MA38011B1 - Dérivés d'éthynyle comme modulateurs de l'activité du récepteur mglur5 - Google Patents
Dérivés d'éthynyle comme modulateurs de l'activité du récepteur mglur5Info
- Publication number
- MA38011B1 MA38011B1 MA38011A MA38011A MA38011B1 MA 38011 B1 MA38011 B1 MA 38011B1 MA 38011 A MA38011 A MA 38011A MA 38011 A MA38011 A MA 38011A MA 38011 B1 MA38011 B1 MA 38011B1
- Authority
- MA
- Morocco
- Prior art keywords
- modulators
- ethynyl derivatives
- receptor activity
- mglur5 receptor
- disease
- 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)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Epidemiology (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
La présente invention concerne des dérivés d'éthynyle de formule (i) ou leur sel d'addition aux acides pharmaceutiquement acceptables, leur mélange racémique, ou leur énantiomère et/ou isomère optique et/ou stéréoisomère correspondant. Il a été découvert avec surprise que les composés de formule générale (i) sont des antagonistes des récepteurs métabotropes au glutamate (modulateurs allostériques négatifs) destinés à être utilisés dans le traitement de l'anxiété et de la douleur, de la dépression, du syndrome de l'x fragile, des troubles du spectre autistique, de la maladie de parkinson et de la maladie du reflux gastroœsophagien.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12189015 | 2012-10-18 | ||
| PCT/EP2013/071493 WO2014060394A1 (fr) | 2012-10-18 | 2013-10-15 | Dérivés d'éthynyle comme modulateurs de l'activité du récepteur mglur5 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MA38011A1 MA38011A1 (fr) | 2016-01-29 |
| MA38011B1 true MA38011B1 (fr) | 2016-10-31 |
Family
ID=47049073
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MA38011A MA38011B1 (fr) | 2012-10-18 | 2015-04-17 | Dérivés d'éthynyle comme modulateurs de l'activité du récepteur mglur5 |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US9328070B2 (fr) |
| EP (1) | EP2909179B1 (fr) |
| JP (1) | JP5989253B2 (fr) |
| KR (1) | KR101656634B1 (fr) |
| CN (1) | CN104718191B (fr) |
| AR (1) | AR093043A1 (fr) |
| AU (1) | AU2013333984B2 (fr) |
| BR (1) | BR112015007991A2 (fr) |
| CA (1) | CA2882484A1 (fr) |
| CL (1) | CL2015000708A1 (fr) |
| CR (1) | CR20150143A (fr) |
| EA (1) | EA025668B1 (fr) |
| ES (1) | ES2599509T3 (fr) |
| IL (1) | IL237116A (fr) |
| MA (1) | MA38011B1 (fr) |
| MX (1) | MX2015004086A (fr) |
| MY (1) | MY170152A (fr) |
| PE (1) | PE20150628A1 (fr) |
| PH (1) | PH12015500496A1 (fr) |
| SG (1) | SG11201501375YA (fr) |
| TW (1) | TWI468393B (fr) |
| UA (1) | UA114934C2 (fr) |
| WO (1) | WO2014060394A1 (fr) |
| ZA (1) | ZA201500896B (fr) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA114008C2 (xx) * | 2012-10-18 | 2017-04-10 | Похідні етинілу як модулятори активності рецептора mglur5 | |
| KR20180026438A (ko) | 2015-07-15 | 2018-03-12 | 에프. 호프만-라 로슈 아게 | 대사형 글루타메이트 수용체 조절제로서의 에틴일 유도체 |
| PL3484889T3 (pl) | 2016-07-18 | 2020-12-28 | F. Hoffmann-La Roche Ag | Pochodne etynylu |
| 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 |
| CA2689282A1 (fr) * | 2007-06-03 | 2008-12-11 | Vanderbilt University | Derives benzamides modulateurs allosteriques positifs recepteurs metabotropiques du glutamate 5 (mglur5) et leurs procedes de fabrication et d'utilisation |
| US8853392B2 (en) * | 2007-06-03 | 2014-10-07 | Vanderbilt University | Benzamide mGluR5 positive allosteric modulators and methods of making and using same |
| CN101970018A (zh) * | 2007-09-28 | 2011-02-09 | 纳幕尔杜邦公司 | 离子液体稳定剂组合物 |
| 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 SG SG11201501375YA patent/SG11201501375YA/en unknown
- 2013-10-15 CN CN201380053650.6A patent/CN104718191B/zh not_active Expired - Fee Related
- 2013-10-15 EP EP13776810.7A patent/EP2909179B1/fr not_active Not-in-force
- 2013-10-15 ES ES13776810.7T patent/ES2599509T3/es active Active
- 2013-10-15 CA CA2882484A patent/CA2882484A1/fr not_active Abandoned
- 2013-10-15 MX MX2015004086A patent/MX2015004086A/es unknown
- 2013-10-15 PE PE2015000395A patent/PE20150628A1/es not_active Application Discontinuation
- 2013-10-15 MY MYPI2015000492A patent/MY170152A/en unknown
- 2013-10-15 WO PCT/EP2013/071493 patent/WO2014060394A1/fr not_active Ceased
- 2013-10-15 EA EA201590722A patent/EA025668B1/ru not_active IP Right Cessation
- 2013-10-15 UA UAA201504379A patent/UA114934C2/uk unknown
- 2013-10-15 BR BR112015007991A patent/BR112015007991A2/pt active Search and Examination
- 2013-10-15 KR KR1020157009546A patent/KR101656634B1/ko not_active Expired - Fee Related
- 2013-10-15 JP JP2015537221A patent/JP5989253B2/ja not_active Expired - Fee Related
- 2013-10-15 AU AU2013333984A patent/AU2013333984B2/en not_active Ceased
- 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/PH12015500496A1/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
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| MA38012B1 (fr) | Dérivés d'éthynyle comme modulateurs de l'activité des récepteurs mglur5 | |
| MA42442B1 (fr) | Dérivés d'éthynyle comme modulateurs du récepteur métabotropique au glutamate | |
| CL2011001263A1 (es) | Compuestos derivados de pirimidinonas opcionalmente sustituidas; composicion farmaceutica que los comprende; y su uso como inhibidores de fosfodiesterasa 1 (pde1) para el tratamiento de enfermedades que involucran trastornos de la trayectoria intracelular del receptor de dopamina d1 como parkinson, alzheimer, depresion, enfermedad bipolar, hipertension, glaucoma. | |
| MA42239B1 (fr) | Nouveaux dérivés d'hydroxyester, leur procédé de préparation et compositions pharmaceutiques les contenant | |
| NI201100100A (es) | Moduladores de aril metil benzoquinazolinona alostéricos positivos del receptor m1. | |
| MA35062B1 (fr) | Dérivés d'amines hétérocycliques | |
| TN2016000188A1 (fr) | Derives de purines 2,6-substitues et leur utilisation dans le traitement de troubles proliferatifs. | |
| MA38079A1 (fr) | Composés de 2-phényl-5-hétérocyclyl-tétrahydro-2h-pyran-3-amine destinés à être utilisés dans le traitement du diabète et de ses troubles associés | |
| MA38217B1 (fr) | Nouveaux dérivés de pyrazine comme agonistes des récepteurs cb2 | |
| MA38260B1 (fr) | Nouveaux dérivés de cyclohexyl et quinuclidinyl carbamate ayant une activité d'agoniste adrénergique beta2 et une activité d'antagoniste muscarinique m3 | |
| MA38011B1 (fr) | Dérivés d'éthynyle comme modulateurs de l'activité du récepteur mglur5 | |
| TN2010000025A1 (fr) | Derives de l'indol -2-one disubstitues en 3, leur preparation et leur application en therapeutique | |
| EA201001586A1 (ru) | Соединения и композиции в качестве ингибиторов itpkb | |
| TN2015000240A1 (fr) | Derives d'aminocyclobutane, leur procede de preparation et leur utilisation a titre de medicaments | |
| MA38659B1 (fr) | Dérivés éthynyle comme antagonistes du récepteur métabotrope du glutamate | |
| MA38885A1 (fr) | Dérivés d'éthynyle modulateurs allosteriques positifs (pam) du recepteur metabotropique du glutamate 4 (mglu4) | |
| PH12015500346A1 (en) | Ethynyl derivatives as modulators of mglur5 receptor activity | |
| MA42508B1 (fr) | Dérivés d'éthynyle | |
| TH2001006044A (th) | อนุพันธ์ของพิราโซ-เททระไฮโดรไอโซควิโนลีนในฐานะเป็นตัวควบคุมเชิงบวกของตัวรับโดพามีน d1 | |
| MA34198B1 (fr) | Dérivés de chroménone convenant comme antagonistes trpv3 |