Abstract: The present invention relates generally to compositions and methods for treating cancer and hypercortisolism. Provided herein are substituted steroidal derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of glucocorticoid receptors. Furthermore, the subject compounds and compositions are useful for the treatment of cancer and hypercortisolism.

Abstract: The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

Abstract: The invention relates to a process for the preparation of a compound of formula (I): wherein R1 and R2 are as defined in the description, by reaction of a compound of formula (II) with a base. Compound (I) is an intermediate useful in the preparation of gestodene.

Abstract: The invention discloses a method for producing 30-halogenated betulinic acid. Betulin is used as a raw material and selectively oxidized and halogenated to generate 30-betulinic acid, and the selected oxidation and halogenation agent has high selectivity and does not affect C-3 hydroxyl or carbon-carbon double bonds. Oxidation and halogenation are completed in one step, so the process route is short, the treatment method is simple, and the product is purified easily.

Abstract: The present invention relates to the synthesis of ent-progesterone and intermediates thereof.

Abstract: Disclosed herein are compositions and methods for the treatment of otic disorders with steroid, NSAID, and/or adenosine triphosphatase (“ATPase”) modulator agents. In these methods, the steroidal, NSAID, and/or ATPase compositions and formulations are administered locally to an individual afflicted with an otic disorder, through direct application of these compositions and formulations onto or via perfusion into the targeted auris structure(s).

Abstract: The present invention provides a cosmetic composition containing one or more selected from a group consisting of green tea saponin and green tea polyphenol as active ingredients. The cosmetic composition of the invention is very safe to the skin and can greatly enhance biological mechanisms in the skin, and thus can serve as an anti-aging cosmetic composition.

Abstract: The present invention provides targeting lipids of structure L100-linker-L101??(CI), where L100 is a lipid, lipophile, alkyl, alkenyl or alkynyl, L101 is a ligand or —CH2CH2(OCH2CH2)pO(CH2)qCH2-ligand, p is 1-1000, and q is 1-20. In addition, the invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo.

Abstract: The present invention provides insecticidal lipids and lipid fractions from fungi of the phylum Ascomycota, together with compositions comprising such lipids and lipid fractions and methods of preparing same. Methods for the biological control of insects, such as phytopathogenic insects, using the lipids and lipid fractions or compositions comprising said lipids optionally together with one or more insecticidal or entomopathogenic agents including entomopathogenic fungi, are also provided.

Abstract: The invention provides skin protecting and penetrating, easy-to-administer base and active agent-containing compositions, such as those including hydrocortisone, for treating the skin of mammals for different dermatologic disorders. This is effected by topically administering effective amounts of the compositions thereto in forms that address the skin and mucosa of the mouth and lips, and the rest of the body. Additionally, an optional flavoring addition to these products affords significantly better tasting, and less bitter, compositions, allowing a more pleasant experience and better compliance by patients. The compositions include a unique formulation of FANCOL VB, Natunola Castor 1023, Finsolv TN, bees wax and, optionally, one or a plurality of plant or plant seed oils, fatty alcohols, fats and flavorings, in desirable weight percents thereof, in various forms, and preferably in a form of a solid roll-on stick in a variety of sizes and of a jar or pot.

Abstract: Disclosed herein are compositions and methods for the treatment of otic disorders with steroid, NSAID, and/or adenosine triphosphatase (“ATPase”) modulator agents. In these methods, the steroidal, NSAID, and/or ATPase compositions and formulations are administered locally to an individual afflicted with an otic disorder, through direct application of these compositions and formulations onto or via perfusion into the targeted auris structure(s).

Abstract: Disclosed herein are compositions and methods for the treatment of otic disorders with steroid, NSAID, and/or adenosine triphosphatase (“ATPase”) modulator agents. In these methods, the steroidal, NSAID, and/or ATPase compositions and formulations are administered locally to an individual afflicted with an otic disorder, through direct application of these compositions and formulations onto or via perfusion into the targeted auris structure(s).

Abstract: Disclosed herein are compositions and methods for the treatment of otic disorders with steroid, NSAID, and/or adenosine triphosphatase (“ATPase”) modulator agents. In these methods, the steroidal, NSAID, and/or ATPase compositions and formulations are administered locally to an individual afflicted with an otic disorder, through direct application of these compositions and formulations onto or via perfusion into the targeted auris structure(s).

Abstract: The present invention relates to processes for obtaining abiraterone and derivatives thereof, such as abiraterone acetate, by means of a Suzuki coupling through a steroid borate of general formula (IV) or a C—C coupling through a steroid hydrazone of general formula (II), as well as to intermediates useful in said processes.

Abstract: Compounds of formula (I) wherein: the groups are as defined in the description, are useful for the preparation of medicaments for the treatment of cardiovascular disorders, in particular heart failure and hypertension. The compounds are inhibitors of the enzymatic activity of the Na+, K+-ATPase. Said compounds are used for the preparation of a medicament for the treatment of a disease caused by the hypertensive effects of endogenous ouabain, such as renal failure progression in autosomal dominant polycystic renal disease (ADPKD), preeclamptic hypertension and proteinuria and renal failure progression in patients with adducin polymorphisms.

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: A compound with general formula I for treatment of various diseases of the central nervous system, in treatment of neuropsychiatric disorders related to imbalance of glutamatergic neurotransmitter system, ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, PTSD and other diseases related to stress, anxiety, schizophrenia and psychotic disorders, pain, addictions, multiple sclerosis, epilepsy and gliomas.

Abstract: The present invention relates to extracted lipid with high levels, for example 90% to 95% by weight, oleic acid. The present invention also provides genetically modified plants, particularly oilseeds such as safflower, which can used to produce the lipid. Furthermore, provided are methods for genotyping and selecting plants which can be used to produce the lipid.

Abstract: The invention relates to a method for obtaining and purifying phytosterols and/or tocopherols from distillation residue from a transesterification of vegetable oils, in particular from the vegetable oil-based fatty acid methyl ester production for the field of use of biodiesel (FAME), comprising a first transesterification stage for converting partial glycerides contained in the distillation residue; separating the glycerin phase from a reaction mixture resulting from the first transesterification stage; a second transesterification stage for converting sterol esters contained in the reaction mixture; adding water to the reaction mixture after the second transesterification stage in order to generate a multiphase system; simultaneously or sequentially separating the phases of the multiphase system into a substantially sterol-containing phase; a substantially glycerin- and methanol-containing aqueous phase; and a tocopherol-containing methyl ester phase; and obtaining phytosterols from the sterol-containing ph

Abstract: The invention disclosed herein relates to methods and means for allocating, allotting, apportioning, dispensing, distributing, preparing, portioning, meting out and/or otherwise providing, controlling and/or regulating access to quantities of foods, beverages, and/or other substances. Various embodiments of the methods and means of the invention may be performed by and/or implemented in hardware, in software, by one or more entities, and/or by some combination of hardware, software and/or one or more entities.

Abstract: Provided are methods and compositions for reducing superoxide anions such that a prophylactic or therapeutic effect against conditions associated with excess oxidative stress achieved. The compositions and methods provide for reducing inflammation and for enhancing lifespan of eukaryotic organisms. A screen for identifying compounds that can be used in these methods is also provided.

Abstract: The invention relates to a process for the preparation of a compound of formula wherein R1 and R2 are as defined in the description, by reaction of a compound of formula (II) with a base. Compound (I) is an intermediate useful in the preparation of gestodene.

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 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: Drug carriers, methods of synthesizing, and methods of use thereof are provided.

Abstract: The invention relates to hybrid molecules made of two lipids or lipid-analogous compounds which are linked to each other via their lipophilic end. The hybrid molecules thereby have at least one hydrophilic group at their hydrophilic end for increasing the hydration shell of the hybrid molecule. The hybrid molecules according to the invention can be used as pharmaceutical or as a cosmetic preparation.

Abstract: Substituted estratriene compounds of formula (I) useful in therapy, especially in the treatment or inhibition of a steroid hormone dependent disorder requiring the inhibition of a 17?-hydroxysteroid dehydrogenase (17?-HSD) type 1, type 2 and/or type 3 enzyme, as well as their salts, pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Abstract: The invention relates to 21-keto triterpene compounds of formula (I): wherein R1, X, and Y are as defined herein, and pharmaceutically acceptable salts and solvates thereof. These compounds exhibit significant anti-HIV activity. Thus, the invention also relates to methods for prevention or treatment of HIV infections by administering therapeutically effective amounts of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof to a subject in need of such treatment.

Abstract: A saponin or a sapogenin, or a saponin or sapogenin derivative, from a plant of the capsicum genus for use in the treatment of a disease other than eczema and dermatitis. A process for preparing a plant of the capsicum genus, extracts, or seeds thereof for use as a medicament suitable for the treatment of diseases other than skin conditions which process comprises storing the plant, extracts or seeds thereof at a temperature of 20° C. or below.

Abstract: The present invention relates to a method of producing a phytosterol ester and/or a phytostanol ester comprising: a) admixing a phospholipid composition comprising at least between about 10% to about 70% plant phospholipid and at least about 5% water; a lipid acyltransferase; and a phytosterol and/or a phytostanol; and b) separating or isolating or purifying at least one phytosterol ester and/or phytostanol ester from said admixture. The present invention also relates to compositions comprising the phytosterol ester and/or phytostanol ester produced by this method, including foodstuffs and personal care product (cosmetic) compositions.

Abstract: A method of making biofuels and valuable food and neutraceutical products includes dewatering intact algal cells to make an algal biomass, extracting neutral lipids along with carotenoids and chlorophylls from the algal biomass, and separating the carotenoids and chlorophylls. The remaining neutral lipids are esterified with a catalyst in the presence of an alcohol. The method also includes separating a water soluble fraction comprising glycerin from a water insoluble fraction comprising fuel esters and distilling the fuel esters under vacuum to obtain a C16 or shorter fuel esters fraction, a C16 or longer fuel ester fraction, and a residue comprising omega-3 fatty acids esters and remaining carotenoids. The method further includes hydrogenating and deoxygenating at least one of (i) the C16 or shorter fuel esters to obtain a jet fuel blend stock and (ii) the C16 or longer fuel esters to obtain a diesel blend stock.

Abstract: The present invention provides methods of designing molecularly imprinted polymers (MIPs) which have applications in extracting bioactive compounds from a range of bioprocessing feedstocks and wastes. The present invention is further directed to MIPs designed by the methods of the present invention.

Abstract: The present invention relates to the identification of an intranucleosomal DNA loop formed during transcription through a nucleosome and use of the same to identify an agent that modulates the RNA Polymerase II-histone surface.

Abstract: A new industrial process for the synthesis of solvate-free 17?-acetoxy-11?-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione [CDB-2914] of formula (I) which is a strong antiprogestogene and antiglucocorticoid agent. The invention also relates to compounds of formula (VII) and (VIII) used as intermediates in the process.

Abstract: Polymeric platinum amidomalonate complexes, where the platinum is in +2 or +4 oxidation state, and where the complexes optionally contain tumor seeking groups, are useful in the treatment of cancer.

Abstract: Disclosed are compositions and methods for targeted drug delivery using image-guided energy deposition to help localize active compounds to particular sites within the body of an animal. Also provided are compounds and formulations thereof for use in the targeted administration of therapeutically, prophylactically, and/or diagnostically effective amounts of such agents to a population of cells or tissues of a mammal in need thereof.

Abstract: The invention relates to a method for the fractionation of knotwood extract, which has been obtained by extraction of knotwood with a hydrophilic solvent. The hydrophilic extract is extracted with a lipophilic solvent to remove lipophilic impurities. The invention also relates to the use of a liquid-liquid extraction for the purification of hydrophilic knotwood extract. The present process provides a purified knotwood extract, which contains more than 90% lignans, flavonoids and stilbenes and less than 10% impurities selected from resin acids, fatty acids, sterols, juvabiones, triglycerides and combinations thereof.

Abstract: Compositions and methods for administering a therapeutic agent to a mammal are disclosed. The compositions comprise either (i) vesicles comprising an amphiphilic substituted fullerene, wherein the therapeutic agent is present in the vesicle interior or between layers of the vesicle wall, (ii) a substituted fullerene, comprising a fullerene core and a functional moiety, wherein the therapeutic agent is associated with the substituted fullerene, or (iii) carbon nanotubes, wherein the therapeutic agent is covalently bonded to the carbon nanotubes.

Abstract: The invention relates to methods to prevent, treat, ameliorate or slow the progression of one or more of a blood cell deficiency, unwanted inflammation, allergy, immune suppression condition, immunosenescence, autoimmune disorder, infection, neurological disorder, cardiovascular disorder, pulmonary disorder, trauma, hemorrhage, bone fracture or unwanted or excess bone loss with steroid compounds containing carbon-carbon double bonds within the fused four-ring system such that the steroid compounds are unsaturated. The unsaturated steroid compounds include 3,16?,17?-trihydroxy-7-acetoxy-androst-1,3,5(10),6-tetraene, 3,16?,17?-trihydroxy-7-methoxy-androst-1,3,5(10),6-tetraene, 3,17?-dihydroxy-7-acetoxy-16?-fluoro-androst-1,3,5(10),6-tetraene, 3,17?-dihydroxy-7-methoxy-16?-fluoro-androst-1,3,5(10),6-tetraene, 3,17?-dihydroxy-7,16?-diacetoxy-androst-1,3,5(10),6-tetraene and 3,17?-dihydroxy-7-methoxy-16?-acetoxy-androst-1,3,5(10),6-tetraene.

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 relates to a method for preparing 2-alkoxy and 2-aryloxyestrogen compounds, and the intermediate compounds prepared during the use of this method, which intermediate compounds are useful intermediates in the preparation of certain physiologically active compounds.

Abstract: Compounds of formula (I) wherein: the groups are as defined in the description, are useful for the preparation of medicaments for the treatment of cardiovascular disorders, in particular heart failure and hypertension. The compounds are inhibitors of the enzymatic activity of the Na+, K+-ATPase. Said compounds are used for the preparation of a medicament for the treatment of a disease caused by the hypertensive effects of endogenous ouabain, such as renal failure progression in autosomal dominant polycystic renal disease (ADPKD), preeclamptic hypertension and proteinuria and renal failure progression in patients with adducin polymorphisms.

Abstract: The invention discloses a steroid compound having the formula (1), wherein dotted bonds represent optional double bonds; R6 is H, ?CH2, or —CH3, or —CH2—CH3; R7 is H, C1-4-alkyl, C2-5 alkenyl or C2-5-alkynyl, wherein the alkyl, alkenyl or alkynyl group may be substituted with 1 to 3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; R11 is H, C1-4-alkyl, C2-4-alkenyl, C2-4-alkynyl or C1-4-alkylidene, wherein the alkyl, alkenyl, alkynyl or alkylidene group may be substituted with 1-3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; E represents together with carbon atoms 16 and 17 of the steroid skeleton a four to seven-membered ring, said ring being ? and in cis-configuration with respect to the steroid skeleton, optionally comprising one or two endocyclic bonds; or a prodrug thereof. Such compounds can be used in therapy and for methods for selective modification of the activity of estrogen receptors.

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 presently disclosed subject matter is directed to metallo-oxidoreductase inhibitors having metal binding moities linked to a targeting moiety through a linking group or a direct bond, methods for screening for metallo-oxidoreductase inhibitors, and methods of treating an oxidoreductase related disorder by administering a metallo-oxidoreductase inhibitor to a subject in need of treatment thereof.

Abstract: A method for preparing porous microparticles containing phytosterol, by preparing a homogeneous melt of phytosterol and a partially water soluble component, cooling the melt to obtain an amorphous solid material, processing the material into a fine powder, and bringing the powder into contact with an aqueous phase under stirring conditions. A composition suitable for preparing a porous microparticle containing phytosterol. A porous microparticle containing phytosterol. A pharmaceutical or food product useful for lowering the cholesterol level in blood.

Abstract: A solid, implantable dosage form comprising a therapeutically active agent in solid form, optionally with one or more pharmaceutically acceptable excipients, wherein the one or more excipients, when present, do not lead to a significant delay or prolongation of the release of active agent, as compared to an equivalent dosage form containing no excipients when tested in vitro.

Abstract: A method of fractionating biomass, by permeability conditioning biomass suspended in a pH adjusted solution of at least one water-based polar solvent to form a conditioned biomass, intimately contacting the pH adjusted solution with at least one non-polar solvent, partitioning to obtain an non-polar solvent solution and a polar biomass solution, and recovering cell and cell derived products from the non-polar solvent solution and polar biomass solution. Products recovered from the above method. A method of operating a renewable and sustainable plant for growing and processing algae.

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: The present invention relates to Y-shape branched PEG derivatives of formulae (I) to (IV). The present invention also relates to conjugates of these Y-shape derivatives and drug molecules, pharmaceutical compositions comprising those conjugates.