FRAGMENT SYNTHESIS OF CYCLIC PEPTIDES

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 KAFAL, Adam Paul, POUPART, Marc-André, VAZQUEZ, Manuel Perez, HICKEY, Jennifer L, ROUGHTON, Andrew L, MORSHED, M. Monzur, GILLARD, James, YANG, Gaoqiang
Format Patent
LanguageEnglish
Published 19.11.2020
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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: US202016985096