Prodrugs of neuroactive steroids
AssigneeBrii Biosciences, Inc.
InventorLianhong XU
Life of this patent
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Abstract
The present application relates to novel compounds that are prodrugs of brexanolone, ganaxolone and zuranolone, pharmaceutical compositions comprising one or more compounds disclosed herein and salts thereof, and a pharmaceutically acceptable excipient, and use of the compounds disclosed herein and salts thereof for treating diseases or conditions related to GABAA receptor function, such as major depression disorder (MDD) and postpartum depression (PPD), in mammals and especially in humans.
Claims52
A compound of Formula (I):
- or a pharmaceutically acceptable salt thereof, wherein:
- R1a and R1b each is independently hydrogen or methyl;
- Q is methyl or
- L is selected from the group consisting of null, alkyl, —O—, and —N(R2)—;
- W is selected from the group consisting of null, alkyl, and —O—;
- Y is selected from the group consisting of alkyl, alkenyl, alkynyl, heteroalkyl, heteroalkenyl, heteroalkynyl, saturated or unsaturated cycloalkyl, saturated or unsaturated heterocyclyl, aryl, heteroaryl, —OC(O)OR3, —OC(O)R4, and —NR5R6, wherein said alkyl, alkenyl, alkynyl, heteroalkyl, heteroalkenyl, heteroalkynyl, saturated or unsaturated cycloalkyl, saturated or unsaturated heterocyclyl, aryl, and heteroaryl are optionally substituted with one or more groups independently selected from oxo, halogen, cyano, alkyl, alkenyl, alkynyl, heteroalkyl, heteroalkenyl, heteroalkynyl, saturated or unsaturated cycloalkyl, saturated or unsaturated heterocyclyl, aryl, and heteroaryl;
- R2, R3, R4 and R5 are each independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, heteroalkyl, heteroalkenyl, heteroalkynyl, saturated or unsaturated cycloalkyl, saturated or unsaturated heterocyclyl, aryl, and heteroaryl, wherein said alkyl, alkenyl, alkynyl, heteroalkyl, heteroalkenyl, heteroalkynyl, saturated or unsaturated cycloalkyl, saturated or unsaturated heterocyclyl, aryl, and heteroaryl are optionally substituted with one or more groups independently selected from oxo, halogen, cyano, alkyl, alkenyl, alkynyl, heteroalkyl, heteroalkenyl, heteroalkynyl, saturated or unsaturated cycloalkyl, saturated or unsaturated heterocyclyl, aryl, and heteroaryl;
- R6 is selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, heteroalkyl, heteroalkenyl, heteroalkynyl, and —C(O)R7;
- and
- R7 is selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, heteroalkyl, heteroalkenyl, heteroalkynyl, alkoxyl, saturated or unsaturated cycloalkyl, saturated or unsaturated heterocyclyl, aryl, and heteroaryl, wherein said alkyl, alkenyl, alkynyl, heteroalkyl, heteroalkenyl, heteroalkynyl, alkoxyl, saturated or unsaturated cycloalkyl, saturated or unsaturated heterocyclyl, aryl, and heteroaryl are optionally substituted with one or more groups independently selected from oxo, halogen, cyano, alkyl, alkenyl, alkynyl, heteroalkyl, heteroalkenyl, heteroalkynyl, saturated or unsaturated cycloalkyl, saturated or unsaturated heterocyclyl, aryl, and heteroaryl,
- with the provisos that when L is —O— or —N(R2)—, W is not —O—, when W is —O—, Y is not —NR5NR6, and when W is —O—, Y is —C(O)OR3 or —C(O)R4.
The compound of Formula (I) or a pharmaceutically acceptable salt thereof, of claim 13-16, wherein W is a C1-C6 alkyl.
Dependencies are inferred from the claim text.