| abstract |
Claim 1: A compound of the formula (1) characterized in that M represents a macrolide subunit; D represents a non-steroid subunit; L is a contactor molecule to which one of M and D are covalently bound; and pharmaceutically acceptable salts and solvates thereof and individual diastereoisomers thereof. Claim 31: Process for the preparation of the compound of the formula (1) of claim 1, characterized in that it comprises (1), which comprises: (a) for a compound of the formula (1), wherein X2 is -NHC (O) -, reacting a compound of the formula (2), wherein L1 represents an exit group, and a free amino group of a macrolide represented by the formula (3); (b) for a compound of the formula (1), wherein X2 is -OC (O) -, to react a compound of the formula V and the free hydroxyl group of a macrolide represented by the formula (4); (c) for a compound of the formula (1), wherein X1 is -OC (O) -, Q is -NH- and X2 is -NHC (O) -, to react a macrolide represented by the formula (5) and a free amino group of the compound represented by the formula (6); (d) for a compound of the formula (1), wherein X1 is -OC (O) NH- and X2 is -NHC (O) -, to react a macrolide represented by the formula (7) and a free amino group of the compound represented by the formula (8); (e) for a compound of the formula (1), wherein X1 is -CH2-, Q is -NH- and X2 is -NHC (O) -, to react a macrolide represented by the formula (9) and a compound of the formula (2); (f) for a compound of the formula (1) reacting a macrolide represented by the formula (10) or by formula (11) p per formula (12) having a starting group L2, with a free carboxylic acid of a non-steroidal anti-inflammatory subunit. |