SI22713B - Substituirani benzensulfonamidni derivati kot predzdravila COX-2 inhibitorjev - Google Patents
Substituirani benzensulfonamidni derivati kot predzdravila COX-2 inhibitorjev Download PDFInfo
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- SI22713B SI22713B SI9720101A SI9720101A SI22713B SI 22713 B SI22713 B SI 22713B SI 9720101 A SI9720101 A SI 9720101A SI 9720101 A SI9720101 A SI 9720101A SI 22713 B SI22713 B SI 22713B
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- sulfonyl
- phenyl
- phenylisoxazol
- alkyl
- sodium salt
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Abstract
Predzdravila COX-2 inhibitorjev s formulo (I) so opisana kot koristna pri zdravljenju vnetja in motenj, povezanih z vnetji, kjer je A obročni substituent, izbran izmed delno nenasičenega heterociklila, heteroarila, cikloalkenila in arila, kjer je A po želji substituiran pri legi, ki se da substituirati z enim ali več ostanki, izbranimi izmed naslednjih, kot so alkilkarbonil, formil, halo, alkil, haloalkil, okso, ciano, nitro, karboksil, alkoksi, aminokarbonil, alkoksikarbonil, karboksialkil, cianoalkil,hidroksialkil, haloalkilsulfoniloksi, alkoksialkiloksialkil, karboksialkoksialkil, cikloalkilalkil, alkenil, alkinil, heterocikliloksi, alkiltio, cikloalkil, aril, heterociklil, cikloalkenil, aralkil, heterociklilalkil, alkiltioalkil, arilkarbonil, aralkilkarbonil, aralkenil, alkoksialkil, ariltioalkil, ariloksialkil, aralkiltioalkil, aralkoksialkil, alkoksikarbonilalkil, aminokarbonilalkil, alkilaminokarbonil, N-arilaminokarbonil, N-alkil-N-arilaminokarbonil, alkilaminokarbonilalkil, alkilamino,N-arilamino, N-aralkilamino, N-alkil-N-aralkilamino, N-alkil-N-arilamino, aminoalkil, alkilaminoalkil, N-arilaminoalkil, N-aralkilaminoalkil, N-alkil-N-aralkilaminoalkil, N-alkil-N-arilaminoalkil, ariloksi, aralkoksi, ariltio, aralkiltio, alkilsulfinil, alkilsulfonil, aminosulfonil, alkilaminosulfonil, N-arilaminosulfonil, arilsufonil in N-alkil-N-arilaminosulfonil; kjer R1 izberemo izmed heterociklila, cikloalkila, cikloalkenila in arila, kjer je R1 po želji substituiran pri legi, ki se da substituirati,z enim ali več ostanki izbranimi izmed alkila, haloalkila, ciano, karboksila, alkoksikarbonila, hidroksila, hidroksialkila, haloalkoksi, amino, alkilamino, arilamino, nitro, alkoksialkila, alkilsulfinila, halo, alkoksi in alkiltio; kjer R2 izberemo izmed hidrido in alkoksikarbonilalkila; in kjer R3 izberemo izmed alkila, karboksialkila, acila, alkoksikarbonila, heteroarilkarbonila, alkoksikarbonilalkilkarbonila, alkoksikarbonilkarbonila, amino kislinskega ostanka in alkilakarbonilaminoalkilkarbonila; podpogojem, da A ni tetrazolij ali piridinij; in nadalje pod pogojem, da A ni indanon, kadar je R3 alkil ali karboksialkil; ali njihova farmacevtsko sprejemljiva sol.
Claims (15)
1 SI 22713 -UO PATENTNI ZAHTEVKI 1. Spojina, izbrana izmed spojin in njihovih farmacevtsko sprejemljivih soli, iz skupine, v kateri so kalijeva sol N- [ [4- [5-metil-3 -fenilizoksazol-4-il] fenil] sulfonil] acetamida; natrijeva sol N-[[4-[3-(3-fluorofenil)-5-metilizoksazol-4-il]fenil]sulfonil] acetamida; natrijeva sol 2-metil-N-[[4-[5-metil-3-fenilizoksazol-4-il]fenil]sulfonil] propanamida; natrijeva sol N-[[4-[5-metil-3-fenilizoksazol-4-il]fenil]sulfonil]benzamida; natrijeva sol 2,2-dimetil-N-[[4-[5-metil-3-fenilizoksazol-4-il]fenil]sulfonil] propanamida; natrij eva sol N- [ [4- [ 5 -metil-3 -fenilizoksazol-4-il] fenil]sulfonil]butanamida; natrijeva sol N-[[4-[5-metil-3-fenilizoksazol-4-il]fenil]sulfonil]pentanamida; natrijeva sol N-[[4-[5-metil-3-fenilizoksazol-4-il]fenil]sulfonil]heksanamida; natrijeva sol N-[[4-[2-metil-4-feniloksazol-5-il]fenil]sulfonil]acetamida; natrij evasolN-[[4-[5 -difluorometil-3 -fenilizoksazol-4-il] fenil] sulfonil] propanamida; natrijeva sol N-[[4-[5-difluorometil-3-fenilizoksazol-4-il]fenil]sulfonil] butanamida; natrijeva sol N-[[4-[5-hidroksimetil-3-fenilizoksazol-4-il]fenil]sulfonil] propanamida; natrijeva sol N-[[4-[5-metil-3-fenilizoksazol-4-il]fenil]sulfonil]glicina; in natrijeva sol N-[[4-[5-hidroksimetil-3-fenilizoksazol-4-il]fenil]sulfonil]acetamida.
2. Farmacevtski sestavek, ki obsega terapevtsko učinkovito količino spojine ali njene farmacevtsko sprejemljive soli po zahtevku 1. 2 SI 22713 -UO
3. Postopek za pripravo spojine ali njene farmacevtsko sprejemljive soli po zahtevku 1, ki obsega obdelavo nesubstituiranega sulfonamida z acilimim sredstvom v prisotnosti baze in topila.
4. Postopek po zahtevku 3, kjer acilimo sredstvo izberemo izmed anhidridov, kislinskih kloridov, acila, imidazolov in aktivnih estrov.
5. Postopek po kateremkoli od zahtevkov 3 ali 4, kjer je topilo tetrahidrofuran.
6. Postopek za pripravo spojine ali njene farmacevtsko sprejemljive soli po zahtevku 1, ki obsega obdelavo nesubstituiranega izoksazol benzen-sulfonamida z acilimim sredstvom v prisotnosti baze in topila.
7. Postopek za pripravo farmacevtsko sprejemljive soli spojine po zahtevku 1, ki obsega tvogenje bis(N-aciliranega)sulfonamida z obdelavo nesubstituiranega sulfonamida s prebitkom anhidrida, kislinskega klorida ali karbamilklorida v prisotnosti terc.aminske baze in obdelavo bis(N-aciliranega)sulfonamida z okoli dvema ekvivalentoma močne baze, da dobimo sol.
8. Uporaba spojine ali njene farmacevtsko sprejemljive soli po zahtevku 1 za pripravo zdravila za zdravljenje stanja, izbranega izmed vnetja in motnje, povezane z vnetjem.
9. Uporaba po zahtevku 8, kjer je stanje vnetje.
10. Uporaba po zahtevku 8, kjer je stanje motnja, povezana z vnetjem.
11. Uporaba po zahtevku 10, kjer je motnja, povezana z vnetjem, bolečina.
12. Uporaba po zahtevku 11, kjer je bolečina povezana z rakom. SI 22713 -UO 3
13. Uporaba po zahtevku 11, kjer je bolečina dentalna bolečina.
14. Uporaba po zahtevku 11, kjer zdravilo dajemo intravensko.
15. Uporaba po zahtevku 11, kjer zdravilo dajemo intramuskulamo.
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US63151496A | 1996-04-12 | 1996-04-12 | |
PCT/US1997/005497 WO1997038986A1 (en) | 1996-04-12 | 1997-04-11 | Substituted benzenesulfonamide derivatives as prodrugs of cox-2 inhibitors |
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SI22713A SI22713A (sl) | 2009-08-31 |
SI22713B true SI22713B (sl) | 2009-12-31 |
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SI9720101A SI22713B (sl) | 1996-04-12 | 1997-04-11 | Substituirani benzensulfonamidni derivati kot predzdravila COX-2 inhibitorjev |
SI9720035A SI9720035B (sl) | 1996-04-12 | 1997-04-11 | Substituirani benzensulfonamidni derivati kot predzdravila COX-2 inhibitorjev |
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SI9720035A SI9720035B (sl) | 1996-04-12 | 1997-04-11 | Substituirani benzensulfonamidni derivati kot predzdravila COX-2 inhibitorjev |
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