ECSP13012990A - Derivados de pirazolidin-3-ona - Google Patents
Derivados de pirazolidin-3-onaInfo
- Publication number
- ECSP13012990A ECSP13012990A ECSP13012990A ECSP13012990A EC SP13012990 A ECSP13012990 A EC SP13012990A EC SP13012990 A ECSP13012990 A EC SP13012990A EC SP13012990 A ECSP13012990 A EC SP13012990A
- Authority
- EC
- Ecuador
- 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
- 102000012777 Metabotropic Glutamate 5 Receptor Human genes 0.000 abstract 2
- 108010065028 Metabotropic Glutamate 5 Receptor 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
- 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)
- 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
La presente invención se refiere a derivados de etinilo de la fórmula Ien 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-C6;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.Ahora se ha encontrado de modo sorprendente que los compuestos de la fórmula general I son moduladores alostéricos positivos (PAM) del receptor del glutamato metabotrópico del subtipo 5 (mGluR5).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11163708 | 2011-04-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP13012990A true ECSP13012990A (es) | 2013-11-29 |
Family
ID=45998366
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSP13012990 ECSP13012990A (es) | 2011-04-26 | 2013-10-24 | 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 |
| JP6603334B2 (ja) | 2015-06-03 | 2019-11-06 | エフ．ホフマン−ラ ロシュ アーゲー | エチニル誘導体 |
| LT3322701T (lt) | 2015-07-15 | 2019-07-10 | F. Hoffmann-La Roche Ag | Etinilo dariniai kaip metabotropinių glutamato receptorių moduliatoriai |
| AR105556A1 (es) * | 2015-08-03 | 2017-10-18 | Hoffmann La Roche | Derivados de etinilo |
| CR20190014A (es) | 2016-07-18 | 2019-03-04 | Hoffmann La Roche | Derivados 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 |
| 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 |
| 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 |
| WO2007020426A1 (en) * | 2005-08-19 | 2007-02-22 | Astrazeneca Ab | Pyrazolone derivatives for the treatment of tuberculosis |
| EP2162136A4 (en) | 2007-06-03 | 2012-02-15 | Univ Vanderbilt | GLUTAMATE METABOTROPIC POSITIVE RECEPTOR-BASED ALLOSTERIC-MODULATOR BENZAMIDE DERIVATIVES (MGLUR5) AND METHODS OF MAKING AND USING THEM |
| 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 KR KR1020137031117A patent/KR101576343B1/ko not_active Expired - Fee Related
- 2012-04-23 MY MYPI2013003847A patent/MY165141A/en unknown
- 2012-04-23 EA EA201391538A patent/EA023146B1/ru not_active IP Right Cessation
- 2012-04-23 CN CN201280019941.9A patent/CN103492374B/zh not_active Expired - Fee Related
- 2012-04-23 EP EP12716007.5A patent/EP2702050B1/en active Active
- 2012-04-23 SG SG2013074414A patent/SG194095A1/en unknown
- 2012-04-23 WO PCT/EP2012/057336 patent/WO2012146552A1/en not_active Ceased
- 2012-04-23 UA UAA201313476A patent/UA113625C2/uk unknown
- 2012-04-23 ES ES12716007.5T patent/ES2580333T3/es active Active
- 2012-04-23 PE PE2013002402A patent/PE20141168A1/es active IP Right Grant
- 2012-04-23 PH PH1/2013/501928A patent/PH12013501928A1/en unknown
- 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 MX MX2013011107A patent/MX2013011107A/es active IP Right Grant
- 2012-04-24 AR ARP120101406A patent/AR086037A1/es unknown
- 2012-04-24 US US13/454,167 patent/US8648088B2/en not_active Expired - Fee Related
- 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
Also Published As
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