| abstract |
Compounds of formula (I) are CRTH2 antagonists, useful in the treatment of inflammatory, autoimmune, respiratory or allergy disease: wherein X1 is -S-, -O-, -N=N-. -NR5-, -CR5=CR6-, -CR5=N-, wherein R5 and R6 are independently hydrogen or C1-C3 alkyl; R1 is hydrogen or C1-C3 alkyl or cyclopropyl; R2 is an optionally substituted phenyl or 5- or 6-membered monocyclic heteroaryl ring; R3 is an optionally substituted carbocyclic ring of 3 to 7 ring atoms, or an optionally substituted 4-, 5- or 6-membered monocyclic heterocyclic ring; R4 is a group other than hydrogen, methyl or ethyl of formula Q-[Alk1]m-[X]n-[Alk2]p-[Z}s- wherein m, n p, and s are independently 0 or 1 ; Q is hydrogen or an optionally substituted 4-, 5- or 6-membered monocyclic heterocyclic ring; Alk1 and Alk2 are independently optionally substituted C1-C3 alkylene radicals; X is -O-, -S-, -C(=O)-, - S(=O)-, -S(=O)2-, -CH(R7)-, -N(R7)-, or, in either orientation -SO2N(R7)- or - C(=O)N(R7)-, wherein R7 is hydrogen, or R7 represents a C2-C4 bridge between the C or N atom of X to which it is attached and a carbon atom of Alk2 and Z is -CH2, - C(=O) or -S(=O)2. |