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 KAFAL, Adam Paul, PATEL, Narendra, POUPART, Marc-André, VAZQUEZ, Manuel Perez, HICKEY, Jennifer L, CHAKKA, Sai Kumar, ROUGHTON, Andrew L, MORSHED, M. Monzur, GILLARD, James, YANG, Gaoqiang
Format Patent
LanguageEnglish
Published 30.09.2021
Subjects
ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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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: US202117214530