Steroid compounds

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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540106, C07J 4300, C07J 4100

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active

053730950

ABSTRACT:
Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.

REFERENCES:
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patent: 3370070 (1968-02-01), Klimstra et al.
patent: 4000125 (1976-12-01), Casagrande et al.
patent: 4239780 (1980-12-01), Wallach
patent: 5075434 (1991-12-01), Youngdale
Isakson, P. C. et al., "Lipases and Prostaglandin Biosynthesis", Advances in Prostaglandin and Thromboxane Research, 3, p. 113, (1978).
Vargaftig, B. B., "Carrageenan and thrombin trigger prostaglandin synthetase-independent aggregation of rabbit platelets: inhibition by phospholipase A.sub.2 inhibitors", J. Pharm. Pharmacol., 29, pp. 222-228 (1977).
Flower, R. J. and Blackwell, G. J., "Anti-inflammatory steroids induce biosynthesis of a phospholipase A.sub.2 inhibitor which prevents prostaglandin generation", Nature, 278, pp. 456-459 (1979).
Kaplan, K. L., et al., "Low concentrations of indomethacin inhibit phospholipase A.sub.2 of rabbit polymorphonuclear leukocytes", Proc. Natl. Acad. Sci., 75, pp. 2955-2988 (1978).
Vallee, E., et al., "Anti-inflammatory and platelet anti-aggregant activity of phospholipase-A.sub.2 inhibitors", J. Pharm. Pharmacol., 31, pp. 588-592 (1979).
Roberts, M. F., et al., "Chemical Modification of the Histidine Residue in Phospholipase A.sub.2 ", J. of Biol. Chem., 252, pp. 2405-2411 (1977).
Blackwell, G. J., et al., "Phospholipase A.sub.2 Activity of Guinea-Pig Isolated Perfused Lungs: Stimulation, and Inhibition by Anti-Inflammatory Steroids", British J. Pharmacy, 62, pp. 79-89 (1978).
Wallach, D. P. and Brown, V. J. R., "Studies on the Arachidonic Acid Cascade-I", Bioch. Pharmacol., 30, pp. 1315-1324 (1981).
Doctoral thesis, L. J. Griggs, "Part I. Synthetic Approaches to 6- and 16-Thiaestrone. Part II. Estrone with a Diazacholesterol Side Chain," University of Michigan (1965).
Klimstra, P. D., et al., "Hypocholesterolemic Agents. VI. A- and B-Ring-Modified Azacholesterols", J. Med. Chem., 9, pp. 323-326 (1966).

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