Abstract: The present invention is directed to a method of using a certain compounds which are 2,19-methyleneoxy or 2,19 methylenethio bridged steroids, and related steroidal compounds as inhibitors of the enzyme steroid aromatase, 19-hydroxylase and as treatment for various estrogen dependent/mediated disorders including hormonal dependent breast cancer.

Abstract: The present invention is directed to a method of using a certain compounds which are 2,19-methyleneoxy or 2,19 methylenethio bridged steroids, and related steroidal compounds as inhibitors of the enzyme steroid aromarase, 19-hydroxylase and as treatment for various estrogen dependent/mediated disorders including hormonal dependent breast cancer.

Abstract: This invention is directed to 4-amino-17.beta.-(cyclopropyloxy)androst-4-en-3-one, 4-amino-17.beta.-(cyclopropylylamino)androst-4-en-3-one and related compounds, a process for their synthesis, a pharmaceutical composition having C.sub.17-20 lyase and 5.alpha.-reductase inhibitory activity, the use of the present compounds as C.sub.17-20 lyase and 5.alpha.-reductase inhibitors and also to a method for using such compounds in the treatment of androgen and/or estrogen dependent disorders, including bengin prostatic hyperplasia, breast cancer and prostatic cancer. The 4-amino compounds are prepared by the reaction of the appropriate 4,5-epoxide with sodium azide in an inert solvent in the presence of a catalytic amount of strong acid under appropriate reaction conditions. Alternatively, the 4-amino compounds are prepared by first nitration and then reduction of the appropriate steroid under appropriate reaction conditions.

Abstract: The present invention is directed to a group of compounds which are haloethyl substituted steroidal enzyme inhibitors. These compounds are useful as aromatase, 19-hydroxylase, and aldosterone biosynthesis inhibitors and they are prepared from the corresponding epoxide.

Abstract: The present invention is directed to a group of androstane compounds which contain an ethylene radical bridging the 2- and 19-positions. These compounds are useful as aromatase inhibitors and they are prepared by the cyclization of a 19-[2-(4-toluenesulfonyloxy)ethyl]androst-4-ene-3,17-dione using a strong base.

Abstract: The present invention is directed to 2.beta.,19-(methyleneamino)androst-4-ene-3,17-dione which has the formula ##STR1## and the corresponding 17.beta.-ol which are useful as aromatase inhibitors. The compounds are prepared by the cyclization of an appropriate 19-[N-protected-[(2-methoxyethoxy)methylamino] steroid using titanium tetrachloride followed by, if desired, selective reduction of the 17-ketone.

Abstract: The present invention is directed to a group of compounds which are 2,19-methylenoxy or 2,19-methylenethio bridged steroids, and related steroidal compounds. These compounds are useful as aromatase and 19-hydroxylase inhibitors.

Abstract: The present invention is directed to a method for the treatment of hyperaldosteronism and related disorders which comprises administering to an appropriate patient an appropriate 18-cyanopregnane.

Abstract: The present invention is directed to a method for the treatment of hyperaldosteronism and related disorders which comprises administering to an appropriate patient an appropriate 17.beta.-cyclopropylaminoandrostene.

Abstract: 19-Fluoro- and cyano- substituted 21-hydroxyprogesterone derivatives and related compounds which are active as 19-hydroxylase inhibitors and useful as antihypertensive agents are described herein. The compounds are prepared using appropriate synthetic pathways which will vary according to the nature of the specific 19-substituted progesterone or related compound desired.

Abstract: 19-Substituted progesterone derivatives and related compounds which are active as 19-hydroxylase inhibitors and useful as antihypertensive agents are described herein. The compounds are prepared using appropriate synthetic pathways which will vary according to the nature of the specific 19-substituted progesterone or related compound desired.

Abstract: The present invention is directed to a group of compounds which are 3.beta.,17.beta.-hydroxy steriods, and related steroidal structures. These compounds are armatase inhibitors, and thus, regulate or inhibit the conversion of androgens to estrogens. These compounds may be utilized to treat conditions potentiated by the presence of estrogens. These compounds exhibit a slower onset of action and a longer half life relative to the 10-(2-alkynyl) steroidal aromatase inhibitors disclosed in U.S. Pat. No. 4,322,416.

Abstract: Aromatase inhibitors are provided having the formula ##STR1## wherein represents a single or double bond; R is hydrogen or C.sub.1-4 alkyl; R.sup.1 is methyl or ethyl; R.sup.2 is (H) (OR.sup.8) or .dbd.O; R.sup.3 is H or C.sub.1-3 alkyl; R.sup.4 is H or OR.sup.8 ; R.sup.5 is H, C.sub.1-3 alkyl or, when the 5,6-bond is saturated, R.sup.5 is divalent .dbd.O; R.sup.6 and R.sup.7 are each H or C.sub.1-3 alkyl; and R.sup.8 is H or C.sub.2-4 alkanoyl. Intermediates useful in preparing the foregoing aromatase inhibitors, and methods of using the aromatase inhibitors of the invention are also provided.

Abstract: Progesterone derivatives having a vinylidene or a 1-alkynyl substituent at the 18-position and further optionally hydroxylated at the 11-position and the 21-position are described herein. Compounds having both an ethynyl substituent and a hydroxy substituent at the 18-position are also described herein. The compounds are useful as aldosterone inhibitors.

Abstract: Irreversible aromatase inhibitors are provided having the formulae ##STR1## wherein represents a single or a double bond; R.sup.1 is CH.sub.3 or C.sub.2 H.sub.5 ; R.sup.2 is (H) (OR.sup.8) or O; R.sup.3 is H or C.sub.1-3 alkyl; R.sup.4 is H or OR.sup.8 ; R.sup.5 is H.sub.2, O or (H) (C.sub.1-3 alkyl); R.sup.6 and R.sup.7 are each independently H or C.sub.1-3 alkyl; and R.sup.8 is H or C.sub.1-4 alkanoyl. Intermediates useful in preparing the foregoing aromatase inhibitors, methods of using them and a pharmaceutical composition containing them are also provided.