Abstract: Compounds according to formula I in which formula R1 and R2, which may be the same or different, represent halogen, (C1-C6)hydrocarbyl, optionally substituted with one or two hydroxyl group or one or more fluorine atoms, or, together with the carbon atom to which they are both attached, R1 and R2 form a (C3-C6)carbocyclic ring, or one of R1 and R2 taken together with R3 forms a direct bond, such that a triple bond is constituted, or R1 and R2 represent both hydrogen; R3 when not forming a direct bond with one of R1 and R2 represents hydrogen or (C1-C3)hydrocarbyl; X represents (E)-ethylene, (Z)-ethylene, ethynylene, or a bond; Y and Z independently represent hydrogen or methyl; and prodrugs and stereo isomeric forms thereof are provided together with their use in therapy, and their use in the manufacture of medicaments.

Abstract: Pyridyl cyanoguanidine compounds of the general formula I wherein A, X1, X2, X3, Y1, Y2, Y3, R1, R2, R5, R6 and n are as indicated in the description are suitable as prodrugs in human and veterinary therapy of proliferative diseases such as cancers.

Abstract: Compounds of the formula I wherein X represents hydrogen or hydroxy; Y represents oxygen or sulphur or oxidized sulphur selected from the groups S(O) and S(O2); R1 and R2, which may be the same or different, represent hydrogen or a residue after removal of 1 hydrogen atom from a straight, branched or cyclic, saturated or unsaturated, C1–C6-hydrocarbon; or R1 and R2, together with the carbon atom to which they are attached (marked with an asterisk in formula I), bearing the group X, form a C3–C8 carbocyclic ring; Q represents a diradical residue after removal of 2 hydrogen atoms from a straight, branched or cyclic, saturated or unsaturated C1–C8-hydrocarbon; and R3 represents hydrogen or a residue after removal of 1 hydrogen atom from a straight, branched or cyclic, saturated or unsaturated C1–C6-hydrocarbon; may be used for the preparation of a medicament for the treatment and/or prophylaxis of osteoporosis and related bone disorders.

Abstract: Compounds of the formula (I) wherein X represents hydrogen or hydroxy; Y represents oxygen or sulphur or oxidized sulphur selected from the groups S(O) and S(O2); R1 and R2, which may be the same or different, represent hydrogen or a residue after removal of 1 hydrogen atom from a straight, branched or cyclic, saturated or unsaturated, C1-C6-hydrocarbon; or R1 and R?2, together with the carbon atom to which they are attached (marked with an asterisk in formula (I)), bearing the group X, form a C3-C8 carbocyclic ring; Q represents a diradical residue after removal of 2 hydrogen atoms from a straight, branched or cyclic, saturated or unsaturated C1-C8-hydrocarbon; R3 represents hydrogen or a residue after removal of 1 hydrogen atom from a straight, branched or cyclic, saturated or unsaturated C1-C6-hydrocarbon; R1, R2 and/or Q is optionally substituted with one or more deuterium or fluorine atoms; and n is 0 or 1; and derivatives of the compounds of formula (I) in which one or more hydroxy groups have bee

Abstract: The present invention relates to pivaloyloxymethyl D(-)-.alpha.-aminobenzylpenicillinate of the formula I in a novel and improved form, i.e. the crystalline form ##SPC1##To methods of producing said crystalline pivaloyloxymethyl D(-)-.alpha.-aminobenzylpenicillinate and to pharmaceutical preparations containing said crystalline pivaloyloxymethyl D(-)-.alpha.-aminobenzylpenicillinate.Crystalline pivaloyloxymethyl D(-)-.alpha.-aminobenzylpenicillinate has no bitter taste, is only slightly soluble in water, and is stable and readily absorbable.