Patent ID: 8410065
Filing Date: 2013-04-02
Classification: A61P,C07H

Abstract:
1. Macrolide compound of formula I: wherein R1 is a residue -Y-X-Q; Y is S, SO or SO X is a bond or a linear group consisting of hydrogen atoms and 1 to 9 atoms selected from C, N, O and S, of which up to 2 atoms can be N and one atom can be O or S, one carbon atom can appear as a CO group and the sulphur atom can appear as an SO Q is a residue —V-A1-L-A2-W or, if X does not represent a bond, may also be —NR10R11 V is an optionally substituted divalent aromatic or heterocyclic group; W is optionally substituted aryl or heterocyclyl; A1 and A2 are, independently of each other, either absent or a C L is —O—, —S—, —SO R2 is OR2a or R2a is hydrogen, acetyl, —(C═O)CH R2b and R2c independently of each other, are hydrogen or C1-C6 alkyl which can be substituted or unsubstituted and wherein up to two atoms can be N, O or S and one carbon atom can appear as C═O or, taken together with the nitrogen atom to which they are linked, form a 4-7 membered-ring of which up to two atoms can be N, O or S and one carbon can appear as C═O; R3 is hydrogen or R2 and R3 taken together with the carbon atom to which they are linked, represent a C═O group; R4 is hydrogen or R2 and R4 taken together with the bond between the carbon atoms to which they are linked, represent a double bond between said carbon atoms; Z is R5 is hydrogen or —OR5a or —NR5bR5c; R6 is hydrogen or —OR6a or —NR6bR6c; or R5 and R6 taken together with the carbon atom to which they are linked, represent a C═O group; R7 is hydrogen or —OR7a or —NR7bR7c; R8 is hydrogen or —OR8a or —NR8bR8c; or R7 and R8 taken together with the carbon atom to which they are linked, represent a C═O group; or one of R5 and R6 taken together with one of R7 and R8 represent a group of formula —NR56(CO)O— or —O(CO)NR78— R9 is hydrogen or R8 and R9 taken together with the bond between the carbon atoms to which they are linked, represent a double bond between said carbon atoms; R5a, R7a and R8a, independently of each other, are hydrogen or C1-C6 alkyl which can be substituted or unsubstituted and wherein one or more single bonds can be replaced by double and/or triple bonds and where one carbon atom can appear as C═O and up to two atoms can be N, O or S; R6a is hydrogen or C1-C6 alkyl; R56 and R78 are hydrogen or C1-C6 alkyl; R5b, R5c, R6b, R6c, R7b, R7c, R8b and R8c independently of one another, are hydrogen, C1-C6alkyl which can be substituted or unsubstituted and up to two atoms can be N, O or S and where one carbon atom can appear as C═O, or —(C═O)heterocyclyl or, taken together with the nitrogen atom to which they are linked, form a 4-7 membered-ring of which up to two atoms can be N, O or S and one carbon can appear as C═O; R10 and R11 are independently selected from optionally substituted groups selected from aryl; aralkyl; heterocyclyl and heterocyclylalkyl; groups, and one of R10 and R11 can also be a group -L-A2-W; and * indicates a chiral centre which is in the (R) or (S) form; provided that Z is not a group of formula or an acid addition salt, a N-oxide or an in vivo cleavable ester thereof.