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Penicillin-binding protein inhibitors

A compound and solvate technology, applied in the field of penicillin-binding protein inhibitors, can solve problems such as loss of efficacy

Pending Publication Date: 2021-03-09
VENATORX PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

They are very valuable treatment options, but are currently losing efficacy due to the evolution and spread of resistance genes, resulting in multidrug resistant bacterial organisms

Method used

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  • Penicillin-binding protein inhibitors
  • Penicillin-binding protein inhibitors
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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0414] Compound preparation

[0415] Described herein are compounds of formula (Ia), (IIa), (IIa-1), (Ib), (IIb) or (IIb-1) that inhibit the activity of penicillin-binding proteins and methods for their preparation. Also described herein are pharmaceutically acceptable salts, solvates, stereoisomers, mutual isomers, N-oxides, dimers or trimers.

[0416] Compounds of formula (Ia), (IIa), (IIa-1), (Ib), (IIb) or (IIb-1) can be synthesized using standard synthetic reactions known to those skilled in the art or using methods known in the art synthesis. These reactions can be used in a linear sequence to provide compounds, or they can be used to synthesize fragments that are subsequently ligated by methods known in the art.

[0417] Starting materials for the synthesis of compounds described herein can be synthesized or can be obtained from commercial sources. The compounds described herein and other related compounds with different substituents can be synthesized using techniq...

Embodiment 1

[0480] Example 1: (R)-3-((R)-2-amino-2-phenylacetamido)-2-hydroxy-3,4-dihydro-2H-benzo[e][1,2 ]oxaborinane-8-carboxylic acid

[0481]

Embodiment 2

[0482] Example 2: (R)-3-((S)-2-amino-2-phenylacetamido)-2-hydroxy-3,4-dihydro-2H-benzo[e][1,2 ]oxaborinane-8-carboxylic acid

[0483]

[0484] According to general procedure C, the chloride was treated with LiHMDS, then coupled with Boc-D-α-phenylglycine in the presence of HATU and NMM, after flash chromatography on silica gel (hexane-Et 2 O, 4:1–1:2) purified to give two products that were tentatively assigned as two diastereomers (Boc-D-α-phenylglycine that racemized during the reaction). ESI-MSm / z663(MH) + .

[0485] with BCl 3 Workup of these two products afforded the two title compounds (1 and 2). ESI-MS m / z 341(MH) + .

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Abstract

Described herein are certain boron-containing compounds, compositions, preparations and their use as modulators of the transpeptidase function of bacterial penicillin-binding proteins and as antibacterial agents. In some embodiments, the compounds described herein inhibit penicillin-binding proteins. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.

Description

[0001] cross reference [0002] This application claims the benefit of U.S. Provisional Application Serial No. 62 / 676,793, filed May 25, 2018, and U.S. Provisional Application Serial No. 62 / 772,056, filed November 27, 2018, which are incorporated by reference in their entirety into this article. [0003] Statement Regarding Federally Funded Research [0004] This invention is based on SBIR grant 5R43AI094827 from the National Institutes of Health (NIH) and Federal Award 6 IDSEP16030-01-02 awarded by the Assistant Secretary for Preparedness and Response Office of Health and Human Affairs (HHS / ASPR) under CARB-XPass Through Entity, Subfund 4500002377 and contract HDTRA117C0070 awarded by the Defense Threat Reduction Agency (DTRA), with support from the U.S. Government. The US Government has certain rights in this invention. Background technique [0005] Antibiotics are the most effective drugs clinically used to treat bacterial-associated infectious diseases. They are ver...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F5/02C07F5/04A61K31/69A61P31/04
CPCA61P31/04C07F5/025
Inventor 克里斯多佛·J·伯恩斯丹尼斯·戴格尔楚国华朱迪·哈姆里克史蒂文·A·博伊德阿莉森·L·祖利尤根·F·米萨罗斯斯蒂芬·M·康登罗伯特·E·李·特劳特卡伦·L·梅尔斯徐真荣
Owner VENATORX PHARMA INC
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