PE20140784A1 - Composiciones que contienen, metodos que involucran, y usos de derivados de dolastatina unidos a aminoacidos no naturales - Google Patents

Composiciones que contienen, metodos que involucran, y usos de derivados de dolastatina unidos a aminoacidos no naturales

Info

Publication number
PE20140784A1
PE20140784A1 PE2013002721A PE2013002721A PE20140784A1 PE 20140784 A1 PE20140784 A1 PE 20140784A1 PE 2013002721 A PE2013002721 A PE 2013002721A PE 2013002721 A PE2013002721 A PE 2013002721A PE 20140784 A1 PE20140784 A1 PE 20140784A1
Authority
PE
Peru
Prior art keywords
dolastatin
formula
amino acids
alkyl
natural amino
Prior art date
Application number
PE2013002721A
Other languages
English (en)
Inventor
Zhenwei Miao
Kyle Atkinson
Sandra Biroc
Timothy Buss
Melissa Neal
Vadim Kraynov
Robin Marsden
Jason Pinkstaff
Lillian Skidmore
Ying Sun
Agnieszka Szydlik
De Valenta Delia Ianina Lopez
Original Assignee
Ambrx 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=47259774&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20140784(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Ambrx Inc filed Critical Ambrx Inc
Publication of PE20140784A1 publication Critical patent/PE20140784A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/101—Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/07—Tetrapeptides
    • 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
    • A61K47/6801—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
    • A61K47/6801—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
    • A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • A61K47/6817—Toxins
    • 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
    • A61K47/6835—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
    • A61K47/6855—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
    • 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
    • A61K47/6861—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 kidney or bladder 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • 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
    • C07D207/04—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 no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—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 no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07K16/2866—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 cytokines, lymphokines, interferons
    • 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
    • C07K16/32—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products of oncogenes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0205—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)3-C(=0)-, e.g. statine or derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02—Linear peptides containing at least one abnormal peptide link
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07K5/06043—Leu-amino acid

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Cell Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Oncology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Toxicology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Compression Of Band Width Or Redundancy In Fax (AREA)
  • Polyamides (AREA)

Abstract

SE REFIERE A DERIVADOS DE DOLASTATINA DE FORMULA (I) DONDE Z ES DE FORMULA -CH(R5)-CR6(Ar)-, EN DONDE R5 ES H, ALQUILO(C1-C6), TIAZOL, ENTRE OTROS; R6 ES OH O H; Ar ES FENILO O PIRIDINA; R7 ES H O ALQUILO(C1-C6); Y ES HIDROXILAMINA, METILO, CETONA, AZIDA, ENTRE OTROS; L ES UN ENLAZADOR TAL COMO ALQUILENO, ALQUILENO-C(O)-, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA Y A UN METODO PARA DERIVATIZAR ANALOGOS DE DOLASTATINA DE FORMULA (I) PARA OBTENER DERIVADOS DE DOLASTATINA UNIDOS A AMINOACIDOS NO NATURALES, EL CUAL COMPRENDE PONER EN CONTACTO EL ANALOGO DE DOLASTATINA CON UN REACTIVO DE FORMULA (XXXVII) EN CONDICIONES LIGERAMENTE ACIDAS DONDE A ES ALQUILENO INFERIOR, ARILENO, ENTRE OTROS; B ES ALQUILENO INFERIOR, -O-, -S-, ENTRE OTROS; K ES CO, CS, CO-CO, ENTRE OTROS; R ES H, ALQUILO, CICLOALQUILO, ENTRE OTROS; R1 ES H, UN AMINOACIDO, UN POLINUCLEOTIDO, ENTRE OTROS; R2 ES OH, RESINA, UN AMINOACIDO, ENTRE OTROS; R3 Y R4 SON CADA UNO H, HALOGENO, ALQUILO INFERIOR, ENTRE OTROS
PE2013002721A 2011-05-27 2012-05-24 Composiciones que contienen, metodos que involucran, y usos de derivados de dolastatina unidos a aminoacidos no naturales PE20140784A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201161491146P 2011-05-27 2011-05-27

Publications (1)

Publication Number Publication Date
PE20140784A1 true PE20140784A1 (es) 2014-07-03

Family

ID=47259774

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2013002721A PE20140784A1 (es) 2011-05-27 2012-05-24 Composiciones que contienen, metodos que involucran, y usos de derivados de dolastatina unidos a aminoacidos no naturales

Country Status (22)

Country Link
US (4) US9796754B2 (es)
EP (2) EP2714684B1 (es)
JP (4) JP6581774B2 (es)
KR (4) KR102179369B1 (es)
CN (4) CN103717595A (es)
AU (4) AU2012262560B2 (es)
BR (1) BR112013030372A2 (es)
CA (1) CA2837586C (es)
CL (1) CL2013003406A1 (es)
CO (1) CO6811816A2 (es)
CR (1) CR20130667A (es)
DK (1) DK2714684T3 (es)
EA (1) EA201391756A1 (es)
EC (1) ECSP13013115A (es)
ES (1) ES2690993T3 (es)
GT (1) GT201300295A (es)
IL (3) IL229505A (es)
MX (1) MX359217B (es)
NI (1) NI201300130A (es)
PE (1) PE20140784A1 (es)
WO (1) WO2012166560A1 (es)
ZA (1) ZA201309654B (es)

Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101963460B1 (ko) 2010-08-17 2019-03-28 암브룩스, 인코포레이티드 변형된 릴랙신 폴리펩타이드 및 그것의 용도
US9567386B2 (en) 2010-08-17 2017-02-14 Ambrx, Inc. Therapeutic uses of modified relaxin polypeptides
EP2714684B1 (en) * 2011-05-27 2018-09-05 Ambrx, Inc. Compositions containing, methods involving, and uses of non-natural amino acid linked dolastatin derivatives
MX345538B (es) * 2011-05-27 2017-02-03 Ambrx Inc Composiciones que contienen, metodos que incluyen, y usos de derivados de dolastatina enlazados a aminoacidos no naturales.
US20130190248A1 (en) * 2011-07-26 2013-07-25 Agensys, Inc. Substituted peptide analogs
EP2850059A4 (en) 2012-05-15 2016-06-29 Concortis Biosystems Corp CONJUGATES OF MEDICATION, METHODS OF CONJUGATION AND USE THEREOF
JP6425650B2 (ja) * 2012-06-07 2018-11-21 アンブルックス, インコーポレイテッドAmbrx, Inc. 前立腺特異的膜抗原抗体薬物複合体
WO2013192360A1 (en) * 2012-06-19 2013-12-27 Ambrx, Inc. Anti-cd70 antibody drug conjugates
US10226535B2 (en) 2012-12-10 2019-03-12 Mersana Therapeutics, Inc. Auristatin compounds and conjugates thereof
WO2014153164A1 (en) 2013-03-14 2014-09-25 The California Institute For Biomedical Research Targeting agent antibody conjugates and uses thereof
WO2014151030A1 (en) * 2013-03-15 2014-09-25 Novartis Ag Cell proliferation inhibitors and conjugates thereof
EP3590922A1 (en) 2013-03-15 2020-01-08 Zymeworks Inc. Cytotoxic and anti-mitotic compounds, and methods of using the same
FR3005051A1 (fr) * 2013-04-25 2014-10-31 Pf Medicament Derives de la dolastatine 10 et d'auristatines
ES2759503T3 (es) 2013-05-02 2020-05-11 Glykos Finland Oy Conjugados de una glicoproteína o un glicano con una carga útil tóxica
ES2845924T3 (es) 2013-10-15 2021-07-28 Scripps Research Inst Interruptores de células T con receptores de antígenos quiméricos peptídicos y usos de los mismos
CN106132431A (zh) 2013-10-15 2016-11-16 索伦托治疗有限公司 具有靶向分子和两种不同药物的药物偶联物
CA2921707C (en) 2013-10-15 2023-03-28 Seattle Genetics, Inc. Pegylated drug-linkers for improved ligand-drug conjugate pharmacokinetics
CN103665104B (zh) * 2013-12-09 2015-05-20 天津市康信医药科技有限公司 一种mmaf中间体五肽的合成方法
WO2015095301A2 (en) 2013-12-17 2015-06-25 Irm Llc Cytotoxic peptides and conjugates thereof
JP6560681B2 (ja) 2013-12-27 2019-08-14 ザイムワークス インコーポレイティド 薬物結合体のためのスルホンアミド含有連結系
CA2946796C (en) 2014-04-25 2019-10-22 Pierre Fabre Medicament Antibody-drug-conjugate and its use for the treatment of cancer
PT3134124T (pt) 2014-04-25 2019-06-03 Pf Medicament Conjugado anticorpo-fármaco igf-1r e a sua utilização para o tratamento de cancro
JP6681346B2 (ja) 2014-06-13 2020-04-15 ノバルティス アーゲー オーリスタチン誘導体およびその抱合体
WO2016001485A1 (en) 2014-06-30 2016-01-07 Glykos Finland Oy Saccharide derivative of a toxic payload and antibody conjugates thereof
US9879086B2 (en) 2014-09-17 2018-01-30 Zymeworks Inc. Cytotoxic and anti-mitotic compounds, and methods of using the same
MX2017007169A (es) 2014-12-03 2018-05-02 Genentech Inc Compuestos de amina cuaternaria y conjugados de anticuerpofármaco de los mismos.
JP6871858B2 (ja) 2015-01-28 2021-05-19 ソレント・セラピューティクス・インコーポレイテッドＳｏｒｒｅｎｔｏ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． 抗体薬物コンジュゲート
ES2884844T3 (es) 2015-03-09 2021-12-13 Agensys Inc Conjugados de anticuerpo fármaco (ADC) que se unen a proteínas FLT3
WO2016154621A1 (en) 2015-03-26 2016-09-29 The California Institute For Biomedical Research SWITCHABLE NON-scFv CHIMERIC RECEPTORS, SWITCHES, AND USES THEREOF
US11091546B2 (en) 2015-04-15 2021-08-17 The Scripps Research Institute Optimized PNE-based chimeric receptor T cell switches and uses thereof
CN105949277B (zh) * 2015-05-05 2019-03-01 成都永泰诺科技有限公司 一种抗肿瘤化合物及其用途
EP3165532B1 (en) 2015-11-03 2018-12-19 Industrial Technology Research Institute Auristatin derivatives, linker-drugs and ligand-drug conjugates
AU2017225982B2 (en) 2016-03-02 2023-10-05 Eisai R&D Management Co., Ltd. Eribulin-based antibody-drug conjugates and methods of use
CN109843919A (zh) 2016-03-25 2019-06-04 西雅图基因公司 用于制备聚乙二醇化的药物-接头及其中间体的方法
WO2018075807A1 (en) 2016-10-19 2018-04-26 California Institute For Biomedical Research Chimeric antigen receptor effector cell switches with humanized targeting moieties and/or optimized chimeric antigen receptor interacting domains and uses thereof
WO2018148419A1 (en) 2017-02-08 2018-08-16 Bristol-Myers Squibb Company Modified relaxin polypeptides comprising a pharmacokinetic enhancer and uses thereof
CN110430901A (zh) 2017-03-24 2019-11-08 西雅图基因公司 制备葡糖苷酸药物-接头及其中间体的方法
KR20200085807A (ko) 2017-11-07 2020-07-15 리제너론 파마슈티칼스 인코포레이티드 항체 약물 접합제용 친수성 링커
KR20200094185A (ko) 2017-11-30 2020-08-06 시애틀 지네틱스, 인크. 약물 링커 화합물의 제조방법
BR112020019611A2 (pt) 2018-03-29 2021-01-05 Ambrx, Inc. Conjugados de anticorpo anti-antígeno de membrana específico da próstata (amep) humanizado e fármaco
CN109232712B (zh) * 2018-08-21 2021-08-03 联宁（苏州）生物制药有限公司 一种用于抗体药物偶联物的中间体的制备方法
WO2020047176A1 (en) 2018-08-28 2020-03-05 Ambrx, Inc. Anti-cd3 antibody folate bioconjugates and their uses
EP4017586A1 (en) * 2019-08-21 2022-06-29 Kalvista Pharmaceuticals Limited Enzyme inhibitors
CA3154710A1 (en) 2019-10-04 2021-04-08 TAE Life Sciences Antibody compositions comprising fc mutations and site-specific conjugation properties
WO2021173889A1 (en) 2020-02-26 2021-09-02 Ambrx, Inc. Uses of anti-cd3 antibody folate bioconjugates
WO2023000171A1 (zh) * 2021-07-20 2023-01-26 浙江新码生物医药有限公司 一种含有抗her2-药物偶联物的冻干组合物、冻干制剂及其制备方法和用途
KR20240051956A (ko) 2021-09-03 2024-04-22 도레이 카부시키가이샤 암의 치료 및/또는 예방용 의약 조성물
WO2024077277A1 (en) 2022-10-07 2024-04-11 Ambrx, Inc. Drug linkers and antibody conjugates thereof

Family Cites Families (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2504010B1 (fr) 1981-04-15 1985-10-25 Sanofi Sa Medicaments anticancereux contenant la chaine a de la ricine associee a un anticorps antimelanome et procede pour leur preparation
US4671958A (en) 1982-03-09 1987-06-09 Cytogen Corporation Antibody conjugates for the delivery of compounds to target sites
US4542225A (en) 1984-08-29 1985-09-17 Dana-Farber Cancer Institute, Inc. Acid-cleavable compound
US4659839A (en) 1984-10-10 1987-04-21 Mallinckrodt, Inc. Coupling agents for radiolabeled antibody fragments
ATE66469T1 (de) 1985-01-14 1991-09-15 Neorx Corp Metall-radionuklid markiertes protein fuer diagnose und therapie.
US4680338A (en) 1985-10-17 1987-07-14 Immunomedics, Inc. Bifunctional linker
US4699784A (en) 1986-02-25 1987-10-13 Center For Molecular Medicine & Immunology Tumoricidal methotrexate-antibody conjugate
US4816444A (en) * 1987-07-10 1989-03-28 Arizona Board Of Regents, Arizona State University Cell growth inhibitory substance
US5252714A (en) 1990-11-28 1993-10-12 The University Of Alabama In Huntsville Preparation and use of polyethylene glycol propionaldehyde
US5831002A (en) * 1992-05-20 1998-11-03 Basf Aktiengesellschaft Antitumor peptides
US6034065A (en) * 1992-12-03 2000-03-07 Arizona Board Of Regents Elucidation and synthesis of antineoplastic tetrapeptide phenethylamides of dolastatin 10
US5635483A (en) * 1992-12-03 1997-06-03 Arizona Board Of Regents Acting On Behalf Of Arizona State University Tumor inhibiting tetrapeptide bearing modified phenethyl amides
US5599902A (en) * 1994-11-10 1997-02-04 Arizona Board Of Regents Acting On Behalf Of Arizona State University Cancer inhibitory peptides
DE69921102T2 (de) 1998-03-05 2006-02-02 Chiron Corp., Emeryville Verfahren zur verbesserung der serum-halbwertszeit von biologisch aktiven molekülen
CA2376057A1 (en) * 1999-06-08 2000-12-14 La Jolla Pharmaceutical Company Valency platform molecules comprising aminooxy groups
US6323315B1 (en) * 1999-09-10 2001-11-27 Basf Aktiengesellschaft Dolastatin peptides
CN1457260A (zh) 2000-06-16 2003-11-19 华盛顿大学肿瘤放射部 填装有配体－二生物素结合物的可重复使用的体外柱
EP1456360B1 (en) 2001-04-19 2015-06-03 The Scripps Research Institute Methods and composition for the production of orthoganal trna-aminoacyltrna synthetase pairs
US6649402B2 (en) 2001-06-22 2003-11-18 Wisconsin Alumni Research Foundation Microfabricated microbial growth assay method and apparatus
US6737409B2 (en) 2001-07-19 2004-05-18 Hoffmann-La Roche Inc. Dolastatin 10 derivatives
WO2003043583A2 (en) * 2001-11-20 2003-05-30 Seattle Genetics, Inc. Treatment of immunological disorders using anti-cd30 antibodies
ES2544527T3 (es) * 2002-07-31 2015-09-01 Seattle Genetics, Inc. Conjugados de fármacos y su uso para tratar el cáncer, una enfermedad autoinmune o una enfermedad infecciosa
US7642085B2 (en) 2002-12-22 2010-01-05 The Scripps Research Institute Protein arrays
US7662387B2 (en) * 2003-02-20 2010-02-16 Seattle Genetics Anti-cd70 antibody-drug conjugates and their use for the treatment of cancer and immune disorders
JP5020636B2 (ja) * 2003-11-06 2012-09-05 シアトル ジェネティックス， インコーポレイテッド リガンドに結合体化可能なモノメチルバリン化合物
CN1960965A (zh) * 2004-06-02 2007-05-09 霍夫曼-拉罗奇有限公司 氨基－烷氧基－庚酸烷基酯的合成
US7807619B2 (en) 2004-11-01 2010-10-05 The Regents Of The University Of California Compositions and methods for modification of biomolecules
KR20150126978A (ko) * 2005-06-20 2015-11-13 피에스엠에이 디벨롭먼트 캄파니, 엘엘씨 Ｐｓｍａ 항체-약물 접합체
DK1954710T3 (da) * 2005-11-08 2011-06-27 Ambrx Inc Acceleratorer til modifikation af unaturlige aminosyrer og unaturlige aminosyrepolypeptider
US7750116B1 (en) * 2006-02-18 2010-07-06 Seattle Genetics, Inc. Antibody drug conjugate metabolites
PL2842575T3 (pl) * 2008-03-18 2018-02-28 Seattle Genetics, Inc. Koniugaty aurystatyny lek łącznik
CN102448486A (zh) * 2009-03-06 2012-05-09 艾更斯司股份有限公司 结合于24p4c12蛋白的抗体药物偶联物(adc)
PE20120877A1 (es) * 2009-04-01 2012-08-06 Genentech Inc ANTICUERPOS ANTI-FcRH5 E INMUNOCONJUGADOS
US8521087B2 (en) 2009-07-15 2013-08-27 Lg Electronics Inc. System and method for cognitive radio transmission
WO2011038159A2 (en) * 2009-09-24 2011-03-31 Seattle Genetics, Inc. Dr5 ligand drug conjugates
WO2011058188A1 (en) * 2009-11-16 2011-05-19 Centre National De La Recherche Scientifique - Cnrs - Compounds and methods for purifying peptides produced by solid phase peptide synthesis
DK2707031T3 (da) * 2011-05-08 2019-10-07 Legochem Biosciences Inc Protein-active agent conjugates and method for preparing the same
MX345538B (es) * 2011-05-27 2017-02-03 Ambrx Inc Composiciones que contienen, metodos que incluyen, y usos de derivados de dolastatina enlazados a aminoacidos no naturales.
EP2714684B1 (en) 2011-05-27 2018-09-05 Ambrx, Inc. Compositions containing, methods involving, and uses of non-natural amino acid linked dolastatin derivatives

Also Published As

Publication number Publication date
AU2016204454B2 (en) 2018-03-01
EP3470413A3 (en) 2019-08-07
AU2012262560A1 (en) 2013-05-09
AU2020217337B2 (en) 2022-11-17
IL274204A (en) 2020-06-30
KR20140028073A (ko) 2014-03-07
AU2018203639B2 (en) 2020-05-14
ECSP13013115A (es) 2014-06-30
US20220411469A1 (en) 2022-12-29
NZ618079A (en) 2016-04-29
CA2837586A1 (en) 2012-12-06
CR20130667A (es) 2014-03-12
CN110078788B (zh) 2021-08-06
CN113527414A (zh) 2021-10-22
CL2013003406A1 (es) 2014-07-25
KR20190115109A (ko) 2019-10-10
ZA201309654B (en) 2016-08-31
DK2714684T3 (en) 2018-11-26
NI201300130A (es) 2014-12-22
EP3470413A2 (en) 2019-04-17
WO2012166560A1 (en) 2012-12-06
JP2018109033A (ja) 2018-07-12
MX2013013683A (es) 2014-01-08
KR102179369B1 (ko) 2020-11-16
JP6581774B2 (ja) 2019-09-25
KR20200128601A (ko) 2020-11-13
JP6781721B2 (ja) 2020-11-04
AU2016204454A1 (en) 2016-07-21
MX359217B (es) 2018-09-19
AU2020217337A1 (en) 2020-08-27
IL254879A0 (en) 2017-12-31
EP2714684A1 (en) 2014-04-09
KR20210106023A (ko) 2021-08-27
CO6811816A2 (es) 2013-12-16
BR112013030372A2 (pt) 2016-08-30
JP2023002671A (ja) 2023-01-10
CN110078788A (zh) 2019-08-02
US10954270B2 (en) 2021-03-23
KR102030856B1 (ko) 2019-10-10
JP2014516050A (ja) 2014-07-07
CA2837586C (en) 2018-12-11
AU2012262560B2 (en) 2016-06-09
CN110078787A (zh) 2019-08-02
EP2714684A4 (en) 2015-04-08
US11420999B2 (en) 2022-08-23
GT201300295A (es) 2014-11-24
ES2690993T3 (es) 2018-11-23
JP2020147587A (ja) 2020-09-17
EA201391756A1 (ru) 2014-05-30
IL229505A0 (en) 2014-01-30
US20210277056A1 (en) 2021-09-09
IL254879B (en) 2020-05-31
US20160052966A1 (en) 2016-02-25
CN103717595A (zh) 2014-04-09
IL274204B (en) 2022-03-01
US9796754B2 (en) 2017-10-24
EP2714684B1 (en) 2018-09-05
KR102356286B1 (ko) 2022-02-08
US20180009845A1 (en) 2018-01-11
AU2018203639A1 (en) 2018-06-14
IL229505A (en) 2017-10-31

Similar Documents

Publication Publication Date Title
PE20140784A1 (es) Composiciones que contienen, metodos que involucran, y usos de derivados de dolastatina unidos a aminoacidos no naturales
AR122198A2 (es) Formulaciones líquidas estabilizadas contentivas de anticuerpos
PE20141358A1 (es) Polimorfos de inhibidores de cinasas
SV2017005384A (es) Compuestos aminopirimidinilo
PE20142452A1 (es) AMIDAS CICLICAS COMO INHIBIDORES DE MetAP-2
PE20142164A1 (es) Inhibidores de diacilglicerol aciltransferasa 2
PE20181024A1 (es) Derivados de ciclohexano sustituido con amido
CO2017003132A2 (es) Inhibidores de la aldosterona sintasa derivados de la 2,6-diazaspiro[3.3]heptán-6-il]-3-piridil]isoindolín-1-ona o 2,7-diazaspiro[3.5]nonán-2-il]-3-piridil]isoindolín-1-ona
PE20160501A1 (es) Derivados de quinolizina sustituidos utiles como inhibidores de integrasa del vih
PE20201165A1 (es) Analogos de piridazina 1,4-disustituida y metodos para el tratamiento de condiciones relacionadas con la deficiencia de smn
CL2014003181A1 (es) Compuestos derivados de benzamidas n- sustituidas o piridinamidas n-sustituidas; composicion farmaceutica que los comprende; metodo de tratamiento; y su uso para el tratamiento de enfermedades o trastornos seleccionados de dolor, depresion y enfermedades cardiovasculares, respiratorias o psiquiatricas o combinaciones de estas.
PE20170925A1 (es) Composiciones y metodos para el tratamiento de trastornos del snc
EA202092187A1 (ru) Способы лечения эпителиоидно-клеточных опухолей
BR112013030362A8 (pt) Composto derivado de dolastatina, método para derivatizar o mesmo e composição farmacêutica que compreende o dito composto
EA201890086A1 (ru) 1,4-замещенные производные пиперидина
BR112014012789A2 (pt) agentes terapêuticos compreendendo sequências de aminoácidos de insulina
AR068756A1 (es) Compuestos peptidicos, formulacion farmaceutica y sus usos como moduladores del virus de la hepatitis c
UY36101A (es) Herbicidas de piridazinona
PE20180024A1 (es) Triazolopirazinonas como inhibidores de pde1
AR076219A1 (es) Analogos de isoxazol-3 (2h)-ona como agentes terapeuticos
MX2018015302A (es) Esteres de acidos grasos de cadena media de beta-hidroxibutirato y butanodiol y composiciones y metodos para usar los mismos.
BR112014015905A2 (pt) composição
EA201490709A1 (ru) Адъювантное соединение
PE20170303A1 (es) Derivados de la indolizina como inhibidores de las fosfoinositido-3 quinasas
PE20171433A1 (es) Nueva triterpenona c-3 con derivados de amida inversa c-17 como inhibidores de vih

Legal Events

Date Code Title Description
FD Application declared void or lapsed