EA201400838A1 - ЗАМЕЩЕННЫЕ АМИДИНОМ β-ЛАКТАМЫ, ИХ ПОЛУЧЕНИЕ И ПРИМЕНЕНИЕ В КАЧЕСТВЕ АНТИБАКТЕРИАЛЬНЫХ СРЕДСТВ - Google Patents
ЗАМЕЩЕННЫЕ АМИДИНОМ β-ЛАКТАМЫ, ИХ ПОЛУЧЕНИЕ И ПРИМЕНЕНИЕ В КАЧЕСТВЕ АНТИБАКТЕРИАЛЬНЫХ СРЕДСТВInfo
- Publication number
- EA201400838A1 EA201400838A1 EA201400838A EA201400838A EA201400838A1 EA 201400838 A1 EA201400838 A1 EA 201400838A1 EA 201400838 A EA201400838 A EA 201400838A EA 201400838 A EA201400838 A EA 201400838A EA 201400838 A1 EA201400838 A1 EA 201400838A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- substituted
- application
- lactama
- amidin
- receiving
- Prior art date
Links
- 230000000844 anti-bacterial effect Effects 0.000 title 1
- 150000003952 β-lactams Chemical class 0.000 abstract 2
- 239000004599 antimicrobial Substances 0.000 abstract 1
- WZPBZJONDBGPKJ-VEHQQRBSSA-N aztreonam Chemical class O=C1N(S([O-])(=O)=O)[C@@H](C)[C@@H]1NC(=O)C(=N/OC(C)(C)C(O)=O)\C1=CSC([NH3+])=N1 WZPBZJONDBGPKJ-VEHQQRBSSA-N 0.000 abstract 1
Classifications
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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
- A61K31/41—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
- 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
- A61K31/4164—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
- 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
- A61K31/433—Thidiazoles
-
- 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
- A61K31/44—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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- 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
- A61K31/435—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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- A61K31/00—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
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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
- A61K31/4965—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
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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
- A61K31/505—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
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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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
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- 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)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
В заявке описаны новые β-лактамы формулы (I), их получение и применение. В частности, в заявке описаны новые β-лактамы, которые являются замещенными амидином производными монобактама, применимые в качестве противомикробных средств, и их получение.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12152279 | 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 |
|---|---|
| EA201400838A1 true EA201400838A1 (ru) | 2014-12-30 |
| EA027126B1 EA027126B1 (ru) | 2017-06-30 |
Family
ID=47603723
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201400838A EA027126B1 (ru) | 2012-01-24 | 2013-01-23 | ЗАМЕЩЕННЫЕ АМИДИНОМ β-ЛАКТАМЫ, ИХ ПОЛУЧЕНИЕ И ПРИМЕНЕНИЕ В КАЧЕСТВЕ АНТИБАКТЕРИАЛЬНЫХ СРЕДСТВ |
Country Status (42)
Cited By (1)
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| RU2746129C2 (ru) * | 2015-12-15 | 2021-04-07 | Мерк Шарп И Доум Корп. | Биарильные монобактамные соединения и способы их применения для лечения бактериальных инфекций |
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| WO2015103583A1 (en) * | 2014-01-06 | 2015-07-09 | President And Fellows Of Harvard College | Monobactams and methods of their synthesis and use |
| CN106164072B (zh) | 2014-03-24 | 2019-10-01 | 诺华股份有限公司 | 用于治疗细菌感染的单环内酰胺有机化合物 |
| 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 |
| ES2817537T3 (es) * | 2015-09-23 | 2021-04-07 | Novartis Ag | Sales y formas sólidas de un antibiótico monobactámico |
| 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 |
| SG10202111589RA (en) | 2016-08-26 | 2021-11-29 | Codexis Inc | Engineered imine reductases and methods for the reductive amination of ketone and amine compounds |
| WO2018091671A1 (en) | 2016-11-18 | 2018-05-24 | Aicuris Anti-Infective Cures Gmbh | Liposomal formulations of amidine substituted beta-lactam compounds for use in the treatment of bacterial infections |
| WO2018091668A1 (en) | 2016-11-18 | 2018-05-24 | Aicuris Anti-Infective Cures Gmbh | Novel formulations of amidine substituted beta-lactam compounds on the basis of modified cyclodextrins and acidifying agents, their preparation and use as antimicrobial pharmaceutical compositions |
| MX2019007613A (es) | 2016-12-21 | 2019-09-04 | Aicuris Gmbh & Co Kg | Terapia de combinacion con compuestos ?-lactamicos sustituidos con amidina e inhibidores de ?-lactamasa para infecciones con cepas bacterianas resistentes a antibioticos. |
| RU2020107152A (ru) | 2017-07-18 | 2021-08-27 | Байер Кропсайенс Акциенгезельшафт | Замещенные 3-гетероарилокси-1н-пиразолы и их соли, а также применение в качестве гербицидных активных веществ |
| WO2019020810A1 (en) | 2017-07-28 | 2019-01-31 | Aicuris Anti-Infective Cures Gmbh | CRYSTALLINE FORM OF (2S) -2 - [[(Z) - [- 1- (2-AMINO-4-THIAZOLYL) -2 - [[(3S) -2,2-DIMETHYL-4-OXO] -Acid 1- (SULFOOXY) -3-AZETIDINYL] AMINO] -2-OXOETHYLIDENE] AMINO] OXY] -3- [4- [IMINO [(3R) -3-PIPERIDINYLAMINO] METHYL] PHENOXY] -PROPANOIC |
| ES2912656T3 (es) | 2017-08-02 | 2022-05-26 | Novartis Ag | Proceso para preparar ácido 1-(((Z)-(1-(2-aminotiazol-4-il)-2-oxo-2-(((3S,4R)-2-oxo-4-((2-oxooxazolidin-3-il)metil)-1-sulfoacetidin-3-il)amino)etiliden)amino)oxi)ciclopropano carboxílico |
| MA50629A (fr) * | 2017-10-02 | 2021-03-31 | Merck Sharp & Dohme | Composés monobactames de chromane pour le traitement d'infections bactériennes |
| MX2020004071A (es) * | 2017-10-02 | 2020-07-28 | Arixa Pharmaceuticals Inc | Derivados de aztreonam y usos de los mismos. |
| JP7280273B2 (ja) * | 2018-01-29 | 2023-05-23 | メッドシャイン ディスカバリー インコーポレイテッド | 細菌感染を治療するための単環β－ラクタム化合物 |
| WO2020098635A1 (zh) * | 2018-11-13 | 2020-05-22 | 南京圣和药业股份有限公司 | 单环内酰胺化合物及其应用 |
| CN113227088B (zh) | 2018-12-18 | 2022-05-31 | 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 |
| US20230295149A1 (en) * | 2020-07-16 | 2023-09-21 | Ningxia Academy Of Agriculture And Forestry Sciences | Monobactam compounds, their preparation and use as antibacterial agents |
| CN114728953B (zh) * | 2020-08-06 | 2024-04-09 | 宁夏农林科学院 | β-内酰胺类化合物，及其制备方法以及其作为抗菌素的应用 |
| 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 |
| WO2023082055A1 (zh) * | 2021-11-09 | 2023-05-19 | 中国医学科学院医药生物技术研究所 | 包含β-内酰胺类化合物的药物组合物及其用途 |
| 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 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2746129C2 (ru) * | 2015-12-15 | 2021-04-07 | Мерк Шарп И Доум Корп. | Биарильные монобактамные соединения и способы их применения для лечения бактериальных инфекций |
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