Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.

Disclosed herein are synthesis and use of covalent inhibitors selective for Transcriptional Enhancer Factor TEF-1 (TEAD1), which can be used for treatment of cancers such as glioblastoma, gastric cancer, colorectal cancer, pancreatic ductal adenocarcinoma (PDAC), and malignant pleural mesothelioma (MPM). Further disclosed herein are pharmaceutical compositions including the TEAD1 inhibitor and methods of treating cancers using the same.

Disclosed herein are synthesis and use of covalent inhibitors selective for Transcriptional Enhancer Factor TEF-1 (TEAD1), which can be used for treatment of cancers such as glioblastoma, gastric cancer, colorectal cancer, pancreatic ductal adenocarcinoma (PDAC), and malignant pleural mesothelioma (MPM). Further disclosed herein are pharmaceutical compositions including the TEAD1 inhibitor and methods of treating cancers using the same.

A zwitterionic compound has a structure of following formula (1), formula (2), formula (3), or formula (4):

##STR00001## R.sub.1 is —O.sup.−, —(CH.sub.2).sub.aSO.sub.3.sup.−, or —(CH.sub.2).sub.bCO.sub.2.sup.−, a is 1 to 10, and b is 1 to 10. R.sub.2 and R.sub.3 are each independently an alkyl group or a phenyl group. x, z, and v are each independently 1 to 20. y and t are each independently 0 to 10.

A zwitterionic compound has a structure of following formula (1), formula (2), formula (3), or formula (4):

##STR00001## R.sub.1 is —O.sup.−, —(CH.sub.2).sub.aSO.sub.3.sup.−, or —(CH.sub.2).sub.bCO.sub.2.sup.−, a is 1 to 10, and b is 1 to 10. R.sub.2 and R.sub.3 are each independently an alkyl group or a phenyl group. x, z, and v are each independently 1 to 20. y and t are each independently 0 to 10.

Disclosed is a method for preparing a 2-iodoheterocyclic aryl ether at room temperature, including adding an alkali metal hydride and a phenol to a solvent, then adding a diiodoheterocyclic aromatic hydrocarbon, and performing a reaction at 0-100° C., so as to obtain a 2-iodoheterocyclic aryl ether product. In the coupling process of the present invention, no transition metal catalyst needs to be added, and no metal pollution will be caused to the product. The product of the present invention can be used as an organic synthesis raw material for a further reaction, and can also be used as an additive flame retardant reagent to improve the flame retardant performance of plastics.

Disclosed is a method for preparing a 2-iodoheterocyclic aryl ether at room temperature, including adding an alkali metal hydride and a phenol to a solvent, then adding a diiodoheterocyclic aromatic hydrocarbon, and performing a reaction at 0-100° C., so as to obtain a 2-iodoheterocyclic aryl ether product. In the coupling process of the present invention, no transition metal catalyst needs to be added, and no metal pollution will be caused to the product. The product of the present invention can be used as an organic synthesis raw material for a further reaction, and can also be used as an additive flame retardant reagent to improve the flame retardant performance of plastics.

A biosensing composition having sensing glucose content is provided, including a substrate, glucose oxidase, an antioxidant, heme-protein, and a molecular chromogenic chromophore. In addition, a contact lens having sensing glucose content and a method of preparation thereof are provided, so as to achieve the effect of maintaining a low discoloration in normal blood sugar and obvious discoloration in high blood sugar.

A compound represented by the following General Formula (I), a tautomer or a stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof, is used as a voltage-dependent T-type calcium channel blocker: ##STR00001## wherein A represents a 5-membered heteroaryl group or a fused ring of a 5-membered or 6-membered heterocyclic ring with a benzene ring or a pyridine ring, each of which may have a substituent; R represents a hydrogen atom or the like; B represents CR5(Q1) or NQ2, herein Q1 represents a benzimidazole group which may have a substituent, or the like; Q2 represents an alkyl group having 1 to 8 carbon atoms which may have a substituent, a heteroaryl group which may have a substituent, or the like; R0, R1, R2, R3, R4, and R5 each represent a hydrogen atom or the like; and n and m each represent 0, 1, or 2.

A compound represented by the following General Formula (I), a tautomer or a stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof, is used as a voltage-dependent T-type calcium channel blocker: ##STR00001## wherein A represents a 5-membered heteroaryl group or a fused ring of a 5-membered or 6-membered heterocyclic ring with a benzene ring or a pyridine ring, each of which may have a substituent; R represents a hydrogen atom or the like; B represents CR5(Q1) or NQ2, herein Q1 represents a benzimidazole group which may have a substituent, or the like; Q2 represents an alkyl group having 1 to 8 carbon atoms which may have a substituent, a heteroaryl group which may have a substituent, or the like; R0, R1, R2, R3, R4, and R5 each represent a hydrogen atom or the like; and n and m each represent 0, 1, or 2.