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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.

Patent No.:

US 12071421 B1

PDFFull Text
Date of Patent:
Aug. 27, 2024

Filed:

Mar. 21, 2022

Process for the synthesis of substituted chloromethyl dialkylphosphates

Applicant:

Helsinn Healthcare SA, Lugano/Pazzallo, CH;

Inventors:

Luca Fadini, Giubiasco, CH;

Peter Manini, Giubiasco, CH;

Claudio Pietra, Como, IT;

Claudio Giuliano, Como, IT;

Emanuela Lovati, Mendrisio, CH;

Roberta Cannella, Varese, CH;

Alessio Venturini, Varese, IT;

Valentino J. Stella, Lawrence, KS (US);

Assignee:

Helsinn Healthcare SA, Lugano/Pazzallo, CH;

Attorney:

Clark G. Sullivan

Primary Examiner:

Douglas M Willis

Int. Cl.
CPC ...
C07D 401/04 (2006.01); A61K 9/00 (2006.01); A61K 31/4178 (2006.01); A61K 31/439 (2006.01); A61K 31/44 (2006.01); A61K 31/473 (2006.01); A61K 31/496 (2006.01); A61K 31/56 (2006.01); A61K 31/573 (2006.01); A61K 31/675 (2006.01); A61K 45/06 (2006.01); A61P 1/08 (2006.01); A61P 13/10 (2006.01); A61P 25/22 (2006.01); A61P 25/24 (2006.01); C07D 213/74 (2006.01); C07D 213/76 (2006.01); C07D 213/89 (2006.01); C07F 9/02 (2006.01); C07F 9/6509 (2006.01);
U.S. Cl.
CPC ...
C07D 401/04 (2013.01); A61K 9/0019 (2013.01); A61K 31/4178 (2013.01); A61K 31/439 (2013.01); A61K 31/44 (2013.01); A61K 31/473 (2013.01); A61K 31/496 (2013.01); A61K 31/56 (2013.01); A61K 31/573 (2013.01); A61K 31/675 (2013.01); A61K 45/06 (2013.01); A61P 1/08 (2018.01); A61P 13/10 (2018.01); A61P 25/22 (2018.01); A61P 25/24 (2018.01); C07D 213/74 (2013.01); C07D 213/76 (2013.01); C07D 213/89 (2013.01); C07F 9/025 (2013.01); C07F 9/650952 (2013.01);
Abstract

Disclosed are compounds including phosphate and N-oxide prodrugs of the NK1 antagonist netupitant, useful in the prevention and/or treatment of diseases including emesis induced by chemotherapy. Also disclosed are methods of making a di-tert-butyl (chloromethyl) phosphate useful in the manufacture of such prodrugs by reacting a dialkylphosphate salt with an acid to obtain the corresponding ester of phosphoric acid, reacting the ester with a quaternary ammonium hydroxide base to form a monobasic salt, and reacting the monobasic salt with chloroiodomethane to form the corresponding chloromethyl dialkyl phosphate.

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