Cyclic hydrocarbons with an aminoalkyl sidechain

Details Cyclic hydrocarbons with an aminoalkyl sidechain Cyclic hydrocarbons with an aminoalkyl sidechain

1992-11-06

1993-12-28

Cintins, Marianne M.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

552522, C07J 4300, C07J 4100

Patent

active

052740897

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:
patent: 3284475 (1966-11-01), Klimstra
patent: 3326758 (1967-06-01), Irmscher et al.
patent: 3370070 (1968-02-01), Klimstra et al.
patent: 4239780 (1980-12-01), Wallach
patent: 4330539 (1982-05-01), Sleigh et al.
patent: 5187299 (1993-02-01), Johson et al.
Vogt, W., "Role of Phospholipase A.sub.2 in Prostaglandin Formation", Advances in Prostaglandins and Thromboxane Research, 3, p. 89 (1978).
Isakson, P. C. et al., "Lipases and Prostaglandin Biosynthesis", Advances in Prostaglandin and Thromboxane Research, 3, p. 113, (1978).
Plummer, N. A., et al., "Activation of the Arachidonate Cascade in Human Skin Inflamed by Irradiation with UVC and the Effects of Indomethacin", abstracted in Journal of Investigative Dermatology, 68, p. 246 (1977).
Vargaftig, B. B., "Carrageenan and thrombin trigger prostaglandin synthetase-independent aggregation of rabbit platelets: inhibition by phospholipase A.sub.2 inhibotors", 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 (1974).
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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