The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Aug. 23, 2022

Filed:

Apr. 09, 2020
Applicant:

Indena S.p.a., Milan, IT;

Inventors:

Gabriele Fontana, Milan, IT;

Ruggero Beretta, Milan, IT;

Maurizio Taddei, Siena, IT;

Salvatore Princiotto, Milan, IT;

Assignee:

Indena S.P.A., Milan, IT;

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
C07D 498/18 (2006.01); C07D 498/12 (2006.01);
U.S. Cl.
CPC ...
C07D 498/12 (2013.01);
Abstract

The invention discloses a process for the preparation of maytansinoid esters of formula (I) comprising a thiol or disulphide group wherein R, Rand Rand the asterisk are as defined in the description, by reacting maytansinol with an enantiopure alpha-azido acid, followed by reduction of the azido group and reacting the obtained amino-ester with a compound of formula (IX) (IX) R—S—S—X—COOH wherein X and Rare as defined in the description, or with a reactive derivative thereof and optionally reducing the obtained disulfide-containing maytansinoid ester to give a maytansinoid ester wherein Ris a —X—SH group.


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