IP Library Granted Patent US 10,702,521
Granted Patent B2
US 10,702,521 · App. 15/505,715 · Granted Jul 7, 2020

Methods for treating neisseria gonorrhoeae infection with substituted 1,2-dihydro-2A,5,8A-triazaacenaphthylene-3,8-diones

Inventor: Katherine Louisa Widdowson (San Diego, CA)
Assignee: GlaxoSmithKline Intellectual Property Development Limited
A61K31/4985A61K31/4375A61K31/4545A61K31/4725A61K31/538A61K31/5377A61K31/5383A61K31/542A61K31/5415A61K31/554
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Quick Facts
Patent No.
US 10,702,521
App. No.
15/505,715
Granted
Jul 7, 2020
Kind
B2
Abstract

The present invention relates to methods for treating Neisseria Gonorrhoeae infection which comprises administering to a subject in need thereof novel 1,2-dihydro-2a,5,8a-triazaacenaphthylene-3,8-dione compounds: or pharmaceutically acceptable salts thereof and/or corresponding pharmaceutical compositions.

Claims (16)

1. A method for treating Neisseria gonorrhoeae infection in a subject in need thereof, which comprises administering to the subject 2-({4-[(3,4-dihydro-2H-pyrano[2,3-c]pyridin-6-ylmethyl)amino]-1-piperidinyl{methyl)-1,2-dihydro-3H,8H-2a,5,8triazaacenaphthylene-3,8-dione as shown below:

or a pharmaceutically acceptable salt thereof.

2. A method for treating Neisseria gonorrhoeae infection in a subject in need thereof, which comprises administering to the subject 2-({4-[(3,4-dihydro-2H-pyrano[2,3-c]pyridin-6-ylmethyl)amino]-1-piperidinyl}methyl)-1,2-dihydro-3H,8H-2a,5,8a-triazaacenaphthylene-3,8-dione as shown below:

3. A method for treating Neisseria gonorrhoeae infection in a subject in need thereof, which comprises administering to the subject a pharmaceutical composition comprising one or more pharmaceutically acceptable excipients and 2-({4-[(3,4-dihydro-2H-pyrano[2,3-c]pyridin-6-ylmethyl)amino]-1-piperidinyl}methyl)-1,2-dihydro-3H,8H-2a,5,8a-triazaacenaphthylene-3,8-dione as shown below:

or a pharmaceutically acceptable salt thereof.

4. A method for treating Neisseria gonorrhoeae infection in a subject in need thereof, which comprises administering to the subject a pharmaceutical composition comprising one or more pharmaceutically acceptable excipients and 2-({4-[(3,4-dihydro-2H-pyrano[2,3-c]pyridin-6-ylmethyl)amino]-1-piperidinyl}methyl)-1,2-dihydro-3H,8H-2a,5,8a-triazaacenaphthylene-3,8-dione as shown below:

5. A method for treating Neisseria gonorrhoeae infection in a subject in need thereof, which comprises administering to the subject (2R)-2-({4-[(3,4-dihydro-2H-pyrano[2,3-c]pyridin-6-ylmethyl)amino]-1-piperidinyl}methyl)-1,2-dihydro-3H,8H-2a,5,8a-triazaacenaphthylene-3,8-dione as shown below:

or a pharmaceutically acceptable salt thereof.

6. The method according to claim 5 , which comprises administering to the subject (2R)-2-({4-[(3,4-dihydro-2H-pyrano[2,3-c]pyridin-6-ylmethyl)amino]-1-piperidinyl}methyl)-1,2-dihydro-3H,8H-2a,5,8a-triazaacenaphthylene-3,8-dione as shown below:

7. The method according to claim 5 , wherein the pharmaceutically acceptable salt is an acid addition salt formed from an acid selected from the group consisting of hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, acetic acid, fumaric acid, succinic acid, maleic acid, citric acid, benzoic acid, p-toluenesulfonic acid, methanesulfonic acid, naphthalenesulfonic acid, and tartaric acid.

8. The method according to claim 5 , wherein the pharmaceutically acceptable salt is an acid addition salt formed from methanesulfonic acid.

9. A method for treating Neisseria gonorrhoeae infection in a subject in need thereof, which comprises administering to the subject a mesylate salt of (2R)-2-({4-[(3,4-dihydro-2H-pyrano[2,3-c]pyridin-6-ylmethyl)amino]-1-piperidinyl}methyl)-1,2-dihydro-3H,8H-2 a, 5,8 a -triazaacenaphthylene-3,8-dione as shown below:

10. A method for treating Neisseria gonorrhoeae infection in a subject in need thereof, which comprises administering to the subject a pharmaceutical composition comprising one or more pharmaceutically acceptable excipients and (2R)-2-({4-[(3,4-dihydro-2H-pyrano[2,3-c]pyridin-6-ylmethyl)amino]-1-piperidinyl}methyl)-1,2-dihydro-3H,8H-2 a, 5,8 a -triazaacenaphthylene-3,8-dione as shown below:

or a pharmaceutically acceptable salt thereof.

11. The method according to claim 10 , wherein the pharmaceutically acceptable salt is an acid addition salt formed from an acid selected from the group consisting of hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, acetic acid, fumaric acid, succinic acid, maleic acid, citric acid, benzoic acid, p-toluenesulfonic acid, methanesulfonic acid, naphthalenesulfonic acid, and tartaric acid.

12. The method according to claim 10 , wherein the pharmaceutically acceptable salt is an acid addition salt formed from methanesulfonic acid.

Assignments (2)
CHANGE OF ADDRESS Recorded Oct 8, 2025
From: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
To: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
Reel/Frame 073032/0390 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 19, 2018
From: WIDDOWSON, KATHERINE LOUISA
To: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
Reel/Frame 046400/0269 →
Continuity (2)
Provisional Application 62040488 · Aug 22, 2014
Related Publication 20170304301A1 · Oct 26, 2017