MA37895A1 - Dérivés d'aryléthynylpyrimidine substitués modulateurs allostériques du récepteur métabotrope 5 de glutamate, utiles pour le traitement, par ex. Schizophrénie, maladies cognitives, syndrome x fragile, autisme, psychose et obésité - Google Patents
Dérivés d'aryléthynylpyrimidine substitués modulateurs allostériques du récepteur métabotrope 5 de glutamate, utiles pour le traitement, par ex. Schizophrénie, maladies cognitives, syndrome x fragile, autisme, psychose et obésitéInfo
- Publication number
- MA37895A1 MA37895A1 MA37895A MA37895A MA37895A1 MA 37895 A1 MA37895 A1 MA 37895A1 MA 37895 A MA37895 A MA 37895A MA 37895 A MA37895 A MA 37895A MA 37895 A1 MA37895 A1 MA 37895A1
- Authority
- MA
- Morocco
- Prior art keywords
- autism
- schizophrenia
- treatment
- metabotropic glutamate
- allosteric modulators
- Prior art date
Links
Classifications
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61P25/18—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
- A61P25/28—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
-
- 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
Abstract
La présente invention concerne des dérivés éthynyle de formule (i) dans laquelle r1 représente un hydrogène ou un halogène ; r2 représente un alkyle en c1 à c3 ou -(ch2)m-o-ch3 ; n représente 2 ou 3 ; m représente 1 ou 2 ; ou leurs sels d'addition d'acide de qualité pharmaceutique, leurs mélanges racémiques, ou leurs énantiomères et/ou isomères optiques et/ou stéréo-isomères correspondants. Il a été observé que les composés de formule générale (i) sont des modulateurs allostériques du récepteur métabotropique du glutamate de sous-type 5 (mglur5) possédant des propriétés améliorées pour le traitement de la schizophrénie, de maladies cognitives, du syndrome de l'x fragile ou de l'autisme.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP12180209 | 2012-08-13 | ||
PCT/EP2013/066443 WO2014026880A1 (fr) | 2012-08-13 | 2013-08-06 | Aryléthynyl-pyrimidines |
Publications (2)
Publication Number | Publication Date |
---|---|
MA37895A1 true MA37895A1 (fr) | 2016-12-30 |
MA37895B1 MA37895B1 (fr) | 2017-08-31 |
Family
ID=46851291
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MA37895A MA37895B1 (fr) | 2012-08-13 | 2013-08-06 | Dérivés d'aryléthynylpyrimidine substitués modulateurs allostériques du récepteur métabotrope 5 de glutamate, utiles pour le traitement, par ex. Schizophrénie, maladies cognitives, syndrome x fragile, autisme, psychose et obésité |
Country Status (36)
Country | Link |
---|---|
US (1) | US9199971B2 (fr) |
EP (1) | EP2882742B1 (fr) |
JP (1) | JP5974179B2 (fr) |
KR (1) | KR101747005B1 (fr) |
CN (1) | CN104540815B (fr) |
AR (1) | AR092097A1 (fr) |
AU (1) | AU2013304212B2 (fr) |
BR (1) | BR112015002921A2 (fr) |
CA (1) | CA2880257C (fr) |
CL (1) | CL2015000290A1 (fr) |
CO (1) | CO7180198A2 (fr) |
CR (1) | CR20150028A (fr) |
CY (1) | CY1118595T1 (fr) |
DK (1) | DK2882742T3 (fr) |
EA (1) | EA025165B1 (fr) |
ES (1) | ES2601511T3 (fr) |
HK (1) | HK1207378A1 (fr) |
HR (1) | HRP20161692T1 (fr) |
HU (1) | HUE030237T2 (fr) |
IL (1) | IL237015A (fr) |
LT (1) | LT2882742T (fr) |
MA (1) | MA37895B1 (fr) |
MX (1) | MX358011B (fr) |
MY (1) | MY170255A (fr) |
NZ (1) | NZ704858A (fr) |
PE (1) | PE20150685A1 (fr) |
PH (1) | PH12015500261B1 (fr) |
PL (1) | PL2882742T3 (fr) |
PT (1) | PT2882742T (fr) |
RS (1) | RS55397B1 (fr) |
SG (1) | SG11201501055SA (fr) |
SI (1) | SI2882742T1 (fr) |
TW (1) | TWI501958B (fr) |
UA (1) | UA113223C2 (fr) |
WO (1) | WO2014026880A1 (fr) |
ZA (1) | ZA201500582B (fr) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
MY174339A (en) | 2012-08-13 | 2020-04-09 | Novartis Ag | 1,4-disubstituted pyridazine analogs and methods for treating smn-deficiency-related conditions |
NZ703537A (en) * | 2012-10-18 | 2018-06-29 | Hoffmann La Roche | Ethynyl derivatives |
CN107849006B (zh) * | 2015-06-03 | 2020-11-13 | 豪夫迈·罗氏有限公司 | 乙炔基衍生物 |
Family Cites Families (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB0325956D0 (en) | 2003-11-06 | 2003-12-10 | Addex Pharmaceuticals Sa | Novel compounds |
EP1756086B1 (fr) * | 2004-06-01 | 2008-06-04 | F.Hoffmann-La Roche Ag | Pyridin-4-yl-ethynyl-imidazoles et pyrazoles, antagonistes du recepteur mglur5 |
EP1809620B1 (fr) | 2004-11-04 | 2010-12-29 | Addex Pharma SA | Nouveaux derives de tetrazole utilises comme modulateurs allosteriques positifs des recepteurs de glutamate metabotropiques |
GB0503646D0 (en) * | 2005-02-22 | 2005-03-30 | Novartis Ag | Organic compounds |
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 |
WO2008151184A1 (fr) | 2007-06-03 | 2008-12-11 | Vanderbilt University | Dérivés benzamides modulateurs allostériques positifs récepteurs métabotropiques du glutamate 5 (mglur5) et leurs procédés de fabrication et d'utilisation |
WO2009054794A1 (fr) * | 2007-10-26 | 2009-04-30 | Astrazeneca Ab | Dérivés d'amino1,2,4-triazoles en tant que modulateurs du mglur5 |
US8334287B2 (en) * | 2009-07-17 | 2012-12-18 | Hoffmann-La Roche Inc. | Imidazoles |
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 |
SG186107A1 (en) * | 2010-07-09 | 2013-01-30 | Recordati Ireland Ltd | Novel spiroheterocyclic compounds as mglu5 antagonists |
JPWO2012015024A1 (ja) * | 2010-07-29 | 2013-09-12 | 大正製薬株式会社 | エチニル−ピラゾール誘導体 |
EP2702050B1 (fr) * | 2011-04-26 | 2016-05-18 | F.Hoffmann-La Roche Ag | Dérivés de pyrazolidine-3-one |
US20130123254A1 (en) * | 2011-09-30 | 2013-05-16 | Barbara Biemans | Pharmaceutically acceptable mglur5 positive allosteric modulators and their methods of identification |
UA110862C2 (uk) * | 2011-10-07 | 2016-02-25 | Ф. Хоффманн-Ля Рош Аг | Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5 |
UA110995C2 (uk) * | 2011-10-07 | 2016-03-10 | Ф. Хоффманн-Ля Рош Аг | Етинільні похідні як модулятори метаботропного глутаматного рецептора |
SI2875000T1 (sl) * | 2012-07-17 | 2017-01-31 | F.Hoffmann-La Roche Ag | Ariletinilni derivati |
EA025482B1 (ru) * | 2012-09-27 | 2016-12-30 | Ф. Хоффманн-Ля Рош Аг | Производные арилэтинила |
-
2013
- 2013-06-08 UA UAA201501613A patent/UA113223C2/uk unknown
- 2013-08-06 LT LTEP13747827.7T patent/LT2882742T/lt unknown
- 2013-08-06 EA EA201590252A patent/EA025165B1/ru not_active IP Right Cessation
- 2013-08-06 RS RS20161001A patent/RS55397B1/sr unknown
- 2013-08-06 CA CA2880257A patent/CA2880257C/fr not_active Expired - Fee Related
- 2013-08-06 NZ NZ704858A patent/NZ704858A/en not_active IP Right Cessation
- 2013-08-06 SI SI201330420A patent/SI2882742T1/sl unknown
- 2013-08-06 MA MA37895A patent/MA37895B1/fr unknown
- 2013-08-06 CN CN201380042690.0A patent/CN104540815B/zh active Active
- 2013-08-06 DK DK13747827.7T patent/DK2882742T3/en active
- 2013-08-06 PE PE2015000196A patent/PE20150685A1/es active IP Right Grant
- 2013-08-06 JP JP2015526930A patent/JP5974179B2/ja active Active
- 2013-08-06 MY MYPI2015000358A patent/MY170255A/en unknown
- 2013-08-06 MX MX2015001599A patent/MX358011B/es active IP Right Grant
- 2013-08-06 PT PT137478277T patent/PT2882742T/pt unknown
- 2013-08-06 KR KR1020157006196A patent/KR101747005B1/ko active IP Right Grant
- 2013-08-06 AU AU2013304212A patent/AU2013304212B2/en not_active Ceased
- 2013-08-06 SG SG11201501055SA patent/SG11201501055SA/en unknown
- 2013-08-06 PL PL13747827T patent/PL2882742T3/pl unknown
- 2013-08-06 WO PCT/EP2013/066443 patent/WO2014026880A1/fr active Application Filing
- 2013-08-06 BR BR112015002921A patent/BR112015002921A2/pt not_active Application Discontinuation
- 2013-08-06 HU HUE13747827A patent/HUE030237T2/en unknown
- 2013-08-06 ES ES13747827.7T patent/ES2601511T3/es active Active
- 2013-08-06 EP EP13747827.7A patent/EP2882742B1/fr active Active
- 2013-08-09 TW TW102128724A patent/TWI501958B/zh not_active IP Right Cessation
- 2013-08-12 AR ARP130102851A patent/AR092097A1/es not_active Application Discontinuation
-
2015
- 2015-01-22 CR CR20150028A patent/CR20150028A/es unknown
- 2015-01-23 CO CO15013232A patent/CO7180198A2/es unknown
- 2015-01-26 ZA ZA2015/00582A patent/ZA201500582B/en unknown
- 2015-01-29 IL IL237015A patent/IL237015A/en active IP Right Grant
- 2015-02-06 PH PH12015500261A patent/PH12015500261B1/en unknown
- 2015-02-06 CL CL2015000290A patent/CL2015000290A1/es unknown
- 2015-02-13 US US14/622,232 patent/US9199971B2/en active Active
- 2015-08-19 HK HK15108051.2A patent/HK1207378A1/xx unknown
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2016
- 2016-12-12 HR HRP20161692TT patent/HRP20161692T1/hr unknown
- 2016-12-16 CY CY20161101305T patent/CY1118595T1/el unknown
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