C - Chemistry – Metallurgy – 07 – F
Patent
C - Chemistry, Metallurgy
07
F
167/119, 260/429
C07F 15/00 (2006.01) A61K 31/28 (2006.01)
Patent
CA 2017741
ABSTRACT OF THE DISCLOSURE Platinum (II) antitumor agents of the general formula: Image Y wherein A1 and A2 are the same or different and are selected from ammonia or a monodentate amine and substituted monodentate amines, or A1 and A2 together are a diamine represented by the general formula: Image wherein R2 and R3 are the same or different and are each selected from hydrogen, linear or branched C1-C6 alkyl and substituted linear or branched C1-C6 alkyl wherein the substituents are selected from hydroxy, C1-C4 alkoxy, halo, carboxy, C1-C4 alkylcarboxy or C1-C4 alkoxylcarbonyl, or R2 and R3, taken together, form a 1,2-diaminocycloalkane containing 4-8 nuclear carbon atoms or a substituted 1,2-diaminocycloalkane wherein the substituents are selected from linear or branched C1-C6 alkyl groups, hydroxy, C1-C4 alkoxy, halo, carboxy, C1-C4 alkylcarboxy or C1-C4 alkoxylcarbonyl; wherein L is aniline or aniline substituted with one or more of C1-C6 linear or branched alkyl, hydroxy, C1-C4 alkoxy, halo, carboxy, cyano, isocyano, phenyl, nitro, C1-C4 alkylcarboxy or C1-C4 alkoxylcarbonyl; wherein X is a monodentate anionic ligand and wherein Y is an anion. Members of this class of compounds have demonstrated activity in a number of in vivo antitumor screens. The platinum-triamine complexes are typically cationic species and as such possess desirable physical properties which include high stability and solubility in aqueous media.
Amundsen Alan R.
Gramiccioni Gary A.
Hollis Leslie S.
Stern Eric W.
Amundsen Alan R.
Engelhard Corporation
Gramiccioni Gary A.
Hollis Leslie S.
Sim & Mcburney
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