Sulfated bis-cyclic agents

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C546S139000, C546S146000

Reexamination Certificate

active

10556906

ABSTRACT:
Sulfated bis-cyclic compounds that are potent anticoagulants and methods for their manufacture are provided. The sulfated compounds are bis-cyclic moieties comprised of an isoquinoline ring joined to a phenyl ring with the general chemical structure formula (I) where R2is hydrogen or a sulfate moiety, R3is either hydrogen or carboxylate moiety; R4is a hydrogen or oxygen; and R5is a hydrogen if R4is a hydrogen, and is absent if R4is oxygen. Counterions such as sodium may also be coordinated to the sulfate and carboxylate moieties.

REFERENCES:
patent: 5578729 (1996-11-01), Bringmann et al.
patent: 6849644 (2005-02-01), Bromidge et al.
Gunnarsson et al., “Designing Small, Nonsugar Activators of Antithrombin Using Hydrophathic Interaction Analyses”, J. Med. Chem, 2000 vol. 45, pp. 1233-1243.
Gannarsson et al., Interaction of designed Sulfated Falvanoids with Antithrombin: Lessons on the Design of Organic Activators; J. Med. Chem,; 2002, vol. 45, pp. 4460-4470.

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