Abstract: The present invention concerns antitumor compounds. More particularly, the invention provides novel taxane derivatives, pharmaceutical compositions thereof, and their use as antitumor agents.

Abstract: Provided are very highly water soluble, stable, crystalline salts of 2′,3′-dideoxy-2′,3′-didehydrothymidine (“d4T”), 2′,3′-dideoxyinosine (“ddI”), and 2′,3′-dideoxy-2′-fluoroinosine (“F-ddI”). Such salts are useful as intermediates or as antiviral agents.

Abstract: The present invention concerns antitumor compounds. More particularly, the invention provides novel taxane derivatives, pharmaceutical compositions thereof, and their use as antitumor agents.

Abstract: The present invention concerns a novel process using controlled cooling for obtaining d.sub.4 T polymorphic Form I from a mixture containing one or more of polymorphic Forms I, II and III. Compound d.sub.4 T has been approved for use in the treatment of AIDS.

Abstract: Solutions of carboplatin and other malonato platinum(II) antitumor agents are prepared containing stabilizing amounts of 1,1-cyclobutanedicarboxylic acid or salt at pH 4-8. The stabilizers inhibit unacceptable discoloration and precipitation. The solutions may also be stabilized by purging the carrier with air or oxygen and, optionally, blanketing the headspace with air or oxygen.

Abstract: The present invention provides physical admixtures of a new crystalline dihydrochloride dihydrate salt of the cephalosporin antibiotic, cefepime with a pharmaceutically acceptable non-toxic organic or inorganic base. In particular, this invention provides physical admixtures having a temperature and moisture stable crystalline dihydrochloride dihydrate form of cefepime having a specific X-ray powder diffraction pattern as described herein.

Abstract: The present invention relates to a new crystalline dihydrochloride dihydrate salt of the cephalosporin antibiotic, cefepime. In particular, this invention provides a temperature and moisture stable crystalline dihydrochloride dihydrate form of cefepime having enhanced stability and a specific x-ray powder diffraction pattern as described herein.

Abstract: Crystalline sulfuric, di-nitric, mono-hydrochloric, di-hydrochloric, and di- and sesqui-orthosphosphoric acid addition salts of 7-[.alpha.-(2-aminothiazol-4-yl)-.alpha.-(Z)-methoxyiminoacetamido]-3-[(1- methyl-1-pyrrolidinio)methyl]-3-cephem-4-carboxylate are stable even at elevated temperatures. The crystalline sulfuric acid addition salt is made by forming an admixture of (a) at least one molar equivalent of sulfuric acid with (b) zwitterion in an amount so as to be present in the admixture at a concentration of greater than 25 milligrams/ml, causing crystallization, separating the crystals, washing and drying. The crystalline monohydrochloride, dihydrochloride, and orthophosphate salts are prepared by dissolving the zwitterion in the appropriate amount of acid, causing crystallization by adding acetone and isolating the crystals. Physical admixtures of the salts with certain bases in proportions to give a pH ranging from about 3.

Abstract: Platinum complexes are disclosed in which the formula is ##STR1## wherein A and B are each independently ammine or monodentate amine, or A and B taken together represent a bidentate amine, and A and B are coordinated to the platinum atom through their nitrogen atom; X and Y are each independently halogen; R' is C.sub.1 -C.sub.20 alkanoyl, aroyl, heteroaroyl, or a group selected from the group consisting of ##STR2## wherein u' is an integer from 1 to 5; and R" is hydrogen with the proviso that A, B, X, and Y are structually equatorial substituents with respect to OR'--Pt--OR". These platinum complexes show antitumor activity with relatively lower kidney or bone marrow toxicity.

Abstract: A stable, amorphous, lyophilized dihydrochloride salt of 7-[.alpha.-(2-aminothiazol-4-yl)-.alpha.-(z)-methoxyiminoacetamido]-3-[(1- methyl-1-pyrrolidinium) methyl]-3-cephem-4-carboxylate is described. This lyophilized salt is more easily prepared than the crystalline counterpart and can be reconstituted in effective concentrations for intramuscular and intravenous injection utilizing suitable organic and inorganic bases to pH 3-7.0.

Abstract: A new antitumor antibiotic designated BMY-40800 is produced by fermentation of Streptomyces hygroscopicus ATCC 53653. The new compound inhibits the growth of tumors in experimental animals.

Abstract: This invention relates to novel compositions of the antitumor agent [4'-9-(acridinylamino) methanesulfon-m-anisidide], (m-AMSA). Acid salts of m-AMSA are dissolved in 1-methyl-2-pyrrolidinone to provide highly stable solutions. The solutions may be diluted with Sterile Water for Injection, U.S.P. to provide stable, non-precipitating solutions for intravenous use.

Abstract: Crystalline sulfuric, di-nitric, mono-hydrochloric, di-hydrochloric, and di- and sesqui-orthosphosphoric acid addition salts of 7-[.alpha.-(2-aminothiazol-4-yl)-.alpha.-(Z)-methoxyiminoacetamido]-3-[(1- methyl-1-pyrrolidinio)methyl]-3-cephem-4-carboxylate are stable even at elevated temperatures. The crystalline sulfuric acid addition salt is made by forming an admixture of (a) at least one molar equivalent of sulfuric acid with (b) zwitterion in an amount so as to be present in the admixture at a concentration of greater than 25 milligrams/ml, causing crystallization, separating the crystals, washing and drying. The crystalline monohydrochloride, dihydrochloride, and orthophosphate salts are prepared by dissolving the zwitterion in the appropriate amount of acid, causing crystallization by adding acetone and isolating the crystals. Physical admixtures of the salts with certain bases in proportions to give a pH ranging from about 3.

Abstract: A new antitumor antibiotic designated BMY-40800 is produced by fermentation of Streptomyces hygroscopicus ATCC 53653. The new compound inhibits the growth of tumors in experimental animals.

Abstract: The invention relates to chemically stable, concentrated solutions of cis-diamminedinitratoplatinum which are pH-stabilized with nitric acid and are readily convertible to parenteral cisplatin solutions by addition of sources of chloride ion.

Abstract: A solution of etoposide in dimethylisosorbide is disclosed. The solution is useful for filling gelatin capsules and may also be formulated into parenteral dosage forms.

Abstract: Crystalline sulfuric, di-nitric, mono-hydrochloric, di-hydrochloric, and di- and sesqui-orthosphosphoric acid addition salts of 7-[.alpha.-(2-aminothiazol-4-yl)-.alpha.-(Z)-methoxyiminoacetamido]-3-[(1- methyl-1-pyrrolidinio)methyl]-3-cephem-4-carboxylate are stable even at elevated temperatures. The crystalline sulfuric acid addition salt is made by forming an admixture of (a) at least one molar equivalent of sulfuric acid with (b) zwitterion in an amount so as to be present in the admixture at a concentration of greater than 25 milligrams/ml, causing crystallization, separating the crystals, washing and drying. The crystalline monohydrochloride, dihydrochloride, and orthophosphate salts are prepared by dissolving the zwitterion in the appropriate amount of acid, causing crystallization by adding acetone and isolating the crystals. Physical admixtures of the salts with certain bases in proportions to give a pH ranging from about 3.

Abstract: Amorphous solid formed by lyophilization or cosolvent precipitation of an aqueous solution of 7-[.alpha.-(2-aminothiazol-4-yl)-.alpha.-(Z)-methoximinoacetamido]-3-[(1-m ethyl-1-pyrrolidinio)-methyl[-3-cephem-4-carboxylate zwitterion and a salt or mixture of salts from a selected particular group is a broad spectrum antibiotic composition and has better temperature stability at least up to 45.degree. C. than the zwitterion. The salt is one wherein the cation is selected from the group consisting of sodium, lithium, calcium, and magnesium and the anion is selected from the group consisting of chloride, bromide, and iodide. The molar ratio of zwitterion to salt ranges from about 0.5:1 to about 2:l.

Abstract: There is disclosed a process for the in-vial deposition of 7-(dimethylaminomethylene)amino-9a-methoxymitosane in sterile unit dosage form. A solution of this compound is introduced into a sterile vial in a solution of tertiary-butanol. The tertiary-butanol is then removed, e.g., by evaporation or lyophilization, and the vial is closed by appropriate means. The thus deposited material can contain up to 0.5 mole equivalent of tertiary-butanol as a hemi-solvate and is very stable to heat.

Abstract: A stable solution of etoposide in 1-methyl-2-pyrrolidinone is disclosed. The solution can be diluted with a parenteral vehicle to yield an infusion solution containing up to 10 mg/ml etoposide activity without rapid etoposide crystallization. Solutions having etoposide concentration of as high as 500 mg/ml can also be prepared and used to fill gelatin capsules.