A polymorphic substance of a A-decarburization-5 androstane compound (ACP-2), an application thereof and a preparation method therefor are provided. Specifically, a polymorphic substance of a A-decarburization-5 androstane compound (ACP-2), a preparation method therefor and use thereof are provided.

Provided herein is a compound of Formula (I-I) or a pharmaceutically acceptable salt thereof, wherein t, R.sup.7, R.sup.3, R.sup.9, 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.17a, R.sup.17b, R.sup.18a, R.sup.18b, R.sup.19a, R.sup.19b, R.sup.5a, R.sup.5b, R.sup.8 and R.sup.13 are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I-I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.

##STR00001##

Provided herein is a compound of Formula (I-I) or a pharmaceutically acceptable salt thereof, wherein t, R.sup.7, R.sup.3, R.sup.9, 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.17a, R.sup.17b, R.sup.18a, R.sup.18b, R.sup.19a, R.sup.19b, R.sup.5a, R.sup.5b, R.sup.8 and R.sup.13 are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I-I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.

##STR00001##

The present application discloses, among other things, asymmetric synthesis a diastereomeric compound of formula (I) (e.g., -anordrin) or salt thereof. Also provided are methods and compositions for treatment of estrogen deficiency as well as preventing or reducing an estrogen deficiency symptom using a diastereomeric compound of formula (I) (e.g., -anordrin) or salt thereof alone or in combination with at least one additional agent. Further provided are methods and compositions for reducing a side effect of an additional agent in the context of combination therapy with a diastereomeric compound of formula (I) (e.g., -anordrin) or salt thereof.

The present application discloses, among other things, asymmetric synthesis a diastereomeric compound of formula (I) (e.g., -anordrin) or salt thereof. Also provided are methods and compositions for treatment of estrogen deficiency as well as preventing or reducing an estrogen deficiency symptom using a diastereomeric compound of formula (I) (e.g., -anordrin) or salt thereof alone or in combination with at least one additional agent. Further provided are methods and compositions for reducing a side effect of an additional agent in the context of combination therapy with a diastereomeric compound of formula (I) (e.g., -anordrin) or salt thereof.

Provided herein is a compound of Formula I, II, IIIa, IIIb, V, VIa, VIb, VII, VIII, IX, or XI: ##STR00001##
or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of Formula I, II, IIIa, IIIb, V, VIa, VIb, VII, VIII, IX, or X, and methods of using the compounds, e.g., in the treatment of CNS-related disorders.

Provided herein is a compound of Formula I, II, IIIa, IIIb, V, VIa, VIb, VII, VIII, IX, or XI: ##STR00001##
or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of Formula I, II, IIIa, IIIb, V, VIa, VIb, VII, VIII, IX, or X, and methods of using the compounds, e.g., in the treatment of CNS-related disorders.