By a News Reporter-Staff News Editor at Life Science Weekly — From Alexandria, Virginia, NewsRx journalists report that a patent by the inventors Lewis, David E. (Eau Claire, WI); Caldwell, Michael D. (Milladore, WI), filed on September 30, 2010, was published online on July 1, 2014 (see also Marshfield Clinic Health System, Inc.).
The patent’s assignee for patent number 8765982 is Marshfield Clinic Health System, Inc. (Marshfield, WI).
News editors obtained the following quote from the background information supplied by the inventors: “Various anticoagulant compositions, and in particular, warfarin, have long been utilized in different human and animal modalities, e.g., in rodent poison. However, as a result of the continued use of the compound warfarin as a rat poison, rodents have become less susceptible to the effects of warfarin.
“Therefore it is desirable to develop a composition that can be utilized either as a substitute or as a complement to existing anticoagulant compositions, such as warfarin, to increase the effectiveness of the anticoagulant.”
As a supplement to the background information on this patent, NewsRx correspondents also obtained the inventors’ summary information for this patent: “According to one aspect of the present invention, a composition has been developed that, when utilized in combination with warfarin, acts to greatly improve the anticoagulant effects of warfarin in mammalian subjects. The composition is a compound having a naphthohydroquinone ring system substantially similar to the ring system of the reduced form of vitamin K.sub.1 and has the general formula:
“##STR00002##
“where R.sub.1 and R.sub.4 are hydrogen or acyl;
“R.sub.2 is a saturated or unsaturated alkyl group with up to 6 carbons; and
“R.sub.3 is a saturated or unsaturated alkyl group with up to 20 carbons; or
“R.sub.2 and R.sub.3 are part of a cyclic or polycyclic ring system; and
“one or more hydrogen atoms of substituents R.sub.2 and R.sub.3 are replaced by a leaving group, in which the leaving group is chosen from
“an epoxide, an aziridine or N-acyl- or N-sulfonylaziridine, a halide (bromide, chloride or iodide), a sulfonate ester (methanesulfonate, benzenesulfonate, p-toluenesulfonate, p-bromobenzenesulfonate, p-nitrobenzenesulfonate, naphthalene-1-sulfonate, naphthalene-2-sulfonate);
“and in which the leaving group is located so that it is not more than four atoms removed from the closest carbon atom of the naphthalene ring;
“and which is capable of being oxidized in the presence or absence of an enzyme such as the vitamin K-dependent gamma-glutamyl carboxylase to give a structural analogue of vitamin K 2,3-epoxide that is capable of binding to the enzyme VKORC-1 in the vitamin K 2,3-epoxide binding site in the presence of warfarin.
“Numerous additional aspects, features and advantages of the present invention will be made apparent from the following drawing figures taken together with the detailed description.”
For additional information on this patent, see: Lewis, David E.; Caldwell, Michael D.. Synergistic Anticoagulant Composition. U.S. Patent Number 8765982, filed September 30, 2010, and published online on July 1, 2014. Patent URL: http://patft.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PALL&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&r=1&f=G&l=50&s1=8765982.PN.&OS=PN/8765982RS=PN/8765982
Keywords for this news article include: Marshfield Clinic Health System Inc.
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