Abstract: The present invention includes bis- and tris-benzamide compounds that block AR signaling and have activity against prostate cancer. Uses for these compounds, and pharmaceutical compositions containing the same, also are provided.

Abstract: The invention provides a compound conforming to the structure of Formula (CX) The invention also provides a thermoplastic polymer composition comprising a polyolefin polymer and a compound conforming to the structure of Formula (CX) as a nucleating agent.

Abstract: The present invention relates to the use of a tryptophan metabolite, 3-hydroxyanthranilic acid (3-HAA) or a functional analogue thereof, for prophylactic and/or therapeutic treatment of mammals, in special humans, against hyperlipidemia and its cardiovascular complications, i.e. atheroma formation, myocardial infarction and heart failure, ischemic stroke and transient ischemic attacks, renal impairment, aortic aneurysms and critical limb ischemia caused by atherosclerosis.

Abstract: The present invention provides a compound that has high solubility in a highly polar solvent and is usefully usable for an application method using a highly polar solvent, the compound that can manufacture an electroluminescent device having high light-emitting efficiency. Specifically, the present invention provides a compound containing a structure represented by Formula (1): wherein: Ar1, Ar2, Ar3, and Ar4 each independently represent a divalent aromatic group optionally having substituent(s); Ar5 represents a monovalent aromatic group optionally having substituent(s); p and q each independently represent an integer of 0 or more; and R1 represents a given monovalent group.

Abstract: Disclosed are improved granular pharmaceutical preparations, together with improved methods and apparatus for preparation of granules for use in such preparations. Such methods are especially useful for making granules for solid oral dose pharmaceutical preparations, and are particularly suited to the production of granules comprising 5-aminosalicylic acid (5-ASA) for the treatment of inflammatory bowel disease. The granules exhibit a more sharply peaked length distribution, and hence aspect ratio distribution, and have a consequently much sharper dissolution profile after further processing.

Abstract: The invention relates to compositions and co-crystals each comprising VX-950 and a co-crystal former selected from the group consisting of 4-hydroxybenzoic acid, 4-amino salicylic acid, phenylalanine, threonline, tartaric acid, adipic acid, succinic acetate, proline, methyl 4-hydroxybenzoate, anthranilic acid, and d-Biotin. Also within the scope of this invention are methods of making and using the same.

Abstract: A polymerizable monomer is provided which is represented by the following formula (1): wherein R1 represents a hydrogen atom or an alkyl group; A represents —CO— or —SO2—; and the moiety represented by the formula (1) is, at the part shown by an asterisk *, linked to a moiety represented by the following formula (2), at any position of a, b, c or d thereof; wherein the sites among a, b, c and d at which the moiety represented by the formula (2) is not linked to the moiety represented by the formula (1) each has a hydrogen atom or a substituent selected from the group consisting of an alkyl group, an alkoxy group and a sulfonic acid group, or any of which may connect at mutually adjoining positions to form a ring.

Abstract: The present invention includes compound compositions and methods of making compounds that include an oligo-benzamide compound having at least two optionally substituted benzamides.

Abstract: This disclosure relates to methods and compositions for modulating disease resistance in plants and transgenic plants.

Abstract: [Problem] To provide a stable industrially-manufactured intermediate, enabling an industrially stable supply of 2-pyridyl-benz[d][1,3]oxazine to be provided. [Solution] The compound represented by formula (6) (wherein M represents sodium or potassium).

Abstract: A method for the treatment or prophylaxis of non-inflammatory bowel diseases, diarrhoea-predominant irritable bowel syndrome or other non-specific bowel disorder is disclosed comprising administering to a patient in need of such treatment or prophylaxis an effective amount of balsalazide, or a 4-ASA or 5-ASA compound modified to include a 4-ABA side chain, or a salt or a derivative thereof, or a composition comprising balsalazide the modified compound, or a salt or a derivative thereof together with a suitable carrier. Use of balsalazide, a 4-ASA or 5-ASA compound modified to include a 4-ABA side chain, or a salt or derivative thereof, for the manufacture of a medicament for the treatment or prophylaxis of non-inflammatory bowel diseases, diarrhoea-predominant Irritable Bowel Syndrome or other non-specific bowel disorder is also disclosed.

Abstract: The present invention includes bis- and tris-benzamide compounds that block AR signaling and have anticancer activity. Uses for these compounds, and pharmaceutical compositions containing the same, also are provided.

Abstract: The invention relates to a method for producing crystalline 5-aminosalicylic acid with a particularly high tap and/or bulk density.

Abstract: The present invention provides pharmaceutical compositions comprising a pharmaceutically acceptable excipient and a conjugate having a degradable linkage. The conjugates include at least one of each the following: an aromatic moiety comprising an ionizable hydrogen atom, a spacer moiety, and a water-soluble polymer. Methods for delivering such compositions are also provided.

Abstract: The present invention provides methods for the design and identification of novel antimicrobial compounds, and provides antimicrobial compounds identified using these methods. These antimicrobial compounds inhibit the binding of a prokaryotic single-stranded DNA binding protein to a polypeptide that binds to the prokaryotic single-stranded DNA binding protein. In some examples, the prokaryotic single-stranded DNA binding protein is prokaryotic Exonuclease I. In one embodiment, the antimicrobial compound has the structure wherein Y is selected from the group consisting of CH2, O, and NH, R1 is selected from the group consisting of H, F, Cl, Br, and I, R2 is selected from the group consisting of H and CF3, R3 is selected from the group consisting of H and CO2H, R4 is selected from the group consisting of H and OH, and R5 is selected from the group consisting of H, alkoxy, and NO2.

Abstract: Disclosed are improved granular pharmaceutical preparations, together with improved methods and apparatus for preparation of granules for use in such preparations. Such methods are especially useful for making granules for solid oral dose pharmaceutical preparations, and are particularly suited to the production of granules comprising 5-aminosalicylic acid (5-ASA) for the treatment of inflammatory bowel disease. The granules exhibit a more sharply peaked length distribution, and hence aspect ratio distribution, and have a consequently much sharper dissolution profile after further processing.

Abstract: Derivatives of anacardic acid having antimicrobial properties and method for preparing said derivatives. The antimicrobial properties include bacteriostatic and bacteriocidal activity.

Abstract: The present invention relates to compounds of formula (I), where R1 and R2, which may be identical or different, are selected from the group comprising H, CnH2n-1, a linear or branched alkyl group having 1 to 6 carbons, or together form an aromatic or aliphatic ring with 5 or 6 atoms; R3 is —CO—CH3, —NHOH, —OH, or —OR6 where R6 is a linear or branched alkyl group having 1 to 6 carbon atoms; R4 is H, linear or branched alkyl group having from 1 to 6 atoms, phenyl, benzyl, —CF3 or CF2CF3, vinyl or allyl; R5, R7, R8 are hydrogen atoms; or R3 and R4, R4 and R5, or R7 and R8 together form a ring, fused to the benzene, aromatic or aliphatic ring with 5 or 6 atoms comprising from 1 to 2 heteroatoms selected independently from the group comprising N, O, and use thereof in the medical field.

Abstract: Method for preparing carboxylic acid derivatives by aromatic nucleophilic substitution, in which a carboxylic acid derivative having a single carboxyl functional group, or one of the salts thereof, the carboxylic acid derivative having, in the ortho position of the carboxyl functional group, a leaving group, which is preferably an atom of fluorine or of chlorine or an alkoxy group, chiral or not, preferably a methoxy group, the carboxylic acid derivative not being substituted by an electro attractive group other than the leaving group if any; is reacted with a reactant MNu, where M is a metal and Nu is a nucleophile, chiral or not, the aromatic nucleophilic substitution reaction being carried out without a catalyst and without a step of protecting/deprotecting the acid functional group of the starting compound.

Abstract: The present invention relates to a pharmaceutical composition and the method of use for treating or preventing burn injury in patients or subjects in need, including the compound represented by the specific chemical formula as an active ingredient or its pharmaceutically acceptable salts or solvates.

Abstract: The present invention provides a peptide degradation reagent with the following characteristics: 1) it has no marked toxicity such as carcinogenicity, 2) it does not produce metastable peaks resulting from excessive degradation property, 3) it does not produce multiply-charged ion peaks which are interference peaks, and 4) it can secure separation and sharpness of peaks. The present invention also provides a method for specifically cleaving N—C? bonds on a peptide backbone using the above-described reagent, and a method of determining the amino acid sequence of a peptide utilizing this specific cleavage. A method for specifically cleaving N—C? bonds on the backbone of a peptide, comprising irradiating the peptide with laser light in the presence of 5-amino salicylic acid. A method for determining the amino acid sequence of a peptide, comprising irradiating the peptide with laser light in the presence of 5-amino salicylic acid to thereby specifically cleave N—C? bonds on the peptide backbone.

Abstract: The present invention relates to a pharmaceutical composition useful for treating or preventing inflammatory disease and cell damage, and a method for treating or preventing inflammatory disease and cell damage. The present invention uses the 2-hydroxybenzoic acid derivative represented by the specific chemical formula or its pharmaceutically acceptable salt. The compound of the present invention is useful for treating or preventing cell damage and inflammatory disease including gastritis, gastric ulcer, pancreatitis, colitis, arthritis, diabetes, arteriosclerosis, nephritis, hepatitis, Alzheimer's disease, Parkinson's disease and Lou Gehrig's disease.

Abstract: The process of the present invention creates a sustainable and closed water loop allowing inherent recycles of all liquid streams generated in the process. The liquid streams generated during the process of the invention are inherently recycled completely, making the process of the present invention a zero liquid discharge process which is environmentally friendly and sustainable. This invention further relates to a sustainable chemical process of reduction of R—NO2 or R—NO into corresponding R—NH2 that produces environmentally friendly R—NH2 in good yields and selectivity with large of mother liquor recycle. The process has a wide scope in that it can be applied to a number of molecules.

Abstract: The present invention includes methods of making and methods of using peptidomimetics compositions that mimic ?-helical BH3 sequences in cells. The peptidomimetics can be used to mimic ?-helical BH3 sequences and kill cancer cells.

Abstract: Certain poly(oxyalkylene) colorants are disclosed along with method of preparation thereof. A method of using these colorants as fluorescent security taggants is also disclosed.

Abstract: The present invention provides methods for prevention and prophylaxis of neurological diseases accompanied by neuronal death in a patient. The invention includes use of 5-benzylamino salicylic acid (BAS) and its derivatives. Thus, the present invention provides methods for reducing neuronal death in nervous system injuries resulting from amyotrophic lateral sclerosis.

Abstract: The present invention provides compositions and methods for prevention and prophylaxis of neurological diseases accompanied by neuronal death. The invention includes synthesis of 5-benzylamino salicylic acid (BAS) and its derivatives. BAS and its derivatives protect cortical neurons from toxic insults by N-methyl-D-aspartate, Zn2+, and reactive oxygen species. Thus, the present invention provides compositions and methods for treating stroke, traumatic brain and spinal cord injury, epilepsy, and neurodegenerative diseases that are accompanied by severe neuronal loss via excitotoxicity, Zn2+ neurotoxicity, and free radical neurotoxicity.

Abstract: The use of specific compounds of the Formula 1 (and also corresponding mixtures) in particular as cosmetic agents for the inhibition of the substance P-induced release of histamine from mast cells is described.

Abstract: Disclosed are 4,5-diamino-3-halo-2-hydroxybenzoic acid derivatives and manufactures thereof. The 4,5-diamino-3-halo-2-hydroxybenzoic acid derivatives are presented by formula (I): wherein R1 group is H, CH3, or C2H5; R2 group is H, or Br; R3 group is CH3, or C3H7; and R4 group is H, or C(?NH)—NH2. 4,5-diamino-3-halo-2-hydroxybenzoic acid derivatives provided here were non-toxic to MDCK cells, particularly compounds 6a, 6b, 6c, 6e, 6f, 7a, 7b and 8 had better anti-H1N1 activity. In the future, these compounds can be used to focus on viral neuraminidases as targets to develop effective anti-influenza drugs.

Abstract: The present invention relates to a pharmaceutical composition for treating or preventing stress disorder, depression, anxiety disorder, comprising 5-benzylaminosalicylic acid derivative or its pharmaceutically acceptable salt. The present invention relates to a method for treating or preventing stress disorder, depression, anxiety disorder, comprising 5-benzylaminosalicylic acid derivative or its pharmaceutically acceptable salt.

Abstract: The present invention provides new derivatives of 4- or 5-aminosalicylic acid, and a pharmaceutical composition containing these derivatives of 4- or 5-aminosalicylic acid as active ingredients, useful for the treatment of intestinal diseases such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS) and for the prevention/treatment of colon cancer. More particularly, these derivatives comprise a hydrogen sulfide releasing moiety linked via an azo, an ester, an anhydride, a thioester or an amide linkage to a molecule of 4- or 5-aminosalicylic acid. Furthermore, the present invention provides a process for preparing these compounds and their use for treating IBD and IBS and the prevention/treatment of colon cancer.

Abstract: The present invention relates to a water soluble photosensitive polyimide polymer, preparation thereof and a photoresist composition containing the same. The water soluble photosensitive polyimide polymer is characterized by having repeat units represented by the following formula (I): the other symbols are defined in the specification].

Abstract: The invention relates to the use of and mainly novel compounds of the formula I wherein the moieties are as defined in the description, which are useful as farnesyl pyrophosphate synthase modulators and e.g. in the treatment of proliferative diseases.

Abstract: The present invention relates in general to a compound (activator) which is characterized by a formula selected from the following formulas A, B and/or C or a pharmaceutically acceptable salt thereof. The present invention further relates to pharmaceutical composition comprising the activator(s) of the invention and to their use in the treatment of (for treating) and/or preventing diseases or medical conditions which benefit from an increased transport of hyaluronan across a lipid bilayer. The present invention also relates to a method for manufacturing a pharmaceutical composition comprising the steps of formulating the activator defined herein in a pharmaceutically acceptable form.

Abstract: The present invention relates to a novel water soluble polyimide resin, which contains a hydrophilic functional group such as —OH, —COOH to increase the solubility of the polyimide resin in alkali aqueous solution, and is suitable for using as an insulation film in electronic and photoelectric products. The present invention also relates to preparation and use of the above polyimide.

Abstract: A simple and efficient method for the production of stable, clear, high-potency oat extracts is disclosed. The method employs the use of differential dissociation constants and ultrafiltration to stabilise extracts, prevent hazing, and prevent the loss of functional activity as an anti-irritant and anti-oxidant. Also disclosed are compositions of oat extracts derived from whole oat grains and oatmeal. Further disclosed are compositions of oat extracts for use in cosmetic, nutraceutical, therapeutic medical and veterinary preparations.

Abstract: There is provided compounds of formula I, wherein ring A, D1, D2a, D2b, D3, L1, Y1, L3 and Y3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.

Abstract: Novel pyruvate derivatives exhibiting outstanding neuroprotective effect, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions for prevention and treatment of brain disease including them as effective ingredient are provided.

Abstract: The present invention provides an efficient method for mass-producing 2-hydroxy-5-(substituted)phenylalkylaminobenzoic acid derivative represented by the specific Chemical formula or its salt, particularly 2-hydroxy-5-[2-(4-trifluoromethylphenyl)ethylamino] benzoic acid or its salt.

Abstract: The present invention provides new derivatives of 4- or 5-aminosalicylic acid, and a pharmaceutical composition containing these derivatives of 4- or 5-aminosalicylic acid as active ingredients, useful for the treatment of intestinal diseases such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS) and for the prevention/treatment of colon cancer. More particularly, these derivatives comprise a hydrogen sulfide releasing moiety linked via an azo, an ester, an anhydride, a thioester or an amide linkage to a molecule of 4- or 5-aminosalicylic acid. Furthermore, the present invention provides a process for preparing these compounds and their use for treating IBD and IBS and the prevention/treatment of colon cancer.

Abstract: The present invention provides compositions and methods for prevention and prophylaxis of neurological diseases accompanied by neuronal death. The invention includes synthesis of 5-benzylamino salicylic acid (BAS) and its derivatives. BAS and its derivatives protect cortical neurons from toxic insults by N-methyl-D-aspartate, Zn2+, and reactive oxygen species. Thus, the present invention provides compositions and methods for treating stroke, traumatic brain and spinal cord injury, epilepsy, and neurodegenerative diseases that are accompanied by severe neuronal loss via excitotoxicity, Zn2+ neurotoxicity, and free radical neurotoxicity.

Abstract: In one aspect, the present invention relates to amino-salicylic-aminophenylpropionic compounds for the use in the treatment of the inflammatory component of the celiac disease. These compounds act by blocking the cytokines released in the celiac disease and are specifically useful in the treatment of cases refractory to the diet, in dietary errors and in the reduction of the celiac disease remission time.

Abstract: The present invention is related to a family of phenyl-prenyl-ether derivatives of formula (I), and to their use in the treatment of cognitive, neurodegenerative or neuronal diseases or disorders, such as Alzheimer's disease or 5 Parkinson's Disease. The present invention also relates to pharmaceutical compositions comprising the same. Further, the present invention is directed to the use of the compounds in the manufacture of a medicament for the treatment and/or prevention of a cognitive, neurodegenerative or neuronal disease or disorder.

Abstract: The present invention relates to cinnamic acid dimers, their preparation and the use thereof for treating neurodegenerative disease, which have excellent effect on enhancing the learning and memory-retention ability in vivo and have fewer side-effects by showing no hormone properties, even when administered for a long period of time, and thus which can be used for neurodegenerative disease including dementia.

Abstract: Fermentation of a nutrient medium with a eubacterium Streptomyces sp. yields a novel antibacterial compound of structural formula (I).

Abstract: Disclosed is a method for inhibition of necrosis induced by neurotrophin, and more specifically a method for inhibition of necrosis by administrating oxidative stress inhibitor and a method for simultaneous inhibition of necrosis and apoptosis by administrating oxidative stress inhibitor and neurotrophin. The oxidative stress inhibitor of the present invention can inhibit nerve cell necrosis induced by neurotrophin. Moreover, it can be used for protecting nerve cell damage connected with alzheimer disease, parkinson's disease, degenerating cerebropathia and promoting regeneration of the nerve cells by administrating oxidative stress inhibitor and neurotrophin.

Abstract: The present invention provides new derivatives of 4- or 5-aminosalicylic acid, and a pharmaceutical composition containing these derivatives of 4- or 5-aminosalicylic acid as active ingredients, useful for the treatment of intestinal diseases such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS) and for the prevention/treatment of colon cancer. More particularly, these derivatives comprise a hydrogen sulfide releasing moiety linked via an azo, an ester, an anhydride, a thioester or an amide linkage to a molecule of 4- or 5-aminosalicylic acid. Furthermore, the present invention provides a process for preparing these compounds and their use for treating IBD and IBS and the prevention/treatment of colon cancer.

Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.

Abstract: A new class of non-glycosidic and non-peptidic inhibitors of selectins with low molecular weight according to the general formula 1 is described, as well as methods for their production. These compounds represent a new class of non-toxic, in vivo anti-inflammatory effective inhibitors of selectins, and do not exhibit the disadvantages of the glycosidic inhibitor complexes, and are furthermore more potent in vitro, compared to the known drug bimosiamose. Furthermore, medicaments containing the compounds and their uses in the treatment of diseases are described.

Abstract: The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.