Ng-monomethyl-l-arginine hydrochloride derivatives and their use

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...

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562560, A01N 3710, C07C24100

Patent

active

058831304

ABSTRACT:
Crystalline N.sup.G -monomethyl-L-arginine hydrochloride is disclosed. At least three distinguishable isomorphic forms are present. The solid salt can be made by dissolving N.sup.G -monomethyl-L-arginine in hydrochloric acid and crystallising out N.sup.G -monomethyl-L-arginine hydrochloride. The crystallising step requires several months at low temperature. However, the process can be facilitated by seeding with crystals of N.sup.G -monomethyl-L-arginine hydrochloride. Alternatively, crystalline N.sup.G -monomethyl-L-arginine hydrochloride can be prepared by dissolving a salt of N.sup.G -monomethyl-L-arginine other than the hydrochloride salt with hydrochloric acid and removing the original salt forming ion by crystallising out the hydrochloride salt.

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Kilbourn et al Proc. Natl. Acad. Sci. USA; vol. 87, pp. 3629-3632; May 1990 NG-Methyl-L-arginine inhibits tumor necrosis factor-induced hypotension: Implications for the involvement of nitric oxide.
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Prabhakaran et al J.Am. Chem. Soc. 1988, 110, 5785-5791 Biosynthesis of Blasticidin S from L-.alpha.-Arginine etc.
546C88 for Septic Shock -Study termination Apr. 24, 1998 London.
Scrip Display Apr. 27, 1998 Glaxo Wellcome hits problems in sepsis.

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