IP Library Granted Patent US 12,122,803
Granted Patent B2
US 12,122,803 · App. 18/597,990 · Granted Oct 22, 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 12,122,803
App. No.
18/597,990
Granted
Oct 22, 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 8.9±0.3, 14.6±0.3, 16.4±0.3, 18.0±0.3, and 20.0±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 11.6±0.3, 15.0±0.3, 17.4±0.3, 21.2±0.3 and 29.0±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 160° C. to about 166° 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 200.2±0.3 ppm, 199.1±0.3 ppm, 162.8±0.3 ppm, 82.9±0.3 ppm, 82.1±0.3, and 12.6±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 70.4±0.3 ppm, 63.6=0.3 ppm, 49.7±0.3 ppm, 35.5±0.3 ppm, and 15.5±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 62.9±0.3 ppm, 61.4±0.3 ppm, 60.6±0.3 ppm, 45.4±0.3 ppm, and 37.9±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 Mar 19, 2024
From: KUANG, SHANMING; LI, TIANRUI
To: SAGE THERAPEUTICS, INC.
Reel/Frame 066823/0463 →
Continuity (4)
Continuation 18363942 · Aug 2, 2023
Continuation PCTUS2022038459 · Jul 27, 2022
Provisional Application 63226374 · Jul 28, 2021
Related Publication 20240218012A1 · Jul 4, 2024