PE20150629A1 - Derivados de etinilo como moduladores de la actividad del receptor de mglur5 - Google Patents
Derivados de etinilo como moduladores de la actividad del receptor de mglur5Info
- Publication number
- PE20150629A1 PE20150629A1 PE2015000396A PE2015000396A PE20150629A1 PE 20150629 A1 PE20150629 A1 PE 20150629A1 PE 2015000396 A PE2015000396 A PE 2015000396A PE 2015000396 A PE2015000396 A PE 2015000396A PE 20150629 A1 PE20150629 A1 PE 20150629A1
- Authority
- PE
- Peru
- Prior art keywords
- disease
- modulators
- receptor activity
- phenyletinyl
- methanone
- Prior art date
Links
- 101150087728 Grm5 gene Proteins 0.000 title 1
- 102100038357 Metabotropic glutamate receptor 5 Human genes 0.000 title 1
- 201000010099 disease Diseases 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 208000019901 Anxiety disease Diseases 0.000 abstract 1
- 102000016193 Metabotropic glutamate receptors Human genes 0.000 abstract 1
- 108010010914 Metabotropic glutamate receptors Proteins 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 230000036506 anxiety Effects 0.000 abstract 1
- 208000029560 autism spectrum disease Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 1
- 229940126662 negative allosteric modulator Drugs 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic 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
-
- 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
- A61P25/22—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
-
- 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
-
- 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
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)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Epidemiology (AREA)
- Pyridine Compounds (AREA)
Abstract
SE REFIERE A DERIVADOS DE ETINILO DE FORMULA (I) DONDE Y ES N O CH; R1 ES F O Cl; R2 ES H O METILO, O UNA SAL DE ADICION DE ACIDO FARMACEUTICAMENTE ACEPTABLE. SON COMPUESTOS PREFERIDOS: (3,3-DIMETIL-MORFOLIN-4-IL)-[5-(3-CLORO-FENILETINIL)-PIRIMIDIN-2-IL]-METANONA; [5-(3-CLORO-FENILETINIL)-PIRIDIN-2-IL]-MORFOLIN-4-IL-METANONA; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON ANTAGONISTAS DEL RECEPTOR DE GLUTAMATO METABOTROPICO (MODULADORES ALOSTERICOS NEGATIVOS) SIENDO UTILES PARA EL TRATAMIENTO DE LA ANSIEDAD Y EL DOLOR, LA DEPRESION, TRASTORNOS DEL ESPECTRO AUTISTA, LA ENFERMEDAD DE PARKINSON, Y LA ENFERMEDAD DEL REFLUJO GASTROESOFAGICO (GERD)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12188940 | 2012-10-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20150629A1 true PE20150629A1 (es) | 2015-05-11 |
Family
ID=47049067
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2015000396A PE20150629A1 (es) | 2012-10-18 | 2013-10-15 | Derivados de etinilo como moduladores de la actividad del receptor de mglur5 |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US9227959B2 (es) |
| EP (1) | EP2909180B1 (es) |
| JP (1) | JP5989250B2 (es) |
| KR (1) | KR101684816B1 (es) |
| CN (1) | CN104718192B (es) |
| AR (1) | AR093042A1 (es) |
| AU (1) | AU2013333988B2 (es) |
| BR (1) | BR112015006454A8 (es) |
| CA (1) | CA2882520A1 (es) |
| CL (1) | CL2015000891A1 (es) |
| CO (1) | CO7200248A2 (es) |
| CR (1) | CR20150144A (es) |
| EA (1) | EA025667B1 (es) |
| ES (1) | ES2599553T3 (es) |
| IL (1) | IL237380A (es) |
| MA (1) | MA38012B1 (es) |
| MX (1) | MX2015004898A (es) |
| MY (1) | MY168937A (es) |
| NZ (1) | NZ705144A (es) |
| PE (1) | PE20150629A1 (es) |
| PH (1) | PH12015500398B1 (es) |
| SG (1) | SG11201501392TA (es) |
| TW (1) | TWI490208B (es) |
| UA (1) | UA114529C2 (es) |
| WO (1) | WO2014060398A1 (es) |
| ZA (1) | ZA201500856B (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MY171517A (en) * | 2012-10-18 | 2019-10-16 | Hoffmann La Roche | Ethynyl derivatives as modulators of mglur5 receptor activity |
| AU2016273751B2 (en) | 2015-06-03 | 2020-04-02 | F. Hoffmann-La Roche Ag | Ethynyl derivatives |
| CN108271370B (zh) * | 2015-09-25 | 2021-03-19 | (由卫生与公众服务部部长代表的)美利坚合众国 | 作为p2y14受体拮抗剂的三唑衍生物 |
| MY203080A (en) | 2017-12-08 | 2024-06-07 | Boehringer Ingelheim Int | Imidazopyridine derivatives and the use thereof as medicament |
| TW202035395A (zh) | 2018-10-17 | 2020-10-01 | 德商百靈佳殷格翰國際股份有限公司 | 4-嘧啶-5-基甲基-嗎啉衍生物及其作為藥物之用途 |
| CN112888685B (zh) | 2018-10-17 | 2023-09-22 | 勃林格殷格翰国际有限公司 | 4-吡嗪-2-基甲基-吗啉衍生物及其作为药物的用途 |
| JP7093469B2 (ja) | 2018-10-17 | 2022-06-29 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ４－ピリジニルメチル－モルホリン誘導体および医薬としてのその使用 |
| WO2020245136A1 (en) | 2019-06-04 | 2020-12-10 | Boehringer Ingelheim International Gmbh | Purine derivatives, as nr2b negative modulators and the use thereof as medicament, in particular for treating depressive disorders |
| CN113906033B (zh) | 2019-06-04 | 2024-04-02 | 勃林格殷格翰国际有限公司 | 咪唑并吡嗪衍生物及其作为药剂的用途 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW544448B (en) * | 1997-07-11 | 2003-08-01 | Novartis Ag | Pyridine derivatives |
| UA80888C2 (en) * | 2003-06-05 | 2007-11-12 | Hoffmann La Roche | Imidazole derivatives as glutmate receptor antagonists |
| MX2009013169A (es) * | 2007-06-03 | 2010-04-30 | Univ Vanderbilt | Moduladores alostericos positivos del mglur5 benzamida y metodos de elaboracion y uso de los mismos. |
| US8853392B2 (en) * | 2007-06-03 | 2014-10-07 | Vanderbilt University | Benzamide mGluR5 positive allosteric modulators and methods of making and using same |
| US8389536B2 (en) * | 2009-10-27 | 2013-03-05 | Hoffmann-La Roche Inc. | Positive allosteric modulators (PAM) |
| 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 |
-
2013
- 2013-10-15 UA UAA201504680A patent/UA114529C2/uk unknown
- 2013-10-15 MX MX2015004898A patent/MX2015004898A/es unknown
- 2013-10-15 WO PCT/EP2013/071500 patent/WO2014060398A1/en not_active Ceased
- 2013-10-15 NZ NZ705144A patent/NZ705144A/en not_active IP Right Cessation
- 2013-10-15 KR KR1020157009544A patent/KR101684816B1/ko not_active Expired - Fee Related
- 2013-10-15 BR BR112015006454A patent/BR112015006454A8/pt not_active Application Discontinuation
- 2013-10-15 EA EA201590699A patent/EA025667B1/ru not_active IP Right Cessation
- 2013-10-15 CA CA2882520A patent/CA2882520A1/en not_active Abandoned
- 2013-10-15 JP JP2015535066A patent/JP5989250B2/ja not_active Expired - Fee Related
- 2013-10-15 MY MYPI2015000470A patent/MY168937A/en unknown
- 2013-10-15 ES ES13783003.0T patent/ES2599553T3/es active Active
- 2013-10-15 SG SG11201501392TA patent/SG11201501392TA/en unknown
- 2013-10-15 AU AU2013333988A patent/AU2013333988B2/en not_active Ceased
- 2013-10-15 CN CN201380053660.XA patent/CN104718192B/zh not_active Expired - Fee Related
- 2013-10-15 PE PE2015000396A patent/PE20150629A1/es active IP Right Grant
- 2013-10-15 EP EP13783003.0A patent/EP2909180B1/en active Active
- 2013-10-17 AR ARP130103764A patent/AR093042A1/es unknown
- 2013-10-17 TW TW102137560A patent/TWI490208B/zh not_active IP Right Cessation
-
2015
- 2015-02-05 ZA ZA2015/00856A patent/ZA201500856B/en unknown
- 2015-02-16 CO CO15032736A patent/CO7200248A2/es unknown
- 2015-02-23 IL IL237380A patent/IL237380A/en not_active IP Right Cessation
- 2015-02-24 PH PH12015500398A patent/PH12015500398B1/en unknown
- 2015-03-18 CR CR20150144A patent/CR20150144A/es unknown
- 2015-04-09 CL CL2015000891A patent/CL2015000891A1/es unknown
- 2015-04-17 US US14/689,375 patent/US9227959B2/en active Active
- 2015-04-17 MA MA38012A patent/MA38012B1/fr unknown
Also Published As
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration |