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
-
- 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
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (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)
- Peptides Or Proteins (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 (enExample) |
| EP (1) | EP3774764A1 (enExample) |
| JP (1) | JP7326319B2 (enExample) |
| KR (1) | KR102755259B1 (enExample) |
| CN (1) | CN111971277B (enExample) |
| AU (1) | AU2019248545B2 (enExample) |
| CA (1) | CA3095646A1 (enExample) |
| MA (1) | MA52189A (enExample) |
| MX (1) | MX2020010407A (enExample) |
| TW (1) | TWI793294B (enExample) |
| WO (1) | WO2019195124A1 (enExample) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019046511A1 (en) | 2017-08-31 | 2019-03-07 | Sperovie Biosciences, Inc. | COMPOUNDS, COMPOSITIONS AND METHODS FOR THE TREATMENT OF DISEASE |
| 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 |
| JP7843695B2 (ja) | 2019-08-02 | 2026-04-10 | メルサナ セラピューティクス インコーポレイテッド | がんの処置用のＳＴＩＮＧ（インターフェロン遺伝子刺激因子）アゴニストとしてのビス－［Ｎ－（（５－カルバモイル）－１Ｈ－ベンゾ［ｄ］イミダゾール－２－イル）－ピラゾール－５－カルボキサミド］誘導体および関連化合物 |
| WO2021083060A1 (zh) * | 2019-10-28 | 2021-05-06 | 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 |
| EP4069683A1 (en) * | 2019-12-06 | 2022-10-12 | Mersana Therapeutics, Inc. | Dimeric compounds as sting agonists |
| EP4077318B1 (en) | 2019-12-18 | 2025-10-15 | Ctxt Pty Ltd | Benzimidazole dimers as modulators of sting |
| 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 |
| IL296901A (en) | 2020-04-02 | 2022-12-01 | Mersana Therapeutics Inc | Antibody-drug conjugates comprising sting agonists |
| TW202200136A (zh) | 2020-04-10 | 2022-01-01 | 日商小野藥品工業股份有限公司 | 癌治療方法 |
| US20230293716A1 (en) | 2020-05-08 | 2023-09-21 | Bolt Biotherapeutics, Inc. | Elastase-substrate, peptide linker immunoconjugates, and uses thereof |
| 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 |
| KR20230061482A (ko) * | 2020-09-02 | 2023-05-08 | 더 스크립스 리서치 인스티튜트 | 인터페론 유전자 자극제 (stimulator of interferon genes)(STING) 의 작용제들 |
| WO2022206725A1 (en) * | 2021-03-30 | 2022-10-06 | Jacobio Pharmaceuticals Co., Ltd. | Novel compounds useful as sting agonists and uses thereof |
| US11964978B2 (en) * | 2021-03-18 | 2024-04-23 | Pfizer Inc. | Modulators of STING (stimulator of interferon genes) |
| 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 |
| CN118891043A (zh) * | 2022-01-20 | 2024-11-01 | 俄亥俄州创新基金会 | 包含脂质化合物的组合物以及制备和使用其的方法 |
| JP2025515330A (ja) * | 2022-04-25 | 2025-05-14 | ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン | Ｓｔｉｎｇアゴニスト、製剤、及びその使用 |
| CA3258147A1 (en) | 2022-06-06 | 2023-12-14 | Sutro Biopharma, Inc. | INTERFERON GENE STIMULATOR 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 |
| JP2026507091A (ja) * | 2023-02-24 | 2026-02-27 | 深▲セン▼真実生物医薬科技有限公司 | アリール基三環式ｓｔｉｎｇ作動薬及びその使用 |
| 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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2019
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- 2019-04-01 KR KR1020207031242A patent/KR102755259B1/ko active Active
- 2019-04-01 MA MA052189A patent/MA52189A/fr unknown
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- 2019-04-01 US US16/372,103 patent/US10793557B2/en active Active
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| KR20200139203A (ko) | 2020-12-11 |
| BR112020020085A2 (pt) | 2021-02-17 |
| JP2021520345A (ja) | 2021-08-19 |
| CA3095646A1 (en) | 2019-10-10 |
| TWI793294B (zh) | 2023-02-21 |
| WO2019195124A1 (en) | 2019-10-10 |
| KR102755259B1 (ko) | 2025-01-15 |
| JP7326319B2 (ja) | 2023-08-15 |
| AU2019248545A1 (en) | 2020-10-15 |
| EP3774764A1 (en) | 2021-02-17 |
| MA52189A (fr) | 2021-02-17 |
| TW202003509A (zh) | 2020-01-16 |
| AU2019248545B2 (en) | 2022-08-11 |
| BR112020020085A8 (pt) | 2023-04-11 |
| RU2020132585A (ru) | 2022-05-06 |
| MX2020010407A (es) | 2020-10-22 |
| US20190300513A1 (en) | 2019-10-03 |
| US10793557B2 (en) | 2020-10-06 |
| CN111971277A (zh) | 2020-11-20 |
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