EA201590722A1 - Производные этинила в качестве модуляторов активности метаботропного глутаматного рецептора подтипа 5 - Google Patents
Производные этинила в качестве модуляторов активности метаботропного глутаматного рецептора подтипа 5Info
- Publication number
- EA201590722A1 EA201590722A1 EA201590722A EA201590722A EA201590722A1 EA 201590722 A1 EA201590722 A1 EA 201590722A1 EA 201590722 A EA201590722 A EA 201590722A EA 201590722 A EA201590722 A EA 201590722A EA 201590722 A1 EA201590722 A1 EA 201590722A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- glutamate receptor
- derivatives
- metabotropic glutamate
- ethynes
- subtle
- Prior art date
Links
Classifications
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- 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
Настоящее изобретение относится к производным этинила формулы Iили к их фармацевтически приемлемым солям присоединения кислоты, рацемическим смесям или соответствующим энантиомерам, и/или оптическим изомерам, и/или стереоизомерам. Неожиданно оказалось, что соединения общей формулы I являются антагонистами метаботропного глутаматного рецептора (негативные аллостерические модуляторы) для применения при лечении тревожности и боли, депрессии, синдрома ломкой Х-хромосомы, связанных с аутизмом расстройств, болезни Паркинсона и гастроэзофагеальной рефлюксной болезни (ГЭРБ).
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 (2)
| Publication Number | Publication Date |
|---|---|
| EA201590722A1 true EA201590722A1 (ru) | 2015-07-30 |
| EA025668B1 EA025668B1 (ru) | 2017-01-30 |
Family
ID=47049073
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201590722A EA025668B1 (ru) | 2012-10-18 | 2013-10-15 | Производные этинила в качестве модуляторов активности метаботропного глутаматного рецептора подтипа 5 |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US9328070B2 (ru) |
| EP (1) | EP2909179B1 (ru) |
| JP (1) | JP5989253B2 (ru) |
| KR (1) | KR101656634B1 (ru) |
| CN (1) | CN104718191B (ru) |
| AR (1) | AR093043A1 (ru) |
| AU (1) | AU2013333984B2 (ru) |
| BR (1) | BR112015007991A2 (ru) |
| CA (1) | CA2882484A1 (ru) |
| CL (1) | CL2015000708A1 (ru) |
| CR (1) | CR20150143A (ru) |
| EA (1) | EA025668B1 (ru) |
| ES (1) | ES2599509T3 (ru) |
| HK (1) | HK1208032A1 (ru) |
| IL (1) | IL237116A (ru) |
| MA (1) | MA38011B1 (ru) |
| MX (1) | MX2015004086A (ru) |
| MY (1) | MY170152A (ru) |
| PE (1) | PE20150628A1 (ru) |
| PH (1) | PH12015500496B1 (ru) |
| SG (1) | SG11201501375YA (ru) |
| TW (1) | TWI468393B (ru) |
| UA (1) | UA114934C2 (ru) |
| WO (1) | WO2014060394A1 (ru) |
| ZA (1) | ZA201500896B (ru) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ703537A (en) * | 2012-10-18 | 2018-06-29 | Hoffmann La Roche | Ethynyl derivatives |
| PE20180356A1 (es) | 2015-07-15 | 2018-02-21 | Hoffmann La Roche | Derivados de etinilo como moduladores del receptor metabotropico del glutamato |
| CN109476671B (zh) | 2016-07-18 | 2021-09-24 | 豪夫迈·罗氏有限公司 | 乙炔基衍生物 |
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 |
| CA2689282A1 (en) * | 2007-06-03 | 2008-12-11 | Vanderbilt University | Benzamide mglur5 positive allosteric modulators and methods of making and using same |
| EP2190487A1 (en) * | 2007-09-28 | 2010-06-02 | E. I. du Pont de Nemours and Company | Ionic liquid stabilizer compositions |
| 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 UA UAA201504379A patent/UA114934C2/uk unknown
- 2013-10-15 AU AU2013333984A patent/AU2013333984B2/en not_active Ceased
- 2013-10-15 MX MX2015004086A patent/MX2015004086A/es unknown
- 2013-10-15 EP EP13776810.7A patent/EP2909179B1/en not_active Not-in-force
- 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 CN CN201380053650.6A patent/CN104718191B/zh not_active Expired - Fee Related
- 2013-10-15 CA CA2882484A patent/CA2882484A1/en not_active Abandoned
- 2013-10-15 SG SG11201501375YA patent/SG11201501375YA/en unknown
- 2013-10-15 ES ES13776810.7T patent/ES2599509T3/es active Active
- 2013-10-15 EA EA201590722A patent/EA025668B1/ru not_active IP Right Cessation
- 2013-10-15 PE PE2015000395A patent/PE20150628A1/es not_active Application Discontinuation
- 2013-10-15 BR BR112015007991A patent/BR112015007991A2/pt active Search and Examination
- 2013-10-15 KR KR1020157009546A patent/KR101656634B1/ko active IP Right Grant
- 2013-10-15 MY MYPI2015000492A patent/MY170152A/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/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
Also Published As
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG TJ TM |
|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): RU |