| 摘要 |
<p>Ar1Ar2XC(R1R2)C(=O)N(R3)Ar3Ar4 (I) Compounds of structure I for modulating WNT activity wherein Ar1, Ar2, Ar3 and Ar4 are independently, optionally substituted aryl or heteroaryl groups; R1 and R3 are independently H or an optionally substituted alkyl; R2 is H or an optionally alkyl or alkylene group which, together with the carbon atom to which it is attached and X, forms a non-aromatic ring or an alkylene group which, together with the carbon atom to which it is attached and X and two adjacent atoms of Ar2, forms a non-aromatic ring; X is O, CR4R5, CH2O, N or NR4, wherein if X is N it is bonded to R2; R4 is H, optionally substituted alkyl or alkylene chain, optionally containing a heteroatom and/or a carbonyl group, which together with the C or N to which it is attached and two adjacent atoms of Ar2, forms a non-aromatic ring; and R5 is H, NH2 or an optionally substituted alkyl. Processes for the preparation of compounds of structure I are also provided. Preferably the compounds are for use in treating a condition characterised by excessive WNT activity, wherein the condition is a cancer, or a fibrotic disease or stem cell or diabetic retinopathy or a degenerative disease.</p> |
