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US 2019/0099403 A1Published application
Use of ddx3 inhibitors as antiproliferative agents
AssigneeAzienda Ospedaliera Universitaria Senrese
InventorsAnnalaura BRAI, Maurizio BOTTA, Cristina TINTPRO, Glovanni MAGA
Life of this patent
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Abstract
The present invention refers to compounds of formula I or II endowed with DDX3 inhibitory activity, relative pharmaceutical compositions and their use as antihyperproliferative agents. (I) or (II)
Claims24
A method for the treatment and/or prevention of a hyperproliferative disorder, comprising administering an effective amount of a compound of formula:
- wherein
- X and Y are each independently C or N;
- A is unsubstituted or substituted aryl or unsubstituted or substituted heteroaryl, wherein the one or more substituents on the aryl or heteroaryl are independently selected from unsubstituted or substituted C1-C6 alkyl, unsubstituted or substituted C2-C6 alkenyl, unsubstituted or substituted C2-C6 alkynyl, haloalkyl, halogen, ORA, SRA, S(═O)(═O)—RA, SO2NHRA, COORB, OC(O)RB, C(O)RB, NRARB, OP(O)(ORA)2, NHC(O)RA, COONRARB, OS or
- wherein the one or more substituents on the C1-C6 alkyl or on the C2-C6 alkenyl or on the C2-C6 alkynyl are independently selected from ORA, COORB, OC(O)RB, C(O)RB, NRARB, OP(O)(ORA)2, NHC(O)RA, NHC(O)ORA, COONRARB, SRA, S(═O)(═O)—RA, SO2NHRA;
- R1, R2, R3, R4, R6, R7 and R10 are each independently selected from H, halogen, alkoxy, C1-C6 alkyl, haloalkyl, ORA, SRA, S(═O)(═O)—RA, SO2NHRA, COORB, OC(O)RB, NRARB, OP(O)(ORA)2, NHC(O)RA, COONRARB, NO2, CN;
- Z is a heteroaryl group selected from:
- wherein
- R5 is H, unsubstituted or substituted C1-C10-alkyl, unsubstituted or substituted phenyl, wherein the one or more substituents on the C1-C10-alkyl are independently selected from halogen, ORA, COORB, OC(O)RB, NRARB, OP(O)(ORA)2, OC(O)NRARB, C(O)RB, NHC(O)ORA, NHC(O)RA, COONRARB, OC(O)CHCHRC,
- RA and RB are each independently selected from H, substituted or unsubstituted C1-C6 alkyl, C1-C6 cycloalkyl, unsubstituted or substituted aralkyl, haloalkyl,
- or RA and RB together with the nitrogen to which they are attached, form a 4-7 membered saturated or partially unsaturated ring optionally containing one or more additional heteroatoms independently selected from N, S and O the ring being optionally substituted by one, two or more groups independently selected from halogen, C1-C6 alkyl, haloalkyl, OH, alkoxy;
- RC is substituted or unsubstituted phenyl, 1,3 benzodioxolyl, wherein the one or more substituent(s) on the phenyl are independently selected from halogen, haloalkyl, alkoxy, C1-C3 alkyl, or OH;
- wherein the one or more substituents on the phenyl are independently selected from halogen, haloalkyl, alkoxy, C1-C3 alkyl, OH;
- R8 and R9 are each independently selected from H, halogen, alkoxy, COOH, nitro and at least one of R8 and R9 is a heteroaryl group selected from:
- or salt, solvate, stereoisomer thereof,
- provided that compounds:
- are excluded.
13 more elements
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Dependencies are inferred from the claim text.