Neuroactive steroids and compositions thereof

Patent metadata

Field	Value
Publication number	US-2025236639-A1
Application number	US-202519176652-A
Country	US
Kind code	A1
Filing date	Apr 11, 2025
Priority date	May 31, 2019
Publication date	Jul 24, 2025
Grant date	—

Abstract

Provided herein is a compound of Formula (I):or a pharmaceutically acceptable salt thereof, wherein R1a, R1b, R2a, R2b, R3, R4a, R4b, R5, R6a, R16b, R7a, R7a, R11a, R11b, R12a, R12b, R16a, R16b, R19, R11a, R22, RX, RY 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.

First claim

1 - 104 . (canceled)

105 . A compound of Formula (I-e6):

wherein:
each of R 2a , R 2b , R 15a , and R 15b is hydrogen;
R 3 is unsubstituted C 1-3 alkyl, —CH 2 OCH 3 , or —CH 2 OCH 2 CH 3 ;
R 19 is hydrogen, methyl, or ethyl;
R X is —OH;
R Y is methyl; and
R 22 is —CN.

106 . The compound of claim 105 , wherein R 3 is methyl.

107 . The compound of claim 105 , wherein R 3 is ethyl.

108 . The compound of claim 105 , wherein R 3 is propyl.

109 . The compound of claim 105 , wherein R 3 is —CH 2 OCH 3 .

110 . The compound of claim 105 , wherein R 3 is —CH 2 OC 2 H 5 .

111 . The compound of claim 105 , wherein R 19 is hydrogen.

112 . The compound of claim 105 , wherein R 19 is methyl.

113 . A compound selected from:

Com-

pound

No.
Structure

2

3

7

11

15

24

26

29

42

44

114 . The compound of claim 113 , wherein the compound has the structural formula

115 . The compound of claim 113 , wherein the compound has the structural formula

116 . The compound of claim 113 , wherein the compound has the structural formula

117 . The compound of claim 113 , wherein the compound has the structural formula

118 . The compound of claim 113 , wherein the compound has the structural formula

119 . The compound of claim 113 , wherein the compound has the structural formula

120 . The compound of claim 113 , wherein the compound has the structural formula

121 . The compound of claim 113 , wherein the compound has the structural formula

122 . The compound of claim 113 , wherein the compound has the structural formula

123 . The compound of claim 113 , wherein the compound has the structural formula

124 . A pharmaceutical composition comprising a compound according to claim 105 , and a pharmaceutically acceptable excipient.

125 . A pharmaceutical composition comprising a compound according to claim 114 , and a pharmaceutically acceptable excipient.

126 . A pharmaceutical composition comprising a compound according to claim 115 , and a pharmaceutically acceptable excipient.

127 . A pharmaceutical composition comprising a compound according to claim 116 , and a pharmaceutically acceptable excipient.

128 . A pharmaceutical composition comprising a compound according to claim 117 , and a pharmaceutically acceptable excipient.

129 . A pharmaceutical composition comprising a compound according to claim 118 , and a pharmaceut

Assignees

• Sage Therapeutics Inc

Inventors

• Salituro Francesco G
• Blanco-Pillado Maria Jesus
• Morningstar Marshall Lee

Classifications

• A61P25/24

  Antidepressants · CPC title

• A61K31/58

  containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin (digitoxin {A61K31/7048}) · CPC title

• C07J21/008

  at position 17 · CPC title

• C07J5/0015

  not substituted in position 16 · CPC title

• C07J13/007

  with double bond in position 17 (20) · CPC title