Novel spironolactone derivatives characterized by the C.sub.11 -C.sub.12 double bond which have a potent aldosterone-antagonistic activity without causing potassium loss, used alone in diagnosis and improvement of condition of primary aldosteronism, or together with other drugs in treatment of essential or renal hypertension as well as cardiac or renal edema; prepared from 3,17-bis(ethylene-dioxy)-5,11-androstadiene.

Shionogi &amp; Co., Ltd.

Aldosterone-antagonistic steroids

The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases, nephropathy, fibrosis, primary aldosteronism or edema. The compound is of the following general formula (I): wherein R.sup.1 represents a C1-C3 alkyl group; R.sup.2 represents a hydroxy-C1-C4 alkyl group and the like; R.sup.3 represents a halogeno group, a halogeno-C1-C3 alkyl group and the like; R.sup.4 represents a hydrogen atom, a halogeno group and the like, --R.sup.5 represents a sulfamoyl group or a C1-C3 alkylsulfonyl group; R.sup.6 represents a hydrogen atom, a halogeno group and the like] or an N-oxide, atropisomer of the foregoing, or pharmaceutically acceptable salt of the foregoing. ##STR00001##

Nuss; John

Williams; Matthew

Mohan; Raju

Martin; Richard

Wang; Tie-Lin

Tsuruoka; Hiroyuki

Aoki; Kazumasa

Honzumi; Masatoshi

Asoh; Yusuke

Saito; Keiji

Homma; Tsuyoshi

Exelixis, Inc.

Daiichi Sankyo Company, Limited

1-phenylpyrrole derivatives

hyperaldosteronism

edema

hyperaldosteronism/edema

Aldosterone-antagonistic steroids

1-phenylpyrrole derivatives

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