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Therapeutic modulators of the reverse mode of atp synthase

A compound and composition technology, applied in the direction of drug combination, organic active ingredient, heterocyclic compound active ingredient, etc.

Pending Publication Date: 2020-06-12
迈克尔大卫福雷斯特
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In fact, no journal published years after biorxiv submission would be very negative as one of the art points out

Method used

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  • Therapeutic modulators of the reverse mode of atp synthase
  • Therapeutic modulators of the reverse mode of atp synthase
  • Therapeutic modulators of the reverse mode of atp synthase

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[0186]

[0187] The structure on the left has a low EC50 against F1F0 ATP hydrolysis (0.018 μΜ), with a [EC50F1F0 ATP synthesis / EC50F1F0 ATP hydrolysis] ratio >5556. In rats, the drug (administration polyethylene glycol:water:ethanol, 1:1:1) was orally bioavailable (47%) with good pharmacokinetics (blood = 2.1 hours after intravenous administration of the drug half-life, Cmax is 21 microns, volume distribution = 2.39 liters / kg). On the right, where the hydrogen atom on the chiral carbon is replaced by deuterium, the deuterated analogue (KIE, [37]) that confers greater stereoisomer stability because of kinetic isotope effects is more preferred. Greater % deuterium enrichment at the chiral carbon (21 carbon atoms) and greater enantiomeric excess, more preferred embodiments. The other atom or isotope in other preferred embodiments positions the hydrogen at the chiral carbon, blocking its racemization, ensuring a permanent stereomeric excess. For example, fluorine. or carbo...

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Abstract

Compounds of the following formula (I) slow the ATP-hydrolysing mode of ATP synthase and are useful for treating various diseases and disorders including cancer, particularly cancers that utilize theWarburg effect.

Description

[0001] related application [0002] This application claims the priority of GB application numbers GB1711250.9 (submitted on July 13, 2017), GB1715756.1 (submitted on September 28, 2017), and GB1715758.7 (submitted on September 28, 2017). , GB1715938.5 (submitted on October 1, 2017), GB1716492.2 (submitted on October 9, 2017), GB1800092.7 (submitted on January 4, 2018), GB1800291.5 (submitted on January 8, 2018 Submitted), GB1800581.9 (submitted on January 15, 2018), GB1801536.2 (submitted on January 30, 2018), GB1806421.2 (submitted on April 19, 2018), GB1808331.1 (submitted on May 2018 21), GB1809497.9 (submitted on June 8, 2018), GB1810236.8 (submitted on June 21, 2018), GB1811188.0 (submitted on July 8, 2018) and PCT application number PCT / EP2018 / 051127 (filed 17 January 2017) which claims priority to some of the above applications and claims priority to GB Application No. GB1700772.5 (filed 17 January 2017). , GB1706046.8 (submitted on April 14, 2017), GB1707945.0 (submi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D233/56C07D251/54C07D403/06A61K31/4164A61K31/551A61P35/00
CPCC07D233/56C07D403/06C07D251/54A61P35/00A61K31/4164A61K31/53Y02A50/30C07D233/61
Inventor 迈克尔·大卫·福雷斯特
Owner 迈克尔大卫福雷斯特
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