AR092097A1 - Derivados de ariletinilo - Google Patents
Derivados de ariletiniloInfo
- Publication number
- AR092097A1 AR092097A1 ARP130102851A ARP130102851A AR092097A1 AR 092097 A1 AR092097 A1 AR 092097A1 AR P130102851 A ARP130102851 A AR P130102851A AR P130102851 A ARP130102851 A AR P130102851A AR 092097 A1 AR092097 A1 AR 092097A1
- Authority
- AR
- Argentina
- Prior art keywords
- derivatives
- aryletinyl
- formula
- mglur5
- autism
- Prior art date
Links
- 206010003805 Autism Diseases 0.000 abstract 1
- 208000020706 Autistic disease Diseases 0.000 abstract 1
- 208000001914 Fragile X syndrome 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
- 230000003281 allosteric effect Effects 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 abstract 1
- 229910052736 halogen Chemical group 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000003287 optical effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
Classifications
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
La presente se refiere a derivados de etinilo de la fórmula (1) en la que: R¹ es hidrógeno o halógeno; R² es alquilo C₁₋₃ o -(CH₂)ₙ-O-CH₃; n es el número 2 ó 3; m es el número 1 ó 2; o a una sal de adición de ácido farmacéuticamente aceptable, a una mezcla racémica, o a su enantiómero correspondiente y/o isómero óptico y/o estereoisómero de los mismos. Se ha encontrado que los compuestos de la fórmula general (1) son moduladores alostéricos del receptor de glutamato metabotrópico del subtipo 5 (mGluR5) con propiedades mejoradas para el tratamiento de la esquizofrenia, las enfermedades cognitivas, el síndrome de la X frágil o el autismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12180209 | 2012-08-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR092097A1 true AR092097A1 (es) | 2015-03-25 |
Family
ID=46851291
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130102851A AR092097A1 (es) | 2012-08-13 | 2013-08-12 | Derivados de ariletinilo |
Country Status (35)
| Country | Link |
|---|---|
| US (1) | US9199971B2 (es) |
| EP (1) | EP2882742B1 (es) |
| JP (1) | JP5974179B2 (es) |
| KR (1) | KR101747005B1 (es) |
| CN (1) | CN104540815B (es) |
| AR (1) | AR092097A1 (es) |
| AU (1) | AU2013304212B2 (es) |
| BR (1) | BR112015002921A2 (es) |
| CA (1) | CA2880257C (es) |
| CL (1) | CL2015000290A1 (es) |
| CO (1) | CO7180198A2 (es) |
| CR (1) | CR20150028A (es) |
| CY (1) | CY1118595T1 (es) |
| DK (1) | DK2882742T3 (es) |
| EA (1) | EA025165B1 (es) |
| ES (1) | ES2601511T3 (es) |
| HR (1) | HRP20161692T1 (es) |
| HU (1) | HUE030237T2 (es) |
| IL (1) | IL237015A (es) |
| LT (1) | LT2882742T (es) |
| MA (1) | MA37895B1 (es) |
| MX (1) | MX358011B (es) |
| MY (1) | MY170255A (es) |
| NZ (1) | NZ704858A (es) |
| PE (1) | PE20150685A1 (es) |
| PH (1) | PH12015500261B1 (es) |
| PL (1) | PL2882742T3 (es) |
| PT (1) | PT2882742T (es) |
| RS (1) | RS55397B1 (es) |
| SG (1) | SG11201501055SA (es) |
| SI (1) | SI2882742T1 (es) |
| TW (1) | TWI501958B (es) |
| UA (1) | UA113223C2 (es) |
| WO (1) | WO2014026880A1 (es) |
| ZA (1) | ZA201500582B (es) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8729263B2 (en) | 2012-08-13 | 2014-05-20 | Novartis Ag | 1,4-disubstituted pyridazine analogs there of and methods for treating SMN-deficiency-related conditions |
| 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 |
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 (en) * | 2004-06-01 | 2008-06-04 | F.Hoffmann-La Roche Ag | Pyridin-4-yl-ethynyl-imidazoles and pyrazoles as mglu5 receptor antagonists |
| EP1809620B1 (en) | 2004-11-04 | 2010-12-29 | Addex Pharma SA | Novel tetrazole derivatives as positive allosteric modulators of metabotropic glutamate receptors |
| 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 |
| 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. |
| JP2011500798A (ja) * | 2007-10-26 | 2011-01-06 | アストラゼネカ・アクチエボラーグ | ｍＧｌｕＲ５のモジュレーターとしてのアミノ１，２，４−トリアゾール誘導体 |
| 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 |
| ES2492694T3 (es) * | 2010-07-09 | 2014-09-10 | Recordati Ireland Limited | Nuevos compuestos espiroheterocíclicos como antagonistas de mGlu5 |
| US8642626B2 (en) * | 2010-07-29 | 2014-02-04 | Taisho Pharmaceutical Co., Ltd. | Ethinyl-pyrazole derivative |
| PH12013501928A1 (en) * | 2011-04-26 | 2013-11-25 | Hoffmann La Roche | Pyrazolidin-3-one derivatives |
| US20130123254A1 (en) * | 2011-09-30 | 2013-05-16 | Barbara Biemans | Pharmaceutically acceptable mglur5 positive allosteric modulators and their methods of identification |
| UA110995C2 (uk) * | 2011-10-07 | 2016-03-10 | Ф. Хоффманн-Ля Рош Аг | Етинільні похідні як модулятори метаботропного глутаматного рецептора |
| UA110862C2 (uk) * | 2011-10-07 | 2016-02-25 | Ф. Хоффманн-Ля Рош Аг | Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5 |
| ES2600133T3 (es) * | 2012-07-17 | 2017-02-07 | F. Hoffmann-La Roche Ag | Derivados de ariletinilo |
| WO2014056710A1 (en) * | 2012-09-27 | 2014-04-17 | F. Hoffmann-La Roche Ag | Arylethynyl derivatives |
-
2013
- 2013-06-08 UA UAA201501613A patent/UA113223C2/uk unknown
- 2013-08-06 SG SG11201501055SA patent/SG11201501055SA/en unknown
- 2013-08-06 HR HRP20161692TT patent/HRP20161692T1/hr unknown
- 2013-08-06 LT LTEP13747827.7T patent/LT2882742T/lt unknown
- 2013-08-06 MX MX2015001599A patent/MX358011B/es active IP Right Grant
- 2013-08-06 AU AU2013304212A patent/AU2013304212B2/en not_active Ceased
- 2013-08-06 EP EP13747827.7A patent/EP2882742B1/en active Active
- 2013-08-06 BR BR112015002921A patent/BR112015002921A2/pt not_active Application Discontinuation
- 2013-08-06 HU HUE13747827A patent/HUE030237T2/en unknown
- 2013-08-06 CA CA2880257A patent/CA2880257C/en not_active Expired - Fee Related
- 2013-08-06 DK DK13747827.7T patent/DK2882742T3/en active
- 2013-08-06 MY MYPI2015000358A patent/MY170255A/en unknown
- 2013-08-06 MA MA37895A patent/MA37895B1/fr unknown
- 2013-08-06 NZ NZ704858A patent/NZ704858A/en not_active IP Right Cessation
- 2013-08-06 KR KR1020157006196A patent/KR101747005B1/ko not_active Expired - Fee Related
- 2013-08-06 EA EA201590252A patent/EA025165B1/ru not_active IP Right Cessation
- 2013-08-06 JP JP2015526930A patent/JP5974179B2/ja active Active
- 2013-08-06 SI SI201330420A patent/SI2882742T1/sl unknown
- 2013-08-06 WO PCT/EP2013/066443 patent/WO2014026880A1/en not_active Ceased
- 2013-08-06 PL PL13747827T patent/PL2882742T3/pl unknown
- 2013-08-06 PE PE2015000196A patent/PE20150685A1/es active IP Right Grant
- 2013-08-06 ES ES13747827.7T patent/ES2601511T3/es active Active
- 2013-08-06 CN CN201380042690.0A patent/CN104540815B/zh active Active
- 2013-08-06 PT PT137478277T patent/PT2882742T/pt unknown
- 2013-08-06 RS RS20161001A patent/RS55397B1/sr unknown
- 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 CL CL2015000290A patent/CL2015000290A1/es unknown
- 2015-02-06 PH PH12015500261A patent/PH12015500261B1/en unknown
- 2015-02-13 US US14/622,232 patent/US9199971B2/en active Active
-
2016
- 2016-12-16 CY CY20161101305T patent/CY1118595T1/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |