The present invention relates to pyrazolo[3,4-b]pyridine compounds. The present invention further relates to methods for inhibiting Plasmodium comprising contacting Plasmodium with pyrazolo[3,4-b]pyridine compounds described herein. Also described herein are methods of treating malaria comprising administering pyrazolo[3,4-b]pyridine compounds to a subject in need thereof.

The present invention relates to pyrazolo[3,4-b]pyridine compounds. The present invention further relates to methods for inhibiting Plasmodium comprising contacting Plasmodium with pyrazolo[3,4-b]pyridine compounds described herein. Also described herein are methods of treating malaria comprising administering pyrazolo[3,4-b]pyridine compounds to a subject in need thereof.

Novel compounds having a D3 receptor antagonistic effect are provided. The compound represented by Formula (IA)′: ##STR00001##
wherein A is S or O; R.sup.1a is substituted or unsubstituted alkyloxy or the like, R.sup.2a to R.sup.2d are each independently hydrogen atoms or the like, ring B is a 4- to 8-membered non-aromatic carbocycle or the like, R.sup.3 is each independently halogen or the like, r is an integer of 0 to 4, R.sup.4 is substituted or unsubstituted aromatic heterocyclyl or the like,
or a pharmaceutically acceptable salt thereof.

Novel compounds having a D3 receptor antagonistic effect are provided. The compound represented by Formula (IA)′: ##STR00001##
wherein A is S or O; R.sup.1a is substituted or unsubstituted alkyloxy or the like, R.sup.2a to R.sup.2d are each independently hydrogen atoms or the like, ring B is a 4- to 8-membered non-aromatic carbocycle or the like, R.sup.3 is each independently halogen or the like, r is an integer of 0 to 4, R.sup.4 is substituted or unsubstituted aromatic heterocyclyl or the like,
or a pharmaceutically acceptable salt thereof.

The invention relates to compounds of formula (I) inhibiting Rho Kinase that are oxidazole derivatives, processes for preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. Particularly the compounds of the invention may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH). ##STR00001##

The invention relates to compounds of formula (I) inhibiting Rho Kinase that are oxidazole derivatives, processes for preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. Particularly the compounds of the invention may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH). ##STR00001##

The present invention provides compounds for inhibiting matriptase 2, or a mutant thereof, and compositions and methods of use thereof.

The present invention provides compounds for inhibiting matriptase 2, or a mutant thereof, and compositions and methods of use thereof.

This invention is in the field of medicinal chemistry. In particular, the invention relates to anew class of small-molecules having a tetrahydroindazole structure which function as modulators (e.g., activators or inhibitors) of sigma-1 and/or sigma-2 receptors, and their use as therapeutics for the treatment of cancer and other diseases (e.g., neurological conditions) characterized with sigma-1 and/or sigma-2 receptor activity.

This invention is in the field of medicinal chemistry. In particular, the invention relates to anew class of small-molecules having a tetrahydroindazole structure which function as modulators (e.g., activators or inhibitors) of sigma-1 and/or sigma-2 receptors, and their use as therapeutics for the treatment of cancer and other diseases (e.g., neurological conditions) characterized with sigma-1 and/or sigma-2 receptor activity.