The present invention relates to guanidine compounds for inhibiting mitochondrial oxidative phosphorylation (OXPHOS) and use thereof. More specifically, the present invention relates to a pharmaceutical composition for preventing or treating a OXPHOS-related disease, particularly cancer by inhibiting mitochondrial oxidative phosphorylation and reprogramming cellular metabolism.

The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.

##STR00001##

The present invention relates to an unsaturated fluorinated ether or amine compound of formula (I) with low global warming potential and method of making the compound (I), where R.sub.H.sup.1 is and R.sub.H.sup.2 are independently selected from H or CH.sub.3, wherein when R.sub.H.sup.1 is CH.sub.3 then R.sub.H.sup.2 is H and when R.sub.H.sup.2 is CH.sub.3, then R.sub.H.sup.1 is H; X is O or N and when X is O, then n is 1 and R.sub.f is a linear or branched perfluorinated alkyl group comprising 1-10 carbon atoms and optionally comprising at least one catenated O or N atom; X is N, then n is 2 and (i) each R.sub.f is independently selected from a linear or branched perfluorinated alkyl group comprising 1-8 carbon atoms and optionally comprising at least one catenated O or N atom, or (ii) the two R.sub.f's are bonded together to form a ring structure optionally comprising at least one catenated O or N atom, wherein the ring of the ring structure consists of 5-7 atoms, no more than 10 carbon atoms, and is perfluorinated. The applications of the compound include solvent cleaning, electrolyte solvents or additives, heat transfer, and vapour phase soldering.

The present invention provides novel diarylurea derivatives (compounds of formula (I)) and their uses. The compounds of the present invention are demonstrated to be allosteric modulators of the CB1 receptor, and therefore useful for the treatment of diseases and conditions mediated by CB1.

The present invention provides novel diarylurea derivatives (compounds of formula (I)) and their uses. The compounds of the present invention are demonstrated to be allosteric modulators of the CB1 receptor, and therefore useful for the treatment of diseases and conditions mediated by CB1.

The invention concerns compounds that possess a high affinity at 5-HT.sub.1A receptors and an agonist efficacy, as measured by Emax values from a cellular activation assay, that is higher than that of the compounds described in prior art. The capacity of the compounds of the invention to activate an effector protein complex is higher than that the most efficacious agonist described in prior art. Compounds of the invention also exhibit an exceptionally high selectivity (Ki ratio greater than 1000-fold) with respect, in particular, to dopamine D2 receptors and adrenergic receptors of the alpha1 subtype. This selectivity which constitutes a great advantage since it means that the compounds will avoid inducing (central and peripheral) effects associated with activating or inhibiting such receptors.

The invention concerns compounds that possess a high affinity at 5-HT.sub.1A receptors and an agonist efficacy, as measured by Emax values from a cellular activation assay, that is higher than that of the compounds described in prior art. The capacity of the compounds of the invention to activate an effector protein complex is higher than that the most efficacious agonist described in prior art. Compounds of the invention also exhibit an exceptionally high selectivity (Ki ratio greater than 1000-fold) with respect, in particular, to dopamine D2 receptors and adrenergic receptors of the alpha1 subtype. This selectivity which constitutes a great advantage since it means that the compounds will avoid inducing (central and peripheral) effects associated with activating or inhibiting such receptors.

In its many embodiments, the present invention provides certain substituted N-aryl and N-heteroaryl piperidine compounds of the Formula (I):

##STR00001## and pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, L, R.sup.4, L.sub.1, Q, R.sup.5 and R.sup.6 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, may be useful as Liver X- receptor (LXR) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.

The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.

##STR00001##

The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.

##STR00001##