PE20150685A1 - Pirimidinas de ariletinilo - Google Patents
Pirimidinas de ariletiniloInfo
- Publication number
- PE20150685A1 PE20150685A1 PE2015000196A PE2015000196A PE20150685A1 PE 20150685 A1 PE20150685 A1 PE 20150685A1 PE 2015000196 A PE2015000196 A PE 2015000196A PE 2015000196 A PE2015000196 A PE 2015000196A PE 20150685 A1 PE20150685 A1 PE 20150685A1
- Authority
- PE
- Peru
- Prior art keywords
- aryletinyl
- pyrimidines
- 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)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (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 invencion se refiere a derivados de etinilo de la formula l: en la que: R1 es hidrogeno o halogeno; R2 es alquilo C1-3 O -(CH2)n-O-CH3; n es el numero 2 o 3; m es el numero 1 o 2; o a una sal de adicion de acido farmaceuticamente aceptable, a una mezcla racemica, o a su enantiomero correspondiente y/o isomero optico y/o estereoisomero de los mismos. Se ha encontrado que los compuestos de la formula general I son moduladores alostericos del receptor de glutamato metabotropico del subtipo 5 (mGluR5) con propiedades mejoradas para el tratamiento de la esquizofrenia, las enfermedades cognitivas, el sindrome de la X fragil o el autismo
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12180209 | 2012-08-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20150685A1 true PE20150685A1 (es) | 2015-05-11 |
Family
ID=46851291
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2015000196A PE20150685A1 (es) | 2012-08-13 | 2013-08-06 | Pirimidinas 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 |
| 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 |
| DE602005007350D1 (de) * | 2004-06-01 | 2008-07-17 | Hoffmann La Roche | Pyridin-4-yl-ethynylimidazole und -pyrazole als antagonisten des mglu5-rezeptors |
| WO2006048771A1 (en) | 2004-11-04 | 2006-05-11 | Addex Pharmaceuticals 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 |
| NZ581817A (en) | 2007-06-03 | 2012-05-25 | 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 |
| NZ603868A (en) * | 2010-07-09 | 2014-08-29 | Recordati Ireland Ltd | Novel spiroheterocyclic compounds as mglu5 antagonists |
| US8642626B2 (en) * | 2010-07-29 | 2014-02-04 | Taisho Pharmaceutical Co., Ltd. | Ethinyl-pyrazole derivative |
| PE20141168A1 (es) * | 2011-04-26 | 2014-09-22 | Hoffmann La Roche | 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 |
| 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 |
| LT2875000T (lt) * | 2012-07-17 | 2016-11-10 | F.Hoffmann-La Roche Ag | Ariletinilo dariniai |
| PL2900659T3 (pl) * | 2012-09-27 | 2017-02-28 | F.Hoffmann-La Roche Ag | Pochodne aryloetynylowe |
-
2013
- 2013-06-08 UA UAA201501613A patent/UA113223C2/uk unknown
- 2013-08-06 NZ NZ704858A patent/NZ704858A/en not_active IP Right Cessation
- 2013-08-06 PT PT137478277T patent/PT2882742T/pt unknown
- 2013-08-06 PL PL13747827T patent/PL2882742T3/pl unknown
- 2013-08-06 HU HUE13747827A patent/HUE030237T2/en unknown
- 2013-08-06 SG SG11201501055SA patent/SG11201501055SA/en unknown
- 2013-08-06 MY MYPI2015000358A patent/MY170255A/en unknown
- 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 HR HRP20161692TT patent/HRP20161692T1/hr unknown
- 2013-08-06 ES ES13747827.7T patent/ES2601511T3/es active Active
- 2013-08-06 WO PCT/EP2013/066443 patent/WO2014026880A1/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 EA EA201590252A patent/EA025165B1/ru not_active IP Right Cessation
- 2013-08-06 JP JP2015526930A patent/JP5974179B2/ja active Active
- 2013-08-06 CN CN201380042690.0A patent/CN104540815B/zh active Active
- 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 MA MA37895A patent/MA37895B1/fr unknown
- 2013-08-06 DK DK13747827.7T patent/DK2882742T3/en active
- 2013-08-06 SI SI201330420A patent/SI2882742T1/sl unknown
- 2013-08-06 KR KR1020157006196A patent/KR101747005B1/ko not_active Expired - Fee Related
- 2013-08-06 AU AU2013304212A patent/AU2013304212B2/en not_active Ceased
- 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 |
|---|---|---|---|
| FG | Grant, registration |