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公开(公告)号：US20220204449A1
公开(公告)日：2022-06-30
申请号：US17548288
申请日：2021-12-10
发明人： Woojin JEON , Do Sup LEE , Suh-Youn SHON , Junsu BAN , Sungjun HONG , Jin Hee LEE , Jaeho HEO , Jungwoo LEE , JoonTae PARK , Kyung Mi AN , Hongchul YOON
IPC分类号： C07D209/08 , C07D307/79 , C07D319/18
摘要： The present disclosure provides pharmaceutical compositions and compounds having dual agonist activity at the μ and δ opioid receptors. The agonist compounds of this disclosure can also provide GPCR functional selectivity, including selective activity in the Gi pathway. In some embodiments, the compounds of this disclosure are biased μ-opioid and/or δ-opioid receptor agonists that do not significantly recruit β-arrestins, but can activate G-protein-dependent pathways, and thus can be administered without risk of significant undesirable side effects exhibited by conventional opioid receptor agonists. In some embodiments there is provided a substantially optically pure compound having dual agonist activity at the μ and δ opioid receptors.
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公开(公告)号：US20230136331A1
公开(公告)日：2023-05-04
申请号：US17937428
申请日：2022-09-30
发明人： Hong Seok BAN , Seok-Woo YANG , Hye Mi KWON , Jea Won CHO , Suh-Youn SHON , Do Sup LEE , Ji-Hyung LEE , Seong Wook LEE , Ukjin SON , Jun Su BAN , Jihye KIM
摘要： Provided herein is an immunocytokine comprising (i) an antigen binding protein (ABP) specific to a target protein; (ii) an IL-21 domain; and (iii) an IL-21Rα mutein, wherein the IL-21Rα mutein has a reduced binding affinity to the IL-21 domain compared to a wild-type IL-21Rα. Further provided includes a method of using the immunocytokine to selectively activate an IL-21Rα on a target cell, thereby enhance immune response or treat cancer.
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