MX337443B - Derivados de etinilo como moduladores alostericos positivos del receptor de glutamato metabotropico del subtipo 5 (mglur5). - Google Patents
Derivados de etinilo como moduladores alostericos positivos del receptor de glutamato metabotropico del subtipo 5 (mglur5).Info
- Publication number
- MX337443B MX337443B MX2013011105A MX2013011105A MX337443B MX 337443 B MX337443 B MX 337443B MX 2013011105 A MX2013011105 A MX 2013011105A MX 2013011105 A MX2013011105 A MX 2013011105A MX 337443 B MX337443 B MX 337443B
- Authority
- MX
- Mexico
- Prior art keywords
- hydrogen
- lower alkyl
- mglur5
- positive allosteric
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
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- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P70/00—Climate change mitigation technologies in the production process for final industrial or consumer products
- Y02P70/50—Manufacturing or production processes characterised by the final manufactured product
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02T—CLIMATE CHANGE MITIGATION TECHNOLOGIES RELATED TO TRANSPORTATION
- Y02T10/00—Road transport of goods or passengers
- Y02T10/60—Other road transportation technologies with climate change mitigation effect
- Y02T10/70—Energy storage systems for electromobility, e.g. batteries
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- General Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Secondary Cells (AREA)
- Steroid Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Liquid Crystal Substances (AREA)
Abstract
La presente invención se refiere a derivados de etinilo de la fórmula I, en donde X es N o C-R, en donde R es hidrógeno o halógeno; G es N o CH; con la condición de que como máximo uno de G o X pueda ser nitrógeno; R1 es fenilo o piridinilo, que están opcionalmente sustituidos por halógeno; es hidrógeno, alquilo inferior, hidroxi, alcoxi inferior o C(Q)Q-bencilo; R3, R3', R4, R4', R6, R6' son independientemente entre sí hidrógeno o alquilo inferior; o R6 y R4 junto con el átomo de carbono al que están unidos pueden formar un anillo cicloalquilo C4-6, si m es 0 y n es 1 ó 2; R5 es hidrógeno o alquilo inferior; n es 0, 1 ó 2; m es 0 ó 1; con la condición de que n y m no sean simultáneamente 0; 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. Ahora se ha encontrado de modo sorprendente que los compuestos de la fórmula general I son moduladores alostéricos positivos (PAM) del receptor de glutamato metabotrópico del subtipo 5 (mGluR5). Pueden utilizarse para el tratamiento de la esquizofrenia o trastornos cognitivos.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11163683 | 2011-04-26 | ||
| PCT/EP2012/057335 WO2012146551A1 (en) | 2011-04-26 | 2012-04-23 | Ethynyl derivatives as positive allosteric modulators of the mglur5 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2013011105A MX2013011105A (es) | 2013-10-17 |
| MX337443B true MX337443B (es) | 2016-03-07 |
Family
ID=46025665
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2013011105A MX337443B (es) | 2011-04-26 | 2012-04-23 | Derivados de etinilo como moduladores alostericos positivos del receptor de glutamato metabotropico del subtipo 5 (mglur5). |
Country Status (33)
| Country | Link |
|---|---|
| US (2) | US8957213B2 (es) |
| EP (1) | EP2702051B1 (es) |
| JP (1) | JP5753627B2 (es) |
| KR (1) | KR101554803B1 (es) |
| CN (1) | CN103492373B (es) |
| AR (1) | AR086036A1 (es) |
| AU (1) | AU2012247653B2 (es) |
| BR (1) | BR112013026116A2 (es) |
| CA (1) | CA2829170C (es) |
| CL (1) | CL2013003056A1 (es) |
| CO (1) | CO6801734A2 (es) |
| CR (1) | CR20130475A (es) |
| CY (1) | CY1116391T1 (es) |
| DK (1) | DK2702051T3 (es) |
| EA (1) | EA022019B1 (es) |
| ES (1) | ES2534090T3 (es) |
| HK (1) | HK1191330A1 (es) |
| HR (1) | HRP20150555T1 (es) |
| HU (1) | HUE025031T2 (es) |
| IL (1) | IL228835A (es) |
| MA (1) | MA35133B1 (es) |
| MX (1) | MX337443B (es) |
| MY (1) | MY163164A (es) |
| PE (1) | PE20141169A1 (es) |
| PL (1) | PL2702051T3 (es) |
| PT (1) | PT2702051E (es) |
| RS (1) | RS53903B1 (es) |
| SG (1) | SG194120A1 (es) |
| SI (1) | SI2702051T1 (es) |
| TW (2) | TWI436993B (es) |
| UA (1) | UA110378C2 (es) |
| WO (1) | WO2012146551A1 (es) |
| ZA (1) | ZA201306586B (es) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2829170C (en) * | 2011-04-26 | 2019-02-26 | F. Hoffmann-La Roche Ag | Ethynyl derivatives as positive allosteric modulators of the mglur5 |
| UA110862C2 (uk) * | 2011-10-07 | 2016-02-25 | Ф. Хоффманн-Ля Рош Аг | Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5 |
| EP2875000B1 (en) * | 2012-07-17 | 2016-09-21 | F. Hoffmann-La Roche AG | Arylethynyl derivatives |
| NZ703537A (en) * | 2012-10-18 | 2018-06-29 | Hoffmann La Roche | Ethynyl derivatives |
| UA116023C2 (uk) * | 2013-07-08 | 2018-01-25 | Ф. Хоффманн-Ля Рош Аг | Етинільні похідні як антагоністи метаботропного глутаматного рецептора |
| MA42508B1 (fr) | 2015-06-03 | 2020-05-29 | Hoffmann La Roche | Dérivés d'éthynyle |
| LT3322701T (lt) | 2015-07-15 | 2019-07-10 | F. Hoffmann-La Roche Ag | Etinilo dariniai kaip metabotropinių glutamato receptorių moduliatoriai |
| US10423423B2 (en) * | 2015-09-29 | 2019-09-24 | International Business Machines Corporation | Efficiently managing speculative finish tracking and error handling for load instructions |
| PL3484889T3 (pl) | 2016-07-18 | 2020-12-28 | F. Hoffmann-La Roche Ag | Pochodne etynylu |
| EP3694510A4 (en) * | 2017-10-10 | 2021-06-30 | Biogen Inc. | SPIRO DERIVATIVE PREPARATION PROCESS |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI292318B (en) | 2003-03-10 | 2008-01-11 | Hoffmann La Roche | Imidazol-4-yl-ethynyl-pyridine derivatives |
| GB0325956D0 (en) | 2003-11-06 | 2003-12-10 | Addex Pharmaceuticals Sa | Novel compounds |
| JP5635727B2 (ja) * | 2004-10-07 | 2014-12-03 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | チアゾリルｍｇｌｕｒ５アンタゴニスト及びそれらの使用のための方法 |
| EP1809620B1 (en) | 2004-11-04 | 2010-12-29 | Addex Pharma SA | Novel tetrazole derivatives as positive allosteric modulators of metabotropic glutamate receptors |
| GB0510139D0 (en) | 2005-05-18 | 2005-06-22 | Addex Pharmaceuticals Sa | Novel compounds B1 |
| AU2007267183B2 (en) | 2006-05-31 | 2011-10-20 | F. Hoffmann-La Roche Ag | Aryl-4-ethynyl-isoxazole derivatives |
| JP5622568B2 (ja) * | 2007-06-03 | 2014-11-12 | バンダービルト ユニバーシティ | ベンズアミドｍＧｌｕＲ５の正のアロステリック調節因子ならびにその作製および使用方法 |
| US8034806B2 (en) * | 2007-11-02 | 2011-10-11 | Vanderbilt University | Bicyclic mGluR5 positive allosteric modulators and methods of making and using same |
| AR072940A1 (es) | 2008-08-20 | 2010-09-29 | Schering Corp | Derivados de piridina y pirimidina sustituidos con etinilo y su uso en el tratamiento de infecciones virales |
| US8586581B2 (en) | 2009-12-17 | 2013-11-19 | Hoffmann-La Roche Inc | Ethynyl compounds useful for treatment of CNS disorders |
| US8420661B2 (en) | 2010-04-13 | 2013-04-16 | Hoffmann-La Roche Inc. | Arylethynyl derivatives |
| CA2829170C (en) * | 2011-04-26 | 2019-02-26 | F. Hoffmann-La Roche Ag | Ethynyl derivatives as positive allosteric modulators of the mglur5 |
-
2012
- 2012-04-23 CA CA2829170A patent/CA2829170C/en not_active Expired - Fee Related
- 2012-04-23 PT PT127181535T patent/PT2702051E/pt unknown
- 2012-04-23 RS RS20150192A patent/RS53903B1/en unknown
- 2012-04-23 PL PL12718153T patent/PL2702051T3/pl unknown
- 2012-04-23 HU HUE12718153A patent/HUE025031T2/en unknown
- 2012-04-23 AU AU2012247653A patent/AU2012247653B2/en not_active Ceased
- 2012-04-23 BR BR112013026116A patent/BR112013026116A2/pt not_active IP Right Cessation
- 2012-04-23 US US13/452,973 patent/US8957213B2/en active Active
- 2012-04-23 UA UAA201313475A patent/UA110378C2/uk unknown
- 2012-04-23 SI SI201230199T patent/SI2702051T1/sl unknown
- 2012-04-23 JP JP2014506826A patent/JP5753627B2/ja active Active
- 2012-04-23 MX MX2013011105A patent/MX337443B/es active IP Right Grant
- 2012-04-23 WO PCT/EP2012/057335 patent/WO2012146551A1/en active Application Filing
- 2012-04-23 CN CN201280019903.3A patent/CN103492373B/zh active Active
- 2012-04-23 EA EA201391537A patent/EA022019B1/ru not_active IP Right Cessation
- 2012-04-23 SG SG2013074810A patent/SG194120A1/en unknown
- 2012-04-23 ES ES12718153.5T patent/ES2534090T3/es active Active
- 2012-04-23 DK DK12718153T patent/DK2702051T3/en active
- 2012-04-23 KR KR1020137031119A patent/KR101554803B1/ko active IP Right Grant
- 2012-04-23 EP EP20120718153 patent/EP2702051B1/en active Active
- 2012-04-23 PE PE2013002401A patent/PE20141169A1/es active IP Right Grant
- 2012-04-23 MY MYPI2013003846A patent/MY163164A/en unknown
- 2012-04-24 AR ARP120101405 patent/AR086036A1/es unknown
- 2012-04-24 TW TW101114577A patent/TWI436993B/zh not_active IP Right Cessation
- 2012-04-24 TW TW101114538A patent/TW201306355A/zh unknown
-
2013
- 2013-08-29 CO CO13205214A patent/CO6801734A2/es active IP Right Grant
- 2013-09-02 ZA ZA2013/06586A patent/ZA201306586B/en unknown
- 2013-09-23 CR CR20130475A patent/CR20130475A/es unknown
- 2013-10-10 IL IL228835A patent/IL228835A/en active IP Right Grant
- 2013-10-22 CL CL2013003056A patent/CL2013003056A1/es unknown
- 2013-11-22 MA MA36462A patent/MA35133B1/fr unknown
-
2014
- 2014-05-09 HK HK14104405.5A patent/HK1191330A1/xx unknown
-
2015
- 2015-01-06 US US14/590,530 patent/US9212171B2/en active Active
- 2015-05-20 CY CY20151100452T patent/CY1116391T1/el unknown
- 2015-05-26 HR HRP20150555TT patent/HRP20150555T1/hr unknown
Also Published As
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