AR057728A1 - Piperazinas sustituidas como antagonistas de receptores de glutamato metabotropicos. composiciones farmaceuticas. - Google Patents
Piperazinas sustituidas como antagonistas de receptores de glutamato metabotropicos. composiciones farmaceuticas.Info
- Publication number
- AR057728A1 AR057728A1 ARP060103442A ARP060103442A AR057728A1 AR 057728 A1 AR057728 A1 AR 057728A1 AR P060103442 A ARP060103442 A AR P060103442A AR P060103442 A ARP060103442 A AR P060103442A AR 057728 A1 AR057728 A1 AR 057728A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkylhalo
- alkyl
- group
- independently selected
- co2r2
- Prior art date
Links
- 102000016193 Metabotropic glutamate receptors Human genes 0.000 title 1
- 108010010914 Metabotropic glutamate receptors Proteins 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 4
- 125000001424 substituent group Chemical group 0.000 abstract 3
- -1 C1-6-alkylhalo Chemical group 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 abstract 1
- 125000002373 5 membered heterocyclic group Chemical group 0.000 abstract 1
- 102000001708 Protein Isoforms Human genes 0.000 abstract 1
- 108010029485 Protein Isoforms Proteins 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 230000003287 optical effect Effects 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000003107 substituted aryl group Chemical group 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Cardiology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Psychiatry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Reivindicacion 1: Un compuesto caracterizado porque responde a la formula (1): en donde: Ar1 y Ar2 son grupos arilo o heteroarilo seleccionados en forma independiente opcionalmente sustituidos, en donde los sustituyentes se seleccionan del grupo formado por F, Cl, Br, I, OH, nitro, C1-6-alquilo, C1-6-alquilhalo, OC1-6-alquilo, OC1-6-alquilhalo, C2-6-alquenilo, C2-6-alquinilo, CN, CO2R2, SR2, S(O)R2, SO2R2, arilo, heteroarilo, cicloalquilo y heterocicloalquilo, en donde cualquier sustituyente cíclico puede también estar sustituido con al menos un sustituyente selecccionado del grupo formado por F, Cl, Br, I, OH, nitro, C1-6-alquilo, C1-6-alquilhalo, OH1-6-alquilo, OC1-6-alquilhalo, C2-6-alquenilo, C2-6-alquinilo, CN, CO2R2, SR2, S(O)R2 y SO2R2; R1, en cada caso, se selecciona en forma independiente del grupo formado por F, Cl, Br, I, OH, CN, nitro, C1-6-alquilo, OC1-6-alquilo, C1-6-alquilhalo, OC1-6-alquilhalo, (CO)R2, O(CO)R2, O(CO)OR2, CO2R2, CONR2R3, C1-6- alquilenoOR2, OC2-6-alquilenoOr2 y C1-6-alquilenociano; R2 y R3 se seleccionan en forma independiente del grupo formado por H, C1-6-alquilo, C1-6-alquilhalo, C2-6-alquenilo, C2-6-alquinilo y cicloalquilo; Hy es un anillo heterocíclico de 5 miembros que contiene dos o tres heteroátomos seleccionados en forma independiente del grupo formado por N, O y S, en donde el anillo está opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo formado por F, Cl, Br, I, OH, nitro, C1-6- alquilo, C1-6-alquilhalo, OC1-6-alquilo, OC1-6-alquilhalo, CN, CO2R2, CONR2R3, SR2, S(O)R2 y SO2R2; L se selecciona del grupo formado por -CR4R5-, -C(O)-, -C(NR4)- y -C(S)-; R4 y R5 se seleccionan en forma independiente del grupo formado por H, C1-6- alquilo, -C1-6-alquilhalo, C2-6-alquenilo y C2-6-alquinilo; m es un entero seleccionado del gurpo formado por 0, 1, 2, 3 y 4; y n es un entero seleccionado del grupo formado por 1 y 2; o una sal aceptable para uso faracéutico, hidrato, solvato, isoforma, tautomero, isomero optico, o combinacion de los mismos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US70794605P | 2005-08-15 | 2005-08-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR057728A1 true AR057728A1 (es) | 2007-12-12 |
Family
ID=37451198
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060103442A AR057728A1 (es) | 2005-08-15 | 2006-08-08 | Piperazinas sustituidas como antagonistas de receptores de glutamato metabotropicos. composiciones farmaceuticas. |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US20080312246A1 (es) |
| EP (1) | EP1919901A1 (es) |
| JP (1) | JP2009504734A (es) |
| KR (1) | KR20080057224A (es) |
| CN (1) | CN101287722A (es) |
| AR (1) | AR057728A1 (es) |
| AU (1) | AU2006280231A1 (es) |
| BR (1) | BRPI0615163A2 (es) |
| CA (1) | CA2616307A1 (es) |
| IL (1) | IL188806A0 (es) |
| MX (1) | MX2008001606A (es) |
| NO (1) | NO20080670L (es) |
| TW (1) | TW200800946A (es) |
| UY (1) | UY29735A1 (es) |
| WO (1) | WO2007021573A1 (es) |
| ZA (1) | ZA200801035B (es) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0711521D0 (en) * | 2007-06-14 | 2007-07-25 | Glaxo Group Ltd | Novel compounds |
| JP2011515359A (ja) * | 2008-03-18 | 2011-05-19 | グラクソ グループ リミテッド | 治療用トリアゾールアミド誘導体 |
| JP5508400B2 (ja) * | 2008-06-05 | 2014-05-28 | グラクソ グループ リミテッド | Ｐｉ３キナーゼの阻害剤としてのベンズピラゾール誘導体 |
| ATE552255T1 (de) * | 2008-06-05 | 2012-04-15 | Glaxo Group Ltd | 4-aminoindazole |
| JP5502076B2 (ja) | 2008-06-05 | 2014-05-28 | グラクソ グループ リミテッド | 新規化合物 |
| WO2010102958A1 (en) | 2009-03-09 | 2010-09-16 | Glaxo Group Limited | 4-oxadiazol-2 -yl- indazoles as inhibitors of p13 kinases |
| PL2424864T3 (pl) | 2009-04-30 | 2015-05-29 | Glaxo Group Ltd | Podstawione oksazolami indazole jako inhibitory kinazy pi3 |
| GB2497476B (en) * | 2010-09-06 | 2018-01-10 | Guangzhou Inst Biomed & Health | Amide Compounds |
| GB201018124D0 (en) | 2010-10-27 | 2010-12-08 | Glaxo Group Ltd | Polymorphs and salts |
| US8822464B2 (en) | 2011-11-28 | 2014-09-02 | Boehringer Ingelheim International Gmbh | N-aryl-piperazine derivatives and their use as positive allosteric modulators of mGluR5 receptors |
| US8741892B2 (en) | 2011-12-05 | 2014-06-03 | Boehringer Ingelheim International Gmbh | Compounds |
| US8642774B2 (en) | 2011-12-08 | 2014-02-04 | Boehringer Ingelheim International Gmbh | Compounds |
| US8796467B2 (en) * | 2011-12-13 | 2014-08-05 | Boehringer Ingelheim International Gmbh | Compounds |
| US8846948B2 (en) | 2011-12-13 | 2014-09-30 | Boehringer Ingelheim International Gmbh | Compounds |
| US8716277B2 (en) * | 2011-12-14 | 2014-05-06 | Boehringer Ingelheim International Gmbh | Substituted imidazole compounds useful as positive allosteric modulators of mGlu5 receptor activity |
| US8883789B2 (en) | 2011-12-14 | 2014-11-11 | Boehringer Ingelheim International Gmbh | Piperazine derivatives and their use as positive allosteric modulators of mGluR5 receptors |
| US8937176B2 (en) * | 2011-12-14 | 2015-01-20 | Boehringer Ingelheim International Gmbh | Compounds |
| US8889677B2 (en) | 2012-01-17 | 2014-11-18 | Boehringer Ingellheim International GmbH | Substituted triazoles useful as mGlu5 receptor modulators |
| CN113087669B (zh) * | 2019-12-23 | 2023-11-17 | 南京药石科技股份有限公司 | 一种4-氰基-5-溴嘧啶的制备方法 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA1279645C (en) * | 1986-02-27 | 1991-01-29 | Ineke Van Wijngaarden | Aryl-substituted (n-piperidinyl)methyl- and (n-piperazinyl)methylazoles having antipsychotic properties |
| US5681956A (en) * | 1990-12-28 | 1997-10-28 | Neurogen Corporation | 4-aryl substituted piperazinylmethyl phenylimidazole derivatives; a new class of dopamine receptor subtype specific ligands |
| JP2000504336A (ja) * | 1996-02-02 | 2000-04-11 | ゼネカ・リミテッド | 薬学製剤として有用なヘテロ環式化合物 |
| WO2003093236A1 (en) * | 2002-05-02 | 2003-11-13 | Euro-Celtique, S.A. | 1-(pyrid-2-yl)-piperazine compounds as metabotropic glutamate receptor inhibitor |
| MXPA05001592A (es) * | 2002-08-09 | 2005-05-05 | Astrazeneca Ab | Oxadiazoles como moduladores de receptor-5 de glutamato metabotropico. |
| AU2004218260A1 (en) * | 2003-01-28 | 2004-09-16 | Aventis Pharma S.A. | N-aryl heteroaromatic products, compositions containing same and use thereof |
| AR044586A1 (es) * | 2003-06-04 | 2005-09-21 | Aventis Pharma Sa | Productos aril - heteroaromaticos, composiciones que los contienen y su utilizacion |
| GB0325956D0 (en) * | 2003-11-06 | 2003-12-10 | Addex Pharmaceuticals Sa | Novel compounds |
| WO2005077373A2 (en) * | 2004-02-03 | 2005-08-25 | Astrazeneca Ab | Treatment of gastro-esophageal reflux disease (gerd) |
-
2006
- 2006-08-03 TW TW095128483A patent/TW200800946A/zh unknown
- 2006-08-04 KR KR1020087003230A patent/KR20080057224A/ko not_active Application Discontinuation
- 2006-08-04 EP EP06789371A patent/EP1919901A1/en not_active Withdrawn
- 2006-08-04 JP JP2008526973A patent/JP2009504734A/ja active Pending
- 2006-08-04 BR BRPI0615163A patent/BRPI0615163A2/pt not_active IP Right Cessation
- 2006-08-04 CA CA002616307A patent/CA2616307A1/en not_active Abandoned
- 2006-08-04 CN CNA2006800289759A patent/CN101287722A/zh active Pending
- 2006-08-04 US US11/997,444 patent/US20080312246A1/en not_active Abandoned
- 2006-08-04 AU AU2006280231A patent/AU2006280231A1/en not_active Abandoned
- 2006-08-04 WO PCT/US2006/030392 patent/WO2007021573A1/en active Application Filing
- 2006-08-04 MX MX2008001606A patent/MX2008001606A/es not_active Application Discontinuation
- 2006-08-04 US US11/498,835 patent/US20070037820A1/en not_active Abandoned
- 2006-08-08 AR ARP060103442A patent/AR057728A1/es unknown
- 2006-08-08 UY UY29735A patent/UY29735A1/es not_active Application Discontinuation
-
2008
- 2008-01-16 IL IL188806A patent/IL188806A0/en unknown
- 2008-01-31 ZA ZA200801035A patent/ZA200801035B/xx unknown
- 2008-02-05 NO NO20080670A patent/NO20080670L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| WO2007021573A1 (en) | 2007-02-22 |
| ZA200801035B (en) | 2008-12-31 |
| JP2009504734A (ja) | 2009-02-05 |
| EP1919901A1 (en) | 2008-05-14 |
| KR20080057224A (ko) | 2008-06-24 |
| CN101287722A (zh) | 2008-10-15 |
| MX2008001606A (es) | 2008-04-14 |
| TW200800946A (en) | 2008-01-01 |
| UY29735A1 (es) | 2007-02-28 |
| NO20080670L (no) | 2008-04-01 |
| IL188806A0 (en) | 2008-08-07 |
| CA2616307A1 (en) | 2007-02-22 |
| BRPI0615163A2 (pt) | 2016-09-13 |
| AU2006280231A1 (en) | 2007-02-22 |
| US20080312246A1 (en) | 2008-12-18 |
| US20070037820A1 (en) | 2007-02-15 |
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