WO2015151079A3 - Auristatin analogues and their conjugates with cell-binding molecules - Google Patents
Auristatin analogues and their conjugates with cell-binding molecules Download PDFInfo
- Publication number
- WO2015151079A3 WO2015151079A3 PCT/IB2015/054653 IB2015054653W WO2015151079A3 WO 2015151079 A3 WO2015151079 A3 WO 2015151079A3 IB 2015054653 W IB2015054653 W IB 2015054653W WO 2015151079 A3 WO2015151079 A3 WO 2015151079A3
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- conjugates
- cell
- binding molecules
- analogues
- auristatin
- Prior art date
Links
- 108010044540 auristatin Proteins 0.000 title 1
- MFRNYXJJRJQHNW-DEMKXPNLSA-N (2s)-2-[[(2r,3r)-3-methoxy-3-[(2s)-1-[(3r,4s,5s)-3-methoxy-5-methyl-4-[methyl-[(2s)-3-methyl-2-[[(2s)-3-methyl-2-(methylamino)butanoyl]amino]butanoyl]amino]heptanoyl]pyrrolidin-2-yl]-2-methylpropanoyl]amino]-3-phenylpropanoic acid Chemical compound CN[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N(C)[C@@H]([C@@H](C)CC)[C@H](OC)CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C(O)=O)CC1=CC=CC=C1 MFRNYXJJRJQHNW-DEMKXPNLSA-N 0.000 abstract 2
- 229940127089 cytotoxic agent Drugs 0.000 abstract 2
- 239000002254 cytotoxic agent Substances 0.000 abstract 2
- 231100000599 cytotoxic agent Toxicity 0.000 abstract 2
- 108010059074 monomethylauristatin F Proteins 0.000 abstract 2
- 230000002159 abnormal effect Effects 0.000 abstract 1
- 239000011230 binding agent Substances 0.000 abstract 1
- 230000010261 cell growth Effects 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 230000035755 proliferation Effects 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
- A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
- A61K47/68031—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being an auristatin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
- A61K47/6851—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
- A61K47/6869—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 a cell of the reproductive system: ovaria, uterus, testes, prostate
-
- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Immunology (AREA)
- Cell Biology (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Reproductive Health (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Abstract
Provided are analogues of auristatins, in particular monomethyl auristatin F (MMAF), as cytotoxic agents, conjugates of such agents with a cell-binding agent, the preparation and the therapeutic uses of these cytotoxic agents and conjugates thereof to arrest or retard abnormal cell growth and /or proliferation.
Priority Applications (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN202310609261.2A CN116726190A (en) | 2015-06-20 | 2015-06-20 | Aureostatin analogs and conjugate conjugates thereof with cell-binding molecules |
CN201580080907.6A CN107921144B (en) | 2015-06-20 | 2015-06-20 | Aureostatin analogs and conjugate conjugates thereof with cell-binding molecules |
PCT/IB2015/054653 WO2015151079A2 (en) | 2015-06-20 | 2015-06-20 | Auristatin analogues and their conjugates with cell-binding molecules |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/IB2015/054653 WO2015151079A2 (en) | 2015-06-20 | 2015-06-20 | Auristatin analogues and their conjugates with cell-binding molecules |
Publications (2)
Publication Number | Publication Date |
---|---|
WO2015151079A2 WO2015151079A2 (en) | 2015-10-08 |
WO2015151079A3 true WO2015151079A3 (en) | 2016-05-06 |
Family
ID=54241396
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/IB2015/054653 WO2015151079A2 (en) | 2015-06-20 | 2015-06-20 | Auristatin analogues and their conjugates with cell-binding molecules |
Country Status (2)
Country | Link |
---|---|
CN (2) | CN116726190A (en) |
WO (1) | WO2015151079A2 (en) |
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US10441654B2 (en) | 2014-01-24 | 2019-10-15 | Children's Hospital Of Eastern Ontario Research Institute Inc. | SMC combination therapy for the treatment of cancer |
EP3160513B1 (en) | 2014-06-30 | 2020-02-12 | Glykos Finland Oy | Saccharide derivative of a toxic payload and antibody conjugates thereof |
TW201740979A (en) * | 2016-02-29 | 2017-12-01 | 瑪德瑞高製藥公司 | HSP90 inhibitor drug conjugates |
SG10202007520WA (en) | 2016-03-02 | 2020-09-29 | Eisai R&D Man Co Ltd | Eribulin-based antibody-drug conjugates and methods of use |
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AU2018209164B2 (en) | 2017-01-17 | 2021-11-04 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
CN108452318B (en) * | 2017-02-17 | 2023-05-26 | 浙江特瑞思药业股份有限公司 | CD 20-targeted antibody coupling drug as well as preparation method and application thereof |
CN108452319A (en) * | 2017-02-20 | 2018-08-28 | 浙江特瑞思药业股份有限公司 | Target the antibody coupling pharmaceutical preparation of CD20 |
WO2018156180A1 (en) | 2017-02-24 | 2018-08-30 | Kindred Biosciences, Inc. | Anti-il31 antibodies for veterinary use |
US12018093B2 (en) | 2017-08-10 | 2024-06-25 | Sumitomo Pharma Co., Ltd. | Hemiasterlin derivatives and antibody-drug conjugates including same |
ES2974288T3 (en) | 2017-08-10 | 2024-06-26 | Sumitomo Pharma Co Ltd | Antibody-drug conjugates including a hemiasterlin derivative |
JP2021504414A (en) * | 2017-11-29 | 2021-02-15 | マジェンタ セラピューティクス インコーポレイテッドMagenta Therapeutics, Inc. | Compositions and Methods for CD2 + Cell Depletion |
AU2018374634A1 (en) | 2017-12-01 | 2020-05-28 | Abbvie Inc. | Glucocorticoid receptor agonist and immunoconjugates thereof |
WO2019142147A2 (en) * | 2018-01-18 | 2019-07-25 | Magenta Therapeutics, Inc. | Compositions and methods for the depletion of cd134+ cells |
CN108912212B (en) * | 2018-06-28 | 2019-08-30 | 中山大学附属口腔医院 | A kind of polypeptide and its application with CD105 specific binding |
JP2021530545A (en) * | 2018-07-23 | 2021-11-11 | マジェンタ セラピューティクス インコーポレイテッドMagenta Therapeutics, Inc. | Use of anti-CD2 antibody drug conjugate (ADC) in allogeneic cell therapy |
CN109187941B (en) * | 2018-08-31 | 2022-04-29 | 暨南大学 | Application of CD4+ CD70+ T cell subset in preparation of kit for auxiliary diagnosis of very severe aplastic anemia |
JP2020132638A (en) * | 2019-02-13 | 2020-08-31 | 大日本住友製薬株式会社 | Medicine containing antibody drug conjugate containing hemiasterlin derivative |
CN113121639B (en) * | 2019-12-30 | 2024-05-14 | 江苏恒瑞医药股份有限公司 | Aureostatin analogue and conjugate thereof, preparation method and application thereof |
CN110940764B (en) * | 2019-12-31 | 2022-06-28 | 湖南九典制药股份有限公司 | Separation method of statin optical isomer |
US11045546B1 (en) | 2020-03-30 | 2021-06-29 | Cytodyn Inc. | Methods of treating coronavirus infection |
CN111558044B (en) * | 2020-06-01 | 2022-02-11 | 中山大学肿瘤防治中心(中山大学附属肿瘤医院、中山大学肿瘤研究所) | Pharmaceutical composition containing sunitinib, and preparation and application thereof |
CN111393346B (en) * | 2020-06-02 | 2020-08-25 | 凯莱英生命科学技术(天津)有限公司 | Synthesis method of N-Boc-Dolaprine and Boc-Dap DCHA |
CN114073702B (en) * | 2021-03-05 | 2023-12-12 | 中以海德人工智能药物研发股份有限公司 | Use of quinolones for treating or preventing hepatitis B |
CN116482370B (en) * | 2023-06-25 | 2023-08-25 | 北京大学人民医院 | Antibody combination for screening plasma cell tumor treatment target and/or abnormal phenotype and application thereof |
CN117430660A (en) * | 2023-09-04 | 2024-01-23 | 诺灵生物医药科技(北京)有限公司 | Oritastatin F analogue, antibody drug conjugate thereof and application |
Citations (5)
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WO2005081711A2 (en) * | 2003-11-06 | 2005-09-09 | Seattle Genetics, Inc. | Monomethylvaline compounds capable of conjugation to ligands |
WO2009052431A2 (en) * | 2007-10-19 | 2009-04-23 | Seattle Genetics, Inc. | Cd19 binding agents and uses thereof |
WO2012143497A2 (en) * | 2011-04-21 | 2012-10-26 | Bayer Intellectual Property Gmbh | Novel binder-drug conjugates (adcs) and their use |
WO2014009774A1 (en) * | 2012-07-12 | 2014-01-16 | Hangzhou Dac Biotech Co., Ltd | Conjugates of cell binding molecules with cytotoxic agents |
WO2014080251A1 (en) * | 2012-11-24 | 2014-05-30 | Hangzhou Dac Biotech Co., Ltd. | Hydrophilic linkers and their uses for conjugation of drugs to cell binding molecules |
-
2015
- 2015-06-20 WO PCT/IB2015/054653 patent/WO2015151079A2/en active Application Filing
- 2015-06-20 CN CN202310609261.2A patent/CN116726190A/en active Pending
- 2015-06-20 CN CN201580080907.6A patent/CN107921144B/en active Active
Patent Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2005081711A2 (en) * | 2003-11-06 | 2005-09-09 | Seattle Genetics, Inc. | Monomethylvaline compounds capable of conjugation to ligands |
WO2009052431A2 (en) * | 2007-10-19 | 2009-04-23 | Seattle Genetics, Inc. | Cd19 binding agents and uses thereof |
WO2012143497A2 (en) * | 2011-04-21 | 2012-10-26 | Bayer Intellectual Property Gmbh | Novel binder-drug conjugates (adcs) and their use |
WO2014009774A1 (en) * | 2012-07-12 | 2014-01-16 | Hangzhou Dac Biotech Co., Ltd | Conjugates of cell binding molecules with cytotoxic agents |
WO2014080251A1 (en) * | 2012-11-24 | 2014-05-30 | Hangzhou Dac Biotech Co., Ltd. | Hydrophilic linkers and their uses for conjugation of drugs to cell binding molecules |
Also Published As
Publication number | Publication date |
---|---|
CN116726190A (en) | 2023-09-12 |
WO2015151079A2 (en) | 2015-10-08 |
CN107921144B (en) | 2023-11-28 |
CN107921144A (en) | 2018-04-17 |
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