IP Library Granted Patent US 11,643,420
Granted Patent B2
US 11,643,420 · App. 17/037,910 · Granted May 9, 2023

Benzoxazinone compounds as KLK5/7 dual inhibitors

Inventors: Andreas Betz (Palo Alto, CA); Robert Zamboni (Palo Alto, CA)
Assignee: MOLECULAR SKIN THERAPEUTICS, INC.
C07D498/04A61K9/0014A61P17/00
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Quick Facts
Patent No.
US 11,643,420
App. No.
17/037,910
Granted
May 9, 2023
Kind
B2
Abstract

The present invention provides compounds and pharmaceutical compositions including the compounds for the treatment of a skin disease associated with proteolytic activity of one or more KLK proteases, wherein the compounds are according to formula (I): wherein R is as described herein.

Claims (25)

1. A compound represented by formula (I):

or a pharmaceutically acceptable complex thereof; wherein R is H or a member selected from the group consisting of —R 1 and —C(O)R 1a , wherein R 1 is C 1-12 alkyl, and R 1a is H or C 1-12 alkyl.

2. The compound of claim 1 , represented by formula (Ia):

or a pharmaceutically acceptable complex thereof.

3. The compound of claim 1 , represented by formula (Ib):

or a pharmaceutically acceptable complex thereof.

4. The compound of claim 1 , represented by formula (Ic):

or a pharmaceutically acceptable complex thereof.

5. The compound of claim 1 , represented by the formula:

or a pharmaceutically acceptable complex thereof.

6. The compound of claim 1 , represented by the formula:

or a pharmaceutically acceptable complex thereof.

7. A pharmaceutical composition comprising a compound of claim 1 , and a pharmaceutically acceptable carrier.

8. The pharmaceutical composition of claim 7 , wherein said compound has the formula:

or a pharmaceutically acceptable complex thereof.

9. The pharmaceutical composition of claim 7 , wherein said compound has the formula:

or a pharmaceutically acceptable complex thereof.

10. The pharmaceutical composition of claim 7 , prepared for topical administration.

11. A method of treating Netherton Syndrome in a subject in need thereof, comprising administering to said subject an effective amount of a compound having a formula selected from the group consisting of:

or a pharmaceutically acceptable complex thereof.

12. The method in accordance with claim 11 , wherein said compound has the formula:

or a pharmaceutically acceptable complex thereof.

13. The method in accordance with claim 11 , wherein said compound has the formula:

or a pharmaceutically acceptable complex thereof.

14. The method in accordance with claim 11 , wherein said compound is administered topically.

Assignments (4)
RELEASE OF SECURITY INTEREST IN PATENT COLLATERAL Recorded Mar 5, 2025
From: BLUE OWL CAPITAL CORPORATION, AS ADMINISTRATIVE AGENT
To: BRIDGEBIO PHARMA, INC.; QED THERAPEUTICS, INC.; EIDOS THERAPEUTICS, INC.; ML BIO SOLUTIONS INC.; CALCILYTIX THERAPEUTICS INC.; ADRENAS THERAPEUTICS INC.; PHOENIX TISSUE REPAIR, INC.; NAVIRE PHARMA, INC.; VENTHERA, INC.; MOLECULAR SKIN THERAPEUTICS, INC.; CANTERO THERAPEUTICS, INC.; COA THERAPEUTICS, INC.; PORTAL THERAPEUTICS, INC.; BRIDGEBIO GENE THERAPY RESEARCH, INC.; FERRO THERAPEUTICS, INC.
Reel/Frame 070551/0095 →
SECURITY INTEREST Recorded Jan 19, 2024
From: BRIDGEBIO PHARMA, INC.; QED THERAPEUTICS, INC.; EIDOS THERAPEUTICS, INC.; THERAS, INC.; ML BIO SOLUTIONS INC.; CALCILYTIX THERAPEUTICS INC.; ADRENAS THERAPEUTICS INC.; PHOENIX TISSUE REPAIR, INC.; NAVIRE PHARMA, INC.; VENTHERA, INC.; MOLECULAR SKIN THERAPEUTICS, INC.; CANTERO THERAPEUTICS, INC.; COA THERAPEUTICS, INC.; PORTAL THERAPEUTICS, INC.; BRIDGEBIO GENE THERAPY RESEARCH, INC.; FERRO THERAPEUTICS, INC.; SUB21, INC.
To: BLUE OWL CAPITAL CORPORATION, AS ADMINISTRATIVE AGENT
Reel/Frame 066355/0126 →
SECURITY INTEREST Recorded Jan 17, 2024
From: CALCILYTIX THERAPEUTICS INC.; ADRENAS THERAPEUTICS INC.; PHOENIX TISSUE REPAIR, INC.; NAVIRE PHARMA, INC.; VENTHERA, INC.; MOLECULAR SKIN THERAPEUTICS, INC.; CANTERO THERAPEUTICS, INC.; COA THERAPEUTICS, INC.; PORTAL THERAPEUTICS, INC.; BRIDGEBIO GENE THERAPY RESEARCH, INC.; FERRO THERAPEUTICS, INC.; SUB21, INC.
To: BLUE OWL CAPITAL CORPORATION, AS ADMINISTRATIVE AGENT
Reel/Frame 066342/0154 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 3, 2020
From: BETZ, ANDREAS; ZAMBONI, ROBERT
To: MOLECULAR SKIN THERAPEUTICS, INC.
Reel/Frame 054539/0641 →
Cited By (1)
US 12,281,123