Abstract: The invention relates to novel indazole derivatives as cited in claim 1, which are inhibitors of CHK1, CHK2 and SGK kinases and can be used to treat cancer and other diseases.

Abstract: A novel epoxy compound represented by the following general formula (I), and a production process thereof, is provided: Y—(CH2)3—Si(OR1)nR23-n??(I) (wherein, Y is represented by any of the following formulas: wherein, R1 and R2 represent alkyl groups having 1 to 5 carbon atoms, n represents an integer of 1 to 3, R3 and R4 represent hydrogen atoms, alkyl groups having 1 to 6 carbon atoms or trialkylsilyl groups having 1 to 4 carbon atoms, R5 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or a trialkylsilyl group having 1 to 4 carbon atoms, R6 to R12 represent hydrogen atoms, alkyl groups having 1 to 6 carbon atoms or trialkylsilyl groups having 1 to 4 carbon atoms, and R13 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a trialkylsilyl group having 1 to 4 carbon atoms or an aryl group).

Abstract: A compound comprising or a pharmaceutically acceptable salt thereof, or a prodrug thereof is disclosed herein. Y, A, and B are as described herein. Methods, compositions, and medicaments related to these compounds are also disclosed.

Abstract: This invention relates to novel isopentylcarboxanilides of the formula (I) in which L, R1, R3 and A are as defined in the disclosure, to a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.

Abstract: An optically active 3-aminopyrrolidine (3AP) salt has a high optical purity which is useful as an intermediate in an industrial production method of an optically active 3AP, an efficient method for producing it, and an efficient industrial method for optical resolution of 3AP. Optical resolution of 3AP is efficiently carried out by reacting racemic 3AP with optically active 2-methoxyphenylacetic acid in the presence of a mineral acid such as hydrochloric acid in an aqueous solvent, followed by separation of the resulting diastereomer salt constituted by 1 mole of optically active 3AP and 2 moles of optically active 2-methoxyphenylacetic acid.

Abstract: The present invention provides a process for the preparation of imidazoles by reacting a cyano compound with a silylalkylisocyanide compound. Such imidazoles are useful pharmacologically-active compounds and/or intermediates for the preparation of pharmacologically-active compounds.

Abstract: The present invention relates to a compound of the following formula 1, pharmaceutically acceptable salt and isomer thereof effective as agonist of melanocortin receptor, and an agonistic composition of melanocortin receptor comprising the same as active ingredient.

Abstract: The present invention describes novel methods for using 9-deoxy-2?,9-?-methano-3-oxa-4,5,6-trinor-3,7-(1?,3?-interphenylene)-13,14-dihydro-prostaglandin F1 (also known as Treprostinil) or its derivative, or a pharmaceutically acceptable salt thereof, for the treatment and/or prevention of foot ulcers in subjects with diabetic neuropathy. The invention also relates to kits for treatment and/or prevention of foot ulcers, comprising an effective amount of Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides a compound of the formula (Cat)+z[M++(5-nitro-1H-tetrazolato-N2)?x(H2O)y] where x is 3 or 4, y is 2 or 3, x+y is 6, z is 1 or 2, and M++ is selected from the group consisting of iron, cobalt, nickel, copper, zinc, chromium, and manganese, and (Cat)+ is selected from the group consisting of ammonium, sodium, potassium, rubidium and cesium. A method of preparing the compound of that formula is also disclosed.

Abstract: Compounds of the formula (I), in which R1, R2, R3a, R3b, R3c and R3d have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.

Abstract: Process for the preparation of a carboxamide derivative of formula (I) or a salt thereof Intermediates for preparing this compound are also provided.

Abstract: Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.

Abstract: The present invention is directed to 1,3,4-oxadiazalones, compounds of formula I and their pharmaceutically acceptable salts stereoisomers, tautomers, or solvates thereof. Novel compounds include those of formula I, in which radicals are as defined herein. The compounds of this invention are modulators of PPARdelta and therefore useful as pharmaceutical agents, especially for the treatment of demyelinating diseases and disorders of fatty acid metabolism and glucose utilization.

Abstract: It is disclosed a process for the preparation of 2-(4-hydroxy-3-morfolinyl)-2-cycloesenone (BTG-1675A) comprising the steps of: i) reacting N-hydroxymorpholine with cycloesanone in the presence of an oxidation agent thus obtaining an isoxazolidine of Formula IV; and ii) converting the isoxazolidine of Formula IV into 2-(4-hydroxy-3-morfolinyl)-2-cycloesenone. Advantageously, the oxidation agent of the step i) is selected from the group consisting of metal oxides, esters and amides of the azodicarboxylic acid and the step ii) of conversion is carried out by basic catalysis followed by trituration in an aromatic hydrocarbon, preferably toluene. The process disclosed allows to obtain BTG-1675A according to the invention in an amount of hundreds of grams and on an industrial scale. The invention further concerns a new process for preparing hydroxylamines, particularly N-hydroxymorpholine, which is used in the process for preparing BTG-1675A.

Abstract: Provided herein are isolated compounds of formula I: processes for their preparation and isolation, as well as pharmaceutical compositions which comprise these therapeutic agents, and methods of use therefore the treatment and/or control of conditions associated with or mediated by effects of histone deacetylase.

Abstract: The present invention provides an improved process for the purification of ropinirole hydrochloride. The process includes (i) treating ropinirole hydrochloride with sodium dithionate and charcoal in suitable alcoholic solvent; (ii) triturating the ropinirole hydrochloride obtained in step (i) with ethanol; (iii) reacting the triturated solid with base in water immiscible solvent and isolating the free base; and (iv) treating the free base obtained in step (iii) with ethanolic HCl to give ropinirole hydrochloride.

Abstract: Methods of inhibiting the cytokine or biological activity of Macrophage Migration Inhibitory Factor (MIF) comprising contacting MIF with a compound of formula (I) are provided. The invention also relates to methods of treating diseases or conditions where MIF cytokine or biological activity is implicated comprising administration of compounds of formula (I), either alone or as a part of combination therapy. Novel compounds of formula (I) are also provided for.

Abstract: In a process for producing 1-substituted-3-fluoroalkyl-pyrazole-4-carboxylate (3) by a reaction of 2-alkoxymethylenefluoroacylacetate (1) and hydrazine (2), the reaction is conducted in the presence of a base and water, to produce 1-substituted-3-fluoroalkylpyrazole-4-carboxylate (3) with high selectivity and yield. This novel process enables to produce 1-substituted-3-fluoroalkylpyrazole-4-carboxylate (3), which is useful as an intermediate for pharmaceuticals and agrochemicals, with high selectivity and yield by simple and safe operations.

Abstract: A process for the preparation of indoles, e.g. 1,2,3,9-tetrahydro-carbazol-4-one and derivatives thereof.

Abstract: Provided herein are compounds or hypochlorous acid probes which can be used as reagents for measuring, detecting and/or screening, directly or indirectly, hypochlorous acid or hypochlorite. Provided also herein are methods that can be used to measure, directly or indirectly, the amount of hypochlorous acid or hypochlorite in chemical samples and biological samples such as cells and tissues in living organisms. Specifically, the methods include the steps of contacting the hypochlorous acid probes disclosed herein with the samples to form one or more fluorescent compounds, and measuring fluorescence properties of the fluorescent compounds. Provided also herein are high-throughput screening fluorescent methods for detecting or screening hypochlorous acid or compounds that can increase or decrease, directly or indirectly, the level of hypochlorous acid or hypochlorite in chemical and biological samples.