12 (S)--hete receptor blockers

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

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514560, 514732, 4242541, A61K 3141

Patent

active

060462248

ABSTRACT:
The 12-lipoxygenase product, 12(S)-HETE, mediates hyperproliferative and hyperplastic responses seen in atherosclerosis, diabetes, Parkinson's disease, Alzheimer's, stroke-induced nerve damage and cancer. 12-HETE also mediates inflammation and cell death in some cell systems, particularly B-islet cells of the pancreas. The present invention involves amelioration of disease states mediated by 12(S)-HETE by blocking specific 12(S)-HETE receptors.

REFERENCES:
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patent: 5795914 (1998-08-01), Konno et al.
Arenberger, P., et al., "The Lipoxygenase Inhibitor 2-phenylmethyl-1-naphthol (DuP 654) is a 12(S)-Hydroxyeicosatetraenoic Acid Receptor Antagonist in the Human Epidermal Cell Line SCL-II" Skin Pharmacol. 6:148-151 (1993).
Bleich et al. "The Stress-activated C-jun Protein Kinase (JNK) Is Stimulated by Lipoxygenase Pathway Product 12-HETE in RIN m5F Cells" Biochem. Biophys. Res. Commun. 230:448-451 (1997).
Wen et al. "Mechanisms of ANG II-Induced Mitogenic Responses: Role of 12-lipoxygenase and Biphasic MAP Kinase" Am. J. Physiol. 271 (Cell Physiol. 40): C1212-C1220 (1996).
Natarajan, R. et al., "Mechanism of Angiotensin-II-Induced Proliferation in Bovine Adrenocortical Cells" Endocrinology, 131(3):1174-1180 (Sep. 1992).
PCT International Search Report in the corresponding international application.

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