Abstract: The present invention relates to a compound of formula (I), wherein: X is methyl or chlorine; R1 is methyl or chlorine; R2 is hydrogen, methyl, ethyl, n-propyl, cyclopropyl, vinyl, ethynyl, fluorine, chlorine, bromine, C1-C3alkoxy, C1-C2-fluoroalkoxy, C1-C2alkoxy-C1-C3alkoxy- or C1fluoroalkoxy-C1-C3alkoxy-; and Y is O, S, S(O), S(O)2, N(C1-C2alkyl), N(C1-C2alkoxy), C(O), CR8R9 or —CR10R11CR12R13—; and G, R3, R4, R5 and R6 are as defined herein; wherein the compound of formula (I) is optionally present as an agrochemically acceptable salt thereof. These compounds are suitable for use as herbicides. The invention therefore also relates to a method of controlling weeds, especially grassy monocotyledonous weeds, in crops of useful plants, comprising applying a compound of formula (I), or a herbicidal composition comprising such a compound, to the plants or to the locus thereof.

Abstract: 3-(3-Chloro-1H-pyrazol-1-yl)pyridine is prepared by cyclizing 3-hydrazinopyridine-·dihydrochloride with acrylonitrile to provide 1-(pyridin-3-yl)-4,5-dihydro-1H-pyrazol-3-amine, by oxidizing to provide 3-(3-amino-1H-pyrazol-1-yl)pyridine, and by converting the amino group to a chloro group by a Sandmeyer reaction.

Abstract: The invention relates to substituted pyridine compounds of Formula (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R1a, A1, A2, E, G, Z1, and Z2 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.

Abstract: Provided is a compound represented by the following formula (1) or a salt thereof, which has an SSTR5 antagonistic action: wherein each symbol has the same definition as in the specification.

Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.

Abstract: The present invention relates to a method for preparing the pyripyropene compound of the formula (I) which method comprises the following steps: i) subjecting a pyripyropene compound of formula Pyripyropene A to an alkaline hydrolysis to yield a 1,7,11 -trideacetylpyripyropene A, ii) reacting 1,7,11-trideacetylpyripyropene A obtained in step i) with cyclopropane carbonyl chloride to yield a raw product containing the pyripyropene compound of formula (I); iii) subjecting the raw product of step ii) to crystallization to yield a crystalline pyripyropene compound of formula (I) and a mother liquor; and iv) recycling the mother liquor or a pyripyropene compound containing fraction thereof to the alkaline hydrolysis of step i).

Abstract: A process for increasing the overall yield of pyridine or its alkyl pyridine derivatives during a base synthesis reaction is disclosed. The process comprises reacting a C2 to C5 aldehyde, a C3 to C5 ketone or a combination thereof, with ammonia and, optionally, formaldehyde, in the gas phase and in the presence of an effective amount of a particulate catalyst comprising a zeolite, zinc, a binder, and clay and optionally a matrix, wherein the catalyst has a L/B ratio of about 1.5 to about 4.0. Preferably, the zeolite is ZSM-5. A process for enhancing the catalytic activity of a zinc and zeolite containing catalyst to increase the overall yield of pyridine and/or its derivatives during a base synthesis reaction is also disclosed.

Abstract: The present invention concerns particular fluorenes, the use of the compound in an electronic device, and an electronic device containing at least one of these compounds. The present invention further concerns a method for producing the compound and a formulation and composition containing one or more of the compounds.

Abstract: The present invention relates to the crystalline mono mesylate monohydrate salt of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide in a definite particle size range, particle size distribution and a specific surface area range, which has demonstrated increased long term stability and release kinetics from pharmaceutical compositions, as well as to pharmaceutical compositions containing said crystalline N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mono mesylate monohydrate having the afore-mentioned particle size range, particle size distribution and specific surface area range.

Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof: I useful as HIV attachment inhibitors.

Abstract: A process is provided for preparing 4-(8-(2-chlorophenoxy)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)bicyclo[2.2.1]heptan-1-ol and novel intermediates used in the process. The compound is a 11-beta hydroxysteroid dehydrogenase type I inhibitor which exhibits activity in the treatment of various metabolic diseases.

Abstract: The present invention belongs to the field of pharmaceutical chemistry, and disclosed are two crystal forms of Childamide, that is, Chidamide crystal form A and Chidamide crystal form B, and the method for preparing the new crystal forms of Chidamide. The Chidamide crystal form A and Chidamide crystal form B of the present invention can be used for preparing drugs for treating diseases related to cell differentiation and proliferation.

Abstract: The invention relates to polymorphs of deuterated omega-diphenylurea or salts thereof. In particular, the invention provides polymorphs of 4-(4-{3-[4-chloro-3-(trifluoromethyl)phenyl)-ureido]-phenoxy}-2-(N-1?,1?,1?-trideutero-methyl)picolinamide or its salt, namely, polymorphs of the compound as shown in formula (I) or its salt. The polymorphs are suited for preparing the pharmaceutical composition used for inhibiting phosphokinase (such as raf kinases).

Abstract: The present invention provides a process for the preparation and purification of apixaban.

Abstract: The present invention relates to compound of general formula (1) wherein R1 represents C6-C10 aryl comprising one or two fused rings, wherein from 2 to 5 carbon atoms may be replaced with a heteroatom selected from O, S and NR6, and eventually substituted with from 5 to 11 substituents selected from R6, halo, CN, NO2, CF3, OCF3, COOR6, OCOR6, SO2NR6R7, CONR6R7, NR6R7, NR6COR7, (CH2)p—NR6R7, (CH2)p—OR6 and (CH2)pSR6, as well as, if appropriate, their pharmaceutically acceptable salts and/or isomers, tautomers, solvates or isotopic variations thereof. The compounds are useful for the treatment of cancers.

Abstract: A process for preparation of a sodium salt of (2S,5R)-2-carboxamido-7-oxo-6-sulfooxy-1,6-diaza-bicyclo[3.2.1]octane is disclosed which is comprising the amidation of a compound of Formula (II) to obtain a compound of Formula (III).

Abstract: An object of the present invention is to provide a novel endoparasite control agent as a parasiticide, an antiprotozoal or the like. Provided is an endoparasite control agent comprising a carboxamide derivative represented by the general formula (I): (wherein Het represents a 5- or 6-membered heterocyclic group), or a salt thereof as an active ingredient.

Abstract: The present invention relates to a process for preparing an N-substituted 1H-pyrazole-5-carboxylate compound of the formula (I-A) comprising the steps of i) deprotonating a compound of the formula (II) in which the variables R1, R2 and r are each as defined in the description and the claims, with a magnesium-organic base having a carbon bound magnesium; and ii) subjecting the product obtained in step (i) to a carbonylation by reacting it with a reagent selected from the group consisting carbon dioxide or a carbon dioxide equivalent, to obtain a compound of formula (I-A); and it relates to further conversions to yield a N-substituted 1H-pyrazole-5-carbonyl chloride compound of the formula (I)

Abstract: The present application relates to novel pyridyloxyalkylcarboxamides of the formula (I) and to their use as endoparasiticides against endoparasites in animals or humans, and to their use as nematicides for controlling phytopathogenic nematodes, and furthermore to endoparasiticides and nematicides comprising pyridyloxyalkylcarboxamides.

Abstract: An object of the present invention is to provide a novel endoparasite control agent as a parasiticide, an antiprotozoal or the like. Provided is an endoparasite control agent comprising a carboxamide derivative represented by the general formula (I): or a salt thereof as an active ingredient.