The present invention addresses the problem of providing an inhibitor which has an excellent inhibitory activity on a p21-activated kinase. The present invention, by which has been solved the above-mentioned problem, is a p21-activated kinase 1 inhibitor containing, as an active ingredient, one or more compounds selected from the group consisting of dehydrokawain compounds, derivatives of dehydrokawain compounds, mimosine, derivatives of mimosine, and cucurbitacin compounds.

The present invention addresses the problem of providing an inhibitor which has an excellent inhibitory activity on a p21-activated kinase. The present invention, by which has been solved the above-mentioned problem, is a p21-activated kinase 1 inhibitor containing, as an active ingredient, one or more compounds selected from the group consisting of dehydrokawain compounds, derivatives of dehydrokawain compounds, mimosine, derivatives of mimosine, and cucurbitacin compounds.

Provided herein is a compound of Formula (I), or a pharmaceutically acceptable salt thereof, wherein R.sup.2a, R.sup.2b, R.sup.3, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6a, R.sup.6b, R.sup.11a, R.sup.11b, R.sup.15a, R.sup.15b, R.sup.16a, R.sup.16b, R.sup.18, R.sup.19, R.sup.20a, R.sup.20b, X, A, Z, q, u, r, s, t, m, and n are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.

##STR00001##

Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I) and (III):

##STR00001##

where R.sup.1, R.sup.2, R.sup.3, R.sup.3′, R.sup.4, R.sup.6a, R.sup.6a, R.sup.11a, and R.sup.11b are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, insomnia, anxiety, depression, traumatic brain injury (TBI), stress, and epilepsy.

Described herein are neuroactive steroids of the Formula (II): or a pharmaceutically acceptable salt thereof; wherein A, R.sup.1, R.sup.2a, R.sup.2b, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6 and are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.

##STR00001##

The compositions and methods provided herein are related, in part, to the discovery of cholic acid 7-sulfate as a treatment for diabetes. Selective transport of the microbial metabolite lithocholic acid (LCA) from the gut to the liver after bariatric surgery activates hepatic vitamin D receptor (VDR), thereby inducing expression of bile acid sulfotransferase SULT2A, which produces the antidiabetic molecule CA7S. Provided herein is a method for treating diabetes, obesity, or an inflammatory disease in a subject, the method comprises administering to a subject in need thereof a compound of Formula I-XV or Formula F-XV′ or an agent that increases levels or activity or cholic acid 7-sulfate or upstream targets in a subject.

The compositions and methods provided herein are related, in part, to the discovery of cholic acid 7-sulfate as a treatment for diabetes. Selective transport of the microbial metabolite lithocholic acid (LCA) from the gut to the liver after bariatric surgery activates hepatic vitamin D receptor (VDR), thereby inducing expression of bile acid sulfotransferase SULT2A, which produces the antidiabetic molecule CA7S. Provided herein is a method for treating diabetes, obesity, or an inflammatory disease in a subject, the method comprises administering to a subject in need thereof a compound of Formula I-XV or Formula F-XV′ or an agent that increases levels or activity or cholic acid 7-sulfate or upstream targets in a subject.

To provide a mogrol glycosyltransferase and a method for producing a mogrol glycoside using the enzyme. The present invention provides a mogrol glycosyltransferase and a method for producing a mogrol glycoside using the enzyme, and a transformant into which a mogrol glycosyltransferase gene is introduced and a method for preparing the transformant.

The present invention relates to compounds and their uses, in particular, compounds in the form of prodrugs that promote transport of a pharmaceutical agent to the lymphatic system and subsequently enhance release of the parent drug.

The present disclosure is directed to formulations comprising (1) at least one formulation transport agent, (2) at least one complexing agent, and (3) at least one active agent that modulates one or more traits of a target insect, plant, or plant pathogen. The present disclosure is also directed to methods of delivering such formulations to the target organism, as well as to formulation transport agents used to prepare such formulations.