N-SUBSTITUIERTE THIAZOLYLDERIVATE DER 7-AMINO-CEPHALSOSPORANSAEURE, VERFAHREN ZU IHRER HERSTELLUNG UND SIE ENTHALTENDE PHARMAZEUTISCHE UND VETERINAERMEDIZINISCHE MITTEL
Compounds of general formula (I> wherein A is wherein R2 represents a hydrogen atom or a free or protected hydroxy group; R is 1) -OR3 in which R3 is hydrogen or a branched or straight chain saturated or unsaturated C1-C6 aliphatic hydrocarbon group which is unsubstituted or substituted by one or...
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Zusammenfassung: | Compounds of general formula (I> wherein A is wherein R2 represents a hydrogen atom or a free or protected hydroxy group; R is 1) -OR3 in which R3 is hydrogen or a branched or straight chain saturated or unsaturated C1-C6 aliphatic hydrocarbon group which is unsubstituted or substituted by one or more substituents selected from a) cyano, b) -COOR' in which R' is hydrogen, C1-C6-alkyl or a carboxy-protecting group; in which each of the groups R4 and R5, which may be the same or different, represents a hydrogen atom, a C1-C6 alkyl or a C2-C6 aliphatic acyl group, or, when R4 is hydrogen, R5 may be also an amino-protecting group; or wherein R4 and R5 are as defined above; R1 is hydrogen or an amino- protecting group; n is zero, 1 or 2; Y is a') hydrogen; b') halogen; c') hydroxy; d') C1-C6-alkoxy; e') C1-C6 alkyl; f') -CH2OCOCH3; g') a group where R'' may be hydrogen, C1-C6 alkyl, carboxy, cyano or carbamoyl; h') a group -CH2-S-Het, wherein Het represents 1) a pentatomic or hexatomic heteromonocyclic ring containing at least one double bond and at least one heteroatom selected from N, S and O, which ring may be unsubstituted or substituted by one or more substituents selected from: a'') hydroxy, C1-C6 alkoxy, halogen, C2-C6 aliphatic acyl; b'') C1-C6 alkyl unsubstituted or substituted by one or more substituents selected from hydroxy and halogen; c'') C2-C6 alkenyl unsubstituted or substituted by one or more substituents selected from hydroxy and halogen; d'') -S-R6 wherein R6 is hydrogen or C1-C6 alkyl -S- CH2COOR' wherein R' is as defined above; e'') -(CH2)m-COOR', -CH=CH-COOR', -(CH2)m- CONH2 or -(CH2)m-CN wherein m is zero, 1, 2 or 3 and R' is as defined above; f'') (CH2)mSO3H wherein m is as defined above; or g''> wherein m, R4 and R5 are as defined above; or 2) a heterobicyclic ring containing at least two double bonds wherein each of the condensed heteromonocyclic rings thereof is the same or different pentatomic or hexatomic heteromonocyclic ring containing at least a heteroatom selected from N, S and O, the heterobicyclic ring being unsubstituted or substituted by one or more substituents selected from a''), b''), c''), d''), e''), f'') and g'') defined above; X is a free or esterified carboxy group; provided that when A is a -CH2- group, R is not -OH; and the pharmaceutically and veterinarily acceptable salts of compounds of general formula (I) are useful antibacterial agents for treatment of humans and animals. |
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