MX2020001928A - Proceso para la preparacion de tubulisinas e intermediarios de las mismas. - Google Patents
Proceso para la preparacion de tubulisinas e intermediarios de las mismas.Info
- Publication number
- MX2020001928A MX2020001928A MX2020001928A MX2020001928A MX2020001928A MX 2020001928 A MX2020001928 A MX 2020001928A MX 2020001928 A MX2020001928 A MX 2020001928A MX 2020001928 A MX2020001928 A MX 2020001928A MX 2020001928 A MX2020001928 A MX 2020001928A
- Authority
- MX
- Mexico
- Prior art keywords
- intermediates
- preparation
- tubulysins
- tubulysin
- compounds
- Prior art date
Links
- 239000000543 intermediate Substances 0.000 title abstract 2
- 229930184737 tubulysin Natural products 0.000 title abstract 2
- DLKUYSQUHXBYPB-NSSHGSRYSA-N (2s,4r)-4-[[2-[(1r,3r)-1-acetyloxy-4-methyl-3-[3-methylbutanoyloxymethyl-[(2s,3s)-3-methyl-2-[[(2r)-1-methylpiperidine-2-carbonyl]amino]pentanoyl]amino]pentyl]-1,3-thiazole-4-carbonyl]amino]-2-methyl-5-(4-methylphenyl)pentanoic acid Chemical class N([C@@H]([C@@H](C)CC)C(=O)N(COC(=O)CC(C)C)[C@H](C[C@@H](OC(C)=O)C=1SC=C(N=1)C(=O)N[C@H](C[C@H](C)C(O)=O)CC=1C=CC(C)=CC=1)C(C)C)C(=O)[C@H]1CCCCN1C DLKUYSQUHXBYPB-NSSHGSRYSA-N 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 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
-
- 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
-
- 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
- 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)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Immunology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Pharmacology & Pharmacy (AREA)
- Molecular Biology (AREA)
- Crystallography & Structural Chemistry (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Proteomics, Peptides & Aminoacids (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)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (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 |
|---|---|
| MX2020001928A true MX2020001928A (es) | 2020-03-24 |
Family
ID=63963374
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2020001928A MX2020001928A (es) | 2017-09-08 | 2018-09-07 | Proceso para la preparacion de tubulisinas e intermediarios de las mismas. |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US11389543B2 (https=) |
| EP (1) | EP3679036A1 (https=) |
| JP (2) | JP2020533308A (https=) |
| KR (1) | KR20200051733A (https=) |
| CN (1) | CN111601803A (https=) |
| AU (1) | AU2018329951B2 (https=) |
| BR (1) | BR112020004495A2 (https=) |
| CA (1) | CA3073766A1 (https=) |
| EA (1) | EA202090670A1 (https=) |
| IL (1) | IL272837B2 (https=) |
| MA (1) | MA50124A (https=) |
| MX (1) | MX2020001928A (https=) |
| SG (1) | SG11202001543XA (https=) |
| TW (2) | TWI820038B (https=) |
| WO (1) | WO2019051322A1 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20200051733A (ko) * | 2017-09-08 | 2020-05-13 | 시애틀 지네틱스, 인크. | 튜불리신 및 그 중간물의 제조 공정 |
| US20230002440A1 (en) * | 2018-09-07 | 2023-01-05 | Seattle Genetics, Inc. | Alternative processes for the preparation of tubulysins and intermediates thereof |
| BR112023018676A2 (pt) | 2021-03-18 | 2023-10-10 | Seagen Inc | Conjugado anticorpo-fármaco, composição farmacêutica, métodos de tratamento de uma doença ou condição e de um câncer, e, composição de conjugado ligante-fármaco |
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 |
| ES2708763T3 (es) | 2005-07-07 | 2019-04-11 | Seattle Genetics Inc | Compuestos de monometilvalina que tienen modificaciones de la cadena lateral de fenilalanina en el extremo C |
| EP2032606B1 (en) | 2006-05-30 | 2013-11-27 | Genentech, Inc. | Antibodies and immunoconjugates and uses therefor |
| ES2649941T3 (es) | 2007-02-23 | 2018-01-16 | Aileron Therapeutics, Inc. | Aminoácidos sustituidos para preparar péptidos macrocíclicos unidos a triazol |
| US20100047841A1 (en) * | 2007-02-27 | 2010-02-25 | 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 |
| CN104640572B (zh) | 2012-05-15 | 2018-04-27 | 索伦托医疗有限公司 | 药物偶联物，偶联方法，及其用途 |
| WO2013173337A2 (en) | 2012-05-15 | 2013-11-21 | Seattle Genetics, Inc. | Self-stabilizing linker conjugates |
| EP2708243A1 (en) * | 2012-09-17 | 2014-03-19 | OntoChem GmbH | Receptor ligand linked cytotoxic molecules |
| MX369022B (es) | 2013-05-31 | 2019-10-25 | Genentech Inc | Anticuerpos anti-ácido teicoico de la pared celular y conjugados. |
| RU2687044C2 (ru) | 2013-05-31 | 2019-05-06 | Дженентек, Инк. | Антитела против стеночной тейхоевой кислоты и их конъюгаты |
| FI3900742T3 (fi) * | 2014-09-11 | 2024-08-16 | Seagen Inc | Tertiääristä amiinia sisältävien lääkeaineiden kohdennettu antaminen |
| AU2015358532C1 (en) * | 2014-12-03 | 2020-10-29 | Genentech, Inc. | Quaternary amine compounds and antibody-drug conjugates thereof |
| US10808007B2 (en) * | 2015-02-25 | 2020-10-20 | William Marsh Rice University | Desacetoxytubulysin H and analogs thereof |
| KR20200051733A (ko) * | 2017-09-08 | 2020-05-13 | 시애틀 지네틱스, 인크. | 튜불리신 및 그 중간물의 제조 공정 |
-
2018
- 2018-09-07 KR KR1020207009940A patent/KR20200051733A/ko not_active Ceased
- 2018-09-07 EP EP18792575.5A patent/EP3679036A1/en not_active Withdrawn
- 2018-09-07 MA MA050124A patent/MA50124A/fr unknown
- 2018-09-07 US US16/645,369 patent/US11389543B2/en active Active
- 2018-09-07 TW TW107131484A patent/TWI820038B/zh not_active IP Right Cessation
- 2018-09-07 BR BR112020004495-4A patent/BR112020004495A2/pt not_active Application Discontinuation
- 2018-09-07 EA EA202090670A patent/EA202090670A1/ru unknown
- 2018-09-07 IL IL272837A patent/IL272837B2/en unknown
- 2018-09-07 MX MX2020001928A patent/MX2020001928A/es unknown
- 2018-09-07 WO PCT/US2018/050095 patent/WO2019051322A1/en not_active Ceased
- 2018-09-07 SG SG11202001543XA patent/SG11202001543XA/en unknown
- 2018-09-07 TW TW112136966A patent/TW202428569A/zh unknown
- 2018-09-07 CA CA3073766A patent/CA3073766A1/en active Pending
- 2018-09-07 AU AU2018329951A patent/AU2018329951B2/en not_active Ceased
- 2018-09-07 JP JP2020513753A patent/JP2020533308A/ja not_active Ceased
- 2018-09-07 CN CN201880062053.2A patent/CN111601803A/zh active Pending
-
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 |
| BR112020004495A2 (pt) | 2020-09-08 |
| IL272837A (en) | 2020-04-30 |
| EA202090670A1 (ru) | 2020-07-28 |
| CA3073766A1 (en) | 2019-03-14 |
| TW202428569A (zh) | 2024-07-16 |
| IL272837B1 (en) | 2024-02-01 |
| CN111601803A (zh) | 2020-08-28 |
| JP2020533308A (ja) | 2020-11-19 |
| KR20200051733A (ko) | 2020-05-13 |
| AU2018329951B2 (en) | 2023-12-14 |
| TWI820038B (zh) | 2023-11-01 |
| EP3679036A1 (en) | 2020-07-15 |
| US20220323601A1 (en) | 2022-10-13 |
| WO2019051322A1 (en) | 2019-03-14 |
| AU2018329951A1 (en) | 2020-04-16 |
| JP2023053386A (ja) | 2023-04-12 |
| US11389543B2 (en) | 2022-07-19 |
| IL272837B2 (en) | 2024-06-01 |
| US20200297864A1 (en) | 2020-09-24 |
| SG11202001543XA (en) | 2020-03-30 |
| TW201920128A (zh) | 2019-06-01 |
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