Abstract: Prodrug compounds which metabolize into 5-ASA or analogs thereof, and taurine or analogs thereof, in the colon site are disclosed. Pharmaceutical compositions including the compounds, and methods of treatment using the compounds, are also disclosed. Such compounds have utility for treating or preventing gastrointestinal disorders, including colon cancer, ulcerative colitis and Crohn's disease.

Abstract: A pharmaceutical composition including at least one compound of the Formulas (I), (II), or (III), or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, as defined herein. Also disclosed is a method of treatment of diseases which are pathophysiologically related to GPR35, the GPR35-hERG signaling complex, or both, as defined herein.

Abstract: Prodrug compounds which metabolize into 5-ASA or analogs thereof, and taurine or analogs thereof, in the colon site are disclosed. Pharmaceutical compositions including the compounds, and methods of treatment using the compounds, are also disclosed. Such compounds have utility for treating or preventing gastrointestinal disorders, including colon cancer, ulcerative colitis and Crohn's disease.

Abstract: Disclosed herein is a way to produce a series of discrete sized slender, rigid oligoparaxylene molecules ranging from 1-5 nm in length. Molecules, based on 1-7, 9-11 paraxylene rings, have been synthesized as part of a homologous series of oligoparaxylenes (OPXs) with a view to providing a molecular tool box for the construction of nano architectures—such as spheres, cages, capsules, metal-organic frameworks (MOFs), metal-organic polyhedrons (MOPs) and covalent-organic frameworks (COFs), to name but a few—of well-defined sizes and shapes. Twisting between the planes of contiguous paraxylene rings is generated by the steric hindrance associated with the methyl groups and leads to the existence of soluble molecular gauge blocks without the need—at least in the case of the lower homologues—to introduce long aliphatic side chains onto the phenylene rings in the molecules.

Abstract: Methods are disclosed for preparing compounds of Formula I: where R1, R3, and R4 are independently hydrogen or C1 to C4 alkyl, and R2 is: where R5 is selected from the group consisting of hydrogen and C1 to C4 alkyl, or where R6, R7 and R8 are independently hydrogen or C1 to C4 alkyl; or the esters or pharmacologically acceptable salts thereof. The methods can involve converting a suitably functionalized aniline compound to a diazonium salt (which aniline compound can be first formed by reduction of a nitrobenzene) and coupling the diazonium salt with a suitably functionalized benzene compound. The suitably functionalized aniline compound either includes a primary alcohol or aldehyde group, which is then oxidized to a carboxylic acid group, or includes a nitrile or amide group, which is hydrolyzed to a carboxylic acid group. The methods can also involve the direct coupling (via reduction of nitro groups to form an azo linkage) of suitably functionalized nitrobenzenes.

Abstract: Prodrug compounds which metabolize into 5-ASA or analogs thereof, and taurine or analogs thereof, in the colon site are disclosed. Pharmaceutical compositions including the compounds, and methods of treatment using the compounds, are also disclosed. Such compounds have utility for treating or preventing gastrointestinal disorders, including colon cancer, ulcerative colitis and Crohn's disease.

Abstract: Compounds, particularly, glucopyranosyl lipid adjuvant (GLA) compounds, having the following structure (I) are provided: or a pharmaceutically acceptable salt thereof, wherein L1, L2, L3, L4, L5, L6, L7, L8, L9, L10, Y1, Y2, Y3, Y4, R1, R2, R3, R4, R5, R6, are as defined herein. Pharmaceutical compositions, vaccine compositions, and related methods for inducing or enhancing immune responses, are also provided.

Abstract: The present invention refers to a process for preparing a compound of general formula (A), as reported in the description, wherein R is a radical of a drug and R1-R12 are hydrogen or alkyl groups, m, n, o, q, r and s are each independently an integer from 0 to 6, and p is 0 or 1, and X is O, S, SO, SO2, NR13 or PR13 or an aryl, heteroaryl group, said process comprising reacting a compound of formula (B) R—COOZ (B) wherein R is as defined above and Z is hydrogen or a cation selected from: Li+, Na+, K+, Ca++, Mg++, tetralkylammonium, tetralkylphosphonium, with a compound of formula (C), as reported in the description, wherein R1-R12 and m, n, o, p, q, r, s are as defined above and Y is a suitable leaving group.

Abstract: This invention relates to novel compounds that display retinoid like activities, including HB-EGF (Heparin Binding Epidermal Growth Factor) release from keratinocytes, cell proliferation, and epidermal thickening without the irritation potentials, such as release of interleukin 8 and inhibition of terminal differentiation of keratinocytes. This invention also relates to the use of such a compound for both external and non-external applications.

Abstract: Provided herein are compounds, compositions and methods for decreasing NF?B DNA-binding activity in a patient comprising administering of a therapeutically effective amount of a compound or composition of the application to the patient to reduce, alleviate or treat various gastrointestinal diseases, such as inflammatory bowel disease (IBD).

Abstract: A process for the preparation of Balsalazide and its pharmaceutically acceptable salts wherein the reaction comprises: a. the intermediate N-(4-aminobenzoyl)-?-alanine is converted to N-(4-ammoniumbenzoyl)-?-alanine sulfonate salt using a sulfonic acid in water, b. the N-(4-ammoniumbenzoyl)-?-alanine sulfonate salt is treated with aqueous sodium nitrite solution at low temperature to generate N-(4-diazoniumbenzoyl)-?-alanine sulfonate salt, c. the aqueous solution obtained is quenched with aqueous disodium salicylate to furnish Balsalazide disodium solution, d. the solution is acidified to allow isolation of Balsalazide, and e. optionally converting the Balsalazide to a pharmaceutically acceptable salt (such as disodium salt).

Abstract: The present invention relates to a process for the preparation of aromatic azo-compounds, in particular 3,3?-azo-bis(6-hydroxybenzoic acid) (olsalazine) and its salts and derivatives.

Abstract: Compounds are disclosed having the structure of Formula I: where R1, R3, and R4 are independently hydrogen or C1 to C4 alkyl, and R2 is: where R5 is selected from the group consisting of hydrogen and C1 to C4 alkyl, or where R6, R7 and R8 are independently hydrogen or C1 to C4 alkyl; or the esters or pharmacologically acceptable salts thereof. Such compounds may be utilized for the prophylaxis or treatment of various diseases, particularly inflammatory conditions of the GI tract. Methods of treating inflammatory conditions of the GI tract such as inflammatory bowel disease using compounds having the following formula are also disclosed: where R9, R10 and R11 are independently selected from the group consisting of hydrogen and C1 to C4 alkyl, and R12 is selected from the group consisting of hydrogen and —C(O)R13, where R13 is a C1 to C6 alkyl or an aryl group.

Abstract: Compounds are disclosed represented by the following formula: where R1 is a substituted or unsubstituted phenyl group, and where Z is selected such that a compound, Z-R1-NH2, formed by cleavage of the azo bond is a non-absorbable antibiotic; or an ester or pharmacologically acceptable salt of the compound of Formula I. Compounds of the present invention may be utilized for the prophylaxis or treatment of various diseases including, but not limited to, intestinal diseases such as inflammatory bowel disease and/or traveler's diarrhea, liver diseases such as hepatic encephalopathy, and/or diseases treatable by a non-absorbable antibiotic.

Abstract: New compounds and their compositions having anti-inflammatory, analgesic and anti-thrombotic activities, of the general formula: A--X.sub.1 --NO.sub.2 or their salts, wherein: A is R(COX.sub.u).sub.t, wherein t is zero or 1 and u is zero or 1; and X is O, NH or NR.sub.1C wherein R.sub.1C is C.sub.1 -C.sub.10 alkyl; and R is(Ia) wherein R.sub.1 is acetoxoy, preferably n ortho-position with respect to --CO-- and R.sub.2 is hydrogen; or derivatives of acetylsalylsalicyclic acid; and X.sub.1 is --YO-- wherein Y is C.sub.1 -C.sub.20 alkylene, C.sub.5 -C.sub.7 cycloalkylene, oxy-alkyl derivatives and oxy-methyl benzyl derivatives.

Abstract: Transition metal complexes of the compounds of the formulae I and II ##STR1## in which A is an isocylic or heterocyclic aromatic radical, R is --H, halogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy, R.sub.1 is --H, C.sub.1 -C.sub.4 -alkyl or phenyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, --NO.sub.2, --CONH.sub.2, --CONHR.sub.2 or C.sub.2 -C.sub.5 -N-alkylcarbamoyl, X is --CH.dbd. or --N.dbd. andB is --H, C.sub.1 -C.sub.4 -alkyl, --NHCONH.sub.2, --NHCONH-C.sub.1 -C.sub.4 -alkyl, --NHCONR.sub.2, --NHCSNH.sub.2, --NHCSR.sub.3, --NHC(NH)NH.sub.2, --NHR.sub.2, --NHCOR.sub.3, --NHSO.sub.2 R.sub.3 or a heterocyclic aromatic radical, and R.sub.2 and R.sub.3 are phenyl or substituted phenyl, are suitable for pigmenting high-molecular organic material.

Abstract: The present invention is concerned with compounds having a pharmaceutically acceptable degree of purity, and with formulations of these compounds for the treatment of inflammatory disorders in the intestine (IBD), especially ulcerative colitis. These compounds are 4,5'-azo-bis-salicylic acid (I) and its pharmaceutically acceptable salts, especially the disodium salt. The invention is also concerned with a method for treating inflammatory conditions in the intestine, especially ulcerative colitis. Finally the invention also comprises a method of producing 4,5'-azo-bis-salicylic acid with a pharmaceutically acceptable degree of purity.

Abstract: A method of preparing 3,3'-azo-bis-(6-hydroxy benzoic acid) of formula I ##STR1## and salts thereof in at least 98% purity for treating inflammatory intestinal diseases. According to the invention a compound II ##STR2## is diazotized, and the diazonium salt obtained is coupled with a compound III ##STR3## The formed intermediate IV, which is also comprised by the invention, ##STR4## is hydrolized in alkaline medium to form the compound I. R.sub.1, R.sub.2 and R.sub.3 signify lower alkyl, R.sub.2 also possibly substituted phenyl.