AR079467A1 - Derivados heterociclicos nitrogenados de etinilo, composiciones farmaceuticas que los contienen, proceso para prepararlos y uso de los mismos para tratar y/o prevenir enfermedades cognitivas o esquizofrenia. - Google Patents
Derivados heterociclicos nitrogenados de etinilo, composiciones farmaceuticas que los contienen, proceso para prepararlos y uso de los mismos para tratar y/o prevenir enfermedades cognitivas o esquizofrenia.Info
- Publication number
- AR079467A1 AR079467A1 ARP100104641A ARP100104641A AR079467A1 AR 079467 A1 AR079467 A1 AR 079467A1 AR P100104641 A ARP100104641 A AR P100104641A AR P100104641 A ARP100104641 A AR P100104641A AR 079467 A1 AR079467 A1 AR 079467A1
- Authority
- AR
- Argentina
- Prior art keywords
- nitrogen
- lower alkyl
- schizophrenia
- treat
- prepare
- Prior art date
Links
Classifications
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- 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
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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
- A61K31/495—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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/24—Antidepressants
-
- 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
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Addiction (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyridine Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
La presente se refiere a derivados de etinilo de la formula 1 en la que: X es N o C-R; Y es No C-R2 Z es CH o N; - R4 es un sustituyente aromático de 6 eslabones que contiene 0, 1 o 2 átomos de nitrogeno, opcionalmente sustituido de 1 a 3 veces por grupos elegidos entre halogeno, alquilo inferior, alcoxi inferior y NRR'; R1 es hidrogeno, alquilo inferior, alcoxi inferior, hidroxi, hidroxialquilo inferior, cicloalquilo inferior o es heterocicloalquilo opcionalmente sustituido por hidroxi o alcoxi; R2 es hidrogeno, CN, alquilo inferior o heterocicloalquilo; R y R' son con independencia entre sí hidrogeno o alquilo inferior; o a una sal farmacéuticamente aceptable o una sal de adicion de ácido, a una mezcla racémica, o a sus correspondientes enantiomeros y/o isomeros opticos y/o estereoisomeros. Los compuestos de la formula general 1 son moduladores alostéricos positivos (PAM) del receptor de glutamato metabotropico del subtipo 5 (mGIuR5) y por tanto son utiles para el tratamiento de enfermedades relacionadas con este receptor.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP09179719 | 2009-12-17 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR079467A1 true AR079467A1 (es) | 2012-01-25 |
Family
ID=43446449
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP100104641A AR079467A1 (es) | 2009-12-17 | 2010-12-15 | Derivados heterociclicos nitrogenados de etinilo, composiciones farmaceuticas que los contienen, proceso para prepararlos y uso de los mismos para tratar y/o prevenir enfermedades cognitivas o esquizofrenia. |
Country Status (27)
Country | Link |
---|---|
US (2) | US8586581B2 (es) |
EP (1) | EP2513102B1 (es) |
JP (1) | JP5763094B2 (es) |
KR (1) | KR101407856B1 (es) |
CN (1) | CN102686589B (es) |
AR (1) | AR079467A1 (es) |
AU (1) | AU2010332987B2 (es) |
BR (1) | BR112012014770A2 (es) |
CA (1) | CA2780155A1 (es) |
CL (1) | CL2012001596A1 (es) |
CO (1) | CO6531478A2 (es) |
CR (1) | CR20120269A (es) |
EC (1) | ECSP12011977A (es) |
ES (1) | ES2551582T3 (es) |
HK (1) | HK1171225A1 (es) |
IL (1) | IL219371A (es) |
MA (1) | MA33802B1 (es) |
MX (1) | MX2012006789A (es) |
MY (1) | MY162998A (es) |
NZ (1) | NZ599553A (es) |
PE (1) | PE20121443A1 (es) |
RU (1) | RU2553461C2 (es) |
SG (1) | SG181779A1 (es) |
TW (1) | TWI448465B (es) |
UA (1) | UA107002C2 (es) |
WO (1) | WO2011073172A1 (es) |
ZA (1) | ZA201204429B (es) |
Families Citing this family (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2689956T3 (es) * | 2010-11-05 | 2018-11-16 | Oat Agrio Co., Ltd. | Compuesto de etinilfenilamidina o sal del mismo, procedimiento para producir el mismo y fungicida para una utilización agrícola y hortícola |
US8957213B2 (en) | 2011-04-26 | 2015-02-17 | Hoffman-La Roche Inc. | Ethynyl compounds |
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 |
DK2900659T3 (en) * | 2012-09-27 | 2016-10-03 | Hoffmann La Roche | ARYLETHYNYL DERIVATIVES |
PE20150733A1 (es) * | 2012-10-18 | 2015-05-17 | Hoffmann La Roche | Derivados de etinilo como moduladores de la actividad del receptor mglur5 |
CA2888324A1 (en) * | 2012-11-07 | 2014-05-15 | Alexander Flohr | Triazolo compounds |
KR102035048B1 (ko) | 2015-06-03 | 2019-10-22 | 에프. 호프만-라 로슈 아게 | 에틴일 유도체 |
LT3322701T (lt) | 2015-07-15 | 2019-07-10 | F. Hoffmann-La Roche Ag | Etinilo dariniai kaip metabotropinių glutamato receptorių moduliatoriai |
DK3484889T3 (da) | 2016-07-18 | 2020-10-26 | Hoffmann La Roche | Ethynylderivater |
Family Cites Families (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PT1117403E (pt) * | 1998-10-02 | 2004-04-30 | Sibia Neurosciences Inc | Antagonistas de mglurs para o tratamento da dor e ansiedade |
AR029803A1 (es) | 2000-02-21 | 2003-07-16 | Smithkline Beecham Plc | Imidazoles sustituidos con piridilo y composiciones farmaceuticas que las comprenden |
GB0027987D0 (en) | 2000-11-16 | 2001-01-03 | Smithkline Beecham Plc | Compounds |
US6910976B2 (en) | 2001-06-26 | 2005-06-28 | Stx, Llc | Multi-component lacrosse stick head |
GB0127433D0 (en) * | 2001-11-15 | 2002-01-09 | Smithkline Beecham Corp | Compounds |
GB0127430D0 (en) * | 2001-11-15 | 2002-01-09 | Smithkline Beecham Corp | Compounds |
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 |
GB0413605D0 (en) | 2004-06-17 | 2004-07-21 | Addex Pharmaceuticals Sa | Novel compounds |
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 |
JP2008542322A (ja) * | 2005-06-01 | 2008-11-27 | ユセベ ファルマ ソシエテ アノニム | 2−オキソ−1−ピロリジン誘導体 |
CN102887891B (zh) | 2005-11-15 | 2016-03-09 | 阿雷生物药品公司 | N4-苯基-喹唑啉-4-胺衍生物和相关化合物 |
MX2008016523A (es) | 2006-06-30 | 2009-01-19 | Astrazeneca Ab | Derivados de pirimidina utiles en el tratamiento de cancer. |
EP1972628A1 (en) | 2007-03-21 | 2008-09-24 | Schwarz Pharma Ag | Indolizines and aza-analog derivatives thereof as CNS active compounds |
MX2009011753A (es) * | 2007-04-30 | 2009-12-01 | Abbott Lab | Inhibidores de enzima de diacilglicerol o-aciltransferasa tipo 1. |
SG185285A1 (en) | 2007-06-03 | 2012-11-29 | Univ Vanderbilt | Benzamide mglur5 positive allosteric modulators and methods of making and using same |
TW201116532A (en) * | 2009-08-05 | 2011-05-16 | Merz Pharma Gmbh & Co Kgaa | Metabotropic glutamate receptor modulators |
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2010
- 2010-12-10 US US12/964,785 patent/US8586581B2/en not_active Expired - Fee Related
- 2010-12-14 RU RU2012128551/04A patent/RU2553461C2/ru not_active IP Right Cessation
- 2010-12-14 JP JP2012543676A patent/JP5763094B2/ja not_active Expired - Fee Related
- 2010-12-14 MX MX2012006789A patent/MX2012006789A/es active IP Right Grant
- 2010-12-14 AU AU2010332987A patent/AU2010332987B2/en not_active Ceased
- 2010-12-14 ES ES10790960.8T patent/ES2551582T3/es active Active
- 2010-12-14 TW TW099143811A patent/TWI448465B/zh not_active IP Right Cessation
- 2010-12-14 CN CN201080057081.9A patent/CN102686589B/zh not_active Expired - Fee Related
- 2010-12-14 SG SG2012044814A patent/SG181779A1/en unknown
- 2010-12-14 MY MYPI2012002710A patent/MY162998A/en unknown
- 2010-12-14 UA UAA201207427A patent/UA107002C2/uk unknown
- 2010-12-14 NZ NZ599553A patent/NZ599553A/en not_active IP Right Cessation
- 2010-12-14 CA CA2780155A patent/CA2780155A1/en not_active Abandoned
- 2010-12-14 KR KR1020127018589A patent/KR101407856B1/ko not_active IP Right Cessation
- 2010-12-14 WO PCT/EP2010/069593 patent/WO2011073172A1/en active Application Filing
- 2010-12-14 PE PE2012000817A patent/PE20121443A1/es not_active Application Discontinuation
- 2010-12-14 EP EP10790960.8A patent/EP2513102B1/en not_active Not-in-force
- 2010-12-14 BR BR112012014770A patent/BR112012014770A2/pt not_active Application Discontinuation
- 2010-12-15 AR ARP100104641A patent/AR079467A1/es unknown
-
2012
- 2012-04-23 IL IL219371A patent/IL219371A/en not_active IP Right Cessation
- 2012-04-25 CO CO12068169A patent/CO6531478A2/es active IP Right Grant
- 2012-05-22 CR CR20120269A patent/CR20120269A/es unknown
- 2012-05-24 MA MA34890A patent/MA33802B1/fr unknown
- 2012-06-14 CL CL2012001596A patent/CL2012001596A1/es unknown
- 2012-06-15 ZA ZA2012/04429A patent/ZA201204429B/en unknown
- 2012-06-15 EC ECSP12011977 patent/ECSP12011977A/es unknown
- 2012-11-23 HK HK12112004.5A patent/HK1171225A1/xx not_active IP Right Cessation
-
2013
- 2013-10-16 US US14/055,047 patent/US8933094B2/en not_active Expired - Fee Related
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