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Compounds, compositions, and methods for selectively inhibiting beta-glucuronidases and alleviating side effects associated with drug treatment induced diarrhea

A compound, pharmaceutical technology, applied in the direction of drug combination, silicon organic compounds, chemical instruments and methods, etc., can solve the problem of partial or complete elimination of intestinal bacteria is not ideal, increased risk of pathogenic bacterial infection, drug resistance crisis, etc.

Pending Publication Date: 2021-06-11
シムベリックスインコーポレーティッド
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, partial or complete removal of gut bacteria is not ideal for subjects already challenged with cancer and chemotherapy
Second, even elimination of commensal gut bacteria from healthy subjects greatly increased the risk of infection by pathogenic bacteria, including EHEC (Escherichia coli) and Clostridium difficile
Third, bacterial resistance to antibiotics is a crisis for human health, and the unnecessary use of antibiotics is a significant contributor to this crisis

Method used

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  • Compounds, compositions, and methods for selectively inhibiting beta-glucuronidases and alleviating side effects associated with drug treatment induced diarrhea
  • Compounds, compositions, and methods for selectively inhibiting beta-glucuronidases and alleviating side effects associated with drug treatment induced diarrhea
  • Compounds, compositions, and methods for selectively inhibiting beta-glucuronidases and alleviating side effects associated with drug treatment induced diarrhea

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0524] 2,6-Dimethyl-3-nitro-benzoic acid

[0525]

[0526] To the acid (10 g, 66.6 mmol) in nitromethane (100 mL) cooled to 0 °C was added concentrated sulfuric acid (67 mL), after stirring for 10 minutes, then concentrated nitric acid (42 mL) was added dropwise over 1 hour. The reaction mixture was stirred for 6 hours. After adding ice water (300 mL), ethyl acetate was added, and the two layers were separated. The organic layer was then dried over magnesium sulfate and concentrated in vacuo to give the desired product. This crude product was used in the next step.

Embodiment 2

[0528] (2,6-Dimethyl-3-nitro-phenyl)methanol

[0529]

[0530] To nitric acid (2.7 g, 13.8 mmol) in THF (15 mL) cooled to 0° C. was added a 2.0 M borane / THF complex solution (14.0 mL). The contents were then stirred at room temperature for 4 hours. The reaction mixture was then quenched with methanol. Ethyl acetate was then added followed by saturated NaHCO 3 . The organic layer was then dried over magnesium sulfate and concentrated under vacuum to provide the desired product.

Embodiment 3

[0532] (3-amino-2,6-dimethyl-phenyl)methanol

[0533]

[0534] To a solution of nitroalcohol (20 g, 110 mmol) in methanol (200 mL) was added 10% Pd / C (2 g). The contents were then pressurized under hydrogen at 80 psi for 16 hours. After filtration through celite and concentration in vacuo, the crude product was used in the next step.

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PUM

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Abstract

The present disclosure describes compounds and compositions that inhibit beta-glucuronidase activity, and methods for attenuating the side effects of one or more drugs and improving the efficacy of drugs by administration of selective beta-glucuronidase inhibitors.

Description

[0001] This invention was made with Government support under Grant No. 1R43CA180270 awarded by the National Cancer Institute, National Institutes of Health. The government has certain rights in this invention. [0002] Cross References to Related Applications [0003] This application claims the benefit of U.S. Provisional Application No. 62 / 555,847, filed September 8, 2017, the entire contents of which are incorporated herein by reference. technical field [0004] The disclosure describes compounds and compositions that inhibit the activity of β-glucuronidase (β-glucuronidase), as well as reducing the effect of one or more drugs by administering a selective β-glucuronidase inhibitor. Side effects and ways to improve drug efficacy. Background technique [0005] Diarrhea is a common adverse effect associated with drug therapy. Hundreds of drugs have been implicated in causing diarrhea or gastrointestinal distress, including antibiotics, laxatives, antacids containing magne...

Claims

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Application Information

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IPC IPC(8): C07D215/227C07D413/12C07D405/12C07D401/12C07F7/08A61P35/00A61P35/02A61P9/00A61P27/02A61P31/00A61P37/06A61P29/00A61P37/08A61P37/02A61K31/4704A61K31/4709A61K31/496A61K31/5377A61K31/695
CPCC07D215/227C07D413/12C07D405/12C07D401/12C07F7/0812A61P35/00A61P35/02A61P9/00A61P27/02A61P31/00A61P37/06A61P29/00A61P37/08A61P37/02C07H15/26A61P1/12A61K45/06
Inventor F·X·塔瓦雷斯B·D·华莱士W·派特森
Owner シムベリックスインコーポレーティッド
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