Abstract: The present invention relates to pharmaceutically active ornithine compounds, particularly to pharmaceutically acceptable ammonium salts of N?-acyl derivatives of N?(4-amino-4-deoxypteroyl)-L-ornithine compounds; and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such ammonium salts. The ammonium salts provided by the invention exhibit superior chemical stability than corresponding acidic N?-acyl derivatives of N?-acyl derivatives of N?(4-amino-4-deoxypteroyl)-L-ornithine compounds.

Abstract: The present invention relates to pharmaceutically active ornithine compounds, particularly to pharmaceutically acceptable ammonium salts of N?-acyl derivatives of N?(4-amino-4-deoxypteroyl)-L-ornithine compounds; and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such ammonium salts. The ammonium salts provided by the invention exhibit superior chemical stability than corresponding acidic N?-acyl derivatives of N?-acyl derivatives of N?(4-amino-4-deoxypteroyl)-L-ornithine compounds.

Abstract: In one embodiment, the present invention relates to a new class of ammonium salts of N?-acyl derivatives of N?-(4-amino-4-deoxypteroyl)-L-ornithine compounds having a structure according to formula II-IV. Formula II has the structure of: wherein: R2 represents up to four groups independently selected at each occurrence of R2 from the group consisting of hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, C1-6 alkoxy, chloro, fluoro, hydroxy, and —COOH; R3, R4, and R5 are each independently selected from hydrogen and C1-6 alkyl; or NR3R4 taken combination can form a 5 to 7 member heterocycle having at least one nitrogen ring atom; and x is a real number greater than 0 and less than about 4. The ammonium salts provided by the invention exhibit high inhibitory activity against the growth o methotrexate-resistant cells, and also exhibit superior chemical stability than corresponding acidic N?-acyl derivatives of N?-acyl derivatives of N?(4-amino-4-deoxypteroyl)-L-ornithine compounds.

Abstract: The present invention relates to pharmaceutically active ornithine compounds, particularly to pharmaceutically acceptable ammonium salts of N&dgr;-acyl derivatives of N&agr;(4-amino-4-deoxypteroyl)-L-omithine compounds; and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such ammonium salts. The ammonium salts provided by the invention exhibit superior chemical stability than corresponding acidic N&dgr;-acyl derivatives of N&dgr;-acyl derivatives of N&agr;(4-amino-4-deoxypteroyl)-L-ornithine compounds.

Abstract: There is described a novel method for preparing and isolating novel salts of 6-chloropurine and strong acids. According to the method hypoxanthine is reacted with phosphorus oxychloride in the presence of an organic base to form 6-chloropurine, a solvent is added to the reaction mixture and the latter is reacted with a strong acid to form a 6-chloropurine salt which is then isolated. In a preferred embodiment 6-chloropurine is freed from the salt with water, preferably in the presence of a base. In another preferred embodiment the 6-chloropurine is aminated with various amines.

Abstract: There is described a process for synthesizing 4-aminopyrazolo(3,4-d)pyrimidine wherein 3-amino-4-cyanopyrazole is reacted with formamidine or a salt of formamidine at a temperature in the range of from about 85.degree. C. to about 125.degree. C.

Abstract: There is described a process for synthesizing a thiacyanine dye wherein a 2-halo, 2-alkoxy or 2-aryloxybenzothiazole is alkylated by a strong alkylating agent to form a quaternized benzothiazole which, without being isolated, is condensed with a benzothiazolium betaine in a nonaqueous homogeneous medium. The thiacyanine dye is useful for enhancing the photosensitivity of a blue-sensitive silver halide emulsion.

Abstract: In one embodiment, this application is directed to an improved method of synthesizing certain bis-pyrazolone oxonol compounds useful as antihalation dyes in photography which method comprises synthesizing a pyrazolone ethyl ester by reacting a p-N-alkylsulfonamidophenylhydrazine or its hydrochloride and sodium diethyl oxalacetate, hydrolyzing the pyrazolone ethyl ester thus formed to give the corresponding pyrazolonecarboxylic acid, esterifying the pyrazolonecarboxylic acid with a glycol to give the corresponding pyrazolone hydroxyalkyl ester and condensing said pyrazolone hydroxyalkyl ester with an aldehyde dianil hydrochloride to yield the dye product.

Abstract: A process for an acid catalyzed esterification of a mercapto-carboxylic acid followed by an in situ S-alkylation of the mercapto-ester by slow addition of aqueous base to a mixture of said ester and an alkylating agent.

Abstract: A process for preparing a silver halide developing agent of the formula: ##STR1## where R.sup.1 can be the same or different substituent which will not impair the functionality of the compound as a silver halide developing agent. Specific substituents include hydrogen, alkyl radicals and alkoxy radicals among others. The silver halide developing agents are known as "ligand developers" and are particularly useful in diffusion transfer photographic products and processes.

Abstract: A novel process which comprises the step of reacting a metal complexed dye of the formula: ##STR1## WITH A CYCLIZED COMPOUND OF THE FORMULA: ##STR2## to form a metal complexed dye developer which is represented by the formula ##STR3## where A is a phenyl radical or a substituted phenyl radical; B is a phenyl or nitrogen containing heterocyclic radical or substituted derivatives of these radicals; R is N or CH, Y is a silver halide developing substituent; each n is 0 or 1; X is oxygen or an oxygen containing substituent; Me is a metal complexing atom; L represents a molecule(s) that can satisfy the coordination sphere of the Me atom and each R.sup.2 can be hydrogen or any substituent which will not interfere with the functionality of the complexed cyclized compound as a silver halide developing agent. The process generally comprises mixing the reactants in a suitable solubilizing medium and heating the solution. The reaction product can be precipitated by the addition of acid to the reaction medium.

Abstract: An improved method for preparing a compound of the formula: ##SPC1##Where each R can be hydrogen, an alkyl substituent, preferably having from 1-6 carbon atoms or an alkoxy substituent preferably having from 1-6 carbon atoms and each R.sup.1 is hydrogen or an alkyl or an alkanol group. R.sup.2 is an alkylene radical having from 1-6 carbon atoms and X represents the atoms to complete a cyclopentyl or cyclohexyl ring.Metal complexed dyes of the above formula are especially useful in the preparation of photographic image patterns.The improved feature of the method presented involves the preparation of compounds of formula 1 in the presence of weakly basic anion exchange resins to obtain high yields of especially high purity products.