EA202090670A1 - Способ получения тубулизинов и их промежуточных соединений - Google Patents
Способ получения тубулизинов и их промежуточных соединенийInfo
- Publication number
- EA202090670A1 EA202090670A1 EA202090670A EA202090670A EA202090670A1 EA 202090670 A1 EA202090670 A1 EA 202090670A1 EA 202090670 A EA202090670 A EA 202090670A EA 202090670 A EA202090670 A EA 202090670A EA 202090670 A1 EA202090670 A1 EA 202090670A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- tubulisins
- obtaining
- intermediate compounds
- compounds
- tubulizin
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
-
- 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
- A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
- A61K47/6817—Toxins
-
- 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
- A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
-
- 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
-
- 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
-
- 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
- C07D417/14—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 three or more hetero rings
-
- 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
- C07K5/021—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)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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Immunology (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Crystallography & Structural Chemistry (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Toxicology (AREA)
- Cell Biology (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762556234P | 2017-09-08 | 2017-09-08 | |
| PCT/US2018/050095 WO2019051322A1 (en) | 2017-09-08 | 2018-09-07 | PROCESS FOR THE PREPARATION OF TUBULYSINS AND INTERMEDIATES THEREOF |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EA202090670A1 true EA202090670A1 (ru) | 2020-07-28 |
Family
ID=63963374
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA202090670A EA202090670A1 (ru) | 2017-09-08 | 2018-09-07 | Способ получения тубулизинов и их промежуточных соединений |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US11389543B2 (enExample) |
| EP (1) | EP3679036A1 (enExample) |
| JP (2) | JP2020533308A (enExample) |
| KR (1) | KR20200051733A (enExample) |
| CN (1) | CN111601803A (enExample) |
| AU (1) | AU2018329951B2 (enExample) |
| BR (1) | BR112020004495A2 (enExample) |
| CA (1) | CA3073766A1 (enExample) |
| EA (1) | EA202090670A1 (enExample) |
| IL (1) | IL272837B2 (enExample) |
| MA (1) | MA50124A (enExample) |
| MX (1) | MX2020001928A (enExample) |
| SG (1) | SG11202001543XA (enExample) |
| TW (2) | TWI820038B (enExample) |
| WO (1) | WO2019051322A1 (enExample) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111601803A (zh) * | 2017-09-08 | 2020-08-28 | 西雅图基因公司 | 微管溶素及其中间体的制备方法 |
| US20230002440A1 (en) * | 2018-09-07 | 2023-01-05 | Seattle Genetics, Inc. | Alternative processes for the preparation of tubulysins and intermediates thereof |
| CA3213636A1 (en) | 2021-03-18 | 2022-09-22 | Seagen Inc. | Selective drug release from internalized conjugates of biologically active compounds |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10230872A1 (de) * | 2002-07-09 | 2004-01-22 | Morphochem AG Aktiengesellschaft für kombinatorische Chemie | Verfahren zur Herstellung von substituierten Thiazol-2-ylmethylestern |
| JP5171621B2 (ja) | 2005-07-07 | 2013-03-27 | シアトル ジェネティックス， インコーポレイテッド | フェニルアラニン側鎖修飾をｃ末端に有するモノメチルバリン化合物 |
| WO2007140371A2 (en) | 2006-05-30 | 2007-12-06 | Genentech, Inc. | Antibodies and immunoconjugates and uses therefor |
| CA2678941C (en) | 2007-02-23 | 2018-11-27 | Aileron Therapeutics, Inc. | Triazole macrocycle systems |
| WO2008106080A2 (en) * | 2007-02-27 | 2008-09-04 | University Of Pittsburgh - Of The Commonwealth System Of Higher Education | Synthesis of desacetoxytubulysin h and analogs thereof |
| AU2013229786B2 (en) | 2012-03-08 | 2017-06-22 | Halozyme, Inc. | Conditionally active anti-epidermal growth factor receptor antibodies and methods of use thereof |
| EP3925627A1 (en) | 2012-05-15 | 2021-12-22 | Concortis Biosystems, Corp | Drug-conjugates and uses thereof |
| AU2013263002C1 (en) | 2012-05-15 | 2018-05-31 | Seagen Inc. | Self-stabilizing linker conjugates |
| EP2708243A1 (en) * | 2012-09-17 | 2014-03-19 | OntoChem GmbH | Receptor ligand linked cytotoxic molecules |
| MA38686A1 (fr) | 2013-05-31 | 2017-10-31 | Genentech Inc | Anticorps anti-acide téichoïque de la paroi cellulaire et conjugués associés |
| BR112015029754A2 (pt) | 2013-05-31 | 2017-09-26 | Genentech Inc | anticorpos anti-teicoico da parede e conjugados |
| HRP20241124T1 (hr) * | 2014-09-11 | 2024-11-22 | Seagen Inc. | Ciljana isporuka lijekovitih tvari koje sadrže tercijarni amin |
| MX2017007169A (es) | 2014-12-03 | 2018-05-02 | Genentech Inc | Compuestos de amina cuaternaria y conjugados de anticuerpofármaco de los mismos. |
| EA201791896A1 (ru) * | 2015-02-25 | 2018-02-28 | Уильям Марш Райс Юниверсити | Дезацетокситубулизин н и его аналоги |
| CN111601803A (zh) * | 2017-09-08 | 2020-08-28 | 西雅图基因公司 | 微管溶素及其中间体的制备方法 |
-
2018
- 2018-09-07 CN CN201880062053.2A patent/CN111601803A/zh active Pending
- 2018-09-07 SG SG11202001543XA patent/SG11202001543XA/en unknown
- 2018-09-07 JP JP2020513753A patent/JP2020533308A/ja not_active Ceased
- 2018-09-07 KR KR1020207009940A patent/KR20200051733A/ko not_active Ceased
- 2018-09-07 EA EA202090670A patent/EA202090670A1/ru unknown
- 2018-09-07 US US16/645,369 patent/US11389543B2/en active Active
- 2018-09-07 MA MA050124A patent/MA50124A/fr unknown
- 2018-09-07 EP EP18792575.5A patent/EP3679036A1/en not_active Withdrawn
- 2018-09-07 CA CA3073766A patent/CA3073766A1/en active Pending
- 2018-09-07 AU AU2018329951A patent/AU2018329951B2/en not_active Ceased
- 2018-09-07 TW TW107131484A patent/TWI820038B/zh not_active IP Right Cessation
- 2018-09-07 TW TW112136966A patent/TW202428569A/zh unknown
- 2018-09-07 IL IL272837A patent/IL272837B2/en unknown
- 2018-09-07 BR BR112020004495-4A patent/BR112020004495A2/pt not_active Application Discontinuation
- 2018-09-07 WO PCT/US2018/050095 patent/WO2019051322A1/en not_active Ceased
- 2018-09-07 MX MX2020001928A patent/MX2020001928A/es unknown
-
2022
- 2022-06-08 US US17/835,841 patent/US20220323601A1/en not_active Abandoned
-
2023
- 2023-02-16 JP JP2023022825A patent/JP2023053386A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| MA50124A (fr) | 2020-07-15 |
| IL272837B1 (en) | 2024-02-01 |
| SG11202001543XA (en) | 2020-03-30 |
| TW201920128A (zh) | 2019-06-01 |
| MX2020001928A (es) | 2020-03-24 |
| EP3679036A1 (en) | 2020-07-15 |
| JP2020533308A (ja) | 2020-11-19 |
| KR20200051733A (ko) | 2020-05-13 |
| US11389543B2 (en) | 2022-07-19 |
| BR112020004495A2 (pt) | 2020-09-08 |
| IL272837B2 (en) | 2024-06-01 |
| AU2018329951A1 (en) | 2020-04-16 |
| IL272837A (en) | 2020-04-30 |
| US20220323601A1 (en) | 2022-10-13 |
| AU2018329951B2 (en) | 2023-12-14 |
| TW202428569A (zh) | 2024-07-16 |
| WO2019051322A1 (en) | 2019-03-14 |
| JP2023053386A (ja) | 2023-04-12 |
| US20200297864A1 (en) | 2020-09-24 |
| TWI820038B (zh) | 2023-11-01 |
| CA3073766A1 (en) | 2019-03-14 |
| CN111601803A (zh) | 2020-08-28 |
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