Abstract: The present invention refers to a new process for the synthesis of (9?,10?)-pregn-4-ene-3,20-dione, commonly known as retroprogesterone, having the formula (1) shown below.

Abstract: The present invention provides therapeutically active compounds and compositions as NMDA and MC receptor antagonists, which are useful in treating central nervous system disorders by over-activation of NMDA and/or MC receptors. In one aspect, the present invention provides methods of enhancing brain's cognitive function and reducing neuronal cell death in mammals and humans.

Abstract: Steroid compounds having increased resistance against metabolism and increased water solubility are disclosed, together with methods for their production. These substances are suitable for the manufacture of pharmaceuticals for the treatment of steroid related or steroid induced CNS disorders and for use in methods of prevention, alleviation or treatment of such disorders.

Abstract: Steroid compounds having increased resistance against metabolism and increased water solubility are disclosed, together with methods for their production. These substances are suitable for the manufacture of pharmaceuticals for the treatment of steroid related or steroid induced CNS disorders and for use in methods of prevention, alleviation or treatment of such disorders.

Abstract: The invention relates to methods to manipulate stem cells in vivo and in vitro to treat, e.g., a condition where cell or tissue repair is needed.

Abstract: The present invention relates to a compound of formula (I): for its use as progesterone receptor antagonist, in particular for its use for the prevention and/or the treatment of cancer or uterine pathologies.

Abstract: Applicants have discovered a method for the stereoselective and regioselective synthesis of 3?-hydroxy, 3?-methyl-5?-pregnan-20-one (ganaxolone) comprising reacting 5?-pregnane-3,20-dione; with an organometallic methylating agent in an inert solvent to provide a compound of the formula

Abstract: Applicants have discovered a method for the stereoselective and regioselective synthesis of 3?-hydroxy, 3?-methyl-5?-pregnan-20-one (ganaxolone) comprising reacting 5?-pregnane-3,20-dione; with an organometallic methylating agent in an inert solvent to provide a compound of the formula

Abstract: The present invention provides therapeutically active compounds and compositions as NMDA and MC receptor antagonists, which are useful in preventing and treating central nervous system disorders by inhibiting over-activation of NMDA and/or MC receptors. In one aspect, the present invention provides methods of treating and/or preventing neurodegenerative diseases and neuropathological disorders, methods of providing neuroprotection under stress conditions such as a stroke, methods of enhancing the brain's cognitive functions and methods of treating depression, anxiety and cachexia induced by a chronic disease in mammals and humans.

Abstract: Novel antiandrogenic agents are provided. An exemplary group of compounds has the structural formula (I) ##STR1## wherein R.sup.1 through R.sup.10, a and b are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat androgen-related clinical conditions are provided, as are methods and compositions for using the compounds as contraceptive agents.

Abstract: A process for the production of 1-methyl-3-keto-.DELTA..sup.1,4 steroids of general formula I ##STR1## in which St symbolizes the radical of asteroid molecule, where a 3-keto-.DELTA..sup.1,4 steroid of general formula II ##STR2## in which St has the above-mentioned meaning, is reacted in an inert solvent in the presence of a nickel salt soluble therein with an organometallic compound of formula III, IV or V ##STR3## where X, Y.sub.1, Y.sub.2, Y.sub.3, Z.sub.1 and Z.sub.2 are as defined in the specification.

Abstract: There are described spontaneously dispersible agents containing sterolester and/or sterolphosphor compounds having a pronounced antitumour activity. Novel sterolesters and sterolphosphor compounds, their use for treating tumors, and processes for their preparation are disclosed.

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: A process for the preparation of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms optionally substituted by halogen or a nitrogen or oxygen function and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms and the A, B, C and D rings are optionally substituted by at least one member of the group consisting of optionally protected --OH or .dbd.0, halogen, alkyl and alkoxy of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms comprising reacting a compound of the formula ##STR2## wherein R.sub.1 and R.sub.2 and the A, B, C and D rings are defined as above with an oxidizing agent in the presence of water and an at least partially water-miscible solvent to obtain a compound of the formula ##STR3## wherein R.sub.1 and R.sub.

Abstract: 11.beta.-substituted-16.alpha., 17.alpha.-methylene-estra-4,9-dien-3-ones of formula I ##STR1## wherein R.sup.1 is a methyl or ethyl group;R.sup.2 is H; a C.sub.1-6 -alkyl, -alkoxymethyl, -alkanoyl or -alkoxcarbonyl group ; 2-methoxyethyl; 2-hydroxyethyl; 2-C.sub.1-4 -alkanoyloxyethyl; or a tri-C.sub.1-4 -alkylsilyl group;R.sup.3 is vinyl; a C.sub.1-6 -alkyl; or a phenyl radical para-substituted by --OCH.sub.3, --SCH.sub.3, --N(CH.sub.3), --CN, --CHO, CH.sub.3 CO--, CH.sub.3 CHOH-- or --CH.sub.2 OH;R.sup.6 is H or a C.sub.1-4 -alkyl group;X is O, a hydroxy- or methoxyimino group (.dbd.N.about.OH or --N.about.OCH.sub.3), or a cyclic thioketal with 2 or 3 carbon ring atomsare provided, as well as pharmaceutical compositions containing said compounds, methods of use of said compounds, and processes for their production.

Abstract: A process for the production of 3-deoxy-4-ene steroids of the general formula I ##STR1## is described, in which R.sub.1, R.sub.2 and R.sub.3 mean a hydrogen atom or a methyl group,R.sub.4 represents a lower alkyl group, a phenyl group or a free, esterified or etherified hydroxy group,R.sub.5 symbolizes a hydrogen atom, a vinyl group or the grouping --C.tbd.CR.sub.6 with R.sub.6 meaning a hydrogen atom, an alkyl group with a maximum of 4 carbon atoms or a halogen atom,X represents a methylene group, a fluoromethylene group, an ethylidene group or a vinylidene group,Y and U represent a methylene group or an ethylidene group andZ symbolizes a methylene group, an ethylidene group, a vinylidene group, a chloromethylene group or a hydroxymethylene group and in which the bonds represent three single bonds or one double bond and two single bonds or a conjugated double bond.

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 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: Invented are carboxyl and carboxyl alkyl ester substituted 7-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. Also invented are methods for preparing these compounds.

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