IP Library Granted Patent US 9,241,943
Granted Patent B2
US 9,241,943 · App. 14/409,352 · Granted Jan 26, 2016

Oxathiazine derivatives as antibacterial and anticancer agents

Inventor: Rolf W. Pfirrmann (Weggis, CH)
Assignee: Geistlich Pharma AG
A61K31/54A61K31/39A61K45/06C07D291/06C07D327/10
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Quick Facts
Patent No.
US 9,241,943
App. No.
14/409,352
Granted
Jan 26, 2016
Kind
B2
Abstract

New oxathiazin-like compounds and their derivatives are useful as antineoplastic and antimicrobial agents.

Claims (18)

1. A compound selected from the group consisting of:

2. The compound of claim 1 , comprising compound 2250.

3. A method of treating cancer in a subject comprising administering to said subject a compound selected from the group consisting of:

wherein said cancer is glioblastoma, glioma, neuroblastoma, astrocytoma, carcinomatous meningitis, colon cancer, rectal cancer, colo-rectal cancer, ovarian cancer, breast cancer, prostate cancer, lung cancer, mesothelioma, melanoma, renal cancer, liver cancer, pancreatic cancer, gastric cancer, esophageal cancer, urinary bladder cancer, cervical cancer, cardiac cancer, gall bladder cancer, skin cancer, bone cancer, cancers of the head or neck, leukemia, lymphoma, lymphosarcoma, adenocarcinoma, or fibrosarcoma, or metastases thereof.

4. The method of claim 3 , wherein cancer cells of said cancer are killed, or growth of said cancer cells is inhibited, by at least one of oxidative stress, apoptosis, anti-angiogenesis or antitubulogenesis.

5. The method of claim 3 , wherein said compound is 2250.

6. A method of treating glioblastoma in a subject, comprising administering to said subject the compound of claim 2 .

7. A method of treating glioma in a subject, comprising administering to said subject the compound of claim 2 .

8. A method of treating bacterial infection in a subject comprising administering to said subject a compound selected from the group consisting of:

9. The method of claim 8 wherein said compound is 2250.

10. The method of claim 8 wherein said bacterial infection is S. aureaus, E. coli, H. pylori or MRSA infection.

11. A method of treating tumor stem cells in a subject comprising administering to said subject a compound selected from the group consisting of:

wherein said tumor stem cells are in a subject suffering from glioblastoma, glioma, neuroblastoma, astrocytoma, carcinomatous meningitis, colon cancer, rectal cancer, colo-rectal cancer, ovarian cancer, breast cancer, prostate cancer, lung cancer, mesothelioma, melanoma, renal cancer, liver cancer, pancreatic cancer, gastric cancer, esophageal cancer, urinary bladder cancer, cervical cancer, cardiac cancer, gall bladder cancer, skin cancer, bone cancer, cancers of the head or neck, leukemia, lymphoma, lymphosarcoma, adenocarcinoma, or fibrosarcoma, or metastases thereof.

12. The method of claim 11 wherein said compound is 2250.

13. A method of treating glioblastoma tumor stem cells in a subject comprising administering to said subject a compound selected from the group consisting of:

14. The method of claim 13 wherein said compound is 2250.

15. A method of killing tumor stem cells comprising administering to a subject in need thereof a compound selected from the group consisting of

in combination with taurolidine and/or taurultam.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 1, 2026
From: GEISTLICH PHARMA AG
To: PERSEVERE THERAPEUTICS INC.
Reel/Frame 075325/0017 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 29, 2015
From: PFIRRMANN, ROLF W.
To: GEISTLICH PHARMA AG
Reel/Frame 035526/0934 →
Continuity (3)
Provisional Application 61661092 · Jun 18, 2012
Provisional Application 61694452 · Aug 29, 2012
Related Publication 20150182534A1 · Jul 2, 2015