3 results about "Selective antagonist" patented technology

The application discloses a kind of deuterated benzamide diazepine compounds and preparation method and purposes thereof, and structure is as shown in general formula I.The compound is used as selective OX2R antagonist, and shows good activity, selectivity, brain exposure, brain blood ratio (the ratio of drug concentration in brain and drug concentration in blood, is called B / P), little toxic side effect, moderate half-life effect etc..It can be used for preventing, treating and / or reducing the disease related to orexin receptor.General formula I

A method of treating premature ejaculation in men may include administering a therapeutically effective dosage of a formulation to a patient in need thereof. The formulation for treating male premature ejaculation may include a phosphodiesterase 5 inhibitor (PDE5i), such as Tadalafil; an alpha-1 adrenoreceptor (alpha-1a) selective antagonist, such as Silodosin; and a selective serotonin reuptake inhibitor (SSRI), such as Paroxetine.

Based on co-drugs representing two different chemical entities, and the co-administration and sequential administration of said two chemical entities, novel therapies are provided for macular degeneration, non-alcoholic fatty liver disease (NAFLD), and gouty arthritis (gout). The first component (“Selective RBP4 Antagonist”) is a chemical entity that interacts with RBP4 (retinol-binding protein 4), part of the RBP4-TTR (transthyretin) complex that delivers retinol to the retina. This component reduces the transport of retinol from circulation to the retina. The second component (“C20-D3-Visual Chromosome-Generating Compound”) is a C20-D3-modified retinoid or carotenoid that, when metabolized in mammals, ultimately produces a C20-D3 visual chromophore in the retina representing either C20-D3-9-cis-retinal or C20-D3-11-cis-retinal. Deuteration at the C20 position reduces the formation of lipofuscin biretinol, while other functions (such as providing a precursor for the in vivo synthesis of visual chromophore 11-cis-retinaldehyde) are not reduced.