CR20150158A - Derivados de etinilo como moduladores de receptor de actividad mglur5 - Google Patents
Derivados de etinilo como moduladores de receptor de actividad mglur5Info
- Publication number
- CR20150158A CR20150158A CR20150158A CR20150158A CR20150158A CR 20150158 A CR20150158 A CR 20150158A CR 20150158 A CR20150158 A CR 20150158A CR 20150158 A CR20150158 A CR 20150158A CR 20150158 A CR20150158 A CR 20150158A
- Authority
- CR
- Costa Rica
- Prior art keywords
- derivatives
- ethylly
- mglur5 activity
- activity receiver
- receiver modulators
- Prior art date
Links
- 101150087728 Grm5 gene Proteins 0.000 title 1
- 102100038357 Metabotropic glutamate receptor 5 Human genes 0.000 title 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 abstract 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 239000000460 chlorine Substances 0.000 abstract 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 239000011737 fluorine Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000003287 optical effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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
- 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
- A61P25/22—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (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)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Epidemiology (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente invención se refiere a derivados de etinilo de la fórmula I en la que Y es N o CH R1 es flúor o cloro, o a una sal de adición de ácido farmacéuticamente aceptable, a una mezcla racémica, o a sus correspondientes enantiómeros y/o isómeros ópticos y/o estereoisómeros.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12188943 | 2012-10-18 | ||
| PCT/EP2013/071476 WO2014060384A1 (en) | 2012-10-18 | 2013-10-15 | Ethynyl derivatives as modulators of mglur5 receptor activity |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CR20150158A true CR20150158A (es) | 2015-04-30 |
Family
ID=47049068
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CR20150158A CR20150158A (es) | 2012-10-18 | 2015-03-20 | Derivados de etinilo como moduladores de receptor de actividad mglur5 |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US9359301B2 (es) |
| EP (1) | EP2909178B1 (es) |
| JP (1) | JP6263542B2 (es) |
| KR (1) | KR20150070102A (es) |
| CN (1) | CN104603110B (es) |
| AR (1) | AR093029A1 (es) |
| AU (1) | AU2013331782B2 (es) |
| BR (1) | BR112015002320A2 (es) |
| CA (1) | CA2879489A1 (es) |
| CL (1) | CL2015000890A1 (es) |
| CR (1) | CR20150158A (es) |
| EA (1) | EA026941B1 (es) |
| ES (1) | ES2599507T3 (es) |
| IL (1) | IL237217A (es) |
| MA (1) | MA38010B1 (es) |
| MX (1) | MX2015002823A (es) |
| MY (1) | MY171517A (es) |
| NZ (1) | NZ703537A (es) |
| PE (1) | PE20150733A1 (es) |
| PH (1) | PH12015500346B1 (es) |
| SG (1) | SG11201500729SA (es) |
| TW (1) | TWI504593B (es) |
| UA (1) | UA114008C2 (es) |
| WO (1) | WO2014060384A1 (es) |
| ZA (1) | ZA201500343B (es) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6603334B2 (ja) * | 2015-06-03 | 2019-11-06 | エフ．ホフマン−ラ ロシュ アーゲー | エチニル誘導体 |
| LT3322701T (lt) | 2015-07-15 | 2019-07-10 | F. Hoffmann-La Roche Ag | Etinilo dariniai kaip metabotropinių glutamato receptorių moduliatoriai |
| BR112018069868A2 (pt) | 2016-03-30 | 2019-01-29 | Sinntaxis AB | modulador alostérico negativo do receptor metabotrópico de glutamato 5, usos de um nam, e método de tratamento ou atenuação de dano cerebral maduro |
| CR20190014A (es) | 2016-07-18 | 2019-03-04 | Hoffmann La Roche | Derivados etinilo |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4536518A (en) * | 1979-11-01 | 1985-08-20 | Pfizer Inc. | Antidepressant derivatives of cis-4-phenyl-1,2,3,4-tetrahydro-1-naphthalenamine |
| UA80888C2 (en) * | 2003-06-05 | 2007-11-12 | Hoffmann La Roche | Imidazole derivatives as glutmate receptor antagonists |
| US7531529B2 (en) * | 2003-06-05 | 2009-05-12 | Roche Palo Alto Llc | Imidazole derivatives |
| US8853392B2 (en) * | 2007-06-03 | 2014-10-07 | Vanderbilt University | Benzamide mGluR5 positive allosteric modulators and methods of making and using same |
| WO2010124047A1 (en) * | 2009-04-23 | 2010-10-28 | Wyeth Llc | Bisaryl alkynylamides as negative allosteric modulators of metabotropic glutamate receptor 5 (mglur5) |
| US8389536B2 (en) * | 2009-10-27 | 2013-03-05 | Hoffmann-La Roche Inc. | Positive allosteric modulators (PAM) |
| US8586581B2 (en) * | 2009-12-17 | 2013-11-19 | Hoffmann-La Roche Inc | Ethynyl compounds useful for treatment of CNS disorders |
| US8772300B2 (en) * | 2011-04-19 | 2014-07-08 | Hoffmann-La Roche Inc. | Phenyl or pyridinyl-ethynyl derivatives |
| CA2829170C (en) * | 2011-04-26 | 2019-02-26 | F. Hoffmann-La Roche Ag | Ethynyl derivatives as positive allosteric modulators of the mglur5 |
| WO2013049255A1 (en) * | 2011-09-26 | 2013-04-04 | Vanderbilt University | Substitued 5-(prop-1-yn-1-yl)picolinamide analogs as allosteric modulators of mglur5 receptors |
| UA110995C2 (uk) * | 2011-10-07 | 2016-03-10 | Ф. Хоффманн-Ля Рош Аг | Етинільні похідні як модулятори метаботропного глутаматного рецептора |
| UA110862C2 (uk) * | 2011-10-07 | 2016-02-25 | Ф. Хоффманн-Ля Рош Аг | Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5 |
| WO2014012851A1 (en) * | 2012-07-17 | 2014-01-23 | F. Hoffmann-La Roche Ag | Arylethynyl derivatives |
| UA113223C2 (xx) * | 2012-08-13 | 2016-12-26 | Арилетинілпіримідини | |
| WO2014056710A1 (en) * | 2012-09-27 | 2014-04-17 | F. Hoffmann-La Roche Ag | Arylethynyl derivatives |
| BR112015007991A2 (pt) * | 2012-10-18 | 2017-07-04 | Hoffmann La Roche | derivados de etinila como moduladores da atividade do receptor de mglur5 |
| SG11201501392TA (en) * | 2012-10-18 | 2015-05-28 | Hoffmann La Roche | Ethynyl derivatives as modulators of mglur5 receptor activity |
-
2013
- 2013-10-15 CN CN201380046124.7A patent/CN104603110B/zh not_active Expired - Fee Related
- 2013-10-15 MX MX2015002823A patent/MX2015002823A/es unknown
- 2013-10-15 UA UAA201504679A patent/UA114008C2/uk unknown
- 2013-10-15 ES ES13776507.9T patent/ES2599507T3/es active Active
- 2013-10-15 JP JP2015537217A patent/JP6263542B2/ja not_active Expired - Fee Related
- 2013-10-15 EP EP13776507.9A patent/EP2909178B1/en active Active
- 2013-10-15 KR KR1020157006701A patent/KR20150070102A/ko not_active Abandoned
- 2013-10-15 PE PE2015000287A patent/PE20150733A1/es not_active Application Discontinuation
- 2013-10-15 CA CA2879489A patent/CA2879489A1/en not_active Abandoned
- 2013-10-15 EA EA201590676A patent/EA026941B1/ru not_active IP Right Cessation
- 2013-10-15 BR BR112015002320A patent/BR112015002320A2/pt not_active Application Discontinuation
- 2013-10-15 AU AU2013331782A patent/AU2013331782B2/en not_active Ceased
- 2013-10-15 MY MYPI2015000250A patent/MY171517A/en unknown
- 2013-10-15 WO PCT/EP2013/071476 patent/WO2014060384A1/en not_active Ceased
- 2013-10-15 NZ NZ703537A patent/NZ703537A/en not_active IP Right Cessation
- 2013-10-15 SG SG11201500729SA patent/SG11201500729SA/en unknown
- 2013-10-16 AR ARP130103749A patent/AR093029A1/es unknown
- 2013-10-17 TW TW102137559A patent/TWI504593B/zh not_active IP Right Cessation
-
2015
- 2015-01-16 ZA ZA2015/00343A patent/ZA201500343B/en unknown
- 2015-02-12 IL IL237217A patent/IL237217A/en not_active IP Right Cessation
- 2015-02-17 PH PH12015500346A patent/PH12015500346B1/en unknown
- 2015-03-20 CR CR20150158A patent/CR20150158A/es unknown
- 2015-04-09 CL CL2015000890A patent/CL2015000890A1/es unknown
- 2015-04-17 US US14/689,387 patent/US9359301B2/en active Active
- 2015-04-17 MA MA38010A patent/MA38010B1/fr unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CR20130307A (es) | Composiciones y métodos para modular el fxr | |
| CR20140238A (es) | Derivados nucleósidos con sustitución 2´, 4´- difluoro-2´-metilo como inhibidores de la replicación del arn del vhc | |
| MX2020010330A (es) | Proceso para preparar un compuesto antiviral de formula i. | |
| CR20130129A (es) | Anàlogos de buprenorfina | |
| CR20120410A (es) | Pirrolidina-2-carboxamidas sustituidas | |
| CR20130369A (es) | Novedosos derivados heterocíclicos | |
| UY35818A (es) | Composiciones y métodos para modular los receptores x farnesoides | |
| CR20140042A (es) | Indazoles | |
| ECSP11011517A (es) | Compuestos antivirales | |
| UY36073A (es) | ?2-AMINO-6-METIL-4,4a,5,6-TETRAHIDROPIRANO[3,4-d][1,3]TIAZIN-8a(8H)-IL-1,3-TIAZOL-4-ILAMIDAS?. | |
| CR20140294A (es) | Derivados de dihidro-benzo-oxazina y dihidro-pirido-oxazina | |
| EA201500298A1 (ru) | Алкоксипиразолы в качестве активаторов растворимой гуанилатциклазы | |
| CR20130625A (es) | Derivados de la piperidina 3-espirocíclica como agonistas de receptores de la ghrelina | |
| MX2013012211A (es) | Derivados biciclicos substituidos de metil amina como moduladores de receptores de esfingosina-1-fosfato. | |
| CR20130415A (es) | Derivados de heteroarilo como moduladores de nachr alfa 7 | |
| PH12012501853A1 (en) | Pyrimidinylpiperidinyloxypyridinone analogues as gpr119 modulators | |
| AR093042A1 (es) | Derivados de etinilo | |
| CO6761304A2 (es) | Nuevos compuestos de bezodioxol-piperazina | |
| CR20140564A (es) | Derivados de pirimidinona como agentes antimaláricos | |
| CR20130476A (es) | Derivados de pirazolidin-3-ona | |
| CR20150158A (es) | Derivados de etinilo como moduladores de receptor de actividad mglur5 | |
| ECSP13013016A (es) | Derivados de 2-amino-3-(imidazol-2-il)-piridin-4-ona, y su uso como inhibidores de la cinasa del receptor vegf | |
| ECSP13012548A (es) | Inhibidores de oxadiazol de la producción de leucotrienos. | |
| CR20150143A (es) | Derivados de etinilo como moduladores del receptor de actividad mglur5 | |
| CR20150650A (es) | Derivados de etinilo como antagonistas receptores de glutamato metabotrópico |