Disclosed herein are tucaresol derivative compound and composition containing the same. Also disclosed herein are methods of enhancing immune response in a subject by administering the tucaresol derivative compound or by co-administering the tucaresol derivative compound and one or more additional agents. Also disclosed herein are use of the tucaresol derivative compound and composition containing the same in the manufacture of a medicament for treating cancer or enhancing immune response in a subject.

##STR00001##

Disclosed herein is a salt of formula I: where R.sup.1, X, n, R, R.sup.1, Y, m, p, q, Z and o are as defined herein. Also disclosed herein are methods of using said salts in chemical synthesis, such as to prepare compounds isotopically enriched in 18F for use in PET & imaging, as well as methods to make the compounds of formula I.

##STR00001##

Disclosed herein is a salt of formula I: where R.sup.1, X, n, R, R.sup.1, Y, m, p, q, Z and o are as defined herein. Also disclosed herein are methods of using said salts in chemical synthesis, such as to prepare compounds isotopically enriched in 18F for use in PET & imaging, as well as methods to make the compounds of formula I.

Compound of formula 4 or formula 5 ##STR00001##
wherein
L is a neutral ligand, preferably a nitrogen-containing heterocyclic carbene (NHC) such as carbene containing at least two nitrogen atoms, a cyclic aminoalkyl carbene (CAAC) or a bicyclic aminoalkyl carbene (BICAAC);
R.sup.1, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10 and R.sup.11 are, independently, H, unbranched or branched C.sub.1-20 alkyl, C.sub.5-9 cycloalkyl, unbranched or branched C.sub.1-20 alkoxy, optionally bearing one or more halogen atoms, respectively; or aryl, optionally substituted with one or more of unbranched or branched C.sub.1-20 alkyl, C.sub.5-9 cycloalkyl, unbranched or branched C.sub.1-20 alkoxy, aryl, aryloxy, unbranched or branched C.sub.1-20 alkylcarbonyl, arylcarbonyl, unbranched or branched C.sub.1-20 alkoxycarbonyl, aryloxycarbonyl, heteroaryl, carboxyl, cyano, nitro, amido, aminosulfonyl, N-heteroarylsulfonyl, unbranched or branched C.sub.1-20 alkylsulfonyl, arylsulfonyl, unbranched or branched C.sub.1-20 alkylsulfinyl, arylsulfinyl, unbranched or branched C.sub.1-20 alkylthio, arylthio, sulfonamide, halogen or N(R.sup.y)(R.sup.z), wherein R.sup.y and R.sup.z are independently selected from H and C.sub.1-20 alkyl:
R.sup.2 is H, unbranched or branched C.sub.1-20 alkyl.

Compound of formula 4 or formula 5 ##STR00001##
wherein
L is a neutral ligand, preferably a nitrogen-containing heterocyclic carbene (NHC) such as carbene containing at least two nitrogen atoms, a cyclic aminoalkyl carbene (CAAC) or a bicyclic aminoalkyl carbene (BICAAC);
R.sup.1, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10 and R.sup.11 are, independently, H, unbranched or branched C.sub.1-20 alkyl, C.sub.5-9 cycloalkyl, unbranched or branched C.sub.1-20 alkoxy, optionally bearing one or more halogen atoms, respectively; or aryl, optionally substituted with one or more of unbranched or branched C.sub.1-20 alkyl, C.sub.5-9 cycloalkyl, unbranched or branched C.sub.1-20 alkoxy, aryl, aryloxy, unbranched or branched C.sub.1-20 alkylcarbonyl, arylcarbonyl, unbranched or branched C.sub.1-20 alkoxycarbonyl, aryloxycarbonyl, heteroaryl, carboxyl, cyano, nitro, amido, aminosulfonyl, N-heteroarylsulfonyl, unbranched or branched C.sub.1-20 alkylsulfonyl, arylsulfonyl, unbranched or branched C.sub.1-20 alkylsulfinyl, arylsulfinyl, unbranched or branched C.sub.1-20 alkylthio, arylthio, sulfonamide, halogen or N(R.sup.y)(R.sup.z), wherein R.sup.y and R.sup.z are independently selected from H and C.sub.1-20 alkyl:
R.sup.2 is H, unbranched or branched C.sub.1-20 alkyl.

Compounds having a structure of formula (I), (I-A), (Ia)-(Ie), (A)-(E), and (II) or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of disorders including prostate cancer are also provided.

Provided is a compound having one or more halogens and an unsaturated double bond. Provided is a method for producing an iodine-containing vinyl monomer comprising: a) a step of providing an iodine-containing alcohol substrate having a general structure represented by the formula (1-1):

##STR00001##

(the definitions of the variables in the formula (1-1) are as described in the specification); and b) a step of dehydrating the iodine-containing alcohol substrate to obtain the iodine-containing vinyl monomer having a general structure represented by the formula (1):

##STR00002##

(the definitions of the variables in the formula (1) are as described in the specification).

The present application provides a medicament having an anti-inflammatory bowel disease function, and a preparation method therefor and an application thereof. The medicament has a structure as represented in formula I or formula II. The medicament and a pharmaceutically acceptable salt, a solvate, a prodrug, a tautomer, a stereoisomer, or a pharmaceutical composition thereof provided by the present application have a good effect on inflammatory bowel diseases, can be used for preparing medicaments for treating the inflammatory bowel diseases, and have important clinical significance and wide application prospects.

The present application provides a small-molecule inhibitor targeting an EB virus nuclear antigen protein, and/or a pharmaceutical composition containing the same, which can be used for the treatment of a disease caused by EBNA1 activity, such as, but not limited to, cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and/or rheumatoid arthritis. The present application further provides a small-molecule inhibitor targeting an EB virus nuclear antigen protein, and/or a pharmaceutical composition containing the same, which can be used for the treatment of a disease caused by EBV infection in a lytic and/or latent phase.

A salt having formula (1) or (2) serving as an acid diffusion inhibitor is provided as well as a resist composition comprising the acid diffusion inhibitor. When processed by lithography, the resist composition exhibits a high sensitivity, and excellent lithography properties such as CDU and LWR.

##STR00001##