Abstract: Substrate-spacer-prodrug compounds (pro-prodrugs) suited for site specific delivery of drugs, a process of preparing them and their use are described.

Abstract: Enzymatically clearable prodrugs with reduced Michaelis-Menten constant (Km) are described.

Abstract: Organic nitrates, processes for their preparation and their use in the treatment of vascular diseases and in particular in the treatment of angina.The said nitrates correspond to the following formula I:R--CO--(A).sub.n --Y--B (I)in which:R represents, in particular, a sulphur-containing radical and a sulphur-containing amino acid residue; A represents, in particular, a CH.sub.2 group or a substituted amino acid; n is 0 or 1 or greater than 1; Y represents an oxygen atom or an NH group and B represents, in particular, a 1,4:3,6-dianhydro hexitol mononitrate radical, an itol nitrate radical or an inositol radical.The said organic nitrates are prepared by reacting:I. either a thio acid of the type R--COOH, in which R has the same meaning as above, with a derivative of formula II: (A).sub.n --Y--B, in which A, Y, B and n have the same meaning as above,II. or a derivative of formula III: R--CO--(A).sub.

Abstract: Glycosylated prodrugs, a preparation method therefor, and their use with tumor-specific immunoenzymatic conjugates for the treatment of cancer, are described. These anthracycline prodrugs have formula (I).

Abstract: The present invention relates to new anthracyclines corresponding to the general formula I below: ##STR1## in which R' and R", which may be identical or different, denote a hydrogen atom (and in this case R' is different from R") or the group --(CH.sub.2).sub.n --R.sub.1 --(CH.sub.2).sub.m --R.sub.2 where n is between 1 and 6,m is between 0 and 4 (with the proviso, of course, that if m=0, R.sub.2 is nonexistent)R.sub.1 denotes one of the following groups: ##STR2## (in this case, m=0) ##STR3## (in this case m=0) where R.sub.3 and R.sub.4, which may be identical or different, denote a hydrogen atom or a substituted or unsubstituted alkyl group)--C.tbd.N (in this case m=0)--S----O--(with the proviso that m is other than 0) ##STR4## (m=0 and R.sub.3 R.sub.4 have the same meaning as above) and R.sub.2 denotes (in the case where m is other than 0) a hydrogen atom or alkyl or alkoxy groups or ##STR5## (R.sub.3 and R.sub.4 having the same meaning as above).

Abstract: New drugs comprising 2,3- or 3,4-diphenyl derivatives of .gamma.-nitrile-esters or the products of cyclization of the 2,3-diphenyl derivatives according to the formulae A, B and C are claimed.Process for cyclization of 2,3-diphenyl derivatives of .gamma.-nitrile-esters, new 2,3-diphenyl derivatives of .gamma.-nitrile-esters corresponding to the formulae I to VIII are claimed; new 3,4-diphenyl derivatives of the said esters coresponding to the formulae IX and X, and new 3,4-diphenylpiperidone derivatives corresponding to the specific formulae IX to XXVII are described.

Abstract: The present invention relates to new aglycons which correspond to the general formula: ##STR1## in which: R.sub.1, R.sub.2, R.sub.3 and R.sub.5, which can be identical or different, represent a hydrogen atom or a group OH, OMetal or OR.sub.4, R.sub.4 being a substituted or unsubstituted C.sub.1 to C.sub.6 alkyl group,R represents a hydrogen atom or a group COCH.sub.2 R', R' being hydrogen or an alkyl, hydroxyl, alkoxy or aryl group,R.sub.6 and R.sub.7, which are always different, represent either a hydrogen atom or an OH group, andR.sub.8 represents a hydrogen atom or the group CH.sub.3 CO--.Application to the preparation of antibiotics and antitumoral agents.

Abstract: Halogen derivatives of 8-hydroxycarboxylic acids, which correspond to the formula ##STR1## (open form, in a basic medium) or to the formula ##STR2## (cyclized form, in an acid medium) in which formulae: X.sub.1 and X.sub.2 are halogen atoms, n.sub.1 and n.sub.2 are integers between 0 and 5, but, if n.sub.1 =0, n.sub.2 is different from 0, and vice versa, R is a hydrogen atom or an alkyl or aryl group, and Cation represents an ion originating from a base, or a metal ion, which is pharmaceutically compatible are suitable as antidepressants having a psychostimulant action.