Abstract: The present invention relates to Rifaximin polymorphic, salt, hydrate, and amorphous forms, to their use in medicinal preparations and to therapeutic methods using them.

Abstract: The present invention relates to Rifaximin polymorphic, salt, hydrate, and amorphous forms, to their use in medicinal preparations and to therapeutic methods using them.

Abstract: The invention relates to substantially enantiopure crystalline salt forms of (2RS)-I-(4-Ethylphenyl)-2-methyl-3-piperidin-1-ylpropan-1-one. The preparation and characterization of the substantially enantiopure crystalline salt forms according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the substantially enantiopure crystalline salt forms, which are useful to treat and/or prevent various conditions such as pathological muscle contracture, myotome conditions, and spastic paralysis or spasticity caused by various neurologic conditions, and are also useful for the treatment and/or prevention of various types of pain and pathological muscle tension.

Abstract: The invention relates to a novel choline cocrystal of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel choline cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel choline cocrystal and the therapeutic use of the novel choline cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, treating and/or preventing homocystinuria reducing levels of homocysteine in blood serum, inhibiting aldose reductase, and affording cardioprotection in non-diabetic patients.

Abstract: The invention relates to crystalline forms of flupirtine, particularly to 1:1 flupirtine hydrochloride maleic acid cocrystal. The preparation and characterization of 1:1 flupirtine hydrochloride maleic acid cocrystal is described. The invention also relates to the therapeutic use of the flupirtine hydrochloride maleic acid cocrystal to treat nervous system disorders, pain disorders, and musculoskeletal disorders and to pharmaceutical compositions containing the cocrystal.

Abstract: The invention relates to novel crystalline salts of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid and a novel betaine cocrystal of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel crystalline salts and cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel crystalline salts and cocrystal and the therapeutic use of the novel crystalline salts and cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, inhibiting aldose reductase, and affording cardioprotection in patients who may be non-diabetic.

Abstract: The present invention relates to Rifaximin polymorphic, salt, hydrate, and amorphous forms, to their use in medicinal preparations and to therapeutic methods using them.

Abstract: The present invention relates to Rifaximin polymorphic forms, to their use in medicinal preparations and to therapeutic methods using them.

Abstract: A process to prepare aryldiphosphate esters without forming an emulsion in the product is described. In one embodiment of this process, the ester is formed by initially reacting a phosphoryl oxyhalide with a dihydric aromatic compound in the presence of an insoluble catalyst to form an intermediate. The intermediate is then reacted with a monohydric aromatic compound in the presence of an insoluble catalyst to form the aryldiphosphate ester and the catalyst is then filtered from the aryldiphosphate ester. In another form of this process the ester is formed reacting a dihydric aromatic compound in the presence of an insoluble catalyst with a compound corresponding to the formula (RO).sub.2 POX, where X is bromine or chlorine and R is an aromatic group and contains no more than 1 ortho substituent. Thereafter, the catalyst is then filtered from the aryldiphosphate ester.

Abstract: Disclosed are bis-meta-benzotrifluoride compounds having the general formula ##STR1## where each A is independently selected from the group consisting of NO.sub.2, NH.sub.2, and NH.sub.3.sup.+ Z.sup.-, Z.sup.- is an anion and B is selected from the group consisting of O, CO, S, SO, and SO.sub.2. The diamine compounds are useful as monomers in making polyimides, polyamide-imides, and polyamides.

Abstract: Crude mixtures of dioxydiphthalic anhydride containing alkali metal salts are purified by treating the crude mixture with an alkanol, such as n-butanol, to form the dioxydiphthalic acid diester; removing the insoluble alkali metal salts by filtration; removing the excess alkanol; and reconverting the dioxydiphthalic acid diester to dioxydiphthalic anhydride.

Abstract: Disclosed are bis-meta-benzotrifluoride compounds having the general formula ##STR1## where each A is independently selected from the group consisting of NO.sub.2, NH.sub.2, and NH.sub.3.sup.+ Z.sup.-, Z.sup.- is an anion and B is selected from the group consisting of O, CO, S, SO, and SO.sub.2. The diamine compounds are useful as monomers in making polyimides, polyamide-imides, and polyamides.

Abstract: Polyimide polymers of the following recurring structure and the corresponding polyamic acids are disclosed: ##STR1## wherein AR.sub.1 is ##STR2## where X is O, S, SO, SO.sub.2, CO, C(CF.sub.3).sub.2, C(CH.sub.3).sub.2, Si(CH.sub.3).sub.2, or a single bond, wherein AR.sub.2 may be pyromellitic dianhydride, a substituted pyromellitic dianhydride, naphthanoic dianhydride, or ##STR3## where Y is O, S, SO, SO.sub.2, CO, C(CF.sub.3).sub.2, C(CH.sub.3).sub.2, Si(CH.sub.3).sub.2 --O--AR--O--, or a single bond, where AR is an aromatic nucleus.

Abstract: Disclosed is a method of making a 4-substituted phthalic anhydride. A halomaleic (including halofumaric anhydride (or the acid or ester thereof) is made by the reaction of-maleic anhydride with chlorine or bromine. The halomaleic anhydride is reacted with a conjugated diene to form a first cycloadduct having the formula ##STR1## The first cycloadduct is heated to eliminate HX and produce a second cycloadduct having the formula ##STR2## The second cyclo adduct is dehydrogenated to produce a 4substituted phthalic anhydride which has the formula ##STR3## where R.sub.1, R.sub.2, and R.sub.4 are preferably H and R.sub.3 is preferably Cl or F.

Abstract: Disclosed is a method of making 1,1'-sulfonylbis[3-nitro-5-(trifluoromethyl) benzene] by reacting dibenzotrifluoride sulfide with at least four equivalents of fuming nitric acid and at least four equivalents of fuming sulfuric acid at a temperature below 20.degree. C., until the sulfide link is oxidized to a sulfone link, then raising the temperature to above 20.degree. C. until the reaction is complete. Also disclosed is the preparation of 1,1'-sulfonylbis[3-nitro-(5-trifluoromethyl) benzenamine] by reducing the benzene compound.

Abstract: A process for the selective hydrodefluorination of a tetrafluorophthalimide compound of the formula ##STR1## where X is 1 and R is a monovalent organo group; or X is 2 and R is a divalent organo group; comprises reacting (I) the tetrafluorophthalimide with zinc in an aqueous alkali metal hydroxide medium. The product may be hydrolyzed to form 3,4,6-trifluorophthalic acid.

Abstract: A process for the preparation of 1,1'-oxy-bis(3-trifluoromethyl-4-nitrobenzene) which comprises reacting a compound of the formula ##STR1## where X is F, Cl, Br or I; with an inorganic base selected from the group consisting of alkali metal hydroxides, alkali metal carbonates, and alkali metal bicarbonates, in the presence of a catalytic quantity of a benzoate catalyst. In addition, benzoate esters of 4-nitro-3-trifluoromethylphenol may be isolated.

Abstract: Bis-imides of dioxydiphthalic or oxydiphthalic anhydride, are characterized by the formula ##STR1## where Z is H, alkyl of 1-12 carbon atoms, or ##STR2## A is H, Cl, F, NO.sub.2, OH, CF.sub.3, alkyl, alkoxy, alkylaryl or aryloxy, wherein the alkyl groups are 1-6 carbon atoms and the aryl groups are 6-14 carbon atoms; alkenyl or alkynyl of 2-6 carbon atoms; or benzoyl; and Y is H, Cl, F, NO.sub.2, OH, or CF.sub.3 ; X is halogen; X' is hydrogen or halogen; or X and X' together represent an oxygen atom, forming a second ether linkage.

Abstract: Oxydiphthalic acid esters of the formula ##STR1## where Z is H or alkyl, and X is halo, X' is H or halo, or X and X' together represent an oxygen atom; are prepared by the esterification reaction of the corresponding halo-oxydiphthalic anhydride or dioxydiphthalic anhydride with an alkanol.

Abstract: A method for the preparation of acyloxyphthalic anhydride or oxydiphthalic anhydride which comprises the reaction of a halophthalic anhydride with an alkali metal salt and at least a catalytically effective amount of an acid or acid derivative selected from the group consisting of benzoic acids, substituted benzoic acids, benzoic acid salts or substituted benzoic acid salts, and hydrolyzable benzoyl esters, and hydrolyzable substituted benzoyl esters, alkyl carboxylic acids, hydrolyzable esters of alkyl carboxylic acids, and salts of alkyl carboxylic acids. The process may be conducted without solvent, in a polar solvent or in a non-polar solvent using a phase transfer catalyst.