Patent classifications
C07D235/32
Compositions and Methods for Treating Toxoplasmosis, Cryptosporidiosis, and Other Apicomplexan Protozoan Related Diseases
Compositions and methods for the treatment of toxoplasmosis, caused by the infectious eukaryotic parasite Toxoplasma gondii (T. gondii) and for the treatment of cryptosporidiosis, caused by the infectious eukaryotic parasites Cryptosporidium parvum (C. parvum) and Cryptosporidium hominus (C. hominus) are described. In particular, the present disclosure is directed to compositions and methods for inhibiting either T. gondii calcium dependent protein kinases (TgCDPKs) or C. parvum and C. hominus calcium dependent protein kinases (CpCDPKs) using pyrazolopyrimidine and/or imidazo[1,5-a]pyrazine inhibitors, of the formula,
##STR00001##
wherein the variables X, Y, Z, L, R.sup.1, and R.sup.3 are defined herein.
Compositions and Methods for Treating Toxoplasmosis, Cryptosporidiosis, and Other Apicomplexan Protozoan Related Diseases
Compositions and methods for the treatment of toxoplasmosis, caused by the infectious eukaryotic parasite Toxoplasma gondii (T. gondii) and for the treatment of cryptosporidiosis, caused by the infectious eukaryotic parasites Cryptosporidium parvum (C. parvum) and Cryptosporidium hominus (C. hominus) are described. In particular, the present disclosure is directed to compositions and methods for inhibiting either T. gondii calcium dependent protein kinases (TgCDPKs) or C. parvum and C. hominus calcium dependent protein kinases (CpCDPKs) using pyrazolopyrimidine and/or imidazo[1,5-a]pyrazine inhibitors, of the formula,
##STR00001##
wherein the variables X, Y, Z, L, R.sup.1, and R.sup.3 are defined herein.
Substituted-1H-benzo[d]imidazole series compounds as lysine-specific demethylase 1 (LSD1) inhibitors
The present invention provides compounds which are useful as inhibitors of lysine-specific demethylase 1 (LSD1). The present invention also relates to pharmaceutical compositions containing these compounds. The present invention also relates to a method for preparing these compounds. The present invention also relates to a method of treating a mammalian disorder in which LSD1 levels are elevated by administering these compounds and compositions to a patient in need thereof. The present invention also relates to a method for decreasing histone demethylase activity in a mammal comprising administering to the mammal an effective amount of these compounds and compositions.
Substituted-1H-benzo[d]imidazole series compounds as lysine-specific demethylase 1 (LSD1) inhibitors
The present invention provides compounds which are useful as inhibitors of lysine-specific demethylase 1 (LSD1). The present invention also relates to pharmaceutical compositions containing these compounds. The present invention also relates to a method for preparing these compounds. The present invention also relates to a method of treating a mammalian disorder in which LSD1 levels are elevated by administering these compounds and compositions to a patient in need thereof. The present invention also relates to a method for decreasing histone demethylase activity in a mammal comprising administering to the mammal an effective amount of these compounds and compositions.
THIOBENZIMIDAZOLE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND USE THEREOF
The present invention relates to a thiobenzimidazole derivative or a pharmaceutically acceptable salt thereof, and a composition for preventing or treating cancer, the composition comprising the derivative as an active ingredient. The thiobenzimidazole derivative according to the present invention inhibits tubulin polymerization by being activated in cancer cells, and exhibits cytotoxicity by blocking the cell cycle of cancer cells and inducing apoptosis when administered to an individual, and thus can be used for preventing or treating cancer and preferably, for preventing or treating HER-2 positive breast cancer or triple-negative breast cancer.
THIOBENZIMIDAZOLE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND USE THEREOF
The present invention relates to a thiobenzimidazole derivative or a pharmaceutically acceptable salt thereof, and a composition for preventing or treating cancer, the composition comprising the derivative as an active ingredient. The thiobenzimidazole derivative according to the present invention inhibits tubulin polymerization by being activated in cancer cells, and exhibits cytotoxicity by blocking the cell cycle of cancer cells and inducing apoptosis when administered to an individual, and thus can be used for preventing or treating cancer and preferably, for preventing or treating HER-2 positive breast cancer or triple-negative breast cancer.