DISUBSTITUTED AMINO ACIDS AND METHODS OF PREPARATION AND USE THEREOF (Fri, 09 May 2014)
<p id="p-0001" num="0000">Provided are crystalline α, α-disubstituted amino acids and their crystalline salts containing a terminal alkene on one of their side chains, as well as optionally crystalline halogenated and deuterated analogs of the α, α-disubstituted amino acids and their salts; methods of making these, and methods of using these.</p>
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DISUBSTITUTED AMINO ACIDS AND METHODS OF PREPARATION AND USE THEREOF (Fri, 09 May 2014)
Provided are crystalline α, α-disubstituted amino acids and their crystalline salts containing a terminal alkene on one of their side chains, as well as optionally crystalline halogenated and deuterated analogs of the a, a-disubstituted amino acids and their salts; methods of making these, and methods of using these.
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PEPTIDOMIMETIC MACROCYCLES (Fri, 18 Oct 2013)
<p id="p-0001" num="0000">Provided herein are peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.</p>
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TRIAZOLE-CROSSLINKED AND THIOETHER-CROSSLINKED PEPTIDOMIMETIC MACROCYCLES (Fri, 23 Aug 2013)
Provided herein are peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.
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PEPTIDOMIMETIC MACROCYCLES (Fri, 23 Aug 2013)
Provided herein are peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.
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TRIAZOLE-CROSSLINKED AND THIOETHER-CROSSLINKED PEPTIDOMIMETIC MACROCYCLES (Fri, 16 Aug 2013)
<p id="p-0001" num="0000">Provided herein are peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.</p>
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PEPTIDOMIMETIC MACROCYCLES (Fri, 17 May 2013)
<p id="p-0001" num="0000">The present invention provides peptidomimetic macrocycles capable of modulating growth hormone levels and methods of using such macrocycles for the treatment of disease.</p>
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PEPTIDOMIMETIC MACROCYCLES (Fri, 26 Apr 2013)
Provided are novel peptidomimetic macrocycles and methods of using the macrocycles for the treatment of disease.
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PEPTIDOMIMETIC MACROCYLES (Fri, 26 Apr 2013)
The present invention provides peptidomimetic macrocycles capable of modulating growth hormone levels and methods of using such macrocycles for the treatment of disease.
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Triazole linked macrocyclic peptides (Thu, 07 Mar 2013)
The present invention provides novel peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production.
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Triazole linked macrocyclic peptides (Thu, 07 Mar 2013)
The present invention provides novel peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production.
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PEPTIDOMIMETIC MACROCYCLES (Fri, 21 Dec 2012)
The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.
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Peptidomimetic macrocycles (Fri, 06 Jul 2012)
<p id="p-0001" num="0000">Biologically active crosslinked polypeptides with improved properties relative to their corresponding precursor polypeptides; and methods of making and identifying such improved polypeptides.</p>
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PEPTIDOMIMETIC MACROCYCLES (Fri, 17 Feb 2012)
The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.
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PEPTIDOMIMETIC MACROCYCLES WITH TRIAZOLE LINKERS (Fri, 17 Feb 2012)
The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.
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PEPTIDOMIMETIC MACROCYCLES WITH THIOETHER LINKERS (Fri, 17 Feb 2012)
The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.
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PEPTIDOMIMETIC MACROCYCLES (Fri, 17 Feb 2012)
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Triazole macrocycle systems (Fri, 28 Oct 2011)
<p id="p-0001" num="0000">Provided herein are novel alkynyl and azide containing amino acids; kits containing these amino acids; peptides containing these amino acids; peptide macrocycles whose secondary structures are stabilized with linkers containing triazoles synthesized by reacting the side chains of the alkynyl and azide containing amino acids; and methods of making and using the alkynyl and azide containing amino acids, kits, peptides, triazole containing linkers, and peptide macrocycles.</p>
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PEPTIDOMIMETIC MACROCYCLES (Fri, 16 Sep 2011)
<p id="p-0001" num="0000">The present invention provides biologically active peptidomimetic macrocycles with improved properties, such as protease resistance, relative to their corresponding polypeptides. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.</p>
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Biologically Active Peptidomimetic Macrocycles (Fri, 17 Jun 2011)
<p id="p-0001" num="0000">The present invention provides biologically active peptidomimetic macrocycles with improved properties relative to their corresponding polypeptides. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.</p>
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IMPROVED PEPTIDOMIMETIC MACROCYCLES (Fri, 22 Apr 2011)
The present invention provides biologically active peptidomimetic macrocycles with improved properties, such as protease resistance, relative to their corresponding polypeptides. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.
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IMPROVED PEPTIDOMIMETIC MACROCYCLES (Fri, 22 Apr 2011)
The present invention provides biologically active peptidomimetic macrocycles with improved properties, such as protease resistance, relative to their corresponding polypeptides. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.</p>
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PEPTIDOMIMETIC MACROCYCLES (Fri, 01 Apr 2011)
Disclosed are peptidomimetic macrocycles comprising a helix, such as an alpha helix, and methods of using such macrocycles for the treatment of disease such as cancer. In other aspects, the peptidomimetic macrocycle comprises an a,a-disubstituted amino acid, or may comprise a crosslinker linking the a-positions of at least two amino acids or at least one of said two amino acids may be an a,a-disubstituted amino acid. Further included is the targeting of components of the Wnt signaling pathway such as the Tcf4-/3-catenin complex.
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PEPTIDOMIMETIC MACROCYCLES (Fri, 01 Apr 2011)
Disclosed are peptidomimetic macrocycles comprising a helix, such as an alpha helix, and methods of using such macrocycles for the treatment of disease such as cancer. In other aspects, the peptidomimetic macrocycle comprises an a,a-disubstituted amino acid, or may comprise a crosslinker linking the a-positions of at least two amino acids or at least one of said two amino acids may be an a,a-disubstituted amino acid. Further included is the targeting of components of the Wnt signaling pathway such as the Tcf4-/3-catenin complex.</p>
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PEPTIDOMIMETIC MACROCYCLES WITH IMPROVED PROPERTIES (Fri, 26 Nov 2010)
<p id="p-0001-en" num="0000">The present invention provides biologically active peptidomimetic macrocycles with improved properties relative to their corresponding polypeptides. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.</p>
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Methods for preparing internally constrained peptides and peptidomimetics (Fri, 17 Sep 2010)
<p id="p-0001" num="0000">The present invention relates to a method for preparing a peptide having a stable, internally constrained alpha-helical, beta-sheet/beta-turn, 3<sub>10</sub>-helical, or pi-helical region and a method of stabilizing an alpha-helical, beta-sheet/beta-turn, 3<sub>10</sub>-helical, or pi-helical region within a peptide structure. The resulting peptides and methods of using them are also disclosed.</p>
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Peptidomimetic macrocycles (Fri, 27 Aug 2010)
<p id="p-0001" num="0000">Biologically active crosslinked polypeptides with improved properties relative to their corresponding precursor polypeptides, having good cell penetration properties and reduced binding to human proteins, and methods of identifying and making such improved polypeptides are described.</p>
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METHODS FOR PREPARING PURIFIED POLYPEPTIDE COMPOSITIONS (Fri, 20 Aug 2010)
<p id="p-0001-en" num="0000">The present invention relates to purified peptidomimetic macrocycles. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.</p>
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Bis-sulfhydryl macrocyclization systems (Fri, 23 Jul 2010)
<p id="p-0001" num="0000">Novel peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production are provided.</p>
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PEPTIDOMIMETIC MACROCYCLES (Fri, 23 Jul 2010)
The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of viral disease.
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PEPTIDOMIMETIC MACROCYCLES (Fri, 23 Jul 2010)
The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of viral disease. </p>
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PEPTIDOMIMETIC MACROCYCLES WITH IMPROVED PROPERTIES (Fri, 28 May 2010)
The present invention provides biologically active peptidomimetic macrocycles with improved properties relative to their corresponding polypeptides. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.
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PEPTIDOMIMETIC MACROCYCLES WITH IMPROVED PROPERTIES (Fri, 28 May 2010)
The present invention provides biologically active peptidomimetic macrocycles with improved properties relative to their corresponding polypeptides. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications. </p>
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PEPTIDOMIMETIC MARCROCYCLES (Fri, 26 Mar 2010)
The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.
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PEPTIDOMIMETIC MACROCYCLES (Fri, 26 Mar 2010)
The present invention provides biologically active crosslinked polypeptides with improved properties relative to their corresponding precursor polypeptides, having good cell penetration properties and reduced binding to human proteins. The invention additionally provides methods of identifying and making such improved polypeptides.
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METHODS FOR PREPARING PURIFIED POLYPEPTIDE COMPOSITIONS (Fri, 26 Mar 2010)
The present invention relates to purified peptidomimetic macrocycles. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.
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PEPTIDOMIMETIC MACROCYCLES (Fri, 26 Mar 2010)
The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.
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PEPTIDOMIMETIC MACROCYCLES (Fri, 26 Mar 2010)
The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.
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PEPTIDOMIMETIC MACROCYCLES (Fri, 26 Mar 2010)
The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.
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PEPTIDOMIMETIC MACROCYCLES (Fri, 26 Mar 2010)
The present invention provides biologically active crosslinked polypeptides with improved properties relative to their corresponding precursor polypeptides, having good cell penetration properties and reduced binding to human proteins. The invention additionally provides methods of identifying and making such improved polypeptides. </p>
>> read more

METHODS FOR PREPARING PURIFIED POLYPEPTIDE COMPOSITIONS (Fri, 26 Mar 2010)
The present invention relates to purified peptidomimetic macrocycles. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications. </p>
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PEPTIDOMIMETIC MACROCYCLES (Fri, 26 Mar 2010)
The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease. </p>
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PEPTIDOMIMETIC MACROCYCLES (Fri, 26 Mar 2010)
The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease. </p>
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PEPTIDOMIMETIC MACROCYCLES (Fri, 26 Mar 2010)
The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease. </p>
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PEPTIDOMIMETIC MACROCYCLES (Fri, 26 Mar 2010)
The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease. </p>
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BIOLOGICALLY ACTIVE PEPTIDOMIMETIC MACROCYCLES (Fri, 01 Jan 2010)
<p id="p-0001-en" num="0000">The present invention provides biologically active peptidomimetic macrocycles with improved properties relative to their corresponding polypeptides. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.</p>
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COMPOSITIONS AND METHODS FOR ENHANCING CELLULAR TRANSPORT OF BIOMOLECULES (Fri, 11 Dec 2009)
The present invention discloses compositions and methods for delivery of biomolecules into cells. Compositions comprise peptidomimetic macrocycles complexed or conjugated to biomolecules such as nucleic acids.
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Therapeutic peptidomimetic macrocycles (Fri, 06 Nov 2009)
<p id="p-0001-en" num="0000">The present invention provides biologically active peptidomimetic macrocycles for the treatment of cell proliferative disorders such as cancer and immunoproliferative disease.</p>
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BIOLOGICALLY ACTIVE PEPTIDOMIMETIC MACROCYCLES (Fri, 16 Oct 2009)
The present invention provides biologically active peptidomimetic macrocycles with improved properties relative to their corresponding polypeptides The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.
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THERAPEUTIC PEPTIDOMIMETIC MACROCYCLES (Fri, 14 Aug 2009)
The present invention provides biologically active peptidomimetic macrocycles for the treatment of cell proliferative disorders such as cancer and immunoproliferative disease.
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THERAPEUTIC PEPTIDOMIMETIC MACROCYCLES (Fri, 14 Aug 2009)
The present invention provides biologically active peptidomimetic macrocycles for the treatment of cell proliferative disorders such as cancer and immunoproliferative disease. </p>
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Bis-sulfhydryl macrocyclization systems (Fri, 03 Apr 2009)
<p id="p-0001" num="0000">Peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production, are provided.</p>
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Bis-sulfhydryl macrocyclization systems (Fri, 20 Feb 2009)
<p id="p-0001" num="0000">Peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production, are provided.</p>
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Triazole macrocycle systems (Fri, 24 Oct 2008)
<p id="p-0001" num="0000">The present invention provides novel peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production. In various embodiments, the peptidomimetic macrocycles are of Formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="20.32mm" wi="62.31mm" file="US07981999-20110719-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">The linker L includes a triazole moiety. Peptidomimetic macrocycles according to the invention may exhibit increased α-helical or beta sheet structure in aqueous solution compared to a corresponding non-macrocyclic polypeptide.</p>
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TRIAZOLE MACROCYCLE SYSTEMS (Fri, 29 Aug 2008)
The present invention provides novel peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production.
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TRIAZOLE MACROCYCLE SYSTEMS (Fri, 29 Aug 2008)
The present invention provides novel peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production.</p>
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BIS-SULFHYDRYL MACROCYCLIZATION SYSTEMS (Fri, 27 Jun 2008)
The present invention provides novel peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production.
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BIS-SULFHYDRYL MACROCYCLIZATION SYSTEMS (Fri, 27 Jun 2008)
The present invention provides novel peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production.</p>
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