Anti-androgenic cyclo and bicyclo alkenes

Organic compounds -- part of the class 532-570 series – Organic compounds – Carboxylic acid esters

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C07C 6702, A61K 3112, A61K 3122

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active

052646190

ABSTRACT:
Compounds having the formula (i), (ii) and (iii), ##STR1## where R is H, alkyl of 1 to 6 carbons, or CO--R.sub.2 where R.sub.2 is alkyl of 1 to 6 carbons; R.sub.1 is H, CH.sub.3, or (CH.sub.2).sub.m --CH.sub.3 ; n is an integer having the values of 2 to 10, m is an integer having the values of 1 to 6, have anti-androgen activity on secondary androgen receptor sites. The compounds are useful for treating mammals, including humans afflicted with acne, male pattern baldness, adhesions and keloids. The compounds are also effective for treating other diseases or conditions which are related to androgen receptors, such as undesirable formation of breast capsules in females after breast augmentation surgery, osteoarthritis and symptoms of Alzheimer's disease. The compounds also have inhibitory effect on the metabolism of certain microorganisms and fungi of the kind, the metabolism of which is normally known to be controllable by anti-androgen compounds.

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King, et al, "Increased Androgen Binding in Keloids and Its Inhibition with Cyoctol", Recent Advances in Chemotherapy, Antimicrobial Section 1 14th International Congress of Chemotherapy, Kyoto, 1985, pp. 259-260.
Ford, et al, "Dense Intraabdominal Adhesions: A Manifestation of Localized, Hyper-Androgen Receptors", Recent Advances in Chemotherapy Antimicrobinal Sect. 1, 14th International Congress of Chemotherapy, Kyoto, 1985, pp. 265-266.
Ford, et al., "Increased Androgen Binding in Keloids: A Preliminary Communication", J. Dermatol, Surg. Oncol., 9:7 Jul. 1983, pp. 545-547.
Hammill, et al., "A Rat Model of Unilateral Utero-Tubo-Ovarian Abscess", Reviews of Infectious Diseases, vol. 6, Supplement, Mar.-Apr. 1984, pp. 896-900.

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