IP Library › Granted Patent US 10,780,102
Granted Patent B2
US 10,780,102 · App. 16/253,393 · Granted Sep 22, 2020

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
A61K31/58A61K31/54A61K45/06C07C309/65C07F5/025C07F5/04C07J63/008C07C2601/16
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Quick Facts
Patent No.
US 10,780,102
App. No.
16/253,393
Granted
Sep 22, 2020
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 (3)

1. A pharmaceutical composition comprising a pharmaceutically acceptable salt of the compound

2. A pharmaceutical composition according to claim 1 wherein said composition is in the form of a tablet.

3. A pharmaceutical composition according to claim 1 further comprising dolutegravir.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 22, 2019
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 048083/0428 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 22, 2019
From: BRISTOL-MYERS SQUIBB COMPANY
To: VIIV HEALTHCARE UK (NO.4) LIMITED
Reel/Frame 048083/0583 →
Continuity (5)
Continuation 15678381 · Aug 16, 2017
Continuation 15344756 · Nov 7, 2016
Continuation 14682179 · Apr 9, 2015
Provisional Application 61978306 · Apr 11, 2014
Related Publication 20190151336A1 · May 23, 2019