AR086037A1 - Derivados de pirazolidin-3-ona - Google Patents
Derivados de pirazolidin-3-onaInfo
- Publication number
- AR086037A1 AR086037A1 ARP120101406A ARP120101406A AR086037A1 AR 086037 A1 AR086037 A1 AR 086037A1 AR P120101406 A ARP120101406 A AR P120101406A AR P120101406 A ARP120101406 A AR P120101406A AR 086037 A1 AR086037 A1 AR 086037A1
- Authority
- AR
- Argentina
- Prior art keywords
- lower alkyl
- hydrogen
- derivatives
- pirazolidin
- ona
- Prior art date
Links
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-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
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 150000002431 hydrogen Chemical group 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 230000003281 allosteric effect Effects 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 230000003287 optical effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (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
La presente se refiere a derivados de etinilo de la fórmula (1) en la que: X es N o CH; G es N o CH; con la condición de que como máximo uno de X y G pueda ser nitrógeno; R1 es fenilo o piridilo, que están opcionalmente sustituidos por halógeno, alquilo inferior o alcoxi inferior; R2 es hidrógeno, alquilo inferior o junto con R4 puede formar un cicloalquilo C3-6; R3/R3’/R4/R4’ con independencia entre sí son hidrógeno, alquilo inferior o CF3; o a una sal de adición de ácido farmacéuticamente aceptable, a una mezcla racémica, o a sus enantiómeros y/o isómeros ópticos y/o estereoisómeros correspondientes. Los compuestos de la fórmula general (1) son moduladores alostéricos positivos (PAM) del receptor del glutamato metabotrópico del subtipo 5 (mGluR5). Procesos de obtención y composiciones farmacéuticas.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11163708 | 2011-04-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR086037A1 true AR086037A1 (es) | 2013-11-13 |
Family
ID=45998366
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120101406A AR086037A1 (es) | 2011-04-26 | 2012-04-24 | Derivados de pirazolidin-3-ona |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US8648088B2 (es) |
| EP (1) | EP2702050B1 (es) |
| JP (1) | JP5753626B2 (es) |
| KR (1) | KR101576343B1 (es) |
| CN (1) | CN103492374B (es) |
| AR (1) | AR086037A1 (es) |
| CA (1) | CA2829171C (es) |
| CL (1) | CL2013003068A1 (es) |
| CO (1) | CO6801735A2 (es) |
| CR (1) | CR20130476A (es) |
| EA (1) | EA023146B1 (es) |
| EC (1) | ECSP13012990A (es) |
| ES (1) | ES2580333T3 (es) |
| IL (1) | IL229005A (es) |
| MA (1) | MA35134B1 (es) |
| MX (1) | MX2013011107A (es) |
| MY (1) | MY165141A (es) |
| PE (1) | PE20141168A1 (es) |
| PH (1) | PH12013501928A1 (es) |
| SG (1) | SG194095A1 (es) |
| TW (1) | TWI434840B (es) |
| UA (1) | UA113625C2 (es) |
| WO (1) | WO2012146552A1 (es) |
| ZA (1) | ZA201307404B (es) |
Families Citing this family (7)
| 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 |
| AU2016273751B2 (en) | 2015-06-03 | 2020-04-02 | F. Hoffmann-La Roche Ag | Ethynyl derivatives |
| MA42442B1 (fr) | 2015-07-15 | 2019-07-31 | Hoffmann La Roche | Dérivés d'éthynyle comme modulateurs du récepteur métabotropique au glutamate |
| AR105556A1 (es) * | 2015-08-03 | 2017-10-18 | Hoffmann La Roche | Derivados de etinilo |
| CA3030788A1 (en) | 2016-07-18 | 2018-01-25 | F. Hoffmann-La Roche Ag | Ethynyl derivatives |
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 |
| CA2583572C (en) * | 2004-10-07 | 2016-07-12 | Merck & Co., Inc. | Thiazolyl mglur5 antagonists and methods for their use |
| 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 |
| EP1919890A1 (en) * | 2005-08-19 | 2008-05-14 | AstraZeneca AB | Pyrazolone derivatives for the treatment of tuberculosis |
| MX2009013169A (es) | 2007-06-03 | 2010-04-30 | Univ Vanderbilt | Moduladores alostericos positivos del mglur5 benzamida y metodos de elaboracion y uso de los mismos. |
| 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 PH PH1/2013/501928A patent/PH12013501928A1/en unknown
- 2012-04-23 WO PCT/EP2012/057336 patent/WO2012146552A1/en not_active Ceased
- 2012-04-23 CN CN201280019941.9A patent/CN103492374B/zh not_active Expired - Fee Related
- 2012-04-23 KR KR1020137031117A patent/KR101576343B1/ko not_active Expired - Fee Related
- 2012-04-23 MY MYPI2013003847A patent/MY165141A/en unknown
- 2012-04-23 SG SG2013074414A patent/SG194095A1/en unknown
- 2012-04-23 UA UAA201313476A patent/UA113625C2/uk unknown
- 2012-04-23 EA EA201391538A patent/EA023146B1/ru not_active IP Right Cessation
- 2012-04-23 PE PE2013002402A patent/PE20141168A1/es active IP Right Grant
- 2012-04-23 MX MX2013011107A patent/MX2013011107A/es active IP Right Grant
- 2012-04-23 CA CA2829171A patent/CA2829171C/en not_active Expired - Fee Related
- 2012-04-23 JP JP2014505663A patent/JP5753626B2/ja not_active Expired - Fee Related
- 2012-04-23 ES ES12716007.5T patent/ES2580333T3/es active Active
- 2012-04-23 EP EP12716007.5A patent/EP2702050B1/en active Active
- 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
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| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |