Abstract: Novel luciferins, methods of making luciferins, and uses of the same are disclosed.

Abstract: The present invention relates to isoxazole-3-carboxamide derivative having the general Formula (I), or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-3-carboxamide derivatives for the treatment of TRPV1 mediated disorders, such as acute and chronic pain disorders, acute and chronic neuropathic pain, acute and chronic inflammatory pain, respiratory diseases, and lower urinary tract disorders.

Abstract: This invention provides compounds of formula I where the dashed line represents an optional double bond; where R1 is phenyl, naphthyl, pyridyl, pyrimidyl, pyrrolyl, imidazolyl, pyrazyl, furyl, thienyl, oxazolyl, isoxazolyl, thiazolyl, or isothiazolyl, optionally substituted, and other substituents are defined herein. Such compounds are potassium channel modulators.

Abstract: The present invention relates to substituted pyrazoline compounds, 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: A method for treating an inflammatory process selected from the group consisting of oedema, erythema, articular inflammation, rheumatoid arthritis, arthrosis, a colorectal tumor, a pulmonary carcinoma, an adenocarcinoma, and combinations thereof, in a person in need thereof, the method comprising administering to the person in need thereof, in an amount sufficient to treat the inflammatory process, a 3-aminocarbazole or a salt thereof.

Abstract: The present invention relates to a compound of formula (I), stereoisomers thereof or the mixture of these stereoisomers, wherein: X represents a halogen atom, i.e. F, Cl, Br. The present invention also relates to a process for preparing the compound, and to a use of the compound in the preparation of an insecticide for controlling or killing vectors in the public hygiene and disease control, and to a use of the compound in the preparation of an insecticide for controlling or killing insects, nematodes, and mites in agriculture or horticulture.

Abstract: The invention relates to compounds of formula I: wherein R1, R2, Ra, Rb, W, Q and S have the meanings given in claim 16. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.

Abstract: The present invention relates to a process for preparing fluoroalkyl nitriles by reacting fluorinated carboxamides with halides and fluorinated carboxylic acids.

Abstract: The present invention provides adamantyl-diamide derivatives of formula (I): wherein R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.

Abstract: The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.

Abstract: A sustained release apparatus including at least one sustained release mini tablet implant; the or each mini tablet implant including a pharmaceutically active composition including at least one pharmaceutically active component; and a carrier therefor, wherein the or each tablet implant is of the coated tablet or covered rod type; the or each mini tablet implant being approximately 0.1 to 0.5 times the length and/or diameter of a single immediate release tablet capable of providing the desired threshold blood level depending on the pharmaceutical active selected, and having a payload of approximately 30% to 70% by weight of the total payload of an equivalent immediate release treatment conducted for an equivalent period; the sustained release apparatus providing, in use, zero order release of pharmaceutical active.

Abstract: A compound of formula (I) wherein A1, A2, A3, A4, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests.

Abstract: A novel (?)-enantiomer of 2-[2-(1-chloro-cyclopropyl)-3-(2-chloro-phenyl)-2-hydroxypropyl]-2,4-dihydro-[1,2,4]-triazole-3-thione of the formula a process for preparing this novel active compound and its use as microbicide in crop protection and in the protection of materials.

Abstract: 3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula (I), wherein the symbols have the meanings defined in the specification.

Abstract: The present invention relates to compounds of formula (I): in which R1, R2, R3, X, Y and A are as defined in the specification. The compounds are modulators of the estrogen receptors.

Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Abstract: Substituted pyrazolo[4,3-c]pyridine derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer.

Abstract: Novel amidoacetonitrile compounds are disclosed. The compounds have pesticidal properties and are suitable for controlling endoparasites on warm-blooded animals.

Abstract: This invention comprises the novel compounds of formula (1) wherein R1, R2, R3, R4, R5, X and Y have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.

Abstract: The present invention relates to a new process for the preparation of N-[5-(3-dimethylamino-acryloyl)-2-fluorophenyl]-N-methyl-acetamide (I) in a high yield and high purity, which is an intermediate in the synthesis of compounds with affinity for GABAA receptor. In this process, N-(5-acetyl-2-fluorophenyl)-N-methyl-acetamide (VI) is reacted with an excess of N,N-dimethylformamide dimethyl acetal (NNDMF-DMA). The present invention also provides a new process for the preparation of a compound with affinity for GABAA receptor, N-{2-fluoro-5-[3-(thiophene)-2-carbonyl-pyrazolo[1,5-a]pyrimidin-7-yl]phenyl}-N-methyl-acetamide (II), which comprises the following steps: a) methylation of N-(5-acetyl-2-fluorophenyl)-N-acetamide (IV) with a methyl sulfonate, b) reaction of the resulting compound (VI) with NNDMF-DMA, and c) reaction of the resulting compound (I) with (5-amino-1H-pirazol-4-yl)thiophen-2-yl-methanone (III) in glacial acetic acid. The present invention also relates to new intermediate (VI).