N-(benzoyl)-phenylalanine compound, pharmaceutical composition containing same, and use thereof
AssigneesHangzhou Apeloa Medicine Research Institute Co., Ltd., Apeloa Pharmaceutical Co., Ltd.
InventorsWeiqiang Zhan, Zhanguo Wang, Fanglei Chen, Fengming Yang, Jianbo Wu, Fangmeng Zhu
Life of this patent
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Abstract
The present invention belongs to the field of pharmaceutical chemistry, and relates to an N-(benzoyl)-phenylalanine compound used as an α4β7 integrin antagonist, including the pharmaceutical composition and the use, and in particular to a compound represented by general formula (1). The compound exhibits good α4β7 integrin binding inhibitory activity, can be used as a high-efficiency α4β7 integrin antagonist, and used for preventing and/or treating α4β7 integrin-related diseases such as autoimmune diseases and inflammatory diseases.
Claims13
A compound as shown in general formula (1) or a pharmaceutically acceptable salt, ester, solvate, optical isomer, tautomer, isotope marker, or prodrug thereof,
- wherein:
- R3 is hydrogen;
- each R4 is independently hydrogen;
- each X1 is independently fluorine, chlorine, or bromine;
- X2 is hydrogen, halogen, di (C1-6 alkyl) amino, or 3-7-membered heterocyclic alkyl;
- each X3 is independently hydrogen;
- A is a group as shown in general formula (2-1), (2-2), or (2-3),
- ring H is C3-6 cyclic alkylene or 3-7 membered heterocyclic alkylene;
- Y is O or S;
- each Z is independently CR1 or N;
- if present, each R1 is independently hydrogen, halogen, C1-6 alkoxy, or di (C1-6 alkyl) amino;
- if present, each R2 is independently C1-6 alkyl, C3-6 cyclic alkyl or 3-7 membered heterocyclic alkyl.
A compound or pharmaceutically acceptable salt, ester, solvate, optical isomer, tautomer, isotope marker, or prodrug thereof having a structure selected from the group consisting of:
Dependencies are inferred from the claim text.