WO2014052537A1 - Improved methods for the acylation of maytansinol - Google Patents

Improved methods for the acylation of maytansinol Download PDF

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Publication number
WO2014052537A1
WO2014052537A1 PCT/US2013/061839 US2013061839W WO2014052537A1 WO 2014052537 A1 WO2014052537 A1 WO 2014052537A1 US 2013061839 W US2013061839 W US 2013061839W WO 2014052537 A1 WO2014052537 A1 WO 2014052537A1
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WO
WIPO (PCT)
Prior art keywords
reaction mixture
formula
carboxyanhydride
represented
group
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.)
Ceased
Application number
PCT/US2013/061839
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English (en)
French (fr)
Inventor
Wayne C. Widdison
Robert Yongxin Zhao
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Immunogen Inc
Original Assignee
Immunogen Inc
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
Priority to MX2015003745A priority Critical patent/MX366701B/es
Priority to EP21166484.2A priority patent/EP3904358A1/en
Priority to HK16100242.8A priority patent/HK1212341B/en
Priority to DK13774881.0T priority patent/DK2900676T3/en
Priority to HRP20190473TT priority patent/HRP20190473T1/hr
Priority to BR122021022582-6A priority patent/BR122021022582B1/pt
Priority to RS20190314A priority patent/RS58493B1/sr
Priority to CN201380049853.8A priority patent/CN104768955B/zh
Priority to SI201331374T priority patent/SI2900676T1/sl
Priority to EP13774881.0A priority patent/EP2900676B1/en
Priority to CA2884873A priority patent/CA2884873C/en
Priority to AU2013323572A priority patent/AU2013323572B2/en
Priority to NZ706019A priority patent/NZ706019A/en
Priority to MX2019008652A priority patent/MX390615B/es
Priority to PL13774881T priority patent/PL2900676T3/pl
Priority to SM20190170T priority patent/SMT201900170T1/it
Priority to ES13774881T priority patent/ES2716561T3/es
Priority to JP2015534641A priority patent/JP6517693B2/ja
Application filed by Immunogen Inc filed Critical Immunogen Inc
Priority to PL18213678T priority patent/PL3486248T3/pl
Priority to EP18213678.8A priority patent/EP3486248B1/en
Priority to BR112015006505-8A priority patent/BR112015006505B1/pt
Priority to SG11201501918UA priority patent/SG11201501918UA/en
Priority to LTEP13774881.0T priority patent/LT2900676T/lt
Priority to RU2015111635A priority patent/RU2648992C2/ru
Publication of WO2014052537A1 publication Critical patent/WO2014052537A1/en
Priority to ZA2015/01898A priority patent/ZA201501898B/en
Priority to IL237899A priority patent/IL237899A/en
Anticipated expiration legal-status Critical
Priority to IL253988A priority patent/IL253988B/en
Priority to AU2018201392A priority patent/AU2018201392B2/en
Priority to CY20191100302T priority patent/CY1121415T1/el
Priority to AU2020203823A priority patent/AU2020203823B2/en
Priority to CY20211100594T priority patent/CY1124337T1/el
Priority to AU2022201557A priority patent/AU2022201557A1/en
Ceased legal-status Critical Current

Links

Classifications

    • H—ELECTRICITY
    • H01—ELECTRIC ELEMENTS
    • H01R—ELECTRICALLY-CONDUCTIVE CONNECTIONS; STRUCTURAL ASSOCIATIONS OF A PLURALITY OF MUTUALLY-INSULATED ELECTRICAL CONNECTING ELEMENTS; COUPLING DEVICES; CURRENT COLLECTORS
    • H01R12/00—Structural associations of a plurality of mutually-insulated electrical connecting elements, specially adapted for printed circuits, e.g. printed circuit boards [PCB], flat or ribbon cables, or like generally planar structures, e.g. terminal strips, terminal blocks; Coupling devices specially adapted for printed circuits, flat or ribbon cables, or like generally planar structures; Terminals specially adapted for contact with, or insertion into, printed circuits, flat or ribbon cables, or like generally planar structures
    • H01R12/50—Fixed connections
    • H01R12/51—Fixed connections for rigid printed circuits or like structures
    • H01R12/55—Fixed connections for rigid printed circuits or like structures characterised by the terminals
    • H01R12/58—Fixed connections for rigid printed circuits or like structures characterised by the terminals terminals for insertion into holes
    • H01R12/585—Terminals having a press fit or a compliant portion and a shank passing through a hole in the printed circuit board
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • 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
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/16—Peri-condensed systems
    • H—ELECTRICITY
    • H05—ELECTRIC TECHNIQUES NOT OTHERWISE PROVIDED FOR
    • H05K—PRINTED CIRCUITS; CASINGS OR CONSTRUCTIONAL DETAILS OF ELECTRIC APPARATUS; MANUFACTURE OF ASSEMBLAGES OF ELECTRICAL COMPONENTS
    • H05K1/00—Printed circuits
    • H05K1/02—Details
    • H05K1/0201—Thermal arrangements, e.g. for cooling, heating or preventing overheating
    • H05K1/0203—Cooling of mounted components
    • H—ELECTRICITY
    • H05—ELECTRIC TECHNIQUES NOT OTHERWISE PROVIDED FOR
    • H05K—PRINTED CIRCUITS; CASINGS OR CONSTRUCTIONAL DETAILS OF ELECTRIC APPARATUS; MANUFACTURE OF ASSEMBLAGES OF ELECTRICAL COMPONENTS
    • H05K1/00—Printed circuits
    • H05K1/02—Details
    • H05K1/11—Printed elements for providing electric connections to or between printed circuits
    • H05K1/115—Via connections; Lands around holes or via connections
    • H05K1/116—Lands, clearance holes or other lay-out details concerning the surrounding of a via
    • H—ELECTRICITY
    • H05—ELECTRIC TECHNIQUES NOT OTHERWISE PROVIDED FOR
    • H05K—PRINTED CIRCUITS; CASINGS OR CONSTRUCTIONAL DETAILS OF ELECTRIC APPARATUS; MANUFACTURE OF ASSEMBLAGES OF ELECTRICAL COMPONENTS
    • H05K1/00—Printed circuits
    • H05K1/18—Printed circuits structurally associated with non-printed electric components
    • H05K1/181—Printed circuits structurally associated with non-printed electric components associated with surface mounted components

Definitions

  • the naturally occurring and synthetic C-3 esters of maytansinol can be classified into two groups: (a) Maytansine (2) and its analogs (e.g., DM1 and DM4), which are C-3 esters with N-methyl-L-alanine or derivatives of N-methyl-L-alanine (U.S. Pat. Nos. 4,137,230; 4,260,608; 5,208,020; and Chem. Pharm. Bull. 12:3441 (1984)); (b) Ansamitocins, which are C-3 esters with simple carboxylic acids (U.S. Pat. Nos.
  • nucleophilic reagent refers to a reactant that reacts with electropositive centers in the N-carboxyanhydride represented by Formula (II) to decompose the N- carboxyanhydride.
  • suitable nucleophilic reagent include water, an alcohol (methanol, ethanol, n-propanol, isopropanol, or tert-butanol) and a primary or secondary amine (e.g., methylamine, ethylamine, dimethylamine, diethylamine, etc.).
  • the nucleophilic reagent is an alcohol.
  • the nucleophilic reagent is water.
  • X' is a halide
  • n isl
  • Linear or branched Alkyl refers to a saturated linear or branched- chain monovalent hydrocarbon radical of one to twenty carbon atoms.
  • alkyl include, but are not limited to, methyl, ethyl, 1 -propyl, 2-propyl, 1 -butyl, 2-methyl-l -propyl, - CH 2 CH(CH ) 2 , 2-butyl, 2-methyl-2-propyl, 1-pentyl, 2-pentyl, 3-pentyl, 2-methyl-2-butyl, 3- methyl-2-butyl, 3-methyl-l -butyl, 2-methyl-l -butyl, -CH 2 CH 2 CH(CH 3 ) 2 ,l-hexyl, 2-hexyl, 3- hexyl, 2-methyl-2-pentyl, 3-methyl-2-pentyl, 4-methyl-2-pentyl, 3-methyl-3-pentyl, 2- methyl-3-pentyl, 2- methyl-3-p
  • Suitable substituents for an alkyl group are those which do not significantly interfere with the disclosed reactions. Substituents that do interfere with the disclosed reactions can be protected according to methods well known to one of ordinary skill in the art, for example, in T.W. Greene and P. G. M. Wuts "Protective Groups in Organic Synthesis” John Wiley & Sons, Inc., New York 1999. Exemplary substituents include aryl (e.g., phenyl, phenol and protected phenol), heteroaryl (e.g., indolyl and imidazolyl) halogen, guanidinium

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Microelectronics & Electronic Packaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Polyamides (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
PCT/US2013/061839 2012-09-26 2013-09-26 Improved methods for the acylation of maytansinol Ceased WO2014052537A1 (en)

Priority Applications (32)

Application Number Priority Date Filing Date Title
EP21166484.2A EP3904358A1 (en) 2012-09-26 2013-09-26 Improved methods for the acylation of maytansinol
HK16100242.8A HK1212341B (en) 2012-09-26 2013-09-26 Improved method for the acylation of maytansinol
DK13774881.0T DK2900676T3 (en) 2012-09-26 2013-09-26 IMPROVED PROCEDURES FOR ACYLATION OF MAYTANSINOL
HRP20190473TT HRP20190473T1 (hr) 2012-09-26 2013-09-26 Poboljšani postupci za aciliranje majtanzinola
BR122021022582-6A BR122021022582B1 (pt) 2012-09-26 2013-09-26 Método de preparação de intermediários na síntese de maitansinoides
RS20190314A RS58493B1 (sr) 2012-09-26 2013-09-26 Poboljšani postupak za acilaciju majtanzinola
CN201380049853.8A CN104768955B (zh) 2012-09-26 2013-09-26 用于美登醇酰化的改进的方法
SI201331374T SI2900676T1 (sl) 2012-09-26 2013-09-26 Izboljšana metoda za aciliranje majtanzinola
EP13774881.0A EP2900676B1 (en) 2012-09-26 2013-09-26 Improved method for the acylation of maytansinol
CA2884873A CA2884873C (en) 2012-09-26 2013-09-26 Improved methods for the acylation of maytansinol
AU2013323572A AU2013323572B2 (en) 2012-09-26 2013-09-26 Improved methods for the acylation of maytansinol
NZ706019A NZ706019A (en) 2012-09-26 2013-09-26 Improved methods for the acylation of maytansinol
MX2019008652A MX390615B (es) 2012-09-26 2013-09-26 Metodos mejorados para la acilacion del maitansinol.
PL13774881T PL2900676T3 (pl) 2012-09-26 2013-09-26 Ulepszony sposób acylowania majtansynolu
SM20190170T SMT201900170T1 (it) 2012-09-26 2013-09-26 Metodo migliorato per l'acilazione di maytansinolo
JP2015534641A JP6517693B2 (ja) 2012-09-26 2013-09-26 マイタンシノールをアシル化する改善された方法
ES13774881T ES2716561T3 (es) 2012-09-26 2013-09-26 Métodos mejorados para la acilación de maitansinol
MX2015003745A MX366701B (es) 2012-09-26 2013-09-26 Métodos mejorados para la acilación del maitansinol.
PL18213678T PL3486248T3 (pl) 2012-09-26 2013-09-26 Ulepszone sposoby acylacji majtansynolu
EP18213678.8A EP3486248B1 (en) 2012-09-26 2013-09-26 Improved methods for the acylation of maytansinol
BR112015006505-8A BR112015006505B1 (pt) 2012-09-26 2013-09-26 Métodos de preparo de intermediários na síntese de maitansinoides
SG11201501918UA SG11201501918UA (en) 2012-09-26 2013-09-26 Improved methods for the acylation of maytansinol
LTEP13774881.0T LT2900676T (lt) 2012-09-26 2013-09-26 Maitanzinolio acilinimo patobulintas būdas
RU2015111635A RU2648992C2 (ru) 2012-09-26 2013-09-26 Улучшенные способы ацилирования майтанзинола
ZA2015/01898A ZA201501898B (en) 2012-09-26 2015-03-19 Improved methods for the acylation of maytansinol
IL237899A IL237899A (en) 2012-09-26 2015-03-23 Methanesylene Acylation Methods
IL253988A IL253988B (en) 2012-09-26 2017-08-14 Acylation methods of maytansinol
AU2018201392A AU2018201392B2 (en) 2012-09-26 2018-02-27 Improved methods for the acylation of maytansinol
CY20191100302T CY1121415T1 (el) 2012-09-26 2019-03-13 Βελτιωμενη μεθοδος για την ακυλιωση μεϋτανσινολης
AU2020203823A AU2020203823B2 (en) 2012-09-26 2020-06-10 Improved methods for the acylation of maytansinol
CY20211100594T CY1124337T1 (el) 2012-09-26 2021-07-02 Βελτιωμενες μεθοδοι για την ακυλιωση μεϋτανσινολης
AU2022201557A AU2022201557A1 (en) 2012-09-26 2022-03-07 Improved methods for the acylation of maytansinol

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261705731P 2012-09-26 2012-09-26
US61/705,731 2012-09-26

Publications (1)

Publication Number Publication Date
WO2014052537A1 true WO2014052537A1 (en) 2014-04-03

Family

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Family Applications (1)

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PCT/US2013/061839 Ceased WO2014052537A1 (en) 2012-09-26 2013-09-26 Improved methods for the acylation of maytansinol

Country Status (27)

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US (9) US9012629B2 (cg-RX-API-DMAC7.html)
EP (3) EP3904358A1 (cg-RX-API-DMAC7.html)
JP (7) JP6517693B2 (cg-RX-API-DMAC7.html)
CN (2) CN104768955B (cg-RX-API-DMAC7.html)
AU (4) AU2013323572B2 (cg-RX-API-DMAC7.html)
BR (2) BR112015006505B1 (cg-RX-API-DMAC7.html)
CA (2) CA2884873C (cg-RX-API-DMAC7.html)
CY (2) CY1121415T1 (cg-RX-API-DMAC7.html)
DK (2) DK3486248T3 (cg-RX-API-DMAC7.html)
ES (2) ES2880754T3 (cg-RX-API-DMAC7.html)
HR (2) HRP20190473T1 (cg-RX-API-DMAC7.html)
HU (2) HUE055443T2 (cg-RX-API-DMAC7.html)
IL (2) IL237899A (cg-RX-API-DMAC7.html)
LT (2) LT3486248T (cg-RX-API-DMAC7.html)
MX (2) MX390615B (cg-RX-API-DMAC7.html)
MY (1) MY169250A (cg-RX-API-DMAC7.html)
NZ (2) NZ739573A (cg-RX-API-DMAC7.html)
PL (2) PL2900676T3 (cg-RX-API-DMAC7.html)
PT (2) PT3486248T (cg-RX-API-DMAC7.html)
RS (2) RS62075B1 (cg-RX-API-DMAC7.html)
RU (2) RU2648992C2 (cg-RX-API-DMAC7.html)
SG (1) SG11201501918UA (cg-RX-API-DMAC7.html)
SI (2) SI3486248T1 (cg-RX-API-DMAC7.html)
SM (2) SMT201900170T1 (cg-RX-API-DMAC7.html)
TR (1) TR201903625T4 (cg-RX-API-DMAC7.html)
WO (1) WO2014052537A1 (cg-RX-API-DMAC7.html)
ZA (1) ZA201501898B (cg-RX-API-DMAC7.html)

Cited By (5)

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Publication number Priority date Publication date Assignee Title
WO2016061718A1 (zh) * 2014-10-24 2016-04-28 南京联宁生物制药有限公司 一种化合物及其制备方法以及美登素dm1的制备方法
JP2018510157A (ja) * 2015-03-17 2018-04-12 レゲネロン ファーマシューティカルス，インコーポレーテッド アミノ酸アシル化試薬及びその使用方法
WO2020212256A1 (en) * 2019-04-18 2020-10-22 Indena S.P.A. Diasteroselective process for the preparation of thiol- or disulfide-containing maytansinoid esters and intermediates thereof
WO2021107133A1 (ja) 2019-11-29 2021-06-03 日本マイクロバイオファーマ株式会社 メイタンシノールの酵素的生産方法
WO2024225377A1 (ja) 2023-04-28 2024-10-31 中外製薬株式会社 Ｎ－カルボキシアミノ酸無水物を用いたアミド基含有化合物の製造方法

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EP3554544A4 (en) 2016-12-16 2020-07-29 Bluefin Biomedicine, Inc. ANTI-PROTEIN 1 ANTIBODY CONTAINING AN ANTI-CUB DOMAIN (CDCP1), ANTIBODY-DRUG CONJUGATES AND THEIR METHODS OF USE

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Cited By (7)

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WO2016061718A1 (zh) * 2014-10-24 2016-04-28 南京联宁生物制药有限公司 一种化合物及其制备方法以及美登素dm1的制备方法
CN105585579A (zh) * 2014-10-24 2016-05-18 南京联宁生物制药有限公司 一种化合物及其制备方法以及美登素dm1的制备方法
JP2018510157A (ja) * 2015-03-17 2018-04-12 レゲネロン ファーマシューティカルス，インコーポレーテッド アミノ酸アシル化試薬及びその使用方法
WO2020212256A1 (en) * 2019-04-18 2020-10-22 Indena S.P.A. Diasteroselective process for the preparation of thiol- or disulfide-containing maytansinoid esters and intermediates thereof
US11420981B2 (en) 2019-04-18 2022-08-23 Indena S.P.A. Diasteroselective process for the preparation of thiol- or disulfide-containing maytansinoid esters and intermediates thereof
WO2021107133A1 (ja) 2019-11-29 2021-06-03 日本マイクロバイオファーマ株式会社 メイタンシノールの酵素的生産方法
WO2024225377A1 (ja) 2023-04-28 2024-10-31 中外製薬株式会社 Ｎ－カルボキシアミノ酸無水物を用いたアミド基含有化合物の製造方法

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