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MX375928B - Conjugado anticuerpo anti-trop2-farmaco. - Google Patents

Conjugado anticuerpo anti-trop2-farmaco.

Info

Publication number
MX375928B
MX375928B MX2016008192A MX2016008192A MX375928B MX 375928 B MX375928 B MX 375928B MX 2016008192 A MX2016008192 A MX 2016008192A MX 2016008192 A MX2016008192 A MX 2016008192A MX 375928 B MX375928 B MX 375928B
Authority
MX
Mexico
Prior art keywords
sup
sub
trop2 antibody
drug conjugate
antitumor
Prior art date
Application number
MX2016008192A
Other languages
English (en)
Other versions
MX2016008192A (es
Inventor
Daisuke Okajima
Hirofumi Hamada
Jun Hasegawa
Miki Yamaguchi
Shu Takahashi
Toshinori Agatsuma
Original Assignee
Daiichi Sankyo Co Ltd
Univ Sapporo Medical
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=53477995&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=MX375928(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Daiichi Sankyo Co Ltd, Univ Sapporo Medical filed Critical Daiichi Sankyo Co Ltd
Publication of MX2016008192A publication Critical patent/MX2016008192A/es
Publication of MX375928B publication Critical patent/MX375928B/es

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    • 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
    • A61K47/68Medicinal 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
    • A61K47/6889Conjugates 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
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
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    • A61K47/68Medicinal 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
    • A61K47/6835Medicinal 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
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    • A61K47/6857Medicinal 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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Abstract

El propósito de la presente invención es proporcionar un fármaco antitumoral que es sobresaliente en efecto antitumoral y en seguridad, y que tiene un excelente efecto terapéutico. Se proporciona un conjugado anticuerpo- fármaco caracterizado porque un compuesto antitumoral representado por una fórmula y el anticuerpo anti-TROP2 son enlazados vía un ligador que tiene una estructura representada por la fórmula -L1-L2-LP-NH- (CH2) n1-La- (CH2) n2-C(=O)- (en donde el anticuerpo anti-TROP2 se enlaza con el extremo L1 y el compuesto antitumoral con el grupo carbonilo de la porción -(CH2) n2-C(=O)- utilizando el átomo de nitrógeno del grupo amino en la posición 1 como el sitio de enlace).
MX2016008192A 2013-12-25 2014-12-24 Conjugado anticuerpo anti-trop2-farmaco. MX375928B (es)

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PH12020551943A1 (en) 2021-06-07
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