CN111971277B - 作为sting激动剂的苯并噻吩及相关化合物 - Google Patents
作为sting激动剂的苯并噻吩及相关化合物 Download PDFInfo
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- CN111971277B CN111971277B CN201980024834.7A CN201980024834A CN111971277B CN 111971277 B CN111971277 B CN 111971277B CN 201980024834 A CN201980024834 A CN 201980024834A CN 111971277 B CN111971277 B CN 111971277B
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
- C07D277/62—Benzothiazoles
- C07D277/64—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
- C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
- C07D333/56—Radicals substituted by oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862652018P | 2018-04-03 | 2018-04-03 | |
| US62/652,018 | 2018-04-03 | ||
| US201962809956P | 2019-02-25 | 2019-02-25 | |
| US62/809,956 | 2019-02-25 | ||
| PCT/US2019/025088 WO2019195124A1 (en) | 2018-04-03 | 2019-04-01 | Benzothiophenes and related compounds as sting agonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN111971277A CN111971277A (zh) | 2020-11-20 |
| CN111971277B true CN111971277B (zh) | 2023-06-06 |
Family
ID=66175500
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201980024834.7A Active CN111971277B (zh) | 2018-04-03 | 2019-04-01 | 作为sting激动剂的苯并噻吩及相关化合物 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US10793557B2 (https=) |
| EP (1) | EP3774764A1 (https=) |
| JP (1) | JP7326319B2 (https=) |
| KR (1) | KR102755259B1 (https=) |
| CN (1) | CN111971277B (https=) |
| AU (1) | AU2019248545B2 (https=) |
| CA (1) | CA3095646A1 (https=) |
| MA (1) | MA52189A (https=) |
| MX (1) | MX2020010407A (https=) |
| TW (1) | TWI793294B (https=) |
| WO (1) | WO2019195124A1 (https=) |
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| JP7270608B2 (ja) | 2017-08-31 | 2023-05-10 | エフ－スター・セラピューティクス・インコーポレイテッド | 化合物、組成物、及び疾患の治療方法 |
| GB201807924D0 (en) | 2018-05-16 | 2018-06-27 | Ctxt Pty Ltd | Compounds |
| CN111393405B (zh) * | 2019-01-02 | 2022-11-25 | 中国科学院上海药物研究所 | 一类含氟取代的苯并噻吩类化合物及其药物组合物及应用 |
| EP3964504A4 (en) * | 2019-04-30 | 2022-12-28 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | AMINOPYRIMIDINE COMPOUND, METHOD OF PRODUCTION THEREOF AND USE THEREOF |
| GB201910304D0 (en) | 2019-07-18 | 2019-09-04 | Ctxt Pty Ltd | Compounds |
| GB201910305D0 (en) | 2019-07-18 | 2019-09-04 | Ctxt Pty Ltd | Compounds |
| CA3149482A1 (en) | 2019-08-02 | 2021-02-11 | Mersana Therapeutics, Inc. | Bis-[n-((5-carbamoyl)-1h-benzo[d]imidazol-2-yl)-pyrazol-5-carboxamide] derivatives and related compounds as sting (stimulator of interferon genes) agonists for the treatment of cancer |
| CN112724127B (zh) * | 2019-10-28 | 2023-02-17 | 中国科学院上海药物研究所 | 五元杂环氧代羧酸类化合物及其医药用途 |
| WO2021113679A1 (en) * | 2019-12-06 | 2021-06-10 | Mersana Therapeutics, Inc. | Dimeric compounds as sting agonists |
| CN114981265B (zh) | 2019-12-18 | 2025-01-03 | Ctxt私人有限公司 | 化合物 |
| CN113087668B (zh) * | 2019-12-23 | 2022-11-04 | 中国科学院上海药物研究所 | 一类苯并咪唑二聚体、其制备方法及用途 |
| CN113248475B (zh) * | 2020-02-11 | 2023-03-17 | 中国科学院上海药物研究所 | 一类杂环取代的苯并咪唑二聚体或其药学上可接受的盐、组合物及其用途 |
| WO2021202984A1 (en) | 2020-04-02 | 2021-10-07 | Mersana Therapeutics, Inc. | Antibody drug conjugates comprising sting agonists |
| WO2021206158A1 (ja) | 2020-04-10 | 2021-10-14 | 小野薬品工業株式会社 | がん治療方法 |
| CN115996756A (zh) | 2020-05-08 | 2023-04-21 | 博尔特生物治疗药物有限公司 | 弹性蛋白酶底物肽连接子免疫缀合物及其用途 |
| CN113861161A (zh) * | 2020-06-30 | 2021-12-31 | 上海海和药物研究开发股份有限公司 | 一种芳基并芳杂环衍生物及其制备方法和用途 |
| EP4208260A1 (en) * | 2020-09-02 | 2023-07-12 | The Scripps Research Institute | Agonists of stimulator of interferon genes sting |
| US11964978B2 (en) * | 2021-03-18 | 2024-04-23 | Pfizer Inc. | Modulators of STING (stimulator of interferon genes) |
| JP2024511832A (ja) * | 2021-03-30 | 2024-03-15 | ジャコバイオ ファーマスーティカルズ カンパニー リミテッド | Ｓｔｉｎｇアゴニストとして有用な新規化合物およびその使用 |
| CN113429384B (zh) * | 2021-05-12 | 2022-04-08 | 中山大学附属第五医院 | 一类干扰素基因刺激因子靶向的放射性pet显像剂 |
| CN115772154B (zh) * | 2021-09-08 | 2024-04-30 | 上海交通大学 | 一类含有氘取代的苯并噻吩类衍生物及其制备与用途 |
| CN114213315A (zh) * | 2021-12-31 | 2022-03-22 | 上海陶术生物科技有限公司 | 含氮杂环类化合物及其中间体的合成方法 |
| US20250099392A1 (en) * | 2022-01-20 | 2025-03-27 | Ohio State Innovation Foundation | Compositions comprising lipid compounds and methods of making and use thereof |
| CN119212984A (zh) * | 2022-04-25 | 2024-12-27 | 密歇根大学董事会 | Sting激动剂、制剂及其用途 |
| AU2023283720A1 (en) * | 2022-06-06 | 2025-01-02 | Sutro Biopharma, Inc. | Sting agonist compounds |
| WO2024032782A1 (en) * | 2022-08-12 | 2024-02-15 | Jacobio Pharmaceuticals Co.Ltd. | Vaccine adjuvants and uses thereof |
| WO2024137619A1 (en) | 2022-12-20 | 2024-06-27 | Bolt Biotherapeutics, Inc. | Anti-claudin, bis-benzimid azole sting agonist immunoconjugates, and uses thereof |
| EP4671250A1 (en) * | 2023-02-24 | 2025-12-31 | Shenzhen Genuine Biotechnology Co., Ltd. | Tricyclic Sting Agonist and its Use |
| WO2024186626A1 (en) | 2023-03-03 | 2024-09-12 | Bolt Biotherapeutics, Inc. | Aza-bicyclic sting agonist immunoconjugates, and uses thereof |
| CN116332903B (zh) * | 2023-03-29 | 2024-11-12 | 中国药科大学 | 一种具有苯并[b]硒吩结构的二聚化合物及其用途 |
| CN116354922B (zh) * | 2023-03-31 | 2025-04-25 | 药康众拓(江苏)医药科技有限公司 | 氘代苯并噻吩类化合物及其药物组合物和用途 |
| WO2025007743A1 (en) * | 2023-07-04 | 2025-01-09 | Primelink Biotherapeutics (Shenzhen) Co., Ltd. | Sting agonists and uses thereof |
| WO2025081077A1 (en) * | 2023-10-13 | 2025-04-17 | University Of Rhode Island Board Of Trustees | Targeted intracellular delivery of dimeric msa stinga by two phlip® peptides |
| CN117402139B (zh) * | 2023-10-18 | 2026-01-27 | 南通大学 | Sting激动剂msa-2的锰盐合成和肿瘤治疗应用 |
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| RU2020132585A (ru) | 2022-05-06 |
| BR112020020085A2 (pt) | 2021-02-17 |
| JP7326319B2 (ja) | 2023-08-15 |
| US10793557B2 (en) | 2020-10-06 |
| CN111971277A (zh) | 2020-11-20 |
| TW202003509A (zh) | 2020-01-16 |
| AU2019248545A1 (en) | 2020-10-15 |
| US20190300513A1 (en) | 2019-10-03 |
| CA3095646A1 (en) | 2019-10-10 |
| AU2019248545B2 (en) | 2022-08-11 |
| KR102755259B1 (ko) | 2025-01-15 |
| EP3774764A1 (en) | 2021-02-17 |
| MX2020010407A (es) | 2020-10-22 |
| JP2021520345A (ja) | 2021-08-19 |
| BR112020020085A8 (pt) | 2023-04-11 |
| MA52189A (fr) | 2021-02-17 |
| TWI793294B (zh) | 2023-02-21 |
| WO2019195124A1 (en) | 2019-10-10 |
| KR20200139203A (ko) | 2020-12-11 |
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