The present disclosure relates generally to derivatives of capsazepine and methods of use thereof. In some aspects, the present disclosure relates to using capsazepine derivatives to treat cancer or other hyperproliferative diseases.

Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.

Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.

The present invention relates to novel 5HT receptor modulators, such as compounds of the general Formula (I) and general Formula (II):

##STR00001##

or a pharmaceutically acceptable salt thereof. Methods of using the compounds include, for example, modulation of 5-hydroxytryptamine (5-HT) receptor subtypes, including 5-hydroxytryptamine 2A receptor and/or 5-hydroxytryptamine 2C receptor, and treatment of a condition or disease where the treatment is associated with the modulation of 5-hydroxytryptamine 2A receptor and/or 5-hydroxytryptamine 2C receptor.

The present invention relates to novel 5HT receptor modulators, such as compounds of the general Formula (I) and general Formula (II):

##STR00001##

or a pharmaceutically acceptable salt thereof. Methods of using the compounds include, for example, modulation of 5-hydroxytryptamine (5-HT) receptor subtypes, including 5-hydroxytryptamine 2A receptor and/or 5-hydroxytryptamine 2C receptor, and treatment of a condition or disease where the treatment is associated with the modulation of 5-hydroxytryptamine 2A receptor and/or 5-hydroxytryptamine 2C receptor.

Disclosed herein are dihydroceramide desaturase 1 (Des1) inhibitor compounds and compositions, which are useful in the treatment of diseases, such as metabolic, cardiovascular, fibrotic, autoimmune/chronic inflammatory diseases, cystic fibrosis, various cancers, neurodegenerative diseases, lipid storage disorders, and ischemia/reperfusion injury, where inhibition of Des1 is expected to be therapeutic to a patient. Methods of inhibition of Des1 activity in a human or animal subject are also provided.

The present disclosure provides methods of increasing proliferation of adult salivary stem cells. The methods include contacting adult salivary stem cells in vivo, in vitro, or ex vivo with an aldehyde dehydrogenase (ALDH) agonist. Increasing proliferation of adult salivary stem cells can be carried out to provide for an increase in the number of adult salivary stem cells in an individual undergoing radiotherapy for head and neck cancer.

The present disclosure provides methods of increasing proliferation of adult salivary stem cells. The methods include contacting adult salivary stem cells in vivo, in vitro, or ex vivo with an aldehyde dehydrogenase (ALDH) agonist. Increasing proliferation of adult salivary stem cells can be carried out to provide for an increase in the number of adult salivary stem cells in an individual undergoing radiotherapy for head and neck cancer.

The present disclosure relates generally to derivatives of capsazepine and methods of use thereof In some aspects, the present disclosure relates to using capsazepine derivatives to treat cancer or other hyperproliferative diseases. In some aspects of the present disclosure, the disclosure provides capsazepine derivatives which may be useful in the treatment of cancer. Such cancers that the compounds may be used to treating include but are not limited to breast, cervical, oral, head, neck, or prostate cancer. In some aspects, the compounds may be useful in treating a tumor by direct injection of the compound into the tumor, particularly an oral tumor. In other aspects, the compounds are administered systemically. The compounds of the present disclosure may also be used to treat the pain associated with a tumor for which it is being administered.

The present disclosure relates generally to derivatives of capsazepine and methods of use thereof In some aspects, the present disclosure relates to using capsazepine derivatives to treat cancer or other hyperproliferative diseases. In some aspects of the present disclosure, the disclosure provides capsazepine derivatives which may be useful in the treatment of cancer. Such cancers that the compounds may be used to treating include but are not limited to breast, cervical, oral, head, neck, or prostate cancer. In some aspects, the compounds may be useful in treating a tumor by direct injection of the compound into the tumor, particularly an oral tumor. In other aspects, the compounds are administered systemically. The compounds of the present disclosure may also be used to treat the pain associated with a tumor for which it is being administered.