AZALIDAS DE 13 MIEMBROS

• Main Authors: BERTINATO PETER, BLIZE ALAN ELWOOD, MORTON BARRY JAMES, DIRLAM JOHN PHILIP, ZIEGLER CARL BERNARD, RAFKA ROBERT JOHN, RAGAN COLMAN BRENDAN
• Format: Patent
• Language: Spanish
• Published: 14.12.2000
• Edition: 7
• Subjects: CHEMISTRY; DERIVATIVES THEREOF; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; NUCLEIC ACIDS; NUCLEOSIDES; NUCLEOTIDES; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; SUGARS

SE REFIERE A COMPUESTOS DERIVADOS DE AZALIDAS DE FORMULA I, DONDE: R1 ES CH3-CH2-CH(OH)-C(CH3)(OH)-, ACETILO, 3-N,N-DIMETILAMINO-2-PROPENOILO, 1-N-METIL-5-PIRAZOLILO, 3-PIRAZOLILO, 1-METIL-N-3-PIRAZOLILO, 1-N-BENCIL-3-PIRAZOLILO, 1-N-(3HIDROXIBENCIL)-3-PIRAZOLILO, 3-ISOXAZOLILO, ENTRE OTROS; R2 ES H, ALQUILO C1-C4; R3 ES H, ALQUILO C1-C10, ALQUENILO C2-C10, ALQUINILO C2-C10, -(CH2)m(ARILO C6-C10), -(CH2)m(HETEROCICLO C6-C10), ENTRE OTROS; m ES 0-4; R4 ES H, -(CH2)m(ARILO C6-C10) O (CH2)m(HETEROCICLO C6-C10) OPCIONALMENTE SUSTITUIDO CON HALO, CIANO, NITRO, TRIFLUOROMETIL, AZIDO, ENTRE OTROS; R6 ES H, METILO; R7 ES H, ALQUILO C1-C20, ALQUENILO C2-C20, ALQUINILO C2-C20, -C(O)-ALQUILO C1-C20, ENTRE OTROS; R8 ES H, METILO, R9 ES GRUPO a, 4"-OXOCLADINOSILO; R12 ES ALQUILO C1-C10, ALQUENILO C2-C10, ALQUINILO C2-C10, CIANO, -CH2S(O)p-ALQUILO C1-C10, -CH2S(O)pALQUENILO C2-C10, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO PARA LA PREPARACION Y A COMPUESTOS INTERMEDIOS. LOS COMPUESTOS DE FORMULA I SON MACROLIDOS Y TIENEN ACTIVIDAD CONTRA LAS BACTERIAS Y PROTOZOARIOS The invention relates to a method of preparing compounds of the formula 1and to pharmaceutically acceptable salts thereof. The compounds of formula 1 are antibacterial agents that may be used to treat various bacterial and protozoa infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial protozoa infections by administering the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1 and to intermediates useful in such preparation.