IP Library Granted Patent US 9,226,932
Granted Patent B2
US 9,226,932 · App. 14/102,213 · Granted Jan 5, 2016

Phosphoramidate alkylator prodrugs

Inventors: Mark Matteucci (Portola Valley, CA); Jian-Xin Duan (South San Francisco, CA); Hailong Jiao (Foster City, CA)
Assignee: Threshold Pharmaceuticals, Inc.
A61K31/675A61K31/337A61K31/513A61K31/7068A61K33/24C07F9/65062C07F9/65065C07F9/65397
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Quick Facts
Patent No.
US 9,226,932
App. No.
14/102,213
Granted
Jan 5, 2016
Kind
B2
Abstract

Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.

Claims (13)

1. A method for treating cancer, said method comprising administering to a patient in need of treatment for cancer a therapeutically effective dose of N,N′-bis(2-bromoethyl)phosphorodiamidic acid (1-methyl-2-nitro-1H-imidazol-5-yl)methyl ester (TH302) having the formula:

2. The method of claim 1 , wherein said cancer is colorectal cancer.

3. The method of claim 2 wherein a therapeutically effective dose of 5-fluorouracil is also administered to said patient.

4. The method of claim 2 , wherein a therapeutically effective dose of cisplatin is also administered to said patient.

5. The method of claim 1 , wherein said cancer is lung cancer.

6. The method of claim 5 , wherein a therapeutically effective dose of paclitaxel is also administered to said patient.

7. The method of claim 5 , wherein a therapeutically effective dose of 5-fluorouracil is also administered to said patient.

8. The method of claim 5 , wherein a therapeutically effective dose of cisplatin is also administered to said patient.

9. The method of claim 1 , wherein said cancer is pancreatic cancer.

10. The method of claim 9 , wherein a therapeutically effective dose of gemcitabine is also administered to said patient.

11. The method of claim 1 wherein TH-302 is administered in an amount of 0.001 to 0.1 g per day per kg body weight in a single or divided doses.

12. The method of claim 1 wherein TH-302 is administered in a dosage amount of 0.1 to 35 mg/kg/day in single or divided doses.

13. The method of claim 1 wherein TH-302 is administered in a dosage amount of 0.5 to 15 mg/kg/day in single or divided doses.

Assignments (6)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 26, 2022
From: MOLECULAR TEMPLATES, INC.
To: IMMUNOGENESIS, INC.
Reel/Frame 061545/0067 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 2, 2021
From: MOLECULAR TEMPLATES, INC.
To: IMMUNOGENESIS, INC.
Reel/Frame 056414/0241 →
RELEASE OF SECURITY INTEREST Recorded May 22, 2020
From: PERCEPTIVE CREDIT HOLDINGS II, LP
To: MOLECULAR TEMPLATES OPCO, INC.
Reel/Frame 052733/0890 →
CHANGE OF NAME Recorded May 7, 2020
From: THRESHOLD PHARMACEUTICALS, INC.
To: MOLECULAR TEMPLATES, INC.
Reel/Frame 052607/0818 →
SECURITY AGREEMENT Recorded Feb 28, 2018
From: MOLECULAR TEMPLATES OPCO, INC.; MOLECULAR TEMPLATES, INC.
To: PERCEPTIVE CREDIT HOLDINGS II, LP
Reel/Frame 045466/0472 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 4, 2015
From: MATTEUCCI, MARK; DUAN, JIAN-XIN; JIAO, HAILONG
To: THRESHOLD PHARMACEUTICALS, INC.
Reel/Frame 036958/0762 →
Continuity (5)
Continuation 13941261 · Jul 12, 2013
Continuation 13163303 · Jun 17, 2011
Continuation 11993822
Provisional Application 60695755 · Jun 29, 2005
Related Publication 20140170240A1 · Jun 19, 2014