DK2421829T3 - 2,5-disubstituerede arylsulfonamid-ccr3-antagonister - Google Patents

2,5-disubstituerede arylsulfonamid-ccr3-antagonister Download PDF

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DK2421829T3
DK2421829T3 DK10714821.5T DK10714821T DK2421829T3 DK 2421829 T3 DK2421829 T3 DK 2421829T3 DK 10714821 T DK10714821 T DK 10714821T DK 2421829 T3 DK2421829 T3 DK 2421829T3
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compound
mhz
nmr
acid
dmso
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Tai Wei Ly
Marie Chantal Siu-Ying Tran
Erik Dean Raaum
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Axikin Pharmaceuticals Inc
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Claims (13)

1. Forbindelse med formel II:
(II) eller en enantiomer, en blanding af enantiomerer, en blanding af to eller flere diastereomerer, en tautomer eller en blanding af to eller flere tautomerer deraf; eller et farmaceutisk acceptabelt salt, solvat eller hydrat deraf; hvor: R1 og R2 hver for sig er fluor, chlor eller methyl; R3 er cyano eller nitro; R5 er methyl, oxo eller methoxycarbonyl; X er 0 eller S; Y er -0-, -S-, -S(0)- eller -S(0)2-; m er et helt tal på 1; n er et helt tal på 1 eller 2; og p er et helt tal på 0, 1 eller 2.
2. Forbindelse ifølge krav 1, hvor R1 og R2 er fluor.
3. Forbindelse ifølge krav 1, hvor R1 og R2 er chlor.
4. Forbindelse ifølge krav 1, hvor R1 og R2 er methyl.
5. Forbindelse ifølge krav 1, der er udvalgt fra gruppen, der består af:
58 71
82 85
86 ΠΟ
111 112
113 H4
115 116
117 140
141 142
143 144 og enantiomerer, blandinger af enantiomerer, blandinger af to eller flere diastereomerer, tautomerer og blandinger af to eller flere tautomerer deraf; og farmaceutisk acceptable salte, solvater og hydrater deraf.
6. Forbindelse ifølge et hvilket som helst af kravene 1 til 5, hvor forbindelsen er et hydrochloridsalt.
7. Farmaceutisk præparat, der omfatter en forbindelse ifølge et hvilket som helst af kravene 1 til 6 eller et farmaceutisk acceptabelt salt, solvat, hydrat eller en farmaceutisk acceptabel stereoisomer eller tautomer deraf; og et eller flere farmaceutisk acceptable bærematerialer eller excipienser; og eventuelt yderligere omfatter et andet terapeutisk middel.
8. Farmaceutisk præparat ifølge krav 7, hvor præparatet er formuleret til enkeltdosisadministration; eventuelt hvor præparatet er formuleret som en oral, parenteral eller intravenøs doseringsform; hvor den orale doseringsform fortrinsvis er en tablet eller en kapsel.
9. Forbindelse ifølge et hvilket som helst af kravene 1 til 6 eller farmaceutisk præparat ifølge krav 7 eller 8 til anvendelse i en fremgangsmåde til behandling, forebyggelse eller lindring af et eller flere symptomer på en CCR3-medieret forstyrrelse, sygdom eller tilstand.
10. Forbindelse ifølge et hvilket som helst af kravene 1 til 6 eller farmaceutisk præparat ifølge krav 7 eller 8 til anvendelse i en fremgangsmåde til behandling, forebyggelse eller lindring af et eller flere symptomer på en eosinofilforbundet forstyrrelse, sygdom eller tilstand; eller en fremgangsmåde til behandling, forebyggelse eller lindring af et eller flere symptomer på en basofilforbundet forstyrrelse, sygdom eller tilstand; eller en fremgangsmåde til behandling, forebyggelse eller lindring af et eller flere symptomer på en mastcelleforbundet forstyrrelse, sygdom eller tilstand.
11. Forbindelse ifølge et hvilket som helst af kravene 1 til 6 eller farmaceutisk præparat ifølge krav 7 eller 8 til anvendelse i en fremgangsmåde til behandling, forebyggelse eller lindring af et eller flere symptomer på en inflammationssygdom.
12. Forbindelse til anvendelse ifølge et hvilket som helst af kravene 9 til 11, hvor forstyrrelsen, sygdommen eller tilstanden er udvalgt fra gruppen, der består af astma, allergisk astma, anstrengelsesinduceret astma, allergisk rhinitis, helårs allergisk rhinitis, sæsonbetinget allergisk rhinitis, atopisk dermatitis, kontaktallergi, kontaktdermatitis, konjunktivitis, allergisk konjunktivitis, eosinofil bronkitis, fødevareallergier, eosinofil gastroenteritis, inflammatorisk tarmsygdom, ulcerativ colitis, Crohns sygdom, mastocytose, hyper-IgE-syndrom, systemisk lupus erythematous, psoriasis, akne, multipel sklerose, allograftafstødning, reperfusionsskade, Churg-Strauss-syndrom, sinusitis, basofil leukæmi, kronisk urticaria, basofil leukocytose, eksem, KOL (kronisk obstruktiv lungesygdom), arthritis, rheumatoid arthritis, psoriatisk arthritis, osteoarthritis og kardiovaskulære forstyrrelser; eller hvor forstyrrelsen, sygdommen eller tilstanden er astma, anstrengelsesinduceret astma, allergisk rhinitis, atopisk dermatitis, kronisk obstruktiv lungesygdom eller allergisk konjunktivitis.
13. Forbindelse til anvendelse ifølge et hvilket som helst af kravene 9 til 12, hvor forbindelsen skal administreres oralt, parenteralt eller topisk; og/eller hvor forbindelsen skal administreres i kombination med et andet terapeutisk middel.
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