DK3019486T3 - Ethynylderivater som antagonister for metabotrope glutamatreceptorer - Google Patents
Ethynylderivater som antagonister for metabotrope glutamatreceptorer Download PDFInfo
- Publication number
- DK3019486T3 DK3019486T3 DK14739714.5T DK14739714T DK3019486T3 DK 3019486 T3 DK3019486 T3 DK 3019486T3 DK 14739714 T DK14739714 T DK 14739714T DK 3019486 T3 DK3019486 T3 DK 3019486T3
- Authority
- DK
- Denmark
- Prior art keywords
- compound
- formula
- imidazol
- compounds
- trimethyl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Rheumatology (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Claims (10)
1. Forbindelse med formlen I
hvor Y er N eller CH; R1 er hydrogen, fluor eller chlor; og R2 er hydrogen eller en lavere alkyl; eller et farmaceutisk acceptabelt syreadditionssalt deraf.
2. Forbindelse med formlen I ifølge krav 1, hvor Y er N.
3. Forbindelse med formlen (I) ifølge et hvilket som helst af kravene 1 og 2, hvilke forbindelser er 2-[5-[2-(3-chlorphenyl)ethynyl]-2-pynmidyl]-3,5,5-trimethyl-imidazol-4-on 3.5.5- trimethyl-2-[5-(2-phenylethynyl)-2-pyrimidyl]imidazol-4-on eller 2-[5-[2-(3-fluorphenyl)ethynyl]-2-pyrimidyl]-3,5,5-trimethyl-imidazol-4-on.
4. Forbindelse med formlen I ifølge krav 1, hvor Y er CH.
5. Forbindelse med formlen I ifølge et hvilket som helst af kravene 1 og 4, hvilke forbindelser er 2-[5-[2-(3-fluorphenyl)ethynyl]-2-pyridyl]-3,5,5-trimethyl-imidazol-4-on 3.5.5- trimethyl-2-[5-(2-phenylethynyl)-2-pyridyl]imidazol-4-on eller 2-[5-[2-(3-chlorphenyl)ethynyl]-2-pyridyl]-3,5,5-trimethyl-imidazol-4-on.
6. Forbindelse ifølge et hvilket som helst af kravene 1-5 til anvendelse som terapeutisk aktivt stof.
7. Fremgangsmåde til fremstilling af en forbindelse med formlen I ifølge et hvilket som helst af kravene 1-5, hvilken fremgangsmåde omfatter varianterne a) at omsætte en forbindelse med formlen
med en forbindelse med formlen
6 til en forbindelse med formlen
hvor substituenterne er som beskrevet i krav 1, eller b) at ringslutte en forbindelse med formlen
til en forbindelse med formlen
og, hvis det ønskes, at alkylere den opnåede forbindelse til en forbindelse med formlen
I (for R2 = alkyl) hvor substituenterne er som beskrevet i krav 1.
8. Farmaceutisk sammensætning, der omfatter en forbindelse ifølge et hvilket som helst af kravene 1-5 og en terapeutisk aktiv bærer.
9. Anvendelse af en forbindelse ifølge et hvilket som helst af kravene 1-5 til fremstilling af et lægemiddel til behandling af angst og smerte, depression, fragilt X-syndrom, autismespektrumforstyrrelser, Parkinsons sygdom og gastroøsofageal reflukssygdom.
10. Forbindelse ifølge et hvilket som helst af kravene 1-5 til anvendelse ved behandling af angst og smerte, depression, fragilt X-syndrom, autismespektrumforstyrrelser, Parkinsons sygdom og gastroøsofageal reflukssygdom.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13175535 | 2013-07-08 | ||
| PCT/EP2014/064272 WO2015004007A1 (en) | 2013-07-08 | 2014-07-04 | Ethynyl derivatives as metabotropic glutamate receptor antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK3019486T3 true DK3019486T3 (da) | 2017-06-19 |
Family
ID=48745843
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK14739714.5T DK3019486T3 (da) | 2013-07-08 | 2014-07-04 | Ethynylderivater som antagonister for metabotrope glutamatreceptorer |
Country Status (28)
| Country | Link |
|---|---|
| US (2) | US9682959B2 (da) |
| EP (1) | EP3019486B1 (da) |
| JP (1) | JP6116761B2 (da) |
| KR (1) | KR101767348B1 (da) |
| CN (1) | CN105358543B (da) |
| AR (1) | AR096824A1 (da) |
| AU (1) | AU2014289398B2 (da) |
| BR (1) | BR112015029724A2 (da) |
| CA (1) | CA2914282A1 (da) |
| CL (1) | CL2015003761A1 (da) |
| CR (1) | CR20150650A (da) |
| DK (1) | DK3019486T3 (da) |
| EA (1) | EA027882B1 (da) |
| ES (1) | ES2628206T3 (da) |
| HK (1) | HK1215573A1 (da) |
| HU (1) | HUE033270T2 (da) |
| IL (1) | IL242682B (da) |
| MA (1) | MA38659B1 (da) |
| MY (1) | MY181847A (da) |
| PE (1) | PE20160604A1 (da) |
| PH (1) | PH12015502692B1 (da) |
| PL (1) | PL3019486T3 (da) |
| SG (1) | SG11201510607RA (da) |
| SI (1) | SI3019486T1 (da) |
| TW (1) | TWI527808B (da) |
| UA (1) | UA116023C2 (da) |
| WO (1) | WO2015004007A1 (da) |
| ZA (1) | ZA201508410B (da) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CR20170536A (es) | 2015-06-03 | 2018-02-01 | Hoffmann La Roche | Derivados de etinilo |
| US10034861B2 (en) | 2016-07-04 | 2018-07-31 | H. Lundbeck A/S | 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors |
| AR113926A1 (es) | 2017-12-14 | 2020-07-01 | H Lundbeck As | Derivados de 1h-pirazolo[4,3-b]piridinas |
| US11634416B2 (en) | 2017-12-14 | 2023-04-25 | H. Lundbeck A/S | Combination treatments comprising administration of 1H-pyrazolo[4,3-b]pyridines |
| CN111511742B (zh) | 2017-12-20 | 2023-10-27 | H.隆德贝克有限公司 | 作为PDE1抑制剂的吡唑并[4,3-b]吡啶和咪唑并[1,5-a]嘧啶 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5724364A (en) * | 1980-06-02 | 1982-02-08 | American Cyanamid Co | 2-(2-imidazoline-2-yl)pyridines and quinolines, manufacture and intermediate and herbicidal use |
| FI90869C (fi) * | 1986-11-14 | 1994-04-11 | Tanabe Seiyaku Co | Menetelmä lääkeaineena käyttökelpoisten imidatsolidinonijohdannaisten valmistamiseksi |
| TW544448B (en) * | 1997-07-11 | 2003-08-01 | Novartis Ag | Pyridine derivatives |
| TWI292318B (en) | 2003-03-10 | 2008-01-11 | Hoffmann La Roche | Imidazol-4-yl-ethynyl-pyridine derivatives |
| WO2007050050A2 (en) * | 2004-10-07 | 2007-05-03 | Merck & Co., Inc. | Thiazolyl mglur5 antagonists and methods for their use |
| US8389536B2 (en) * | 2009-10-27 | 2013-03-05 | Hoffmann-La Roche Inc. | Positive allosteric modulators (PAM) |
| US8420661B2 (en) | 2010-04-13 | 2013-04-16 | Hoffmann-La Roche Inc. | Arylethynyl derivatives |
| DK2702051T3 (da) * | 2011-04-26 | 2015-03-16 | Hoffmann La Roche | Ethynylderivater som positive allosteriske modulatorer af mglur5 |
| MY165141A (en) * | 2011-04-26 | 2018-02-28 | Hoffmann La Roche | Pyrazolidin-3-one derivatives |
| UA110862C2 (uk) * | 2011-10-07 | 2016-02-25 | Ф. Хоффманн-Ля Рош Аг | Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5 |
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2014
- 2014-04-07 UA UAA201600580A patent/UA116023C2/uk unknown
- 2014-07-04 HU HUE14739714A patent/HUE033270T2/en unknown
- 2014-07-04 PE PE2015002663A patent/PE20160604A1/es not_active Application Discontinuation
- 2014-07-04 BR BR112015029724A patent/BR112015029724A2/pt not_active Application Discontinuation
- 2014-07-04 EA EA201690162A patent/EA027882B1/ru not_active IP Right Cessation
- 2014-07-04 DK DK14739714.5T patent/DK3019486T3/da active
- 2014-07-04 CA CA2914282A patent/CA2914282A1/en not_active Abandoned
- 2014-07-04 TW TW103123204A patent/TWI527808B/zh not_active IP Right Cessation
- 2014-07-04 EP EP14739714.5A patent/EP3019486B1/en active Active
- 2014-07-04 CN CN201480038739.XA patent/CN105358543B/zh active Active
- 2014-07-04 MY MYPI2015003036A patent/MY181847A/en unknown
- 2014-07-04 ES ES14739714.5T patent/ES2628206T3/es active Active
- 2014-07-04 JP JP2016524753A patent/JP6116761B2/ja active Active
- 2014-07-04 SG SG11201510607RA patent/SG11201510607RA/en unknown
- 2014-07-04 KR KR1020167000013A patent/KR101767348B1/ko active IP Right Grant
- 2014-07-04 PL PL14739714T patent/PL3019486T3/pl unknown
- 2014-07-04 WO PCT/EP2014/064272 patent/WO2015004007A1/en active Application Filing
- 2014-07-04 AU AU2014289398A patent/AU2014289398B2/en not_active Ceased
- 2014-07-04 SI SI201430233A patent/SI3019486T1/sl unknown
- 2014-07-07 AR ARP140102508A patent/AR096824A1/es unknown
-
2015
- 2015-11-13 ZA ZA2015/08410A patent/ZA201508410B/en unknown
- 2015-11-19 IL IL242682A patent/IL242682B/en not_active IP Right Cessation
- 2015-12-02 PH PH12015502692A patent/PH12015502692B1/en unknown
- 2015-12-08 CR CR20150650A patent/CR20150650A/es unknown
- 2015-12-10 MA MA38659A patent/MA38659B1/fr unknown
- 2015-12-30 CL CL2015003761A patent/CL2015003761A1/es unknown
-
2016
- 2016-01-08 US US14/991,748 patent/US9682959B2/en active Active
- 2016-03-24 HK HK16103513.4A patent/HK1215573A1/zh unknown
-
2017
- 2017-04-17 US US15/489,295 patent/US9751856B2/en active Active
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