Cyclic peptides targeting alpha-4-beta-7 integrin

There is described herein antagonists of α4β7 integrin, and more particularly to cyclic peptide antagonists. Accordingly, there is described herein a compound of formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and R8 are various substituents; stereocentres 1*, 2* and 3* are each independently selecte...

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Main Authors Vazquez, Manuel Perez, Chakka, Sai Kumar, Morshed, M. Monzur, Hickey, Jennifer L, Roughton, Andrew L, Poupart, Marc-André, Yang, Gaoqiang, Gillard, James, Patel, Narendra, Kafal, Adam Paul
Format Patent
LanguageEnglish
Published 27.07.2021
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Summary:There is described herein antagonists of α4β7 integrin, and more particularly to cyclic peptide antagonists. Accordingly, there is described herein a compound of formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and R8 are various substituents; stereocentres 1*, 2* and 3* are each independently selected from R and S; n is 1, 2, 3, or 4 and where n is 2-4, Z is an amino terminus of an amino acid; -C═O- adjacent L is the carboxy terminus of an amino acid; and L along with Z and -C═O- is a peptide.
Bibliography:Application Number: US201615775309