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US 10,857,196 B2Granted
Bicyclic peptide ligands and uses thereof
AssigneeBicycleTx Limited
InventorsPaul John Beswick, Gabriela Ivanova-Berndt, Gemma Elizabeth Mudd, Silvia Pavan, Michael Skynner, Daniel Paul Teufel, Katerine Van Rietschoten
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Abstract
The present invention provides compounds, compositions thereof, and methods of using the same.
Claims20
A compound of formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- each of L1, L2, and L3 is independently a covalent bond or a C1-8 bivalent hydrocarbon chain wherein one, two or three methylene units of the chain are optionally and independently replaced by —S—, —N(R)—,—O—,—C(O)—,—OC(O)—, —C(O)O—, —C(O)N(R)—, —N(R)C(O)—,—S(O)—,—S(O)2— or —N(R)CH2C(O)—;
- each R is independently hydrogen or C1-4 alkyl;
- Scaffold is selected from the group consisting of
- Loop A
- and Loop B is
- or
- Loop A is
- and Loop B is
- indicates the site of attachment to the N-terminus of the Bicycle;
- indicates the site of attachment to the C-terminus of the Bicycle;
- Peptide1 is hydrogen, or a natural or unnatural amino acid wherein the acid is connected to the N-terminus of the Bicycle via an amide bond;
- Peptide2 is —OH, —NH2, or a natural or unnatural amino acid wherein the amino group is connected to the C-terminus of the Bicycle via an amide bond;
- each of R1 and R2 is independently
- each of R4 is independently hydrogen, C1-4 aliphatic, and
- each of n is independently 0 or 1, and
- wherein a value of n=0 for R′ results in a terminal amine, —NH2, and a value of n=0 for R2 results in a terminal carboxamide, —C(O)NH2.
14 more elements
Dependencies are inferred from the claim text.