CD4 mimic compound with anti-HIV activity

Patent metadata

Field	Value
Publication number	US-12508251-B2
Application number	US-202017755366-A
Country	US
Kind code	B2
Filing date	Oct 29, 2020
Priority date	Oct 29, 2019
Publication date	Dec 30, 2025
Grant date	Dec 30, 2025

Abstract

CD4 mimic compounds having improved efficacy for anti-HIV treatment and more improved pharmacokinetics are provided. The compounds are represented by formula (I): wherein R1 is C2H4(OC2H4)n—OCH3 or CmH2m+1; R2 is O or NH; n is 3 to 25; and m is 4 to 22, or a salt thereof. HIV infection inhibitor compositions including the compound or a salt thereof as an active ingredient are also disclosed.

First claim

The invention claimed is:

1 . A compound represented by the formula (I):

wherein R 1 is C 2 H 4 (OC 2 H 4 ) n —OCH 3 or C m H 2m+1 ; R 2 is O or NH; n is 3 to 25; and m is 4 to 22, or a salt thereof.

2 . The compound or a salt thereof according to claim 1 , represented by the formula:

wherein n is 3 to 25.

3 . The compound or a salt thereof according to claim 2 , wherein n is 4 to 23.

4 . An HIV infection inhibitor composition comprising a compound or a salt thereof according to claim 1 .

5 . A method for treating HIV infection, comprising administering a composition of claim 4 to a patient in need thereof.

6 . The method according to claim 5 , wherein the HIV infection inhibitor is administered in combination with an anti-HIV antibody.

7 . The method according to claim 6 , wherein the anti-HIV antibody is a neutralizing antibody specific to V3 loop on a surface of HIV-1.

8 . A method for treating HIV infection, comprising administering a compound or a salt thereof of claim 1 to a patient in need thereof.

9 . The method of claim 8 , further comprising administering an anti-HIV antibody with said compound or salt thereof.

10 . The method of claim 9 , wherein the anti-HIV antibody is a neutralizing antibody specific to V3 loop on a surface of HIV-1.

Assignees

• Univ Kumamoto Nat Univ Corp
• Univ Nat Corp Tokyo Medical & Dental
• Japan As Represented By Director General Of Nat Institute Of Infectious Diseases

Inventors

• Matsushita Shuzo
• Yoshimura Kazuhisa
• Tamamura Hirokazu
• Masuda Ami
• Takahashi Kohei
• Kobayakawa Takuya
• Harada Shigeyoshi
• Miura Tomoyuki

Classifications

• C07D221/20 Primary

  Spiro-condensed ring systems · CPC title

• A61K39/42

  viral · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P31/18 Primary

  for HIV · CPC title

• A61K31/4468

  having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl · CPC title