Abstract: The invention relates to a compound of Formula (I), or a pharmaceutically acceptable salt thereof: wherein R1 is C1-8 alkyl, C1-8 alkoxy, CN, NO2, amino, COOH, COOCH3, OH, N3, or halogen and R2 is H, OH, C1-8 alkyl, C1-8 alkoxy, C2-C6 alkenyl, halogen, Bn-O—, Bn- optionally substituted, or Ph- optionally substituted.

Abstract: The invention relates to a compound of Formula (I), or a pharmaceutically acceptable salt thereof: wherein R1 is C1-8 alkyl, C1-8 alkoxy, CN, NO2, amino, COOH, COOCH3, OH, N3, or halogen and R2 is H, OH, C1-8 alkyl, C1-8 alkoxy, C2-C6 alkenyl, halogen, Bn-O—, Bn- optionally substituted, or Ph- optionally substituted.

Abstract: The invention relates to a compound of Formula (I), or a pharmaceutically acceptable salt thereof: wherein R1 is C1-8 alkyl, C1-8 alkoxy, CN, NO2, amino, COOH, COOCH3, OH, N3, or halogen and R2 is H, OH, C1-8 alkyl, C1-8 alkoxy, C2-C6 alkenyl, halogen, Bn-O—, Bn- optionally substituted, or Ph- optionally substituted.

Abstract: A method as well as new intermediates for preparing Ulipristal acetate (a compound I) and a method for preparing the new intermediates are provided. The intermediate in a constitutional formula IV is conductive to reacting with methyl lithium or methyl Grignard reagent, a protective group is easy to be removed after a reaction, side reactions are few, a mid-term treatment is simple, the reagents used are cheap, costs are low and a yield is high, if a compound in a constitutional formula V is obtained by the reaction of a compound in a constitutional formula III and the intermediate in the constitutional formula IV, the yield of a two-step reaction is 75%, a purity is above 98%. wherein R is defined in the specification.

Abstract: The invention provides methods to treating conditions such as prostate cancer, or for ameliorating one or more symptoms associated with prostate cancer, or for agents that modulate the biological activity of the androgen receptor. The invention also provides methods and compositions suitable for therapeutic applications.

Abstract: A method for producing highly crystalline and stable microparticles of an active substance with a very narrow size distribution. The microparticles being crystallized out of a suspension made of primary particles of the active substance, a solution of the active substance, a non-solvent for the active substance and inert formed pieces. The resulting microparticles hare highly stable largely independent of the physiochemical properties of the active substance and can be especially suitable for fast release dosage forms of pharmaceuticals.

Abstract: Provided herein are steroidal compounds that are androsta-5,7-dienes or a pregna-5,7-dienes and ultraviolet B (UVB) conversion products thereof which includes pharmaceutical compositions of the steroidal compounds as shown in Tables 1 and 2. Also provided is a method for producing hydroxylated metabolites of cholecalciferol or ergocalciferol via the P450scc (CYP11A1) or CYP27B1 enzyme systems where the hydroxylase has an activity to hydroxylate position C20 of a secosteroid or its 5,7-dieneal precursor and the hydroxylated metabolites so produced. In addition, a method for inhibiting proliferation of either a normally or abnormally proliferating cell by contacting the cell with any of the compounds described herein. A related method is provided of treating a condition associated with the proliferating cell such as a cancer, a skin disorder, a defect in cell differentiation, cosmetic, prophylaxsis, or healthy cell maintenance.

Abstract: The instant invention provides potent antiandrogen compounds, such as 3?-acetoxyandrost-1,5-diene-17-ethylene ketal and 3?-hydroxyandrost-1,5-diene-17-ethylene ketal, and methods for their use in the prevention and treatment of biological conditions mediated by androgen receptors. Thus, for example, compounds of the invention are useful in the prevention and treatment of prostrate cancer. Furthermore, it has been discovered that compounds of the invention are useful in the prevention and treatment of androgen-independent cancers such as androgen-independent prostrate cancer. Finally, inventive compounds may be used to treat antiandrogen induced withdrawal syndrome.

Abstract: The invention relates to a process for synthesising 3?-hydroxychlormadinone acetate.

Abstract: The invention provides and describes solid state 17?-ethynyl-5?-androstane-3?,17?-diol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17?-ethynyl-5?-androstane-3?,17?-diol include Form III anhydrate and Form I solvate. The invention further relates to solid and suspension formulations containing 17?-ethynyl-5?-androstane-3?,17?-diol in a described solid state form and use of the formulations to treat cancers or precancers such as prostate cancer or breast cancer in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17?-ethynyl-5?-androstane-3?,17?-diol and uses of such formulations in treating the described conditions.

Abstract: The instant invention provides potent antiandrogen compounds, such as 3?-acetoxyandrost-1,5-diene-17-ethylene ketal and 3?-hydroxyandrost-1,5-diene-17-ethylene ketal, and methods for their use in the prevention and treatment of biological conditions mediated by androgen receptors. Thus, for example, compounds of the invention are useful in the prevention and treatment of prostrate cancer. Furthermore, it has been discovered that compounds of the invention are useful in the prevention and treatment of androgen-independent cancers such as androgen-independent prostrate cancer. Finally, inventive compounds may be used to treat antiandrogen induced withdrawal syndrome.

Abstract: Disclosed are androgen-related steroids having a &Dgr;14 double bond and carrying a substituent at either or both of the carbon atoms nos. 15 and 16. The present steroids are characterized by possessing a mixed profile of androgenic and progestagenic activities. This makes these compounds suitable for male or female hormone replacement therapy, as well as male contraception.

Abstract: The present invention concerns with steroid compounds of formula (I) wherein R1 is cyclohexyl or cycloheptyl, R2 is hydrogen or C1-C6 alkyl, R3 is hydrogen, C1-C6 alkyl or methylol, R4 is hydrogen or hydroxymethylene and a pharmaceutically acceptable salt thereof. The invention also concerns with a method for preparation of the compounds, pharmaceutical compositions containing the compounds as its active component and use of the compounds and the pharmaceutical compositions in preparing medicines for treating diseases, e.g. those associated with progestin dependence.

Abstract: The invention relates to compounds of the formula: in which R1, R2, R3, R4, R5, R6, n and X are as defined in the specification, and to pharmaceutical compositions containing them. These compounds are excellent progestogens which are devoid of residual androgenic activity.

Abstract: A C-11 substituted steroid and a method of use of a C-11 substituted steroid to treat osteoporosis.

Abstract: Methods and compositions for preventing and treating neovascularization with steroids is disclosed.

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 C-11 substituted steroid and a method of use of a C-11 substituted steroid to treat osteoporosis.

Abstract: The present invention relates to a method of using a perchloric acid catalyzed reaction to make acyl derivatives of norprogesterone compounds and, in particular, 16-methylene-17.alpha.-hydroxy-19-norpregn-4-ene-3,20-dione.

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: There are provided 13-alkyl-11beta-phenyl-gonanes of formula I ##STR1## wherein Z is an oxygen atom or N--OH;R.sup.2 is alpha- or beta-position methyl or ethyl;R.sup.1 is selected from heteroaryl radicals, cycloalkyl radicals, cycloalkenyl radicals, aryl radicals, alkenyl radicals, and alkyl radicals where R.sup.2 is in the alpha-position and an ethyl radical where R.sup.2 is in the beta-position; andR.sup.3 and R.sup.4 are selected from one of two different groups of substituent pairs, the group from which the selection is made being determined by the position of R.sup.2.

Abstract: New 11.beta.-phenyl-14.beta.H-steroids of general formula (I), where Z is an oxygen atom or the hydroxyimino-grouping N.about.OH, and M and N are either jointly a second compound or L is a hydrogen atom and M is an .alpha.-permanent hydroxy group and either A and B together are a second compound and D is a hydrogen atom, where R.sup.1 is a five or six-part heteroalkyl residue or a cycloalkyl, cycloalkenyl or aryl residue or A is a hydrogen atom and B and D together are a methylene bridge, where R.sup.1 besides the aforementioned residues may be a possibly substituted hydrocarbon residue with up to 10 C atoms, a possibly substituted amino group, a hydroxy or C.sub.1-8 alkoxy, mercapto or thioalkyl group, R.sup.2 is a methyl or ethyl residue, and R.sup.3 /R.sup.4 represents the usual combination of substituents on the C17 atom in steroid chemistry, having antigestagenic and other properties.

Abstract: The invention relates to a novel process for the preparation of 17 .alpha.-hydroxy-20-oxopregnane derivatives of the general formula (I), ##STR1## wherein R.sub.1 means a hydroxy or an oxo group; andthe dotted lines optionally represent one or more additional valence bond(s), with the proviso that the dotted line in the 4-position and the dotted line in the 5-position cannot each simultaneously be an additional valence bond from steroids having 23,24-dinor-17(20)-dehydrocholan-22-oic -22-oic acid structure.According to the process of the invention a steroid derivative having 23,24-dinorcholan-22-oic acid structure, containing a double bond in 17(20)-position, is transformed to 17.alpha., 20-epoxy-23,24-dinorcholanoic acid, the latter is converted to a reactive acid derivative, which is then reacted with a salt-containing azide ion to yield a 17.alpha., 20-epoxy-23,24-dinorcholanoic acyl azide derivative and the azide obtained is reacted with a mineral or organic acid in an aqueous medium.

Abstract: The invention is directed to novel angiotropic (angiogenic and angiostatic) steroids. They are halogenated in the 21 position. The invention is also directed to novel methods of treating gastrointestinal ulcers by the administration of the novel angiotropic (angiogenic) steroids.

Abstract: A process for the preparation of ethynyl carbinols of the formula: ##STR1## wherein R" is hydrogen, a substituted or unsubstituted aliphatic or aromatic hydrocarbon, R'" is a substituted or unsubstituted aliphatic or aromatic hydrocarbon or R" and R'" together to the carbon atom to which they are joined represent a steroid, which comprises the steps ofA. reacting in a solvent system comprising an aromatic hydrocarbon, at least one lithium alkylamide selected from the group consisting of: ##STR2## wherein R is a hydrogen or lower alkyl, R' is hydrogen, lower alkyl, a substituted or unsubstituted aliphatic, alicyclic or aromatic hydrocarbon, x is an integer of 2 to 8, y and z are each 0 to 1, with acetylene to form a monolithium acetylideB. reacting in a solvent system comprising an aromatic hydrocarbon, the monolithium acetylene from Part A with a ketone of the formula R"R'"C.dbd.O, wherein R" and R'" are as hereinbefore defined, and thenC.

Abstract: A composition for in vivo inhibition of aromatase in a mammal, which comprises an in vivo inhibitory amount of a compound having the following general formula: ##STR1## wherein R.sub.1 is hydrogen or C.sub.1-20 acyl, in combination with a pharmaceutically acceptable carrier or diluent thereof.

Abstract: Disclosed are .DELTA..sup.9(11) -steroids of the formula ##STR1## which have been found to be angiostatic and therefore are useful in the control of embryogenesis, inflammatory conditions, tumor growth as well as other abnormalities.

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.