CN112996778A - 制备微管溶素及其中间体的替代方法 - Google Patents

制备微管溶素及其中间体的替代方法 Download PDF

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Publication number
CN112996778A
CN112996778A CN201980071734.XA CN201980071734A CN112996778A CN 112996778 A CN112996778 A CN 112996778A CN 201980071734 A CN201980071734 A CN 201980071734A CN 112996778 A CN112996778 A CN 112996778A
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China
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optionally substituted
formula
moiety
compound
alkyl
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CN201980071734.XA
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English (en)
Chinese (zh)
Inventor
吴坤亮
金庆武
W·道布尔迪
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Xigen Co
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Xigen Co
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Publication of CN112996778A publication Critical patent/CN112996778A/zh
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K1/00General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/107General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
    • C07K1/1072General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups
    • C07K1/1077General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups by covalent attachment of residues other than amino acids or peptide residues, e.g. sugars, polyols, fatty acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/56Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/26Acyclic or carbocyclic radicals, substituted by hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/021Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)n-C(=0)-, n being 5 or 6; for n > 6, classification in C07K5/06 - C07K5/10, according to the moiety having normal peptide bonds
    • 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
    • C07K5/1024Tetrapeptides with the first amino acid being heterocyclic
    • 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
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Engineering & Computer Science (AREA)
  • Analytical Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Biotechnology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201980071734.XA 2018-09-07 2019-09-06 制备微管溶素及其中间体的替代方法 Pending CN112996778A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862728639P 2018-09-07 2018-09-07
US62/728,639 2018-09-07
PCT/US2019/050023 WO2020051503A1 (en) 2018-09-07 2019-09-06 Alternative processes for the preparation of tubulysins and intermediates thereof

Publications (1)

Publication Number Publication Date
CN112996778A true CN112996778A (zh) 2021-06-18

Family

ID=68000124

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980071734.XA Pending CN112996778A (zh) 2018-09-07 2019-09-06 制备微管溶素及其中间体的替代方法

Country Status (17)

Country Link
US (1) US20230002440A1 (https=)
EP (1) EP3847161A1 (https=)
JP (1) JP7511543B2 (https=)
KR (1) KR20210073525A (https=)
CN (1) CN112996778A (https=)
AU (1) AU2019336231A1 (https=)
BR (1) BR112021004317A2 (https=)
CA (1) CA3111149A1 (https=)
EA (1) EA202190699A1 (https=)
IL (1) IL281090A (https=)
MA (1) MA53550A (https=)
MX (1) MX2021002570A (https=)
SA (1) SA521421375B1 (https=)
SG (1) SG11202102126VA (https=)
TW (1) TWI825169B (https=)
UA (1) UA128730C2 (https=)
WO (1) WO2020051503A1 (https=)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115867283A (zh) * 2020-12-23 2023-03-28 启德医药科技(苏州)有限公司 包含开环硫代琥珀酰亚胺基团、寡肽片段和手性部分的新型异构化合物
BR112023018676A2 (pt) 2021-03-18 2023-10-10 Seagen Inc Conjugado anticorpo-fármaco, composição farmacêutica, métodos de tratamento de uma doença ou condição e de um câncer, e, composição de conjugado ligante-fármaco

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008138561A1 (en) * 2007-05-10 2008-11-20 R & D Biopharmaceuticals Gmbh Tubulysine derivatives

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1394860B1 (it) 2009-07-22 2012-07-20 Kemotech S R L Composti farmaceutici
KR20180090290A (ko) 2015-12-04 2018-08-10 시애틀 지네틱스, 인크. 사차화 튜불리신 화합물들의 컨쥬게이트들
KR20200051733A (ko) * 2017-09-08 2020-05-13 시애틀 지네틱스, 인크. 튜불리신 및 그 중간물의 제조 공정

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008138561A1 (en) * 2007-05-10 2008-11-20 R & D Biopharmaceuticals Gmbh Tubulysine derivatives

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
AZA-MICHAEL REACTIONS OF 2-ENOYLTHIAZOLES SREEJITH SHANKAR P. 等: "Studies towards a Novel Synthesis of Tubulysins: Highly Asymmetric Aza-Michael Reactions of 2-Enoylthiazoles with Metalated Chiral Oxazolidinones", SYNLETT *
MONICA SANI 等: "Total Synthesis of Tubulysins U and V", ANGEW. CHEM. INT. ED., pages 8 - 9 *

Also Published As

Publication number Publication date
JP2021536475A (ja) 2021-12-27
JP7511543B2 (ja) 2024-07-05
IL281090A (en) 2021-04-29
MA53550A (fr) 2021-12-15
UA128730C2 (uk) 2024-10-09
WO2020051503A1 (en) 2020-03-12
TW202024043A (zh) 2020-07-01
TWI825169B (zh) 2023-12-11
CA3111149A1 (en) 2020-03-12
BR112021004317A2 (pt) 2021-05-25
SG11202102126VA (en) 2021-04-29
EA202190699A1 (ru) 2021-06-08
EP3847161A1 (en) 2021-07-14
US20230002440A1 (en) 2023-01-05
MX2021002570A (es) 2021-06-08
AU2019336231A1 (en) 2021-03-18
SA521421375B1 (ar) 2024-02-11
KR20210073525A (ko) 2021-06-18

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Application publication date: 20210618