- SMALL MOLECULE INHIBITORS OF BACTERIAL TOXINS
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Described herein are compounds and compositions for use in treatment or prevention of an inflammatory bowel disease, gastrointestinal cancer, or a systemic bacterial infection in a subject in need thereof. The subject may be colonized by one or more pathogenic bacterial strains such as B. fragilis, E. faecalis, or C. perfringens. In certain aspects, the disclosure provides a method of diminishing the pathogenic effects of these bacterial strains by administering a compound that binds to and/or inhibits one or more toxins produced thereby.
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- INDOLE AND AZAINDOLE HALOALLYLAMINE DERIVATIVE INHIBITORS OF LYSYL OXIDASES AND USES THEREOF
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The present invention relates to novel compounds which are capable of inhibiting certain amine oxidase enzymes. These compounds are useful for treatment of a variety of indications, e.g., fibrosis, cancer and/or angiogenesis in human subjects as well as i
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Paragraph 0285
(2017/09/05)
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- Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in compositions and use thereof
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The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.
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- Identification of human T2R receptors that respond to bitter compounds that elicit the bitter taste in compositions, and the use thereof in assays to identify compounds that inhibit (block) bitter taste in composition and use thereof
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The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.
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- INHIBITORS OF HISTONE DEACETYLASE FOR THE TREATMENT OF DISEASE
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Disclosed herein are carbonyl compounds of having the structural formula: or a salt, ester, or prodrug thereof, Methods and compositions are disclosed for treating disease states including, but not limited to cancers, autoimmune diseases, tissue damage, c
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Page/Page column 21
(2010/11/27)
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- 4-OXY-N-[1 ,3,4]-THIADIAZOL-2-YL-BENZENE SULFONAMIDES, PROCESSES FOR THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS
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The invention relates to 4-oxy-N-[1 ,3,4]-thiadiazol-2-yl-benzene sulfonamides and to their physiologically acceptable salts and physiologically functional derivatives showing PPARalpha, PPARdelta and PPARgamma agonist activity. What is described are comp
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Page/Page column 68-69
(2008/06/13)
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- INDOLE DERIVATIVE COMPOUNDS AND DRUGS CONTAINING THE COMPOUNDS AS THE ACTIVE INGREDIENT
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An indole derivative compound represented by formula (I) (wherein the symbols in the formula are as mentioned in the specification) and a salt thereof Since the compounds represented by formula (I) binds to PGD2 receptors and shows antagonistic activity, they are believed to be useful for prevention and/or treatment of diseases such as allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, systemic mast cell activating disorder, anaphylaxis shock, airway contraction, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis, urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleep disorder) which are generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, autoimmune disease, chronic articular rheumatism, pleuritis, ulcerative colitis and irritable bowel syndrome.
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Page/Page column 121
(2010/02/14)
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- CARBOXYOIC ACID COMPOUNDS AND DRUGS CONTAINING THE COMPOUNDS AS THE ACTIVE INGREDIENT
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A carboxylic acid compound represented by formula (I): (meanings of the symbols in the formula are as mentioned in the specification) and a pharmaceutical agent comprising the compound. Since the compound represented by formula (I) binds to a DP receptor and shows antagonistic activity for the DP receptor, it is useful for prevention and/or treatment of diseases such as allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like.
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- METABOLITES OF PRINOMASTAT AND THEIR SYTHESIS
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Metabolites of a matrix metalloproteinase inhibitor prinomastat their synthesis composition, and method of using same. These metabolites are: (3S)-N-hydroxy-4-(4-((1-oxy-pyrid-4-yl)oxy)benzenesulfonyl)-2,2-dimethyl-tetrahydro-2H-1,4-thiazine-3-carboxamide
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- Structure-reactivity correlations in the dissociative hydrolysis of 2′,4′-dinitrophenyl 4-hydroxy-X-benzenesulfonates
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The hydrolysis reactions of several title esters in water at 60°C follow the rate law kobs = (ka + kb[OH-])/(1 + αH/Ka), where Ka is the ionization constant of the hydroxy group of the ester and kb is the second-order rate constant for the SN2(S) attack of hydroxide ion on the ionized ester. Hammett and Br?nsted correlations are consistent with a previous proposal that the mechanism related to ka is dissociative. An unusual relationship between ka values and redox equilibrium constants for substituted quinones is found to hold: this finding further supports the dissociative nature of the pathway related to ka.
- Cevasco, Giorgio,Thea, Sergio
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p. 6814 - 6817
(2007/10/03)
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- Oxime sulfonates containing reactive groups
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Oxime sulfonates of formula I STR1 wherein Y is a polymerizable unsaturated group or epoxide group or an --OH, --NHR5, --COOH, COOR6, --COCl, --CH2 Hal, --SO2 Cl or --NCO group, Z is an (x+y)-valent connecting member, R1 and R2 are monovalent organic radicals, m is 0 or 1, x is 1 or 2 and y is 1 or 2, can be converted into polymers which can be thermally or photochemically dissociated to form free sulfonic acid groups. Said polymers can therefore be used as photoresists which can be developed with aqueous alkalis.
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