Methods of treating or preventing disorders using compounds that regulate TRPV 4 pathway are described. Methods and cells that can be used to evaluate compounds, such as TRPV 4 antagonists, for treatment or prevention disorders are also provided. In some embodiments, the TRPV 4 antagonist is selected, at least in part, on the basis that it is a TRPV 4 antagonist. In some embodiments, the TRPV 4 antagonist does not inhibit one, two, or all of TRPV1, TRPV2, and TRPV3. In some embodiments, the TRPV...

3-pyrazole carboxylic acid amides, the preparation methods and the uses thereof in manufacture of the medicines as cannabinoid-1(CB1) receptor inhibitors are disclosed. The chemical structures of 3-pyrazole carboxylic acid amides are shown as the general formula (I) , wherein R1 is shown as formula (II): . The compounds have equivalent CB1 receptor inhibiting activity in vitro with Rimonabant, and remarkably reduced toxicity. The compounds can be used in manufacture of the medicines for detoxifi...

The present invention relates to a chiral low-toxicity CB1 receptor inhibitor, a preparation method therefor, and a use thereof. The CB1 receptor inhibitor is a compound represented by General Formula I or a pharmaceutically acceptable salt, solvate, polymorph, an enantiomer or a racemic mixture thereof. The chiral, low-toxicity diaryl substituted pyrazole derivative CB1 receptor inhibitor has an in-vitro CB1 receptor inhibition activity equivalent to that of rimonabant and blood-brain barrier p...

PROBLEM TO BE SOLVED: To provide a method for producing a new crystal polymorph of rimonabant.SOLUTION: The method for producing a crystal polymorph of rimonabant (form II) characterized by an infrared spectrum absorption band lines of powder X ray diffraction pattern and a melting peak comprises (a) a step to heat rimonabant up to the refluxing temperature of a solvent composed of methylcyclohexane containing 1-10% water and dissolve at concentration of 150-220 g/L (b) a step to cool the medium...

Use of a CB1 receptor antagonist and/or inverse agonist, preferably rimonabant, for the preparation of drugs useful for increasing motor neuron excitability in the cerebral cortex and/or in the brain stem and/or at the spinal level, as well as a method for increasing motor neuron excitability through the administration of a CB1 antagonist/inverse agonist receptors, and to the use of a pharmaceutical composition which comprises a CB1 receptor antagonist and/or inverse agonist, preferably rimonaba...

Use of an inverse antagonist and/or agonist of CB1 receptors, preferably rimonabant, for preparing drugs that are useful for increasing motor neurone excitability at the level of the cerebral cortex and/or the brainstem and/or at the spinal level, and also a method for increasing motor neurone excitability by means of the administration of an inverse antagonist/agonist of CB1 receptors, and to the use of a pharmaceutical composition that comprises an inverse antagonist and/or agonist of CB1 rece...

THE PRESENT INVENTION RELATES TO A NOVEL CRYSTALLINE POLYMORPH OF RIMONABANT CALLED FORM II ITS METHOD OF PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THIS NOVEL POLYMORPH.