AR067513A1 - 1,2-OXAZOL DERIVATIVES - Google Patents

1,2-OXAZOL DERIVATIVES

Info

Publication number
AR067513A1
AR067513A1 ARP080102987A ARP080102987A AR067513A1 AR 067513 A1 AR067513 A1 AR 067513A1 AR P080102987 A ARP080102987 A AR P080102987A AR P080102987 A ARP080102987 A AR P080102987A AR 067513 A1 AR067513 A1 AR 067513A1
Authority
AR
Argentina
Prior art keywords
methyl
alkyl
dichlorophenyl
oxazol
alkoxy
Prior art date
Application number
ARP080102987A
Other languages
Spanish (es)
Original Assignee
Astrazeneca Ab
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR067513A1 publication Critical patent/AR067513A1/en

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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)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (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

Reivindicacion 1: Un compuesto de la formula 1, en la cual R1 es hidrogeno, halo, ciano, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, alcoxi C1-3, cicloalquilo C3-6, fluoralquilo C1-4, fluoralcoxi C1-6, hidroxialquilo C1-6, alcoxi C1-3-alquilo C1-4, o cianoalquilo C1-6; cada uno de R2 y R3 es independientemente seleccionado entre halo, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, cicloalquilo C3-7, fluoralquilo C1-4, alcoxi C1-3, fluoralcoxi C1-4 y ciano; R4 es hidrogeno o alquilo C1-4 que puede estar optativamente sustituido con alcoxi C1-3, halo o ciano; R5 es halogeno, alquilo C1-4, alquenilo C2-4, alquinilo C2-4 cicloalquilo C3-6, heterocicloalquilo C3-10, fluoralquilo C1-6, fluoralcoxi C1-6, CN, alcoxi C1-3-alquilo C1-3, hidroxialquilo C1-6 o cianoalquilo C1-6; m es 0 a 3; A es NH u O; L es alquileno C1-4, donde cada hidrogeno del alquileno puede estar optativamente sustituido con R6; R6 es alquilo C1-4, alquenilo C2-4, alquinilo C2-4, cicloalquilo C3-6, heterocicloalquilo C3-10, fluoralquilo C1-6, fluoralcoxi C1-6, ciano, alcoxi C1-3-alquilo C1-3, hidroxialquilo C1-6 o cianoalquilo C1-6; M es arilo C6-10 o heteroarilo C5-10, cada uno de los cuales está optativamente sustituido con uno o más sustituyentes R7; R7 es hidroxi, halo, ciano, nitro, alquilo C1-6, alquinilo C2-6, alcoxi C1-6, alcoxialquilo C1-6, trifluormetoxi, difluormetoxi, fluoralquilo C1-6 mono- o polisustituido, fluoralcoxi C1-6, mono- o polisustituido, carbamoilo, sulfamoilo, cianoalquilo C1-6, fenilo, cicloalquilo C3-6, cicloalquiloxi C3-6-heterocicloalquilo C5-6, heterocicloalquiloxi C5-6, heteroarilo C5-6, alcoxicarbonilo C1-6, alcanoílo C1-6, alcanoiloxi C1-4, N-(alquil C1-6)ncarbamoílo donde n es 0 a 2, alquil C1-6S(O)a donde a es 0 a 2, fluoralquil C1-6SO2O mono- o polisustituido, NR9R10, N-alquilC1-6sulfamoílo o N,N-(alquil C1-6)2sulfamoílo; y cada uno de R9 y R10 es independientemente seleccionado entre hidrogeno y alquilo C1-4; como así también una sal aceptable para uso farmacéutico o isomero del mismo o una sal de dicho isomero; a excepcion de los compuestos: 3-[[2,6-bis(dimetilamino)fenil]metil]-1-[3-(2,6-diclorofenil)-5-metil-1,2-oxazol-4-il]urea; 1-[(2,6-diclorofenil)metil]-3-[3-(2,6-diclorofenil)-5-metil-1,2-oxazol-4-il]urea; 1-[3-(2,6-diclorofenil)-5-metil-1,2-oxazol-4-il]-3-[3,3,3-trifluor-2-(1H-pirrol-2-il)propil]urea; 1-[3-(2,6-diclorofenil)-5-metil-1,2-oxazol-4-il]-3-(3-imidazol-1-ilpropil)urea; [3-(2,5-dimetilpirrol-1-iI)tiofen-2-il]metil, N-[3-(2,6-diclorofenil)-5-metil-1,2-oxazol-4-il]carbamato; [3-(2,5-dimetilpirrol-1-il)tiofen-2-il]metil N-[3-(2-cloro-6-fluor--fenil)-5-metil-1,2-oxazol-4-il]carbamato; (2,3,4,5,6-pentametilfenil)metil N-[3-(2,6-diclorofenil)-5-metil-1,2-oxazol-4-il]carbamato; (2-cloro-6-fluor-fenil)metil N-[3-(2,6-diclorofenil)-5-metil-1,2-oxazol-4-il]carbamato: (3,5-diclorofenil)metil N-[3-(2,6-diclorofenil)-5-metil-1,2-0xazol-4-iI]carbamato; y (2,6-dicloropiridin-4-il)metil N-[3-(2,6-diclorofenil)-5-metil-1,2-oxazol-4-il]carbamato.Claim 1: A compound of the formula 1, wherein R 1 is hydrogen, halo, cyano, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, C 1-3 alkoxy, C 3-6 cycloalkyl, C 1-4 fluoralkyl , C1-6 fluoralkoxy, C1-6 hydroxyalkyl, C1-3 alkoxy-C1-4 alkyl, or C1-6 cyanoalkyl; each of R2 and R3 is independently selected from halo, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C3-7 cycloalkyl, C1-4 fluoralkyl, C1-3 alkoxy, C1-4 fluoralkoxy and cyano; R4 is hydrogen or C1-4 alkyl which may be optionally substituted with C1-3 alkoxy, halo or cyano; R 5 is halogen, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl C 3-6 cycloalkyl, C 3-10 heterocycloalkyl, C 1-6 fluororalkyl, C 1-6 fluororalkoxy, CN, C 1-3 alkoxy-C 1-3 alkyl, C1-6 hydroxyalkyl or C1-6 cyanoalkyl; m is 0 to 3; A is NH or O; L is C1-4 alkylene, where each alkylene hydrogen may be optionally substituted with R6; R 6 is C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, C 3-6 cycloalkyl, C 3-10 heterocycloalkyl, C 1-6 fluororalkyl, C 1-6 fluororalkoxy, cyano, C 1-3 alkoxy-C 1-3 alkyl, hydroxyalkyl C1-6 or C1-6 cyanoalkyl; M is C6-10 aryl or C5-10 heteroaryl, each of which is optionally substituted with one or more R7 substituents; R 7 is hydroxy, halo, cyano, nitro, C 1-6 alkyl, C 2-6 alkynyl, C 1-6 alkoxy, C 1-6 alkoxy, trifluoromethoxy, difluoromethoxy, C 1-6 fluoralkyl mono- or polysubstituted, C 1-6 fluoralkoxy, mono- or polysubstituted, carbamoyl, sulfamoyl, C 1-6 cyanoalkyl, phenyl, C 3-6 cycloalkyl, C 3-6 cycloalkyloxy, C 5-6 heterocycloalkyl, C 5-6 heterocycloalkyloxy, C 1-6 alkoxycarbonyl, C 1-6 alkanoyl, alkanoxy C1-4, N- (C1-6 alkyl) ncarbamoyl where n is 0 to 2, C1-6S alkyl (O) to where a is 0 to 2, mono- or polysubstituted C1-6SO2O fluoralkyl, NR9R10, N-alkylC1- 6sulfamoyl or N, N- (C1-6 alkyl) 2sulfamoyl; and each of R9 and R10 is independently selected from hydrogen and C1-4 alkyl; as well as a salt acceptable for pharmaceutical or isomeric use thereof or a salt of said isomer; with the exception of the compounds: 3 - [[2,6-bis (dimethylamino) phenyl] methyl] -1- [3- (2,6-dichlorophenyl) -5-methyl-1,2-oxazol-4-yl] urea; 1 - [(2,6-dichlorophenyl) methyl] -3- [3- (2,6-dichlorophenyl) -5-methyl-1,2-oxazol-4-yl] urea; 1- [3- (2,6-Dichlorophenyl) -5-methyl-1,2-oxazol-4-yl] -3- [3,3,3-trifluor-2- (1H-pyrrole-2-yl) propyl] urea; 1- [3- (2,6-Dichlorophenyl) -5-methyl-1,2-oxazol-4-yl] -3- (3-imidazol-1-ylpropyl) urea; [3- (2,5-dimethylpyrrol-1-iI) thiophene-2-yl] methyl, N- [3- (2,6-dichlorophenyl) -5-methyl-1,2-oxazol-4-yl] carbamate ; [3- (2,5-dimethylpyrrol-1-yl) thiophen-2-yl] methyl N- [3- (2-chloro-6-fluorophenyl) -5-methyl-1,2-oxazol-4 -yl] carbamate; (2,3,4,5,6-pentamethylphenyl) methyl N- [3- (2,6-dichlorophenyl) -5-methyl-1,2-oxazol-4-yl] carbamate; (2-Chloro-6-fluorophenyl) methyl N- [3- (2,6-dichlorophenyl) -5-methyl-1,2-oxazol-4-yl] carbamate: (3,5-dichlorophenyl) methyl N - [3- (2,6-Dichlorophenyl) -5-methyl-1,2-0xazol-4-i]] carbamate; and (2,6-dichloropyridin-4-yl) methyl N- [3- (2,6-dichlorophenyl) -5-methyl-1,2-oxazol-4-yl] carbamate.

ARP080102987A 2007-07-13 2008-07-11 1,2-OXAZOL DERIVATIVES AR067513A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US94966507P 2007-07-13 2007-07-13

Publications (1)

Publication Number Publication Date
AR067513A1 true AR067513A1 (en) 2009-10-14

Family

ID=39709355

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP080102987A AR067513A1 (en) 2007-07-13 2008-07-11 1,2-OXAZOL DERIVATIVES

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 (19)

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PT2616465E (en) * 2010-09-13 2016-03-09 Novartis Ag Triazine-oxadiazoles
BR112014010368A2 (en) 2011-10-31 2017-04-25 Xenon Pharmaceuticals Inc biaryl ether sulfonamides and their use as therapeutic agents
RU2014121984A (en) 2011-10-31 2015-12-10 Ксенон Фармасьютикалз Инк. BENZENESULPHONAMIDE COMPOUNDS AND THEIR APPLICATION AS A THERAPEUTIC MEDICINES
MX2014014234A (en) 2012-05-22 2015-05-07 Genentech Inc N-substituted benzamides and their use in the treatment of pain.
KR101663436B1 (en) 2012-07-06 2016-10-06 제넨테크, 인크. N-substituted benzamides and methods of use thereof
RU2015143906A (en) 2013-03-14 2017-04-18 Дженентек, Инк. SUBSTITUTED TRIAZOLOPYRIDINES AND WAYS OF THEIR APPLICATION
MX2015010775A (en) 2013-03-15 2016-04-25 Genentech Inc Substituted benzoxazoles and methods of use thereof.
CA2931732A1 (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
CN106715418A (en) 2014-07-07 2017-05-24 基因泰克公司 Therapeutic compounds and methods of use thereof
BR112017024853A2 (en) 2015-05-22 2018-08-07 Genentech Inc compound, pharmaceutical composition, method for treating a disease or condition in a mammal, for treating itching in a mammal, for treating or prophylaxis and use of a compound
EP3341353A1 (en) 2015-08-27 2018-07-04 Genentech, Inc. Therapeutic compounds and methods of use thereof
JP6987746B2 (en) 2015-09-28 2022-01-05 ジェネンテック， インコーポレイテッド Therapeutic compounds and their usage
EP3380466A1 (en) 2015-11-25 2018-10-03 Genentech, Inc. Substituted benzamides useful as sodium channel blockers
EP3854782A1 (en) 2016-03-30 2021-07-28 Genentech, Inc. Substituted benzamides and methods of use thereof
CA3039853A1 (en) 2016-10-17 2018-04-26 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
AR114263A1 (en) 2018-02-26 2020-08-12 Genentech Inc THERAPEUTIC COMPOUNDS AND METHODS TO USE THEM
US10947251B2 (en) 2018-03-30 2021-03-16 Genentech, Inc. Therapeutic compounds and methods of use thereof

Family Cites Families (1)

* Cited by examiner, † Cited by third party
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WO2007075896A2 (en) * 2005-12-22 2007-07-05 Kemia, Inc. Heterocyclic cytokine inhibitors

Also Published As

Publication number Publication date
WO2009010784A1 (en) 2009-01-22
UY31219A1 (en) 2009-03-02
PE20090477A1 (en) 2009-05-24
TW200911766A (en) 2009-03-16
CL2008002038A1 (en) 2009-07-17

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