PE20211473A1 - Conjugados de anticuerpo-farmaco de herboxidieno y metodos de uso - Google Patents

Conjugados de anticuerpo-farmaco de herboxidieno y metodos de uso

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Publication number
PE20211473A1
PE20211473A1 PE2021000860A PE2021000860A PE20211473A1 PE 20211473 A1 PE20211473 A1 PE 20211473A1 PE 2021000860 A PE2021000860 A PE 2021000860A PE 2021000860 A PE2021000860 A PE 2021000860A PE 20211473 A1 PE20211473 A1 PE 20211473A1
Authority
PE
Peru
Prior art keywords
alkyl
antibody
hydroxyl
herboxidiene
methods
Prior art date
Application number
PE2021000860A
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English (en)
Inventor
Nathan Fishkin
Thiwanka Samarakoon
James Palacino
Kenzo Arai
Yoshihiko Kotake
Shinya Okubo
Norio Murai
Masayuki Miyano
Original Assignee
Eisai Randd Man Co Ltd
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 Eisai Randd Man Co Ltd filed Critical Eisai Randd Man Co Ltd
Publication of PE20211473A1 publication Critical patent/PE20211473A1/es

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    • 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
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    • 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
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/0005—Vertebrate antigens
    • A61K39/0011—Cancer antigens
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    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/39558—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against tumor tissues, cells, antigens
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    • 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
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    • A61K47/6855—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 breast cancer cell
    • A—HUMAN NECESSITIES
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    • 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
    • A61K47/6857—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 lung cancer cell
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
    • A61K47/6867—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 a cell of a blood cancer
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    • A61K47/6869—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 a cell of the reproductive system: ovaria, uterus, testes, prostate
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    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/04—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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Abstract

Referida a un conjugado anticuerpo-farmaco de formula (I): Ab-(L-H)p (I) en donde: Ab es un anticuerpo o fragmento de union a antigeno que se dirige a una celula neoplasica; H es un modulador de empalme de herboxidieno; L es un ligador que une covalentemente Ab a H; y p es un numero entero de 1 a 15. El modulador de empalme de herboxidieno comprende un compuesto de Formula (I), donde: Y es O, S, entre otros; R1 , R2 , y R3 son hidrogeno, hidroxilo, -O-(alquilo C1-C6), entre otros; R4 es alquilo C1-C6, -C(= O)-(alquilo C1-C6), entre otros; R5 es hidrogeno, hidroxilo, -CH2-OH,-CO2H,-C(=O)-O- (alquilo C1-C6), entre otros; R1, R2, R3, R4 y R5 estan cada uno independientemente sustituidos con 0 a 3 grupos elegidos independientemente entre halogenos, hidroxilo, grupos alquilo C1-C6, grupos -O-(alquilo C1-C6), entre otros. Dichos conjugados son utiles en el tratamiento de trastornos neoplasicos
PE2021000860A 2018-12-13 2019-12-12 Conjugados de anticuerpo-farmaco de herboxidieno y metodos de uso PE20211473A1 (es)

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US201862779400P 2018-12-13 2018-12-13
US201862779406P 2018-12-13 2018-12-13
US201962941220P 2019-11-27 2019-11-27
PCT/US2019/066029 WO2020123836A2 (en) 2018-12-13 2019-12-12 Herboxidiene splicing modulator antibody-drug conjugates and methods of use

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JP2023500875A (ja) 2019-11-07 2023-01-11 エーザイ・アール・アンド・ディー・マネジメント株式会社 抗メソテリンエリブリン抗体－薬物コンジュゲート及び使用方法
CA3199753A1 (en) 2020-11-04 2022-05-12 Eisai R&D Management Co., Ltd. Biomarkers for myelodysplastic syndrome (mds) and methods of using the same
WO2023131866A1 (en) 2022-01-05 2023-07-13 Eisai R&D Management Co., Ltd. Biomarkers for myelodysplastic syndrome (mds) and methods of using the same
WO2023225320A1 (en) * 2022-05-20 2023-11-23 Novartis Ag Epha2 bcl-xl inhibitor antibody-drug conjugates and methods of use thereof

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