C-3 and C-17 modified triterpenoids as HIV-1 inhibitors

Patent metadata

Field	Value
Publication number	US-11084845-B2
Application number	US-201916534208-A
Country	US
Kind code	B2
Filing date	Aug 7, 2019
Priority date	Feb 4, 2016
Publication date	Aug 10, 2021
Grant date	Aug 10, 2021

Abstract

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I:These compounds are useful for the treatment of HIV and AIDS.

First claim

What is claimed is:

1. A pharmaceutical composition comprising the compound

or salt thereof and further comprising one or more pharmaceutically acceptable carriers, excipients, and/or diluents.

2. A composition according to claim 1 suitable for administration orally, or for administration parenterally.

3. A method of treating HIV infection in a mammal comprising administering to said mammal a compound or salt of claim 1 wherein said administration is oral.

4. A method of treating HIV infection in a mammal comprising administering to said mammal a compound or salt of claim 1 wherein said administration is parenterally.

5. The method of claim 3 wherein said method further comprises administration of one or more other agents useful for treatment of HIV infection in a mammal.

6. The method of claim 5 wherein said other agent is S/GSK1265744.

7. The method of claim 4 wherein said method further comprises administration of at least one other agent useful for treatment of HIV infection in a mammal.

8. The method of claim 7 wherein said other agent is S/GSK1265744.

Assignees

• Viiv Healthcare Uk No 5 Ltd

Inventors

• Chen Jie
• Chen Yan
• Dicker Ira B
• Hartz Richard A
• Meanwell Nicholas A
• Nowicka-Sans Beata
• Regueiro-Ren Alicia
• Sit Sing-Yuen
• Sin Ny
• Swidorski Jacob
• Venables Brian Lee

Classifications

• A61K31/56

  Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids · CPC title

• C12N9/506 Primary

  derived from RNA viruses · CPC title

• C12N2740/16222

  New viral proteins or individual genes, new structural or functional aspects of known viral proteins or genes · CPC title

• A61P31/18 Primary

  for HIV · CPC title

• C07J63/008 Primary

  Expansion of ring D by one atom, e.g. D homo steroids · CPC title