Methods of treating cataracts and diabetic retinopathy with...

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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C514S292000, C514S912000

Reexamination Certificate

active

06916824

ABSTRACT:
Water-soluble, cell permeable aldose reductase inhibitors are presented. These compounds prevent the effects of galactosemia in patients. The compounds prevent both the accumulation of polyols and the change in levels of protein kinase C gamma observed during diabetes and galactosemia.

REFERENCES:
patent: 5958970 (1999-09-01), Hua et al.
Aiello et al., (Mar. 1999), “Amelioration of Abnormal Retinal Memodynamics by a Protein Kinase C β-Selective Inhibitor (LY33531) in Patients with Diabetes: Results of a Phase I Safety and Pharmacodynamic Clinical Trial,”IVOS40:S192.
Cervera et al., (1990), “4-Amino-6-Methyl-2H-Pyran-2-One. Preparation and Reactions with Aromatic Aldehydes,”Tetrahedron46:7885-7892.
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Hua et al., (1997), “(5aS,7S)-7-Isopropenyl-3--methyl-5a,6,8,9-tetrahedro-1H,7H-pyrano[4,3-b][1]benzopyran-1-one,”Acta CrystC53:1995-1997.
Hua et al., (1997), A One-Pot Condensation of Pyrones and Enals. Synthesis of 1H,7H-5a,6,8,9-Tetrahydro-1-oxopyrano[4,3-b]benzopyrans.J. Org. Chem.62:6888-6896.
Urzhumtsev et al., (1997), “A ‘specificity’ pocket inferred from the crystal structures of the complexes of aldose reductase with the pharmaceutically important inhibitors tolrestat and sorbinil,”Structure5:601-612.
Vedejs et al., (1978), “Transition-Metal Peroxide Reaction. Synthesis of α-Hydroxycarbonyl Compounds from Enolates,”J. Org. Chem.43:188-196.
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