Abstract: The present invention concerns the use of methods and compositions for the treatment of cancer and other hyperproliferative diseases. In certain embodiments, methods are described for the treatment of cancer and/or hyperproliferative diseases by administration of compositions containing at least one platinum complex alone or in combination with a modulator of glutathione. In particular, the methods may be used to treat cisplatin or carboplatin resistant tumor cells.

Abstract: Antitumor compositions are disclosed, as well as methods of preparing the compositions and methods of using them to inhibit tumor growth in mammals. The invention can take advantage of intraliposomal conversion of a platinum complex having the formula where R1 is diaminocycloalkyl, and R2 and R3 each have the formula where R4, R5, and R6 are each independently hydrocarbon moieties having from 1 to about 10 carbon atoms, into a complex having the formula R1—Pt—X2??(II) where X is halogen.

Abstract: Antitumor compositions are disclosed, as well as methods of preparing the compositions and methods of using them to inhibit tumor growth in mammals.

Abstract: The present invention concerns the use of methods and compositions for the treatment of cancer and other hyperproliferative diseases. In certain embodiments, methods are described for the treatment of cancer and/or hyperproliferative diseases by administration of compositions containing at least one platinum complex alone or in combination with a modulator of glutathione. In particular, the methods may be used to treat cisplatin or carboplatin resistant tumor cells.

Abstract: Antitumor compositions are disclosed, as well as methods of preparing the compositions and methods of using them to inhibit tumor growth in mammals. The invention can take advantage of intraliposomal conversion of a platinum complex having the formula where R1 is diaminocycloalkyl, and R2 and R3 each have the formula where R4, R5, and R6 are each independently hydrocarbon moieties having from 1 to about 10 carbon atoms, into a complex having the formula R1—Pt—X2  (II) where X is halogen.

Abstract: Antitumor compositions are disclosed, as well as methods of preparing the compositions and methods of using them to inhibit tumor growth in mammals.

Abstract: Antitumor compositions are disclosed, as well as methods of preparing the compositions and methods of using them to inhibit tumor growth in mammals. The invention can take advantage of intraliposomal conversion of a platinum complex having the formula ##STR1## where R.sub.1 is diaminocycloalkyl, and R.sub.2 and R.sub.3 each have the formula ##STR2## where R.sub.4, R.sub.5, and R.sub.6 are each independently hydrocarbon moieties having from 1 to about 10 carbon atoms,into a complex having the formulaR.sub.1 --Pt--X.sub.2where X is halogen.

Abstract: Novel 1,4 and 1,2-diaminocyclohexane platinum IV complexes have been synthesized that show activity in vivo against tumor models resistant to cis-platin and tetraplatin. The novel complexes include the chloro, acetate, trifluoroacetate, propionate, butyrate, pentanoate, hexanoate and heptanoate as leaving ligands and 1,4 or 1,2-DACH-amine ligands. The complexes showed good in vitro cytotoxic activity against murine leukemia L1210/0, L1210/DDP and L1210/DACH. High in vivo activity was shown against L1210 leukemia cells and against cis-platin resistant L1210/DDP. Excellent antitumor activity against M5076 was also exhibited by the new complexes. Additionally, the platinum complexes did not elicit any indication of nephrotoxicity in the in vivo tests.

Abstract: Lipophilic complexes having the structureDACH--Pt--R.sub.2where DACH is diaminocyclohexane, and where R is a linear alkyl carboxylato group having from about 5 to about 18 carbon atoms, have desirable stability when entrapped within lipid bilayers, and exhibit high entrapment efficiency and in vivo antitumor activity.

Abstract: Water-soluble complexes having the formula: ##STR1## and stereoisomers thereof, where Z.sup.1 and Z.sup.2 are halogens, and X.sup.1 and X.sup.2 are selected from the group consisting of sulfate, phosphate, nitrate, and monocarboxylate, or are jointly dicarboxylate, have been found to have desirable antitumor activity, as well as relatively low levels of toxicity.

Abstract: Platinum(IV) complexes with mixed carboxylato ligands having the formula: ##STR1## where X.sup.1 and X.sup.2 are carboxylato, or are jointly dicarboxylato, where .sup.1 Y and Y.sup.2 are carboxylato, and where Z is either diaminocyclohexane or ethylenediamine, have been found to have desirable antitumor activity, as well as relatively low levels of toxicity.

Abstract: The present invention involves the synthesis and use of new platinum compounds. These new platinum compounds are easy to encapsulate in liposomes at high efficiencies. They are further characterized as platinum (II) four coordinate complex having the formula: ##STR1## wherein R.sub.1 and R.sub.2 are carboxylato monoanions bearing a hydrophobic radical function or a single carboxylato dianion bearing a hydrophobic radical function and R.sub.3 is a vicinal diaminoalkane or vicinal diaminocycloalkane. The complex is substantially soluble in methanol or chloroform and substantially insoluble in water. Said complex may be incorporated into phospholipid liposomes. Such platinum complexes encapsulated in phospholipid liposomes are useful for chemotherapy of platinum complex-sensitive tumors.

Abstract: The present invention involves the synthesis and use of new platinum compounds. These new platinum compounds are easy to encapsulate in liposomes at high efficiencies. They are further characterized as platinum (II) four coordinate complex having the formula: ##STR1## wherein R.sub.1 and R.sub.2 are carboxylato monoanions bearing a hydrophobic radical function or a single carboxylato dianion bearing a hydrophobic radical function and R.sub.3 is a vicinal diaminoalkane or vicinal diaminocycloalkane. The complex is substantially soluble in methanol or chloroform and substantially insoluble in water. Said complex may be incorporated into phospholipid liposomes. Such platinum complexes encapsulated in phospholipid liposomes are useful for chemotherapy of platinum complex-sensitive tumors.

Abstract: The invention relates to a process for the treatment of tumors in animals with water soluble square-planar cis platinum(II) four-coordinate complexes comprising different nonovalent and divalent organic cations. Monovalent cations include galacturonato and N,N-dimethylglycinato and divalent cations include citraconato, 1,1-cyclobutanedicarboxylato, 1,1-cyclopropanedicarboxylato and Z-iminodiacetato where Z is bound to the nitrogen and is ethyl, propyl, isopropyl, n-butyl, secbutyl, ter-butyl, n-amyl, isoamyl or --OH. The treatment of animals comprises administering to the animals a pharmaceutical composition comprising a platinum complex of the composition described.

Abstract: The present invention concerns a platinum (II) four-coordinant complex having the formula: ##STR1## wherein R.sub.1 is an alkyl diamine or cycloalkyl diamine and R.sub.2 and R.sub.3 are an alkylcarboxylato containing from five to ten carbon atoms. The R.sub.1 is preferably trans-D,L-1,2-diaminocyclohexane, trans-R,R-1,2-diaminocyclohexane, trans-S,S-1,2-diaminocyclohexane, cis-1,2-diaminocyclohexane ethylene diamine or 1,1-bis(aminomethyl)cyclohexane. The R.sub.2 and R.sub.3 are preferably neohexanoato, neoheptanoato, neononanoato, neodecanoato, neooctanoato, neopentanoato, 2-ethylhexanoato, 2-ehtylbutyrato, 2-propylpropanoato, 2-methyl-2-ethylheptanoato, 2,2-diethylhexanoato, 2,2-dimethyl-4-ethylhexanoato, 2,2-diethyl-4-methylpentanoato, 2,2-dimethyloctanoato, 2-methyl-2-ethylheptanoato, 2,2-diethylhexanoato, 2,2-diethyl-4-methylpentanoato or 2,2,4,4-tetramethylpentanoato.

Abstract: The present invention relates to monoclonal antibodies specifically binding platinum (II) complex. The monoclonal antibodies of the present invention are characteristically produced by antibody-producing cell lines such as hybridomas. These cell lines may result, for example, from fusion of a neoplastic cell with an antibody-producing animal cell obtained from an animal immunized against a platinum (II) complex. The cellular fusion products include cell lines forming monoclonal antibody specifically binding platinum (II) complex in competition with an antibody produced by: hybridoma strain 1C.sub.1 H.sub.2 A.sub.5, deposited with the American Type Culture Collection, Rockville, MD on May 1, 1987 and having ATCC accession number HB 9411; strain 3A.sub.2 A.sub.1 ; strain 1A.sub.6 A.sub.2 ; strain 3A.sub.6 B.sub.1 or strain 1B.sub.1.

Abstract: Water-soluble complexes having the formula: ##STR1## and stereoisomers thereof, where Z.sup.1 and Z.sup.2 are halogens and X is selected from the group consisting of sulfate, phosphate, nitrate, monocarboxylate, and dicarboxylate, have been found to have desirable antitumor activity, as well as relatively low levels of toxicity.

Abstract: The present invention involves the synthesis and use of new platinum compounds. These new platinum compounds are easy to encapsulate in liposomes at high efficiencies. They are further characterized as platinum (II) four coordinate complex having the formula: ##STR1## wherein R.sub.1 and R.sub.2 are carboxylato monoanions bearing a hydrophobic radical function or a single carboxylato dianion bearing a hydrophobic radical function and R.sub.3 is a vicinal diaminoalkane or vicinal diaminocycloalkane. The complex is substantially soluble in methanol or chloroform and substantially insoluble in water. Said complex may be incorporated into phospholipid liposomes. Such platinum complexes encapsulated in phospholipid liposomes are useful for chemotherapy of platinum complex-sensitive tumors.

Abstract: The present invention comprises a water-soluble square-planar cis-platinum(II) four-coordinate complex having the formula:trans-R,R-DACH Pt(II) X.sub.2ortrans-R,R-DACH Pt(II) Ywherein X is a monovalvent cation, two of which are present, selected from the group consisting of cyclopropanecarboxylato, shikimato, saccharatolactone, galacturonato and N,N-dimethyglycinato; wherein Y is a divalent cation selected from the group consisting of citraconato, 1,1-cyclobutanedicarboxylato, 1,1-cyclopropanedicarboxylato, isocitratolactone and Z-iminodiacetato where Z is bound to the nitrogen and is ethyl, propyl, Isopropyl, n-butyl, sec-butyl, ter-butyl, n-amyl, isoamyl or OH.In one preferred aspect the water-soluble square-planar cis-platinum(II) four-coordinate complex has the formula:trans-R,R-DACH Pt(II) X.sub.2wherein X is a monovalent cation. Two X substituents are present in the platinum complex.

Abstract: Diaminocyclohexane platinum complexes having the structural formula ##STR1## wherein: X is a monovalent anion selected from the group consisting of isoascorbate, monosaccharate, saccharate-4-lactone, shikimate, isethionate, 2-aminoethylsulfate, azetidinecarboxylate, proline, hydroxyproline, pipecolinate, cyclopropanecarboxylate, cxyclobutanecarboxylate, cyclopentanecarboxylate, cyclopentenecarboxylate, cyclohexanecarboxylate, cyclohexenecarboxylate, bicine, glycine, 2-aminoethanesulfonate, 2-chloroethanesulfonate andY is a divalent anion selected from the group consisting of iminodiacetate, isocitratelactone, furanedicarboxylate, cyclopropane-1,1-dicarboxylate, isocitratomonoethylester, N-methyliminodiacetate, N-(2-hydroxyethyl)-iminodiacetate, N-benzyliminodiacetate, N-phenyliminodiacetate, N-(2-acetamido)-iminodiacetate, cyclohexane-1,1-diacetate, trans-1,2-cyclopropanedicarboxylate, trans-1,2-cyclobutanedicarboxylate, trans-1,2-cyclopentanedicarboxylate and trans-1,2-cyclohexanedicarboxylate and their use