PE20090477A1 - OXAZOLE DERIVATIVES AS INHIBITORS OF SODIUM CHANNELS - Google Patents
OXAZOLE DERIVATIVES AS INHIBITORS OF SODIUM CHANNELSInfo
- Publication number
- PE20090477A1 PE20090477A1 PE2008001166A PE2008001166A PE20090477A1 PE 20090477 A1 PE20090477 A1 PE 20090477A1 PE 2008001166 A PE2008001166 A PE 2008001166A PE 2008001166 A PE2008001166 A PE 2008001166A PE 20090477 A1 PE20090477 A1 PE 20090477A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- halo
- inhibitors
- methyl
- dichlorophenyl
- Prior art date
Links
- 108010052164 Sodium Channels Proteins 0.000 title abstract 2
- 102000018674 Sodium Channels Human genes 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 150000007978 oxazole derivatives Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- -1 2,6-DICHLOROPHENYL Chemical class 0.000 abstract 2
- AKTWUEODUATOIU-UHFFFAOYSA-N (2,5-dichlorophenyl)methyl carbamate Chemical compound NC(=O)OCC1=CC(Cl)=CC=C1Cl AKTWUEODUATOIU-UHFFFAOYSA-N 0.000 abstract 1
- ZIWFMLAKPXPSNC-UHFFFAOYSA-N (2-chlorophenyl)methyl carbamate Chemical compound NC(=O)OCC1=CC=CC=C1Cl ZIWFMLAKPXPSNC-UHFFFAOYSA-N 0.000 abstract 1
- HKTNNHYXHMXXCR-UHFFFAOYSA-N C(N)(OC1=C(C=CC=C1F)Cl)=O Chemical compound C(N)(OC1=C(C=CC=C1F)Cl)=O HKTNNHYXHMXXCR-UHFFFAOYSA-N 0.000 abstract 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical class O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 1
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- 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
- C07D261/10—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D261/14—Nitrogen atoms
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Neurology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
SE REFIERE A COMPUESTOS DERIVADOS DE OXAZOL DE FORMULA (I) DONDE R1 ES H, HALO, CN, ALQUILO(C1-C4), ENTRE OTROS; R2 Y R3 SON CADA UNO HALO, ALQUILO(C1-C4), ALQUENILO(C2-C4), CN, ENTRE OTROS; R4 ES H O ALQUILO(C1-C4) OPCIONALMENTE SUSTITUIDO CON ALCOXI(C1-C3), HALO O CN; R5 ES HALOGENO, ALQUILO(C1-C4), CICLOALQUILO(C3-C6), CN, ENTRE OTROS; m ES DE 0 A 3; A ES NH U O; L ES ALQUILENO(C1-C4) OPCIONALMENTE SUSTITUIDO CON R6, EN DONDE R6 ES ALQUILO(C1-C4), ALQUENILO(C2-C4), FLUOROALQUILO(C1-C6), ENTRE OTROS; M ES ARILO(C6-C10) O HETEROARILO(C5-C10) OPCIONALMENTE SUSTITUIDO CON R7, EN DONDE R7 ES OH, HALO, CN, NITRO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-[3-(2,6-DICLOROFENIL)-5-ETIL-1,2-OXAZOL-4-IL]CARBAMATO DE (2-CLORO-6-FLUORO-FENIL)METILO, N-[3-(2,6-DICLOROFENIL)-5-METIL-1,2-OXAZOL-4-IL]CARBAMATO DE (2-CLOROFENIL)METILO, N-[3-(2,6-DICLOROFENIL)-5-METIL-1,2-OXAZOL-4-IL]CARBAMATO DE (2,5-DICLOROFENIL)METILO, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LOS CANALES DE SODIO SIENDO UTILES EN EL TRATAMIENTO DEL DOLORREFERS TO COMPOUNDS DERIVED FROM OXAZOLE OF FORMULA (I) WHERE R1 IS H, HALO, CN, ALKYL (C1-C4), AMONG OTHERS; R2 AND R3 ARE EACH HALO, ALKYL (C1-C4), ALKENYL (C2-C4), CN, AMONG OTHERS; R4 IS H OR ALKYL (C1-C4) OPTIONALLY SUBSTITUTED WITH ALCOXY (C1-C3), HALO OR CN; R5 IS HALOGEN, ALKYL (C1-C4), CYCLOALKYL (C3-C6), CN, AMONG OTHERS; m IS 0 TO 3; A IS NH U O; L IS ALKYLENE (C1-C4) OPTIONALLY SUBSTITUTE WITH R6, WHERE R6 IS ALKYL (C1-C4), ALKYLENE (C2-C4), FLUOROALKYL (C1-C6), AMONG OTHERS; M IS ARYL (C6-C10) OR HETEROARILO (C5-C10) OPTIONALLY SUBSTITUTED WITH R7, WHERE R7 IS OH, HALO, CN, NITRO, AMONG OTHERS. PREFERRED COMPOUNDS ARE: N- [3- (2,6-DICHLOROPHENYL) -5-ETHYL-1,2-OXAZOL-4-IL] (2-CHLORO-6-FLUORO-PHENYL) CARBAMATE, N- [3 - (2,6-DICHLOROPHENIL) -5-METHYL-1,2-OXAZOL-4-IL] (2-CHLOROPHENYL) METHYL CARBAMATE, N- [3- (2,6-DICHLOROPHENYL) -5-METHYL-1 , 2-OXAZOLE-4-IL] (2,5-DICHLOROPHENYL) METHYL CARBAMATE, AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION. SUCH COMPOUNDS ARE INHIBITORS OF SODIUM CHANNELS, BEING USEFUL IN THE TREATMENT OF PAIN
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94966507P | 2007-07-13 | 2007-07-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20090477A1 true PE20090477A1 (en) | 2009-05-24 |
Family
ID=39709355
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2008001166A PE20090477A1 (en) | 2007-07-13 | 2008-07-11 | OXAZOLE DERIVATIVES AS INHIBITORS OF SODIUM CHANNELS |
Country Status (6)
| Country | Link |
|---|---|
| AR (1) | AR067513A1 (en) |
| CL (1) | CL2008002038A1 (en) |
| PE (1) | PE20090477A1 (en) |
| TW (1) | TW200911766A (en) |
| UY (1) | UY31219A1 (en) |
| WO (1) | WO2009010784A1 (en) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG188438A1 (en) | 2010-09-13 | 2013-05-31 | Novartis Ag | Triazine-oxadiazoles |
| KR20140105445A (en) | 2011-10-31 | 2014-09-01 | 제논 파마슈티칼스 인크. | Biaryl ether sulfonamides and their use as therapeutic agents |
| BR112014010271A2 (en) | 2011-10-31 | 2017-04-18 | Xenon Pharmaceuticals Inc | benzenesulfonamide compounds and their use as therapeutic agents |
| TW201400446A (en) | 2012-05-22 | 2014-01-01 | Genentech Inc | N-substituted benzamides and methods of use thereof |
| CA2878478A1 (en) | 2012-07-06 | 2014-01-09 | Genentech, Inc. | N-substituted benzamides and methods of use thereof |
| CN105263490B (en) | 2013-03-14 | 2018-05-22 | 基因泰克公司 | Substituted triazolopyridines and methods of use thereof |
| JP6227112B2 (en) | 2013-03-15 | 2017-11-08 | ジェネンテック， インコーポレイテッド | Substituted benzoxazole and methods of use |
| WO2015078374A1 (en) | 2013-11-27 | 2015-06-04 | Genentech, Inc. | Substituted benzamides and methods of use thereof |
| WO2015102929A1 (en) | 2013-12-30 | 2015-07-09 | Novartis Ag | Tricyclic sulfonamide derivatives |
| EP3166939B1 (en) | 2014-07-07 | 2019-06-05 | Genentech, Inc. | Therapeutic compounds and methods of use thereof |
| MA42118A (en) | 2015-05-22 | 2018-03-28 | Genentech Inc | BENZAMIDES SUBSTITUTED AND THEIR METHODS OF USE |
| EP3341353A1 (en) | 2015-08-27 | 2018-07-04 | Genentech, Inc. | Therapeutic compounds and methods of use thereof |
| KR20180067561A (en) | 2015-09-28 | 2018-06-20 | 제넨테크, 인크. | Therapeutic compounds and methods for their use |
| US10899732B2 (en) | 2015-11-25 | 2021-01-26 | Genentech, Inc. | Substituted benzamides useful as sodium channel blockers |
| WO2017172802A1 (en) | 2016-03-30 | 2017-10-05 | Genentech, Inc. | Substituted benzamides and methods of use thereof |
| CR20190236A (en) | 2016-10-17 | 2019-09-09 | Genentech Inc | Therapeutic compounds and methods of use thereof |
| EP3601273B1 (en) | 2017-03-24 | 2021-12-01 | Genentech, Inc. | 4-piperidin-n-(pyrimidin-4-yl)chroman-7-sulfonamide derivatives as sodium channel inhibitors |
| WO2019165290A1 (en) | 2018-02-26 | 2019-08-29 | Genentech, Inc. | Pyridine-sulfonamide compounds and their use against pain and related conditions |
| US10947251B2 (en) | 2018-03-30 | 2021-03-16 | Genentech, Inc. | Therapeutic compounds and methods of use thereof |
| TW202003490A (en) | 2018-05-22 | 2020-01-16 | 瑞士商赫孚孟拉羅股份公司 | Therapeutic compounds and methods of use thereof |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007075896A2 (en) * | 2005-12-22 | 2007-07-05 | Kemia, Inc. | Heterocyclic cytokine inhibitors |
-
2008
- 2008-07-09 WO PCT/GB2008/050554 patent/WO2009010784A1/en not_active Ceased
- 2008-07-09 TW TW097125959A patent/TW200911766A/en unknown
- 2008-07-11 CL CL2008002038A patent/CL2008002038A1/en unknown
- 2008-07-11 PE PE2008001166A patent/PE20090477A1/en not_active Application Discontinuation
- 2008-07-11 AR ARP080102987A patent/AR067513A1/en unknown
- 2008-07-11 UY UY31219A patent/UY31219A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2009010784A1 (en) | 2009-01-22 |
| TW200911766A (en) | 2009-03-16 |
| AR067513A1 (en) | 2009-10-14 |
| UY31219A1 (en) | 2009-03-02 |
| CL2008002038A1 (en) | 2009-07-17 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD | Application declared void or lapsed |