Abstract: The object of the present invention is to provide novel carboxamides which exhibit an excellent pesticidal activity as pesticides. Disclosed are the carboxamides represented by the following Formula (I): wherein each substituent is as defined in the specification, and use thereof as pesticides and animal parasite controlling agents.

Abstract: A process is provided for the preparation of aryl-heteroatom-bridged compounds by reacting a halogen-substituted aromatic compound with a trialkylsilyl-substituted heteroatom-containing organic compound.

Abstract: A series of celecoxib derivatives defined by Formula I: were prepared and evaluated for their ability to inhibit the gram-negative bacteria Francisella tularensis. Pharmaceutical compositions including celecoxib derivatives and their use in methods for treating or preventing infection by Francisella tularensis in a subject are described.

Abstract: Provided herein are compounds and methods for use in preventing or treating a viral infection mediated by a virus comprising an IRES-containing RNA molecule or cancer related to an increase or decrease in IRES-mediated translation of an RNA molecule. Also provided are methods of inhibiting or promoting IRES-mediated translation. Also provided are methods of screening for an agent that inhibits IRES-mediated translation.

Abstract: This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is substituted or unsubstituted alkyl or the like, R2 is hydrogen or substituted or unsubstituted alkyl, Ring A is monocyclic or bicyclic aromatic heterocycle, R3 is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocycle, R4 is halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or the like, m is an integer between 0 and 2, n is an integer between 0 and 5, R is halogen, oxo, cyano, nitro, substituted or unsubstituted alkyl or the like, and p is an integer between 0 and 2 as novel compounds having NPY Y5 antagonistic activity.

Abstract: The invention provides compounds of formula wherein R1, R3, R4, R5, R14, X and W are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of human neutrophil elastase.

Abstract: Hydrated celecoxib sodium salt forms and processes to prepare hydrated celecoxib sodium salt forms are disclosed. The celecoxib sodium salt forms are particularly useful and suitable for pharmaceutical applications.

Abstract: The present invention relates to heterocyclyl-substituted-tetrahydro-naphthalen compounds of general formula (I), methods for their preparation, and compositions comprising these compounds as well as their use for the treatment or prophylaxis of various disorders in humans or animals.

Abstract: The invention relates to compounds of formula (I) processes for their preparation, their use as 5-lipoxygenase inhibitors and pharmaceutical compositions containing the same.

Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein Ar1, X, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.

Abstract: The present invention relates to compounds corresponding to formula (I): Wherein X, R1, R2, R3 and R4 are as defined herein. The invention further relates to preparation and therapeutic use of these compounds.

Abstract: The present invention relates to the use of a sulfonamide compound of formula (I): wherein R1 is selected from the group consisting of H, CN, halogen, trifluoromethyl, methyl, ethyl, hydroxy, methoxy, ethoxy, morpholino, R2 is selected from H, phenyl, substituted phenyl, CN, —SO2R, wherein R is phenyl or morpholino, —NC(O)Me, —NC(O)Et, —CH2C(O)OMe, CH2C(O)OEt, R3 is selected from the group consisting of H, NO2, NH2, halogen, —COOMe, —COOEt, RC(O)N—, morpholino, R4 is selected from the group consisting of H, a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, methoxy, ethoxy, propoxy, butoxy, a substituted or unsubstituted phenyl, alkinyl, Me2SO2—, COOR, wherein R is a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, -MeOC(O)—, a substituted or unsubstituted five or sixmembered aromatic or non-aromatic heterocyclic system with one, two or three heteroatoms, a hetaryl system, a condensed benzoheterocyclic system, X is a linker comprising 2 or 3 atoms, selected from the group consisting of

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: The present invention relates to di(hetero)arylcyclohexane derivatives of the formula I, in which Ar1, Ar2, R1 and R2 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds which inhibit ATP-sensitive potassium channels in the heart muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as arrhythmias or a decreased contractility of the heart, such as can occur, for example, in coronary heart disease, cardiac insufficiency or cardiomyopathies. In particular, they are suitable for the prevention of sudden cardiac death. The invention furthermore relates to processes and intermediates for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.

Abstract: Methods useful for preparing compounds of formula I: and salts thereof are disclosed. Also disclosed are intermediates useful in the preparation of such compounds.

Abstract: This invention concerns the synthesis of highly substituted pyrazoles, which are structural components of pharmacological compounds, through reaction of hydrazones with nitroolefins.

Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.

Abstract: The present invention relates to a compound represented by formula (E). The present invention also relates to a compound represented by the formula (E) for use in the treatment or prevention of diseases linked to protein aggregation and/or neurodegenerative diseases. Moreover, the present invention relates to pharmaceutical and diagnostic compositions comprising the compound of the invention as well as to a kit. Furthermore, the present invention relates to a method of imaging deposits of aggregated protein. A kit for preparing a detectably labelled compound of the present invention is also disclosed. Formula (E) wherein X, Y and L are independently nondirectionally selected from —C(R1)(R2)—, —C(R3)?, —N(R4)—, —N?, —N+(R5)?, —O— and —S—; M and Z are independently nondirectionally selected from formula (I) and formula (II).

Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.

Abstract: The invention provides a composition comprising (S) 2-amino-1-(4-chloro-phenyl)-1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanol, wherein the composition is either substantially free of (R) 2-amino-1-(4-chloro-phenyl)-1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanol or the composition contains a mixture of the (S) and (R) enantiomers in which the (S) enantiomer predominates. Also provided are processes for the preparation of the (S) 2-amino-1-(4-chloro-phenyl)-1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanok novel process intermediates and methods for making the novel process intermediates.

Abstract: The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.

Abstract: Provided is a method whereby a heteroaromatic ring aryl can be very rapidly methylated at a high yield. In an N-alkyl-2-pyrrolidinone, a heteroaromatic ring aryltrialkylstannan is cross-coupled with methyl iodide in the presence of a palladium complex, a phosphine ligand, a cuprous halide, a carbonic acid salt and/or an alkali metal fluoride to thereby rapidly methylate the heteroaromatic ring aryl. (Formula shows a case wherein the heteroaromatic ring aryl is a pyridyl group.

Abstract: The present invention relates to substituted pyrazoline compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.

Abstract: Compounds are provided that act as potent antagonists of chemokine receptors. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of chemokine receptor-mediated diseases, and as controls in assays for the identification of chemokine antagonists.

Abstract: A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of Formula I: wherein X wherein X is —CF3, Ar is selected from and R is selected from where R? is L-Lys, D-Lys, ?-Ala, L-Lue, L-Ile, Phe, SO2CH2CH2NH2, SO2NH2, Asn, Glu or Gyl, and R? is methyl, ethyl, allyl, CH2CH2OH, CH2CN, CH2CH2CN, CH2CONH2,

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.

Abstract: Celecoxib crystalline Form Ill substantially free of celecoxib crystalline Forms I and II and a process for its preparation.

Abstract: The present invention is directed to processes and intermediates useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea (Compound I), crystalline forms and solvate forms thereof; and compositions comprising 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea, crystalline forms and solvate forms thereof prepared by processes as described herein.

Abstract: The present invention is directed to 2,5-disubstituted phenyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

Abstract: A compound has a strong analgesic action against both nociceptive pain and neuropathic pain and has less side effects, and is medically useful. The compound includes cyclohexane derivatives represented by the following compound, or pharmaceutically acceptable salts thereof or prodrugs thereof.

Abstract: A method for the fluoridation of an iodonium salt with a fluoride ion source which can be carried out in an aqueous reaction solvent.

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 relates to novel 4-phenyl-1H-pyrazoles and their use as insecticides and/or parasiticides and also to processes for their preparation and to compositions comprising such phenylpyrazoles.

Abstract: Methods useful for preparing compounds of formula I: and salts thereof are disclosed. Also disclosed are intermediates useful in the preparation of such compounds.

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: Compounds of the formula (I) and salts and solvates thereof, in which X, R1, R2, R3, R4, R5 and R6 have the meanings indicated in Claim 1, are suitable as ligands of 5 HT receptors.

Abstract: Novel 1,5 diphenylpyrazole derivatives of the formula (I), in which R1-R6 have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.

Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

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: The present invention relates to compounds of general formula (I), wherein ring A, ring B, R1, R2, R3, Z, and L1 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.

Abstract: Novel 1,5-diphenylpyrazole derivatives of the formula (I) in which R1-R6 have the meanings indicated in claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.

Abstract: The disclosure provides compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their uses in inhibiting ?-amyloid peptide (?-AP) production.

Abstract: The present invention relates to the orexin receptor antagonists compounds of the general formula (I) as well as to their isomers, salts and solvates, to the pharmaceutical compositions containing them and to the therapeutic application thereof.

Abstract: The present invention relates to indane-amine compounds of general formula (I) and compositions thereof, methods for their preparation, and the use of said compounds for the preparation of a medicament for the treatment of humans or animals.

Abstract: This invention relates to compounds of the formulas (1), (2) and (3) having pharmacological activity, to compositions containing these compounds, and to methods of treatment employing the compounds and compositions.

Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein J is Q2 or R1; X is N, CR2 or CQ3; Y is N or CR3; Z is N or CR4; and Q1, Q2, Q3, R1 R2 and R3 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.

Abstract: The present invention constitutes new 3-triazolylphenyl-substituted sulphide derivatives of the formula (I) in which A1, A2, B0, B1, B2, B3, X, R1, R2 and n are as defined in the description, to their use as acaricides and insecticides for controlling animal pests, and to processes for preparing them.

Abstract: The invention relates to 17beta-hydroxysteroid dehydrogenase type 1 (17betaHSD1) inhibitors, the preparation thereof and the use thereof for the treatment and prophylaxis of hormone-related, especially estrogen-related or androgen-related, diseases.

Abstract: The invention relates to a compound of formula (I) wherein A1 and R1 to R5 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.