- 专利标题: MONOCYCLIC AGONISTS OF STIMULATOR OF INTERFERON GENES STING
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申请号: US17753138申请日: 2020-08-21
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公开(公告)号: US20220288065A1公开(公告)日: 2022-09-15
- 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
- 申请人: The Scripps Research Institute
- 申请人地址: US CA La Jolla
- 专利权人: The Scripps Research Institute
- 当前专利权人: The Scripps Research Institute
- 当前专利权人地址: US CA La Jolla
- 国际申请: PCT/US2020/070443 WO 20200821
- 主分类号: A61K31/501
- 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.
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