7 results about "Liver X receptor" patented technology

Incorporation of lipids into a growing hair fibre is provided by a composition comprising at least one of: 1) 0.05 to 8 wt % of a lipid precursor selected from the group consisting of a fatty acid having a chain of 6 to 24 carbon atoms, an ester or an acylglycerol thereof and mixtures thereof; 2) 0.05 to 8.0% of a "gene activator material" that modulates the biosynthesis of lipids in the hair follicle or sebaceous gland, selected from a) at least one activator of a peroxisome proliferator-activated receptor (PPAR activator), b) at least one activator of a liver X receptor (LXR), and c) at least one activator of a retinoid X receptor (RXR); and 3) a fatty alcohol having a chain of 6 to 24 carbon atoms, preferably 8 to 20 carbon atoms, most preferably 10 to 18 carbon atoms; and mixtures thereof; and a cosmetically acceptable carrier.

The invention discloses preparation and application of macrophage targeting nanoparticles entrapped with a cell burial function accelerant. The medicine for enhancing the intercellular function of the macrophages is a liver X receptor stimulant, and the liver X receptor stimulant comprises at least one of T0901317, GW3965, Ouabagenin and LXR-623. The surface of the targeting nanoparticle is coated with a macrophage cell membrane, and meanwhile, a urokinase type plasminogen activator receptor (uPAR) targeting ligand is modified. The nanoparticle can be efficiently accumulated at an inflammatory focus part by utilizing a macrophage cell membrane, and the modified targeting ligand is used for targeting the macrophage with damaged cell burial function, so that the cell burial function of the macrophage is enhanced, the polarization of the macrophage to an anti-inflammatory phenotype is promoted, the release of anti-inflammatory and proinflammatory cytokines is regulated, and the anti-inflammatory effect of the nanoparticle is improved. And finally, the inflammatory microenvironment of a focus part is regulated and controlled, so that a good effect of treating autoimmune diseases is achieved.

The invention belongs to the technical field of medical chemistry, and discloses an aza aromatic amine protein degradation targeting chimera (PROTAC) compound with the activity of degrading nuclear receptor co-inhibitor 1 (NCoR1) in a targeting manner, and a preparation method and application of the aza aromatic amine protein degradation targeting chimera (PROTAC) compound. The aza aromatic amine compound is prepared through acylation and N-alkylation reaction, and the structure of the compound is shown as a formula I to a formula IV. A Liver X Receptor Response Element-Luciferase reporter gene system (LXRE-Luc luciferase reporter gene system) determination experiment shows that when the compound is 10 [mu] M, the compound has an obvious liver receptor (LXR) regulation effect, and the compound has an obvious liver receptor regulation effect when the compound is 10 [mu] M; western blot experiment research shows that the compound has a remarkable degradation effect on NCoR1, and the compound XH-10 with the highest activity can generate a remarkable NCoR1 degradation effect when the concentration is 5 mu M. The compound is PROTAC with NCoR1 targeted degradation activity, and has the advantages of high activity and simple preparation process. The compound has an important value in the aspect of glycometabolism and ester metabolism regulation medicine development.

The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The compounds described herein are selective agonists of LXRβ and / or can be used to treat a disease or condition described herein, including Alzheimer's Disease.

The present disclosure relates to novel compounds which are Liver X Receptor (LXR) modulators and to pharmaceutical compositions containing same. The present disclosure further relates to the use of said compounds in the prophylaxis and / or treatment of diseases which are associated with the modulation of LXR, for example, dyslipidemias. The present disclosure further relates to the use of the present compounds in the prophylaxis and / or treatment of metabolic disorders associated with an impairment in lipid homeostasis.

Incorporation of lipids into scalp skin is provided by a composition comprising at least one of: 1) 0.05 to 8 wt % of a lipid precursor selected from the group consisting of a fatty acid having a chain of 6 to 24 carbon atoms, and mixtures thereof; 2) 0.05 to 8.0% of a "gene activator material" that modulates the biosynthesis of lipids in the scalp skin, selected from a) at least one activator of a peroxisome proliferator-activated receptor (PPAR activator), b) at least one activator of a liver X receptor (LXR), and c) at least one activator of a retinoid X receptor (RXR); and mixtures thereof; and a cosmetically acceptable carrier.

The invention belongs to the technical field of medical chemistry, and discloses a secondary amine PROTAC compound with the activity of degrading a nuclear receptor co-inhibitor 1 (NCoR1) in a targeted manner as well as a preparation method and application of the secondary amine PROTAC compound. The secondary amine compound is prepared through acylation and N-alkylation reaction, and the structure of the compound is shown as a formula I to a formula IV. A Liver X Receptor Response Element-Luciferase reporter gene system (LXRE-Luc luciferase reporter gene system) determination experiment shows that when the compound is 10 [mu] M, the compound has an obvious liver receptor (LXR) regulation effect, and the compound has an obvious liver receptor regulation effect when the compound is 10 [mu] M; western blot experiment research shows that the compound has a remarkable degradation effect on NCoR1, and the compound ZD-5 with the highest activity can generate a remarkable NCoR1 degradation effect when the concentration is 5 mu M. The compound is a protein degradation targeting chimera (PROTAC), has the advantages of being high in activity and easy and convenient to prepare, and has great value in the aspect of glycometabolism and ester metabolism regulation medicine development.