DK2900659T3 - Arylethynylderivater - Google Patents
Arylethynylderivater Download PDFInfo
- Publication number
- DK2900659T3 DK2900659T3 DK13766286.2T DK13766286T DK2900659T3 DK 2900659 T3 DK2900659 T3 DK 2900659T3 DK 13766286 T DK13766286 T DK 13766286T DK 2900659 T3 DK2900659 T3 DK 2900659T3
- Authority
- DK
- Denmark
- Prior art keywords
- formula
- compound
- compounds
- pharmaceutically acceptable
- oxazin
- Prior art date
Links
Classifications
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- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
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- 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
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
-
- 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
- A61P25/06—Antimigraine agents
-
- 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
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- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- 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
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- 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
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- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/34—Tobacco-abuse
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- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (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)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Psychology (AREA)
- Ophthalmology & Optometry (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Otolaryngology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
- Epidemiology (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Claims (8)
1. Ethynylderivater med formel I
hvor Ri er phenyl, 3-fluorphenyl, 4-fluorphenyl eller 2,5-di-fluorphenyl; eller et farmaceutisk acceptabelt syreadditionssalt i enantiomer ren form.
2. Ethynylderivater med formel I, hvor forbindelserne er (4aS,7aR)-l-(5-phenylethynyl-pyridin-2-yl)-hexahydro-cyclopenta[d][l,3]oxazin-2-on (4aS,7aR)-l-[5-(3-fluorphenylethynyl)-pyridin-2-yl]-hexahydro-cyclopenta[d][l,3]oxazin-2-on (4aS,7aR)-l-(5-((4-fluorphenyl)ethynyl)-pyridin-2-yl)hexahydro-cyclopenta[d][l,3]oxazin-2(lH)-on eller (4aS,7aR)-l-[5-(2,5-difluorphenylethynyl)-pyridin-2-yl]-hexahydro- cyclopenta[d][l,3]oxazin-2-on.
3. Fremgangsmåde til fremstillingen af en forbindelse med formel I som beskrevet i krav 1, omfattende varianterne a) omsætning af en forbindelse med formel 3
hvor forbindelsen med formel 3 er en racemisk blanding eller i enantiomer ren form med en egnet arylacetylen halo-pyridinforbindelse med formel 4, hvor Y er halogen, valgt fra fluor, brom eller iod
for at danne en forbindelse med formel I i enantiomer ren form eller som en racemisk blanding, hvor enantiomererne kan adskilles under anvendelse af fremgangsmåder kendt for en fagmand,
hvor substituenterne er beskrevet i krav 1, eller om ønsket, omdanne forbindelserne opnået til de farmaceutisk acceptable syreadditionssalte eller ved b) omsætning afen forbindelse med formel II i enantiomer ren form eller som en racemisk blanding, hvor X er halogen, fortrinsvis lod eller brom
med en acetylenforbindelse med formel 5, hvor Q er hydrogen eller en trialkylsilyigruppe
for at danne en forbindelse med formel I i enantiomer ren form eller som en racemisk blanding der kan adskilles under anvendelse af fremgangsmåder kendt for en fagmand,
hvor substituenterne er beskrevet i krav 1, eller om ønsket, omdanne forbindelserne opnået til de farmaceutiske acceptable syreadditionssalte.
4. Forbindelse ifølge et hvilket som helst af kravene 1 til 2 til anvendelse som terapeutisk aktivt stof.
5. Farmaceutisk sammensætning omfattende mindst én af forbindelserne ifølge et hvilket som helst af kravene 1 til 2 såvel som dets farmaceutisk acceptable salt.
6. Forbindelse ifølge et hvilket som helst af kravene 1 til 2, når anvendelig som blandinger af enantiomerer, diastereomerer, eller i enantiomer ren form; såvel som dets farmaceutisk acceptable salt, til anvendelse som medikament.
7. Anvendelsen af en forbindelse ifølge et hvilket som helst af kravene 1 til 2 såvel som dets farmaceutisk acceptable salt til fremstillingen af et medikament til behandlingen eller forebyggelsen af sygdomme relateret til allosteriske modulatorer af mGluR-receptorer, hvor sygdommen er skizofreni, kognitive sygdomme, fragilt X-syndrom eller autisme.
8. Forbindelse Ifølge et hvilket som helst af kravene 1 til 2 til behandlingen eller forebyggelse af skizofreni, kognitive sygdomme, fragilt X-syndrom eller autisme.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12186265 | 2012-09-27 | ||
| PCT/EP2013/069674 WO2014056710A1 (en) | 2012-09-27 | 2013-09-23 | Arylethynyl derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK2900659T3 true DK2900659T3 (da) | 2016-10-03 |
Family
ID=47044829
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK13766286.2T DK2900659T3 (da) | 2012-09-27 | 2013-09-23 | Arylethynylderivater |
Country Status (30)
| Country | Link |
|---|---|
| US (1) | US9221802B2 (da) |
| EP (1) | EP2900659B1 (da) |
| JP (1) | JP6027251B2 (da) |
| KR (1) | KR101737245B1 (da) |
| CN (1) | CN104684911B (da) |
| AR (1) | AR092673A1 (da) |
| AU (1) | AU2013329739B2 (da) |
| BR (1) | BR112015006218A2 (da) |
| CA (1) | CA2885382A1 (da) |
| CL (1) | CL2015000707A1 (da) |
| CR (1) | CR20150139A (da) |
| DK (1) | DK2900659T3 (da) |
| EA (1) | EA025482B1 (da) |
| ES (1) | ES2594031T3 (da) |
| HK (1) | HK1207376A1 (da) |
| HU (1) | HUE029636T2 (da) |
| IL (1) | IL237596A (da) |
| MA (1) | MA37941B1 (da) |
| MX (1) | MX366136B (da) |
| MY (1) | MY171743A (da) |
| NZ (1) | NZ706283A (da) |
| PE (1) | PE20150708A1 (da) |
| PH (1) | PH12015500538B1 (da) |
| PL (1) | PL2900659T3 (da) |
| SG (1) | SG11201502449RA (da) |
| SI (1) | SI2900659T1 (da) |
| TW (1) | TWI476194B (da) |
| UA (1) | UA113779C2 (da) |
| WO (1) | WO2014056710A1 (da) |
| ZA (1) | ZA201501678B (da) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA113223C2 (xx) * | 2012-08-13 | 2016-12-26 | Арилетинілпіримідини | |
| CA2879489A1 (en) * | 2012-10-18 | 2014-04-24 | F.Hoffmann-La Roche Ag | Ethynyl derivatives as modulators of mglur5 receptor activity |
| MA42508B1 (fr) * | 2015-06-03 | 2020-05-29 | Hoffmann La Roche | Dérivés d'éthynyle |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0325956D0 (en) | 2003-11-06 | 2003-12-10 | Addex Pharmaceuticals Sa | Novel compounds |
| WO2006048771A1 (en) | 2004-11-04 | 2006-05-11 | Addex Pharmaceuticals Sa | Novel tetrazole derivatives as positive allosteric modulators of metabotropic glutamate receptors |
| GB0510139D0 (en) | 2005-05-18 | 2005-06-22 | Addex Pharmaceuticals Sa | Novel compounds B1 |
| TW200811157A (en) * | 2006-05-05 | 2008-03-01 | Astrazeneca Ab | mGluR5 modulators I |
| SG185285A1 (en) | 2007-06-03 | 2012-11-29 | Univ Vanderbilt | Benzamide mglur5 positive allosteric modulators and methods of making and using same |
| US8034806B2 (en) * | 2007-11-02 | 2011-10-11 | Vanderbilt University | Bicyclic mGluR5 positive allosteric modulators and methods of making and using same |
| TW201116532A (en) * | 2009-08-05 | 2011-05-16 | Merz Pharma Gmbh & Co Kgaa | Metabotropic glutamate receptor modulators |
| US8586581B2 (en) * | 2009-12-17 | 2013-11-19 | Hoffmann-La Roche Inc | Ethynyl compounds useful for treatment of CNS disorders |
| US8420661B2 (en) * | 2010-04-13 | 2013-04-16 | Hoffmann-La Roche Inc. | Arylethynyl derivatives |
-
2013
- 2013-09-23 NZ NZ706283A patent/NZ706283A/en not_active IP Right Cessation
- 2013-09-23 CN CN201380050037.9A patent/CN104684911B/zh active Active
- 2013-09-23 BR BR112015006218A patent/BR112015006218A2/pt not_active IP Right Cessation
- 2013-09-23 ES ES13766286.2T patent/ES2594031T3/es active Active
- 2013-09-23 HU HUE13766286A patent/HUE029636T2/en unknown
- 2013-09-23 KR KR1020157010351A patent/KR101737245B1/ko active IP Right Grant
- 2013-09-23 EA EA201590557A patent/EA025482B1/ru not_active IP Right Cessation
- 2013-09-23 AU AU2013329739A patent/AU2013329739B2/en not_active Ceased
- 2013-09-23 PE PE2015000422A patent/PE20150708A1/es active IP Right Grant
- 2013-09-23 JP JP2015533547A patent/JP6027251B2/ja active Active
- 2013-09-23 EP EP13766286.2A patent/EP2900659B1/en active Active
- 2013-09-23 PL PL13766286T patent/PL2900659T3/pl unknown
- 2013-09-23 DK DK13766286.2T patent/DK2900659T3/da active
- 2013-09-23 CA CA2885382A patent/CA2885382A1/en not_active Abandoned
- 2013-09-23 WO PCT/EP2013/069674 patent/WO2014056710A1/en active Application Filing
- 2013-09-23 UA UAA201503791A patent/UA113779C2/uk unknown
- 2013-09-23 MY MYPI2015000777A patent/MY171743A/en unknown
- 2013-09-23 SI SI201330373A patent/SI2900659T1/sl unknown
- 2013-09-23 MX MX2015003560A patent/MX366136B/es active IP Right Grant
- 2013-09-23 SG SG11201502449RA patent/SG11201502449RA/en unknown
- 2013-09-25 AR ARP130103433A patent/AR092673A1/es unknown
- 2013-09-26 TW TW102134845A patent/TWI476194B/zh not_active IP Right Cessation
-
2015
- 2015-03-05 IL IL237596A patent/IL237596A/en active IP Right Grant
- 2015-03-11 ZA ZA2015/01678A patent/ZA201501678B/en unknown
- 2015-03-12 PH PH12015500538A patent/PH12015500538B1/en unknown
- 2015-03-16 CR CR20150139A patent/CR20150139A/es unknown
- 2015-03-20 MA MA37941A patent/MA37941B1/fr unknown
- 2015-03-20 CL CL2015000707A patent/CL2015000707A1/es unknown
- 2015-03-26 US US14/669,653 patent/US9221802B2/en active Active
- 2015-08-19 HK HK15108049.7A patent/HK1207376A1/xx unknown
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