Abstract: The present invention provides an aryl- or heteroaryl compound represented by the formula (Ia) or (Ib) wherein each symbol is as defined in the specification, or a salt thereof, or a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier. The compound has superior acid secretion inhibitory action, an antiulcer activity and the like.

Abstract: The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula I wherein R1 is and A1, A2, A3, A4, X, Z, Z?, R1, R2, R3, R4, R5 and R6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.

Abstract: The present invention relates to a novel benzenedicarboxamide derivative and the use thereof as an insecticide having the formula (I) wherein the chemical groups W1 to W9, and R1 to R3 are as defined here-in.

Abstract: A process for the manufacture of a cyclic compound of formula (I) which comprises (a) adding an acid halide of formula R1—C (O)—X, to a vinyl ether of formula (II): CH2?CH—OR2, to produce an addition product, and (b) reacting the addition product with a compound of formula (III): Y-A-Z; wherein R1 is a halogenated alkyl group; wherein X is fluorine, chlorine, or bromine; wherein R2 is an alkyl group, an aralkyl group, or an aryl group; wherein Z and Y designate independently carbon or a heteroatom; and wherein A is a linking group between Z and Y comprising 0, 1, 2 or 3 atoms in the cycle.

Abstract: This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.

Abstract: This invention relates to a combination product comprising a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7 and R9 are as described herein, and one or more further biologically active compounds as described herein, particularly anti-parasitic agents.

Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

Abstract: Compounds of formula (I) where X1, C1, and D1 are defined herein, are inhibitors of polo-like kinases. The compounds of formula (I) are useful for treatment of diseases of cellular proliferation, such as, for example, cancer.

Abstract: Novel imidazolopyridine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, ECM degradation, joint degradation and/or inflammation, and others.

Abstract: The present invention relates to novel compounds having a xanthine oxidase inhibitory effect and an uricosuric effect and pharmaceutical compositions comprising the same as an active ingredient. That is, the present invention relates nitrogen-containing heterocyclic compounds represented by the following general formula (I): wherein Y1 represents N or C(R4); Y2 represents N or C(R5); R4 and R5 independently represent an alkyl group, a hydrogen atom etc.; one of R1 and R2 represents an optionally substituted aryl group, an alkoxy group or an optionally substituted heterocyclic group; the other of R1 and R2 represents a haloalkyl group, a cyano group, a halogen atom etc.; and R3 represents a 5-tetrazolyl group or a carboxy group, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising the same as an active ingredient.

Abstract: This invention comprises antineoplastic curcumin derivatives and methods of preparation and use thereof. Particular reference is made to the following isomeric compounds wherein R1, R2, and R3 are selected from the group consisting of H, OH, OCH3, and COOH.

Abstract: This invention is directed to a cannabinoid modulator compound of formula (I): or a form thereof, and methods for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.

Abstract: There is provided a process for preparation of celecoxib by reacting 4,4,4-trifluoro-1-[4-(methyl)phenyl]butane-1,3-dione with 4-sulphonamidophenylhydrazine or its salt in a solvent medium that contains an alkyl ester. There is also provided a process for the purification of celecoxib using aromatic hydrocarbon solvents.

Abstract: This invention relates to novel intermediates used in the preparation of iodopyrazolylcarboxanilides of the formula (I) in which R1, R2, R3, R4, R5, R6 and Z are as defined in the disclosure, and to the preparation of such intermediates.

Abstract: The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A2 and R1, R2, R3, R4a, R4b, R5, R6, Ar, X1, X2, X4, X4 and X5 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.

Abstract: There is provided a novel luminescent metal complex. A metal complex having a composition of [(PtII)2(MI)2(X)2(L)4(LH)2], where MI denotes AgI, AuI or CuI, X denotes Cl, Br or I, L denotes a structure represented by the formula (1), and LH denotes a structure represented by the formula (2).

Abstract: A compound of general formula (I): A process for preparing this compound. A fungicide composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.

Abstract: The present invention provides a fluorine-containing pyrazolecarbonitrile derivative and a method for producing the same, and a fluorine-containing pyrazolecarboxylic acid derivative obtained by using the fluorine-containing pyrazolecarbonitrile derivative and a method for producing the same. A fluorine-containing acyacrylonitrile derivative prepared from a fluoroacyl derivative and an aminoacrylonitrile derivative, is reacted with a hydrazine derivative to produce a fluorine-containing pyrazolecarbonitrile derivative represented by Formula (1). In Formula (1), Rf represents an alkyl group having 1 to 6 carbon atoms and substituted with at least one fluorine atom; R1 represents an alkyl group having 1 to 6 carbon atoms and R2 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or the like. The fluorine-containing pyrazolecarbonitrile derivative represented by Formula (1) is reacted with water to produce a fluorine-containing pyrazolecarboxylic acid derivative.

Abstract: Processes are provided for combining nonsubstituted hydrazine (N2H4), a strong acid, alcohol, and tetraalkoxypropane to produce N-alkylpyrazole.

Abstract: The present invention relates to heteroaroyl-substituted serineamides of the formula I in which the variables A and R1 to R6 are as defined in the description, and to their agriculturally useful salts, to processes and intermediates for their preparation, and to the use of these compounds or of the compositions comprising these compounds for controlling unwanted plants.

Abstract: The present invention relates to compounds corresponding to the formula (I): In which R1, R2, R3, R4 and R5 are as described herein. The invention also relates to the method of preparation of said compounds and their application in therapeutics.

Abstract: The invention relates to imidazo[1,5-a]quinoxaline derivatives having Formula IIa: to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10 (PDE10), as active compounds for treating central nervous system diseases of mammals, including humans.

Abstract: The present invention relates to a pyrazole compound having potent CB1-antagonizing activity, having the following formula [I]: wherein R1 and R2 are the same or different and an optionally substituted aryl group etc., R3 is an alkyl group etc., E is one of the following groups of the formula (i) to (iv): Q1 is a single bond, an alkylene group or a group of the formula: —N(R7)—, R7 is a hydrogen atom or an alkyl group, Q2 is a single bond, an oxygen atom or an alkylene group, R4 is a cycloalkyl group, a group of the formula: —N(R5)(R6) etc., one of R5 and R6 is a hydrogen atom or an alkyl group and the other is an alkyl group, a group of the formula: —N(R8)(R9) etc., D is an oxygen atom etc., RA1 is an amino group etc., RA2 is an optionally substituted aliphatic heterocyclic group, R is an alkyl group optionally substituted by one to three halogen atom(s) etc., one of R8 and R9 is a hydrogen atom or an alkyl group and the other is an alkyl group etc., or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides kinase inhibitors of Formula I:

Abstract: The invention relates to substituted phenylureas and phenylamides, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.

Abstract: Compounds of formula wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases.

Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs).

Abstract: Disclosed is an aryl-substituted nitrogen-containing heterocyclic compound represented by the formula (I) below or a pharmaceutically acceptable salt thereof. This compound serves as nociceptin receptor antagonist and is useful as a pharmaceutical agent for treating diseases associated with a nociceptin receptor. (I) [in the formula, A1, A2 and A3 independently represent a carbon atom or a nitrogen atom, and one or two of A1, A2 and A3 represent a carbon atom; R1 represents a lower alkyl group or the like; R2 represents a phenyl group which may be substituted with a halogen atom or the like; R3 represents a hydrogen atom, a lower alkyl group or the like; and R4 represents a lower alkyl group or the like.

Abstract: The invention is amido-borate compounds containing one or more anionic amido-borate moieties comprising an organoborate anion wherein the boron atom is bonded to a nitrogen atom of ammonia or an organic compound containing one or more nitrogen atoms, such as a hydrocarbyl amine, a hydrocarbyl polyamine, or an aromatic heterocycle containing one or more nitrogen atoms, and a cationic counter ion.

Abstract: Provided is a triarylcarboxylic acid derivative, or an isomer, a prodrug, a hydrate, a solvate, a polymorph, or a pharmaceutically acceptable salt thereof, represented by the following general formula (I): wherein A is an optionally substituted aryl or heteroaryl, and B is an optionally substituted monocyclic heteroaryl; and a pharmaceutical composition comprising the same and a pharmaceutically acceptable carrier. The triarylcarboxylic acid derivative (I) exhibits potent xanthine oxidase inhibiting action and is therefore useful as a therapeutic agent for preventing or treating hyperuricemia, gout, inflammatory bowel disease, diabetic nephropathy and diabetic retinopathy.

Abstract: A process for the palladium-catalyzed coupling of terminal alkynes with heteroaryl tosylates and heteroaryl benzenesulfonates The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein D, J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process of heteroaryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional heteroaryl-1-alkynes of the formula I.

Abstract: The present invention relates to novel processes for the production of compounds of formula (I) wherein Hal and Hal? are independently Cl or F, and R1 is H, Cl or F.

Abstract: To provide a process for preparing an arylamine highly selectively and highly efficiently, which is also industrially superior without a fear of a side reaction when a strong base is employed. An aryl compound having an active group is reacted with an amine compound in the presence of a base by means of a catalyst for producing an arylamine which comprises a palladium compound having a tertiary phosphine group and a phase-transfer catalyst.

Abstract: This invention is directed to a tetrahydro-2H-indazole pyrazole cannabinoid modulator compound of formula (I): or a form thereof, wherein p, R1, R2 and Ar are as herein described and * represents a chiral center, and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.

Abstract: The present invention is directed to compounds of Formula (I), and to pharmaceutically acceptable salts thereof, their synthesis, and their use as Raf inhibitors.

Abstract: The invention relates to novel aromatic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, b their use as medicaments and to medicaments comprising them.

Abstract: The present invention relates to compounds useful as inhibitors of protein kinase, represented by Structural Formula (I): wherein the variables in Structural Formula (I) are as described herein. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.

Abstract: Disclosed are compounds of the formula: And pharmaceutically acceptable salts thereof, wherein the variables are as defined herein, which are useful in activating PPAR? and in treating atherosclerosis hypercholesterolemia, primary hypercholesterolemia or mixed dyslipidemia, hypertriglyceridemia, Frederickson Types IV and V hyperlipidemia. Pharmaceutical compositions, intermediates useful in the preparation of the compounds of formula I and methods of making the compounds of formula I are also disclosed.

Abstract: Provided are 1-aryl-5-alkyl pyrazole compounds, of formula (I): wherein: R1 is hydrogen, cyano, halogen, R8, formyl, —C(O)R8, —C(O)OR8, —C(O)NR9R10, or —C(S)NH2; R2 is R8 or —S(O)mR11; R3 is methyl, ethyl or C1-C4 haloalkyl; R4, R5 and R7 are independently hydrogen, halogen, alkyl, haloalkyl, cyano or nitro; R6 is halogen, alkyl, haloalkyl, alkoxy, haloalkyloxy, cyano, nitro, —C(O)R12, —S(O)nR12 or SF5; Z is a nitrogen atom or C—R13; R8 is alkyl, haloalkyl, cycloalkyl or halocycloalkyl; R9 is hydrogen, alkyl, haloalkyl or alkoxy; R10 is hydrogen, alkyl, haloalkyl or alkoxy; R11 is alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl or cycloalkyl; R12 is alkyl or haloalkyl; R13 is hydrogen, halogen, cyano, nitro, alkyl, haloalkyl, alkoxy or haloalkoxy; m is 0, 1 or 2; and n is 0, 1 or 2; or a salt thereof, the method of making compounds of formula (I) and the use of these compounds against ectoparasites, endoparasites and pests.

Abstract: This invention relates to novel pyrazole derivatives that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels.

Abstract: A method for preferentially inhibiting release of pro-inflammatory cytokines over release of anti-inflammatory cytokines using a fused pyrazolyl compound of formula (I): A is R or in which R is H, alkyl, aryl, cyclyl, heteroaryl, or heterocyclyl; each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, or pyrrolyl; each of R1, R2, R3, R4, R5, and R6, independently, is R?, nitro, halogen, —C(O)—OR?, —C(O)—SR?, —C(O)—NR?R?, —(CH2)mOR?, —(CH2)mSR?, —(CH2)mNR?R?, —(CH2)mCN, —(CH2)mC(O)—OR?, —(CH2)mC(O)H, or R1 and R2 together, R3 and R4 together, or R5 and R6 together are —O(CH2)nO—, in which each of R? and R?, independently, is H, alkyl, cyclyl, aryl, heteroaryl, heterocyclyl; and m is 0, 1, 2, 3, 4, 5, or 6; and n is 1, 2, or 3. This invention also covers a method of inhibiting activity of NF-?B with such a compound.

Abstract: The present invention relates to a process for preparing N-substituted (3-dihalomethylpyrazol-4-yl)carboxamides of the formula (I) in which R1 is optionally substituted phenyl or C3-C7-cycloalkyl, R1a is hydrogen or fluorine, or R1a together with R1 is optionally substituted C3-C5-alkanediyl or C5-C7-cycloalkanediyl, R2 is C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or C1-C4-alkoxy-C1-C2-alkyl, X is F or Cl and n is 0, 1, 2 or 3; which comprises A) providing a compound of the formula (II) in which X is F or Cl, Y is Cl or Br and R2 has one of the meanings given above and B) reacting a compound of the formula (II) with carbon monoxide and a compound of the formula (III) in which R1, R1a and n have one of the meanings given above; in the presence of a palladium catalyst; to intermediates used for the preparation according to the process according to the invention, and also to processes for their preparation.

Abstract: Compounds of Formula (I) wherein R1 is a cycloalkylsulphonyl group, or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.

Abstract: Compounds of formula I wherein R1, R2, R4, R5, A, B, D and n are as defined, and pharmaceutically acceptable salts thereof, processes for their preparation, their use as pharmaceuticals and pharmaceutical compositions comprising them.

Abstract: The invention relates to the use of selective phosphodiesterase 9A (PDE9A) inhibitors for producing medicaments for improving perception, concentration, cognitive processes, learning and/or memory.

Abstract: The invention is a system for initiating free radical polymerization comprising: a) in one part, one or more amido-borate compounds containing one or more anionic amido-borate moieties comprising an organoborate wherein the boron atom is bonded to a nitrogen atom of ammonia or an organic compound containing one or more nitrogen atoms, such as a hydrocarbyl amine, a hydrocarbyl polyamine, or an aromatic heterocycle containing one or more nitrogen atoms and optionally containing one or more heteroatoms or heteroatom containing functional moieties, and one or more cationic counter ions and b) in a second part, a liberating compound which reacts with the nitrogen atom(s) bound to the boron atom(s) upon contact with the amido-borate to form an organoborane radical.

Abstract: Novel benzenedicarboxamides of the formula (I) wherein X represents hydrogen, halogen atom, nitro, C1-6alkylsulfonyloxy, C1-6alkylsulfinyl, C1-6alkylsulfenyl or C1-6alkylsulfonyl, R1 represents C1-6alkyl, C1-6alkylthio-C1-6alkyl, C1-6alkylsulfinyl-C1-6alkyl or C1-6 alkylsulfonyl-C1-6alkyl, Y represents halogen or C1-6alkyl, m represents 0 or 1, A represents O, S, SO, SO2, CH2 or CH(CH3), and Q represents a 5- or 6-membered heterocyclic group that contains at least one hetero atom selected from the group consisting of N, O and S and can be optionally substituted; processes for their preparation, their intermediates and their use as insecticides.

Abstract: A thin film transistor comprising at least three terminals consisting of a gate electrode, a source electrode and a drain electrode; an insulating layer and an organic semiconductor layer on a substrate, which controls its electric current flowing between the source and the drain by applying a electric voltage across the gate electrode, wherein the organic semiconductor layer comprises a heterocyclic compound containing a nitrogen atom formed by condensation between five member rings each having a nitrogen atom at their condensation sites or between a five member ring and a six member ring each having a nitrogen atom at their condensation sites. The transistor became to have a fast response speed (driving speed), and further, achieved a large on/off ratio getting an enhanced performance as a transistor.

Abstract: Process for the preparation of oxazole, imidazole, and pyraxole boryl compounds. The compounds are intermediates to functionalized compounds, both natural and synthetic which are cytotoxic, anticancer and antiviral agents.

Abstract: Compounds of formula I in free or salt form, wherein Ar, X, Y and T have the meanings as indicated in the specification, are useful for treating a condition mediated by CCR-3, particularly an inflammatory or allergic condition such as an inflammatory or obstructive airways disease. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.