Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1999-10-28
2000-12-26
Carr, Deborah D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
514144, 514557, A01N 3312
Patent
active
061660892
ABSTRACT:
The invention relates to a pharmaceutically acceptable prodrug which is a covalent conjugate of a pharmacologically active compound and an intracellular transporting adjuvant, characterized by the presence of a covalent bond which is scission-sensitive to intracellular enzyme activity. The prodrug may be used in a technique for treating a condition or disease in a mammal related to supranormal intracellular enzyme activity, whereby on administering it to a human having such condition or disease, the bond is broken in response to such activity, and the pharmacologically active compound is activated selectively within cells having such supranormal intracellular enzyme activity.
REFERENCES:
patent: 4654370 (1987-03-01), Marriott, III et al.
patent: 5149794 (1992-09-01), Yatvin et al.
patent: 5227514 (1993-07-01), Meul et al.
Hadad, S., et al., Pharmacokinetic Analysis and Anticonvulsant Activity of Two Polysteric Prodrugs of Valproic Acid, Biopharmaceutics & Drug Disposition, vol. 14, pp. 51-59 (1993).
Mergen, F., et al., Antiepileptic activity of 1,3-dihexadecanoylamino-2valproyl-propan-2-ol, a Prodrug of Valproic Acid Endowed with a Tropism for the Central Nervous System, J. Pharm.Pharmacol., vol. 43, pp. 815-816 (1991).
NITS Technical Notes. No. 9, 1984, "Prodrugs based on phpospholipid-nucleoside conjugates" Springfield, VA, p. 630.
Stuttgart, DE, Geb. 1992; European J. of Pharmaceutics and Biopharmaceutics, 38(1):1-6. O. Vaizoglu et al., Jul. 26, 1989, EP-A-0325 160 (Hoechst A.G.).
Hostetler et al., Jun. 1991, "Phosphatidylaazothymidine. Mechanism of antiretroviral action in cem cells." J. Biol. Chem. 266(18):11714-11715.
Gusovsky et al., Feb. 1990, "Mechanism of maitotoxin-stimulated phosphoinositide breakdown in HL-60 cells." J. Pharmacol. Ex. Ther. 252(2):469-470.
Govez-Cambronero et al., Apr. 1991, "Platelet-activating induces tyrosine phossssphorylation in human neutrophils." J. Biol. Chem. 266(10):6240-5.
Natarajan et al. "Activation of endothelial cell phospholipase D by hydrogen peroxide and fatty acid hydroperoxide." J. Biol. Chem 268(2):930-7.
Coorsen et al., "GTP.gamma.S and phorbol ester act synergistically to stimulate both calcium independent secretion and phospholipase D activity in permeabilized human platerits. Inhibition by BAPTA and analogs" FEBS Lett. 316(2):170-4.
Duan et al., Feb. 1994, "Conversion to CA(2+)-independent form of Ca2+/calmodulin protein kinase II in rat pancreatic acini." Biochem. Biophys. Res. Commun. 199(1):368-373.
Carr Deborah D.
D-Pharm Ltd.
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