COMPOUNDS AS MODULATORS OF ENDOPLASMIC RETICULUM AMINOPEPTIDASE 1 (ERAP1)

A compound of formula (I-1), or a pharmaceutically accept able salt or hydrate thereof, formula (I-1) wherein: ring A is a monocyclic 5, 6, or 7-membered heterocycloalkyl ring optionally substituted by one or more substituents selected from alkyl, CN, cycloalkyl, OH, alkoxy, halo, haloalkyl and hete...

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Bibliographische Detailangaben
Hauptverfasser: IVENS, Eleanor, SPARENBERG, Michael, QUIBELL, Martin, SHIERS, Jason John
Format: Patent
Sprache:eng ; fre ; ger
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Zusammenfassung:A compound of formula (I-1), or a pharmaceutically accept able salt or hydrate thereof, formula (I-1) wherein: ring A is a monocyclic 5, 6, or 7-membered heterocycloalkyl ring optionally substituted by one or more substituents selected from alkyl, CN, cycloalkyl, OH, alkoxy, halo, haloalkyl and heteroaryl, wherein said heteroaryl group is in turn optionally further substituted with one or more groups selected from halo and alkyl, and wherein one or two carbons in the 5, 6, or 7-membered heterocycloalkyl ring are optionally replaced by a group selected from O, NH, S and CO; L is a linker group which is a 2 to 7-membered saturated or unsaturated aliphatic group, wherein one or two carbon atoms in said group, other than the carbon atom directly bonded to ring A, are optionally replaced by a heteroatom-containing group selected from O, NH and S, and wherein when two carbon atoms are replaced, the heteroatom-containing groups are separated by at least two carbon atoms and the linker group is at least a 5-membered group; the group X-Y is -NR23SO2- or -SO2NR23-; R1 is H, CN or alkyl; R2 is selected from COOH, tetrazolyl and C(O)NHSO2R24; R3 is selected from H, halo and alkyl; R4 is selected from H and halo; R6 is H; R7 is selected from H, CN, haloalkyl, halo, SO2-alkyl, SO2NR18R19, CONR20R21, heteroaryl and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents select ed from alkyl, halo, alkoxy, CN, haloalkyl and OH; R8 is selected from H, alkyl, haloalkyl and halo; R9 is H, alkyl or halo; R18-R21 and R23 are each independently selected from H and alkyl; R24 is selected from alkyl and cyclopropyl. Further aspects of the invention relate to such compounds for use in the field of immuno-oncology and related applications.