Pyrrolopyridine derivative and use thereof

Inventors

Kim, Kyungjin • KIM, Uk-Il • BANG, Hyung Tae • Lee, Seul Ki • Han, Si Yeon

Assignees

ST Pharm Co Ltd

Abstract

The present invention relates to a pyrrolopyridine derivative, a racemate thereof, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and use thereof. The compound of the present invention has high selectivity and bioactivity against human immunodeficiency virus (HIV), and low toxicity, thus being useful as a therapeutic agent for viral infection, particularly human immunodeficiency virus (HIV) infection.

Core Innovation

The disclosure is directed to a pyrrolopyridine derivative represented by Formula I, together with a racemate, a stereoisomer, and pharmaceutically acceptable salts. Formula I defines substituent variables including A, R1-R6, B, and n, with n being 1, 2, 3, or 4, depending on embodiments. A is specified by a group selection that includes hydroxy, amino, azido, cyano, trifluoromethyl, COR1, C̄NOHR2, B(OH)2, SO3H, P̄O(OH)2, and heteroaryl.

R1 and R2 are each independently defined as NR3R4, NR3OR4, or OR5, while R3 and R4 are each independently hydrogen, C1-6 alkyl, or heteroaryl. R5 is defined by a group selection including (CH2)n-O-(CH2)-O-CH3, (CH2)n-OCOO-CH3, and (CH)CH3-OCOO-C3-6 cycloalkyl or (CH2)n-heteroaryl. B is defined as (CH2)n-R6, and R6 is defined by a group selection that includes hydroxy, amino, azido, cyano, trifluoromethyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, and multiple carbonyl- and heterocycle-containing options, including aryl and heteroaryl substituents.

The document further identifies anti-HIV pharmaceutical compositions and methods of treating anti-HIV by administering a therapeutically effective amount of the Formula I compound, including racemates, stereoisomers, or pharmaceutically acceptable salts. The disclosure provides exemplified compounds corresponding to the Formula I scaffold, and it reports comparative antiviral activity and cytotoxicity data using MT-4 and NL4-3 HIV-1 wild-type assessments, including EC50 and CC50 values reported as measures of viral inhibition and cytotoxicity.

Claims Coverage

The independent claims cover three inventive features: a Formula I pyrrolopyridine derivative scaffold, an anti-HIV pharmaceutical composition, and an anti-HIV treatment method. The key inventive structure is defined by substituent variables A, R1-R6, B, and n, and coverage extends to racemate, stereoisomer, and pharmaceutically acceptable salt forms.

The claim set centers on a Formula I pyrrolopyridine derivative defined by A, R1-R6, B, and n, including racemate, stereoisomer, and salt variants. Coverage also extends to anti-HIV pharmaceutical compositions and anti-HIV treatment methods based on administration of a therapeutically effective amount of the Formula I compound.

Stated Advantages

Documented Applications