Abstract: A compound of formula (I) wherein n is 0 to 4; m is 0 or 1 with the proviso that the sulphur atom and R3 are in vicinal position (if m=0 then R3 is in position 2?, and if m=1 then R3 is on position 1?); R is ethyl or vinyl; R1 is hydrogen or (C1-6)alkyl, R2 is hydrogen or (C3-6)cycloalkyl, or unsubstituted (C1-6)alkyl, or (C1-6)alkyl substituted by one or more of hydroxy; preferably one or two, methoxy, halogen, (C3-6)cycloalkyl, or R1 and R2 together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring containing at least 1 nitrogen atom or 1 nitrogen and 1 additional heteroatom e. g.

Abstract: A compound selected from 14-O-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-sulfanyl)-acetyl]-12-epi-mutilins, or 14-O-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-oxy)-acetyl]-12-epi-mutilins, wherein 12-epi-mutilin is characterized in that the mutilin ring at position 12 is substituted by two substituents, the first substituent at position 12 of the mutilin ring is a methyl group which methyl group has the inverse stereochemistry compared with the stereochemistry of the methyl group at position 12 of the naturally occurring pleuromutilin ring, the second substituent at position 12 of the mutilin ring is a hydrocarbon group comprising at least one nitrogen atom and all other substituents of the mutilin ring having the same stereochemistry compared with the stereochemistry of the substituents at the corresponding positions in the naturally occurring pleuromutilin ring; optionally in the form of a salt and/or solvate, wherein the naturally occurring pleuromutilin is of

Abstract: A compound selected from 14-O-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-sulfanyl)-acetyl]-12-epi-mutilins, or 14-O-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-oxy)-acetyl]-12-epi-mutilins, wherein 12-epi-mutilin is characterized in that the mutilin ring at position 12 is substituted by two substituents, the first substituent at position 12 of the mutilin ring is a methyl group which methyl group has the inverse stereochemistry compared with the stereochemistry of the methyl group at position 12 of the naturally occurring pleuromutilin ring, the second substituent at position 12 of the mutilin ring is a hydrocarbon group comprising at least one nitrogen atom and all other substituents of the mutilin ring having the same stereochemistry compared with the stereochemistry of the substituents at the corresponding positions in the naturally occurring pleuromutilin ring; optionally in the form of a salt and/or solvate, wherein the naturally occurring pleuromutilin is of

Abstract: The present invention relates to novel 9a-substituted azalides having antimalarial activity. More particularly, the invention relates to 9a-substituted 9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A, 3-O-decladinosyl-9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A and 3-O-decladinosyl-5-O-dedesosaminyl-9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A compounds having antimalarial activity, to the method of preparation, to the method of use, and to pharmaceutically acceptable derivatives thereof having antimalarial activity.

Abstract: 9a-carbamoyl and thiocarbamoyl azalides A and their pharmaceutically acceptable derivatives are useful for treatment and prevention of malaria.

Abstract: Novel 9a-N?-substituted-carbamoyl- and thiocarbamoyl-aminoalkyl-9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A and 3-O-decladinosyl-9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A compounds having antimalarial activity are claimed. More particularly, the invention relates to 9a-N?-substituted-carbamoyl- and thiocarbamoyl-?-aminoethyl- or -?-aminopropyl-9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A and 3-O-decladinosyl-9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A compounds and to pharmaceutically acceptable derivatives thereof having antimalarial activity.

Abstract: 9a-Carbamoyl-?-aminopropyl- and 9a-thiocarbamoyl-?-aminopropyl-azalides and their pharmaceutically acceptable derivatives are useful for treatment and prevention of malaria.

Abstract: Disclosed are a novel class of components obtained in reactions of condensation of hydroxycoumarin derivatives with aromatic and aliphatic dialdehydes, their preparation and antiviral action thereof, such as against HIV.

Abstract: The present invention relates to novel hydroxy and polyhydroxy derivatives of coumarin fused with dialdehydes and aldehyde acids of the general formulae I, II, III and IV: ##STR1## wherein R.sup.1 =R.sup.2 =4-hydroxycoumarin;R.sup.1 =R.sup.2 =4,7-dihydroxycoumarin;R.sup.1 =R.sup.2 =4,5,7-trihydroxycoumarin;R.sup.1 =4-hydroxycoumarin, R.sup.2 =--CH(OH)CH.sub.3.An object of the invention are also processes for the preparation of hydroxy and polyhydroxy derivatives of coumarin fused with dialdehydes and aldehyde acids, and the antiviral action thereof.Novel hydroxy and polyhydroxy derivatives of coumarin according to the present invention exhibit antiviral action against HIV-1 virus.

Abstract: The present invention relates to novel coumarin quinolone carboxylic acids wherein the pyridone system is fused in 3,4-, 6,7- and 7,8-positions of the coumarin system, of the general formula I ##STR1## wherein R.sup.1 R.sup.2 =--NHCH=C(CO.sub.2 R.sup.6)CO, R.sup.3 =NO.sub.2 or NH.sub.2, R.sup.4 =R.sup.5 =H, R.sup.6 =H or C.sub.2 H.sub.5 ;R.sup.1 R.sup.2 =--NHCH=C(CO.sub.2 R.sup.6)CO, R.sup.3 =R.sup.4 =H, R.sup.5 =F, R.sup.6 =H or C.sub.2 H.sub.5 ;R.sup.1 R.sup.2 =--CO(CO.sub.2 R.sup.6)C=CHNH, R.sup.3 =R.sup.4 =R.sup.5 =H, R.sup.6 =H or C.sub.2 H.sub.5 ;R.sup.1 R.sup.2 =R.sup.3 R.sup.4 =--NHCH=C(CO.sub.2 R.sup.6)CO, R.sup.5 =H, R.sup.6 =H or C.sub.2 H.sub.5 ;R.sup.1 =H or OH, R.sup.2 =R.sup.5 =H, R.sup.3 R.sup.4 =--NHCH (CO.sub.2 R.sup.6)CO, R.sup.6 =H or C.sub.2 H.sub.5 ;R.sup.1 =OH, R.sup.2 =R.sup.3 =H, R.sup.4 R.sup.5 =--CO(CO.sub.2 R.sup.6) C=CHNH, R.sup.6 =H or C.sub.2 H.sub.5 ;R.sup.1 =R.sup.5 =H, R.sup.2 =CH.sub.3 or CF.sub.3, R.sup.3 R.sup.4 =--CO(CO.sub.2 R.sup.6)C=CHNH, R.sup.6 =H or C.sub.2 H.sub.

Abstract: The present invention relates to new coumarin derivatives represented by the general formula I ##STR1## wherein R.sup.1 =NH.sub.2 or --NHCH.dbd.C(CO.sub.2 C.sub.2 H.sub.5).sub.2, R.sup.2 =R.sup.3 =R.sup.4 =H, R.sup.5 =F,R.sup.1 =R.sup.3 =NHCH.dbd.C(CO.sub.2 C.sub.2 H.sub.5).sub.2, R.sup.2 =R.sup.4 =R.sup.5 =H,R.sup.1 =H or OH, R.sup.3 =NHCH.dbd.C(CO.sub.2 C.sub.2 H.sub.5).sub.2, R.sup.2 =R.sup.4 =R.sup.5 =H,R.sup.1 =OH, R.sup.2 =R.sup.3 =R.sup.4 =H, R.sup.5 =--NHCH.dbd.C(CO.sub.2 C.sub.2 H.sub.5).sub.2,R.sup.1 =R.sup.3 =R.sup.5 =H, R.sup.2 =CH.sub.3 or CF.sub.3, R.sup.4 =--NHCH.dbd.C(CO.sub.2 C.sub.2 H.sub.5).sub.2,processes for the preparation thereof and their use as intermediates for the synthesis of new coumarin derivatives with potential biological action.