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US 2021/0332041 A1Published application
Tetrahydropyridopyrimidine derivatives as ahr modulators
AssigneeJaguahr Therapeutics Pte Ltd
InventorsAntonio METE, James HITCHIN, Mark GRAHAM, John KING-UNDERWOOD, Philip Vellacott THORNE
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Abstract
The present disclosure relates to compounds of formula (I), which are suitable as AhR modulators, in particular AhR inhibitors. The disclosure also relates to compositions comprising said compounds and use of said compounds or compositions in treatment, in particular in the treatment of cancer. The disclosure further relates to methods of preparing said compounds.
Claims29
A compound of formula (I)
- wherein:
- Y is a 5 or 6 membered ring optionally comprising 1, 2, or 3 heteroatoms selected from N, O and S, substituted with R5 and R6;
- R1 is H, C1-3 alkyl, (—CH2)pCN, —COC1-3 alkyl, —CO(CH2)qNR7R8, —SO2C1-3 alkyl,
- —SO2NR7R8, —(CH2)qPh, −, —C(O)Z;
- R2 is H or C1-3 alkyl;
- R3 is H or C1-3 alkyl;
- R4 is a-9 or 10 membered heteroaryl with at least one heteroatom selected from N, O or S (Indol-3-yl or Benzimidazol-2-yl), with substituents R9 and R10;
- R5 is H, hydroxy, halogen (such as F, Cl), CN or a C1-3 alkyl group, —CO(CH2)qNR7R8,
- —SO2C1-3 alkyl, —SO2NR7R8;
- R6 is hydroxy, halogen (such as F, Cl), CN or a C1-3 alkyl group, —CO(CH2)qNR7R8,
- —SO2C1-3 alkyl, —SO2NR7R8;
- R7 is H or C1-3 alkyl, such as —CH3;
- R8 is H or C1-3 alkyl, such as —CH3;
- R9 is H, hydroxy, halogen (such as F, Cl), CN or a C1-3 alkyl group, —CO(CH2)q NR7R8,
- —SO2C1-3 alkyl, —SO2NR7R8,
- R10 is H, hydroxy, halogen (such as F, Cl), CN or a C1-3 alkyl group, —CO(CH2)q NR7R8,
- —SO2C1-3 alkyl, —SO2NR7R8;
- R11 is H or C1-3 alkyl, such as —CH3;
- X is NR11 or O;
- Z is a 5 or 6 membered heteroaryl (i.e. with at least one heteroatom selected from N, O and S, for example 1 or 2 nitrogens) optionally bears one or two substituents selected from hydroxy, halogen (such as F, Cl), CN, C1-3 alkyl;
- b is an integer 1 or 2;
- n is an integer 1 or 2;
- m is an integer 1 or 2;
- p is an integer 1, 2 or 3;
- q is 0, 1, 2 or 3,
- or a pharmaceutically acceptable salt thereof.
23 more elements
A compound of formula (II)
- wherein X, R1, R2, R3, R4, R5, R6, b, n and m are defined above for compounds of formula (I) or a pharmaceutically acceptable salt thereof.
A compound of formula (III):
- or a pharmaceutically acceptable salt thereof, wherein X, R1, R2, R3, R4, R5, R6, b, n and m are defined above for compounds of formula (I).
(canceled)
Dependencies are inferred from the claim text.