Methods for preparing internally constrained peptides and peptidomimetics
US-9221871-B2 · Dec 29, 2015 · US
Method for producing intermediates for the production of novel macrocycles that are inhibitors of the proteasomic degradation of p27, such as argyrin and derivatives thereof, and uses of said macrocycles
US9458200B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9458200-B2 |
| Application number | US-200913000516-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jun 23, 2009 |
| Priority date | Jun 23, 2008 |
| Publication date | Oct 4, 2016 |
| Grant date | Oct 4, 2016 |
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Abstract
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The present invention relates to the use of particular macrocycles that are inhibitors of the proteasomic degradation of p27, in particular argyrin and derivatives thereof, for a treatment in a variety of conditions, such as the induction of immunotolerance, autoimmune diseases, bacterial infections, and proliferative diseases, such as cancers.
First claim
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The invention claimed is: 1. A method for producing a macrocycle compound, wherein reaction steps of the method are shown by the following general scheme: wherein R 1 is hydrogen or C 1 -C 4 alkyl, which is unsubstituted or substituted by OH; R 2 is CH 2 Ot-Bu, hydrogen, or C 1 -C 4 alkyl, which is unsubstituted or substituted by OH; R 3 is hydrogen or OMe; R 4 is hydrogen or C 1 -C 4 alkyl; R 5 is hydrogen ; R 6 is C 1 -C 4 alkyl; R 7 is hydrogen or Me; R 8 is hydrogen or Boc; R 9 is hydrogen or Et; X is C═CH 2 ; and PG is a protecting group, wherein the method is performed without enzymatic resolution. 2. The method, according to claim 1 , wherein the PG is selected from the group consisting of: Boc, Fmoc, and Cbz. 3. The method for producing a macrocycle compound according to claim 1 , wherein said macrocycle compound is selected from an argyrin A to F. 4. The method for producing a macrocycle compound according to claim 1 , wherein the synthesis comprises solid phase peptide synthesis. 5. The method for producing a macrocycle compound according to claim 1 , wherein said macrocycle compound is selected from the following formulae:
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- What does patent US9458200B2 cover?
- The present invention relates to the use of particular macrocycles that are inhibitors of the proteasomic degradation of p27, in particular argyrin and derivatives thereof, for a treatment in a variety of conditions, such as the induction of immunotolerance, autoimmune diseases, bacterial infections, and proliferative diseases, such as cancers.
- Who is the assignee on this patent?
- Kalesse Markus, Malek Nisar, Frank Ronald, and 8 more
- What technology area does this patent fall under?
- Primary CPC classification C07K7/56. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Oct 04 2016 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 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).