SG11202001543XA - Process for the preparation of tubulysins and intermediates thereof - Google Patents

Process for the preparation of tubulysins and intermediates thereof

Info

Publication number
SG11202001543XA
SG11202001543XA SG11202001543XA SG11202001543XA SG11202001543XA SG 11202001543X A SG11202001543X A SG 11202001543XA SG 11202001543X A SG11202001543X A SG 11202001543XA SG 11202001543X A SG11202001543X A SG 11202001543XA SG 11202001543X A SG11202001543X A SG 11202001543XA
Authority
SG
Singapore
Prior art keywords
tubulysins
intermediates
preparation
Prior art date
Application number
SG11202001543XA
Inventor
Kun-Liang Wu
Qingwu Jin
Wendel Doubleday
Original Assignee
Seattle Genetics 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 Seattle Genetics Inc filed Critical Seattle Genetics Inc
Publication of SG11202001543XA publication Critical patent/SG11202001543XA/en

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
    • 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
    • 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
    • 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
SG11202001543XA 2017-09-08 2018-09-07 Process for the preparation of tubulysins and intermediates thereof SG11202001543XA (en)

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
SG11202001543XA true SG11202001543XA (en) 2020-03-30

Family

ID=63963374

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11202001543XA SG11202001543XA (en) 2017-09-08 2018-09-07 Process for the preparation of tubulysins and intermediates thereof

Country Status (15)

Country Link
US (2) US11389543B2 (en)
EP (1) EP3679036A1 (en)
JP (2) JP2020533308A (en)
KR (1) KR20200051733A (en)
CN (1) CN111601803A (en)
AU (1) AU2018329951B2 (en)
BR (1) BR112020004495A2 (en)
CA (1) CA3073766A1 (en)
EA (1) EA202090670A1 (en)
IL (1) IL272837B1 (en)
MA (1) MA50124A (en)
MX (1) MX2020001928A (en)
SG (1) SG11202001543XA (en)
TW (1) TWI820038B (en)
WO (1) WO2019051322A1 (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3847161A1 (en) * 2018-09-07 2021-07-14 Seagen Inc. Alternative processes for the preparation of tubulysins and intermediates thereof

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10230872A1 (en) 2002-07-09 2004-01-22 Morphochem AG Aktiengesellschaft für kombinatorische Chemie Process for the preparation of substituted thiazol-2-ylmethyl esters
CA2614436C (en) 2005-07-07 2016-05-17 Seattle Genetics, Inc. Monomethylvaline compounds having phenylalanine side-chain modifications at the c-terminus
AR060978A1 (en) 2006-05-30 2008-07-23 Genentech Inc ANTIBODIES AND IMMUNOCATE PLAYERS AND THEIR USES
WO2008104000A2 (en) 2007-02-23 2008-08-28 Aileron Therapeutics, Inc. Triazole macrocycle systems
WO2008106080A2 (en) * 2007-02-27 2008-09-04 University Of Pittsburgh - Of The Commonwealth System Of Higher Education Synthesis of desacetoxytubulysin h and analogs thereof
EP3296320A1 (en) 2012-03-08 2018-03-21 Halozyme, Inc. Conditionally active anti-epidermal growth factor receptor antibodies and methods of use thereof
KR102433686B1 (en) 2012-05-15 2022-08-19 씨젠 인크. Self-stabilizing linker conjugates
US9981046B2 (en) 2012-05-15 2018-05-29 Concortis Biosystems, Corp., a wholly owned Subsidiary of Sorrento Therapeutics, Inc. Drug-conjugates, conjugation methods, and uses thereof
EP2708243A1 (en) * 2012-09-17 2014-03-19 OntoChem GmbH Receptor ligand linked cytotoxic molecules
RU2687044C2 (en) 2013-05-31 2019-05-06 Дженентек, Инк. Antibodies against teichoic acid conjugate and their conjugates
MX369022B (en) 2013-05-31 2019-10-25 Genentech Inc Anti-wall teichoic antibodies and conjugates.
PL3191502T3 (en) * 2014-09-11 2021-11-08 Seagen Inc. Targeted delivery of tertiary amine-containing drug substances
EP3226909A1 (en) * 2014-12-03 2017-10-11 Genentech, Inc. Quaternary amine compounds and antibody-drug conjugates thereof
EP3261443B1 (en) * 2015-02-25 2021-04-28 William Marsh Rice University Desacetoxytubulysin h and analogs thereof

Also Published As

Publication number Publication date
US11389543B2 (en) 2022-07-19
AU2018329951B2 (en) 2023-12-14
MA50124A (en) 2020-07-15
TW201920128A (en) 2019-06-01
US20220323601A1 (en) 2022-10-13
EA202090670A1 (en) 2020-07-28
TWI820038B (en) 2023-11-01
IL272837B1 (en) 2024-02-01
WO2019051322A1 (en) 2019-03-14
IL272837A (en) 2020-04-30
CN111601803A (en) 2020-08-28
EP3679036A1 (en) 2020-07-15
KR20200051733A (en) 2020-05-13
AU2018329951A1 (en) 2020-04-16
JP2020533308A (en) 2020-11-19
MX2020001928A (en) 2020-03-24
CA3073766A1 (en) 2019-03-14
JP2023053386A (en) 2023-04-12
BR112020004495A2 (en) 2020-09-08
US20200297864A1 (en) 2020-09-24

Similar Documents

Publication Publication Date Title
IL276917A (en) Process for the preparation of elobixibat
SI3380530T1 (en) An improved process for the preparation of sugammadex and its intermediates
IL287140A (en) Process for the preparation of pegylated drug-linkers and intermediates thereof
IL292648A (en) Process for the preparation of glucuronide drug-linkers and intermediates thereof
ZA202003590B (en) Process for the preparation of opicapone and intermediates thereof
PT3458467T (en) Process and intermediates for the 6,7-alpha-epoxidation of steroid 4,6-dienes
ZA202101214B (en) Process and intermediates for the preparation of bilastine
HUE062956T2 (en) Processes for the preparation of niraparib and intermediates thereof
EP3717456A4 (en) Process for the preparation of roxadustat and its intermediates
IL275655A (en) Process for the preparation of an amino-pyrimidine and intermediates thereof
HUE063118T2 (en) Process for the preparation of n-alkyl-nitratoethylnitramines
IL281254A (en) Process for the preparation of lenvatinib
HUE058259T2 (en) Process for the preparation of lubiprostone and intermediates thereof
PL3737685T3 (en) Process for the preparation of crisaborole and its intermediates
IL255819A (en) Improved processes for the preparation of sofosbuvir and intermediates thereof
IL272837A (en) Process for the preparation of tubulysins and intermediates thereof
IL253077A0 (en) Process and intermediates for the preparation of perampanel
IL237572A0 (en) Process and intermediates for the preparation of dasatinib
EP3877361C0 (en) Process for the preparation of arylsulfonylpropenenitriles
PL3599256T3 (en) Process for the preparation of polyorganosiloaxnes
HUE055367T2 (en) Process and new intermediates for the preparation of 11-methylene steroids
IL281090A (en) Alternative processes for the preparation of tubulysins and intermediates thereof
FI4073051T3 (en) Process and intermediate for the preparation of oxetan-2-ylmethanamine
HUP1800278A2 (en) Process for the preparation of boc-linagliptin
HUP1500451A2 (en) Processes for the preparation of 1,4,7-triaza-cyclononane derivatives and intermediates