β-lactam compounds, their use, and methods for their preparation.

Novel β-lactam compounds effectively address the limitations of aztreonam derivatives by providing strong antibacterial activity against Gram-negative bacteria with minimal drug resistance through specific synthesis methods.

JP7876847B2Inactive Publication Date: 2026-06-22GUANGZHOU HC PHARM CO LTD
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Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
GUANGZHOU HC PHARM CO LTD
Filing Date
2021-04-30
Publication Date
2026-06-22
Estimated Expiration
Not applicable · inactive patent

AI Technical Summary

Technical Problem

Current antibacterial agents, particularly aztreonam derivatives, exhibit insufficient antibacterial activity against Gram-negative bacteria and have issues with drug resistance.

Method used

Development of novel β-lactam compounds represented by general formulas (I) and (I-1) to (I-2), which are synthesized through specific chemical reactions involving protecting groups and subsequent removal, ensuring effective antibacterial activity against Gram-negative bacteria with negligible drug resistance.

Benefits of technology

The compounds demonstrate excellent antibacterial activity against Gram-negative bacteria such as Escherichia coli and Pseudomonas aeruginosa while showing negligible drug resistance.

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Patent Text Reader

Abstract

The present invention relates to a compound represented by the following general formula (I): R1 and R2 each independently represent a hydrogen atom or an optionally substituted C1-10 linear or branched alkyl, or R1 and R2 together form a cycloalkyl having 3 to 8 ring carbon atoms; R3 and R4 each independently represent a hydrogen atom or an optionally substituted C1-10 linear or branched alkyl, or an optionally substituted C6-12 aryl; or R3 and R4 together form a cycloalkyl having 3 to 8 ring carbon atoms; X represents C or N; and Y represents an optionally substituted linear or branched alkenyl or alkynyl having 2 to 6 carbon atoms, or carboxyl. The compound has good antibacterial activity against bacteria, particularly gram-negative bacteria, low drug resistance, and good prospects for effective treatment of various pathologies. [Formula 1] TIFF2023527917000064.tif58170
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Citation Information

Patent Citations

  • CN1058593A

  • CN106164072A

  • JP1983206589A

  • JP1986091187A

  • US20140275007A1