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
IL268483B1 (en
IL268483A (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

    • 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
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1019—Tetrapeptides with the first amino acid being basic
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D401/14—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
    • 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
    • C07—ORGANIC CHEMISTRY
    • 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
    • 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
    • C07D403/14—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D405/14—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07—ORGANIC CHEMISTRY
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1016—Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • 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

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 (21)

Country Link
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)
ZA (1) ZA201905371B (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

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
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
MX2013003035A (es) * 2010-09-15 2013-12-16 Scripps Research Inst Analogos de arilomicina como antibióticos de amplio espectro.
WO2012166665A2 (en) * 2011-05-27 2012-12-06 Rqx Pharmaceuticals, Inc. Broad spectrum antibiotics
KR20140140580A (ko) * 2012-03-14 2014-12-09 더 스크립스 리서치 인스티튜트 광범위 항생제 아릴로마이신 유사체
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
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
KR20180109858A (ko) * 2015-11-20 2018-10-08 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
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
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
CN110520413B (zh) 2023-02-17
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
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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