CN114929682A - 苯并硫代吡喃酮类化合物的盐及其制备方法和用途 - Google Patents
苯并硫代吡喃酮类化合物的盐及其制备方法和用途 Download PDFInfo
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- CN114929682A CN114929682A CN202080070377.8A CN202080070377A CN114929682A CN 114929682 A CN114929682 A CN 114929682A CN 202080070377 A CN202080070377 A CN 202080070377A CN 114929682 A CN114929682 A CN 114929682A
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- Prior art keywords
- benzothiopyran
- cyclohexylmethyl
- trifluoromethyl
- nitro
- piperazin
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Classifications
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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
- A61P31/06—Antibacterial agents for tuberculosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D335/00—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
- C07D335/04—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
本发明属于医药技术领域，公开了苯并硫代吡喃酮类化合物的盐及其制备方法和用途，具体为式(I)所示的2‑(4‑(环己基甲基)哌嗪‑1‑基)‑6‑(三氟甲基)‑8‑硝基‑苯并硫代吡喃‑4‑酮的盐、其制备方法、药物组合物及在制备治疗和/或预防结核分枝杆菌引起的感染性疾病药物中的应用。本发明旨在制备一种药代性质和理化性质显著改善并具有强体内外抗结核分支杆菌活性的2‑(4‑(环己基甲基)哌嗪‑1‑基)‑6‑(三氟甲基)‑8‑硝基‑苯并硫代吡喃‑4‑酮的盐，其作为潜在的新药物，可用于由细菌引起的感染性疾病，特别是由结核分枝杆菌引起的肺结核(TB)疾病的治疗或预防性治疗，同时可用于克服与结核分枝杆菌耐药相关的问题。
Description
PCT国内申请，说明书已公开。
Claims (6)
- PCT国内申请，权利要求书已公开。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910849215.3A CN112457291B (zh) | 2019-09-09 | 2019-09-09 | 苯并硫代吡喃酮类化合物的盐及其制备方法和用途 |
| CN2019108492153 | 2019-09-09 | ||
| PCT/CN2020/114126 WO2021047525A1 (zh) | 2019-09-09 | 2020-09-09 | 苯并硫代吡喃酮类化合物的盐及其制备方法和用途 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN114929682A true CN114929682A (zh) | 2022-08-19 |
| CN114929682B CN114929682B (zh) | 2024-05-14 |
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| CN201910849215.3A Active CN112457291B (zh) | 2019-09-09 | 2019-09-09 | 苯并硫代吡喃酮类化合物的盐及其制备方法和用途 |
| CN202080070377.8A Active CN114929682B (zh) | 2019-09-09 | 2020-09-09 | 苯并硫代吡喃酮类化合物的盐及其制备方法和用途 |
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| CN201910849215.3A Active CN112457291B (zh) | 2019-09-09 | 2019-09-09 | 苯并硫代吡喃酮类化合物的盐及其制备方法和用途 |
Country Status (3)
| Country | Link |
|---|---|
| CN (2) | CN112457291B (zh) |
| WO (1) | WO2021047525A1 (zh) |
| ZA (1) | ZA202203673B (zh) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4296674A1 (en) | 2022-06-20 | 2023-12-27 | Université Toulouse III - Paul Sabatier | Innovative molecules decreasing virulence of mycobacterium for the treatment of tuberculosis |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018214639A1 (zh) * | 2017-05-24 | 2018-11-29 | 中国医学科学院药物研究所 | 2-氮杂环-5-三氟甲基-8-硝基苯并(硫代)吡喃-4-酮类化合物及其制备方法和用途 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS57865B2 (zh) * | 1973-02-05 | 1982-01-08 | ||
| CN104211708B (zh) * | 2013-05-29 | 2018-08-24 | 中国医学科学院药物研究所 | 苯并噁嗪酮衍生物及其作为抗菌剂的应用 |
| CN108947952B (zh) * | 2017-05-24 | 2021-09-21 | 中国医学科学院药物研究所 | 2-取代氨基-5-三氟甲基-8-硝基苯并（硫代）吡喃-4-酮类化合物及其制备方法和用途 |
-
2019
- 2019-09-09 CN CN201910849215.3A patent/CN112457291B/zh active Active
-
2020
- 2020-09-09 WO PCT/CN2020/114126 patent/WO2021047525A1/zh active Application Filing
- 2020-09-09 CN CN202080070377.8A patent/CN114929682B/zh active Active
-
2022
- 2022-03-30 ZA ZA2022/03673A patent/ZA202203673B/en unknown
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018214639A1 (zh) * | 2017-05-24 | 2018-11-29 | 中国医学科学院药物研究所 | 2-氮杂环-5-三氟甲基-8-硝基苯并(硫代)吡喃-4-酮类化合物及其制备方法和用途 |
Also Published As
| Publication number | Publication date |
|---|---|
| ZA202203673B (en) | 2024-01-31 |
| CN112457291A (zh) | 2021-03-09 |
| CN112457291B (zh) | 2022-07-22 |
| CN114929682B (zh) | 2024-05-14 |
| WO2021047525A1 (zh) | 2021-03-18 |
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