[go: up one dir, main page]

EA202090670A1 - Способ получения тубулизинов и их промежуточных соединений - Google Patents

Способ получения тубулизинов и их промежуточных соединений

Info

Publication number
EA202090670A1
EA202090670A1 EA202090670A EA202090670A EA202090670A1 EA 202090670 A1 EA202090670 A1 EA 202090670A1 EA 202090670 A EA202090670 A EA 202090670A EA 202090670 A EA202090670 A EA 202090670A EA 202090670 A1 EA202090670 A1 EA 202090670A1
Authority
EA
Eurasian Patent Office
Prior art keywords
tubulisins
obtaining
intermediate compounds
compounds
tubulizin
Prior art date
Application number
EA202090670A
Other languages
English (en)
Inventor
Кунь-Лян У
Цинву Цзинь
Вендел Даблдэй
Original Assignee
Сиэтл Дженетикс, Инк.
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 Сиэтл Дженетикс, Инк. filed Critical Сиэтл Дженетикс, Инк.
Publication of EA202090670A1 publication Critical patent/EA202090670A1/ru

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/68—Medicinal 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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835—Medicinal 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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6851—Medicinal 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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/68—Medicinal 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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/68—Medicinal 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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • A61K47/6817—Toxins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/68—Medicinal 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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic 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
    • C07D277/32—Heterocyclic 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
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/021—Peptides 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Molecular Biology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Toxicology (AREA)
  • Cell Biology (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)
  • Medicinal Preparation (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

Настоящее изобретение относится к улучшенным способам получения соединений тубулизина, соединениям лекарственного линкера тубулизина и их промежуточным соединениям.
EA202090670A 2017-09-08 2018-09-07 Способ получения тубулизинов и их промежуточных соединений EA202090670A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762556234P 2017-09-08 2017-09-08
PCT/US2018/050095 WO2019051322A1 (en) 2017-09-08 2018-09-07 PROCESS FOR THE PREPARATION OF TUBULYSINS AND INTERMEDIATES THEREOF

Publications (1)

Publication Number Publication Date
EA202090670A1 true EA202090670A1 (ru) 2020-07-28

Family

ID=63963374

Family Applications (1)

Application Number Title Priority Date Filing Date
EA202090670A EA202090670A1 (ru) 2017-09-08 2018-09-07 Способ получения тубулизинов и их промежуточных соединений

Country Status (15)

Country Link
US (2) US11389543B2 (ru)
EP (1) EP3679036A1 (ru)
JP (2) JP2020533308A (ru)
KR (1) KR20200051733A (ru)
CN (1) CN111601803A (ru)
AU (1) AU2018329951B2 (ru)
BR (1) BR112020004495A2 (ru)
CA (1) CA3073766A1 (ru)
EA (1) EA202090670A1 (ru)
IL (1) IL272837B2 (ru)
MA (1) MA50124A (ru)
MX (1) MX2020001928A (ru)
SG (1) SG11202001543XA (ru)
TW (2) TW202428569A (ru)
WO (1) WO2019051322A1 (ru)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112020004495A2 (pt) * 2017-09-08 2020-09-08 Seattle Genetics, Inc. composto, composição, e, método para preparar uma composição.
CN112996778A (zh) * 2018-09-07 2021-06-18 西根公司 制备微管溶素及其中间体的替代方法
AU2022238571A1 (en) 2021-03-18 2023-09-14 Seagen Inc. Selective drug release from internalized conjugates of biologically active compounds

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10230872A1 (de) * 2002-07-09 2004-01-22 Morphochem AG Aktiengesellschaft für kombinatorische Chemie Verfahren zur Herstellung von substituierten Thiazol-2-ylmethylestern
ES2708763T3 (es) 2005-07-07 2019-04-11 Seattle Genetics Inc Compuestos de monometilvalina que tienen modificaciones de la cadena lateral de fenilalanina en el extremo C
SG172656A1 (en) 2006-05-30 2011-07-28 Genentech Inc Antibodies and immunoconjugates and uses therefor
CN109627287A (zh) 2007-02-23 2019-04-16 爱勒让治疗公司 三唑大环系统
US20100047841A1 (en) * 2007-02-27 2010-02-25 University Of Pittsburgh-Of The Commonwealth System Of Higher Education Synthesis of desacetoxytubulysin h and analogs thereof
BR112014022228A2 (pt) 2012-03-08 2017-07-11 Halozyme Inc anticorpos anti-epidérmicos de receptor de fator de crescimento condicionalmente ativo e métodos de uso dos mesmos
HK1207388A1 (en) 2012-05-15 2016-01-29 Seattle Genetics, Inc. Self-stabilizing linker conjugates
HK1208216A1 (en) 2012-05-15 2016-02-26 Concortis Biosystems, Corp Drug-conjugates, conjugation methods, and uses thereof
EP2708243A1 (en) 2012-09-17 2014-03-19 OntoChem GmbH Receptor ligand linked cytotoxic molecules
HK1220982A1 (zh) 2013-05-31 2017-05-19 基因泰克公司 抗壁磷壁酸抗體和綴合物
JP6506262B2 (ja) 2013-05-31 2019-04-24 ジェネンテック， インコーポレイテッド 抗細胞壁タイコ酸抗体及びコンジュゲート
SI3191502T1 (sl) * 2014-09-11 2021-10-29 Seagen Inc Ciljana dostava zdravilnih snovi, ki vsebujejo terciarne amine
JP6752204B2 (ja) * 2014-12-03 2020-09-09 ジェネンテック， インコーポレイテッド 四級アミン化合物及びその抗体−薬物コンジュゲート
CR20170438A (es) * 2015-02-25 2018-01-30 Univ Rice William M Desacetoxitubulisina h y análogos de esta
BR112020004495A2 (pt) * 2017-09-08 2020-09-08 Seattle Genetics, Inc. composto, composição, e, método para preparar uma composição.

Also Published As

Publication number Publication date
US20200297864A1 (en) 2020-09-24
AU2018329951B2 (en) 2023-12-14
TW202428569A (zh) 2024-07-16
EP3679036A1 (en) 2020-07-15
MX2020001928A (es) 2020-03-24
IL272837B2 (en) 2024-06-01
SG11202001543XA (en) 2020-03-30
CN111601803A (zh) 2020-08-28
CA3073766A1 (en) 2019-03-14
TW201920128A (zh) 2019-06-01
KR20200051733A (ko) 2020-05-13
US20220323601A1 (en) 2022-10-13
TWI820038B (zh) 2023-11-01
MA50124A (fr) 2020-07-15
BR112020004495A2 (pt) 2020-09-08
IL272837B1 (en) 2024-02-01
JP2020533308A (ja) 2020-11-19
JP2023053386A (ja) 2023-04-12
WO2019051322A1 (en) 2019-03-14
IL272837A (en) 2020-04-30
AU2018329951A1 (en) 2020-04-16
US11389543B2 (en) 2022-07-19

Similar Documents

Publication Publication Date Title
PH12018500034A1 (en) Bicyclic lactams and methods of use thereof
EA201892040A1 (ru) Способ получения пегилированных соединений лекарственный препарат - линкер и их промежуточных соединений
EA202092435A3 (ru) Моноклональные антитела против bcma
EA202091898A1 (ru) Антитела, нейтрализующие вирус иммунодефицита человека
EA201791867A1 (ru) Бициклические гетероциклы как ингибиторы fgfr4
EA201691541A1 (ru) Новые анти-baff антитела
EA202090720A1 (ru) ПРОИЗВОДНЫЕ GalNAc
EA201690372A1 (ru) Азапиридоновые соединения и их применение
EA201892430A1 (ru) Синтез индазолов
EA201890185A1 (ru) Способы лечения опосредованных гепсидином нарушений
CY1121602T1 (el) Συνθεση της κοπανλισιμπης και του διυδροχλωρικου αλατος της
PH12019501359A1 (en) Polymorphs
MX393879B (es) Métodos de preparación de niraparib.
MX389724B (es) Compuestos de fenil-2-hidroxi-acetilamino-2-metil-fenilo
EA201790570A1 (ru) Модуляторы р2х7
EA201790982A1 (ru) Синтез копанлисиба и его дигидрохлорида
MX394645B (es) Compuestos heteroaromáticos como inhibidores de vanina.
JOP20220119A1 (ar) أجسام مضادة trem2 واستخداماتها
EA201692034A1 (ru) Новые макроциклические соединения
EA202091259A1 (ru) Способ получения опикапона и его интермедиатов
MX2018007219A (es) Metodos para preparacion de compuestos heterociclicos de 1,3-benzodioxol.
BR112016029510A2 (pt) métodos para a preparação de um composto, e, composto intermediário.
EA201791249A1 (ru) Получаемые из cd44v6 циклические пептиды для лечения злокачественных опухолей и связанных с ангиогенезом заболеваний
EA201691632A1 (ru) Пиразины в качестве модуляторов gpr6
EA201792262A1 (ru) Пироглутамат вортиоксетина