Design, Synthesis, and SAR of C-3 Benzoic Acid, C-17 Triterpenoid Derivatives. Identification of the HIV-1 Maturation Inhibitor 4-((1R,3aS,5aR,5bR,7aR,11aS,11bR,13aR,13bR)-3a …

A Regueiro-Ren, JJ Swidorski, Z Liu… - Journal of Medicinal …, 2018 - ACS Publications
GSK3532795, formerly known as BMS-955176 (1), is a potent, orally active, second-
generation HIV-1 maturation inhibitor (MI) that advanced through phase IIb clinical trials. The …

Synthesis and anti-HIV activity of bi-functional triterpene derivatives

L Huang, D Yu, P Ho, KH Lee… - Letters in Drug Design & …, 2007 - ingentaconnect.com
We previously reported a bi-functional betulinic acid derivative, A12-2 (4), containing an
optimized C-28 side chain that exhibits potent anti-HIV activity by inhibiting both HIV-1 entry …

The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation

Y Chen, SY Sit, J Chen, JJ Swidorski, Z Liu… - Bioorganic & medicinal …, 2018 - Elsevier
The design and synthesis of a series of C28 amine-based betulinic acid derivatives as HIV-1
maturation inhibitors is described. This series represents a continuation of efforts following …

C-3 cycloalkenyl triterpenoids with HIV maturation inhibitory activity

J Swidorski, NA Meanwell, A Regueiro-Ren… - US Patent …, 2014 - Google Patents
First worldwide family litigation filed litigation Critical https://patents. darts-ip. com/? family=
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C-17 bicyclic amines of triterpenoids with HIV maturation inhibitory activity

N Sin, Z Liu, J Swidorski, SY Sit, J Chen… - US Patent …, 2014 - Google Patents
Compounds having drug and bio-affecting properties, their pharmaceutical compositions
and methods of use are set forth. In particular, C-17 bicyclic amines of triterpenoids that …

Inhibitors of HIV-1 maturation: Development of structure–activity relationship for C-28 amides based on C-3 benzoic acid-modified triterpenoids

JJ Swidorski, Z Liu, SY Sit, J Chen, Y Chen… - Bioorganic & Medicinal …, 2016 - Elsevier
We have recently reported on the discovery of a C-3 benzoic acid (1) as a suitable
replacement for the dimethyl succinate side chain of bevirimat (2), an HIV-1 maturation …

Anti-AIDS agents 81. Design, synthesis, and structure− activity relationship study of betulinic acid and moronic acid derivatives as potent HIV maturation inhibitors

K Qian, RY Kuo, CH Chen, L Huang… - Journal of medicinal …, 2010 - ACS Publications
In our continuing study of triterpene derivatives as potent anti-HIV agents, different C-3
conformationally restricted betulinic acid (BA, 1) derivatives were designed and synthesized …

Design, synthesis, and bio-evaluation of novel triterpenoid derivatives as anti-HIV-1 compounds

R Takeuchi, K Ogihara, J Fujimoto, K Sato… - Bioorganic & Medicinal …, 2022 - Elsevier
Two betulinic acid derivatives, RPR103611 (2) and IC9564 (3) were previously reported to
be potent HIV-1 entry inhibitors. In this current study, a SAR study of the triterpenoid moiety …

Synthesis, Structure–Activity Relationships, and In Vivo Evaluation of Novel C-17 Amine Derivatives Based on GSK3640254 as HIV-1 Maturation Inhibitors with Broad …

RA Hartz, L Xu, SY Sit, J Chen… - Journal of Medicinal …, 2022 - ACS Publications
An investigation of the structure–activity relationships of a series of HIV-1 maturation
inhibitors (MIs) based on GSK3640254 (4) was conducted by incorporating novel C-17 …

Triterpenoids with HIV maturation inhibitory activity

SY Sit, Y Chen, J Chen, J Swidorski… - US Patent …, 2016 - Google Patents
First worldwide family litigation filed litigation Critical https://patents. darts-ip. com/? family=
53002809&utm_source= google_patent&utm_medium= platform_link&utm_campaign …