AR060811A1 - Moduladores de mglur5 v - Google Patents
Moduladores de mglur5 vInfo
- Publication number
- AR060811A1 AR060811A1 ARP070101784A ARP070101784A AR060811A1 AR 060811 A1 AR060811 A1 AR 060811A1 AR P070101784 A ARP070101784 A AR P070101784A AR P070101784 A ARP070101784 A AR P070101784A AR 060811 A1 AR060811 A1 AR 060811A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydrogen
- tetrazol
- cyano
- chloro
- Prior art date
Links
- 101150087728 Grm5 gene Proteins 0.000 title 1
- 102100038357 Metabotropic glutamate receptor 5 Human genes 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 5
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 150000002431 hydrogen Chemical group 0.000 abstract 4
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 abstract 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000001153 fluoro group Chemical group F* 0.000 abstract 2
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- HFKZFNWIEYBGPG-UHFFFAOYSA-N 8-[1-[2-(3-chlorophenyl)tetrazol-5-yl]ethyl]-3-pyridin-3-yl-6,7-dihydro-5h-[1,2,4]triazolo[4,3-a]pyrimidine Chemical compound N1=NN(C=2C=C(Cl)C=CC=2)N=C1C(C)N1CCCN2C1=NN=C2C1=CC=CN=C1 HFKZFNWIEYBGPG-UHFFFAOYSA-N 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
- PRYRJSFZCLYJLA-UHFFFAOYSA-N 9-[[2-(3-chlorophenyl)tetrazol-5-yl]methyl]-3-pyridin-3-yl-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a][1,3]diazepine Chemical compound ClC1=CC=CC(N2N=C(CN3C=4N(C(=NN=4)C=4C=NC=CC=4)CCCC3)N=N2)=C1 PRYRJSFZCLYJLA-UHFFFAOYSA-N 0.000 abstract 1
- 102000001708 Protein Isoforms Human genes 0.000 abstract 1
- 108010029485 Protein Isoforms Proteins 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- JFDZBHWFFUWGJE-UHFFFAOYSA-N benzonitrile Substances N#CC1=CC=CC=C1 JFDZBHWFFUWGJE-UHFFFAOYSA-N 0.000 abstract 1
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 1
- 125000004966 cyanoalkyl group Chemical group 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 150000002391 heterocyclic compounds Chemical class 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 230000001537 neural effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P25/06—Antimigraine agents
-
- 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
- A61P25/22—Anxiolytics
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Compuestos heterocíclicos, un proceso para su preparacion, su utilizacion para preparar medicamentos y composiciones farmacéuticas que los comprenden. Accion neuronal (sobre el SNC), psiquiátrica y tratamiento del dolor. Reivindicacion 1: Un compuesto de formula (1) en donde R1 es metilo, halogeno o ciano; R2 es hidrogeno o fluoro; R3 es hidrogeno, fluoro o C1-3 alquilo, R4 es hidrogeno o C1-3 alquilo; Y es C1-2 alquileno; X es (2) y Z es (3); R5 es hidrogeno, C1-3 alquilo, C1-3 haloalquilo, C1-3 alcoxi, C1-3 haloalcoxi, C1-3 amido alquilo, C1-3 N'alquilamido alquilo, pirazoilo, C1-3 N'N-dialquilamido alquilo, ciano o C1-3 cianoalquilo; R6 es hidrogeno, C1-3 alquilo, C1-3 haloalquilo, C1-3alcoxi, C1-3 haloalcoxi, C1-3 amido alquilo, C1-3 N'alquilamido alquilo, C1-3 N'N-dialquilamido alquilo, ciano o c1-3cianoalquilo; R7 es hidrogeno, cluoro o c1-3 alquilo; así como sus sales aceptables para uso farmacéutico, hidratos, isoformas, tautomeros y/o enantiomeros, con la condicion de que el compuesto de formula 1 no es 3-{5-[3-(2, 6-dimetoxi-pirimidin-4-il)-6,7-dihidro-5H-[1,2,4]triazolo[4,3-a]pirimidin-8-ilmetil]-tetrazol-2-il}-benzonitrilo; 8-[2-(3-Cloro-fenil)-2H-tetrazol-5-ilmetil]-3-piridin-3-il-5,6,7,8- tetrahidro-4H-1,2,3a,8-tetraaza-azuleno; o 8-{1-[2-(3-Cloro-fenil)-2H-tetrazol-5-il]-etil}-3-piridin-3-il-5,6,7,8-tetrahidro-[1,2,4]triazolo[4,3-a]pirimidina.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US79766306P | 2006-05-05 | 2006-05-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR060811A1 true AR060811A1 (es) | 2008-07-16 |
Family
ID=38668441
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP070101784A AR060811A1 (es) | 2006-05-05 | 2007-04-25 | Moduladores de mglur5 v |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US20070259860A1 (es) |
| EP (1) | EP2027129A2 (es) |
| JP (1) | JP2009536213A (es) |
| KR (1) | KR20090018935A (es) |
| CN (1) | CN101484455A (es) |
| AR (1) | AR060811A1 (es) |
| AU (1) | AU2007248292A1 (es) |
| BR (1) | BRPI0710980A2 (es) |
| CA (1) | CA2650255A1 (es) |
| CL (1) | CL2007001178A1 (es) |
| EC (1) | ECSP088884A (es) |
| IL (1) | IL194815A0 (es) |
| MX (1) | MX2008013834A (es) |
| NO (1) | NO20084852L (es) |
| RU (1) | RU2008141511A (es) |
| TW (1) | TW200808800A (es) |
| UY (1) | UY30308A1 (es) |
| WO (1) | WO2007130824A2 (es) |
| ZA (1) | ZA200809019B (es) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200821305A (en) | 2006-10-05 | 2008-05-16 | Astrazeneca Ab | MGluR5 modulators |
| JP2011500798A (ja) * | 2007-10-26 | 2011-01-06 | アストラゼネカ・アクチエボラーグ | ｍＧｌｕＲ５のモジュレーターとしてのアミノ１，２，４−トリアゾール誘導体 |
| WO2009054791A1 (en) * | 2007-10-26 | 2009-04-30 | Astrazeneca Ab | Fused pyrrolidine 1,2,4-triazole derivatives as modulators of mglur5 |
| WO2009054787A1 (en) * | 2007-10-26 | 2009-04-30 | Astrazeneca Ab | 1,2,4-triazole carboxylic acid derivatives as modulators of mglur5 |
| WO2009054786A1 (en) * | 2007-10-26 | 2009-04-30 | Astrazeneca Ab | 1,2,4-triazole aryl n-oxides derivatives as modulators of mglur5 |
| TW200922586A (en) * | 2007-10-26 | 2009-06-01 | Astrazeneca Ab | Thiophene 1,2,4-triazole derivatives as modulators of mGluR5 |
| WO2009054785A1 (en) * | 2007-10-26 | 2009-04-30 | Astrazeneca Ab | 1,2,4-triazole ether derivatives as modulators of mglur5 |
| WO2009054790A1 (en) * | 2007-10-26 | 2009-04-30 | Astrazeneca Ab | Amide linked heteroaromatic derivatives as modulators of mglur5 |
| CN102256950A (zh) * | 2008-12-18 | 2011-11-23 | 阿斯利康(瑞典)有限公司 | 制备1-[5-(3-氯-苯基)-异噁唑-3-基]-乙酮和(r)-1-[5-(3-氯-苯基)-异噁唑-3-基]-乙醇的新方法 |
| JP5620129B2 (ja) * | 2009-03-19 | 2014-11-05 | 富士フイルム株式会社 | 光学フィルム、位相差板、楕円偏光板、液晶表示装置、及び化合物 |
| CA2767764A1 (en) | 2009-07-13 | 2011-01-20 | Takeda Pharmaceutical Company Limited | Heterocyclic compound and use thereof |
| ES2443578T3 (es) | 2009-12-29 | 2014-02-19 | Eli Lilly And Company | Compuestos de tetrahidrotriazolopiridina como potenciadores de receptores selectivos de mGlu5 útiles para el tratamiento de la esquizofrenia |
| MX2013002511A (es) | 2010-09-02 | 2013-07-29 | Takeda Pharmaceutical | Triazoles fusionados para el tratamiento o profilaxis de daño cognitivo moderado. |
| ES2608395T3 (es) | 2013-01-23 | 2017-04-10 | Astrazeneca Ab | Compuestos químicos |
| EP2857387A1 (en) | 2013-10-07 | 2015-04-08 | Boehringer Ingelheim International Gmbh | Process for manufacturing 1,6-dihydro-6-oxo-4-pyridazine carboxylic acid |
| TWI891782B (zh) | 2020-05-06 | 2025-08-01 | 德商拜耳廠股份有限公司 | 作為殺蟲劑之新穎雜芳基三唑化合物 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU3896900A (en) * | 1999-03-19 | 2000-10-09 | Knoll Pharmaceutical Company | Treatment of pain |
| US20040132726A1 (en) * | 2002-08-09 | 2004-07-08 | Astrazeneca Ab And Nps Pharmaceuticals, Inc. | New compounds |
| MXPA05001590A (es) * | 2002-08-09 | 2005-05-23 | Astrazeneca Ab | Compuestos que tienen actividad en los receptores metabotropicos de glutamato. |
| BRPI0507498A (pt) * | 2004-02-18 | 2007-07-10 | Astrazeneca Ab | composto, composição farmacêutica, uso do composto, e, métodos para tratar distúrbios mediados por mglur 5 e para inibir ativação de receptores de mglur 5 |
| KR20070026380A (ko) * | 2004-02-18 | 2007-03-08 | 아스트라제네카 아베 | 융합된 헤테로시클릭 화합물 및 대사성 글루타메이트수용체 길항제로서 이들의 용도 |
| US7585881B2 (en) * | 2004-02-18 | 2009-09-08 | Astrazeneca Ab | Additional heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists |
-
2007
- 2007-04-24 TW TW096114393A patent/TW200808800A/zh unknown
- 2007-04-25 WO PCT/US2007/067371 patent/WO2007130824A2/en not_active Ceased
- 2007-04-25 EP EP07811855A patent/EP2027129A2/en not_active Withdrawn
- 2007-04-25 MX MX2008013834A patent/MX2008013834A/es not_active Application Discontinuation
- 2007-04-25 UY UY30308A patent/UY30308A1/es not_active Application Discontinuation
- 2007-04-25 CN CNA2007800254542A patent/CN101484455A/zh active Pending
- 2007-04-25 JP JP2009509957A patent/JP2009536213A/ja active Pending
- 2007-04-25 US US11/790,429 patent/US20070259860A1/en not_active Abandoned
- 2007-04-25 BR BRPI0710980-6A patent/BRPI0710980A2/pt not_active IP Right Cessation
- 2007-04-25 RU RU2008141511/04A patent/RU2008141511A/ru not_active Application Discontinuation
- 2007-04-25 KR KR1020087029721A patent/KR20090018935A/ko not_active Withdrawn
- 2007-04-25 AU AU2007248292A patent/AU2007248292A1/en not_active Abandoned
- 2007-04-25 CA CA002650255A patent/CA2650255A1/en not_active Abandoned
- 2007-04-25 AR ARP070101784A patent/AR060811A1/es unknown
- 2007-04-25 CL CL2007001178A patent/CL2007001178A1/es unknown
-
2008
- 2008-10-21 ZA ZA200809019A patent/ZA200809019B/xx unknown
- 2008-10-22 IL IL194815A patent/IL194815A0/en unknown
- 2008-11-12 EC EC2008008884A patent/ECSP088884A/es unknown
- 2008-11-18 NO NO20084852A patent/NO20084852L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| US20070259860A1 (en) | 2007-11-08 |
| WO2007130824A3 (en) | 2008-05-22 |
| WO2007130824A2 (en) | 2007-11-15 |
| AU2007248292A8 (en) | 2008-12-04 |
| ZA200809019B (en) | 2009-08-26 |
| IL194815A0 (en) | 2009-08-03 |
| NO20084852L (no) | 2009-01-14 |
| CL2007001178A1 (es) | 2008-01-18 |
| MX2008013834A (es) | 2008-11-10 |
| CA2650255A1 (en) | 2007-11-15 |
| AU2007248292A1 (en) | 2007-11-15 |
| BRPI0710980A2 (pt) | 2011-05-31 |
| TW200808800A (en) | 2008-02-16 |
| KR20090018935A (ko) | 2009-02-24 |
| JP2009536213A (ja) | 2009-10-08 |
| UY30308A1 (es) | 2007-11-30 |
| EP2027129A2 (en) | 2009-02-25 |
| CN101484455A (zh) | 2009-07-15 |
| RU2008141511A (ru) | 2010-06-20 |
| ECSP088884A (es) | 2008-12-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |