公开(公告)号：US20220288065A1

公开(公告)日：2022-09-15

申请号：US17753138

申请日：2020-08-21

申请人： The Scripps Research Institute

发明人： H. Michael PETRASSI ,  Chenguang YU ,  Jie WANG ,  Arnab K. CHATTERJEE ,  Ana Maria Gamo ALBERO ,  Anil GUPTA ,  Junko TAMIYA ,  Peter G. SCHULTZ ,  Kristen JOHNSON ,  Alan CHU ,  Emily N. CHIN ,  Luke L. LAIRSON

IPC分类号： A61K31/501 ,  A61K39/395 ,  A61K45/06 ,  C07D401/04 ,  C07D403/04 ,  C07D413/14 ,  C07D237/24 ,  C07D213/82 ,  C07D401/14 ,  C07D403/14 ,  C07D417/04 ,  C07D413/04 ,  C07D409/14 ,  C07D498/04 ,  C07D239/28 ,  A61K31/497 ,  A61K31/506 ,  A61K31/50 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/536 ,  A61K31/5365

摘要： The invention provides compounds having STimulator of INterferon Genes (STING) agonistic bioactivity that can be used in the treatment of tumors inpatients afflicted therewith. The compounds are of formula (IA), formula (I), and formula (II): wherein the various substituents are as defined herein. Ring A is a 5- or 6-membered heteroaryl comprising 1, 2, or 3 N atoms, unsubstituted or substituted with 1, 2, or 3 groups as defined herein. Compounds for practice of a method of the invention can be delivered via oral delivery for systemic exposure, as well as delivered intratumorally. Antitumor therapy using a compound of formula (I) can further comprise administration of an effective dose of an immunecheckpoint targeting drug.

公开(公告)号：US20220332720A1

公开(公告)日：2022-10-20

申请号：US17753139

申请日：2020-08-21

申请人： The Scripps Research Institute

发明人： H. Michael PETRASSI ,  Chenguang YU ,  Jie WANG ,  Arnab K. CHATTERJEE ,  Peter G. SCHULTZ ,  Kristen JOHNSON ,  Alan CHU ,  Emily N. CHIN ,  Luke L. LAIRSON

IPC分类号： C07D487/04 ,  C07D471/04

摘要： The present disclosure provides compounds having Stimulator of Interferon Genes (STING) agonistic bioactivity that can be used in the treatment of tumors in patients afflicted therewith. The compounds are a compound of formula (I) or formula (II): wherein the substituents are as defined herein. Ring A is a bicyclic fully aromatic or partially reduced heteroaryl ring system comprising 3, 4, or 5 N atoms, substituted with 0, 1, 2, 3,or 4 substituents as defined herein. Compounds for practice of a method of the present disclosure can be delivered via oral delivery for systemic exposure, as well as delivered intratumorally. Antitumor therapy using a compound of formula (I) can further comprise administration of an effective dose of an immune-checkpoint targeting drug.