SG10201805160UA - Methylene carbamate linkers for use with targeted-drug conjugates - Google Patents

Methylene carbamate linkers for use with targeted-drug conjugates

Info

Publication number
SG10201805160UA
SG10201805160UA SG10201805160UA SG10201805160UA SG10201805160UA SG 10201805160U A SG10201805160U A SG 10201805160UA SG 10201805160U A SG10201805160U A SG 10201805160UA SG 10201805160U A SG10201805160U A SG 10201805160UA SG 10201805160U A SG10201805160U A SG 10201805160UA
Authority
SG
Singapore
Prior art keywords
drug
ligand
drug conjugates
targeted
methylene carbamate
Prior art date
Application number
SG10201805160UA
Inventor
Robert Kolakowski
Scott Jeffrey
Patrick Burke
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
Priority claimed from TW103144705A external-priority patent/TWI727919B/en
Publication of SG10201805160UA publication Critical patent/SG10201805160UA/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
    • A61K47/6889—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
    • 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
    • A61K47/56—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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • 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
    • 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
    • A61K47/6863—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 the tumour determinant being from stomach or intestines cancer cell
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection

Abstract

METHYLENECARBAMATE LINKERS FOR USE WITH TARGETED-DRUG CONJUGATES The present invention provides Ligand-Drug Conjugates and Drug-Linker Compounds comprising a methylene carbamate unit. The invention provides inter alia, Ligand-Drug Conjugates, wherein the Ligand-Drug Conjugate is comprised of a Self-immolative Assembly Unit having a methylene carbamate unit for conjugation of a drug to a targeting ligand, methods of preparing and using them, and intermediates thereof. The Ligand-Drug Conjugates of the present invention are stable in circulation, yet capable of inflicting cell death once free drug is released from a Conjugate in the vicinity or within tumor cells. Fig. 217
SG10201805160UA 2013-12-19 2014-12-19 Methylene carbamate linkers for use with targeted-drug conjugates SG10201805160UA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361918539P 2013-12-19 2013-12-19
TW103144705A TWI727919B (en) 2013-12-19 2014-12-19 Methylene carbamate linkers for use with targeted-drug conjugates

Publications (1)

Publication Number Publication Date
SG10201805160UA true SG10201805160UA (en) 2018-08-30

Family

ID=60450373

Family Applications (4)

Application Number Title Priority Date Filing Date
SG10201708878YA SG10201708878YA (en) 2013-12-19 2014-12-19 Methylene carbamate linkers for use with targeted-drug conjugates
SG10201708812YA SG10201708812YA (en) 2013-12-19 2014-12-19 Methylene carbamate linkers for use with targeted-drug conjugates
SG10201708839VA SG10201708839VA (en) 2013-12-19 2014-12-19 Methylene carbamate linkers for use with targeted drug conjugates
SG10201805160UA SG10201805160UA (en) 2013-12-19 2014-12-19 Methylene carbamate linkers for use with targeted-drug conjugates

Family Applications Before (3)

Application Number Title Priority Date Filing Date
SG10201708878YA SG10201708878YA (en) 2013-12-19 2014-12-19 Methylene carbamate linkers for use with targeted-drug conjugates
SG10201708812YA SG10201708812YA (en) 2013-12-19 2014-12-19 Methylene carbamate linkers for use with targeted-drug conjugates
SG10201708839VA SG10201708839VA (en) 2013-12-19 2014-12-19 Methylene carbamate linkers for use with targeted drug conjugates

Country Status (2)

Country Link
EA (1) EA039120B1 (en)
SG (4) SG10201708878YA (en)

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1718667B1 (en) * 2004-02-23 2013-01-09 Genentech, Inc. Heterocyclic self-immolative linkers and conjugates
US20080280937A1 (en) * 2005-08-19 2008-11-13 Christopher Paul Leamon Ligand Conjugates of Vinca Alkaloids, Analogs, and Derivatives
US20110152252A1 (en) * 2007-12-18 2011-06-23 Institut Curie Shiga toxin b-subunit/chemotherapeutics conjugates
US8754190B2 (en) * 2010-05-05 2014-06-17 Prolynx Llc Controlled release from macromolecular conjugates

Also Published As

Publication number Publication date
SG10201708878YA (en) 2017-11-29
SG10201708812YA (en) 2017-12-28
EA201691275A1 (en) 2016-10-31
SG10201708839VA (en) 2017-11-29
EA039120B1 (en) 2021-12-07

Similar Documents

Publication Publication Date Title
ZA202004099B (en) Methylene carbamate linkers for use with targeted-drug conjugates
NZ741261A (en) Pyrrolobenzodiazepine antibody drug conjugates and methods of use
NZ758047A (en) Pegylated drug-linkers for improved ligand-drug conjugate pharmacokinetics
CL2019002858A1 (en) Conjugation of a bis-linked cytotoxic drug.
PH12015501422B1 (en) Hydrophilic self-immolative linkers and conjugates thereof
MX2017003886A (en) Radiopharmaceutical conjugate of a metabolite and an epr agent, for targeting tumour cells.
CY1119616T1 (en) HUMAN ANTI-DUMP DRUG CONSUMPTION AGAINST TISSUE
MX2013005046A (en) Cytotoxic agents comprising new ansamitocin derivatives.
MX2017003246A (en) Macropinocytosing human anti-cd46 antibodies and targeted cancer therapeutics.
NZ720743A (en) Peptidomimetic compounds and antibody-drug conjugates thereof
BR112019008854A2 (en) peptide-containing ligands for antibody-drug conjugates
PH12016501995A1 (en) Tubulysin derivatives
BR112015023333A8 (en) pyrrolbenzodiazepines and conjugates thereof
NZ717003A (en) Novel cytotoxic agents for conjugation of drugs to cell binding molecule
MX344010B (en) Amatoxin-conjugates with improved linkers.
SG10201811124YA (en) Her2 antibody-drug conjugates
MX2019001302A (en) Drug conjugates with self-stabilizing linkers having improved physiochemical properties.
GB2538023A (en) Targeted drug conjugates
WO2017210246A3 (en) Penicillamine conjugates and particles and formulations thereof
EA201690051A1 (en) POLYCONJUGATES FOR DELIVERY OF RNA TRIGGERS INTERFERENCE IN TUMOR IN VIVO CELLS
MX2019004963A (en) Sstr-targeted conjugates and particles and formulations thereof.
WO2014134457A3 (en) Conjugates comprising cell-binding agents and cytotoxic agents
PH12016501185A1 (en) Compounds to fibrolast growth factor receptor-3 (fgfr3) and therapeutic uses
MX2015015434A (en) Targeting corroles for tumor toxicity and mri.
PH12017502392A1 (en) Targeted conjugates and particles and formulations thereof