Therapeutic modulators of the reverse mode of atp synthase
What is Al technical title?
Al technical title is built by PatSnap Al team. It summarizes the technical point description of the patent document.
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
View PDF7 Cites 1 Cited by
Summary
Abstract
Description
Claims
Application Information
AI Technical Summary
This helps you quickly interpret patents by identifying the three key elements:
Problems solved by technology
Method used
Benefits of technology
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
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more
Image
Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
Click on the blue label to locate the original text in one second.
Reading with bidirectional positioning of images and text.
Smart Image
Examples
Experimental program
Comparison scheme
Effect test
specific Embodiment approach
[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...
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more
PUM
Login to view more
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
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more
Application Information
Patent Timeline
Application Date:The date an application was filed.
Publication Date:The date a patent or application was officially published.
First Publication Date:The earliest publication date of a patent with the same application number.
Issue Date:Publication date of the patent grant document.
PCT Entry Date:The Entry date of PCT National Phase.
Estimated Expiry Date:The statutory expiry date of a patent right according to the Patent Law, and it is the longest term of protection that the patent right can achieve without the termination of the patent right due to other reasons(Term extension factor has been taken into account ).
Invalid Date:Actual expiry date is based on effective date or publication date of legal transaction data of invalid patent.
Login to view more 
Login to view more