SG11201608203RA - Tubulysin derivatives - Google Patents

Tubulysin derivatives

Info

Publication number
SG11201608203RA
SG11201608203RA SG11201608203RA SG11201608203RA SG11201608203RA SG 11201608203R A SG11201608203R A SG 11201608203RA SG 11201608203R A SG11201608203R A SG 11201608203RA SG 11201608203R A SG11201608203R A SG 11201608203RA SG 11201608203R A SG11201608203R A SG 11201608203RA
Authority
SG
Singapore
Prior art keywords
tubulysin derivatives
tubulysin
derivatives
Prior art date
Application number
SG11201608203RA
Inventor
Lakshmaiah Gingipalli
Dorin Toader
Fengjiang Wang
Original Assignee
Medimmune Llc
Lakshmaiah Gingipalli
Dorin Toader
Fengjiang Wang
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, Lakshmaiah Gingipalli, Dorin Toader, Fengjiang Wang filed Critical Medimmune Llc
Publication of SG11201608203RA publication Critical patent/SG11201608203RA/en

Links

Classifications

    • 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
    • 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
    • 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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Cell Biology (AREA)
  • Toxicology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
SG11201608203RA 2014-04-11 2015-04-10 Tubulysin derivatives SG11201608203RA (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
SG11201608203RA true SG11201608203RA (en) 2016-10-28

Family

ID=54264545

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201608203RA SG11201608203RA (en) 2014-04-11 2015-04-10 Tubulysin derivatives

Country Status (19)

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

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20160142392A (en) * 2014-04-11 2016-12-12 메디뮨 엘엘씨 Tubulysin derivatives
US10160812B2 (en) 2014-04-11 2018-12-25 Medimmune, Llc Bispecific HER2 antibodies
PE20180355A1 (en) * 2015-02-25 2018-02-21 Univ Rice William M DEACETOXITUBULISIN H AND ANALOGS OF IT
PL3374398T3 (en) 2015-11-10 2020-08-24 Medimmune, Llc Binding molecules specific for asct2 and uses thereof
US11793880B2 (en) 2015-12-04 2023-10-24 Seagen Inc. Conjugates of quaternized tubulysin compounds
MX2018006218A (en) 2015-12-04 2018-09-05 Seattle Genetics Inc Conjugates of quaternized tubulysin compounds.
US10723727B2 (en) * 2016-02-01 2020-07-28 Pfizer Inc. Tubulysin analogs and methods for their preparation
KR102514317B1 (en) 2016-04-15 2023-03-27 마크로제닉스, 인크. Novel B7-H3-binding molecules, antibody drug conjugates thereof and methods of use thereof
JP2019534882A (en) 2016-10-11 2019-12-05 メドイミューン・リミテッドMedImmune Limited Antibody-drug conjugates with immune-mediated therapeutics
MA51447A (en) 2017-08-01 2020-06-10 Medimmune Llc MONOCLONAL ANTIBODY-DRUG CONJUGATE AGAINST BCMA
CN111093707A (en) * 2017-12-31 2020-05-01 杭州多禧生物科技有限公司 Tubulysin homolog conjugates containing branched linkers
CN109456212A (en) * 2018-12-03 2019-03-12 康化(上海)新药研发有限公司 Synthetic method of the one seed sand library than bent intermediate
TWI753252B (en) * 2019-05-03 2022-01-21 中國大陸商杭州多禧生物科技有限公司 A conjugate of a tubulysin analog with branched linkers
WO2020257998A1 (en) * 2019-06-24 2020-12-30 Hangzhou Dac Biotech Co., Ltd A conjugate of a cytotoxic agent to a cell binding molecule with branched linkers
EP4171653A2 (en) * 2020-06-24 2023-05-03 Regeneron Pharmaceuticals, Inc. Tubulysins and protein-tubulysin conjugates
CR20230146A (en) 2020-09-11 2023-06-07 Medimmune Ltd THERAPEUTIC B7-H4 BINDING MOLECULES
WO2023083846A1 (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
WO2024002938A1 (en) 2022-06-27 2024-01-04 Astrazeneca Ab Combinations involving epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer

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 (en) * 2009-07-22 2012-07-20 Kemotech S R L PHARMACEUTICAL COMPOUNDS
US8394922B2 (en) * 2009-08-03 2013-03-12 Medarex, Inc. Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof
EP3327027B9 (en) * 2011-11-17 2021-07-07 Pfizer Inc. Cytotoxic peptides and antibody drug conjugates thereof
IN2014CN04961A (en) * 2011-12-05 2015-09-18 Igenica Biotherapeutics Inc
PT2956173T (en) * 2013-02-14 2017-06-26 Bristol Myers Squibb Co Tubulysin compounds, methods of making and use
WO2015155345A1 (en) * 2014-04-11 2015-10-15 Medimmune Limited Antibodies and antibody-drug conjugates
US10160812B2 (en) * 2014-04-11 2018-12-25 Medimmune, Llc Bispecific HER2 antibodies
KR20160142392A (en) * 2014-04-11 2016-12-12 메디뮨 엘엘씨 Tubulysin derivatives

Also Published As

Publication number Publication date
IL247822A0 (en) 2016-11-30
PH12016501995A1 (en) 2017-01-09
EA201691963A1 (en) 2017-06-30
CL2016002548A1 (en) 2017-02-24
US10159745B2 (en) 2018-12-25
WO2015157594A1 (en) 2015-10-15
NZ725131A (en) 2018-03-23
TW201625662A (en) 2016-07-16
EP3129362A4 (en) 2017-08-23
MA39862A (en) 2017-02-15
US9427479B2 (en) 2016-08-30
MX2016013373A (en) 2017-05-02
AU2015243379A1 (en) 2016-11-03
EP3129362A1 (en) 2017-02-15
CN106458942A (en) 2017-02-22
JP2017510661A (en) 2017-04-13
US20150291657A1 (en) 2015-10-15
UY36075A (en) 2015-10-30
KR20160142392A (en) 2016-12-12
EA032203B1 (en) 2019-04-30
AR100006A1 (en) 2016-08-31
US20160339114A1 (en) 2016-11-24
AU2015243379B2 (en) 2018-02-01
CA2945318A1 (en) 2015-10-15

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