Hybrid cyclic libraries and screens thereof
US-9250237-B2 · Feb 2, 2016 · US
Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses thereof
US10774110B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10774110-B2 |
| Application number | US-201716073746-A |
| Country | US |
| Kind code | B2 |
| Filing date | Feb 3, 2017 |
| Priority date | Feb 4, 2016 |
| Publication date | Sep 15, 2020 |
| Grant date | Sep 15, 2020 |
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Abstract
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A compound of Formula (I), and its analogs are provided. Compositions that include Formula I can be used to inhibit human equilibrative nucleoside transporter 1, increase adenosine signaling and produce effects that include increasing antiviral activity, increasing antiparasitic activity, increasing alcohol tolerance, decreasing pain protecting from ischemia as well as many other conditions.
First claim
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What is claimed is: 1. A compound selected from the group consisting of: wherein each R 1 and R 2 is independently selected from the group consisting of OH, NH 2 , SH, and hydrogen; wherein n is an integer selected from 0 to 6, each R 1 , R 2 , and R 3 is independently selected from the group consisting of methyl, ethyl, propyl, isopropyl, phenyl, OH, NH 2 , and SH; wherein each R 1 and R 2 is independently selected from the group consisting of OH, NH 2 , SH, and hydrogen; wherein each A, B, X, Y, and Z is independently selected from the group consisting of CH and N; wherein each R 1 to R 4 is independently selected from the group consisting of methyl, ethyl, propyl, isopropyl, phenyl, OH, NH 2 , and SH. 2. A method of inhibiting human equilibrative nucleoside transporter 1 (ENT1) comprising administering to a subject in need thereof an effective amount of a compound of claim 1 , thereby inhibiting ENT1. 3. A method of increasing adenosine signaling comprising administering to a subject in need thereof an effective amount of a compound of claim 1 , thereby increasing adenosine signaling. 4. A macrocyclic compound according to Formula (I): wherein residue 1, residue 2, residue 3, and residue 4 are exchanged and selected from below: Peptide Residue 1 Residue 2 Residue 3 Residue 4 JW95-1 mGly dPro mGly Phe JW95-2 mAla dPro mGly Phe JW95-3 mLeu dPro mGly Phe JW95-4 mSer dPro mGly Phe JW95-5 mPhe dPro mGly Phe JW95-6 mGly dPro mAla Phe JW95-7 mAla dPro mAla Phe JW95-8 mLeu dPro mAla Phe JW95-9 mSer dPro mAla Phe JW95-10 mPhe dPro mAla Phe JW95-11 mGly dPro mLeu Phe JW95-12 mAla dPro mLeu Phe JW95-13 mLeu dPro mLeu Phe JW95-14 mSer dPro mLeu Phe JW95-15 mPhe dPro mLeu Phe JW95-16 mGly dPro mSer Phe JW95-17 mAla dPro mSer Phe JW95-18 mLeu dPro mSer Phe JW95-19 mSer dPro mSer Phe JW95-20 mPhe dPro mSer Phe JW95-21 mGly dPro mPhe Phe JW95-22 mAla dPro mPhe Phe JW95-23 mLeu dPro mPhe Phe JW95-24 mSer dPro mPhe Phe JW95-25 mPhe dPro mPhe Phe 95-15-1 mLeu dPro mPhe Phe 95-15-2 mdLeu dPro mPhe Phe 95-15-3 mLeu dPro mPhe dhoPhe 95-15-4 Leu dPro mPhe Phe 95-15-5 mlle dPro mPhe Phe 95-15-6 mNle dPro mPhe Phe 95-15-7 mLeu Pro mPhe Phe 95-15-8 mLeu Gly mPhe Phe 95-15-9 mLeu dPro mdPhe Phe 95-15-10 mLeu dPro Phe Phe 95-15-11 mLeu dPro mPhe dPhe
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- What does patent US10774110B2 cover?
- A compound of Formula (I), and its analogs are provided. Compositions that include Formula I can be used to inhibit human equilibrative nucleoside transporter 1, increase adenosine signaling and produce effects that include increasing antiviral activity, increasing antiparasitic activity, increasing alcohol tolerance, decreasing pain protecting from ischemia as well as many other conditions.
- Who is the assignee on this patent?
- Univ Johns Hopkins
- What technology area does this patent fall under?
- Primary CPC classification C07K7/02. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Sep 15 2020 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 2 related publications on this page (citations in our corpus or others sharing the same primary CPC).