公开(公告)号：US20200165300A1

公开(公告)日：2020-05-28

申请号：US15775309

申请日：2016-11-14

申请人： ENCYCLE THERAPEUTICS, INC. ,  UNIVERSITE DE MONTREAL

发明人： Manuel Perez Vazquez ,  M. Monzur Morshed ,  Jennifer L. Hickey ,  Adam Paul Kafal ,  James Gillard ,  Narendra Patel ,  Sai Kumar Chakka ,  Andrew L. Roughton ,  Marc-André Poupart ,  Gaoqiang Yang

IPC分类号： C07K7/54 ,  C07K7/64 ,  A61P1/04

摘要： 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.

公开(公告)号：US11072616B2

公开(公告)日：2021-07-27

申请号：US15775309

申请日：2016-11-14

申请人： Zealand Pharma A/S ,  UNIVERSITE DE MONTREAL

发明人： Manuel Perez Vazquez ,  M. Monzur Morshed ,  Jennifer L. Hickey ,  Adam Paul Kafal ,  James Gillard ,  Narendra Patel ,  Sai Kumar Chakka ,  Andrew L. Roughton ,  Marc-André Poupart ,  Gaoqiang Yang

IPC分类号： C07D487/04 ,  C07C271/18 ,  C07C271/22 ,  C07D207/16 ,  C07K7/06 ,  C07K7/56 ,  A61P1/04 ,  C07K7/54 ,  C07K7/64 ,  A61K9/00 ,  A61K38/00 ,  C07K1/107

摘要： 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.