AU2018323053A1 - Cyclic di-nucleotides as stimulator of interferon genes modulators - Google Patents
Cyclic di-nucleotides as stimulator of interferon genes modulators Download PDFInfo
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- AU2018323053A1 AU2018323053A1 AU2018323053A AU2018323053A AU2018323053A1 AU 2018323053 A1 AU2018323053 A1 AU 2018323053A1 AU 2018323053 A AU2018323053 A AU 2018323053A AU 2018323053 A AU2018323053 A AU 2018323053A AU 2018323053 A1 AU2018323053 A1 AU 2018323053A1
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- C07H21/00—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
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- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/16—Purine radicals
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- C07H19/213—Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids containing cyclic phosphate
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- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H21/00—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
- C07H21/02—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
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- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H23/00—Compounds containing boron, silicon or a metal, e.g. chelates or vitamin B12
Landscapes
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Applications Claiming Priority (5)
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| US201762552148P | 2017-08-30 | 2017-08-30 | |
| US62/552,148 | 2017-08-30 | ||
| US201862660565P | 2018-04-20 | 2018-04-20 | |
| US62/660,565 | 2018-04-20 | ||
| PCT/IB2018/056658 WO2019043634A2 (en) | 2017-08-30 | 2018-08-30 | CYCLIC DI-NUCLEOTIDES AS STIMULATORS OF INTERFERON GENE MODULATORS |
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| CA3073919A1 (en) | 2017-08-30 | 2019-03-07 | Beijing Xuanyi Pharmasciences Co., Ltd. | Cyclic di-nucleotides as stimulator of interferon genes modulators |
| MX2020004858A (es) | 2017-11-10 | 2020-10-01 | Takeda Pharmaceuticals Co | Compuestos moduladores de sting y metodos de elaboracion y uso. |
| KR20200130362A (ko) * | 2018-03-08 | 2020-11-18 | 브리스톨-마이어스 스큅 컴퍼니 | 항암제로서의 시클릭 디뉴클레오티드 |
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| US20170340658A1 (en) | 2014-12-16 | 2017-11-30 | Invivogen | Combined use of a chemotherapeutic agent and a cyclic dinucleotide for cancer treatment |
| CN107148424B (zh) | 2014-12-16 | 2021-01-08 | 凯拉治疗股份公司 | 用于诱导细胞因子的环状二核苷酸 |
| GB201501462D0 (en) | 2015-01-29 | 2015-03-18 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| JP6692826B2 (ja) | 2015-03-10 | 2020-05-13 | アドゥロ バイオテック，インク． | 「インターフェロン遺伝子刺激因子」依存性シグナル伝達の活性化のための組成物及び方法 |
| BR112018002757A8 (pt) | 2015-08-13 | 2023-04-11 | Merck Sharp & Dohme | Composto, composição farmacêutica, e, métodos para induzir uma resposta imune, para induzir uma produção de interferon tipo i e para tratamento de um distúrbio |
| AU2016343993A1 (en) | 2015-10-28 | 2018-05-10 | Aduro Biotech, Inc. | Compositions and methods for activating "stimulator of interferon gene"-dependent signalling |
| JP6411676B2 (ja) | 2015-12-03 | 2018-10-24 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ | Ｓｔｉｎｇの調節因子としての環状プリンジヌクレオチド |
| US20180369268A1 (en) | 2015-12-16 | 2018-12-27 | Aduro Biotech, Inc. | Methods for identifying inhibitors of "stimulator of interferon gene"- dependent interferon production |
| US10723756B2 (en) | 2016-01-11 | 2020-07-28 | Innate Tumor Immunity Inc. | Cyclic dinucleotides for treating conditions associated with STING activity such as cancer |
| KR20250049441A (ko) | 2016-01-11 | 2025-04-11 | 인네이트 튜머 이뮤니티, 인코포레이티드 | Sting 활성과 연관된 상태 예컨대 암의 치료를 위한 시클릭 디뉴클레오티드 |
| NZ746112A (en) | 2016-03-18 | 2023-01-27 | Immune Sensor Llc | Cyclic di-nucleotide compounds and methods of use |
| EP3448393A1 (en) * | 2016-04-25 | 2019-03-06 | Invivogen | Novel complexes of immunostimulatory compounds, and uses thereof |
| US11098077B2 (en) | 2016-07-05 | 2021-08-24 | Chinook Therapeutics, Inc. | Locked nucleic acid cyclic dinucleotide compounds and uses thereof |
| WO2018045204A1 (en) | 2016-08-31 | 2018-03-08 | Ifm Therapeutics, Inc | Cyclic dinucleotide analogs for treating conditions associated with sting (stimulator of interferon genes) activity |
| US10537590B2 (en) | 2016-09-30 | 2020-01-21 | Boehringer Ingelheim International Gmbh | Cyclic dinucleotide compounds |
| US11001605B2 (en) * | 2016-10-07 | 2021-05-11 | Biolog Life Science Institute Gmbh & Co. Kg | Cyclic dinucleotides containing benzimidazole, method for the production of same, and use of same to activate stimulator of interferon genes (sting)-dependent signaling pathways |
| JOP20170188A1 (ar) * | 2016-11-25 | 2019-01-30 | Janssen Biotech Inc | ثنائي النوكليوتيدات الحلقية كمنبهات ستينغ (sting) |
| JOP20170192A1 (ar) | 2016-12-01 | 2019-01-30 | Takeda Pharmaceuticals Co | داي نوكليوتيد حلقي |
| US20200113924A1 (en) | 2016-12-20 | 2020-04-16 | Merck Sharp & Dohme Corp. | Cyclic dinucleotide sting agonists for cancer treatment |
| WO2018119274A1 (en) * | 2016-12-21 | 2018-06-28 | Fred Hutchinson Cancer Research Center | Scaffolds to treat solid tumor cells and escape variants |
| WO2018138684A1 (en) | 2017-01-27 | 2018-08-02 | Janssen Biotech, Inc. | Cyclic dinucleotides as sting agonists |
| CN110234403A (zh) * | 2017-01-27 | 2019-09-13 | 詹森生物科技公司 | 作为sting激动剂的环状二核苷酸 |
| CA3073919A1 (en) | 2017-08-30 | 2019-03-07 | Beijing Xuanyi Pharmasciences Co., Ltd. | Cyclic di-nucleotides as stimulator of interferon genes modulators |
| CN112867727B (zh) * | 2018-10-12 | 2024-05-17 | 上海济煜医药科技有限公司 | 环二核苷酸类化合物及其应用 |
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2018
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- 2018-08-30 SG SG11202001847WA patent/SG11202001847WA/en unknown
- 2018-08-30 WO PCT/IB2018/056658 patent/WO2019043634A2/en not_active Ceased
- 2018-08-30 AU AU2018323053A patent/AU2018323053A1/en not_active Abandoned
- 2018-08-30 EP EP18850228.0A patent/EP3692048A4/en active Pending
- 2018-08-30 JP JP2020533876A patent/JP7311514B2/ja active Active
- 2018-08-30 RU RU2020112502A patent/RU2020112502A/ru unknown
- 2018-08-30 BR BR112020004047-9A patent/BR112020004047A2/pt not_active IP Right Cessation
- 2018-08-30 KR KR1020207008457A patent/KR102782200B1/ko active Active
- 2018-08-30 TW TW107130419A patent/TWI808092B/zh active
- 2018-08-30 CN CN201880056293.1A patent/CN111263767B/zh active Active
- 2018-08-30 MX MX2020002303A patent/MX2020002303A/es unknown
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2020
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| TWI808092B (zh) | 2023-07-11 |
| WO2019043634A3 (en) | 2019-04-11 |
| RU2020112502A (ru) | 2021-10-01 |
| EP3692048A2 (en) | 2020-08-12 |
| JP2020532585A (ja) | 2020-11-12 |
| US20200331957A1 (en) | 2020-10-22 |
| WO2019043634A2 (en) | 2019-03-07 |
| CN111263767A (zh) | 2020-06-09 |
| BR112020004047A2 (pt) | 2020-09-01 |
| CA3073919A1 (en) | 2019-03-07 |
| US11773132B2 (en) | 2023-10-03 |
| CN111263767B (zh) | 2023-07-18 |
| JP7311514B2 (ja) | 2023-07-19 |
| RU2020112502A3 (enExample) | 2021-10-08 |
| IL272928A (en) | 2020-04-30 |
| MX2020002303A (es) | 2020-09-10 |
| EP3692048A4 (en) | 2021-10-20 |
| TW201919650A (zh) | 2019-06-01 |
| KR102782200B1 (ko) | 2025-03-17 |
| SG11202001847WA (en) | 2020-03-30 |
| KR20200058411A (ko) | 2020-05-27 |
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