Abstract: The present invention provides intermediates for preparing abiraterone, and processes for preparing abiraterone and intermediates thereof. The intermediates include a compound of formula (IV): wherein R represents a hydroxy-protecting group.

Abstract: Methods for treating a subject determined to have a cancer comprising a heterozygous inactivation of a housekeeping gene (or a homozygous deletion of a functionally redundant housekeeping gene) by treating the subject with an inhibitor of the gene. For example, a subject having a cancer with an ENO gene deletion can be treated with a glycolysis inhibitor, such as an enolase inhibitor. In some aspects, a subject having a cancer with an ARS gene deletion can be treated with an ARS inhibitor.

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 SHIP inhibitor compounds and methods for using these compounds. In particular, the present invention discloses the following methods: (i) a method of treating graft versus host disease in a subject; (ii) a method of inhibiting a SHIP1 protein in a cell; (iii) a method of selectively inhibiting a SHIP1 protein in a cell; (iv) a method for treating or preventing graft-versus-host disease (GVHD) in a recipient of an organ or tissue transplant; (v) a method of modulating SHIP activity in a cell expressing SHIP1 or SHIP2; (vi) a method of ex vivo or in vitro treatment of transplants; (vii) a method of inhibiting tumor growth and metastasis in a subject; (viii) a method of treating a hematologic malignancy in a subject; (ix) a method of inducing apoptosis of multiple myeloma cells; (x) a method of treating multiple myeloma in a subject; (xi) a method of inhibiting the proliferation of a human breast cancer cell; and (xii) a method of treating breast cancer in a subject.

Abstract: The present invention provides a novel series of imidazolyl substituted steroidal and indan-1-one derivatives and salts thereof having the following general structural formulae (A and B)

Abstract: The present invention provides an agent that modulates physiological condition of pests, wherein the agent has an ability to modulate the activity of an insect peptidyl-dipeptidase A; a method for assaying pesticidal activity of a test substance, which comprises a step of measuring the activity of a peptidyl-dipeptidase A in a reaction system in which the peptidyl-dipeptidase A contacts with a test substance, and the like.

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 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: Conjugates comprising one or more steroids conjugated with one or more mammalian proteins are disclosed. The conjugates are useful for diagnosis or treatment of solid cancer and haematological malignancies. Further the conjugates exhibits a synergistic action together with a cytoskeleton acting drug such as Taxol®, which enable the treatment of cancers that otherwise would be non responsive to Taxol®.

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: The invention is a process for the preparation of a &Dgr;4,9-steroid of formula (II) 1

Abstract: Intermediates for the preparation of a vitamin D derivative have the following formulas: wherein R9 and R10 may be the same or different and each represents a hydrogen atom or a protecting group, and in Formula (5) the conjugated double bond may be protected by a protecting group.

Abstract: The instant invention involves a process for oxidizing compounds containing an allylic group, i.e. those containing an allylic hydrogen or allylic alcohol group, to the corresponding enones, using a ruthenium-based catalyst in the presence of a hydroperoxide. Particularly, &Dgr;-5-steroidal alkenes can be oxidized to the corresponding &Dgr;-5-7-keto alkenes.

Abstract: Disclosed are compounds of formula II: wherein A is as defined by the specification. Also disclosed are compositions containing the esters and methods for their use in the regulation of skin atrophy and in the treatment of skin disorders such as dry skin, dandruff, acne and eczema.

Abstract: Novel steroid esters useful for regulating skin atrophy, and skin maladies, as well as compositions containing the esters and methods for their use are described. A preferred steroid ester is DHEA salicylate. Such types of skin atrophy to be treated include the thinning and/or general degradation of the dermis often characterized by a decrease in collagen and/or elastin as well as decreased number, size and doubling potential of fibroblast cells. Such skin maladies include but are not limited to dry skin, dandruff, acne, keratoses, psoriasis, eczema, pruritis, age spots, lentigines, melasmas, wrinkles, warts, blemished skin, hyperpigmented skin, hyperkeratotic skin, inflammatory dermatoses, age-related skin changes and skin in need of cleansers.

Abstract: The invention relates to novel, androstane steroids which are the ligand semiochemicals which bind to neuroepithelial receptors. The steroids are useful as ligands to neuroepithelial receptors in the human vomeronasal gland to stimulate autonomic and hypothalamic activity.

Abstract: Disclosed is the use of dehydroepiandrosterone salicylate in the treatment of skin atrophy. ##STR1## Such types skin atrophy to be treated include the thinning and/or general degradation of the dermis often characterized by a decrease in collagen and/or elastin as well as decreased number, size and doubling potential of fibroblast cells.

Abstract: The invention discloses steroid conjugates having the following structure: ##STR1## where Y is NHCH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, NH(CH.sub.2).sub.3 NH(CH.sub.2).sub.4 NH(CH.sub.2).sub.3 NH.sub.2, or NHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 NH.sub.2, and each of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is individually H, OH and OSO.sub.3 H. These conjugates posses antimicrobial properties and are, therefore, useful as antibiotics.

Abstract: A method for promoting weight control by treating a subject with a therapeutic amount of one of the .DELTA.5-androstenes listed below to stimulate weight control without affecting appetite or inducing the synthesis of sex hormones. .DELTA.5-Androstenes providing the desired biological activities include:.DELTA.5-Androstene-3.beta.,7.alpha.-diol-17-one.DELTA.5-Androstene-3.beta.-ol-7,17-dione.DELTA.5-Androstene-3.beta.,7.alpha.,17.beta.-triol.DELTA.5-Androstene-3.beta.,17.beta.-diol-7-one.DELTA.5-Androstene-3.beta.-acetoxy-7,16,17-trione.DELTA.5-Androstene-3.beta.,16.alpha.-dihydroxy-7,17-dione.DELTA.5-Androstene-3.alpha.-propionoxy-16.beta.-acetoxy-7,17-dione.DELTA.5-Androstene-3.beta.,7.alpha.,17.beta.-triol-16-one.DELTA.5-Androstene-3.beta.,17.beta.-diol-7,16-dione.DELTA.5-Androstene-3.beta.,16.alpha.,17.beta.-triol-7-one.

Abstract: Cardioactive steroidal compounds of the formula I ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 have the meanings shown in the description, and pharmaceutical compositions containing them.

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: 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.

Abstract: A 3-methylene-4-androsten-17-one of formula I ##STR1## wherein R.sub.a represents a hydrogen atom or a saturated or unsaturated straight-chain or branched-chain, optionally substituted alkyl radical with 1-6 carbon atoms, in which R.sub.a is in the alpha- or beta-position, andR.sub.b represents a hydrogen atom, a hydroxyl or an --S(O).sub.n R.sub.c group, in which R.sub.c is a hydrogen atom or an alkyl or acyl group with 1-4 carbon atoms, n=0, 1 or 2, andX represents CH.sub.2, CHF, CHCl or CHBr, in which if R.sub.a is hydrogen and R.sub.b is hydroxyl or R.sub.a and R.sub.b each are hydrogen, X is not CH.sub.2.The new compounds of formula I are suitable for fertility control and for treatment of diseases which are promoted by estrogens.