NZ725131A - Tubulysin derivatives - Google Patents

Tubulysin derivatives

Info

Publication number
NZ725131A
NZ725131A NZ725131A NZ72513115A NZ725131A NZ 725131 A NZ725131 A NZ 725131A NZ 725131 A NZ725131 A NZ 725131A NZ 72513115 A NZ72513115 A NZ 72513115A NZ 725131 A NZ725131 A NZ 725131A
Authority
NZ
New Zealand
Prior art keywords
tubulysin
formula
derivatives
tubulysin derivatives
conjugates
Prior art date
Application number
NZ725131A
Other languages
English (en)
Inventor
Dorin Toader
Fengjiang Wang
Lakshmaiah Gingipalli
Original Assignee
Medimmune Llc
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 Medimmune Llc filed Critical Medimmune Llc
Publication of NZ725131A publication Critical patent/NZ725131A/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/07Tetrapeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05Dipeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6811Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6811Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • A61K47/6817Toxins
    • A61K47/6829Bacterial toxins, e.g. diphteria toxins or Pseudomonas exotoxin A
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/6835Medicinal 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
    • A61K47/6851Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/30Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/021Peptides 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)n-C(=0)-, n being 5 or 6; for n > 6, classification in C07K5/06 - C07K5/10, according to the moiety having normal peptide bonds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0212Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -N-C-N-C(=0)-, e.g. retro-inverso peptides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Cell Biology (AREA)
  • Toxicology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
NZ725131A 2014-04-11 2015-04-10 Tubulysin derivatives NZ725131A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201461978460P 2014-04-11 2014-04-11
PCT/US2015/025235 WO2015157594A1 (en) 2014-04-11 2015-04-10 Tubulysin derivatives

Publications (1)

Publication Number Publication Date
NZ725131A true NZ725131A (en) 2018-03-23

Family

ID=54264545

Family Applications (1)

Application Number Title Priority Date Filing Date
NZ725131A NZ725131A (en) 2014-04-11 2015-04-10 Tubulysin derivatives

Country Status (19)

Country Link
US (2) US9427479B2 (OSRAM)
EP (1) EP3129362A4 (OSRAM)
JP (1) JP2017510661A (OSRAM)
KR (1) KR20160142392A (OSRAM)
CN (1) CN106458942A (OSRAM)
AR (1) AR100006A1 (OSRAM)
AU (1) AU2015243379B2 (OSRAM)
CA (1) CA2945318A1 (OSRAM)
CL (1) CL2016002548A1 (OSRAM)
EA (1) EA032203B1 (OSRAM)
IL (1) IL247822A0 (OSRAM)
MA (1) MA39862A (OSRAM)
MX (1) MX2016013373A (OSRAM)
NZ (1) NZ725131A (OSRAM)
PH (1) PH12016501995A1 (OSRAM)
SG (1) SG11201608203RA (OSRAM)
TW (1) TW201625662A (OSRAM)
UY (1) UY36075A (OSRAM)
WO (1) WO2015157594A1 (OSRAM)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3129055B1 (en) 2014-04-11 2020-07-01 MedImmune, LLC Bispecific her2 antibodies
TW201625662A (zh) * 2014-04-11 2016-07-16 麥迪紐有限責任公司 妥布賴森(tubulysin)衍生物
PE20180355A1 (es) 2015-02-25 2018-02-21 Univ Rice William M Desacetoxitubulisina h y analogos de esta
HRP20200882T1 (hr) 2015-11-10 2020-09-04 Medimmune, Llc Vezujuće molekule specifične za asct2 i njihova uporaba
SG11201804268RA (en) 2015-12-04 2018-06-28 Seattle Genetics Inc Conjugates of quaternized tubulysin compounds
US11793880B2 (en) 2015-12-04 2023-10-24 Seagen Inc. Conjugates of quaternized tubulysin compounds
CA3012960A1 (en) * 2016-02-01 2017-08-10 Pfizer Inc. Tubulysin analogs and methods for their preparation
MY198114A (en) 2016-04-15 2023-08-04 Macrogenics Inc Novel b7-h3-binding molecules, antibody drug conjugates thereof and methods of use thereof
JP2019534882A (ja) 2016-10-11 2019-12-05 メドイミューン・リミテッドMedImmune Limited 免疫介在性療法薬を有する抗体−薬物コンジュゲート
WO2019025983A1 (en) 2017-08-01 2019-02-07 Medimmune, Llc CONJUGATED MONOCLONAL ANTIBODY-MEDICINE DIRECTED AGAINST BCMA
SG11202004801WA (en) 2017-12-31 2020-06-29 Hangzhou Dac Biotech Co Ltd A conjugate of a tubulysin analog with branched linkers
CN109456212A (zh) * 2018-12-03 2019-03-12 康化(上海)新药研发有限公司 一种沙库比曲中间体的合成方法
EP3898651A2 (en) 2018-12-21 2021-10-27 Regeneron Pharmaceuticals, Inc. Tubulysins and protein-tubulysin conjugates
TWI753252B (zh) * 2019-05-03 2022-01-21 中國大陸商杭州多禧生物科技有限公司 含支鏈連接體的Tubulysin同系物偶聯物
JP2022539076A (ja) * 2019-06-24 2022-09-07 ハンジョウ ディーエーシー バイオテック シーオー.,エルティディ. 分岐連結体を有する細胞結合分子と細胞毒性剤との共役体
JP2023533218A (ja) * 2020-06-24 2023-08-02 レゲネロン ファーマシューティカルス,インコーポレーテッド ツブリシン及びタンパク質-ツブリシンコンジュゲート
IL301041A (en) 2020-09-11 2023-05-01 Medimmune Ltd Therapeutic B7-H4 binding molecules
CA3237211A1 (en) 2021-11-10 2023-05-19 Astrazeneca Ab Antibody molecules and conjugates
GB202117928D0 (en) 2021-12-11 2022-01-26 Cancer Research Tech Ltd Immunotherapy for cancer
KR20250029133A (ko) 2022-06-27 2025-03-04 아스트라제네카 아베 암 치료를 위한 표피성장인자 수용체 티로신 키나제 억제제를 포함하는 조합물
WO2025078841A2 (en) 2023-10-11 2025-04-17 Antikor Biopharma Limited Antibodies, conjugates, and uses thereof

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7064211B2 (en) * 2002-03-22 2006-06-20 Eisai Co., Ltd. Hemiasterlin derivatives and uses thereof
US20060148014A1 (en) * 2004-12-09 2006-07-06 Sergei Agoulnik Tubulin isotype screening in cancer therapy using hemiasterlin analogs
IT1394860B1 (it) * 2009-07-22 2012-07-20 Kemotech S R L Composti farmaceutici
US8394922B2 (en) * 2009-08-03 2013-03-12 Medarex, Inc. Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof
PT3327027T (pt) * 2011-11-17 2021-02-15 Pfizer Péptidos citotóxicos e seus conjugados de anticorpos e fármacos
BR112014013526A8 (pt) * 2011-12-05 2017-06-13 Igenica Biotherapeutics Inc conjugados de anticorpo-fármaco e compostos, composições e métodos relacionados
SI2956173T1 (sl) * 2013-02-14 2017-06-30 Bristol-Myers Squibb Company Spojine tubulizina, postopki pridobivanja in uporaba
TW201625662A (zh) * 2014-04-11 2016-07-16 麥迪紐有限責任公司 妥布賴森(tubulysin)衍生物
WO2015155345A1 (en) * 2014-04-11 2015-10-15 Medimmune Limited Antibodies and antibody-drug conjugates
EP3129055B1 (en) * 2014-04-11 2020-07-01 MedImmune, LLC Bispecific her2 antibodies

Also Published As

Publication number Publication date
AU2015243379B2 (en) 2018-02-01
MX2016013373A (es) 2017-05-02
KR20160142392A (ko) 2016-12-12
CA2945318A1 (en) 2015-10-15
MA39862A (fr) 2017-02-15
EA201691963A1 (ru) 2017-06-30
TW201625662A (zh) 2016-07-16
EA032203B1 (ru) 2019-04-30
WO2015157594A1 (en) 2015-10-15
US9427479B2 (en) 2016-08-30
CN106458942A (zh) 2017-02-22
EP3129362A1 (en) 2017-02-15
CL2016002548A1 (es) 2017-02-24
AU2015243379A1 (en) 2016-11-03
EP3129362A4 (en) 2017-08-23
PH12016501995A1 (en) 2017-01-09
US20160339114A1 (en) 2016-11-24
JP2017510661A (ja) 2017-04-13
IL247822A0 (en) 2016-11-30
SG11201608203RA (en) 2016-10-28
US10159745B2 (en) 2018-12-25
UY36075A (es) 2015-10-30
AR100006A1 (es) 2016-08-31
US20150291657A1 (en) 2015-10-15

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