MA38659B1 - Dérivés éthynyle comme antagonistes du récepteur métabotrope du glutamate - Google Patents
Dérivés éthynyle comme antagonistes du récepteur métabotrope du glutamateInfo
- Publication number
- MA38659B1 MA38659B1 MA38659A MA38659A MA38659B1 MA 38659 B1 MA38659 B1 MA 38659B1 MA 38659 A MA38659 A MA 38659A MA 38659 A MA38659 A MA 38659A MA 38659 B1 MA38659 B1 MA 38659B1
- Authority
- MA
- Morocco
- Prior art keywords
- receptor antagonists
- glutamate receptor
- metabotropic glutamate
- hydrogen
- derivatives
- Prior art date
Links
- 102000016193 Metabotropic glutamate receptors Human genes 0.000 title abstract 2
- 108010010914 Metabotropic glutamate receptors Proteins 0.000 title abstract 2
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 title abstract 2
- 239000003825 glutamate receptor antagonist Substances 0.000 title abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 208000019901 Anxiety disease Diseases 0.000 abstract 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 1
- 208000001914 Fragile X syndrome Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 230000036506 anxiety Effects 0.000 abstract 1
- 208000029560 autism spectrum disease Diseases 0.000 abstract 1
- 229910052801 chlorine Chemical group 0.000 abstract 1
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 239000011737 fluorine Chemical group 0.000 abstract 1
- 208000021302 gastroesophageal reflux disease Diseases 0.000 abstract 1
- 229940126662 negative allosteric modulator Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- 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)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (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)
Abstract
La présente invention concerne des dérivés éthynyle de formule (i), dans laquelle y est n ou ch; r1 est un atome d'hydrogène, de fluor ou de chlore; et r2 est l'hydrogène ou un alkyle inférieur; ou un sel d'addition d'acide pharmaceutiquement acceptable desdits dérivés. On a découvert de façon surprenante que les composés de formule générale (i) sont des antagonistes du récepteur métabotrope du glutamate (modulateurs allostériques négatifs) pouvant être employés pour traiter l'anxiété et la douleur, la dépression, le syndrome de l'x fragile, les troubles du spectre autistique, la maladie de parkinson et le reflux gastro-œsophagien (gerd).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13175535 | 2013-07-08 | ||
| PCT/EP2014/064272 WO2015004007A1 (fr) | 2013-07-08 | 2014-07-04 | Dérivés éthynyle comme antagonistes du récepteur métabotrope du glutamate |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MA38659A1 MA38659A1 (fr) | 2016-02-29 |
| MA38659B1 true MA38659B1 (fr) | 2016-10-31 |
Family
ID=48745843
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MA38659A MA38659B1 (fr) | 2013-07-08 | 2015-12-10 | Dérivés éthynyle comme antagonistes du récepteur métabotrope du glutamate |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US9682959B2 (fr) |
| EP (1) | EP3019486B1 (fr) |
| JP (1) | JP6116761B2 (fr) |
| KR (1) | KR101767348B1 (fr) |
| CN (1) | CN105358543B (fr) |
| AR (1) | AR096824A1 (fr) |
| AU (1) | AU2014289398B2 (fr) |
| BR (1) | BR112015029724A2 (fr) |
| CA (1) | CA2914282A1 (fr) |
| CL (1) | CL2015003761A1 (fr) |
| CR (1) | CR20150650A (fr) |
| DK (1) | DK3019486T3 (fr) |
| EA (1) | EA027882B1 (fr) |
| ES (1) | ES2628206T3 (fr) |
| HU (1) | HUE033270T2 (fr) |
| IL (1) | IL242682B (fr) |
| MA (1) | MA38659B1 (fr) |
| MY (1) | MY181847A (fr) |
| PE (1) | PE20160604A1 (fr) |
| PH (1) | PH12015502692B1 (fr) |
| PL (1) | PL3019486T3 (fr) |
| SG (1) | SG11201510607RA (fr) |
| SI (1) | SI3019486T1 (fr) |
| TW (1) | TWI527808B (fr) |
| UA (1) | UA116023C2 (fr) |
| WO (1) | WO2015004007A1 (fr) |
| ZA (1) | ZA201508410B (fr) |
Families Citing this family (5)
| 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 |
| 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 |
| RS62551B1 (sr) | 2017-12-14 | 2021-12-31 | H Lundbeck As | Kombinovane terapije koje obuhvataju primenu 1h-pirazolo[4,3-b]piridina |
| EP3728250A1 (fr) | 2017-12-20 | 2020-10-28 | H. Lundbeck A/S | PYRAZOLO[3,4-beta]PYRIDINES ET IMIDAZO[1,5-beta]PYRIDAZINES UTILISÉES EN TANT QU'INHIBITEURS DE PDE1 |
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 |
| JP5635727B2 (ja) * | 2004-10-07 | 2014-12-03 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | チアゾリルｍｇｌｕｒ５アンタゴニスト及びそれらの使用のための方法 |
| 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 |
| KR101576343B1 (ko) * | 2011-04-26 | 2015-12-09 | 에프. 호프만-라 로슈 아게 | 피라졸리딘-3-온 유도체 |
| CA2829170C (fr) * | 2011-04-26 | 2019-02-26 | F. Hoffmann-La Roche Ag | Derives d'ethynyle comme modulateurs allosteriques positifs de mglur5 |
| UA110862C2 (uk) * | 2011-10-07 | 2016-02-25 | Ф. Хоффманн-Ля Рош Аг | Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5 |
-
2014
- 2014-04-07 UA UAA201600580A patent/UA116023C2/uk unknown
- 2014-07-04 WO PCT/EP2014/064272 patent/WO2015004007A1/fr not_active Ceased
- 2014-07-04 JP JP2016524753A patent/JP6116761B2/ja not_active Expired - Fee Related
- 2014-07-04 ES ES14739714.5T patent/ES2628206T3/es active Active
- 2014-07-04 DK DK14739714.5T patent/DK3019486T3/en active
- 2014-07-04 SG SG11201510607RA patent/SG11201510607RA/en unknown
- 2014-07-04 CA CA2914282A patent/CA2914282A1/fr not_active Abandoned
- 2014-07-04 PE PE2015002663A patent/PE20160604A1/es not_active Application Discontinuation
- 2014-07-04 AU AU2014289398A patent/AU2014289398B2/en not_active Ceased
- 2014-07-04 PL PL14739714T patent/PL3019486T3/pl unknown
- 2014-07-04 SI SI201430233A patent/SI3019486T1/sl unknown
- 2014-07-04 MY MYPI2015003036A patent/MY181847A/en unknown
- 2014-07-04 CN CN201480038739.XA patent/CN105358543B/zh active Active
- 2014-07-04 TW TW103123204A patent/TWI527808B/zh not_active IP Right Cessation
- 2014-07-04 BR BR112015029724A patent/BR112015029724A2/pt not_active Application Discontinuation
- 2014-07-04 HU HUE14739714A patent/HUE033270T2/en unknown
- 2014-07-04 EP EP14739714.5A patent/EP3019486B1/fr active Active
- 2014-07-04 KR KR1020167000013A patent/KR101767348B1/ko not_active Expired - Fee Related
- 2014-07-04 EA EA201690162A patent/EA027882B1/ru not_active IP Right Cessation
- 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
-
2017
- 2017-04-17 US US15/489,295 patent/US9751856B2/en active Active
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