MA38011A1 - 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
- MA38011A1 MA38011A1 MA38011A MA38011A MA38011A1 MA 38011 A1 MA38011 A1 MA 38011A1 MA 38011 A MA38011 A MA 38011A MA 38011 A MA38011 A MA 38011A MA 38011 A1 MA38011 A1 MA 38011A1
- 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)
- 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)
- 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 true MA38011A1 (fr) | 2016-01-29 |
| MA38011B1 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 (25)
| 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) |
| HK (1) | HK1208032A1 (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 (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2879489A1 (fr) * | 2012-10-18 | 2014-04-24 | F.Hoffmann-La Roche Ag | Derives d'ethynyl utilises en tant que modulateurs de l'activite des recepteurs mglur5 |
| JP6761821B2 (ja) | 2015-07-15 | 2020-09-30 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | 代謝性グルタミン酸受容体モジュレーターとしてのエチニル誘導体 |
| SG11201811829QA (en) | 2016-07-18 | 2019-02-27 | Hoffmann La Roche | Ethynyl derivatives |
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 |
| NZ581817A (en) * | 2007-06-03 | 2012-05-25 | Univ Vanderbilt | Benzamide mglur5 positive allosteric modulators and methods of making and using same |
| EP2190487A1 (fr) * | 2007-09-28 | 2010-06-02 | E. I. du Pont de Nemours and Company | Compositions stabilisatrices à base d'un liquide ionique |
| 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 KR KR1020157009546A patent/KR101656634B1/ko active IP Right Grant
- 2013-10-15 JP JP2015537221A patent/JP5989253B2/ja not_active Expired - Fee Related
- 2013-10-15 MY MYPI2015000492A patent/MY170152A/en unknown
- 2013-10-15 WO PCT/EP2013/071493 patent/WO2014060394A1/fr active Application Filing
- 2013-10-15 CA CA2882484A patent/CA2882484A1/fr not_active Abandoned
- 2013-10-15 CN CN201380053650.6A patent/CN104718191B/zh not_active Expired - Fee Related
- 2013-10-15 BR BR112015007991A patent/BR112015007991A2/pt active Search and Examination
- 2013-10-15 AU AU2013333984A patent/AU2013333984B2/en not_active Ceased
- 2013-10-15 MX MX2015004086A patent/MX2015004086A/es unknown
- 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 PE PE2015000395A patent/PE20150628A1/es not_active Application Discontinuation
- 2013-10-15 ES ES13776810.7T patent/ES2599509T3/es active Active
- 2013-10-15 EP EP13776810.7A patent/EP2909179B1/fr not_active Not-in-force
- 2013-10-15 SG SG11201501375YA patent/SG11201501375YA/en unknown
- 2013-10-17 TW TW102137557A patent/TWI468393B/zh not_active IP Right Cessation
- 2013-10-17 AR ARP130103765A patent/AR093043A1/es unknown
-
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 US US14/689,366 patent/US9328070B2/en not_active Expired - Fee Related
- 2015-04-17 MA MA38011A patent/MA38011B1/fr unknown
- 2015-09-08 HK HK15108720.3A patent/HK1208032A1/zh not_active IP Right Cessation
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 | |
| EA201070535A1 (ru) | Новые агонисты глюкокортикоидных рецепторов | |
| 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. | |
| MA35133B1 (fr) | Dérivés d'éthynyle comme modulateurs allostériques positifs de mglur5 | |
| MA35062B1 (fr) | Dérivés d'amines hétérocycliques | |
| MA38260A1 (fr) | Nouveaux dérivés de cyclohexyl et quinuclidinyl carbamate ayant une activité d'agoniste adrénergique beta2 et une activité d'antagoniste muscarinique m3 | |
| TN2016000188A1 (fr) | Derives de purines 2,6-substitues et leur utilisation dans le traitement de troubles proliferatifs. | |
| MA38217A1 (fr) | Nouveaux dérivés de pyrazine comme agonistes des récepteurs cb2 | |
| MA38659B1 (fr) | Dérivés éthynyle comme antagonistes du récepteur métabotrope du glutamate | |
| 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 | |
| MA38011B1 (fr) | Dérivés d'éthynyle comme modulateurs de l'activité du récepteur mglur5 | |
| MA38885A1 (fr) | Dérivés d'éthynyle modulateurs allosteriques positifs (pam) du recepteur metabotropique du glutamate 4 (mglu4) | |
| MA29809B1 (fr) | N-[1,3,4]-thiadiazol-2-yl-benzenesulfonamides,procedes pour leur preparation et leur utilisation en tant que produits pharmaceutiques | |
| PH12015500346A1 (en) | Ethynyl derivatives as modulators of mglur5 receptor activity | |
| MA45665B1 (fr) | Dérivés d'éthynyle | |
| TN2015000240A1 (fr) | Derives d'aminocyclobutane, leur procede de preparation et leur utilisation a titre de medicaments | |
| MA42508B1 (fr) | Dérivés d'éthynyle |