CO7180198A2 - Ariletinilo pirimidinas - Google Patents
Ariletinilo pirimidinasInfo
- Publication number
- CO7180198A2 CO7180198A2 CO15013232A CO15013232A CO7180198A2 CO 7180198 A2 CO7180198 A2 CO 7180198A2 CO 15013232 A CO15013232 A CO 15013232A CO 15013232 A CO15013232 A CO 15013232A CO 7180198 A2 CO7180198 A2 CO 7180198A2
- Authority
- CO
- Colombia
- Prior art keywords
- res
- formula
- mglur5
- autism
- schizophrenia
- Prior art date
Links
- 150000003230 pyrimidines Chemical class 0.000 title 1
- 206010003805 Autism Diseases 0.000 abstract 2
- 208000020706 Autistic disease Diseases 0.000 abstract 2
- 208000001914 Fragile X syndrome Diseases 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 102000016193 Metabotropic glutamate receptors Human genes 0.000 abstract 2
- 108010010914 Metabotropic glutamate receptors Proteins 0.000 abstract 2
- 239000002253 acid Substances 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 230000003281 allosteric effect Effects 0.000 abstract 2
- 208000010877 cognitive disease Diseases 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 230000003287 optical effect Effects 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 201000000980 schizophrenia Diseases 0.000 abstract 2
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 presente invención se refiere a derivados de etinilo de la fórmula I: La presente invención se refiere a derivados de etinilo de la fórmula I: en la que: Res hidrógeno o halógeno; 1 Res alquilo Co -(CH)n-O-CH; 2 1-3 2 3 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 I 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. en la que: Res hidrógeno o halógeno; 1 Res alquilo Co -(CH)n-O-CH; 2 1-3 2 3 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 I 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 |
|---|---|
| CO7180198A2 true CO7180198A2 (es) | 2015-02-09 |
Family
ID=46851291
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO15013232A CO7180198A2 (es) | 2012-08-13 | 2015-01-23 | Ariletinilo pirimidinas |
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 |
| UA114008C2 (xx) * | 2012-10-18 | 2017-04-10 | Похідні етинілу як модулятори активності рецептора mglur5 | |
| MX378334B (es) * | 2015-06-03 | 2025-03-10 | Hoffmann La Roche | Modulador alostérico negativo de un receptor de glutamato metabotrópico (nam) y el uso del mismo para tratar ansiedad, dolor, depresión, parkinson y reflujo gastroesofágico. |
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 |
| 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 |
| CA2689282A1 (en) | 2007-06-03 | 2008-12-11 | Vanderbilt University | Benzamide mglur5 positive allosteric modulators and methods of making and using same |
| EA201000656A1 (ru) * | 2007-10-26 | 2010-12-30 | Астразенека Аб | Аминопроизводные 1,2,4-триазола в качестве модуляторов 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 |
| ES2492694T3 (es) * | 2010-07-09 | 2014-09-10 | Recordati Ireland Limited | Nuevos compuestos espiroheterocíclicos como antagonistas de mGlu5 |
| EP2599775A4 (en) * | 2010-07-29 | 2014-04-30 | Taisho Pharmaceutical Co Ltd | ETHINYLPYRAZOLDERIVAT |
| EA023146B1 (ru) * | 2011-04-26 | 2016-04-29 | Ф.Хоффманн-Ля Рош Аг | Производные пиразолидин-3-она |
| 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 |
| WO2014012851A1 (en) * | 2012-07-17 | 2014-01-23 | F. Hoffmann-La Roche Ag | Arylethynyl derivatives |
| BR112015006218A2 (pt) * | 2012-09-27 | 2017-07-04 | Hoffmann La Roche | derivados de ariletinil |
-
2013
- 2013-06-08 UA UAA201501613A patent/UA113223C2/uk 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 BR BR112015002921A patent/BR112015002921A2/pt not_active Application Discontinuation
- 2013-08-06 AU AU2013304212A patent/AU2013304212B2/en not_active Ceased
- 2013-08-06 SG SG11201501055SA patent/SG11201501055SA/en unknown
- 2013-08-06 HR HRP20161692TT patent/HRP20161692T1/hr unknown
- 2013-08-06 PT PT137478277T patent/PT2882742T/pt unknown
- 2013-08-06 HU HUE13747827A patent/HUE030237T2/en unknown
- 2013-08-06 KR KR1020157006196A patent/KR101747005B1/ko not_active Expired - Fee Related
- 2013-08-06 EP EP13747827.7A patent/EP2882742B1/en active Active
- 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 RS RS20161001A patent/RS55397B1/sr unknown
- 2013-08-06 NZ NZ704858A patent/NZ704858A/en not_active IP Right Cessation
- 2013-08-06 LT LTEP13747827.7T patent/LT2882742T/lt unknown
- 2013-08-06 CN CN201380042690.0A patent/CN104540815B/zh active Active
- 2013-08-06 CA CA2880257A patent/CA2880257C/en not_active Expired - Fee Related
- 2013-08-06 PL PL13747827T patent/PL2882742T3/pl unknown
- 2013-08-06 SI SI201330420A patent/SI2882742T1/sl unknown
- 2013-08-06 ES ES13747827.7T patent/ES2601511T3/es active Active
- 2013-08-06 MA MA37895A patent/MA37895B1/fr unknown
- 2013-08-06 WO PCT/EP2013/066443 patent/WO2014026880A1/en not_active Ceased
- 2013-08-06 DK DK13747827.7T patent/DK2882742T3/en 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
-
2016
- 2016-12-16 CY CY20161101305T patent/CY1118595T1/el unknown
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