR112015007991 A2 BR 112015007991A2 BR 112015007991 A BR112015007991 A BR 112015007991A BR 112015007991 A BR112015007991 A BR 112015007991A BR 112015007991 A2 BR112015007991 A2 BR 112015007991A2
- Authority
- BR
- Brazil
- Prior art keywords
- modulators
- receptor activity
- mglur5 receptor
- ethinyl
- derivatives
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
-
- 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
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P25/14—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
- A61P25/24—Antidepressants
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Epidemiology (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
resumo patente de invenção: "derivados de etinila como moduladores da atividade do receptor de mglur5". a presente invenção refere-se aos derivados de etinila da fórmula (i) ou a um sal de adição de ácido farmaceuticamente aceitável, a uma mistura racêmica, ou aos seus enantiômero e/ou isômero óptico e/ou estereoisômero correspondentes dos mesmos. foi agora surpreendentemente descoberto que os compostos da fórmula geral (i) são agonistas do receptor de glutamato metabotrópico (moduladores alostéricos negativos) para o uso no tratamento de ansiedade e dor, depressão, síndrome do x frágil, distúrbios do espectro autista, doença de parkinson, e doença do refluxo gastroesofágico (gerd).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12189015 | 2012-10-18 | ||
| PCT/EP2013/071493 WO2014060394A1 (en) | 2012-10-18 | 2013-10-15 | Ethynyl derivatives as modulators of mglur5 receptor activity |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112015007991A2 true BR112015007991A2 (pt) | 2017-07-04 |
Family
ID=47049073
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112015007991A BR112015007991A2 (pt) | 2012-10-18 | 2013-10-15 | derivados de etinila como moduladores da atividade do receptor de mglur5 |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US9328070B2 (pt) |
| EP (1) | EP2909179B1 (pt) |
| JP (1) | JP5989253B2 (pt) |
| KR (1) | KR101656634B1 (pt) |
| CN (1) | CN104718191B (pt) |
| AR (1) | AR093043A1 (pt) |
| AU (1) | AU2013333984B2 (pt) |
| BR (1) | BR112015007991A2 (pt) |
| CA (1) | CA2882484A1 (pt) |
| CL (1) | CL2015000708A1 (pt) |
| CR (1) | CR20150143A (pt) |
| EA (1) | EA025668B1 (pt) |
| ES (1) | ES2599509T3 (pt) |
| HK (1) | HK1208032A1 (pt) |
| IL (1) | IL237116A (pt) |
| MA (1) | MA38011B1 (pt) |
| MX (1) | MX2015004086A (pt) |
| MY (1) | MY170152A (pt) |
| PE (1) | PE20150628A1 (pt) |
| PH (1) | PH12015500496B1 (pt) |
| SG (1) | SG11201501375YA (pt) |
| TW (1) | TWI468393B (pt) |
| UA (1) | UA114934C2 (pt) |
| WO (1) | WO2014060394A1 (pt) |
| ZA (1) | ZA201500896B (pt) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104603110B (zh) * | 2012-10-18 | 2016-08-31 | 霍夫曼-拉罗奇有限公司 | 作为mGluR5受体活性的调节剂的乙炔基衍生物 |
| DK3322701T3 (da) | 2015-07-15 | 2019-07-08 | H Hoffmann La Roche Ag | Ethynylderivater som metabotropiske glutamatreceptormodulatorer |
| KR20190026805A (ko) | 2016-07-18 | 2019-03-13 | 에프. 호프만-라 로슈 아게 | 에틴일 유도체 |
| KR102027368B1 (ko) * | 2018-05-29 | 2019-10-01 | 서울대학교산학협력단 | 통증의 강도를 측정하는 방법 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW544448B (en) * | 1997-07-11 | 2003-08-01 | Novartis Ag | Pyridine derivatives |
| US8853392B2 (en) * | 2007-06-03 | 2014-10-07 | Vanderbilt University | Benzamide mGluR5 positive allosteric modulators and methods of making and using same |
| AU2008259776A1 (en) * | 2007-06-03 | 2008-12-11 | Vanderbilt University | Benzamide mGluR5 positive allosteric modulators and methods of making and using same |
| KR20100087296A (ko) * | 2007-09-28 | 2010-08-04 | 이 아이 듀폰 디 네모아 앤드 캄파니 | 이온성 액체 안정화제 조성물 |
| TW201124391A (en) * | 2009-10-20 | 2011-07-16 | Lundbeck & Co As H | 2-substituted-ethynylthiazole derivatives and uses of same |
| US8389536B2 (en) * | 2009-10-27 | 2013-03-05 | Hoffmann-La Roche Inc. | Positive allosteric modulators (PAM) |
| US8772300B2 (en) * | 2011-04-19 | 2014-07-08 | Hoffmann-La Roche Inc. | Phenyl or pyridinyl-ethynyl derivatives |
-
2013
- 2013-10-15 AU AU2013333984A patent/AU2013333984B2/en not_active Ceased
- 2013-10-15 CN CN201380053650.6A patent/CN104718191B/zh not_active Expired - Fee Related
- 2013-10-15 SG SG11201501375YA patent/SG11201501375YA/en unknown
- 2013-10-15 PE PE2015000395A patent/PE20150628A1/es not_active Application Discontinuation
- 2013-10-15 UA UAA201504379A patent/UA114934C2/uk unknown
- 2013-10-15 MY MYPI2015000492A patent/MY170152A/en unknown
- 2013-10-15 JP JP2015537221A patent/JP5989253B2/ja not_active Expired - Fee Related
- 2013-10-15 WO PCT/EP2013/071493 patent/WO2014060394A1/en active Application Filing
- 2013-10-15 MX MX2015004086A patent/MX2015004086A/es unknown
- 2013-10-15 CA CA2882484A patent/CA2882484A1/en not_active Abandoned
- 2013-10-15 EP EP13776810.7A patent/EP2909179B1/en not_active Not-in-force
- 2013-10-15 EA EA201590722A patent/EA025668B1/ru not_active IP Right Cessation
- 2013-10-15 BR BR112015007991A patent/BR112015007991A2/pt active Search and Examination
- 2013-10-15 ES ES13776810.7T patent/ES2599509T3/es active Active
- 2013-10-15 KR KR1020157009546A patent/KR101656634B1/ko active IP Right Grant
- 2013-10-17 AR ARP130103765A patent/AR093043A1/es unknown
- 2013-10-17 TW TW102137557A patent/TWI468393B/zh not_active IP Right Cessation
-
2015
- 2015-02-05 IL IL237116A patent/IL237116A/en not_active IP Right Cessation
- 2015-02-06 ZA ZA2015/00896A patent/ZA201500896B/en unknown
- 2015-03-06 PH PH12015500496A patent/PH12015500496B1/en unknown
- 2015-03-18 CR CR20150143A patent/CR20150143A/es unknown
- 2015-03-20 CL CL2015000708A patent/CL2015000708A1/es unknown
- 2015-04-17 MA MA38011A patent/MA38011B1/fr unknown
- 2015-04-17 US US14/689,366 patent/US9328070B2/en not_active Expired - Fee Related
- 2015-09-08 HK HK15108720.3A patent/HK1208032A1/zh not_active IP Right Cessation
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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] | ||
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 6A 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 2536 DE 13-08-2019 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. |
|
| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] |