Abstract: The present invention provides processes for the production of chiral compounds in a stereoisomeric excess. The present processes involve reacting a hydrometallated alkene compound with a compound comprising a conjugated-bond system under conditions such that the compounds undergo an asymmetric 1,4- or 1,6-conjugate addition reaction, generating a chiral compound in a stereoisomeric excess. The reaction is performed in the presence of a metal catalyst, which catalyst preferably comprises a non-racemic chiral ligand.

Abstract: The present application discloses 17? hydroxy steroid dehydrogenase (17? HSD) type 1, 3, 10 inhibitors and use thereof (alone and in combination) in the treatment of cancer and other afflictions. 17? HSD1 inhibitors include estradiol derivatives with a nieta-carbamoylbenzyl substituent at C 16. 17? HSD3/HSD10 inhibitors include androsterone derivatives substituted at the C3 position with a sulfonamide piperazine. Also disclosed are compounds that are inhibitors of both 17? HSD1 and 17? HSD3 that have a spiro-morpholine substituent at C20.

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: 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 provides compositions comprising formula 1 steroids, e.g., 16?-bromo-3?-hydroxy-5?-androstan-17-one hemihydrate and one or more excipients, including compositions that comprise a liquid formulation comprising less than about 3% v/v water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16?-bromo-3?-hydroxy-5?-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using the compounds. The invention also provides methods to make and use these immunomodulatory compositions and formulations.

Abstract: The present invention relates to methods, compounds and compositions for inhibiting effective binding of a chemokine to its cellular receptor. In one form of the invention, a method includes contacting a cellular population with an effective amount of cosalane or an analog thereof. The invention further relates to methods, compounds and compositions for treating inflammatory diseases. In one form, a method includes administering to a patient a therapeutically effective amount of cosalane or an analog thereof.

Abstract: A method is described for stereoselectively reducing an unsaturated alkyl ketone substituent attached to a fused ring base. In this method, the unsaturated alkyl ketone reacts with a chiral oxazaborolidine reagent. This reaction stereoselectively reduces the unsaturated alkyl ketone to an unsaturated alkyl alcohol. The unsaturated alkyl alcohol can be further reduced, if desired, to produce a saturated alkyl alcohol. The fused ring base can be, for example, a steroid ring base or a base of a vitamin D analog. The process in accordance with the invention can be used with an alkeneone substituent (e.g., a 22-ene-24-one substituent) or an alkyneone substituent (e.g., a 22-yne-24-one substituent) on a steroid ring base to make squalamine or other useful aminosterol compounds and intermediates for making aminosterol compounds.

Abstract: Disclosed is an alkylating agent that contains an aluminum reagent Alk.sub.3-m AlL.sub.m, in which Alk means a methyl, ethyl, n- or i-propyl, n-, i- or tert-butyl, pentyl, hexyl, heptyl or octyl group, which all can also be branched, L means an ethoxy group, a chlorine or bromine atom, and m is equal to 1 or 2, as an alkyl source or else zinc dimethyl as a methyl source, which contains in addition catalytic amounts of one or more copper(I) and/or copper(II) compounds and one (or more) silyl reagent(s) of general formula IIIR.sup.1 R.sup.2 R.sup.3 SiZ (III),in whichR.sup.1, R.sup.2 and R.sup.3 are as defined herein, as well as a process for 1,4-addition of an alkyl group to an .alpha.,.beta.-unsaturated ketone or an .alpha.,.beta.-double unsaturated ketone or to an .alpha.,.beta.-unsaturated aldehyde with use of the agent according to the invention.

Abstract: This invention describes a new methylation or ethylation agent containing trimethyl aluminum or dimethyl zinc or triethyl aluminum as methyl or ethyl source, which additionally contains catalytic amounts of one or more copper(I) and/or copper(II) compounds as well as a process for the 1,4-addition of a methyl or ethyl group to an .alpha.,.beta.-unsaturated or an .alpha.,.beta.-double unsaturated ketone or an .alpha.,.beta.-unsaturated aldehyde using the agent according to the invention.By using only catalytic amounts of copper and a CKW (chlorinatedhydrocarbon)-free reaction medium, the new methylation/ethylation agent/process is distinguished by its environmental compatibility and it is, for example, suitable for the production of initial products for the synthesis of biologically effective compounds.

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: The present invention discloses a process for making 1-.alpha.-(carboxyalkyl)testosterone having the following formula: ##STR1## The process involves protecting the 17 position of 1,4-androstadien-17 .beta.-ol-3-one with TBDMS, alkylating with an alkenylmagnesium bromide and ozonolyzing the resulting ether. The resulting product is oxidized with sodium hypochloride followed by removal of the TBDMS protecting group with aqueous hydrofluoric acid in acetonitrile to produce the 1-.alpha.-(carboxyalkyl)-testosterone.

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: The new intermediate products of general formula I ##STR1## in which R.sup.1 stands for a hydrogen atom or a straight-chain or branched alkyl group with 1 to 4 carbon atoms,R.sup.2 stands for a hydrogen atom or a methyl group,R.sup.3 stands for a hydrogen atom,R.sup.4 stands for an acyloxy group with 1 to 4 carbon atoms in the acyl radical orR.sup.3 and R.sup.4 together stand for a keto-oxygen atom, are suitable in an excellent way for introducing a .DELTA..sup.1 double bond in the steroid skelton with the simultaneous presence of a .DELTA..sup.4 double bond, as well as a saturated carbonyl group, by clevage of hydrogen iodide with a base in an amidic solvent at elevated temperature. If R.sup.2 stands for a hydrogen atom, the A-ring is aromatized after the hydrogen iodide cleavage. For the production of a new intermediate products, special iodization processes, which partially also allow a stereoselective control of the iodization, are used.

Abstract: 3.beta.,17.beta.-androstenediol (".beta.AED") and 3.beta.,7.beta.,17.beta.-androstenetriol (".beta.AET") may be used to counteract the antiproliferative and immunosuppressive effects of hydrocortisone and other corticosteroids (i.e., to act as buffers to counteract the lymphosuppressive response to such steroids). .beta.AED and .beta.AET are steroids which mediate immune response to provide the body protection against immune down-regulation. A method for testing analogues of .beta.AED and .beta.AET to compare the effectiveness of such analogues as buffers of certain effects of hydrocortisone and other corticosteroids, including immune response and proliferative effects is described. Cytokines, including most particularly IL-3, are produced by addition of .beta.AET and .beta.AED and their analogues to the growth media of cell cultures of lymphatic cells.

Abstract: Androstane derivatives of the general Formula I ##STR1## in which R.sub.1 represents a hydrogen atom or a methyl group,X and Y each mean hydrogen atoms or together a carbon-carbon bond, andR.sub.2 symbolizes a hydrogen atom or an alkyl group with 1 to 6 carbon atoms,are pharmaceutically effective substances which have a distinct antiandrogenic effectiveness in topical application.