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
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)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (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 (36)
| 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) |
| HK (1) | HK1207378A1 (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) | PH12015500261A1 (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 |
|---|---|---|---|---|
| MY174339A (en) | 2012-08-13 | 2020-04-09 | Novartis Ag | 1,4-disubstituted pyridazine analogs and methods for treating smn-deficiency-related conditions |
| PE20150733A1 (es) * | 2012-10-18 | 2015-05-17 | Hoffmann La Roche | Derivados de etinilo como moduladores de la actividad del receptor mglur5 |
| KR102035048B1 (ko) * | 2015-06-03 | 2019-10-22 | 에프. 호프만-라 로슈 아게 | 에틴일 유도체 |
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 |
| PL1756086T3 (pl) * | 2004-06-01 | 2008-11-28 | Hoffmann La Roche | Pirydyn-4-ylo-etynylo-imidazole i pirazole jako antagoniści receptora mGlu5 |
| 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 |
| SG185285A1 (en) * | 2007-06-03 | 2012-11-29 | Univ Vanderbilt | Benzamide mglur5 positive allosteric modulators and methods of making and using same |
| AU2008317544A1 (en) * | 2007-10-26 | 2009-04-30 | Astrazeneca Ab | Amino 1,2,4-triazole derivatives as modulators of 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 |
| KR101862626B1 (ko) * | 2010-07-09 | 2018-05-31 | 레코르다티 아일랜드 리미티드 | Mglu5 대항체로서의 신 스피로헤테로사이클릭 화합물 |
| EP2599775A4 (en) * | 2010-07-29 | 2014-04-30 | Taisho Pharmaceutical Co Ltd | ETHINYLPYRAZOLDERIVAT |
| ES2580333T3 (es) * | 2011-04-26 | 2016-08-23 | F. Hoffmann-La Roche Ag | Derivados de pirazolidin-3-ona |
| 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 |
| DK2875000T3 (en) * | 2012-07-17 | 2016-10-24 | Hoffmann La Roche | ARYLETHYNYL DERIVATIVES |
| DK2900659T3 (en) * | 2012-09-27 | 2016-10-03 | Hoffmann La Roche | ARYLETHYNYL DERIVATIVES |
-
2013
- 2013-06-08 UA UAA201501613A patent/UA113223C2/uk unknown
- 2013-08-06 KR KR1020157006196A patent/KR101747005B1/ko active IP Right Grant
- 2013-08-06 SG SG11201501055SA patent/SG11201501055SA/en unknown
- 2013-08-06 PL PL13747827T patent/PL2882742T3/pl unknown
- 2013-08-06 RS RS20161001A patent/RS55397B1/sr unknown
- 2013-08-06 BR BR112015002921A patent/BR112015002921A2/pt not_active Application Discontinuation
- 2013-08-06 CN CN201380042690.0A patent/CN104540815B/zh active Active
- 2013-08-06 EP EP13747827.7A patent/EP2882742B1/en active Active
- 2013-08-06 HU HUE13747827A patent/HUE030237T2/en unknown
- 2013-08-06 LT LTEP13747827.7T patent/LT2882742T/lt 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 MX MX2015001599A patent/MX358011B/es active IP Right Grant
- 2013-08-06 PE PE2015000196A patent/PE20150685A1/es active IP Right Grant
- 2013-08-06 AU AU2013304212A patent/AU2013304212B2/en not_active Ceased
- 2013-08-06 EA EA201590252A patent/EA025165B1/ru not_active IP Right Cessation
- 2013-08-06 MA MA37895A patent/MA37895B1/fr unknown
- 2013-08-06 MY MYPI2015000358A patent/MY170255A/en unknown
- 2013-08-06 JP JP2015526930A patent/JP5974179B2/ja active Active
- 2013-08-06 SI SI201330420A patent/SI2882742T1/sl unknown
- 2013-08-06 NZ NZ704858A patent/NZ704858A/en not_active IP Right Cessation
- 2013-08-06 WO PCT/EP2013/066443 patent/WO2014026880A1/en active Application Filing
- 2013-08-06 PT PT137478277T patent/PT2882742T/pt unknown
- 2013-08-06 ES ES13747827.7T patent/ES2601511T3/es 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/PH12015500261A1/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
-
2016
- 2016-12-12 HR HRP20161692TT patent/HRP20161692T1/hr unknown
- 2016-12-16 CY CY20161101305T patent/CY1118595T1/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |