Macrolides with antibacterial activity
AssigneeBAsilea Parmaceutica AG
InventorsPeter Angehrn, Daniel Hunziker, Pierre-Charles Wyss
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Abstract
The invention provides new macrolides antibiotics of formula (I) with improved biological properties and improved stability formula (I): wherein R1 is hydrogen, cyano, —S(L)mR2, —S(O)(L)mR2, or —S(O)2(L)mR2; L represents —(CH2)n— or —(CH2)nZ(CH2)n′—-; m is 0 or 1; n is 1, 2, 3, or 4; n′ is 0, 1, 2, 3, or 4; Z is O, S or NH; R2 is hydrogen, alkyl, heterocyclyl or aryl; which heterocyclyl and the aryl groups may be further substituted; * indicates a chiral center which is in the (R) or (S) form and pharmaceutically acceptable acid addition salts or in vivo cleavable esters thereof. 1
Claims20
Macrolide antibiotics of formula I
- 46
- wherein
- R1 is hydrogen, cyano, —S(L)mR2, —S(O)(L)mR2, or —S(O)2(L)mR2;
- L represents —(CH2)n— or —(CH2)nZ(CH2)n′—;
- m is 0 or 1;
- n is 1, 2, 3, or 4;
- n′ is 0, 1, 2, 3, or4;
- Z is O, S or NH;
- R2 is hydrogen, alkyl, heterocyclyl or aryl;
- which heterocyclyl and the aryl groups may be further substituted;
- * indicates a chiral center which is in the (R) or (S) form.
- and pharmaceutically acceptable acid addition salts or in vivo cleavable esters thereof.
The invention as herein described.
Dependencies are inferred from the claim text.