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:
Feb. 21, 2023

Filed:

Apr. 18, 2019
Applicants:

Merck Sharp & Dohme Corp., Rahway, NJ (US);

Werthenstein Biopharma Gmbh, Werthenstein, CH;

Inventors:

Kevin M. Maloney, Metuchen, NJ (US);

Kallol Basu, Hillsborough, NJ (US);

Michael James Di Maso, Hamilton, NJ (US);

Guy R. Humphrey, Hillsborough, NJ (US);

Alfred Y. Lee, Robbinsville, NJ (US);

Feng Peng, Dayton, NJ (US);

Hong Ren, Green Brook, NJ (US);

Siwei Zhang, Westfield, NJ (US);

Assignees:

Merck Sharp & Dohme LLC, Rahway, NJ (US);

Werthenstein BioPharma GmbH, Werthenstein, CH;

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
C07D 239/48 (2006.01); C07C 41/09 (2006.01); C07C 41/30 (2006.01); C07C 253/30 (2006.01); C07D 487/18 (2006.01);
U.S. Cl.
CPC ...
C07D 239/48 (2013.01); C07C 41/09 (2013.01); C07C 41/30 (2013.01); C07C 253/30 (2013.01); C07D 487/18 (2013.01); C07B 2200/13 (2013.01);
Abstract

Disclosed herein is a novel process for preparing Compound A free base, 5-((2,4-diaminopyrimidin-5-yl)oxy)-4-iso-propyl-2-methoxybenzenesulfonamide, and a citrate salt of Compound A with simplified chemistry and a high overall yield: Compound A. In one embodiment, the overall yield from the starting material 2-isopropylphenol to Compound A citrate salt is greater than 50%. In another embodiment, the overall yield is greater than 60%. Also disclosed herein are novel salts and solvates of Compound A.


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