| abstract |
This refers to immunosuppressive compounds and compositions, process for their production, their uses, and pharmaceutical compositions containing them, compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, in particular diseases associated with signal transduction mediated by the EDG receptor. Claim 1: A compound of the formula (1) wherein: n is selected from 0, 1, and 2; m is selected from 1, 2 and 3; R1 is selected from C6-10 aryl and C5-10 heteroaryl, wherein any aryl or heteroaryl and R1 is optionally substituted by a radical selected from C6-10 aryl-C0-4 alkyl, C5-6-C0- heteroaryl 4, C3-8 cycloalkyl-C0-4 alkyl, C3-8 heterocycloalkyl-C0-4 alkyl, or C1-10 alkyl, wherein any aryl, heteroaryl, cycloalkyl or heterocycloalkyl group of R1 may be optionally substituted by 1 to 5 radicals selected from halogen, C1-10 alkyl, C1-10 alkoxy, C1-10 alkyl substituted by halogen, and C1-10 alkoxy substituted by halogen; and any alkyl group of R1 may optionally have a methylene replaced by an atom or group selected from -S-, -S (O) -, -S (O) 2-, -NR7-, and -O-; wherein R7 is selected from H and C1-6 alkyl; R2, R3, R4 and R5 are independently selected from H, halogen, hydroxyl, C1-10 alkyl, C1-10 alkoxy, C1-10 alkyl substituted by halogen, and C1-10 alkoxy substituted by halogen; A is selected from -X1C (O) OR7; -X1P (O) (R7) OR7, and 1H-tetrazol-5-yl; wherein X1 is selected from a bond, C1-3 alkylene, and C2-3 alkenylene, and R7 is selected from H and C1-6 alkyl; B is CR8R9; wherein R8 and R9 are independently selected from H, hydroxyl, C1-10 alkyl, C1-10 alkoxy, C1-10 alkyl substituted by halogen, and C1-10 alkoxy substituted by halogen; E is selected from CR8 or N; wherein R8 is selected from H, hydroxyl, C1-10 alkyl, C1-10 alkoxy, C1-10 alkyl substituted by halogen, and C1-10 alkoxy substituted by halogen; or B is CR9 and E is C, and B and E are connected via a double link; X is a link or is selected from X1OX2-, -X1NR7X2-, -X1C (O) NR7X2-, -X1NR7C (O) X2-, -X1S (O) X2-, -X1S (O) 2X2-, - X1SX2-, C4-6 heteroarylene, and -X1ON = C (R7) X2-; wherein X1 and X2 are independently selected from a bond, C1-3 alkylene, and C2-3 alkenylene; R7 is selected from H and C1-6 alkyl, and any heteroarylene of X is optionally substituted by a member of the group selected from halogen and C1-6 alkyl; Y is selected from C6-10 aryl and C5-10 heteroaryl, wherein any aryl or heteroaryl of Y may be optionally substituted with 1 to 3 radicals selected from halogen, hydroxyl, nitro, C1-10 alkyl, C1 alkoxy -10, C1-10 alkyl substituted by halogen, and C1-0 alkoxy substituted by halogen; and pharmaceutically acceptable salts, hydrates, solvates, isomers and prodrugs thereof. |