Neuroactive steroids, compositions, and uses thereof
AssigneeSage Therapeutics, Inc.
InventorsBoyd L. Harrison, Gabriel Martinez Botella, Albert Jean Robichaud, Francesco G. Salituro
Life of this patent
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Abstract
Described herein are steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein R1, R2a, R2b, R3, R4, R5a, R5b, R6, and Z are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.
Claims85
A compound of Formula (I):
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, carbocyclyl, or heterocyclyl;
- each of R2a and R2b is independently hydrogen, C1-C6 alkyl, halo, cyano, —ORA, or —NRBRC, or
- R2a and R2b together with the carbon atom to which they are attached form a ring;
- R3 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, —C(O)RA, —C(O)ORA, or —C(O)NRBRC;
- R4 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, carbocyclyl, or —ORA;
- represents a single or double bond, wherein when one is a double bond, the other is a single bond;
- wherein when the between —CR6 and —CR5aR5b is a double bond, then one of R5a or R5b is absent;
- and
- when one of the is a double bond, R6 is absent;
- each of R5a and R5b is independently absent, hydrogen, C1-C6 alkyl, or halo;
- R6 is absent or hydrogen;
- Z is —CR7aR7b—, wherein each of R7a and R7b is independently hydrogen or C1-C6 alkyl, or R7a and R7b, together with the carbon atom to which they are attached, form a ring;
- RA is hydrogen, C1-C6 alkyl, carbocyclyl, heterocyclyl, aryl, or heteroaryl;
- each of RB and RC is independently hydrogen, C1-C6 alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, or taken together with the atom to which they are attached form a ring.
Dependencies are inferred from the claim text.