IP Library Granted Patent US 9,827,232
Granted Patent B2
US 9,827,232 · App. 15/201,843 · Granted Nov 28, 2017

Protein tyrosine phosphatase inhibitor, preparation method and uses thereof

Inventors: Duqiang Luo (Baoding, CN); Jun Zhang (Baoding, CN); Zhiqin Liu (Baoding, CN)
Assignee: Hebei University
A61K31/4412A61K9/0019A61K9/0053A61K9/14A61K9/20A61K9/48C07D213/89C12P17/12
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Quick Facts
Patent No.
US 9,827,232
App. No.
15/201,843
Granted
Nov 28, 2017
Kind
B2
Abstract

Disclosed in the present invention is a protein tyrosine phosphatase inhibitor. The preparation method therefor is: extracting the crude product from the Isaria Fumosorosea Wize solid or liquid fermentation broth using ethyl acetate, ethanol, methanol, or a mixed solvent of chloroform and methanol; separating the obtained extract using column chromatography on silica gel; and obtaining the target product. The inhibitor can be used to prepare pharmaceutical compositions for treating and preventing diabetes, obesity and cancers.

Claims (18)

1. A method for treating diabetes, obesity and cancers in a subject in need thereof, the method comprising:

administering a composition comprising a protein tyrosine phosphatase inhibitor and a pharmaceutically acceptable carrier to the subject,

wherein the composition is administered in an effective amount,

wherein the protein tyrosine phosphatase inhibitor is the following (a) or (b):

(a) a compound having the following structural formula:

or

a pharmaceutically acceptable salt of compound (a), compound (a) in the form of an ester or ether, compound (a) incorporated with a functional group of aldehyde, acid or alcohol by oxidation of double bonds, compound (a) incorporated with a sulfonic acid group in the ring, or compound (a) incorporated with a chain having from 4 to 10 carbon atoms by a Witting reaction.

2. The method according to claim 1 , wherein the composition is parenterally administered in an amount ranging from 0.1 to 10,000 μg/kg body weight of the subject.

3. The method according to claim 1 , wherein the composition is parenterally administered in an amount ranging from 1 to 1,000 μg/kg body weight of the subject.

4. The method according to claim 1 , wherein the composition is parenterally administered in an amount ranging from 1 to 80 μg/kg body weight of the subject.

5. The method according to claim 1 , wherein the composition is orally administered in an amount ranging from 0.2 to 10 mg/kg body weight of the subject.

6. The method according to claim 1 , wherein the composition is orally administered in an amount ranging from 0.6 to 6 mg/kg body weight of the subject.

7. The method according to claim 1 , wherein the composition is orally administered in an amount ranging from 1 to 5 mg/kg body weight of the subject.

8. The method according to claim 1 , wherein the composition is in the form of powder, tablet, dragee, capsule, solution, syrup or dropping pill for oral administration.

9. The method according to claim 1 , wherein the composition is in the form of a powder injection or a solution injection for injection administration.

10. The method according to claim 1 , wherein the pharmaceutically acceptable salt of compound (a) maintains the biological effectiveness of said compound (a) and is an acid addition salt or base addition salt commonly used in pharmacy and derived from non-toxic organic acids, inorganic acids, organic bases or inorganic bases.

11. The method according to claim 10 , wherein the inorganic acids for preparing said acid addition salt are hydrochloric acid, hydrobromic acid, hydroiodic acid, sulfuric acid, sulfamic acid, phosphoric acid or nitric acid; the organic acids used for preparing said acid addition salt are p-toluenesulfonic acid, salicylic acid, methanesulfonic acid, oxalic acid, malic acid, succinic acid, lactic acid, or fumaric acid; and the basic agents for preparing said base addition salt are hydroxides of ammonium, potassium, sodium or quaternary ammonium.

12. The method according to claim 1 , wherein the chain incorporated by the Witting reaction carries OR 1 , NR 2 R 3 or halogen, wherein R 1 , R 2 or R 3 is H or alkyl having from 1 to 5 carbon atoms, and the halogen is F, Cl, Br or I.

Priority Claims (1)
CN 2012 1 0158554 · May 22, 2012 · national
Continuity (2)
Division 14403113
Related Publication 20160310475A1 · Oct 27, 2016