CA3012960A1 - Tubulysin analogs and methods for their preparation - Google Patents
Tubulysin analogs and methods for their preparation Download PDFInfo
- Publication number
- CA3012960A1 CA3012960A1 CA3012960A CA3012960A CA3012960A1 CA 3012960 A1 CA3012960 A1 CA 3012960A1 CA 3012960 A CA3012960 A CA 3012960A CA 3012960 A CA3012960 A CA 3012960A CA 3012960 A1 CA3012960 A1 CA 3012960A1
- Authority
- CA
- Canada
- Prior art keywords
- alkyl
- hydrogen
- c6alkyl
- heterocyclyl
- haloalkyl
- 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.)
- Abandoned
Links
Classifications
-
- 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
-
- 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
- A61K47/62—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
- A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/38—Nitrogen atoms
- C07D277/42—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (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)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662289485P | 2016-02-01 | 2016-02-01 | |
| US62/289,485 | 2016-02-01 | ||
| US201662322328P | 2016-04-14 | 2016-04-14 | |
| US62/322,328 | 2016-04-14 | ||
| PCT/IB2017/050462 WO2017134547A1 (en) | 2016-02-01 | 2017-01-27 | Tubulysin analogs and methods for their preparation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3012960A1 true CA3012960A1 (en) | 2017-08-10 |
Family
ID=57963390
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3012960A Abandoned CA3012960A1 (en) | 2016-02-01 | 2017-01-27 | Tubulysin analogs and methods for their preparation |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US10723727B2 (cg-RX-API-DMAC10.html) |
| EP (1) | EP3411371A1 (cg-RX-API-DMAC10.html) |
| JP (1) | JP2019507126A (cg-RX-API-DMAC10.html) |
| CA (1) | CA3012960A1 (cg-RX-API-DMAC10.html) |
| WO (1) | WO2017134547A1 (cg-RX-API-DMAC10.html) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11274124B2 (en) | 2017-11-29 | 2022-03-15 | William Marsh Rice University | Tubulysin analogues as anticancer agents and payloads for antibody-drug conjugates and methods of treatment therewith |
| WO2020132658A2 (en) | 2018-12-21 | 2020-06-25 | Regeneron Pharmaceuticals, Inc. | Tubulysins and protein-tubulysin conjugates |
| MX2022015769A (es) * | 2020-06-24 | 2023-01-19 | Regeneron Pharma | Tubulisinas y conjugados de proteina-tubulisina. |
| WO2023129518A1 (en) * | 2021-12-29 | 2023-07-06 | Regeneron Pharmaceuticals, Inc. | Tubulysins and protein-tubulysin conjugates |
| CN114920749B (zh) * | 2022-06-02 | 2024-08-16 | 山东鲁抗医药股份有限公司 | 7-氮杂双环[2.2.1]庚烷衍生物溴化物中间体的制备方法 |
| IL327670A (en) | 2023-10-11 | 2026-06-01 | Antikor Biopharma Ltd | Antibodies, conjugates, and uses thereof |
Family Cites Families (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL29945A (en) | 1968-05-06 | 1973-08-29 | Assia Chemical Labor Ltd | Beta-hydrazino carboxylic acids and processes for their preparation |
| GB2036891B (en) | 1978-12-05 | 1983-05-05 | Windsor Smith C | Change speed gear |
| GB8308235D0 (en) | 1983-03-25 | 1983-05-05 | Celltech Ltd | Polypeptides |
| US4816567A (en) | 1983-04-08 | 1989-03-28 | Genentech, Inc. | Recombinant immunoglobin preparations |
| JPS6147500A (ja) | 1984-08-15 | 1986-03-07 | Res Dev Corp Of Japan | キメラモノクロ−ナル抗体及びその製造法 |
| EP0173494A3 (en) | 1984-08-27 | 1987-11-25 | The Board Of Trustees Of The Leland Stanford Junior University | Chimeric receptors by dna splicing and expression |
| GB8422238D0 (en) | 1984-09-03 | 1984-10-10 | Neuberger M S | Chimeric proteins |
| JPS61134325A (ja) | 1984-12-04 | 1986-06-21 | Teijin Ltd | ハイブリツド抗体遺伝子の発現方法 |
| DE3689123T2 (de) | 1985-11-01 | 1994-03-03 | Xoma Corp | Modulare einheit von antikörpergenen, daraus hergestellte antikörper und verwendung. |
| US5225539A (en) | 1986-03-27 | 1993-07-06 | Medical Research Council | Recombinant altered antibodies and methods of making altered antibodies |
| US5530101A (en) | 1988-12-28 | 1996-06-25 | Protein Design Labs, Inc. | Humanized immunoglobulins |
| DE3920358A1 (de) | 1989-06-22 | 1991-01-17 | Behringwerke Ag | Bispezifische und oligospezifische, mono- und oligovalente antikoerperkonstrukte, ihre herstellung und verwendung |
| US5625126A (en) | 1990-08-29 | 1997-04-29 | Genpharm International, Inc. | Transgenic non-human animals for producing heterologous antibodies |
| US5545806A (en) | 1990-08-29 | 1996-08-13 | Genpharm International, Inc. | Ransgenic non-human animals for producing heterologous antibodies |
| ES2246502T3 (es) | 1990-08-29 | 2006-02-16 | Genpharm International, Inc. | Animales no humanos transgenicos capaces de producir anticuerpos heterologos. |
| US5661016A (en) | 1990-08-29 | 1997-08-26 | Genpharm International Inc. | Transgenic non-human animals capable of producing heterologous antibodies of various isotypes |
| US5633425A (en) | 1990-08-29 | 1997-05-27 | Genpharm International, Inc. | Transgenic non-human animals capable of producing heterologous antibodies |
| DE69233528T2 (de) | 1991-11-25 | 2006-03-16 | Enzon, Inc. | Verfahren zur Herstellung von multivalenten antigenbindenden Proteinen |
| US6214345B1 (en) | 1993-05-14 | 2001-04-10 | Bristol-Myers Squibb Co. | Lysosomal enzyme-cleavable antitumor drug conjugates |
| CA2249195A1 (en) | 1996-03-18 | 1997-09-25 | Board Of Regents, The University Of Texas System | Immunoglobin-like domains with increased half lives |
| JP5167473B2 (ja) | 2005-03-03 | 2013-03-21 | コヴェックス・テクノロジーズ・アイルランド・リミテッド | 抗血管新生化合物 |
| EP2148886B1 (en) * | 2007-05-10 | 2014-02-19 | R & D Biopharmaceuticals Gmbh | Tubulysine derivatives |
| US8883832B2 (en) | 2009-07-06 | 2014-11-11 | Aerpio Therapeutics Inc. | Compounds, compositions, and methods for preventing metastasis of cancer cells |
| US8394922B2 (en) | 2009-08-03 | 2013-03-12 | Medarex, Inc. | Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof |
| CA2813411C (en) | 2010-11-05 | 2016-08-02 | Rinat Neuroscience Corporation | Engineered polypeptide conjugates and methods for making thereof using transglutaminase |
| EP2780039B9 (en) | 2011-11-17 | 2018-04-18 | Pfizer Inc | Cytotoxic peptides and antibody drug conjugates thereof |
| EP3539982B1 (en) | 2011-12-23 | 2025-02-19 | Pfizer Inc. | Engineered antibody constant regions for site-specific conjugation and methods and uses therefor |
| US10131682B2 (en) | 2012-11-24 | 2018-11-20 | Hangzhou Dac Biotech Co., Ltd. | Hydrophilic linkers and their uses for conjugation of drugs to a cell binding molecules |
| US10195289B2 (en) | 2013-07-31 | 2019-02-05 | Rinat Neuroscience Corp. | Engineered polypeptide conjugates using transglutaminase |
| WO2015113760A1 (en) * | 2014-01-28 | 2015-08-06 | Tube Pharmaceuticals Gmbh | Cytotoxic tubulysin compounds for conjugation |
| CA2943299A1 (en) | 2014-04-11 | 2015-10-15 | Medimmune, Llc | Bispecific her2 antibodies |
| CA2945318A1 (en) * | 2014-04-11 | 2015-10-15 | Medimmune, Llc | Tubulysin derivatives |
-
2017
- 2017-01-27 CA CA3012960A patent/CA3012960A1/en not_active Abandoned
- 2017-01-27 US US16/072,291 patent/US10723727B2/en active Active
- 2017-01-27 EP EP17703229.9A patent/EP3411371A1/en not_active Withdrawn
- 2017-01-27 JP JP2018539095A patent/JP2019507126A/ja active Pending
- 2017-01-27 WO PCT/IB2017/050462 patent/WO2017134547A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| US20180362519A1 (en) | 2018-12-20 |
| JP2019507126A (ja) | 2019-03-14 |
| EP3411371A1 (en) | 2018-12-12 |
| US10723727B2 (en) | 2020-07-28 |
| WO2017134547A1 (en) | 2017-08-10 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |
Effective date: 20180727 |
|
| FZDE | Discontinued |
Effective date: 20220315 |