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
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LanguageEnglish
Published 19.11.2020
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Abstract 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.
AbstractList 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.
Author HICKEY, Jennifer L
POUPART, Marc-André
ROUGHTON, Andrew L
VAZQUEZ, Manuel Perez
KAFAL, Adam Paul
YANG, Gaoqiang
MORSHED, M. Monzur
GILLARD, James
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– fullname: MORSHED, M. Monzur
– fullname: GILLARD, James
– fullname: YANG, Gaoqiang
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RelatedCompanies Encycle Therapeutics, Inc
Universite de Montreal
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Snippet There is described herein antagonists of α4β7 integrin, and more particularly to cyclic peptide antagonists. Accordingly, there is described herein a compound...
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SubjectTerms 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
Title FRAGMENT SYNTHESIS OF CYCLIC PEPTIDES
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