KR102036393B1 - 아미딘 치환된 베타 - 락탐 화합물, 그의 제조법 및 항박테리아제로서의 용도 - Google Patents
아미딘 치환된 베타 - 락탐 화합물, 그의 제조법 및 항박테리아제로서의 용도 Download PDFInfo
- Publication number
- KR102036393B1 KR102036393B1 KR1020147020410A KR20147020410A KR102036393B1 KR 102036393 B1 KR102036393 B1 KR 102036393B1 KR 1020147020410 A KR1020147020410 A KR 1020147020410A KR 20147020410 A KR20147020410 A KR 20147020410A KR 102036393 B1 KR102036393 B1 KR 102036393B1
- Authority
- KR
- South Korea
- Prior art keywords
- amino
- thiazol
- imino
- ethoxy
- methyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
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- 0 NC1=S*C(C(C(O)=O)=O)=N1 Chemical compound NC1=S*C(C(C(O)=O)=O)=N1 0.000 description 9
- GRRFBMQYCPYMBC-UHFFFAOYSA-N CC(C)(C)OC(NC(c1cc(OCCON)n[o]1)=N)=O Chemical compound CC(C)(C)OC(NC(c1cc(OCCON)n[o]1)=N)=O GRRFBMQYCPYMBC-UHFFFAOYSA-N 0.000 description 1
- AJTKQGMYQBMZGS-UHFFFAOYSA-N CC(C)(C)OC(NCCNC(c(cc1)ccc1OCCON)=N)=O Chemical compound CC(C)(C)OC(NCCNC(c(cc1)ccc1OCCON)=N)=O AJTKQGMYQBMZGS-UHFFFAOYSA-N 0.000 description 1
- JPQCZOUBLNGLCZ-UHFFFAOYSA-N CC(C)(C)OC(Nc1nc(C(C(O)=O)=O)n[s]1)=O Chemical compound CC(C)(C)OC(Nc1nc(C(C(O)=O)=O)n[s]1)=O JPQCZOUBLNGLCZ-UHFFFAOYSA-N 0.000 description 1
- YRAFKVURGTWWAR-UHFFFAOYSA-N CC(C)=NOc(cc(cc1)OCCO)c1C#N Chemical compound CC(C)=NOc(cc(cc1)OCCO)c1C#N YRAFKVURGTWWAR-UHFFFAOYSA-N 0.000 description 1
- YUZJUGRUZGALAN-UHFFFAOYSA-N COC(c1ccc(CON)cc1)=N Chemical compound COC(c1ccc(CON)cc1)=N YUZJUGRUZGALAN-UHFFFAOYSA-N 0.000 description 1
- SVKXAHPZDRANQO-HRFVKAFMSA-N C[C@@H]([C@@H](C1=O)N)N1OS(O)(=O)=O Chemical compound C[C@@H]([C@@H](C1=O)N)N1OS(O)(=O)=O SVKXAHPZDRANQO-HRFVKAFMSA-N 0.000 description 1
- REIVHYDACHXPNH-UHFFFAOYSA-N N#Cc(c(F)c1)ccc1O Chemical compound N#Cc(c(F)c1)ccc1O REIVHYDACHXPNH-UHFFFAOYSA-N 0.000 description 1
- YDTVKCOARXOARR-UHFFFAOYSA-N N#Cc(c(F)c1)ccc1OCCO Chemical compound N#Cc(c(F)c1)ccc1OCCO YDTVKCOARXOARR-UHFFFAOYSA-N 0.000 description 1
- XAASLEJRGFPHEV-UHFFFAOYSA-N N#Cc1ccc(CO)cc1 Chemical compound N#Cc1ccc(CO)cc1 XAASLEJRGFPHEV-UHFFFAOYSA-N 0.000 description 1
- VRWZNQITCNBJML-UHFFFAOYSA-N N#Cc1ccc(CON(C(c2c3cccc2)=O)C3=O)cc1 Chemical compound N#Cc1ccc(CON(C(c2c3cccc2)=O)C3=O)cc1 VRWZNQITCNBJML-UHFFFAOYSA-N 0.000 description 1
- OEIPIJFGEGNECW-UHFFFAOYSA-N NC(c(c(O)c1)ccc1OCCO)=N Chemical compound NC(c(c(O)c1)ccc1OCCO)=N OEIPIJFGEGNECW-UHFFFAOYSA-N 0.000 description 1
- FFECICSIEWAXST-UHFFFAOYSA-N NC(c(c(O)c1)ccc1OCCON)=N Chemical compound NC(c(c(O)c1)ccc1OCCON)=N FFECICSIEWAXST-UHFFFAOYSA-N 0.000 description 1
- JAZANDLWODVWHS-UHFFFAOYSA-N NC(c1ccc(CON)cc1)=N Chemical compound NC(c1ccc(CON)cc1)=N JAZANDLWODVWHS-UHFFFAOYSA-N 0.000 description 1
- GJXXWECMKNBNEN-UHFFFAOYSA-N NOCCOc(cc1)ccc1C(NCc1ccccn1)=N Chemical compound NOCCOc(cc1)ccc1C(NCc1ccccn1)=N GJXXWECMKNBNEN-UHFFFAOYSA-N 0.000 description 1
- ATBANLOLDZIUOW-UHFFFAOYSA-N NOCc(cc1)ccc1C#N Chemical compound NOCc(cc1)ccc1C#N ATBANLOLDZIUOW-UHFFFAOYSA-N 0.000 description 1
- SYSDTUXAHIKTRD-UHFFFAOYSA-N Nc1n[o]c2cc(OCCO)ccc12 Chemical compound Nc1n[o]c2cc(OCCO)ccc12 SYSDTUXAHIKTRD-UHFFFAOYSA-N 0.000 description 1
Classifications
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- A—HUMAN NECESSITIES
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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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/433—Thidiazoles
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- A—HUMAN NECESSITIES
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- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- 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
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- A—HUMAN NECESSITIES
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- 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
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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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
- A61K31/395—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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
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- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
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- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
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- A—HUMAN NECESSITIES
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-
- 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
- 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
- C07D417/14—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 three or more hetero rings
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12152279 | 2012-01-24 | ||
| EP12152279.1 | 2012-01-24 | ||
| PCT/EP2013/051217 WO2013110643A1 (en) | 2012-01-24 | 2013-01-23 | Amidine substituted beta - lactam compounds, their preparation and use as antibacterial agents |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20140114390A KR20140114390A (ko) | 2014-09-26 |
| KR102036393B1 true KR102036393B1 (ko) | 2019-10-24 |
Family
ID=47603723
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020147020410A Expired - Fee Related KR102036393B1 (ko) | 2012-01-24 | 2013-01-23 | 아미딘 치환된 베타 - 락탐 화합물, 그의 제조법 및 항박테리아제로서의 용도 |
Country Status (42)
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015103583A1 (en) * | 2014-01-06 | 2015-07-09 | President And Fellows Of Harvard College | Monobactams and methods of their synthesis and use |
| MX373444B (es) | 2014-03-24 | 2020-04-30 | Novartis Ag | Compuestos organicos de monobactam para el tratamiento de infecciones bacterianas. |
| CN105175335B (zh) * | 2015-08-13 | 2017-11-03 | 南阳师范学院 | 一种3‑(3,3‑二氯烯丙氧基)‑1‑甲基吡唑‑5‑甲酰胺衍生物及其制备方法 |
| PL3353175T3 (pl) * | 2015-09-23 | 2021-02-22 | Novartis Ag | Sole i postacie stałe antybiotyku monobaktamowego |
| US20180339983A1 (en) | 2015-12-15 | 2018-11-29 | Merck Sharp & Dohme Corp. | Biaryl monobactam compounds and methods of use thereof for the treatment of bacterial infections |
| CA3016341A1 (en) * | 2016-03-07 | 2017-09-14 | Merck Sharp & Dohme Corp. | Bicyclic aryl monobactam compounds and methods of use thereof for the treatment of bacterial infections |
| CN107641119B (zh) | 2016-07-21 | 2019-11-08 | 中国科学院上海药物研究所 | 单环β-内酰胺-铁载体轭合物及其制备方法和用途 |
| IL264686B2 (en) | 2016-08-26 | 2024-07-01 | Codexis Inc | Engineered imine reductases and methods for reversible amination of ketone and amine compounds |
| CA3043976A1 (en) | 2016-11-18 | 2018-05-24 | Aicuris Gmbh & Co. Kg | Liposomal formulations of amidine substituted beta-lactam compounds for use in the treatment of bacterial infections |
| CN110022857A (zh) | 2016-11-18 | 2019-07-16 | 艾库里斯抗感染治疗有限公司 | 基于改性环糊精和酸化剂的脒取代β-内酰胺化合物的新制剂、其制备及作为抗微生物药物组合物的用途 |
| AU2017339587A1 (en) | 2016-12-21 | 2019-07-04 | Aicuris Gmbh & Co. Kg | Combination therapy with amidine substituted ß-lactam compounds and ß-lactamase inhibitors for infections with antibiotic resistant bacterial strains |
| CN111132973A (zh) | 2017-07-18 | 2020-05-08 | 拜耳作物科学股份公司 | 取代的3-杂芳氧基-1h-吡唑及其盐及其作为除草活性物质的用途 |
| TW201920163A (zh) | 2017-07-28 | 2019-06-01 | 德商艾庫里斯抗感染治療有限公司 | (2s)‐2‐[[(z)‐[1‐(2‐胺基‐4‐噻唑基)‐2‐[[(3s)‐2,2‐二甲基‐4‐側氧基‐1‐(磺氧)‐3‐吖丁啶基]胺基]‐2‐氧亞乙基]胺基]氧基]‐3‐[4‐[亞胺基[(3r)‐3-哌啶基胺基]甲基]苯氧基]-丙酸之晶型 |
| JP7235718B2 (ja) | 2017-08-02 | 2023-03-08 | ノバルティス アーゲー | モノバクタム系抗生物質およびその中間体を製造するための化学的方法 |
| KR102455390B1 (ko) * | 2017-10-02 | 2022-10-17 | 아릭사 파마슈티컬스 인코포레이티드 | 아즈트레오남 유도체 및 이의 용도 |
| EP3691639B1 (en) * | 2017-10-02 | 2023-11-15 | Merck Sharp & Dohme LLC | Chromane monobactam compounds for the treatment of bacterial infections |
| WO2019144969A1 (zh) | 2018-01-29 | 2019-08-01 | 南京明德新药研发股份有限公司 | 用于治疗细菌感染的单环β-内酰胺化合物 |
| KR20210083285A (ko) * | 2018-11-13 | 2021-07-06 | 난징 산홈 팔마세우티칼 컴퍼니 리미티드 | 모노박탐 화합물 및 그의 사용 |
| WO2020125670A1 (zh) | 2018-12-18 | 2020-06-25 | 南京明德新药研发有限公司 | 单环β-内酰胺化合物在制药中的应用 |
| CN111303144B (zh) * | 2019-12-13 | 2020-11-27 | 苏州信诺维医药科技有限公司 | 一种治疗细菌感染的化合物 |
| CN114828850B (zh) | 2019-12-19 | 2024-08-13 | 深圳嘉科生物科技有限公司 | 化合物在制药中的应用 |
| CN111253405B (zh) * | 2020-03-20 | 2022-12-16 | 南京安伦化工科技有限公司 | 一种比阿培南中间体的制备方法 |
| CN113754651B (zh) | 2020-06-02 | 2023-04-18 | 中国医学科学院医药生物技术研究所 | 一种β-内酰胺化合物、其用途及其制备方法 |
| CN111592536B (zh) * | 2020-06-04 | 2023-11-03 | 宁夏农林科学院农业资源与环境研究所（宁夏土壤与植物营养重点实验室） | 单环β-内酰胺化合物及其制备方法和应用 |
| CN111675641B (zh) * | 2020-06-04 | 2023-09-08 | 宁夏农林科学院农业资源与环境研究所（宁夏土壤与植物营养重点实验室） | 单环β-内酰胺类化合物、单环内酰胺类化合物盐及其制备方法 |
| WO2022011626A1 (en) * | 2020-07-16 | 2022-01-20 | Ningxia Academy Of Agriculture And Forestry Sciences | Novel monobactam compounds, their preparation and use as antibacterial agents |
| US12516048B2 (en) | 2020-08-06 | 2026-01-06 | Ningxia Academy Of Agriculture And Forestry Sciences | B-lactam compounds, their preparation and use as antibacterial agents |
| CN112079791A (zh) * | 2020-08-21 | 2020-12-15 | 宁夏农林科学院农业资源与环境研究所（宁夏土壤与植物营养重点实验室） | 单环β-内酰胺类抗生素侧链酸及其酯、其制备方法和应用 |
| CN111909067B (zh) * | 2020-08-28 | 2022-03-15 | 浙江凯普化工有限公司 | 一种d-青霉胺的有机全合成方法 |
| AU2021473165B2 (en) * | 2021-11-09 | 2025-05-22 | Guangzhou HC New Drug Research Co., Ltd. | PHARMACEUTICAL COMPOSITION CONTAINING β-LACTAM COMPOUND AND USE THEREOF |
| GEAP202416514A (en) | 2021-11-18 | 2024-08-26 | Merck Sharp & Dohme Llc | Chromane amidine monobactam antibiotics |
| JP7671398B2 (ja) * | 2021-11-18 | 2025-05-01 | メルク・シャープ・アンド・ドーム・エルエルシー | クロマンアミジンモノバクタム抗生物質 |
| CN118255695B (zh) * | 2024-02-26 | 2025-03-14 | 广州艾奇西医药科技有限公司 | 一种β-内酰胺类化合物的中间体的纯化方法和制备方法 |
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