CN110520413B - 大环广谱抗生素 - Google Patents

大环广谱抗生素 Download PDF

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Publication number
CN110520413B
CN110520413B CN201880025278.0A CN201880025278A CN110520413B CN 110520413 B CN110520413 B CN 110520413B CN 201880025278 A CN201880025278 A CN 201880025278A CN 110520413 B CN110520413 B CN 110520413B
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alkyl
compound
optionally substituted
formula
another embodiment
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CN110520413A (zh
Inventor
彼得·安德鲁·史密斯
塔克·柯伦·罗伯茨
罗伯特·I·希古奇
普拉苏纳·帕拉塞利
迈克尔·F·T·凯勒
雅各布·布拉德利·施瓦兹
詹姆斯·约翰·克劳福德
强·Q·李
艾米丽·J·哈南
胡慧勇
陈永胜
郁志勇
保罗·科林·迈克尔·温希普
卡卢姆·麦克劳德
托比·布伦奇
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Genentech Inc
RQx Pharmaceuticals Inc
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RQx Pharmaceuticals Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
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    • C07K5/10—Tetrapeptides
    • C07K5/1019—Tetrapeptides with the first amino acid being basic
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06—Tripeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/07—Tetrapeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08—Peptides having 5 to 11 amino acids
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D245/00—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms
    • C07D245/04—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged systems
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    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
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    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
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    • C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
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    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
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    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
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    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Biophysics (AREA)
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  • Biochemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201880025278.0A 2017-02-15 2018-02-22 大环广谱抗生素 Active CN110520413B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CNPCT/CN2017/073575 2017-02-15
CNPCT/CN2017/073575 2017-02-15
CNPCT/CN2017/085075 2017-05-19
CNPCT/CN2017/085075 2017-05-19
PCT/CN2018/076957 WO2018149419A1 (en) 2017-02-15 2018-02-22 Macrocyclic broad spectrum antibiotics

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CN110520413A CN110520413A (zh) 2019-11-29
CN110520413B true CN110520413B (zh) 2023-02-17

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US (2) US20210198316A9 (enExample)
EP (2) EP4371982A3 (enExample)
JP (2) JP7134177B2 (enExample)
KR (1) KR102671585B1 (enExample)
CN (1) CN110520413B (enExample)
AU (2) AU2018222093B2 (enExample)
BR (1) BR112019017003A2 (enExample)
CL (1) CL2019002305A1 (enExample)
CO (1) CO2019010001A2 (enExample)
CR (2) CR20210144A (enExample)
ES (1) ES2979245T3 (enExample)
IL (1) IL268483B2 (enExample)
MA (1) MA47514A (enExample)
MX (2) MX2019009752A (enExample)
MY (1) MY199461A (enExample)
PE (2) PE20191618A1 (enExample)
PH (1) PH12019501904A1 (enExample)
SG (2) SG11201907448RA (enExample)
UA (1) UA126027C2 (enExample)
WO (1) WO2018149419A1 (enExample)
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KR20180109858A (ko) 2015-11-20 2018-10-08 알큐엑스 파마슈티컬스, 인크. 마크로시클릭 광범위 항생제
IL265389B1 (en) 2016-09-16 2026-07-01 Quince Therapeutics Inc Ketone compounds lysine inhibitors gingerapine, preparations containing them and uses thereof
IL288294B (en) 2019-05-28 2022-09-01 Hoffmann La Roche A broad-spectrum macrocyclic antibiotic
CN112480007B (zh) * 2020-12-08 2022-11-18 宿迁市科莱博生物化学有限公司 一种1，3-二甲基-1h-吡唑-4-羧酸的合成方法
EP4284804A1 (en) 2021-01-26 2023-12-06 Schrödinger, Inc. Tricyclic compounds useful in the treatment of cancer, autoimmune and inflammatory disorders
CN116284026B (zh) * 2023-03-16 2024-05-14 天津师范大学 一种水溶性阳离子分子笼及其合成方法与应用

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WO2012166665A2 (en) * 2011-05-27 2012-12-06 Rqx Pharmaceuticals, Inc. Broad spectrum antibiotics
CN102939095A (zh) * 2010-03-09 2013-02-20 默沙东公司 增强β-内酰胺抗菌药物的活性的桥联脂糖肽类
CN103209700A (zh) * 2010-09-15 2013-07-17 斯克里普斯研究所 广谱抗生素Arylomycin类似物
WO2013138187A1 (en) * 2012-03-14 2013-09-19 The Scripps Research Institute Broad spectrum antibiotic arylomycin analogs
CN103788176A (zh) * 2012-10-31 2014-05-14 上海来益生物药物研究开发中心有限责任公司 一种arylomycin类化合物及其制备方法和应用
CN104903302A (zh) * 2012-11-21 2015-09-09 阿奇克斯制药公司 大环广谱抗生素
WO2015179441A2 (en) * 2014-05-20 2015-11-26 Rqx Pharmaceuticals, Inc. Macrocyclic broad spectrum antibiotics
CN108884058A (zh) * 2015-11-20 2018-11-23 阿奇克斯制药公司 大环广谱抗生素

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CN104620391B (zh) * 2012-10-23 2017-09-19 富士电机株式会社 半导体装置及其制造方法
US20190067498A1 (en) * 2017-08-28 2019-02-28 Meng Tao Light-induced aluminum plating on silicon for solar cell metallization
KR20180109858A (ko) * 2015-11-20 2018-10-08 알큐엑스 파마슈티컬스, 인크. 마크로시클릭 광범위 항생제
MX386696B (es) 2017-03-27 2025-03-19 Hoffmann La Roche Proceso para producir analogos de anillo de arilomicina

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CN103209700A (zh) * 2010-09-15 2013-07-17 斯克里普斯研究所 广谱抗生素Arylomycin类似物
WO2012166665A2 (en) * 2011-05-27 2012-12-06 Rqx Pharmaceuticals, Inc. Broad spectrum antibiotics
WO2013138187A1 (en) * 2012-03-14 2013-09-19 The Scripps Research Institute Broad spectrum antibiotic arylomycin analogs
CN103788176A (zh) * 2012-10-31 2014-05-14 上海来益生物药物研究开发中心有限责任公司 一种arylomycin类化合物及其制备方法和应用
CN104903302A (zh) * 2012-11-21 2015-09-09 阿奇克斯制药公司 大环广谱抗生素
WO2015179441A2 (en) * 2014-05-20 2015-11-26 Rqx Pharmaceuticals, Inc. Macrocyclic broad spectrum antibiotics
CN108884058A (zh) * 2015-11-20 2018-11-23 阿奇克斯制药公司 大环广谱抗生素

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MX2019009752A (es) 2019-11-11
US20230133667A1 (en) 2023-05-04
CO2019010001A2 (es) 2020-04-01
US20200024309A1 (en) 2020-01-23
EP3583096A4 (en) 2021-01-06
SG10202108876TA (en) 2021-09-29
MY199461A (en) 2023-10-30
WO2018149419A1 (en) 2018-08-23
IL268483B1 (en) 2023-10-01
RU2019126728A3 (enExample) 2021-09-15
EP3583096B1 (en) 2024-03-27
PE20242298A1 (es) 2024-12-11
ES2979245T3 (es) 2024-09-25
JP2022180390A (ja) 2022-12-06
KR102671585B1 (ko) 2024-06-04
NZ779474A (en) 2025-12-19
ZA201905371B (en) 2025-01-29
EP3583096C0 (en) 2024-03-27
CN110520413A (zh) 2019-11-29
AU2018222093B2 (en) 2022-03-31
IL268483B2 (en) 2024-02-01
BR112019017003A2 (pt) 2020-04-14
SG11201907448RA (en) 2019-09-27
EP3583096A1 (en) 2019-12-25
CR20190428A (es) 2020-02-13
US20210198316A9 (en) 2021-07-01
JP2020507564A (ja) 2020-03-12
AU2022201724B9 (en) 2024-03-21
CL2019002305A1 (es) 2020-04-13
CR20210144A (es) 2021-05-13
KR20190127720A (ko) 2019-11-13
UA126027C2 (uk) 2022-08-03
IL268483A (en) 2019-09-26
MA47514A (fr) 2019-12-25
RU2019126728A (ru) 2021-03-16
EP4371982A2 (en) 2024-05-22
EP4371982A3 (en) 2024-08-21
PH12019501904A1 (en) 2019-10-21
AU2022201724B2 (en) 2024-02-29
PE20191618A1 (es) 2019-11-05
AU2022201724A1 (en) 2022-04-07
JP7461425B2 (ja) 2024-04-03
JP7134177B2 (ja) 2022-09-09
NZ756220A (en) 2021-09-24
AU2018222093A1 (en) 2019-08-29
MX2022014485A (es) 2022-12-13
CA3053205A1 (en) 2018-08-23

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