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US 4,732,893 AGranted
Amino-anthracenediones-platinum complexes useful as anticancer compounds
AssigneeBoehringer Biochemia Robin S.p.A.
InventorsAlessandro Pasini, Franco Zunino, Odoardo Tofanetti, Carmelo A. Gandolfi, Sergio Tongnella
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Abstract
Platinum complex having formula (I) cis-[L-(Pt.sup.II XX').sub.m ].(Solv).sub.n (I) wherein m is 1 or 2; X and X', which are the same or different, are Cl, OH, CH.sub.3 SOCH.sub.3.Cl or CH.sub.3 SOCH.sub.3.H.sub.2 O; L is a bidentate ligand of formula II ##STR1## Solv. represents the crystallization solvents and m is zero, 0.5 or an integer from 1 to 6, are described. The compounds I are useful in therapy as antitumoral agents.
Claims14
A cis-platinum complex of formula I
- cis-[L-(Pt.sup.II XX')].(Solv).sub.n (I)
- wherein
- X and X', which can be the same or different, are a ligand selected from the group consisting of Cl, OH, CH.sub.3 SOCH.sub.3.Cl, CH.sub.3 SOCH.sub.3.OH;
- n is zero or 1/2 or an integer from 1 to 6;
- solv represents a crystallization solvent selected from the group consisting of water, a lower C.sub.1 -C.sub.5 alcohol, acetonitrile or ethylacetate and
- L is a bidentate ligand selected from the group of 1,4-diamino-9,10-anthracenedione of formula II ##STR6## wherein each of R.sub.a and R.sub.b, which are the same or different, are hydrogen or hydroxy;
- R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which are the same or different, are hydrogen, C.sub.1 -C.sub.5 lower alkyl or --(CH.sub.2) .sub.p1 --OH;
- p and p.sub.1 are, independently, the integer 2 or 3;
- or at least one of R.sub.1, R.sub.2 and R.sub.3, R.sub.4 respectively, taken together with the nitrogen atom to which they are connected independently forms an hetercyclic ring having the formula ##STR7## wherein Z is --CH.sub.2 -- or O, while p.sub.2 and p.sub.3 are independently 1 or 2, and a salt of said ligand L with pharmaceutically and veterinary acceptable acids;
- wherein the two central nitrogen atoms of the aminoalkylamine side-chains are coordinated with said platinum.sup.II atom.
7 more elements
Process for the preparation of compounds of general Formula I
- cis-[L-(Pt.sup.II XX')].(Solv).sub.n (II)
- wherein
- X and X', which can be the same or different, are a ligand selected from the group consisting of Cl, OH, CH.sub.3 SOCH.sub.3.Cl, CH.sub.3 SOCH.sub.3.OH;
- n is zero or 1/2 or an integer from 1 to 6;
- solv represents a crystallization solvent selected from the group consisting of water, a lower C.sub.1 -C.sub.5 alcohol, acetonitrile or ethylacetate and
- L is a bidentate ligand
- which is a 1,4-diamino-9,10-anthracenedione of Formula II as defined hereinafter,
- characterized in that a bidentate ligand of formula II ##STR8## wherein each of R.sub.a and R.sub.b, which are the same or different, are hydrogen or hydroxy;
- R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which are the same or different, are hydrogen, C.sub.1 -C.sub.5 lower alkyl or --(CH.sub.2).sub.p1 --OH;
- p and p.sub.1 are independently the integer 2 or 3;
- or at least one of R.sub.1, R.sub.2 and R.sub.3, R.sub.4 respectively, taken together with the nitrogen atom to which they are connected independently form a heterocyclic ring having the formula ##STR9## wherein Z is --CH.sub.2 -- or O;
- and p.sub.2 and p.sub.3 are independently 1 or 2;
- is reacted at room temperature with an equal molar amount of a Pt.sup.II compound selected from the group consisting of K.sub.2 PtCl.sub.4 and PtCl.sub.2 CH.sub.3 CN in a suitable solvent selected from the group consisting of water, low molecular weight alcohols, dimethylformamide, acetonitrile and mixtures thereof.
10 more elements
Dependencies are inferred from the claim text.