IP Library Granted Patent US 11,945,815
Granted Patent B2
US 11,945,815 · App. 17/380,943 · Granted Apr 2, 2024

PTPN11 inhibitors

Inventors: Philip Jones (Houston, TX); Barbara Czako (Bellaire, TX); Christopher L Carroll (Houston, TX); Pijus Mandal (Sugarland, TX); Jason Cross (Pearland, TX)
C07D471/04A61P35/00C07D491/107
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Quick Facts
Patent No.
US 11,945,815
App. No.
17/380,943
Granted
Apr 2, 2024
Kind
B2
Abstract

The present invention relates to compounds which are useful as inhibitors of PTPN11 for the treatment or prevention of cancer and other PTP-mediated diseases. Disclosed herein are new compounds and compounds based on pyrazolopyrazines and their application as pharmaceuticals for the treatment of disease.

Claims (18)

1. A compound, represented by the formula:

2. A pharmaceutically acceptable salt of a compound, wherein the compound is represented by the formula:

3. A pharmaceutical composition comprising the compound of claim 1 , together with a pharmaceutically acceptable carrier.

4. A pharmaceutical composition comprising a pharmaceutically acceptable salt of the compound of claim 2 , together with a pharmaceutically acceptable carrier.

5. A method of treatment of a PTPN11-mediated disease comprising administering a therapeutically effective amount of the compound of claim 1 , to a patient in need thereof, wherein the PTPN11-mediated disease is cancer selected from the group consisting of breast cancer, colon cancer, lung cancer, esophageal cancer, gastric cancer, leukemia, and melanoma.

6. A method of treatment of a PTPN11-mediated disease comprising administering a therapeutically effective amount of a pharmaceutically acceptable salt of the compound of claim 1 , to a patient in need thereof, wherein the PTPN11-mediated disease is cancer selected from the group consisting of breast cancer, colon cancer, lung cancer, esophageal cancer, gastric cancer, leukemia, and melanoma.

7. A compound, represented by the formula:

8. A pharmaceutically acceptable salt of a compound, wherein the compound is represented by the formula:

9. A pharmaceutical composition comprising the compound of claim 7 , together with a pharmaceutically acceptable carrier.

10. A pharmaceutical composition comprising a pharmaceutically acceptable salt of the compound of claim 8 , together with a pharmaceutically acceptable carrier.

11. A method of treatment of a PTPN11-mediated disease comprising administering a therapeutically effective amount of the compound of claim 7 , to a patient in need thereof, wherein the PTPN11-mediated disease is cancer selected from the group consisting of breast cancer, colon cancer, lung cancer, esophageal cancer, gastric cancer, leukemia, and melanoma.

12. A method of treatment of a PTPN11-mediated disease comprising administering a therapeutically effective amount of a pharmaceutically acceptable salt of the compound of claim 8 , to a patient in need thereof, wherein the PTPN11-mediated disease is cancer selected from the group consisting of breast cancer, colon cancer, lung cancer, esophageal cancer, gastric cancer, leukemia, and melanoma.

13. A method of treatment of lung cancer comprising administering to a patient in need thereof a therapeutically effective amount of the compound represented by the formula:

or a pharmaceutically acceptable salt thereof.

14. The method of claim 13 , wherein the lung cancer is non-small cell lung cancer.

15. A method of treatment of colon cancer comprising administering to a patient in need thereof a therapeutically effective amount of the compound represented by the formula:

or a pharmaceutically acceptable salt thereof.

16. The method of claim 15 , wherein the colon cancer is colorectal cancer.

Assignments (6)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 4, 2025
From: NAVIRE PHARMA, INC.
To: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
Reel/Frame 072160/0110 →
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 Oct 26, 2021
From: JONES, PHILIP; CZAKO, BARBARA; CARROLL, CHRISTOPHER L.; MANDAL, PIJUS; CROSS, JASON
To: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
Reel/Frame 057919/0429 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 26, 2021
From: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
To: NAVIRE PHARMA, INC.
Reel/Frame 057919/0638 →
Continuity (4)
Continuation 16536923 · Aug 9, 2019
Provisional Application 62773921 · Nov 30, 2018
Provisional Application 62717588 · Aug 10, 2018
Related Publication 20220041594A1 · Feb 10, 2022