IP Library Granted Patent US 11,230,530
Granted Patent B2
US 11,230,530 · App. 16/845,833 · Granted Jan 25, 2022

Human plasma kallikrein inhibitors

Inventors: Pravin L. Kotian (Hoover, AL); Yarlagadda S. Babu (Birmingham, AL); Minwan Wu (Vestavia Hills, AL); Venkat R. Chintareddy (Vestavia Hills, AL); V. Satish Kumar (Birmingham, AL); Weihe Zhang (Vestavia, AL)
Assignee: BioCryst Pharmaceuticals, Inc.
C07D231/14C07D401/04C07D401/12C07D401/14C07D403/04C07D403/12C07D405/12C07D413/04C07D413/12C07D417/12
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Quick Facts
Patent No.
US 11,230,530
App. No.
16/845,833
Granted
Jan 25, 2022
Kind
B2
Abstract

Disclosed are compounds of formula I: as described herein, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one such compound, and methods involving use of the compounds and compositions in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.

Claims (23)

1. A method of treating or preventing angioedema, comprising orally administering to a subject in need thereof an oral dosage form comprising a therapeutically effective amount of a compound having the structure:

or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein the oral dosage form is administered once per day.

3. The method of claim 1 , wherein the oral dosage form is a capsule and the oral dosage form is administered once per day.

4. The method of claim 1 , wherein the angioedema is hereditary angioedema.

5. The method of claim 4 , wherein the oral dosage form is administered once per day.

6. The method of claim 4 , wherein the oral dosage form is a capsule and the oral dosage form is administered once per day.

7. The method of claim 1 , wherein the compound is the (+)-enantiomer.

8. The method of claim 7 , wherein the angioedema is hereditary angioedema.

9. The method of claim 7 , wherein the oral dosage form is administered once per day.

10. The method of claim 7 , wherein the oral dosage form is a capsule and the oral dosage form is administered once per day.

11. The method of claim 1 , wherein the compound is the (−)-enantiomer.

12. The method of claim 11 , wherein the angioedema is hereditary angioedema.

13. The method of claim 11 , wherein the oral dosage form is administered once per day.

14. The method of claim 11 , wherein the oral dosage form is a capsule and the oral dosage form is administered once per day.

15. The method of claim 1 , wherein the oral dosage form comprises a hydrochloride salt of the compound.

16. The method of claim 15 , wherein the angioedema is hereditary angioedema.

17. The method of claim 15 , wherein the oral dosage form is administered once per day.

18. The method of claim 15 , wherein the oral dosage form is a capsule and the oral dosage form is administered once per day.

19. The method of claim 1 , wherein the oral dosage form comprises a bis(hydrochloride) salt of the compound.

20. The method of claim 19 , wherein the angioedema is hereditary angioedema.

21. The method of claim 19 , wherein the oral dosage form is administered once per day.

22. The method of claim 19 , wherein the oral dosage form is a capsule and the oral dosage form is administered once per day.

Assignments (7)
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 →
RELEASE OF GRANT OF SECURITY INTEREST IN PATENTS Recorded Apr 18, 2023
From: ATHYRIUM OPPORTUNITIES III CO-INVEST 1 LP
To: BIOCRYST PHARMACEUTICALS, INC.
Reel/Frame 063362/0550 →
RELEASE OF SECURITY INTEREST Recorded Apr 17, 2023
From: MIDCAP FINANCIAL TRUST
To: BIOCRYST PHARMACEUTICALS, INC.; MDCP, LLC
Reel/Frame 063342/0116 →
SECURITY INTEREST Recorded Apr 10, 2023
From: BIOCRYST PHARMACEUTICALS, INC.
To: ATHYRIUM OPPORTUNITIES III CO-INVEST 1 LP
Reel/Frame 063284/0001 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 29, 2020
From: KOTIAN, PRAVIN L.; BABU, YARLAGADDA S.; WU, MINWAN; CHINTAREDDY, VENKAT R.; ZHANG, WEIHE; KUMAR, V. SATISH
To: BIOCRYST PHARMACEUTICALS, INC.
Reel/Frame 053338/0434 →