The present disclosure relates to orally bioavailable selective estrogen receptor down-regulators (SERDs) and the synthesis of the same. Further, the present disclosure teaches the utilization of the orally bioavailable selective estrogen receptor down-regulators (SERDs) in a treatment for proliferative diseases, including cancer, particularly breast cancer, and especially ER+ breast cancer.

The present disclosure provides methods for enantioselective synthesis of acyclic -quaternary carboxylic acid derivatives via iridium-catalyzed allylic alkylation.

The present disclosure provides methods for enantioselective synthesis of acyclic -quaternary carboxylic acid derivatives via iridium-catalyzed allylic alkylation.

Disclosed in the present invention is a preparation method for a tetra-substituted allenoic acid compound based on a palladium catalytic system, that is, a highly optically active allenoic acid compound having axial chirality is directly constructed in one step by reacting tertiary propargyl alcohol, carbon monoxide and water in an organic solvent under the action of a palladium catalyst, a chiral bisphosphine ligand, an organophosphoric acid, and an organic additive, and the theoretical yield can reach 100%. The method of the present invention is simple to operate, the raw materials and reagents are readily available, the reaction conditions are mild, the substrate universality is wide, the functional group compatibility is good, the reaction has high enantioselectivity (77%?96% ee), and the reaction is well compatible with complex natural products or substrates of a drug molecular skeleton. The highly optically active allenoic acid compound obtained by the present invention can be used as an important intermediate for constructing a ?-butyrolactone compound containing a tetra-substituted chiral quaternary carbon center, tetra-substituted allenol, tetra-substituted allenal, tetra-substituted allenyl ketone, tetra-substituted allenami de and other compounds.

The present invention relates to the use of compounds for the treatment or prevention of pain in mammals, in particularly in human beings, and also to a process for preparing these compounds.

The present invention relates to the use of compounds for the treatment or prevention of pain in mammals, in particularly in human beings, and also to a process for preparing these compounds.

Synthesis of compounds having varying degrees of conformational rigidity is obtained via a low cost, high yield and efficient synthetic reactions. The library of compounds is structurally diverse, having at least one or more chiral centers and providing large numbers of compounds having building block diversity and substantial scaffold diversity. The compounds further provide a novel method for obtaining candidate therapeutic agents for prevention, treatment or diagnosis of diseases.

Synthesis of compounds having varying degrees of conformational rigidity is obtained via a low cost, high yield and efficient synthetic reactions. The library of compounds is structurally diverse, having at least one or more chiral centers and providing large numbers of compounds having building block diversity and substantial scaffold diversity. The compounds further provide a novel method for obtaining candidate therapeutic agents for prevention, treatment or diagnosis of diseases.

The present invention is directed to itaconic acid derivatives, compounds comprising the derivatives and methods of using the derivatives in the treatment of cancer, inflammation, and autoimmune diseases.

The present disclosure provides methods for enantioselective synthesis of acyclic -quaternary carboxylic acid derivatives via iridium-catalyzed allylic alkylation.