282 results about "Partial agonist" patented technology

Novel non-steroidal tricyclic quinolinone and tricyclic quinoline compounds and compositions that are agonists, partial agonists and / or antagonists for androgen receptors (AR), their preparation and their uses are described.

The invention discloses an FXR receptor modulator, and a preparation method and an application thereof, belonging to the field of medicinal chemistry. The FXR receptor modulator with a structure characteristic as shown in a formula I in the specification or pharmaceutically-acceptable salts or stereoisomers or solvates or prodrugs thereof can bind with an FXR (i.e., NR1H4) receptor and is used as an agonist or a partial agonist of the FXR receptor, thereby being able to be applied to prevention and treatment of FXR mediated diseases, such as chronic intrahepatic or extrahepatic cholestasis, hepatic fibrosis caused by chronic cholestasis or acute intrahepatic cholestasis, or chronic hepatitis B, or gallstone, or liver cancer, or colon cancer, or inflammatory bowel diseases, etc., wherein a part of compounds specifically can reach an FXR-excited EC<50> of 100 nM or below, show good FXR agonist activity, have excellent application prospects, and provide a new medicine choice for clinical treatment of the FXR mediated diseases.

Melanocortin receptor-specific compounds with diamine groups of the general formulaand pharmaceutically acceptable salts thereof, where W is a diamine heteroatom unit with at least one cationic center, hydrogen bond donor or hydrogen bond acceptor, J, Q, L1, L2, L3, R1a, R1b, R2a, R2b and X are as defined in the specification, and the carbon atom marked with an asterisk can have any stereochemical configuration. Compounds disclosed herein bind to one or more melanocortin receptors and may be an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist as to one or more melanocortin receptors, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders, including specifically treatment of obesity and related conditions.

Compounds of Formula I or a pharmaceutically acceptable salt thereof are provided:where R1 through R7 are defined herein. The compounds of Formula I are 5HT2c agonists or partial agonists, and are useful for treating a variety of disorders.