CA2959630A1 - Cytotoxic benzodiazepine derivatives - Google Patents

Cytotoxic benzodiazepine derivatives Download PDF

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Publication number
CA2959630A1
CA2959630A1 CA2959630A CA2959630A CA2959630A1 CA 2959630 A1 CA2959630 A1 CA 2959630A1 CA 2959630 A CA2959630 A CA 2959630A CA 2959630 A CA2959630 A CA 2959630A CA 2959630 A1 CA2959630 A1 CA 2959630A1
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Canada
Prior art keywords
conjugate
antibody
compound
ala
optionally substituted
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CA2959630A
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English (en)
French (fr)
Inventor
Ravi V.J. Chari
Michael Louis Miller
Manami Shizuka
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Immunogen Inc
Original Assignee
Immunogen Inc
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=54140691&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA2959630(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Immunogen Inc filed Critical Immunogen Inc
Publication of CA2959630A1 publication Critical patent/CA2959630A1/en
Pending legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • A—HUMAN NECESSITIES
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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
    • A61K47/545—Heterocyclic compounds
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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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • 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
    • C07K16/2866—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
    • 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
    • C07K5/0202—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-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • 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
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • 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
    • C07K5/06052—Val-amino acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
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    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • C—CHEMISTRY; METALLURGY
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    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
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    • C07K5/0819—Tripeptides with the first amino acid being acidic
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    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
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    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1021—Tetrapeptides with the first amino acid being acidic
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/20—Immunoglobulins specific features characterized by taxonomic origin
    • C07K2317/24—Immunoglobulins specific features characterized by taxonomic origin containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/90—Immunoglobulins specific features characterized by (pharmaco)kinetic aspects or by stability of the immunoglobulin
    • C07K2317/92—Affinity (KD), association rate (Ka), dissociation rate (Kd) or EC50 value

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Virology (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
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CA2959630A 2014-09-03 2015-09-02 Cytotoxic benzodiazepine derivatives Pending CA2959630A1 (en)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201462045248P 2014-09-03 2014-09-03
US62/045,248 2014-09-03
US201462087040P 2014-12-03 2014-12-03
US62/087,040 2014-12-03
US201562149370P 2015-04-17 2015-04-17
US62/149,370 2015-04-17
US201562164305P 2015-05-20 2015-05-20
US62/164,305 2015-05-20
PCT/US2015/048059 WO2016036801A1 (en) 2014-09-03 2015-09-02 Cytotoxic benzodiazepine derivatives

Publications (1)

Publication Number Publication Date
CA2959630A1 true CA2959630A1 (en) 2016-03-10

Family

ID=54140691

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2959630A Pending CA2959630A1 (en) 2014-09-03 2015-09-02 Cytotoxic benzodiazepine derivatives

Country Status (33)

Country Link
US (5) US9669102B2 (enExample)
EP (2) EP3189056B1 (enExample)
JP (4) JP6606545B2 (enExample)
KR (2) KR102632830B1 (enExample)
CN (2) CN116514903A (enExample)
AU (3) AU2015311987B2 (enExample)
BR (1) BR112017002963A2 (enExample)
CA (1) CA2959630A1 (enExample)
CL (1) CL2017000507A1 (enExample)
CO (1) CO2017003011A2 (enExample)
CR (1) CR20170111A (enExample)
CY (1) CY1123325T1 (enExample)
DK (1) DK3189056T3 (enExample)
DO (1) DOP2017000053A (enExample)
EA (1) EA034138B1 (enExample)
EC (1) ECSP17020133A (enExample)
ES (1) ES2815353T3 (enExample)
HU (1) HUE051002T2 (enExample)
IL (4) IL250712B (enExample)
LT (1) LT3189056T (enExample)
MA (1) MA54254A (enExample)
MX (1) MX2017002758A (enExample)
PE (1) PE20170775A1 (enExample)
PH (1) PH12017500358A1 (enExample)
PL (1) PL3189056T3 (enExample)
PT (1) PT3189056T (enExample)
RS (1) RS60751B1 (enExample)
SG (2) SG10201901824UA (enExample)
SI (1) SI3189056T1 (enExample)
SM (1) SMT202000449T1 (enExample)
TN (1) TN2017000070A1 (enExample)
TW (4) TW202417447A (enExample)
WO (1) WO2016036801A1 (enExample)

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ES2815353T3 (es) 2014-09-03 2021-03-29 Immunogen Inc Derivados de benzodiazepina citotóxicos
BR112017027254A2 (pt) 2015-06-29 2019-05-14 Immunogen, Inc. anticorpos anti-cd123 e conjugados e derivados dos mesmos
US10081640B2 (en) 2015-07-21 2018-09-25 Immunogen, Inc. Methods of preparing cytotoxic benzodiazepine derivatives
WO2017091745A1 (en) 2015-11-25 2017-06-01 Immunogen, Inc. Pharmaceutical formulations and methods of use thereof
KR20180115687A (ko) * 2016-02-05 2018-10-23 밀레니엄 파머슈티컬스 인코퍼레이티드 Gcc-표적 항체-약물 콘주게이트
WO2018098258A2 (en) * 2016-11-23 2018-05-31 Immunogen, Inc. Selective sulfonation of benzodiazepine derivatives
WO2018119196A1 (en) 2016-12-23 2018-06-28 Immunogen, Inc. Immunoconjugates targeting adam9 and methods of use thereof
US20180230218A1 (en) 2017-01-04 2018-08-16 Immunogen, Inc. Met antibodies and immunoconjugates and uses thereof
WO2018183494A1 (en) 2017-03-31 2018-10-04 Immunogen, Inc. Cd19-targeting antibody-drug conjugates
CN115448926A (zh) 2017-04-20 2022-12-09 伊缪诺金公司 制备吲哚啉并苯并二氮杂䓬衍生物的方法
US11638760B2 (en) 2017-11-27 2023-05-02 Mersana Therapeutics, Inc. Pyrrolobenzodiazepine antibody conjugates
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