EA201391538A1 - Производные пиразолидин-3-она - Google Patents
Производные пиразолидин-3-онаInfo
- Publication number
- EA201391538A1 EA201391538A1 EA201391538A EA201391538A EA201391538A1 EA 201391538 A1 EA201391538 A1 EA 201391538A1 EA 201391538 A EA201391538 A EA 201391538A EA 201391538 A EA201391538 A EA 201391538A EA 201391538 A1 EA201391538 A1 EA 201391538A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- lower alkyl
- hydrogen
- formula
- pyrazolidin
- derivatives
- Prior art date
Links
Classifications
-
- 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
-
- 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
- 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
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Neurosurgery (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Изобретение относится к этинильным производным формулы I, где X представляет собой N или CH; G представляет собой N или СН; при условии, что максимально один из X или G может представлять собой азот; Rпредставляет собой фенил или пиридил, которые возможно замещены атомом галогена, низшим алкилом или низшим алкокси; Rпредставляет собой водород, низший алкил или вместе с Rможет образовывать С-С-циклоалкил; R, R, R, Rнезависимо друг от друга представляют собой водород, низший алкил или CF; или к фармацевтически приемлемой соли присоединения кислоты, к рацемической смеси, или к ее соответствующему энантиомеру, и/или их оптическому изомеру, и/или стереоизомеру. Было обнаружено, что соединения общей формулы I представляют собой положительные аллостерические модуляторы (РАМ) метаботропного глутаматного рецептора, подтипа 5 (mGluR5).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11163708 | 2011-04-26 | ||
| PCT/EP2012/057336 WO2012146552A1 (en) | 2011-04-26 | 2012-04-23 | Pyrazolidin-3-one derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201391538A1 true EA201391538A1 (ru) | 2014-04-30 |
| EA023146B1 EA023146B1 (ru) | 2016-04-29 |
Family
ID=45998366
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201391538A EA023146B1 (ru) | 2011-04-26 | 2012-04-23 | Производные пиразолидин-3-она |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US8648088B2 (ru) |
| EP (1) | EP2702050B1 (ru) |
| JP (1) | JP5753626B2 (ru) |
| KR (1) | KR101576343B1 (ru) |
| CN (1) | CN103492374B (ru) |
| AR (1) | AR086037A1 (ru) |
| CA (1) | CA2829171C (ru) |
| CL (1) | CL2013003068A1 (ru) |
| CO (1) | CO6801735A2 (ru) |
| CR (1) | CR20130476A (ru) |
| EA (1) | EA023146B1 (ru) |
| EC (1) | ECSP13012990A (ru) |
| ES (1) | ES2580333T3 (ru) |
| HK (1) | HK1191329A1 (ru) |
| IL (1) | IL229005A (ru) |
| MA (1) | MA35134B1 (ru) |
| MX (1) | MX2013011107A (ru) |
| MY (1) | MY165141A (ru) |
| PE (1) | PE20141168A1 (ru) |
| SG (1) | SG194095A1 (ru) |
| TW (1) | TWI434840B (ru) |
| UA (1) | UA113625C2 (ru) |
| WO (1) | WO2012146552A1 (ru) |
| ZA (1) | ZA201307404B (ru) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA110862C2 (uk) * | 2011-10-07 | 2016-02-25 | Ф. Хоффманн-Ля Рош Аг | Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5 |
| UA113223C2 (xx) * | 2012-08-13 | 2016-12-26 | Арилетинілпіримідини | |
| 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 |
| HUE045145T2 (hu) | 2015-07-15 | 2019-12-30 | Hoffmann La Roche | Etinil-származékok metabotróp glutamátreceptor-modulátorokként |
| AR105556A1 (es) * | 2015-08-03 | 2017-10-18 | Hoffmann La Roche | Derivados de etinilo |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0325956D0 (en) | 2003-11-06 | 2003-12-10 | Addex Pharmaceuticals Sa | Novel compounds |
| US7879882B2 (en) * | 2004-10-07 | 2011-02-01 | Merck Sharp & Dohme Corp. | Thiazolyl mglur5 antagonists and methods for their use |
| WO2006048771A1 (en) | 2004-11-04 | 2006-05-11 | Addex Pharmaceuticals 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 |
| AU2006281242A1 (en) * | 2005-08-19 | 2007-02-22 | Astrazeneca Ab | Pyrazolone derivatives for the treatment of tuberculosis |
| SG185285A1 (en) | 2007-06-03 | 2012-11-29 | Univ Vanderbilt | Benzamide mglur5 positive allosteric modulators and methods of making and using same |
| US8853392B2 (en) * | 2007-06-03 | 2014-10-07 | Vanderbilt University | Benzamide mGluR5 positive allosteric modulators and methods of making and using same |
-
2012
- 2012-04-23 MX MX2013011107A patent/MX2013011107A/es active IP Right Grant
- 2012-04-23 EP EP12716007.5A patent/EP2702050B1/en active Active
- 2012-04-23 UA UAA201313476A patent/UA113625C2/uk unknown
- 2012-04-23 CN CN201280019941.9A patent/CN103492374B/zh active Active
- 2012-04-23 PE PE2013002402A patent/PE20141168A1/es active IP Right Grant
- 2012-04-23 MY MYPI2013003847A patent/MY165141A/en unknown
- 2012-04-23 JP JP2014505663A patent/JP5753626B2/ja active Active
- 2012-04-23 KR KR1020137031117A patent/KR101576343B1/ko active IP Right Grant
- 2012-04-23 EA EA201391538A patent/EA023146B1/ru not_active IP Right Cessation
- 2012-04-23 SG SG2013074414A patent/SG194095A1/en unknown
- 2012-04-23 ES ES12716007.5T patent/ES2580333T3/es active Active
- 2012-04-23 CA CA2829171A patent/CA2829171C/en not_active Expired - Fee Related
- 2012-04-23 WO PCT/EP2012/057336 patent/WO2012146552A1/en active Application Filing
- 2012-04-24 AR ARP120101406A patent/AR086037A1/es unknown
- 2012-04-24 US US13/454,167 patent/US8648088B2/en active Active
- 2012-04-25 TW TW101114780A patent/TWI434840B/zh not_active IP Right Cessation
-
2013
- 2013-08-29 CO CO13205224A patent/CO6801735A2/es active IP Right Grant
- 2013-09-23 CR CR20130476A patent/CR20130476A/es unknown
- 2013-10-03 ZA ZA2013/07404A patent/ZA201307404B/en unknown
- 2013-10-21 IL IL229005A patent/IL229005A/en active IP Right Grant
- 2013-10-23 CL CL2013003068A patent/CL2013003068A1/es unknown
- 2013-10-24 EC ECSP13012990 patent/ECSP13012990A/es unknown
- 2013-11-22 MA MA36463A patent/MA35134B1/fr unknown
-
2014
- 2014-05-09 HK HK14104404.6A patent/HK1191329A1/zh unknown
Also Published As
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG MD TJ TM |
|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): RU |