Abstract: The present invention relates to novel 4-pregenen-11?-17-21-triol-3,20-dione derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals, as modulators of glucocorticoid or mineralocorticoid receptors. The invention relates specifically to the use of these compounds and their pharmaceutical compositions to treat disorders associated with glucocorticoid or mineralocorticoid receptor modulation.

Abstract: Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering compounds of the general formula: wherein the variables are defined in the specification.

Abstract: The invention relates to a method for representing compounds of the general formula (1). The invention further relates to the hitherto unknown compounds of general formulas (5, 6 and 7) in the form of intermediate products and to the use of 4,4-dimethyl-3&bgr; hydroxypregna-8,14-diene-21-carboxylic acid esters of the general formula (1) for producing 4,4-dimethyl-5&agr;-cholesta-8,14,24-triene-3&bgr;-ol (2).

Abstract: The invention relates to 20&xgr;-fluoropregna-4,17(20)-dien-3-on-21-oic acid ethyl ester, 20&xgr;-fluoro-3&bgr;-hydroxypregna-5,17(20)-dien-21-oic acid ethyl ester, 20&xgr;-fluoro-21-hydroxypregna-4,17 (20)-dien-3-one, 20&xgr;-fluoropregna-5,17(20)-dien-3&bgr;,21-diol and related compounds and to compositions incorporating these compounds, as well as the inhibition of C17,20 lyase, 5&agr;-reductase and C17-hydroxylase, and to the use of these compounds in the treatment of androgen and estrogen mediated or dependent disorders, including benign prostatic hyperplasia, prostate cancer, breast cancer and DHT-mediated disorders such as acne and hirsutism. Treatment of disorders related to the over synthesis of cortisol, for example, Cushing's Syndrome are also included. The treatment of androgen-dependent disorders also includes a combination therapy with known androgen-receptor antagonists, such as flutamide.

Abstract: The invention relates to a method of altering hypothalamic function in an individual. The method comprises nasally administering a human vomeropherin, e.g. a pregnane or cholane steroid, or a pharmaceutical composition containing a vomeropherin, such that the vomeropherin binds to a specific neuroepithelial receptor. The steroid or steroids is/are preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers. Other embodiments of the invention include pharmaceutical compositions containing the steroids.

Abstract: Disclosed are novel classes of anti-androgens including dihydrophenanthrene derivatives, their method of synthesis and their use in treating disorders associated with excessive androgenic activities.

Abstract: A method for the preparation of a steroidal allylic tertiary alcohol is disclosed which involves the deprotonation of a sulfoxide with a strong base which is capable of deprotonating the methine proton which is .alpha. to the sulfoxide, in an inert solvent to give the anion; reaction of the anion with a steroidal spiro-2'-oxirane to give a steroidal .gamma.-hydroxysulfoxide; and thermolysis in the presence of a base other than calcium carbonate to give the steroidal allylic tertiary alcohol.

Abstract: There are disclosed a process for producing an .alpha.-acyloxy-.alpha.,.beta.-unsaturated carbonyl compound represented by the general formula (VI): ##STR1## wherein R.sub.1, R.sub.2 and R.sub.4 are independently hydrogen atoms or substituted or unsubstituted hydrocarbon residues, or R.sub.1 and R.sub.2, when taken together with one another in an optional combination, form a ring, R.sub.3 is a substituted or unsubstituted hydrocarbon residue, and indicates that the configuration may be either E-configuration or Z-configuration, in particular, a 20-acyloxy-17(20)-methylen-21-al-steroid represented by the partial structural formula (II): ##STR2## wherein R is a hydrocarbon residue, and indicates that the configuration of the acyloxy group and the formyl group bonded to the carbon atom at the 20-position may be either E-configuration or Z-configuration, which comprises oxidizing a propargyl ester represented by the general formula (V): ##STR3## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.

Abstract: Invented are carboxyl and carboxyl alkyl ester substituted 11-keto and hydroxy analogues of synthetic steroidal compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase.

Abstract: A 11.beta.-aryl-19-norprogesterone steroid of the formula: ##STR1## wherein (i) R.sup.1 is H, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, OH, OC(O)CH.sub.3, or OC(O)R.sup.5, wherein R.sup.5 is C.sub.2-8 alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl or aryl, R.sub.2 is H, R.sup.3 is H, C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl, R.sup.4 is H, CH.sub.3, F or Cl, R.sup.6 is H, (CH.sub.3).sub.2 N, CH.sub.3 O, CH.sub.3 CO, CH.sub.3 S, CH.sub.3 SO, CH.sub.3 SO.sub.2, and X is O or NOCH.sub.3 ; or(ii) R.sup.1 and R.sup.2 taken together are a carbon-carbon bond and R.sup.3, R.sup.4, R.sup.6 and X are as defined above; or(iii) R.sup.1 and R.sup.3 taken together are --CH.sub.2 -- or --N.dbd.N--CH.sub.2 --, R.sup.2 is H and R.sup.4, R.sup.6 and X are as defined above; or(iv) R.sup.2 and R.sup.3 taken together are .dbd.CH.sub.2 and R.sup.1, R.sup.4, R.sup.6 and X are as defined above.

Abstract: Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutial compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase including using these compounds to reduce prostate size. Also invented are intermediates used in preparing these compounds.