ES2979245T3 - Antibióticos macrocíclicos de amplio espectro - Google Patents

Antibióticos macrocíclicos de amplio espectro Download PDF

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Publication number
ES2979245T3
ES2979245T3 ES18754727T ES18754727T ES2979245T3 ES 2979245 T3 ES2979245 T3 ES 2979245T3 ES 18754727 T ES18754727 T ES 18754727T ES 18754727 T ES18754727 T ES 18754727T ES 2979245 T3 ES2979245 T3 ES 2979245T3
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Spain
Prior art keywords
alkyl
compound
formula
optionally substituted
heterocycloalkyl
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ES18754727T
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English (en)
Spanish (es)
Inventor
Peter Smith
Tucker Roberts
Robert Higuchi
Prasuna Paraselli
Michael Koehler
Jacob Schwarz
James Crawford
Cuong Q Ly
Emily Hanan
Huiyong Hu
Yongsheng Chen
Zhiyong Yu
Paul Colin Michael Winship
Calum Mccleod
Toby Blench
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Genentech Inc
RQx Pharmaceuticals Inc
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Genentech Inc
RQx Pharmaceuticals Inc
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10Tetrapeptides
    • C07K5/1019Tetrapeptides with the first amino acid being basic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06Tripeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/07Tetrapeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08Peptides having 5 to 11 amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D245/00Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms
    • C07D245/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/08Bridged systems
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    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
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    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0821Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10Tetrapeptides
    • C07K5/1002Tetrapeptides with the first amino acid being neutral
    • C07K5/1016Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/06Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against 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)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • 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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
ES18754727T 2017-02-15 2018-02-22 Antibióticos macrocíclicos de amplio espectro Active ES2979245T3 (es)

Applications Claiming Priority (3)

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

Publications (1)

Publication Number Publication Date
ES2979245T3 true ES2979245T3 (es) 2024-09-25

Family

ID=63169158

Family Applications (1)

Application Number Title Priority Date Filing Date
ES18754727T Active ES2979245T3 (es) 2017-02-15 2018-02-22 Antibióticos macrocíclicos de amplio espectro

Country Status (22)

Country Link
US (2) US20210198316A9 (OSRAM)
EP (2) EP3583096B1 (OSRAM)
JP (2) JP7134177B2 (OSRAM)
KR (1) KR102671585B1 (OSRAM)
CN (1) CN110520413B (OSRAM)
AU (2) AU2018222093B2 (OSRAM)
BR (1) BR112019017003A2 (OSRAM)
CA (1) CA3053205A1 (OSRAM)
CL (1) CL2019002305A1 (OSRAM)
CO (1) CO2019010001A2 (OSRAM)
CR (2) CR20210144A (OSRAM)
ES (1) ES2979245T3 (OSRAM)
IL (1) IL268483B2 (OSRAM)
MA (1) MA47514A (OSRAM)
MX (2) MX2019009752A (OSRAM)
MY (1) MY199461A (OSRAM)
PE (2) PE20191618A1 (OSRAM)
PH (1) PH12019501904A1 (OSRAM)
SG (2) SG11201907448RA (OSRAM)
UA (1) UA126027C2 (OSRAM)
WO (1) WO2018149419A1 (OSRAM)
ZA (1) ZA201905371B (OSRAM)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3377474B1 (en) 2015-11-20 2023-08-16 RQX Pharmaceuticals, Inc. Macrocyclic broad spectrum antibiotics
MX2019003087A (es) 2016-09-16 2019-08-12 Cortexyme Inc Inhibidores cetónicos de gingipain de lisina.
IL295889B2 (en) 2019-05-28 2025-01-01 Hoffmann La Roche 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
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

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112012021931A2 (pt) * 2010-03-09 2016-05-31 Merck Canada Inc composto, composição farmacêutica, método para tratar uma infecção bacteriana, e, uso de composto
KR20130105659A (ko) * 2010-09-15 2013-09-25 더 스크립스 리서치 인스티튜트 광범위 스펙트럼 항생제 아릴로마이신 유사체
WO2012166665A2 (en) * 2011-05-27 2012-12-06 Rqx Pharmaceuticals, Inc. Broad spectrum antibiotics
CA2867448A1 (en) 2012-03-14 2013-09-19 Floyd E. Romesberg Broad spectrum antibiotic arylomycin analogs
EP2913854B1 (en) * 2012-10-23 2020-05-27 Fuji Electric Co., Ltd. Semiconductor device and method for manufacturing same
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
CA2892027A1 (en) 2012-11-21 2014-05-30 Rqx Pharmaceuticals, Inc. Macrocyclic broad spectrum antibiotics
US20190067498A1 (en) * 2017-08-28 2019-02-28 Meng Tao Light-induced aluminum plating on silicon for solar cell metallization
RU2016146581A (ru) * 2014-05-20 2018-06-21 АрКьюЭкс ФАРМАСЪЮТИКЛС, ИНК. Макроциклические антибиотики широкого спектра действия
EP3377474B1 (en) 2015-11-20 2023-08-16 RQX Pharmaceuticals, Inc. Macrocyclic broad spectrum antibiotics
TWI725075B (zh) * 2015-11-20 2021-04-21 美商Rqx製藥公司 巨環廣效抗生素
CA3057997A1 (en) 2017-03-27 2018-10-04 F. Hoffmann-La Roche Ag Process for making arylomyin ring analogs

Also Published As

Publication number Publication date
KR102671585B1 (ko) 2024-06-04
CA3053205A1 (en) 2018-08-23
CN110520413B (zh) 2023-02-17
AU2018222093B2 (en) 2022-03-31
NZ756220A (en) 2021-09-24
EP3583096A1 (en) 2019-12-25
RU2019126728A (ru) 2021-03-16
PH12019501904A1 (en) 2019-10-21
EP3583096A4 (en) 2021-01-06
US20210198316A9 (en) 2021-07-01
MX2019009752A (es) 2019-11-11
MA47514A (fr) 2019-12-25
RU2019126728A3 (OSRAM) 2021-09-15
ZA201905371B (en) 2025-01-29
CR20190428A (es) 2020-02-13
KR20190127720A (ko) 2019-11-13
JP2022180390A (ja) 2022-12-06
CR20210144A (es) 2021-05-13
US20230133667A1 (en) 2023-05-04
AU2022201724A1 (en) 2022-04-07
SG11201907448RA (en) 2019-09-27
UA126027C2 (uk) 2022-08-03
CL2019002305A1 (es) 2020-04-13
CO2019010001A2 (es) 2020-04-01
IL268483B1 (en) 2023-10-01
MX2022014485A (es) 2022-12-13
EP3583096B1 (en) 2024-03-27
MY199461A (en) 2023-10-30
US20200024309A1 (en) 2020-01-23
EP3583096C0 (en) 2024-03-27
AU2018222093A1 (en) 2019-08-29
PE20242298A1 (es) 2024-12-11
SG10202108876TA (en) 2021-09-29
JP2020507564A (ja) 2020-03-12
IL268483A (en) 2019-09-26
PE20191618A1 (es) 2019-11-05
AU2022201724B9 (en) 2024-03-21
EP4371982A3 (en) 2024-08-21
JP7134177B2 (ja) 2022-09-09
BR112019017003A2 (pt) 2020-04-14
JP7461425B2 (ja) 2024-04-03
EP4371982A2 (en) 2024-05-22
CN110520413A (zh) 2019-11-29
WO2018149419A1 (en) 2018-08-23
AU2022201724B2 (en) 2024-02-29
IL268483B2 (en) 2024-02-01

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