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:
Apr. 01, 2014

Filed:

Dec. 22, 2008
Applicants:

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

Ross A. Miller, Fanwood, NJ (US);

Peter E. Maligres, Fanwood, NJ (US);

Steven Weissman, Short Hills, NJ (US);

Inventors:

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

Ross A. Miller, Fanwood, NJ (US);

Peter E. Maligres, Fanwood, NJ (US);

Steven Weissman, Short Hills, NJ (US);

Assignee:

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

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
C07D 239/52 (2006.01); C07D 413/12 (2006.01);
U.S. Cl.
CPC ...
Abstract

Processes for preparing certain N-arylalkyl-1-(alkyl or aralkyl)-2-acylaminoalkyl-5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamides are disclosed. In one embodiment, the process comprises acylating the free amine in the corresponding N-arylalkyl-1-(alkyl or aralkyl)-2-aminoalkyl-5-ester protected hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamide and then deprotecting the 5-hydroxy by base hydrolysis. The hydroxypyrimidinone carboxamide products of the process are HTV integrase inhibitors which are useful for treating HTV infection, treating AIDS, or delaying the onset or progression of AIDS. Certain esterified N-arylalkyl hydroxypyrimidinone carboxamides that can be employed as process intermediates are also disclosed.


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