IP Library › Granted Patent US 10,245,275
Granted Patent B2
US 10,245,275 · App. 15/678,381 · Granted Apr 2, 2019

Triterpenoids with HIV maturation inhibitory activity

Inventors: Sing-Yuen Sit (Meriden, CT); Yan Chen (Wallingford, CT); Jie Chen (Madison, CT); Jacob Swidorski (Southington, CT); Brian Lee Venables (Durham, CT); Ny Sin (East Hampton, CT); Nicholas A. Meanwell (East Hampton, CT); Alicia Regueiro-Ren (Middletown, CT); Richard A. Hartz (Middletown, CT); Li Xu (Middletown, CT); Zheng Liu (Beacon Falls, CT)
Assignee: VIIV HEALTHCARE UK (NO. 4) LIMITED
A61K31/58A61K45/06C07C309/65C07F5/025C07F5/04C07J63/008C07C2601/16
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Quick Facts
Patent No.
US 10,245,275
App. No.
15/678,381
Granted
Apr 2, 2019
Kind
B2
Abstract

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: with X selected from C 4-8 cycloalkyl, C 4-8 cycloalkenyl, C 4-9 spirocycloalkyl, C 4-9 spirocycloalkenyl, C 4-8 oxacycloalkyl, C 4-8 dioxacycloalkyl, C 6-8 oxacycloalkenyl, C 6-8 dioxacycloalkenyl, C 6 cyclodialkenyl, C 6 oxacyclodialkenyl, C 6-9 oxaspirocycloalkyl and C 6-9 oxaspirocycloalkenyl ring, such that X is substituted with A, wherein A is —C 1-6 alkyl-halo. These compounds are useful for the treatment of HIV and AIDS.

Claims (5)

1. A method for treating a human infected with HIV comprising administering to said human the compound

or a pharmaceutically acceptable salt thereof and an additional agent selected from the group consisting of dolutegravir, GSK1265744, and 3TC.

2. The method of claim 1 wherein said additional agent is dolutegravir.

3. The method of claim 1 wherein said additional agent is GSK1265744.

4. The method of claim 1 wherein said additional agent is 3TC.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 29, 2017
From: SIT, SING-YUEN; CHEN, YAN; CHEN, JIE; SWIDORSKI, JACOB; VENABLES, BRIAN LEE; SIN, NY; MEANWELL, NICHOLAS A.; REGUEIRO-REN, ALICIA; HARTZ, RICHARD A.; XU, LI; LIU, ZHENG
To: BRISTOL-MYERS SQUIBB COMPANY
Reel/Frame 043433/0433 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 29, 2017
From: BRISTOL-MYERS SQUIBB COMPANY
To: VIIV HEALTHCARE UK (NO.4) LIMITED
Reel/Frame 043433/0668 →
Continuity (4)
Continuation 15344756 · Nov 7, 2016
Continuation 14682179 · Apr 9, 2015
Provisional Application 61978306 · Apr 11, 2014
Related Publication 20170340650A1 · Nov 30, 2017