SG11202008186RA - Chemoselective thiol-conjugation with alkene or alkyne-phosphonothiolates and -phosphonates - Google Patents

Chemoselective thiol-conjugation with alkene or alkyne-phosphonothiolates and -phosphonates

Info

Publication number
SG11202008186RA
SG11202008186RA SG11202008186RA SG11202008186RA SG11202008186RA SG 11202008186R A SG11202008186R A SG 11202008186RA SG 11202008186R A SG11202008186R A SG 11202008186RA SG 11202008186R A SG11202008186R A SG 11202008186RA SG 11202008186R A SG11202008186R A SG 11202008186RA
Authority
SG
Singapore
Prior art keywords
phosphonothiolates
alkyne
phosphonates
conjugation
alkene
Prior art date
Application number
SG11202008186RA
Other languages
English (en)
Inventor
Christian Hackenberger
Alice Leonie Baumann
Marc-André Kasper
Stephen Byrne
Jonas Helma-Smets
Heinrich Leonhardt
Tina Stoscheck
Marcus Gerlach
Dominik Schumacher
Original Assignee
Forschungsverbund Berlin Ev
Univ Muenchen Ludwig Maximilians
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 Forschungsverbund Berlin Ev, Univ Muenchen Ludwig Maximilians filed Critical Forschungsverbund Berlin Ev
Publication of SG11202008186RA publication Critical patent/SG11202008186RA/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
    • A61K47/6801—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C07F9/4071—Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
    • 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
    • A61K47/68031—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being an auristatin
    • 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
    • A61K47/6849—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
    • 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
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4015—Esters of acyclic unsaturated acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/76—Albumins
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2863—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against receptors for growth factors, growth regulators
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2878—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the NGF-receptor/TNF-receptor superfamily, e.g. CD27, CD30, CD40, CD95
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/42—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against immunoglobulins

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Cell Biology (AREA)
  • Toxicology (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Saccharide Compounds (AREA)
  • Polysaccharides And Polysaccharide Derivatives (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
SG11202008186RA 2018-03-07 2019-03-06 Chemoselective thiol-conjugation with alkene or alkyne-phosphonothiolates and -phosphonates SG11202008186RA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP18160384 2018-03-07
PCT/EP2019/055509 WO2019170710A2 (fr) 2018-03-07 2019-03-06 Conjugaison chimiosélective d'un thiol avec des alcène- ou alcyne-phosphonothiolates et -phosphonates

Publications (1)

Publication Number Publication Date
SG11202008186RA true SG11202008186RA (en) 2020-09-29

Family

ID=61691626

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11202008186RA SG11202008186RA (en) 2018-03-07 2019-03-06 Chemoselective thiol-conjugation with alkene or alkyne-phosphonothiolates and -phosphonates

Country Status (12)

Country Link
US (1) US20200390901A1 (fr)
EP (1) EP3762423A2 (fr)
JP (1) JP7429191B2 (fr)
KR (1) KR20200138750A (fr)
CN (1) CN112088168A (fr)
AU (1) AU2019232602A1 (fr)
BR (1) BR112020018093A2 (fr)
CA (1) CA3092286A1 (fr)
IL (1) IL276981B2 (fr)
RU (1) RU2020128767A (fr)
SG (1) SG11202008186RA (fr)
WO (1) WO2019170710A2 (fr)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4297794A2 (fr) 2021-02-26 2024-01-03 Forschungsverbund Berlin E.V. Absorption cellulaire de grandes biomolécules permise par des additifs peptidiques de pénétration cellulaire réactifs à la surface cellulaire
CN117545511A (zh) 2021-04-23 2024-02-09 柏林合作研究学会 与不饱和磷(v)化合物的硫醇偶联
AU2022385379A1 (en) 2021-11-09 2024-06-20 Forschungsverbund Berlin E.V. Conjugates comprising a phosphorus (v) and a drug moiety
KR20240100415A (ko) 2021-11-09 2024-07-01 투불리스 게엠베하 인(v) 및 캄프토테신 모이어티를 포함하는 접합체
WO2024003002A1 (fr) 2022-06-27 2024-01-04 Diaccurate Dérivés d'indoles n-substitués et conjugués pour le traitement du cancer
WO2024083953A1 (fr) 2022-10-18 2024-04-25 Tubulis Gmbh Nouvel anticorps anti-tpbg et conjugués anticorps-médicament basés sur celui-ci, procédés thérapeutiques et utilisations dudit anticorps
US20240190958A1 (en) 2022-10-18 2024-06-13 Tubulis Gmbh Novel antibody drug conjugates with novel napi2b antibodies, therapeutic methods and uses thereof
WO2024133845A1 (fr) 2022-12-22 2024-06-27 Tubulis Gmbh Conjugués comprenant une fraction phosphore (v) et un médicament

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2535174A (en) 1949-04-07 1950-12-26 Us Rubber Co Mercaptoethanephosphonates
CH410942A (de) 1957-06-05 1966-04-15 Bayer Ag Verfahren zur Herstellung von Phosphonsäurethiolestern
DE1064512B (de) 1958-03-26 1959-09-03 Bayer Ag Verfahren zur Herstellung von beta-Alkylmercaptovinylphosphon-saeurethiolestern
DE1072245B (de) * 1957-06-24 1959-12-31 Farbenfabriken Bayer Aktiengesellschaft, Leverkusen-Bayerwerk Verfahren zur Herstellung von Phosphonsäure-O-alkyl-thiolestern
US3223754A (en) * 1959-12-04 1965-12-14 Bayer Ag Alkyl mercapto alkyl esters of substituted phosphonic acids
US3121662A (en) * 1960-03-09 1964-02-18 Bayer Ag (thiono)-thiolphosphonic and-thiolphosphinic acid esters and a process for their production
NL262130A (fr) * 1960-03-09
GB917085A (en) 1960-12-08 1963-01-30 Bayer Ag Phosphonic and thiophosphonic acid esters
US3904710A (en) 1971-08-19 1975-09-09 Exxon Research Engineering Co Pesticidal O,S{40 -dialkyl S-phenylthioalkyl dithiophosphates and preparation thereof
EP0859841B1 (fr) 1995-08-18 2002-06-19 MorphoSys AG Banques de proteines/(poly)peptides
DK1545613T3 (da) 2002-07-31 2011-11-14 Seattle Genetics Inc Auristatinkonjugater og deres anvendelse til behandling af cancer, en autoimmun sygdom eller en infektiøs sygdom
JP5388856B2 (ja) * 2007-10-18 2014-01-15 片山化学工業株式会社 含リン化合物と含イオウ化合物の触媒
RU2625756C2 (ru) 2011-03-11 2017-07-18 В.Л. Гор Энд Ассошиейтс, Инк. Усовершенствованные иммобилизованные биологические объекты
WO2015169784A1 (fr) 2014-05-09 2015-11-12 Bayer Pharma Aktiengesellschaft Procédé de conjugaison ciblée de peptides et de protéines par pontage c2 par paires d'acides aminés cystéine
JP7217225B2 (ja) * 2016-09-01 2023-02-02 フォルシュングスフェアバント ベルリン エー．ベー． アルケンホスホンアミデートまたはアルキンホスホンアミデートとの化学選択的チオールコンジュゲーション

Also Published As

Publication number Publication date
WO2019170710A3 (fr) 2019-10-24
IL276981B1 (en) 2023-12-01
WO2019170710A2 (fr) 2019-09-12
AU2019232602A1 (en) 2020-09-17
IL276981A (en) 2020-10-29
JP7429191B2 (ja) 2024-02-07
IL276981B2 (en) 2024-04-01
CN112088168A (zh) 2020-12-15
RU2020128767A (ru) 2022-04-07
JP2021516959A (ja) 2021-07-15
BR112020018093A2 (pt) 2020-12-22
US20200390901A1 (en) 2020-12-17
EP3762423A2 (fr) 2021-01-13
CA3092286A1 (fr) 2019-09-12
KR20200138750A (ko) 2020-12-10

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