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: The present invention provides a process for the extraction and isolation of bioactive lignans with high yield and purity from Sesame oil by sequential extraction, crystallization, and saponification. The present invention provides a process for the production of highly pure bioactive lignan crystal, lignan enriched formulations with lignan content varying from 50 to 95% and with product flexibility and also at the same time preserve the starting raw material i.e. sesame oil.

Abstract: The invention relates to portable albumin binders, which are useful for improving the pharmacokinetic properties of diagnostic or therapeutic agents, in particular increasing the blood circulations time and/or the tissue penetration capacity of such agents.

Abstract: The invention relates to new 2-substituted D-homo-estra-1,3,5(10)-trienes of general formula I in which R2 means a C1-C8-alkyl group, a C1-C8-alkyloxy group or a halogen atom, R13 means a hydrogen atom or a methyl group, R17 means a hydrogen atom or a fluorine atom, as well as their pharmaceutically acceptable salts, their manufacture and use as medicaments for prophylaxis and therapy of estrogen-dependent diseases that can be influenced by inhibition of 17?-hydroxy steroid dehydro-genase type 1.

Abstract: Described are steroidal C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic “addition-elimination” substitution reaction of 3?-acetoxy-17-chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles and methods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3?-ol or analogs thereof with tributylstannyl diazines. The compounds are potent inhibitors of human CYP17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds are useful for the treatment of human prostate cancer.

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: The present disclosure provides contrast photoacoustic probes, and compositions comprising such probes, designed to non-invasively detect and monitor various disease states, or targets within a subject human or animal. The probes are designed to be optically excited in tissue, ultimately generating thermal energy, which is transformed into acoustic energy by the response of the aqueous environment in the subject to the thermal emissions. The acoustic energy (sound) can then be detected by suitably applied transducers and digitally transformed into images indicating the location of the probe in the subject. One aspect of the disclosure encompasses photoacoustic probes that comprise: a carbon nanotube and a plurality of dye molecules bound to the carbon nanotube. The probes may further comprise a targeting moiety for localizing the probe at the site of a specific target.

Abstract: A polymerizable liquid crystal compound that has a wide liquid crystal phase temperature range and has a sterol ferulate skeleton, and a liquid crystal composition containing the compound are provided. A polymer that is excellent in various characteristics, and a molded article having optical anisotropy produced with the polymer are obtained with the polymerizable liquid crystal compound. The compound is represented by formula (1): wherein R represents a sterol moiety derived from vegetable organisms; P represents one of polymerizable groups represented by formulae (P1) to (P8); X, Z, X0 and Z0 each represent a bonding group; and A represents a divalent group having a cyclic structure.

Abstract: Use of a composition that modulates a STAT in the manufacture of a medicament for treating or preventing a fibroproliferative disease. The fibroproliferative disease may comprise keloid scarring. The composition may modulate one or more of; activity; phosphorylation; level of expression; or sub-cellular localisation of the STAT. The STAT may be STAT 3.

Abstract: The invention relates to a method of preparation of a soluble formulation of water-insoluble pentacyclic and tetracyclic terpenoids, wherein the water-insoluble terpenoid having a free carboxylic, hydroxy or amino functional group is derivatized on this functional group with a substituent selected from the group comprising substituents of general formula Xa bound to the hydroxy group of the terpenoid, wherein Xa is —OC—R—COOH, substituents of general formula Xa bound to the amino group of the terpenoid, wherein Xa is —OC—R—COOH, quarternary ammonium substituents of general formula Xb bound to the carboxy group of the terpenoid, wherein Xb is —(CH2)nN+R3Y—, quarternary ammonium substituents of general formula Xc bound to the carboxy group of the terpenoid, wherein Xc je —(CH2)nR+Y—, substituents of general formula Xd bound to the carboxy group of the terpenoid, wherein Xd represents —R—COOH, glycosylic substituents Xe bound by alpha or beta glycosidic bond to the hydroxy group or to the carboxy group of the te

Abstract: The present invention relates to a process for production of a steroid compound having a partial structure represented by Formula (2) by oxidizing a steroid compound having a partial structure represented by Formula (1), without the need of any special apparatus, in a safe and economical manner, with less adverse affect on environment, in a simple and high efficient manner. Specifically, the invention relates to a process for producing a steroid compound having a partial structure of ring A and ring B of the steroid skeleton represented by Formula (2): wherein R represents a hydrogen atom or C1-6 alkyl group, comprising the step of reacting a steroid compound having a partial structure of ring A and ring B of the steroid skeleton represented by Formula (1): wherein R is the same as above; with a catalytic amount of copper halide in the presence of oxygen.

Abstract: The invention relates to the use of 2-substituted estra-1,3,5(10)-triene-3-yl sulfamates of general formula I, in addition to their pharmaceutically acceptable salts for producing a medicament. Said compounds have an anti-tumour action.

Abstract: The present invention relates to an improved and integrated process for the extraction and purification of tocotrienols or tocopherols, carotenoids and sterols from vegetable and other edible oils. Fatty acids in the vegetable oils are subjected to alcoholic osterification to form ester-rich layer that includes fatty acid alkyl esters, carotenoids, tocotrienols or tocopherols, and sterols. The advantages of this process are that the tocotrienols or tocopherols, carotenoids and sterols are produced efficiently without any substantial decomposition or degradation of these phytonutrients.

Abstract: This invention is generally related to the fields of fragrance compositions, personal care products, and home consumer products. This invention also relates to 20-pregnenes, in particular those found naturally occurring in corals and which affect mood in humans, to the incorporation of these 20-pregnene compounds into various compositions, and to methods of affecting the mood of individuals using such compounds.

Abstract: Compositions and methods for treating mammalian diseases or conditions characterized by undesirable angiogenesis by administering an effective amount of a compound of the formulae: wherein Ra is selected from —OCH3, —OCH2CH3 or —CCCH3; and Z is selected from >C(H)—OH, >C(H)—O-alkyl, >C(H)—O-sulfamate, where alkyl is a linear, branched and/or cyclic hydrocarbon chain comprising 1 to 10 carbons.

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: The present invention relates to novel thiosulfonates derivatives. The present invention also provides methods for preventing, treating and/or reducing inflammation-associated diseases in the cardiovascular, connective tissue, pulmonary, gastrointestinal, respiratory, urogenital, nervous or cutaneous systems as well as infective and tumoral diseases employing said compounds.

Abstract: The invention provides oxogenous markers, designed and synthesized for the measurement and characterization of oxidative/nitrosative stress levels, thus enable the identification of the type of reactive ROS/NRS involved, characterization of the damaged products and their formation kinetics, and thereby the identification of pathological conditions associated with oxidative/nitrosative stress, before appearing or at the stage of development.

Abstract: The invention relates to a new process for the synthesis of high purity 17?-cyanomethyl-17?-hydroxy-estra-4,9-diene-3-one (further on dienogest) of formula (I) from 3-methoxy-17-hydroxy-estra-2,5(10)-diene of formula (V). The invention relates also to the high purity 17?-cyanomethyl-17?-hydroxy-estra-4,9-diene-3-one and pharmaceutical compositions containing that as active ingredient. The pharmaceutical compositions according to this invention contain high purity dienogest of formula (I) in which the total amount of impurities is less than 0.1%, while the amount of 4-bromo-dienogest is under the detection limit (0.02%) as active ingredient or at least one of the active ingredients and auxiliary materials, which are commonly used in practice, such as carriers, excipients or diluents.

Abstract: A diamine includes a structure of formula (I), wherein X and Y are independently a divalence group selected from the group consisting of: —O—, —(C?O)—O—, —O—(C?O)—, —(C?O)—NH—, and —NH—(C?O)—; and R has a structure of formula (II): wherein R1, R2, R3, R4, R5, m, and n are as defined in Claim 1. A polyamic acid is prepared by reacting a diamine reactant including the aforesaid diamine of formula (I) with a tetracarboxylic dianhydride reactant. A liquid crystal orienting film contains a polyimide converted from the aforesaid polyamic acid.

Abstract: The invention relates to a process for preparing compounds of formula (I): in which R1, R2, R3, n and X are as defined in the description, and to the intermediate compounds for implementing this process.

Abstract: The invention relates to new 2-substituted D-homo-estra-1,3,5(10)-trienes of general formula I in which R2 means a C1-C8-alkyl group, a C1-C8-alkyloxy group or a halogen atom, R13 means a hydrogen atom or a methyl group, R17 means a hydrogen atom or a fluorine atom, as well as their pharmaceutically acceptable salts, their manufacture and use as medicaments for prophylaxis and therapy of estrogen-dependent diseases that can be influenced by inhibition of 17?-hydroxy steroid dehydro-genase type 1.

Abstract: An ABC transporter protein expression inhibitor comprising, as the active ingredient(s), 0.001 to 100 nM of one or more members selected from among steroid hormones, compounds having a female hormone function, analogous compounds thereof and antagonistic inhibitors therefor; an anticancer composition containing this ABC transporter protein expression inhibitor and an anticancer drug; and cells useful in the development of an anticancer drug. The present invention provides a drug which inhibits the expression of an ABC transporter to thereby overcome resistance to anticancer drugs; cancer cells useful in screening such drugs; and an anticancer drug efficacious even against such a cancer as having acquired resistance to anticancer drugs.

Abstract: A method for the degradation of polycyclic aromatic compounds is disclosed that involves dissolving ozone in a bipolar solvent comprising a non-polar solvent in which is of sufficiently non-polar character to solubilized the polycyclic aromatic compounds, and a polar-water-compatible solvent which is fully miscible with the non-polar solvent to form a single phase with the non-polar solvent. The bipolar solvent with dissolved ozone is contacted with the polycyclic aromatic compounds to solubilize the polycyclic aromatic compounds and react the dissolved polycyclic aromatic compounds with the ozone to degrade the dissolved polycyclic aromatic compounds to oxygenated intermediates. The bipolar solvent is then mixed with sufficient water to form separate non-polar and polar phases, the non-polar phase comprising the non-polar solvent and the polar phase comprising the non-polar solvent and the oxygenated intermediates.

Abstract: The present invention provides a method of extracting ginsenoside Rg2, which is applied to mass production. The method of the present invention employs gradient salting-out instead of conventional silica gel chromatography, and therefore enables convenient performance and mass production of ginsenoside Rg2. Provided are also a pharmaceutical composition comprising ginsenoside Rg2 as an active ingredient, and prophylactic and therapeutic agents for preventing and treating dementia, depression, peripheral circulation disorder and related diseases, utilizing the pharmaceutical composition.

Abstract: The present invention provides methods for labeling One or two oxygen atom(s) in a carboxyl group of a carboxyl-containing compound with an oxygen isotope selected from oxygen-17 (17O) or oxygen-18 (18O). The methods of the present invention are characterized in that an activated ester of the carboxyl-containing compound (carboxylic acid) is reacted with H217O or H218O in the presence of an activator. In the methods of the present invention, the reaction between the activated ester of a carboxylic acid and H217O or H218O can be allowed to proceed without including drastic conditions such as strongly acidic conditions or alkaline hydrolysis because an activator is used.

Abstract: The invention concerns compounds called pyrene-cholesterols, of general formula (I), wherein: X represents a CH2 group or an oxygen atom and n is an integer from 2 to 10, as well as their use for implementing a method for detecting and measuring the effects of specific products on biological membranes, and a method for preparing the compounds.

Abstract: The present invention relates to novel cationic lipids, transfection agents, microparticles, nanoparticles, and short interfering nucleic acid (siNA) molecules. The invention also features compositions, and methods of use for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of gene expression and/or activity in a subject or organism. Specifically, the invention relates to novel cationic lipids, microparticles, nanoparticles and transfection agents that effectively transfect or deliver biologically active molecules, such as antibodies (e.g., monoclonal, chimeric, humanized etc.

Abstract: A process of obtaining sterols suitable for human consumption from a crude wood pulping source containing sterol esters is disclosed. The sterols are obtained at high yield and purity. In particular, a process of obtaining sterols at high yield and purity from tall oil pitch (TOP) is disclosed. The sterols obtained can be esterified to sterol esters for use in dietary supplements and as additives for food and beverage products.

Abstract: The invention concerns a method for binding, in solution, at least a peptide composition and at least a lipophilic vector bearing an aldehyde function, the coupling comprising a step which consists in producing a hydrazone bond between the peptide compound and the lipophilic vector. The invention also concerns lipophilic vectors for use in this method, lipopeptides obtained by this method, uses of the lipopeptides for cell screening, and the applications of the invention, in particular for preparing targeting of an active principle of the peptide kind (for example hormone or neuropeptide) through physiological barriers such as cell membranes.

Abstract: The invention relates to ?15-D-homosteroids of general formula (I) process for their production and pharmaceutical compositions that contain these compounds. The compounds of general formula I according to the invention have androgenic activity.

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 hematological malignancies. Further the conjugates exhibit 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: In accordance with the present invention, there are provided lipid-conjugated polyamide compounds and related compositions and methods thereof. Lipid-conjugated polyamide compounds of the present invention are particularly useful as vehicles for delivering biologically active agents to a target site. In particular, the invention compounds are effective at facilitating the delivery of polynucleotides to cells. The present invention also provides a method for producing stable formulations of polynucleotides complexed with a delivery vehicle.

Abstract: The compositions and methods disclosed herein provide heterobifunctional programmable genotoxic compounds that can be designed to kill selected cells present in a heterogenous cell population. The present compounds comprise a first agent that inflicts damage on cellular DNA, and a second agent that attracts a macromolecular cell component such as a protein, which in turn shields genomic lesions from repair. Unrepaired lesions therefore persist in the cellular genome and contribute to the death of selected cells. In contrast, lesions formed in nonselected cells, which lack the cell component, are unshielded and thus are repaired. As a result, compounds described herein are less toxic to nonselected cells. Compounds of this invention can be designed to cause the selective killing of transformed cells, viral-infected cells and the like.

Abstract: The present invention involves a novel crystal form of 17?-hydroxy-7?-(5?-methyl-2?-furyl)-pregna-4,9(11)-dien-3-one-21-carboxylic acid, ?-lactone, having the formula which is an intermediate useful in preparation of an important pharmaceutical, eplerenone.

Abstract: The present invention is a di-steroidal prodrug of ethinyl estradiol according to formula I:

Abstract: The present invention is a di-steroidal prodrug of estradiol having the following formula:

Abstract: An estrogen/antiestrogen-porphyrin conjugate, their composition and methods for their use are claimed. The active compounds of the invention are conjugates consisting of an estrogen or anti estrogen portion, tether or linker portion and a porphyrin portion. The method of invention exploits an active process that involves strong and specific interactions between nuclear receptor and its cognate ligand.

Abstract: In accordance with the present invention, there are provided lipid-conjugated polyamide compounds and related compositions and methods thereof. Lipid-conjugated polyamide compounds of the present invention are particularly useful as vehicles for delivering biologically active agents to a target site. In particular, the invention compounds are effective at facilitating the delivery of polynucleotides to cells. The present invention also provides a method for producing stable formulations of polynucleotides complexed with a delivery vehicle.

Abstract: This invention relates to a group of novel sapogenins, their use in anti-cancer applications, and to a process for their production. More particularly, this invention pertains to a novel group of dammarane sapogenins, PAM-120, PBM-110 and PBM-100 (the dammarance sapogenine structure is specifically clean of any sugar moieties (glycons) at any position and hydroxyl at C-20) and PAN-20 and PAN-30 (the dammarance sapogenin structure has sugar moieties but is free of hydroxyl at C-20), obtained by chemical cleavage of dammarane saponins. The invention also includes a novel application of the said sapogenins for anti-cancer treatment by using them separately or together, and/or jointly with other drugs, as well as to the process of producing these novel sapogenins. Said novel dammarane sapogenins show surprising anti-cancer effect when applied, particularly against multi-drug resistant cancers.

Abstract: Androgenic steroids having a (14?,17?-)-17-(hydroxymetheyl) configuration, useful for the preparation of male contraceptives and pharmaceutical formulations for the treatment of androgen insufficiency.

Abstract: The present invention is directed to modified, hydroxy-bearing aromatic ring structures having cytoprotective activity. More specifically, in a first embodiment the present invention is directed to phenolic compounds, and in particular steriods (e.g., estrogens), wherein a non-fused polycyclic, hydrophobic substituent is attached to the hydroxy-substituted A-ring thereof. The present invention is further directed to a process for conferring cytoprotection to a population of cells involving the administration of the compound.

Abstract: The hormone 7-keto-dehydroepiandrosterone (7-keto-dehydroepiandrosterone; &Dgr;5-androstene 3&bgr;-hydroxy, 17-one; referenced as “7-keto-DHEA”) is modified at the 3rd carbon, the 17th carbon, or at both 3rd carbon and the 17th carbons with one or more of the following: tetrahydropyranyl (both mono and di-ethers), 1-methoxycyclopentane (both mono and di-ethers), cyclopent-1′-enyl (both mono and di-ethers), or combinations thereof. This modification improves oral bioavailability and plasma half-life in humans and mammals.

Abstract: A process for preparing compounds of formula (1): including the convergent steps as defined in the specification, and wherein R groups have any of the values defined in the specification. The invention also provides processes and intermediates useful for preparing compounds of formula (1).

Abstract: Compounds having an ansamycin anitibiotic, or other moiety which binds to hsp90, coupled to a targeting moiety which binds specifically to a protein, receptor or marker can provide effective targeted delivery of the ansamycin antibiotic leading to the degradation of proteins and death of the targeted cells. These compositions may have different specificity than the ansamycin alone, allowing for a more specific targeting of the therapy, and can be effective in instances where the ansamycin alone has no effect. Thus, these compounds provide an entirely new class of targeted chemotherapy agents with application, depending on the nature of the targeting moiety, to treatment of a variety of different forms of cancer. Such agents can further be used to promote selective degradation of proteins associated with the pathogenesis of others diseases, including antigens associated with autoimmune disorders and pathogenic proteins associated with Alzheimer's disease.

Abstract: Novel N-fluorotriazinium electrophilic fluorinating agents have the Formula I: wherein three A moieties are independently CR, where each R is, independently, hydrogen, halogen, hydroxyl, (primary, secondary or tertiary) amino, amino, cyano, perfluorothio, hydroxysulfonyl, halosulfonyl, hydrocarbyloxysulfonyl, or a carbon-containing substituent selected from the group consisting of optionally substituted hydrocarbyl, hydrocarbyloxy, hydrocarbyloxycarbonyl, and hydrocarbylthio groups, and at least one R is neither hydrogen nor halogen; two A moieties are independently Z, where each Z is independently nitrogen or a quaternary nitrogen atom and Y is a counterion or group of counterions which are inert to chemical attack by fluorine, or adjacent triazinium moieties are linked by a common R substituent to provide an oligomer or polymer.

Abstract: Methods for modulating amyloid deposition in a subject are described. An effective amount of at least one ATP binding cassette (ABC) transporter blocker is administered to a subject, such that modulation of amyloid deposition occurs. Methods also include administering and effective amount of at least one ABC transporter blocker, or a pharmaceutically acceptable salt thereof, to a subject such that a disease state associated with amyloidosis is treated. Packaged pharmaceutical compositions for treating amyloidosis are described. The package includes a container for holding an effective amount of a pharmaceutical composition and instructions for using the pharmaceutical composition for treatment of amyloidosis. The pharmaceutical composition includes at least one ABC blocker for modulating amyloid deposition in a subject. Methods for identifying agents which modulate amyloid deposition in a subject are also described.

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: Novel compounds having a formula selected from the group consisting of wherein the substituents are defined as in the specification which are intermediates for the production of vinyl compounds having a remarkable anti-estrogenic and anti-proliferative activity.

Abstract: In accordance with the present invention, there are provided lipid-conjugated polyamide compounds and related compositions and methods thereof. Lipid-conjugated polyamide compounds of the present invention are particularly useful as vehicles for delivering biologically active agents to a target site. In particular, the invention compounds are effective at facilitating the delivery of polynucleotides to cells. The present invention also provides a method for producing stable formulations of polynucleotides complexed with a delivery vehicle.