IP Library › Granted Patent US 12,344,585
Granted Patent B2
US 12,344,585 · App. 18/120,073 · Granted Jul 1, 2025

Crystalline salts of a plasma kallikrein inhibitor

Inventors: Yahya El-Kattan (Vestavia Hills, AL); Yarlagadda S. Babu (Birmingham, AL)
Assignee: BioCryst Pharmaceuticals, Inc.
C07D231/14A61K9/0029A61K9/0053A23L33/10A23V2002/00C07B2200/13
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Quick Facts
Patent No.
US 12,344,585
App. No.
18/120,073
Granted
Jul 1, 2025
Kind
B2
Abstract

Disclosed are crystalline salts of Compound I, methods of preparing them, and related pharmaceutical preparations thereof. Also disclosed are methods of treatment using the crystalline salts of the invention.

Claims (13)

1. A method for prophylaxis to prevent attacks of hereditary angioedema, comprising orally administering once a day to a subject with hereditary angioedema from about 125 mg to about 175 mg of a crystalline salt of Compound I,

wherein the crystalline salt is characterized by peaks in the X-ray powder diffraction (XRPD) pattern at values of two theta (°2θ±0.2°) of 5.3, 9.0, and 22.0; and the crystalline salt is a bis(hydrochloride) salt.

2. The method of claim 1 , wherein about 125 mg of the crystalline salt of Compound I is administered to the subject.

3. The method of claim 1 , wherein about 175 mg of the crystalline salt of Compound I is administered to the subject.

4. The method of claim 1 , wherein the crystalline salt is characterized by peaks in the X-ray powder diffraction (XRPD) pattern at values of two theta (°2θ) of 5.3, 9.0, and 22.0.

5. The method of claim 1 , wherein the crystalline salt is characterized by peaks in the X-ray powder diffraction (XRPD) pattern at values of two theta (°2θ±0.2°) of 5.3, 9.0, 19.8, 21.2, 22.0, and 23.3.

6. The method of claim 5 , wherein the crystalline salt is characterized by peaks in the X-ray powder diffraction (XRPD) pattern at values of two theta (°2θ) of 5.3, 9.0, 19.8, 21.2, 22.0, and 23.3.

7. The method of claim 1 , wherein the crystalline salt is characterized by peaks in the X-ray powder diffraction (XRPD) pattern at values of two theta (°2θ±0.2°) of 5.3, 9.0, 14.3, 16.2, 19.8, 21.2, 22.0, 23.3, 24.6, and 30.3.

8. The method of claim 7 , wherein the crystalline salt is characterized by peaks in the X-ray powder diffraction (XRPD) pattern at values of two theta (°2θ) of 5.3, 9.0, 14.3, 16.2, 19.8, 21.2, 22.0, 23.3, 24.6, and 30.3.

9. The method of claim 1 , wherein the crystalline salt is characterized by an XRPD pattern substantially similar to that shown in FIG. 1 .

10. The method of claim 1 , wherein the crystalline salt has a thermogravimetric-infrared spectrum substantially as shown in FIG. 2 .

11. The method of claim 1 , wherein the hereditary angioedema is type I hereditary angioedema.

12. The method of claim 1 , wherein the hereditary angioedema is type II hereditary angioedema.

Assignments (4)
SECURITY INTEREST Recorded Jan 23, 2026
From: BIOCRYST PHARMACEUTICALS, INC.
To: WILMINGTON TRUST, NATIONAL ASSOCIATION
Reel/Frame 074485/0651 →
TERMINATION AND RELEASE OF SECURITY INTEREST IN PATENT COLLATERAL RECORDED AT REEL 063363/FRAME 0873 Recorded Oct 8, 2025
From: BIOPHARMA CREDIT PLC
To: BIOCRYST PHARMACEUTICALS, INC.
Reel/Frame 073056/0492 →
PATENT SECURITY AGREEMENT Recorded Apr 19, 2023
From: BIOCRYST PHARMACEUTICALS, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 063363/0873 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 10, 2023
From: EL-KATTAN, YAHYA; BABU, YARLAGADDA S.
To: BIOCRYST PHARMACEUTICALS, INC.
Reel/Frame 062948/0730 →
Continuity (5)
Continuation 17465181 · Sep 2, 2021
Continuation 16784016 · Feb 6, 2020
Continuation 16671649 · Nov 1, 2019
Provisional Application 62754983 · Nov 2, 2018
Related Publication 20240109844A1 · Apr 4, 2024
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