Cyclic hydrocarbons with an aminoalkyl sidechain

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

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546333, 564460, 540107, 514357, 514172, C07D21338, C07D31350, A61K 3158, A61K 3144

Patent

active

051965429

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: 3370070 (1968-02-01), Klimstra et al.
patent: 4239780 (1980-12-01), Wallach
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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 Inhibitors", J. Pharm. Pharmacol., 29, pp. 222-228.
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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