CN106188175B - 使用抗菌氨基糖苷化合物治疗肺炎克雷伯杆菌感染 - Google Patents
使用抗菌氨基糖苷化合物治疗肺炎克雷伯杆菌感染 Download PDFInfo
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- CN106188175B CN106188175B CN201610573991.1A CN201610573991A CN106188175B CN 106188175 B CN106188175 B CN 106188175B CN 201610573991 A CN201610573991 A CN 201610573991A CN 106188175 B CN106188175 B CN 106188175B
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- tert
- hydroxy
- butoxycarbonyl
- amino
- sisomicin
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- 229940126575 aminoglycoside Drugs 0.000 title claims abstract description 43
- 206010061259 Klebsiella infection Diseases 0.000 title description 18
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- 208000015181 infectious disease Diseases 0.000 claims abstract description 13
- -1 4-amino-2 (S) -hydroxy-butyryl Chemical group 0.000 claims description 1486
- 229960005456 sisomicin Drugs 0.000 claims description 1087
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims description 59
- 150000003839 salts Chemical class 0.000 claims description 45
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- 241000607715 Serratia marcescens Species 0.000 claims 1
- 238000000034 method Methods 0.000 abstract description 331
- 241000588747 Klebsiella pneumoniae Species 0.000 abstract description 27
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- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 28
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- DYHSDKLCOJIUFX-UHFFFAOYSA-N tert-butoxycarbonyl anhydride Chemical compound CC(C)(C)OC(=O)OC(=O)OC(C)(C)C DYHSDKLCOJIUFX-UHFFFAOYSA-N 0.000 description 20
- MVQXBXLDXSQURK-UHFFFAOYSA-N 2-aminoethanesulfonamide Chemical compound NCCS(N)(=O)=O MVQXBXLDXSQURK-UHFFFAOYSA-N 0.000 description 18
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- 125000003118 aryl group Chemical group 0.000 description 17
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- 239000011592 zinc chloride Substances 0.000 description 1
- 150000003952 β-lactams Chemical class 0.000 description 1
- 229940126085 β‑Lactamase Inhibitor Drugs 0.000 description 1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
- C07H15/20—Carbocyclic rings
- C07H15/22—Cyclohexane rings, substituted by nitrogen atoms
- C07H15/222—Cyclohexane rings substituted by at least two nitrogen atoms
- C07H15/226—Cyclohexane rings substituted by at least two nitrogen atoms with at least two saccharide radicals directly attached to the cyclohexane rings
- C07H15/234—Cyclohexane rings substituted by at least two nitrogen atoms with at least two saccharide radicals directly attached to the cyclohexane rings attached to non-adjacent ring carbon atoms of the cyclohexane rings, e.g. kanamycins, tobramycin, nebramycin, gentamicin A2
- C07H15/236—Cyclohexane rings substituted by at least two nitrogen atoms with at least two saccharide radicals directly attached to the cyclohexane rings attached to non-adjacent ring carbon atoms of the cyclohexane rings, e.g. kanamycins, tobramycin, nebramycin, gentamicin A2 a saccharide radical being substituted by an alkylamino radical in position 3 and by two substituents different from hydrogen in position 4, e.g. gentamicin complex, sisomicin, verdamycin
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- A61K31/00—Medicinal preparations containing organic active ingredients
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- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
- A61K31/7036—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
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- A—HUMAN NECESSITIES
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
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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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- 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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Abstract
Description
试验化合物 | AECO001 | AECO040 | ASMA003 | AACA005 |
西索米星 | 0.5 | 32 | 8 | 32 |
单取代的化合物1 | 1 | >64 | 1 | 2 |
单取代的化合物2 | 1 | 1 | 0.5 | 4 |
单取代的化合物3 | 0.5 | 0.25 | 1 | 0.5 |
单取代的化合物4 | 2 | 16 | 1 | 1 |
单取代的化合物5 | 0.5 | 8 | 2 | 32 |
单取代的化合物6 | 0.5 | 4 | 4 | 16 |
单取代的化合物7 | 1 | 4 | 16 | 32 |
实施例1 | 0.5 | 0.5 | 2 | 2 |
实施例12 | 1 | 0.5 | 4 | 2 |
实施例13 | 1 | 0.125 | 2 | 2 |
实施例16 | 1 | 1 | 2 | 2 |
实施例17 | 1 | 0.5 | 2 | 2 |
实施例18 | 1 | 0.25 | 4 | 2 |
实施例48 | 1 | 0.5 | 2 | 2 |
实施例61 | 1 | 16 | 4 | 2 |
Claims (17)
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
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US17846109P | 2009-05-14 | 2009-05-14 | |
US61/178,461 | 2009-05-14 | ||
US30546310P | 2010-02-17 | 2010-02-17 | |
US61/305,463 | 2010-02-17 | ||
CN201080031078.XA CN102481307B (zh) | 2009-05-14 | 2010-05-14 | 使用抗菌氨基糖苷化合物治疗肺炎克雷伯杆菌感染 |
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CN201080031078.XA Division CN102481307B (zh) | 2009-05-14 | 2010-05-14 | 使用抗菌氨基糖苷化合物治疗肺炎克雷伯杆菌感染 |
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CN106188175A CN106188175A (zh) | 2016-12-07 |
CN106188175B true CN106188175B (zh) | 2020-08-11 |
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CN201610573991.1A Active CN106188175B (zh) | 2009-05-14 | 2010-05-14 | 使用抗菌氨基糖苷化合物治疗肺炎克雷伯杆菌感染 |
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US (2) | US20120214759A1 (zh) |
CN (2) | CN102481307B (zh) |
CA (2) | CA2761674C (zh) |
WO (1) | WO2010132770A1 (zh) |
Families Citing this family (24)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2632968A1 (en) | 2005-12-02 | 2007-06-07 | Isis Pharmaceuticals, Inc. | Antibacterial 4,5-substituted aminoglycoside analogs having multiple substituents |
EP2148884A1 (en) * | 2007-04-10 | 2010-02-03 | Achaogen, Inc. | Antibacterial 1,4,5-substituted aminoglycoside analogs |
CA2706369C (en) | 2007-11-21 | 2014-03-25 | Achaogen, Inc. | Antibacterial aminoglycoside analogs |
WO2010030690A1 (en) | 2008-09-10 | 2010-03-18 | Isis Pharmaceuticals, Inc. | Antibacterial 4,6-substituted 6', 6" and 1 modified aminoglycoside analogs |
WO2010030704A2 (en) | 2008-09-10 | 2010-03-18 | Achaogen, Inc. | Antibacterial aminoglycoside analogs |
WO2010042851A1 (en) | 2008-10-09 | 2010-04-15 | Achaogen, Inc. | Antibacterial aminoglycoside analogs |
WO2010042850A1 (en) | 2008-10-09 | 2010-04-15 | Achaogen, Inc. | Antibacterial aminoglycoside analogs |
WO2010132839A2 (en) * | 2009-05-14 | 2010-11-18 | Achaogen, Inc. | Aminoglycoside dosing regimens |
WO2010132759A1 (en) | 2009-05-15 | 2010-11-18 | Achaogen, Inc. | Antibacterial derivatives of dibekacin |
WO2010132768A1 (en) | 2009-05-15 | 2010-11-18 | Achaogen, Inc. | Antibacterial derivatives of sisomicin |
WO2010132757A2 (en) | 2009-05-15 | 2010-11-18 | Achaogen, Inc. | Antibacterial aminoglycoside analogs |
WO2010132765A2 (en) | 2009-05-15 | 2010-11-18 | Achaogen, Inc. | Antibacterial aminoglycoside analogs |
WO2010132760A1 (en) | 2009-05-15 | 2010-11-18 | Achaogen, Inc. | Antibacterial derivatives of tobramycin |
JP2013507391A (ja) | 2009-10-09 | 2013-03-04 | アカオジェン インコーポレイテッド | 抗ウイルスアミノグリコシド類似体 |
WO2012067978A1 (en) | 2010-11-17 | 2012-05-24 | Achaogen, Inc. | Antibacterial amiinoglycoside analogs |
CN102652751A (zh) * | 2011-03-04 | 2012-09-05 | 珠海联邦制药股份有限公司 | 一种含有头孢噻肟的药物组合物及其制剂和制备方法 |
CN103130881B (zh) * | 2013-02-06 | 2014-09-10 | 王冬国 | 一种肺炎克雷伯菌的耐药新基因 |
US9238670B2 (en) | 2013-03-15 | 2016-01-19 | The Board Of Trustees Of The Leland Stanford Junior University | Aminoglycoside antibiotics with reduced ototoxicity |
CN104356182B (zh) * | 2014-11-11 | 2017-05-24 | 齐鲁天和惠世制药有限公司 | 一种提高制备阿米卡星收率的方法 |
US10197504B2 (en) | 2016-10-10 | 2019-02-05 | Altria Client Services Llc | Method and system of detecting foreign materials within an agricultural product stream |
WO2018155995A1 (ko) * | 2017-02-27 | 2018-08-30 | 한국생명공학연구원 | 시아릴락토오스를 유효성분으로 포함하는 항균용 조성물 |
TWI801438B (zh) | 2017-10-19 | 2023-05-11 | 中國大陸商軒竹(北京)醫藥科技有限公司 | 抗菌胺基糖苷類似物之合成 |
CN110885350A (zh) * | 2019-08-28 | 2020-03-17 | 山东安信制药有限公司 | 一种普拉佐米星的制备方法 |
CN116462721B (zh) * | 2023-04-18 | 2024-02-02 | 江南大学 | 抗菌性氨基糖苷衍生物 |
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2010
- 2010-05-14 CA CA2761674A patent/CA2761674C/en not_active Expired - Fee Related
- 2010-05-14 CN CN201080031078.XA patent/CN102481307B/zh active Active
- 2010-05-14 WO PCT/US2010/034898 patent/WO2010132770A1/en active Application Filing
- 2010-05-14 CA CA2948868A patent/CA2948868A1/en not_active Abandoned
- 2010-05-14 CN CN201610573991.1A patent/CN106188175B/zh active Active
-
2011
- 2011-11-11 US US13/294,426 patent/US20120214759A1/en not_active Abandoned
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2019
- 2019-01-04 US US16/240,370 patent/US20190374563A1/en not_active Abandoned
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CA2761674A1 (en) | 2010-11-18 |
CN102481307B (zh) | 2016-08-24 |
WO2010132770A1 (en) | 2010-11-18 |
US20120214759A1 (en) | 2012-08-23 |
US20190374563A1 (en) | 2019-12-12 |
CA2761674C (en) | 2016-11-29 |
CA2948868A1 (en) | 2010-11-18 |
CN102481307A (zh) | 2012-05-30 |
CN106188175A (zh) | 2016-12-07 |
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