IP Library › Granted Patent US 10,201,533
Granted Patent B2
US 10,201,533 · App. 15/725,407 · Granted Feb 12, 2019

Substituted quinolizine derivatives useful as HIV integrase inhibitors

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Quick Facts
Patent No.
US 10,201,533
App. No.
15/725,407
Granted
Feb 12, 2019
Kind
B2
Abstract

The present invention relates to Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein X, Y, R 1 , R 2 , R 3 , R 4 , R 5 , R 9 and R 10 are as defined herein. The present invention also relates to compositions comprising at least one Substituted Quinolizine Derivative, and methods of using the Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.

Claims (17)

1. A compound selected from

or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising an effective amount of a compound according to claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

3. A method for the inhibition of HIV integrase in a subject in need thereof which comprises administering to the subject an effective amount of the compound according claim 1 , or a pharmaceutically acceptable salt thereof.

4. A method for the treatment of infection by HIV or for the treatment-of AIDS in a subject in need thereof, which comprises administering to the subject an effective amount of the compound according to claim 1 , or a pharmaceutically acceptable salt thereof.

5. The pharmaceutical composition of claim 2 , further comprising one or more additional therapeutic agents selected from, lamivudine, abacavir, ritonavir, darunavir, atazanavir, emtricitabine, tenofovir, rilpivirine and lopinavir.

6. The method of claim 4 , further comprising administering to the subject one or more additional therapeutic agents selected from, abacavir, lamivudine, ritonavir and lopinavir.

7. The compound of the formula

or a pharmaceutically acceptable salt thereof.

8. The compound of the formula

or a pharmaceutically acceptable salt thereof.

9. The compound of the formula

or a pharmaceutically acceptable salt thereof.

10. The compound of the formula

or a pharmaceutically acceptable salt thereof.

11. The compound of the formula

or a pharmaceutically acceptable salt thereof.

Assignments (1)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →