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US 12,655,141 B2Granted
Inhibitors of notch signaling pathway and use thereof in treatment of cancers
AssigneeCellestia Biotech AG
InventorsRajwinder Lehal, Guido Bold, Charlotte Urech, Vincent Zoete
Life of this patent
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Abstract
The present invention relates to new inhibitors of Notch signalling pathway and its use in the treatment and/or prevention of cancers.
Claims17
A compound of formula (I)
- or a pharmaceutically acceptable salt thereof,
- wherein
- X is O;
- Y1 is N and R7 is absent;
- Y2 is N or C and Y3 is C;
- Z is NR10R11, wherein R10 and R11 are each independently H or C1-C6 alkyl;
- R1 is H, halogen, and C1-C4 alkyl;
- R2 is aryl or heteroaryl, wherein the aryl or the heteroaryl are optionally substituted with C1-C6 alkyl or halogen;
- R3 is H, halogen, and C1-C4 alkyl;
- R4, R5, and R6 are each independently H, halogen, and C1-C4 alkyl;
- R8 is selected from H, halogen, and C1-C4 alkyl;
- R9 is absent when Y2 is N or is selected from H, halogen, and C1-C4 alkyl when Y2 is C;
- and
- with the proviso that the compound of formula (I) is not 6-([1,1′-biphenyl]-4-yloxy)-pyridine-3-amine, 6-([1,1′-biphenyl]-4-yloxy)-2-methylpyridin-3-amine, 6-([1,1′-biphenyl]-4-yloxy)-4-methylpyridin-3-amine;
- with the proviso that the compound of formula (I) is not a
- (i) Y2 and Y3 are both C, Z is NH2, R1 is H, R2 is phenyl, R3 is H, R4 is Cl, Br, or Me, R5 is H, R6 is H, R8 is H, and R9 is H;
- or
- (ii) Y2 and Y3 are both C, Z is NH2, R1 is H, R2 is phenyl, R3 is H, R4 is H, R5 is H, R6 is H, R8 is Cl, and R9 is H;
- or
- (iii) Y2 and Y3 are both C, Z is NH2, R1 is H, R2 is pyridyl substituted at the para position with methoxy, R3 is H, R4 is H, R5 is H, R6 is H, R8 is H, and R9 is H;
- or
- (iv) Y2 and Y3 are both C, Z is NH2, R1 is H, R2 is phenyl substituted at the ortho position with methoxy and meta position with F, R3 is H, R4 is H, R5 is H, R6 is H, R8 is H, and R9 is H;
- or
- (v) Y2 and Y3 are both C, Z is NH2, R1 is H, R2 is 1H-pyrazol-4-yl or 5-menthyl-1H-indol-3-yl, R3 is H, R4 is H, R5 is H, R6 is H, R8 is H, and R9 is H.
21 more elements
Dependencies are inferred from the claim text.