CA2918139A1 - 1-(chloromethyl)-2,3-dihydro-1h-benzo[e]indole dimer antibody-drug conjugate compounds, and methods of use and treatment - Google Patents

1-(chloromethyl)-2,3-dihydro-1h-benzo[e]indole dimer antibody-drug conjugate compounds, and methods of use and treatment Download PDF

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Publication number
CA2918139A1
CA2918139A1 CA2918139A CA2918139A CA2918139A1 CA 2918139 A1 CA2918139 A1 CA 2918139A1 CA 2918139 A CA2918139 A CA 2918139A CA 2918139 A CA2918139 A CA 2918139A CA 2918139 A1 CA2918139 A1 CA 2918139A1
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Prior art keywords
antibody
alkylene
hvr
seq
drug conjugate
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Abandoned
Application number
CA2918139A
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English (en)
French (fr)
Inventor
John A. Flygare
Thomas H. PILLOW
Brian Safina
Vishal Verma
Binqing Wei
William Denny
Anna GIDDENS
Ho Lee
Guo-Liang Lu
Christian Miller
Gordon Rewcastle
Moana Tercel
Muriel Bonnet
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Genentech Inc
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Genentech Inc
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Publication of CA2918139A1 publication Critical patent/CA2918139A1/en
Abandoned legal-status Critical Current

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    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052—Val-amino acid
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    • 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
    • A61K47/54—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 compound
    • A61K47/55—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 compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
    • A—HUMAN NECESSITIES
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    • 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
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    • 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
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    • A61K47/6849—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 receptor, a cell surface antigen or a cell surface determinant
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    • 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
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    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
    • C07D207/36—Oxygen or sulfur atoms
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    • C07K16/32—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products of oncogenes

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  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
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CA2918139A 2013-08-12 2014-06-16 1-(chloromethyl)-2,3-dihydro-1h-benzo[e]indole dimer antibody-drug conjugate compounds, and methods of use and treatment Abandoned CA2918139A1 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201361864889P 2013-08-12 2013-08-12
US61/864,889 2013-08-12
US201361916388P 2013-12-16 2013-12-16
US61/916,388 2013-12-16
US201461969499P 2014-03-24 2014-03-24
US61/969,499 2014-03-24
PCT/US2014/042560 WO2015023355A1 (en) 2013-08-12 2014-06-16 1-(chloromethyl)-2,3-dihydro-1h-benzo[e]indole dimer antibody-drug conjugate compounds, and methods of use and treatment

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CA2918139A1 true CA2918139A1 (en) 2015-02-19

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US (1) US10442836B2 (enExample)
EP (1) EP3033111B1 (enExample)
JP (2) JP6993084B2 (enExample)
KR (1) KR20160042080A (enExample)
CN (1) CN105636612B (enExample)
AU (1) AU2014307080B2 (enExample)
BR (1) BR112016002829A2 (enExample)
CA (1) CA2918139A1 (enExample)
CL (1) CL2016000318A1 (enExample)
CR (1) CR20160125A (enExample)
EA (1) EA201690195A1 (enExample)
IL (1) IL243586A0 (enExample)
MX (1) MX2016001862A (enExample)
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EP3539982B1 (en) 2011-12-23 2025-02-19 Pfizer Inc. Engineered antibody constant regions for site-specific conjugation and methods and uses therefor
AR098743A1 (es) 2013-12-13 2016-06-08 Genentech Inc Anticuerpos e inmunoconjugados anti-cd33
UA118113C2 (uk) 2013-12-16 2018-11-26 Дженентек, Інк. Пептидоміметичні сполуки та їх кон'югати антитіла з лікарським засобом
BR112016014126B1 (pt) 2013-12-16 2023-02-14 Medimmune Limited Composto não-peptídico, conjugados de anticorpo-fármaco do mesmo, uso dos ditos conjugados para o tratamento de câncer e composição farmacêutica que compreende os mesmos
JP6980384B2 (ja) * 2013-12-16 2021-12-15 ジェネンテック， インコーポレイテッド １−（クロロメチル）−２，３−ジヒドロ−１ｈ−ベンゾ［ｅ］インドール二量体抗体−薬物コンジュゲート化合物、並びに使用及び処置の方法
SG11201605437YA (en) * 2014-01-27 2016-08-30 Pfizer Bifunctional cytotoxic agents
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