Abstract:
The present invention provides benzothiadiazine and chroman derivatives and particularly diazoxide and cromakalim derivatives for use in treating glaucoma, retinopathy, treating age related macular degeneration, treating, stabilizing and/or inhibiting blood and lymph vascularization, and reducing intraocular pressure by administering a pharmaceutically effective amount of a prodrug disposed in an ophthalmically acceptable carrier to the eye, wherein the prodrug specifically modulates a KATP channel to reduce an intraocular pressure.
Abstract:
A cyclic polycarboxylic acid anhydride, a polycarboxylic acid, or a mixture of them is allowed to react with hydroxylamine or a salt thereof in an organic solvent under dewatering conditions to yield a corresponding cyclic N-hydroxyimide compound. The cyclic polycarboxylic acid anhydride can be, for example, succinic anhydride or glutaric anhydride. The polycarboxylic acid can be, for example, succinic acid, glutaric acid, or adipic acid. In this process, the reaction is preferably carried out using an organic solvent capable of undergoing azeotropy with water as all or part of a reaction solvent while removing water from the reaction system by azeotropy with the organic solvent. This process produces a cyclic N-hydroxyimide compound in a good yield from any of a cyclic polycarboxylic acid anhydride and a polycarboxylic acid.
Abstract:
The invention relates to a composition containing a particulate solid, a plastic material (such as a thermoplastic polymer) and a compound capable of having dispersant properties. The compound may be obtained/obtainable by reacting a fatty acid with either (i) a hydroxy-C4-5-alkylene carboxylic acid, or (ii) a lactone. The invention further relates to novel compounds, and the use of the compound as a dispersant.
Abstract:
Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described.
Abstract:
The present invention provides for a method for inhibiting growth of a bacterium which consists essentially of contacting the bacterium with a compound having the structure: 1 wherein each of R1, R2, R3, R4, R5 and R6 may be independently H, F, Cl, Br, I, nullOH, nullOR7, nullCN, nullCOR7, nullSR7, nullN(R7)2, nullNR7COR8, nullNO2, null(CH2)pOR7, null(CH2)pX(R7)2, null(CH2)pXR7COR8, a straight chain or branched, substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, C3-C10 cycloalkenyl, thioalkyl, methylene thioalkyl, acyl, phenyl, substituted phenyl, or heteroaryl; wherein a linkage to the benzene ring may alternatively be nullNnull, nullSnull, nullOnull or nullCnull; wherein R7 or R8 may be independently H, F, Cl, Br, I, nullOH, nullCN, nullCOH, nullSH2, nullNH2, nullNHCOOH, null(CH2)pOH, null(CH2)pX(CH2), null(CH2)pXCOH, a straight chain or branched, substituted or unsubstituted C1-C10 alkyl, thioalkyl, methylene thioalkyl, acyl, phenyl, substituted phenyl, or heteroaryl; wherein A may be nullN2null, nullNHnull, nullCnullCnullCH2null, nullCnullCnullC2HOHnull, nullCnullCnullCH2null, nullCH2nullCH2nullOnull, nullCH2nullCH2nullCH2nullOnull, nullSnull, nullS(nullO)2null, nullCnullOnull, nullCnullOnullOnull, nullNHnullCnullOnull, nullCnullOnullNHnull; and wherein Q, p, N and X may independently be an integer from 1 to 10, or if Q is 1 A may be a (C1-C10)-alkyl chain, (C1-C10)-alkenyl chain or (C1-C10)-alkynyl chain which can optionally be interrupted 1 to 3 times by nullOnull or nullSnull or nullNnull; or a pharmaceutically acceptable salt or ester thereof, which compound is present in a concentration effective to inhibit growth of the bacterium. A may be an (C1-C10)-alkylene chain, (C1-C10)-alkyl chain, or (C1-C10)-alkynyl chain which is branched or unbranched, substituted or unsubstituted and can optionally be interrupted 1 to 3 times by nullOnull or nullSnull or nullNnull.
Abstract:
A method and composition for sterilizing articles that are contaminated with infectious prion protein, such as surgical instruments, kitchen utensils, laboratory tools, etc., comprising the steps of: (a) heating the articles to be treated at a moderate temperature well below the incineration temperature of said infectious prion protein, wherein said moderate temperature is sufficient to enhance the proteolytic susceptibility of infective prion protein associated with said articles; and (b) exposing the heated articles to a proteolytic enzyme that is effective for at least partial reduction of the infective protein prion associated with said articles under said moderate temperature.
Abstract:
Novel compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
Abstract:
Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
Abstract:
The present invention provides methods for improving the production of recombinant proteins through the use of pharmacological chaperones for the recombinant proteins. As exemplified by the present invention, the binding of a pharmacological chaperone to a recombinant protein expressed by a cell can stabilize the protein and increase export of the protein out of the cell's endoplasmic reticulum, and increase secretion of the protein by the cell.