EA201890150A1 - 3-тетразолил-бензол-1,2-дисульфонамидные производные в качестве ингибиторов металло-бета-лактамазы - Google Patents
3-тетразолил-бензол-1,2-дисульфонамидные производные в качестве ингибиторов металло-бета-лактамазыInfo
- Publication number
- EA201890150A1 EA201890150A1 EA201890150A EA201890150A EA201890150A1 EA 201890150 A1 EA201890150 A1 EA 201890150A1 EA 201890150 A EA201890150 A EA 201890150A EA 201890150 A EA201890150 A EA 201890150A EA 201890150 A1 EA201890150 A1 EA 201890150A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- beta
- lactamase
- compounds
- methogal
- disulphonamide
- Prior art date
Links
- 239000003781 beta lactamase inhibitor Substances 0.000 title abstract 4
- 229940126813 beta-lactamase inhibitor Drugs 0.000 title abstract 4
- FDJGHIHTRSUMLH-UHFFFAOYSA-N 3-(2H-tetrazol-5-yl)benzene-1,2-disulfonamide Chemical class N1N=NN=C1C1=C(C(=CC=C1)S(=O)(=O)N)S(=O)(=O)N FDJGHIHTRSUMLH-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 5
- 239000003782 beta lactam antibiotic agent Substances 0.000 abstract 2
- 102000020235 metallo-beta-lactamase Human genes 0.000 abstract 2
- 108060004734 metallo-beta-lactamase Proteins 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000002132 β-lactam antibiotic Substances 0.000 abstract 2
- 229940124586 β-lactam antibiotics Drugs 0.000 abstract 2
- 229940126085 β‑Lactamase Inhibitor Drugs 0.000 abstract 2
- 208000035143 Bacterial infection Diseases 0.000 abstract 1
- 208000022362 bacterial infectious disease Diseases 0.000 abstract 1
- 230000003115 biocidal effect Effects 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
- C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D257/04—Five-membered 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
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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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
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- 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
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- A61K31/429—Thiazoles condensed with heterocyclic ring systems
- A61K31/43—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems
- A61K31/431—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems containing further heterocyclic rings, e.g. ticarcillin, azlocillin, oxacillin
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Abstract
Настоящее изобретение относится к соединениям формулы I, являющимся ингибиторами металло-β-лактамазы,и их фармацевтически приемлемым солям, где Z, R, X, Xи Rимеют значения, определенные выше. Настоящее изобретение также относится к композициям, которые включают соединение по настоящему изобретению, являющееся ингибитором металло-β-лактамазы, или его фармацевтически приемлемую соль и фармацевтически приемлемый носитель необязательно в комбинации с бета-лактамовым антибиотиком и/или ингибитором бета-лактамазы. Изобретение также относится к способам лечения бактериальной инфекции, включающим введение пациенту терапевтически эффективного количества соединения по изобретению в комбинации с терапевтически эффективным количеством одного или нескольких β-лактамовых антибиотиков и необязательно в комбинации с одним или несколькими соединениями, являющимися ингибиторами бета-лактамазы. Соединения по изобретению являются полезными в способах, описанных в настоящей заявке, для преодоления резистентности к антибиотикам.
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CN106892845B (zh) * | 2017-02-28 | 2018-10-30 | 四川同晟生物医药有限公司 | 一种2,4-二氨基丁酸衍生物及其制备方法 |
US11207312B2 (en) * | 2017-07-17 | 2021-12-28 | Merck Sharp & Dohme Corp. | Metallo-beta-lactamase inhibitors and methods of use thereof |
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CN114531850B (zh) * | 2019-10-04 | 2024-08-06 | 富士胶片株式会社 | 以含有新的青霉素衍生物或其盐以及选自β-内酰胺酶抑制化合物及抗菌性化合物或其盐中的1种以上的化合物为特征的医药组合物及试剂盒 |
CN110840897B (zh) * | 2019-11-28 | 2023-08-08 | 河北旺发生物科技有限公司 | 金属β-内酰胺酶抑制剂 |
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CN111484506A (zh) * | 2020-04-16 | 2020-08-04 | 天津大学 | 添加表面活性剂改进美罗培南侧链中间体硫醇内酯的制备方法 |
WO2021237111A1 (en) * | 2020-05-21 | 2021-11-25 | Stemsynergy Therapeutics, Inc. | Notch inhibitors and uses thereof |
AR124167A1 (es) | 2020-11-30 | 2023-02-22 | Pi Industries Ltd | Una nueva composición agroquímica que comprende compuestos de fenilamidina 3-sustituidos |
CN114349711B (zh) * | 2022-02-28 | 2023-08-15 | 四川依维欣医药科技有限公司 | 一种(R)-1-Boc-3-羟甲基哌嗪的合成方法 |
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