DK3077372T3 - Ror-gamma-modulatorer - Google Patents
Ror-gamma-modulatorer Download PDFInfo
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- DK3077372T3 DK3077372T3 DK14809794.2T DK14809794T DK3077372T3 DK 3077372 T3 DK3077372 T3 DK 3077372T3 DK 14809794 T DK14809794 T DK 14809794T DK 3077372 T3 DK3077372 T3 DK 3077372T3
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- phenyl
- acetamide
- hexafluoro
- hydroxypropan
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Claims (28)
1. Forbindelse med formlen I 0'Rs Ris^L-Rfs Aj3 ''''Au-II I A-m,^, An .N. .O R4 R10 rs ii |T^ Rg'^^'Y’X^ R8 R’ O Ri Meta eller para (Formel I) eller farmaceutisk acceptabelt salt deraf, hvor An - A14 er N eller henholdsvis CRu, CR12, CR-13, CR14 med det forbehold, at ikke mere end to af de fire positioner A samtidigt kan være N Ri er C(1-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, (di)C(1-6)alkylamino, hvor (di)C-(1-6)alkylamino som anvendt heri betyder en aminogruppe, som uafhængigt er monosubstitueret eller disubstitueret med H eller C(1-6)alkylgruppe(r) og, når (di)C(1-6)alkylaminogrupper indeholder to C(1-6)alkylgrupper, kan en af C(1-6)alkylgrupperne erstattes af en C(3-6)cycloalkylgruppe, (di)C(3-6)cycloalkylamino, hvor (di)C(3-6)cycloalkylamino som anvendt heri betyder en aminogruppe, som uafhængigt er monosubstitueret eller disubstitueret med H eller C(3-6)cycloalkylgruppe(r), og når (di)C(3-6)cycloalkylaminogrupperne indeholder to (C3-6)cycloalkylgrupper, kan en af C(3-6)cycloalkylgrupperne erstattes af en C(1-6)alkylgruppe, eller (di)(C(3-6)cycloalkylC(1-3)alkyl)amino, hvor (di)(C(3-6)cycloalkylC(1-3)alkyl)amino som anvendt heri betyder en aminogruppe, som uafhængigt er monosubstitueret eller disubstitueret med H eller C(3-6)cycloalkylC(1-3)alkylgruppe(r), med alle carbonatomer i alkylgrupper, der eventuelt kan være substitueret med én eller flere F’er, og alle carbonatomer i cycloalkylgrupper, der eventuelt kan være substitueret med én eller flere F’er eller methyl R2 og R3 uafhængigt er H, F, methyl, ethyl, hydroxy eller methoxy, eller R2 og R3 sammen er carbonyl, idet alle alkylgrupperne, hvis de forefindes, eventuelt kan være substitueret med én eller flere F'er R4 er Fl eller C(1-6)alkyl R5 er H, hydroxyethyl, methoxyethyl, C(1-6)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)heteroaryl, C(1- 9)heteroarylC(1-3)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(2-5)heterocycloalkyl eller C(2- 5) heterocycloalkylC(1-3)alkyl, idet alle grupper eventuelt kan være substitueret med én eller flere F, Cl, C(1-2)alkyl, C(1-2)alkoxy eller cyano; sulfonylgruppen med Ri udgøres af én af R7, Rs eller R9 de resterende R6-Ri4 uafhængigt er H, halogen, C(1-3)alkoxy, (di)C(1- 3) alkylamino, hvor (di)C(1-3)alkylamino som anvendt heri betyder en aminogruppe, der uafhængigt er monosubstitueret eller disubstitueret med Fl eller C(1-3)alkylgruppe(r), eller C(1-6)alkyl, idet alle alkylgrupperne eventuelt kan være substitueret med én eller flere F'er, og R15 og R16 uafhængigt er H, C(1-6)alkyl, C(3-6)cycloalkyl, C(3- 6) cycloalkylC(1-3)alkyl, C(6-10) aryl, C(6-10)arylC(1-3)alkyl, C (1-9)heteroaryl, C(1 -9) heteroarylC(1-3)alkyl, C(2-5)heterocycloalkyl eller C(2-5)heterocycloalkylC(1-3)alkyl, idet alle grupper eventuelt kan være substitueret med én eller flere F, Cl, C(1-2)alkyl, C(1-2)alkoxy eller cyano.
2. Forbindelse ifølge krav 1, hvor Rier C(1-2)alkyl, cyclopropyl, C(3- 4) cycloalkylC(1-3)alkyl, methylamino eller C(3-4)cycloalkylamino.
3. Forbindelse ifølge krav 2, hvor Ri er ethyl, cyclopropylamino eller cyclopropylmethyl.
4. Forbindelse ifølge krav 3, hvor R-ι er cyclopropylamino eller cyclopropylmethyl.
5. Forbindelse ifølge krav 4, hvor R1 er cyclopropylmethyl.
6. Forbindelse ifølge krav 1-5, hvor R2og R3 uafhængigt er H, methyl eller hydroxy.
7. Forbindelse ifølge krav 6, hvor R2 og R3 uafhængigt er Fl eller methyl.
8. Forbindelse ifølge krav 1-7, hvor R4 er H eller C(1-2)alkyl.
9. Forbindelse ifølge krav 1-8, hvor R5 er H, hydroxyethyl, methoxyethyl eller C(1-6)alkyl, idet alle alkylgrupper eventuelt kan være substitueret med én eller flere F'er.
10. Forbindelse ifølge krav 9, hvor R5 er H eller C(1-3)alkyl.
11. Forbindelse ifølge krav 1-8, hvor R5 er C(6)arylC(1-3)alkyl eller C(3-6)cycloalkylC(1 -3)alkyl.
12. Forbindelse ifølge krav 11, hvor R5 er benzyl.
13. Forbindelse ifølge krav 1-12, hvor R6-Rio er H med det forbehold, at én af grupperne R7, Rs eller Rg er en sulfonylgruppe med R-i.
14. Forbindelse ifølge krav 13, hvor Rs er en sulfonylgruppe med R-i.
15. Forbindelse ifølge krav 1-12, hvor Rs er en sulfonylgruppe med R-ι, og hvor R-io er methyl, og de resterende R6, R7 og R9 er H.
16. Forbindelse ifølge krav 1 -15, hvor alle Αη-Α-ι4 er carbon.
17. Forbindelse ifølge krav 1-15, hvor enten An eller Ai2 er nitrogen, og de resterende An-Ai4 er carbon.
18. Forbindelse ifølge krav 1-17, hvor Rn-Ri4 uafhængigt er H, halogen, methyl eller methoxy.
19. Forbindelse ifølge krav 18, hvor Rn-Ri4 er H.
20. Forbindelse ifølge krav 1-19, hvor R15 er CF3 og R-i6 er H, C(1-6)alkyl, C(3-6)cycloalkyl eller C(3-6)cycloalkylC(1-3)alkyl.
21. Forbindelse ifølge krav 20, hvor R15 er CF3 og R-i6 er CF3, propyl, isopropyl, 2-methylpropyl, 2,2-dimethylpropyl, cyclopropyl, cyclopentyl eller cyclohexylmethyl.
22. Forbindelse ifølge krav 21, hvor både R15 og Rie er CF3.
23. Forbindelse ifølge krav 1, som er valgt fra den gruppe, der består af: N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)-2-(4-(methylsulfonyl)phenyl)acetamid 2-(4-(ethylsulfonyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl) phenyl)acetamid N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)-2-(4-(isopropyl sulfonyl)phenyl)acetamid N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)-2-(4-(propylsulfonyl) phenyl)acetamid 2-(4-(ethylsulfonyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl) phenyl)propanamid N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)-2-(4-(N-methylsulfamoyl)phenyl)acetamid N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)-2-(4-(N-isopropylsulfamoyl)phenyl)acetamid 2-(4-(N-(cyclopropylmethyl)sulfamoyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)acetamid 2-(4-(N-cyclopropylsulfamoyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)acetamid 2-(4-(N-ethylsulfamoyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)acetamid 2-(4-(N,N-dimethylsulfamoyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)acetamid 2-(3-(N-cyclopropylsulfamoyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)acetamid 2-(3-(N-ethylsulfamoyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)acetamid 2-(3-(N,N-dimethylsulfamoyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)acetamid 2-(4-(ethylsulfonyl)phenyl)-N-(3-fluor-4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)-2-methylphenyl)acetamid 2-(4-(N-cyclopropylsulfamoyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)-N-methylacetamid 2-(4-(N-cyclopropylsulfamoyl)phenyl)-N-ethyl-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)acetamid 2-(3-(N-cyclopropylsulfamoyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2- hydroxypropan-2-yl)phenyl)-N-methylacetamid N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)-2-(3-(N- methylsulfamoyl)phenyl)acetamid 2-(4-(ethylsulfonyl)phenyl)-N-(5-fluor-4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)-2-methoxyphenyl)acetamid 2-(4-(ethylsulfonyl)phenyl)-N-(5-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)pyridin-2-yl)acetamid N-(5-chlor-4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)-2-methoxyphenyl)-2-(4-(ethylsulfonyl)phenyl)acetamid 2-(4-(ethylsulfonyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)-2,6-dimethylphenyl)acetamid 2-(3-(N-cyclobutylsulfamoyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)acetamid 2-(4-(N-cyclobutylsulfamoyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxy propan-2-yl)phenyl)acetamid 2-(4-(N-cyclopropylsulfamoyl)phenyl)-N-(3-fluor-4-(1,1,1,3,3,3-hexafluor-2- hydroxypropan-2-yl)-2-methylphenyl)acetamid N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)-2-(4- (isobutylsulfonyl)phenyl)acetamid 2-(4-(ethylsulfonyl)phenyl)-N-(2-fluor-4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)acetamid 2- (4-(ethylsulfonyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)- 3- methylphenyl)acetamid 2-(4-(ethylsulfonyl)phenyl)-N-(3-fluor-4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)acetamid 2-(4-(ethytsulfonyl)pheny))-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)-2-methylphenyl)acetamid 2-(4-(N-cyclopropylsulfamoyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)-3-methylphenyl)acetamid 2-(4-(N-cyclopropylsulfamoyl)phenyl)-N-(3-fluor-4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)acetamid 2-(4-(N-cyclopropylsulfamoyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)-2-methylphenyl)acetamid 2-(4-(N-cyclopropylsulfamoyl)phenyl)-N-(2-fluor-4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)acetamid 2-(3-(N-cyclopropylsulfamoyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)-3-methylphenyl)acetamid 2-(4-((cyclopropylmethyl)sulfonyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)acetamid 2-(3-(N-cyclopropylsulfamoyl)phenyl)-N-(3-fluor-4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)acetamid 2-(3-(N-cyclopropylsulfamoyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)-2-methylphenyl)acetamid 2-(3-(N-cyclopropylsulfamoyl)phenyl)-N-(2-fluor-4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)acetamid 2-(3-(N-(cyclopropylmethyl)sulfamoyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)acetamid 2-(4-(ethylsulfonyl)-3-fluorphenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)acetamid 2-(4-((cyclopropylmethyl)sulfonyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)-2-methylphenyl)acetamid 2-(4-((cydopropylmethy))sulfonyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)-3-methylphenyl)acetamid 2-(4-((cyclopropylmethyl)sulfonyl)phenyl)-N-(3-fluor-4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)acetamid 2-(4-((cyclopropylmethyl)sulfonyl)phenyl)-N-(2-fluor-4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)acetamid 2-(4-(ethylsulfonyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-methoxypropan-2-yl)phenyl)acetamid N-(4-2-ethoxy-1,1,1,3,3,3-hexafluorpropan-2-yl)phenyl)-2-(4-(ethylsulfonyl)phenyl)acetamid 2-(4-(ethylsulfonyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-propoxypropan-2-yl)phenyl)acetamid N-(4-(2-(benzyloxy)-1,1,1,3,3,3-hexafluorpropan-2-yl)phenyl)-2-(4-(ethylsulfonyl)phenyl)acetamid 2-(4-((cyclopropylmethyl)sulfonyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2- isopropoxypropan-2-yl)phenyl)acetamid N-(4-2-butoxy-1,1,1,3,3,3-hexafluorpropan-2-yl)phenyl)-2-(4- ((cyclopropylmethyl)sulfonyl)phenyl)acetamid 2-(4-((cyclopropylmethyl)sulfonyl)phenyl)-N-(4-(2-ethoxy-1,1,1,3,3,3- hexafluorpropan-2-yl)phenyl)acetamid 2-(4-((cyclopropylmethyl)sulfonyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-methoxypropan-2-yl)phenyl)acetamid 2-(4-((cyclopropylmethyl)sulfonyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2- hydroxypropan-2-yl)-2-methoxyphenyl)acetamid 2-(4-(cyclopropylmethyl)sulfonyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2- hydroxypropan-2-yl)-3-methoxyphenyl)acetamid N-(2-amino-4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)-2-(4- ((cyclopropylmethyl)sulfonyl)phenyl)acetamid N-(4-(2-(2-cyclopropylethoxy)-1,1,1,3,3,3-hexafluorpropan-2-yl)phenyl)-2-(4-((cyclopropylmethyl)sulfonyl)phenyl)acetamid N-(4-(2-(benzyloxy)-1,1,1,3,3,3-hexafluorpropan-2-yl)phenyl)-2-(4-((cyclopropylmethyl)sulfonyl)phenyl)acetamid 2-(4-((cyclopropylmethyl)sulfonyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-propoxypropan-2-yl)phenyl)acetamid 2-(4-(N-cyclopropylsulfamoyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-propoxypropan-2-yl)phenyl)acetamid N-(3-chlor-4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)-2-(4-((cyclopropylmethyl)sulfonyl)phenyl)acetamid 2-(4-(ethylsulfonyl)phenyl)-N-(4-(1,1,1 -trifluor-2-hydroxypentan-2-yl)phenyl)acetamid 2-(4-((cyclopropylmethyl)sulfonyl)phenyl)-N-(4-(1,1,1 -trifluor-2-hydroxyhexan-2-yl)phenyl)acetamid 2-(4-(ethylsulfonyl)phenyl)-N-(4-(1,1,1 -trifluor-2-hydroxy-3-methylbutan-2-yl)phenyl)acetamid 2-(4-(ethylsulfonyl)phenyl)-N-(4-(1,1,1 -trifluor-2-hydroxy-4-methylpentan-2-yl)phenyl)acetamid N-(4-(1-cyclopropyl-2,2,2-trifluor-1-hydroxyethyl)phenyl)-2-(4-((cyclopropylmethyl)sulfonyl)phenyl)acetamid N-(4-(3-cyclopentyl-1,1,1 -trifluor-2-hydroxypropan-2-yl)phenyl)-2-(4-((cyclopropylmethyl)sulfonyl)phenyl)acetamid N-(4-(3-cyclohexyl-1,1,1 -trifluor-2-hydroxypropan-2-yl)phenyl)-2-(4-((cyclopropylmethyl)sulfonyl)phenyl)acetamid 2-(4-((cyclopropylmethyl)sulfonyl)phenyl)-N-(4-(2,2,2-trifluor-1-hydroxyethyl)phenyl)acetamid 2-(4-((cyclopropylmethyl)sulfonyl)phenyl)-N-(4-(1,1,1 -trifluor-2-hydroxypropan-2-yl)phenyl)acetamid 2-(4-(ethylsulfonyl)phenyl)-N-(4-(1,1,1 -trifluor-2-hydroxyhexan-2-yl)phenyl)acetamid N-(4-(1-cyclopropyl-2,2,2-trifluor-1-hydroxyethyl)phenyl)-2-(4- (ethylsulfonyl)phenyl)acetamid N-(4-(3-cyclohexyl-1,1,1 -trifluor-2-hydroxypropan-2-yl)phenyl)-2-(4-(ethylsulfonyl)phenyl)acetamid N-(4-(1-cyclopentyl-2,2,2-trifluor-1-hydroxyethyl)phenyl)-2-(4- ((cyclopropylmethyl)sulfonyl)phenyl)acetamid 2-(4-(N-cyclopropylsulfamoyl)phenyl)-N-(4-(1,1,1 -trifluor-2-hydroxy-4-methylpentan-2-yl)phenyl)acetamid 2-(3-(N-cyclopropylsulfamoyl)phenyl)-N-(4-(1,1,1 -trifluor-2-hydroxy-4-methylpentan-2-yl)phenyl)acetamid 2-(4-(N-cyclopropylsulfamoyl)phenyl)-N-(4-(1,1,1 -trifluor-2-hydroxypropan-2-yl)phenyl)acetamid 2-(4-(N-cyclopropylsulfamoyl)phenyl)-N-(4-(1,1,1 -trifluor-2-hydroxybutan-2-yl)phenyl)acetamid 2-(4-(N-cyclopropylsulfamoyl)phenyl)-N-(4-(1,1,1 -trifluor-2-hydroxypentan-2-yl)phenyl)acetamid 2-(3-(N-cyclopropylsulfamoyl)phenyl)-N-(4-(1,1,1 -trifluor-2-hydroxypentan-2-yl)phenyl)acetamid 2-(4-(cyclopropylmethyl)sulfonyl)phenyl)-N-(4-(1,1,1 -trifluor-2-hydroxy-4,4-dimethylpentan-2-yl)phenyl)acetamid 2-(4-((cyclopropylmethyl)sulfonyl)phenyl)-N-(4-(1,1,1 -trifluor-2-hydroxybutan-2-yl)phenyl)acetamid N-(3-chlor-4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)-2-(4-(ethylsulfonyl)phenyl)acetamid N-(4-(1-cyclopentyl-2,2,2-trifluor-1-hydroxyethyl)phenyl)-2-(4- (ethylsulfonyl)phenyl)acetamid N-(4-(3-cyclopentyl-1,1,1 -trifluor-2-hydroxypropan-2-yl)phenyl)-2-(4-(ethylsulfonyl)phenyl)acetamid 2-(4-cyclopropylmethansulfonylphenyl)-N-[4-(1,1,1 -trifluor-2-hydroxy-3-phenylpropan-2-yl)phenyl]acetamid 2-(4-((cyclopropylmethyl)sulfonyl)phenyl)-N-(4-(2,2,2-trifluor-1-hydroxy-1- phenylethyl)phenyl)acetamid N-(3-chlor-4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)-2-(4-(N-cyclopropylsulfamoyl)phenyl)acetamid N-(4-(1-cyclopentyl-2,2,2-trifluor-1-hydroxyethyl)phenyl)-2-(4-(N-cyclopropylsulfamoyl)phenyl)acetamid N-(3-chlor-4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)-2-(3-(N-cyclopropylsulfamoyl)phenyl)acetamid N-(4-(1-cyclopentyl-2,2,2-trifluor-1-hydroxyethyl)phenyl)-2-(3-(N- cyclopropylsulfamoyl)phenyl)acetamid 2-(4-((cyclopropylmethyl)sulfonyl)-2-methylphenyl)-N-(4-1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)acetamid 2-(4-(N-cyclopropylsulfamoyl)phenyl)-N-(4-(1,1,1 -trifluor-2-hydroxy-4,4-di methylpentan-2-yl)phenyl)acetamid 2-(4-(N-cyclopropylsulfamoyl)phenyl)-N-(4-(1,1,1 -trifluor-2-hydroxy-3-methylbutan-2-yl)phenyl)acetamid 2-(4-(ethylsulfonyl)phenyl)-N-(4-(1,1,1 -trifluor-2-hydroxy-4,4-dimethylpentan-2-yl)phenyl)acetamid 2-(4-(ethylsulfonyl)phenyl)-N-(4-(2,2,2-trifluor-1 -hydroxy-1 -phenylethyl)phenyl)acetamid N-(2-chlor-4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)-2-(4-((cyclopropylmethyl)sulfonyl)phenyl)acetamid N-(4-(3-cyclopentyl-1,1,1 -trifluor-2-hydroxypropan-2-yl)phenyl)-2-(4-(N-cyclopropylsulfamoyl)phenyl)acetamid N-(4-(3-cyclohexyl-1,1,1 -trifluor-2-hydroxypropan-2-yl)phenyl)-2-(4-(N-cyclopropylsulfamoyl)phenyl)acetamid 2-(4-(N-cyclopropylsulfamoyl)phenyl)-N-(4-(2,2,2-trifluor-1-hydroxy-1 -phenylethyl)phenyl)acetamid 2-(4-((cyclopropylmethyl)sulfonyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)-2-oxoacetamid 2-(4-((cydopropylmethy)sulfonyl)phenyl)-N-(4-(2-hydroxypropan-2-yl)phenyl)acetamid 2-(4-(cyclopropylmethyl)sulfonyl)phenyl)-N-(4-(1,1,1 -trifluor-2-hydroxy-5-methylhexan-2-yl)phenyl)acetamid 2-(4-(N-cyclopropylsulfamoyl)phenyl)-N-(5-fluor-4-(1,1,1,3,3,3-hexafluor-2- hydroxypropan-2-yl)-2-methoxyphenyl)acetamid 2-(4-((cyclopropylmethyl)sulfonyl)phenyl)-N-(4- (dicyclopropyl(hydroxy)methyl)phenyl)acetamid 2-(4-((cyclopropylmethyl)sulfonyl)phenyl)-N-(5-(1,1,1,3,3,3-hexafluor-2- hydroxypropan-2-yl)pyridin-2-yl)acetamid 2-(4-((cyclopropylmethyl)sulfonyl)phenyl)-N-(4-(1,1,1 -trifluor-2-hydroxy-6-methylheptan-2-yl)phenyl)acetamid 2-(4-((cyclopropylmethyl)sulfonyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)propanamid 2-(4-((cyclopropylmethyl)sulfonyl)phenyl)-N-(6-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)pyridin-3-yl)acetamid 2-(4-(ethylsulfonyl)phenyl)-N-(6-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl) pyridin-3-yl)acetamid 2-(4-(ethylsulfonyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-(2,2,2-trifluorethoxy)propan-2-yl)phenyl)acetamid 2-(4-((cyclopropylmethyl)sulfonyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-(2,2,2-trifluorethoxy)propan-2-yl)phenyl)acetamid og 2-(4-((cyclopropylmethyl)sulfonyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)-2-hydroxyacetamid.
24. Forbindelse ifølge krav 23, som er 2-(4-((cyclopropylmethyl)sulfonyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluor-2-hydroxypropan-2-yl)phenyl)acetamid.
25. Forbindelse ifølge et hvilket som helst af kravene 1 til 24 eller farmaceutisk acceptabelt salt deraf til anvendelse i terapi.
26. Forbindelse ifølge et hvilket som helst af kravene 1 til 24 eller farmaceutisk acceptabelt salt deraf til anvendelse til behandling af RO Rymedierede sygdomme eller tilstande.
27. Farmaceutisk sammensætning, der omfatter en forbindelse med formel I ifølge et af kravene 1 til 24 eller et farmaceutisk acceptabelt salt deraf og et eller flere farmaceutisk acceptable excipienser.
28. Farmaceutisk sammensætning ifølge krav 27, der desuden omfatter mindst ét yderligere terapeutisk aktivt middel.
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AU2015248466A1 (en) * | 2014-04-16 | 2016-09-15 | Glenmark Pharmaceuticals S.A. | Aryl and heteroaryl ether compounds as ROR gamma modulators |
PT3212641T (pt) | 2014-10-30 | 2019-02-11 | Janssen Pharmaceutica Nv | Tiazoles como moduladores de rorãt |
CN108064224B (zh) | 2014-10-30 | 2022-03-29 | 詹森药业有限公司 | 作为Rorγt的调节剂的酰胺取代的噻唑 |
JOP20200117A1 (ar) | 2014-10-30 | 2017-06-16 | Janssen Pharmaceutica Nv | كحولات ثلاثي فلوروميثيل كمُعدلات للمستقبل النووي جاما تي المرتبط بحمض الريتيونَويك ROR?t |
CN107614062A (zh) | 2015-03-12 | 2018-01-19 | 加利福尼亚大学董事会 | 用RORγ抑制剂治疗癌症的方法 |
CN113121497A (zh) | 2015-05-15 | 2021-07-16 | 奥瑞基尼探索技术有限公司 | 用作RORγ调节剂的经过取代的四氢喹啉酮化合物 |
WO2016193894A1 (en) * | 2015-05-29 | 2016-12-08 | Glenmark Pharmaceuticals S.A. | Treatment of respiratory disorders using ror- gamma inhibitors |
EP3101008A1 (en) * | 2015-06-05 | 2016-12-07 | Lead Pharma Cel Models IP B.V. | Ror gamma (rory) modulators |
EP3101005A1 (en) * | 2015-06-05 | 2016-12-07 | Lead Pharma Cel Models IP B.V. | Ror gamma (rory) modulators |
WO2017010399A1 (ja) * | 2015-07-10 | 2017-01-19 | 塩野義製薬株式会社 | RORγt阻害作用を有する化合物およびそれらを含有する医薬組成物 |
TWI728017B (zh) | 2015-12-15 | 2021-05-21 | 瑞典商阿斯特捷利康公司 | 異吲哚化合物、包含其之醫藥組成物及其用途 |
TW201803869A (zh) | 2016-04-27 | 2018-02-01 | 健生藥品公司 | 作為RORγT調節劑之6-胺基吡啶-3-基噻唑 |
AR109042A1 (es) * | 2016-07-14 | 2018-10-24 | Cadila Healthcare Ltd | COMPUESTOS MODULARES DE RORg |
JP2019520400A (ja) | 2016-07-14 | 2019-07-18 | カディラ ヘルスケア リミティド | 新規シクロプロピル誘導体 |
US10196350B2 (en) * | 2016-12-05 | 2019-02-05 | Lead Pharma Holding B.V. | ROR gamma (RORγ) modulators |
WO2018116285A1 (en) * | 2016-12-23 | 2018-06-28 | Glenmark Pharmaceuticals S.A. | Substituted morpholine derivatives as ror gamma modulators |
JP2020524660A (ja) | 2017-06-14 | 2020-08-20 | アストラゼネカ・アクチエボラーグAstrazeneca Aktiebolag | Ror−ガンマモジュレーターとして有用な2,3−ジヒドロイソインドール−1−カルボキサミド |
JP2021528405A (ja) | 2018-06-18 | 2021-10-21 | ヤンセン ファーマシューティカ エヌ.ベー. | RORγtのモジュレータとしてのアミド置換チアゾール |
CA3103770A1 (en) | 2018-06-18 | 2019-12-26 | Janssen Pharmaceutica Nv | Phenyl and pyridinyl substituted imidazoles as modulators of roryt |
JP2021528398A (ja) | 2018-06-18 | 2021-10-21 | ヤンセン ファーマシューティカ エヌ.ベー. | RORγTのモジュレーターとしての6−アミノピリジン−3−イルピラゾール |
CN112292373A (zh) | 2018-06-18 | 2021-01-29 | 詹森药业有限公司 | 作为RORγt的调节剂的吡啶基吡唑类 |
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CN112759541B (zh) * | 2019-10-21 | 2023-03-17 | 复旦大学 | 类吲哚衍生物及其用途 |
CN113072521B (zh) * | 2020-01-06 | 2024-04-05 | 广东东阳光药业股份有限公司 | RORγt抑制剂及其在药物中的应用 |
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EP2909189B8 (en) * | 2012-10-16 | 2017-04-19 | Janssen Pharmaceutica NV | Heteroaryl linked quinolinyl modulators of ror-gamma-t |
WO2013171729A2 (en) | 2013-01-08 | 2013-11-21 | Glenmark Pharmaceuticals S.A. | Aryl and heteroaryl amide compounds as rorgamat modulator |
KR20150128863A (ko) * | 2013-03-15 | 2015-11-18 | 에프. 호프만-라 로슈 아게 | RORc 조절제로서 아릴 설파미드 및 설파메이트 유도체 |
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- 2014-12-03 DK DK14809794.2T patent/DK3077372T3/da active
- 2014-12-03 EP EP14809794.2A patent/EP3077372B8/en active Active
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2016
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- 2016-06-05 IL IL246018A patent/IL246018B/en active IP Right Grant
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2019
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