The present disclosure relates to indole compounds and pharmaceutical compositions thereof, and their use in stimulating the immune system of patients in need thereof and in treating cancer.

Disclosed are a compound as shown by the following formula 1, and a pharmaceutically acceptable salt, an ester, a hydrate and an organic solvate thereof. In the formula (1), the groups R.sub.1 to R.sub.17 are independently selected from the group consisting of hydrogen, fluorine, chlorine, bromine, iodine, C.sub.1-C.sub.8 alkyl, C.sub.1-C.sub.8 alkoxy, carbonyl, hydroxyl, amino, azido, carboxyl and C.sub.1-C.sub.8 alkylsulfinyl, respectively; and X is a carbon or nitrogen atom; Y is selected from the following groups: a single bond, C.sub.1-C.sub.8 alkylene, C.sub.6-C.sub.20 arylene and C.sub.4-C.sub.20 heteroarylene; and n is an integer from 5 to 20. Also provided in the present invention are a pharmaceutical composition containing the compound, and use thereof in the field of tumor therapy. ##STR00001##

Disclosed are a compound as shown by the following formula 1, and a pharmaceutically acceptable salt, an ester, a hydrate and an organic solvate thereof. In the formula (1), the groups R.sub.1 to R.sub.17 are independently selected from the group consisting of hydrogen, fluorine, chlorine, bromine, iodine, C.sub.1-C.sub.8 alkyl, C.sub.1-C.sub.8 alkoxy, carbonyl, hydroxyl, amino, azido, carboxyl and C.sub.1-C.sub.8 alkylsulfinyl, respectively; and X is a carbon or nitrogen atom; Y is selected from the following groups: a single bond, C.sub.1-C.sub.8 alkylene, C.sub.6-C.sub.20 arylene and C.sub.4-C.sub.20 heteroarylene; and n is an integer from 5 to 20. Also provided in the present invention are a pharmaceutical composition containing the compound, and use thereof in the field of tumor therapy. ##STR00001##

Provided are compositions for inhibiting a biological activity of an aldo-keto reductase family 1, member C3 (AKR1C3) polypeptide. In some embodiments, the compositions are indomethacin derivatives that are AKR1C3-specific inhibitors. Also provided are methods for producing disclosed indomethacin derivatives that substantially lack cyclooxygenase inhibitory activity but that have AKR1C3 inhibitory activity, methods for inhibiting AKR1C3 polypeptide biological activities, and methods for treating prostate tumors in subjects.

Provided are compositions for inhibiting a biological activity of an aldo-keto reductase family 1, member C3 (AKR1C3) polypeptide. In some embodiments, the compositions are indomethacin derivatives that are AKR1C3-specific inhibitors. Also provided are methods for producing disclosed indomethacin derivatives that substantially lack cyclooxygenase inhibitory activity but that have AKR1C3 inhibitory activity, methods for inhibiting AKR1C3 polypeptide biological activities, and methods for treating prostate tumors in subjects.

Provided is an acrylamide compound, which is useful for the promotion of platelet production from platelet progenitor cells such as megakaryocytes in vitro and represented by general formula [I]:

##STR00001##

wherein each symbol is as defined in the description.

Provided is an acrylamide compound, which is useful for the promotion of platelet production from platelet progenitor cells such as megakaryocytes in vitro and represented by general formula [I]:

##STR00001##

wherein each symbol is as defined in the description.

Described herein are compounds that are derivatives of DMT or 5-MeO-DMT and can be metabolically converted to N,N-dimethyltryptamine or analogs thereof upon administration to a subject. In certain embodiments, the compounds described herein are useful for the treatment of conditions associated with a neurological disease.

Pharmaceutical compositions comprising 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1 (2H)-pyrimidinyl]methyl]-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions.

Pharmaceutical compositions comprising 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1 (2H)-pyrimidinyl]methyl]-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions.