Virginia Commonwealth University

University of Vermont and State Agricultural College

Hoffmann-la Roche Inc.

Other

F. Hoffmann-la Roche Ag

Boehringer Mannheim Italia, S.p.a.

Setanta Therapeutics, Inc.

Roberto Di Domenico

Nicholas P. Farrell

Ernesto Menta

Silvano Spinelli

Nicholas P Farrell

Mariella Valsecchi

Miles P Hacker

John J McCormack

Carlo Bugatti

Sergio G DeAlmeida

Ulrich Bierbach

Carla Manzotti

James D Hoeschele

Marco Conti

Giovanni Da Re

Ferdinando C Giuliani

Paolo Pavesi

Luisa Del Greco

Erneston Menta

Yun Qu

Fernando Giuliani

Miriam Kloster

John D Roberts

Alexander Hegmans

Trans-platinum compounds comprising carboxylato groups are disclosed, with anti-cancer usefulness. The carboxylato groups participate in solubilizing trans-platinum compounds to which they are attached.

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Pro-drug forms of linear polyamine-bridged platinum compounds and methods for their production and use are provided. The polyamine-bridge portion of the compounds is based on spermine or spermidine, and the central amines of the polyamine-bridge are chemically bonded to labile blocking groups. The presence of the blocking groups serves to minimize the toxicity of the Pt compounds upon administration. Selective removal of the blocking groups and release of the active, unblocked species occurs upon exposure to suitable environmental conditions.

Targeted bisplatinum polyamines as pro-drugs: selective release of platinum

The invention provides a method for enhancing the water solubility of cytotoxic trans-platinum complexes. The present invention also provides a method for killing tumor cells, and a method for the treatment of tumors by the administration of a cytotoxic platinum coordination complex of the general formula SP4-2-&lsqb;PtX(L)(L&prime;)(B)&rsqb; .

Transplatinum complexes as cytotoxic and anticancer agents

The present invention relates to tetra- and penta-nuclear platinum complexes with antitumor activity, to a method for preparing them and to pharmaceutical compositions containing them.

Multinuclear cationic platinum complexes with antitumor activity

The invention provides an improved method for the delivery and stabilization of antisense oligodeoxynucleotides (ODNs) to cells. The unmodified ODNs are complexed to a polynuclear platinum compound or to a structural derivative thereof. Complexation neutralizes the charge of the ODN and makes possible its passage into the cell, without the addition of other transfection agents. The invention may be used in the treatment any disease which is amenable to treatment by antisense ODNs. In addition, the invention provides a new method specifically for the treatment of cancer.

High affinity DNA binding compounds as adjuvants in antisense technology

The present invention relates to treatment of viral infections, such as HIV, with a new class of anti-viral platinum coordination compounds having the general structural formula [PtXA.sub.m B.sub.3-m ] where X is an anionic ligand, A is an acyclic, nitrogen containing monodentate ligand such as amines, ammines, and quinolines, and B is nucleobase.

Platinum complexes with anti-viral activity and method of using same

Bis-platinum complexes with polymethylene derivatives as ligands having

Bis-platinum complexes with polyamine ligands as antitumor agents

Trinuclear cationic platinum complexes having antitumor activity and

The present invention relates to the treatment of tumors with a novel water soluble trans-platinum coordination compound having the general structural formula [PtBX.sub.m (NR*.sub.3)] where B is a planar, heterocyclic ring containing at least one nitrogen atom, and a pendant chelating group; and X is an anionic ligand; and R* is hydrogen or a lower alkyl.

Water soluble transplatinum complexes with anti-cancer activity and

A bis(platinum) complex having the structure: ##STR1## wherein X, Y, Z, X', Y', and Z' are the same or different ligands and are halide, sulphate, phosphate, nitrate, carboxylate, substituted carboxylate, dicarboxylate, substituted dicarboxylate primary or secondary amine, sulfoxide, phosphine, pyridine-type nitrogen and the like; preferably, there is at least one Pt-anion bond on each Pt molecule; and A is a diamine or polyamine. Complexes of trans geometry �PtX.sub.2 (L)(L')! where at least L is a planar ligand such as pyridine but preferably quinoline and L' may be amine, sulfoxide or substituted sulfoxide and X is a chloride, nitrate or carboxylate. A process for obtaining bis(platinum) complexes where the two platinum coordination spheres may contain different ligands in each sphere and where the geometry of each platinum coordination sphere may be the same or different.

Bis-platinum complexes as chemotherapeutic agents

Novel trans-platinum IV complexes which contain heterocycle ligands such as quinoline or isoquinoline, anionic ligands such as halide or sulfate, and which optionally may contain ammonia, or a primary or secondary amine are provided. These complexes have application as pharmaceuticals, in particular as anti-tumor agents.

Trans platinum (IV) complexes

Novel bis(platinum) (IV) complexes coupled via diamine bridging agents are taught as well as methods for their preparation. These complexes are to be used as pharmaceutical agents, e.g., for the treatment of cancer and parasitic diseases.

Bis-platinum (IV) complexes as chemotherapeutic agents

Novel tri(platinum) complexes containing three platinum coordination spheres coupled via diamine or triamine bridging agents are taught as well as methods for their preparation. These complexes are to be used as pharmaceutical agents, e.g., for the treatment of cancer and parasitic diseases.

Tri(platinum) complexes

Growing community of inventors

Richmond, VA, United States of America

Nicholas P Farrell