DK2496084T3 - Sammensætninger og fremgangsmåder til behandling af colitis - Google Patents

Sammensætninger og fremgangsmåder til behandling af colitis Download PDF

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DK2496084T3
DK2496084T3 DK10829180.8T DK10829180T DK2496084T3 DK 2496084 T3 DK2496084 T3 DK 2496084T3 DK 10829180 T DK10829180 T DK 10829180T DK 2496084 T3 DK2496084 T3 DK 2496084T3
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substituted
unsubstituted
methyl
hydroxy
branched
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DK10829180.8T
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Joseph H Gardner
Robert Shalwitz
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Aerpio Therapeutics Inc
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Claims (15)

1. Effektiv mængde af en eller flere forbindelser med formlen:
hvor L er valgt blandt CH2 og S02; R betegner fra 0 til 5 substitutioner for hydrogen; indekset n er et heltal fra 0 til 5; R1 og R2 hver er uafhængigt valgt blandt: i) hydrogen; ii) substitueret eller usubstitueret lineært, forgrenet eller cyklisk (C-|-C10)-alkyl; iii) substitueret eller usubstitueret lineært, forgrenet eller cyklisk (C2-Ci0)-alkenyl; iv) substitueret eller usubstitueret lineært eller forgrenet (C2-C10)-alkynyl; v) substitueret eller usubstitueret C6- eller C10-aryl; vi) en substitueret eller usubstitueret (Ci-C9)-heterocyklisk ring; vii) substitueret eller usubstitueret (Ci-Cg)-heteroaryl; eller viii) R1 og R2 sammen kan udgøre en substitueret eller usubstitueret heterocyklisk ring eller substitueret eller usubstitueret heteroarylring med fra 2 til 20 carbonatomer og fra 1 til 7 heteroatomer; eller et farmaceutisk acceptabelt salt deraf til anvendelse til behandling af en inflammatorisk epitelsygdom hos et individ.
2. Forbindelse til anvendelse ifølge krav 1, hvor forbindelsen eller forbindelserne foreligger i form af et farmaceutisk acceptabelt salt valgt blandt hydrochloridsalt, hydrogensulfatsalt, sulfatsalt, p-toluensulfonylsalt, methansulfonylsalt og blandinger deraf.
3. Forbindelse til anvendelse ifølge enten krav 1 eller 2, hvor L er CH2.
4. Forbindelse til anvendelse ifølge et hvilket som helst af kravene 1 -3, hvor hvert R er en substitution for hydrogen, som er uafhængigt valgt blandt: i) substitueret eller usubstitueret lineært (C1-C12)-, forgrenet (C3-C12)- eller cyklisk (C3-Ci2)-alkyl; ii) substitueret eller usubstitueret lineært (C1-C12)-, forgrenet (C3-C12)- eller cyklisk (C3-C12)-alkenyl; iii) substitueret eller usubstitueret lineært (C2-C12)- eller forgrenet (C3-Ci2)-alkynyl; iv) substitueret eller usubstitueret C6- eller C10-aryl; v) en substitueret eller usubstitueret (Ci-C9)-heterocyklisk ring; vi) substitueret eller usubstitueret (Ci-Cn)-heteroaryl; vii) halogen; viii) -=[C(R23a)(R23b)]xOR10; R10 er valgt blandt: a) -H; b) substitueret eller usubstitueret lineært (C1-C12)-, forgrenet (C3-Ci2)-eller cyklisk (C3-Ci2)-alkyl; c) substitueret eller usubstitueret Ce- eller Cio-aryl eller -alkylenaryl; d) en substitueret eller usubstitueret (Ci-CgJ-heterocyklisk ring; e) substitueret eller usubstitueret (Ci-Cn)-heteroaryl; ix) -[C(R23a)(R23b)]xN(R11a)(R11b); R11aog R11b hver er uafhængigt valgt blandt: a) -H; b) -OR12; R12er hydrogen eller lineært (C1-C4)-alkyl; c) substitueret eller usubstitueret lineært (C1-C12)-, forgrenet (C3-Ci2)-eller cyklisk (C3-Ci2)-alkyl; d) substitueret eller usubstitueret C6- eller C10-aryl; e) en substitueret eller usubstitueret (CrCgJ-heterocyklisk ring; f) substitueret eller usubstitueret (Ci-Cn)-heteroaryl; eller g) R11a og R11b sammen kan udgøre en substitueret eller usubstitueret ring med fra 3 til 10 carbonatomer og fra 0 til 3 heteroatomer valgt blandt oxygen, nitrogen og svovl;
a) substitueret eller usubstitueret lineært (C1-C12)-, forgrenet (C3-C12)-eller cyklisk (C3-Ci2)-alkyl; b) -OR14; R14 er hydrogen, substitueret eller usubstitueret lineært (C1-C4)-alkyl, substitueret eller usubstitueret C6- eller C10-aryl, en substitueret eller usubstitueret (Ci-C9)-heterocyklisk ring, substitueret eller usubstitueret (CrCn)-heteroaryl; c) -N(R15a)(R15b); R15a og R15b hver uafhængigt er hydrogen, substitueret eller usubstitueret lineært (C1-C12)-, forgrenet (C3-C12)- eller cyklisk (C3-C12)-alkyl; substitueret eller usubstitueret C6- eller Cio-aryl; en substitueret eller usubstitueret (CrCgJ-heterocyklisk ring; substitueret eller usubstitueret (Ci-Cn)-heteroaryl; eller R15a og R15b sammen kan udgøre en substitueret eller usubstitueret ring med fra 3 til 10 carbonatomer og fra 0 til 3 heteroatomer valgt blandt oxygen, nitrogen og svovl;
a) substitueret eller usubstitueret lineært (C1-C12)-, forgrenet (C3-C12)-eller cyklisk (C3-Ci2)-alkyl; b) -N(R17a)(R17b); R17a og R17b hver uafhængigt er hydrogen, substitueret eller usubstitueret lineært (CrCi2)-, forgrenet (C3-Ci2)- eller cyklisk (C3-Ci2)- alkyl; substitueret eller usubstitueret C6- eller Ci0-aryl; en substitueret eller usubstitueret (Ci-C9)-heterocyklisk ring; substitueret eller usubstitueret (CrCn)-heteroaryl; eller R17a og R17b sammen kan udgøre en substitueret eller usubstitueret ring med fra 3 til 10 carbonatomer og fra 0 til 3 heteroatomer valgt blandt oxygen, nitrogen og svovl;
a) -H; eller b) substitueret eller usubstitueret lineært (C1-C4)-, forgrenet (C3-C4)-eller cyklisk (C3-C4)-alkyl; R19 er: a) substitueret eller usubstitueret lineært (C1-C12)-, forgrenet (C3-C12)-eller cyklisk (C3-C12)-alkyl; b) -N(R20a)(R20b); R20a og R20b hver uafhængigt er hydrogen, substitueret eller usubstitueret lineært (C1-C4)- eller forgrenet (C2-C4)-alkyl; substitueret eller usubstitueret C6- eller C10-aryl; en substitueret eller usubstitueret (C-i-C9)-heterocyklisk ring; substitueret eller usubstitueret (C-i-C-n)-heteroaryl; eller R20a og R20b sammen kan udgøre en substitueret eller usubstitueret ring med fra 3 til 10 carbonatomer og fra 0 til 3 heteroatomer valgt blandt oxygen, nitrogen og svovl; xiii) -[C(R23a)(R23b)]xCN; xiv) -[C(R23a)(R23b)]xN02; xv) -[C(R23a)(R23b)]xR21; R21 er lineært, forgrenet eller cyklisk (Ci-Cio)-alkyl substitueret med fra 1 til 21 halogenatomer valgt blandt -F, -Cl, -Br og -I; xvi) -[C(R23a)(R23b)]xS02R22; R22 er hydrogen, hydroxyl, substitueret eller usubstitueret lineært (C-1-C4)-eller forgrenet (C2-C4)-alkyl; substitueret eller usubstitueret C6-, C10- eller Ci4-aryl; (C7-Ci5)-alkylenaryl; en substitueret eller usubstitueret (C1-C9)-heterocyklisk ring eller substitueret eller usubstitueret (Ci-Cn)-heteroaryl; R23a og R23b hver uafhængigt er hydrogen eller (C1-C4)-alkyl; og indekset x er et heltal fra 0 til 5.
5. Forbindelse til anvendelse ifølge et hvilket som helst af kravene 1 -4, hvor R1 og R2 sammen udgør en 5-leddet substitueret eller usubstitueret (C1-C4)- heterocyklisk ring eller en substitueret eller usubstitueret (C1-C4)- heteroarylring.
6. Forbindelse til anvendelse ifølge et hvilket som helst af kravene 1-5, hvor R1 og R2 sammen udgør en ring med formlen: i)
ii)
iii)
iv)
v)
vi)
vii)
viii)
ix)
x)
xi)
xii)
xiii)
eller xiv)
7. Forbindelse til anvendelse ifølge et hvilket som helst af kravene 1-6, hvor R1 og R2 sammen udgør en ring valgt blandt pyrrolidin-1-yl, 3-hydroxy-pyrrolidin-1 -yl, 2-(pyridin-2-yl)pyrrolidin-1 -yl, 2-methylcarboxypyrrolidin-1 -yl, 2- (methoxymethyl)pyrrolidin-1-yl, thiazolidin-3-yl, 1 /-/-imidazol-1 -yl, piperidin-1 -yl, 4-benzylpiperidin-1-yl, 1,4'-bipiperidinyl-1'-yl, piperazin-1-yl, 4-benzyl-piperazin-1 -yl, 4-(2-methoxyphenyl)-piperazin-1 -ylmethyl, 4-(6-chlorpyridazin- 3- yl)piperazin-1-yl, 1,4-dioxa-8-azaspiro[4,5]dec-8-yl, morpholin-4-yl, thiomorpholin-4-yl, azepan-1-yl, azocan-1-yl og 3,4-dihydroquinolin-1 (2H)-yl.
8. Forbindelse til anvendelse ifølge et hvilket som helst af kravene 1-4, hvor R2 er hydrogen, og R1 er valgt blandt benzyl, 4-methoxybenzyl, 4-fluorbenzyl, 4- chlorbenzyl, 4-methylbenzyl, 2-(pyridin-2-yl)ethyl, [1,3]dioxolan-2-ylmethyl, tetrahydrofuran-2-ylmethyl, 2-methoxyethyl, 1 -hydroxy-2-methylpropan-2-yl, pyridin-4-ylmethyl, furan-2-ylmethyl, 2-(methylthio)ethyl, 1-phenylethyl, 3-imidazol-1 -ylpropyl, cycloheptyl, 4-methylcyclohexyl, 1 -benzylpiperidin-4-yl, azepan-2-on-3-yl og 1 -benzyl-pyrrolidin-3-yl.
9. Forbindelse til anvendelse ifølge krav 1, hvor forbindelsen eller forbindelserne har formlen:
hvor Z er phenyl substitueret med fra 1 til 5 halogenatomer valgt blandt fluor og chlor; R4 er lineært (CrC4)-alkyl eller forgrenet (C3-C4)-alkyl; eller et farmaceutisk acceptabelt salt deraf.
10. Forbindelse til anvendelse ifølge krav 9, hvor R4 er valgt blandt methyl, ethyl og ferf-butyl.
11. Forbindelse til anvendelse ifølge et hvilket som helst af kravene 9 eller 10, hvor Z er valgt blandt 2-chlorphenyl, 3-chlorphenyl, 4-chlorphenyl, 2-fluorphenyl, 3-fluorphenyl og 4-fluorphenyl.
12. Forbindelse til anvendelse ifølge krav 1, hvor forbindelsen eller forbindelserne er tert- butyl-4-{[1 -(4-chlorbenzyl)-3-hydroxy-2-oxo-1,2-dihydropyridin-4-yl]methyl}-piperazin-1-carboxylat eller et farmaceutisk acceptabelt salt valgt blandt hydrochloridsalt, hydrogensulfatsalt, sulfatsalt, p-toluensulfonylsalt, methansulfonylsalt og blandinger deraf.
13. Forbindelse til anvendelse ifølge krav 1, hvor forbindelsen eller forbindelserne er valgt blandt: methyl-4-{[1-(4-chlorbenzyl)-3-hydroxy-2-oxo-1,2-dihydropyridin-4- yl]methyl}piperazin-1-carboxylat; methyl-4-{[1-(3-chlorbenzyl)-3-hydroxy-2-oxo-1,2-dihydropyridin-4-yl]methyl}piperazin-1-carboxylat; methyl-4-{[1-(2-chlorbenzyl)-3-hydroxy-2-oxo-1,2-dihydropyridin-4- yl]methyl}piperazin-1-carboxylat; ethyl-4-{[1-(4-chlorbenzyl)-3-hydroxy-2-oxo-1,2-dihydropyridin-4- yl]methyl}piperazin-1-carboxylat; ethyl-4-{[1-(3-chlorbenzyl)-3-hydroxy-2-oxo-1,2-dihydropyridin-4- yl]methyl}piperazin-1-carboxylat; ethyl-4-{[1-(2-chlorbenzyl)-3-hydroxy-2-oxo-1,2-dihydropyridin-4- yl]methyl}piperazin-1-carboxylat; fe/?-butyl-4-{[1-(3-chlorbenzyl)-3-hydroxy-2-oxo-1,2-dihydropyridin-4- yl]methyl}piperazin-1-carboxylat; fe/t-butyl-4-{[1-(2-chlorbenzyl)-3-hydroxy-2-oxo-1,2-dihydropyridin-4- yl]methyl}piperazin-1-carboxylat; methyl-4-{[1-(4-fluorbenzyl)-3-hydroxy-2-oxo-1,2-dihydropyridin-4- yl]methyl}piperazin-1-carboxylat; methyl-4-{[1-(3-fluorbenzyl)-3-hydroxy-2-oxo-1,2-dihydropyridin-4- yl]methyl}piperazin-1-carboxylat; methyl-4-{[1-(2-fluorbenzyl)-3-hydroxy-2-oxo-1,2-dihydropyridin-4- yl]methyl}piperazin-1-carboxylat; ethyl-4-{[1-(4-fluorbenzyl)-3-hydroxy-2-oxo-1,2-dihydropyridin-4- yl]methyl}piperazin-1-carboxylat; ethyl-4-{[1-(3-fluorbenzyl)-3-hydroxy-2-oxo-1,2-dihydropyridin-4- yl]methyl}piperazin-1-carboxylat; ethyl-4-{[1-(2-fluorbenzyl)-3-hydroxy-2-oxo-1,2-dihydropyridin-4- yl]methyl}piperazin-1-carboxylat; ieri-butyl-4-{[1-(4-fluorbenzyl)-3-hydroxy-2-oxo-1,2-dihydropyridin-4- yl]methyl}piperazin-1-carboxylat; ieri-butyl-4-{[1-(3-fluorbenzyl)-3-hydroxy-2-oxo-1,2-dihydropyridin-4-yl]methyl}piperazin-1 -carboxylat og ieri-butyl-4-{[1-(2-fluorbenzyl)-3-hydroxy-2-oxo-1,2-dihydropyridin-4-yl]methyl}piperazin-1-carboxylat.
14. Forbindelse ifølge et hvilket som helst af kravene 1-13, hvor den inflammatoriske epitelsygdom er en sygdom, der rammer tarm-epitelvæv; eller hvor den inflammatoriske epitelsygdom er valgt blandt en sygdom, der rammer luftvejene, slimhinderne, huden, mave-tarm-kanalen, slimhinden i vigtige organer og endokrine kirtler, karvæv og kombinationer deraf; eller hvor sygdommen er valgt blandt Crohns sygdom, ulcerativ colitis, kollagen colitis, lymfocytær colitis, iskæmisk colitis, diversionscolitis, Behgets syndrom og uklassificerbar colitis.
15. Sammensætning, som omfatter a) en effektiv mængde af en eller flere forbindelser ifølge et af kravene 1-14 eller et farmaceutisk acceptabelt salt deraf og b) en eller flere excipienser, til anvendelse til behandling af en inflammatorisk epitelsygdom hos et individ.
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