IP Library Granted Patent US 11,952,397
Granted Patent B2
US 11,952,397 · App. 18/363,942 · Granted Apr 9, 2024

Crystalline forms of a neuroactive steroid

Inventors: Shanming Kuang (Plainsboro, NJ); Tianrui Li (Cambridge, NJ)
Assignee: Sage Therapeutics, Inc.
C07J43/003
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Quick Facts
Patent No.
US 11,952,397
App. No.
18/363,942
Granted
Apr 9, 2024
Kind
B2
Abstract

This invention relates to crystalline forms of anhydrous Compound (1) and pharmaceutical compositions thereof. Also disclosed herein are methods of making crystalline solid forms of Compound (1), and methods of using the crystalline forms of Compound (1) and pharmaceutical compositions thereof for modulating GABA activity (e.g., positive allosteric modulation of GABA activity) and treating CNS-related disorders.

Claims (8)

1. A crystalline form of Compound (1), wherein Compound (1) is represented by the following structural formula:

wherein the crystalline form is crystalline anhydrous Compound (1), and wherein the crystalline form is characterized by one or more peaks corresponding to 2-theta values measured in degrees of 15.4±0.3, 15.6±0.3, 18.1±0.3, 18.8±0.3, and 22.6±0.3 in an X-ray powder diffraction pattern.

2. The crystalline form of claim 1 , wherein the crystalline form is further characterized by one or more peaks corresponding to 2-theta values measured in degrees of 9.4±0.3, 11.9±0.3, 22.2±0.3, and 23.4±0.3 in an X-ray powder diffraction pattern.

3. The crystalline form of claim 1 , wherein the crystalline form has an endotherm at a T onset from about 146° C. to about 157° C. when heated at a rate of 10 ° C./min starting at a temperature of about 30° C.

4. The crystalline form of claim 1 , wherein the crystalline form is characterized by one or more peaks corresponding to 200.0±0.3 ppm, 164.3±0.3 ppm, 81.3±0.3 ppm, 70.5±0.3 ppm, and 62.2±0.3 ppm in a 13 C SSNMR spectrum.

5. The crystalline form of claim 4 , wherein the crystalline form is further characterized by one or more peaks corresponding to 60.9±0.3 ppm, 60.0±0.3 ppm, 56.7±0.3 ppm, 47.8±0.3 ppm, and 45.9±0.3 ppm in a 13 C SSNMR spectrum.

6. The crystalline form of claim 5 , wherein the crystalline form is further characterized by one or more peaks corresponding to 42.6±0.3 ppm, 39.3±0.3 ppm, 38.3±0.3 ppm, 35.5±0.3 ppm, 25.8±0.3 ppm, and 22.9±0.3 ppm in a 13 C SSNMR spectrum.

7. A pharmaceutical composition comprising a crystalline form of claim 1 , and a pharmaceutically acceptable excipient.

Assignments (2)
CHANGE OF NAME Recorded Apr 23, 2026
From: SAGE THERAPEUTICS, INC.
To: SAGE THERAPEUTICS, LLC
Reel/Frame 075472/0569 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 26, 2024
From: KUANG, SHANMING; LI, TIANRUI
To: SAGE THERAPEUTICS, INC.
Reel/Frame 066260/0640 →
Continuity (3)
Continuation PCTUS2022038459 · Jul 27, 2022
Provisional Application 63226374 · Jul 28, 2021
Related Publication 20230374061A1 · Nov 23, 2023