IL268483B2 - Macrocyclic broad spectrum antibiotics - Google Patents

Macrocyclic broad spectrum antibiotics

Info

Publication number
IL268483B2
IL268483B2 IL268483A IL26848319A IL268483B2 IL 268483 B2 IL268483 B2 IL 268483B2 IL 268483 A IL268483 A IL 268483A IL 26848319 A IL26848319 A IL 26848319A IL 268483 B2 IL268483 B2 IL 268483B2
Authority
IL
Israel
Prior art keywords
alkyl
compound
formula
another embodiment
optionally substituted
Prior art date
Application number
IL268483A
Other languages
English (en)
Hebrew (he)
Other versions
IL268483A (en
IL268483B1 (en
Original Assignee
Rqx Pharmaceuticals Inc
Genentech Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Rqx Pharmaceuticals Inc, Genentech Inc filed Critical Rqx Pharmaceuticals Inc
Publication of IL268483A publication Critical patent/IL268483A/en
Publication of IL268483B1 publication Critical patent/IL268483B1/en
Publication of IL268483B2 publication Critical patent/IL268483B2/en

Links

Classifications

    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • 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
    • C07K5/08Tripeptides
    • 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

Landscapes

  • 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)
  • 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)
IL268483A 2017-02-15 2018-02-22 Macrocyclic broad spectrum antibiotics IL268483B2 (en)

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 (3)

Publication Number Publication Date
IL268483A IL268483A (en) 2019-09-26
IL268483B1 IL268483B1 (en) 2023-10-01
IL268483B2 true IL268483B2 (en) 2024-02-01

Family

ID=63169158

Family Applications (1)

Application Number Title Priority Date Filing Date
IL268483A IL268483B2 (en) 2017-02-15 2018-02-22 Macrocyclic broad spectrum antibiotics

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
US11072635B2 (en) 2015-11-20 2021-07-27 Rqx Pharmaceuticals, Inc. Macrocyclic broad spectrum antibiotics
EP3512846B1 (en) 2016-09-16 2024-08-14 Lighthouse Pharmaceuticals, Inc. Ketone inhibitors of lysine gingipain
US11208387B2 (en) * 2019-05-28 2021-12-28 Genentech, Inc. Macrocyclic broad spectrum antibiotics
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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014081886A1 (en) * 2012-11-21 2014-05-30 Rqx Pharmaceuticals, Inc. Macrocyclic broad spectrum antibiotics

Family Cites Families (11)

* 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
RU2013112483A (ru) * 2010-09-15 2014-10-20 Дзе Скриппс Рисеч Инститьют Аналоги ариломицина, представляющие собой антибиотики широкого спектра действия
US20140249073A1 (en) * 2011-05-27 2014-09-04 Rqx Pharmaceuticals, Inc Broad spectrum antibiotics
WO2013138187A1 (en) * 2012-03-14 2013-09-19 The Scripps Research Institute Broad spectrum antibiotic arylomycin analogs
JP6090329B2 (ja) * 2012-10-23 2017-03-08 富士電機株式会社 半導体装置およびその製造方法
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
US20190067498A1 (en) * 2017-08-28 2019-02-28 Meng Tao Light-induced aluminum plating on silicon for solar cell metallization
KR20170027721A (ko) * 2014-05-20 2017-03-10 알큐엑스 파마슈티컬스, 인크. 마크로시클릭 광범위 항생제
TWI725075B (zh) * 2015-11-20 2021-04-21 美商Rqx製藥公司 巨環廣效抗生素
US11072635B2 (en) * 2015-11-20 2021-07-27 Rqx Pharmaceuticals, Inc. Macrocyclic broad spectrum antibiotics
MX386696B (es) 2017-03-27 2025-03-19 Hoffmann La Roche Proceso para producir analogos de anillo de arilomicina

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014081886A1 (en) * 2012-11-21 2014-05-30 Rqx Pharmaceuticals, Inc. Macrocyclic broad spectrum antibiotics

Also Published As

Publication number Publication date
RU2019126728A3 (OSRAM) 2021-09-15
MY199461A (en) 2023-10-30
NZ756220A (en) 2021-09-24
SG11201907448RA (en) 2019-09-27
EP4371982A3 (en) 2024-08-21
EP3583096A1 (en) 2019-12-25
WO2018149419A1 (en) 2018-08-23
SG10202108876TA (en) 2021-09-29
JP7134177B2 (ja) 2022-09-09
CR20190428A (es) 2020-02-13
US20210198316A9 (en) 2021-07-01
CN110520413A (zh) 2019-11-29
JP7461425B2 (ja) 2024-04-03
EP3583096C0 (en) 2024-03-27
PE20242298A1 (es) 2024-12-11
UA126027C2 (uk) 2022-08-03
CA3053205A1 (en) 2018-08-23
KR20190127720A (ko) 2019-11-13
US20230133667A1 (en) 2023-05-04
JP2020507564A (ja) 2020-03-12
AU2018222093A1 (en) 2019-08-29
CO2019010001A2 (es) 2020-04-01
US20200024309A1 (en) 2020-01-23
AU2022201724B9 (en) 2024-03-21
CN110520413B (zh) 2023-02-17
MX2019009752A (es) 2019-11-11
AU2022201724B2 (en) 2024-02-29
CR20210144A (es) 2021-05-13
ES2979245T3 (es) 2024-09-25
CL2019002305A1 (es) 2020-04-13
MX2022014485A (es) 2022-12-13
PE20191618A1 (es) 2019-11-05
JP2022180390A (ja) 2022-12-06
IL268483A (en) 2019-09-26
ZA201905371B (en) 2025-01-29
IL268483B1 (en) 2023-10-01
MA47514A (fr) 2019-12-25
EP4371982A2 (en) 2024-05-22
RU2019126728A (ru) 2021-03-16
KR102671585B1 (ko) 2024-06-04
EP3583096B1 (en) 2024-03-27
PH12019501904A1 (en) 2019-10-21
EP3583096A4 (en) 2021-01-06
BR112019017003A2 (pt) 2020-04-14
AU2022201724A1 (en) 2022-04-07
AU2018222093B2 (en) 2022-03-31

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