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.:
Date of Patent:
May. 11, 1993
Filed:
Aug. 26, 1992
Sherman T Waddell, Westfield, NJ (US);
Timothy A Blizzard, Rahway, NJ (US);
Merck & Co., Inc., Rahway, NJ (US);
Abstract
A method of making compounds of the formulae: ##STR1## wherein X is ##STR2## R.sup.1 is hydrogen, methyl, C.sub.1-10 alkoxycarbonyl or arylsulfonyl when X is CH.sub.3 CH.sub.2 CHNH.sub.2 and is additionally aralkoxycarbonyl when X is NH.sub.2 ; one of R.sup.2 and R.sup.3 is hydrogen and the other is OH, NHR.sup.1 or NMeR.sup.1 where R.sup.1 is as defined above; R.sup.4 is hydrogen or C.sub.1-10 alkyl when X is CH.sub.3 CH.sub.2 CHNH.sub.2 and is additionally aralkyl when X is NH.sub.2 ; R.sup.5 is hydrogen or C.sub.1-3 alkyl when X is CH.sub.3 CH.sub.2 CHNH.sub.2 ; R.sup.5 is hydrogen when X is NH.sub.2 ; one of R6 and R7 is hydrogen and the other is methyl except when X is CH.sub.3 CH.sub.2 CHNH.sub.2 and R.sup.2 is H, in which case R.sup.6 is methyl and R.sup.7 is hydrogen. These compounds are made from erythromycin-derived fragments of the formulae: ##STR3## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are defined as before for when X is NH.sub.2 ; R.sup.5 is hydrogen or C.sub.1-3 alkyl; if R.sup.5 is hydrogen, then R.sup.6 is methyl and R.sup.7 is hydrogen and the two structures above exist in equilibrium with each other; if R.sup.5 is alkyl, then one of R.sup.6 and R.sup.7 is hydrogen and the other is methyl and the compound exists only as the structure on the above left.