Abstract: This disclosure relates to progesterone phophate derivatives and uses related thereto. In certain embodiments, the disclosure relates to compounds disclosed herein and uses for managing inflammation such as those resulting from traumatic brain injury or stroke.

Abstract: The present invention provides phosphonate conjugates and methods of preparing the phosphonate conjugates so as to allow, for example, improved methods and compounds for modifying the surface of a nanoparticle to increase in vivo circulation times and targeted delivery performance.

Abstract: Ursodeoxycholic acid (UDCA) is a bile acid with demonstrated anti-apoptotic activity in both in vitro and in vivo models. Water-soluble prodrugs of UDCA for use in indications where intravenous administration of UDCA may be preferable, such as reducing damage from stroke or acute kidney injury, are disclosed. The disclosed prodrugs showed significant anti-apoptotic activity in a series of in vitro assays.

Abstract: This invention discloses a novel compound with the structure of formula I, or pharmaceutically acceptable salts or solvates thereof. In addition, the invention further discloses a method for preparing the compound, a pharmaceutical composition containing the compound, and use thereof in the preparation of a hypoglycemic medicament.

Abstract: Provided is a ultra-high-sensitivity assay in which the assay can be made on a commonly used assay apparatus such as an absorptiometer and a plate reader or with naked eyes. The high-sensitivity assay in which the assay can be made on a commonly used assay apparatus or with naked eyes can be provided by combining an enzyme cycling method using thio-NAD(P) as a coenzyme, a labeling enzyme and a substrate for the labeling enzyme optimally, and by amplifying thio-NAD(P)H, which is a signaling substance, exponentially and then quantifying the thio-NAD(P)H colorimetrically.

Abstract: The invention provides formulations that contain an immunogenic or immunostimulatory cargo, delivery moiety and/or lipid, and a lipid that functions to reduce or prevent induction in a subject of an immune response which would otherwise occur when the immunogenic or immunostimulatory cargo, delivery moiety and/or lipid is administered to a subject as a component of an appropriate control formulation lacking the immune response reducing lipid. Specific immune response reducing lipids and uses thereof are further provided.

Abstract: The present invention provides phosphonate conjugates and methods of preparing the phosphonate conjugates so as to allow, for example, improved methods and compounds for modifying the surface of a nanoparticle to increase in vivo circulation times and targeted delivery performance.

Abstract: This invention discloses a novel compound with the structure of formula I, or pharmaceutically acceptable salts or solvates thereof. In addition, the invention further discloses a method for preparing the compound, a pharmaceutical composition containing the compound, and use thereof in the preparation of a hypoglycemic medicament.

Abstract: A prodrug of 2-methoxyestradiol (2-ME2) can be used for prophylaxis or treatment of cancer, such as esophageal cancer, prostate cancer, or breast cancer, and/or a non-cancerous condition, such as rheumatoid arthritis or pre-clampsia.

Abstract: The present invention relates to a process for the preparation of phosphoric esters, and to selected compounds.

Abstract: The present invention is directed to cationic lipid for the delivery of oligonucleotides and methods of modulating an expression of a targeted gene using the nanoparticle compositions. In particular, the invention relates to cholesterol and its derivatives having multiple positively charged moieties via branching spacers, and nanoparticle compositions of oligonucleotides encapsulated in a mixture of a cationic lipid, a fusogenic lipid and a PEG lipid.

Abstract: The present invention is directed to releasable cationic lipids and nanoparticle compositions for the delivery of nucleic acids and methods of modulating an expression of a target gene using the same. In particular, the invention relates to cationic lipids including an acid labile linker, and nanoparticle compositions containing the same.

Abstract: Disclosed are sterol-modified amphiphilic lipid compounds having two or more hydrophobic tails of which at least one is a sterol. Also disclosed are the processes for the synthesis of these compounds, compositions comprising such compounds, and the use of such compounds in delivery of an agent of interest, e.g., therapeutics, imaging agents, contrast materials for ultrasound applications, vaccines, biosensors, nutritional supplements and skin care products.

Abstract: The present invention relates to novel compounds which are capable as acting as fluorescent sensors or which are precursors for these and for the use of these for the assay of biological processes such as posttranslational modifications of biological molecules such as phosphorylation, de-phosphorylation, proteolytic cleavage, phosphodiesterase mediated hydrolysis of cyclic nucleotides, methylation, acetylation of proteins peptides, DNA, lipids and the detection of biomolecule interactions (e.g., protein-protein interactions). A small molecule sensor is described which can associate to phosphorylated biological targets via metal ion—phosphate association. The association event can be monitored as fluorescence quench, sensitized emission, fluorescence polarization or a combination thereof.

Abstract: A process for obtaining 21-disodium phosphate pregnane derivative compounds of formula (I), wherein X?R?H or X?F and R=?-CH3 or X?F and R=?-CH3 comprises spray drying a solution comprising compound of formula (I).

Abstract: Compounds of the formula, A-L-B, wherein A is glutamate or a glutamate analog; L is a phosphoramidate or a phosphoramidate analog; and B is serine or a serine analog are described which are potent inhibitors of prostate-specific membrane antigen (PMSA). Such compounds are useful in treatment of prostate cancer; and when chemically attached to a fluorescent dye, can efficiently and selectively label prostate cancer cells for fluorescent imaging.

Abstract: The present invention relates to the methods for preparing synthetic guggulphospholipids, their fatty acid analogues and other bioactive molecules. The present invention relates to E-guggulsterone and Z-guggulsterone or mixture of E- and Z-guggulsterones. The present invention also provides a novel method for the preparation of E-guggulsterol and Z-guggulsterol or mixture of E- and Z-guggulsterols from a mixture of E- and Z-guggulsterones. The present invention further relates to guggulphospholipids and other bioactive molecules incorporated into complexes such as liposomes, complexes, emulsions, vesicles, micelles, and mixed micelles, which can include other active agents, such as hydrophobic or hydrophilic drugs for use, e.g., in treatment of human and animal diseases.

Abstract: The present invention relates to a novel delivery system for delivering therapeutic agents into living cells, and more particularly, to novel chemical moieties that are designed capable of targeting and/or penetrating cells or other targets of interest and further capable of binding therapeutic agents to be delivered to these cells, and to delivery systems containing same.

Abstract: The present invention is directed to novel 11-phosphorous steroid derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by a progesterone or glucocorticoid receptor.

Abstract: The present invention is directed to novel 17-phosphorous steroid derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by a progesterone or glucocorticoid receptor.

Abstract: This invention features permeability enhancer molecules, and methods, to increase membrane permeability of various molecules, such as nucleic acids, polynucleotides, oligonucleotides, enzymatic nucleic acid molecules, antisense nucleic acid molecules, 2-5A antisense chimeras, triplex forming oligonucleotides, decoy RNAS, dsRNAs, siRNAs, aptamers, or antisense nucleic acids containing nucleic acid cleaving chemical groups, peptides, polypeptides, proteins, carbohydrates, steroids, metals and small molecules, thereby facilitating cellular uptake of such molecules.

Abstract: A bisphosphonic acid of the general formula (I) wherein R1 is H, OH, C1-C6 alkyl C1-C6 alkoxy, C1-C6 hydroxyalkyl, C1-C6 aminoalkyl, C1-C6 halogen alkyl X is a direct bond, alkylen group with 1 to 20 carbon atoms, (CH3)m—(OCR3HCH2)n—(O)o—, wherein R3 is H or CH3 and m is 0 or a number from 1 to 6, n is a number from 1 to 10, preferably 1 to 6, and o is 0 or 1, —(CR4HCH2O)p—, wherein R4 is H or CH3, p is a number from 1 to 10, preferably 1 to 6, (CH3)q—(OCR5HCH2)r—(O)s—(CH3)t—, wherein R5 is H or CH3 and q is 0 or a number from 1 to 6, r is a number from 1 to 10, preferably 1 to 6, and s is 0 or 1, and t is a number from 1 to 6, R2 is a group of the formula (II) as well as their physiologically compatible derivatives in particular salts and trimethyl silyl derivatives.

Abstract: Bone targeted compounds and methods are provided. Compounds can include a Bone Targeting Portion (RT), having an affinity for bone; a Bone Active Portion (RA) for interacting with and affecting bone; a Linking Portion (RL) connecting the Bone Targeting Portion and the Bone Active Portion. The Bone Active Portion is derived from an estrogenic agent. Compounds can also include a Blocking Group (RP) that reduces or eliminates the estrogenic activity of the Bone Active Portion.

Abstract: Certain chemical entities chosen from compounds of Formula I: and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof are described. Pharmaceutical compositions comprising at least one chemical entity chosen from compounds of Formula I and a pharmaceutically acceptable vehicle are described. Also described are methods for inhibiting ?-2,3-sialyltransferase activity in cells, and methods for treating a patient having a disease responsive to inhibition of ?-2,3-sialyltransferase activity.

Abstract: A platinum complex having antitumor activity in which the metal ligands are dehydrocholic acid and phosphine.

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: Novel nitric-oxide releasing lipid molecules are provided which comprise a lipid molecule selected from (a) phosphoglycerides, (b) lipids having a sphingosine base as a backbone, (c) monoacylglyerols, (d) diacylglycerols, (e) glycosylacylglycerols, and (f) sterol compounds of the formula: 1

Abstract: This invention features conjugates, degradable linkers, compositions, methods of synthesis, and applications thereof, including cholesterol, folate, galactose, galactosamine, N-acetyl galactosamine, PEG, phospholipid, peptide and human serum albumin (HSA) derived conjugates of biologically active compounds, including antibodies, antivirals, chemotherapeutics, peptides, proteins, hormones, nucleosides, nucleotides, non-nucleosides, and nucleic acids including enzymatic nucleic acids, DNAzymes, allozymes, antisense, dsRNA, siNA, siRNA, triplex oligonucleotides, 2,5-A chimeras, decoys and aptamers.

Abstract: The present invention relates to novel estrogenic compounds. The present invention also relates to methods of treating estrogen deprivation in a subject comprising administering novel estrogenic compounds. Additionally, the present invention relates to methods of synthesizing novel estrogenic compounds.

Abstract: A novel class of compounds, i.e., 1,1-bis-H-phosphinates (or 1,1-bis-H-phosphinic acid derivatives) are provided. Also provided are novel methods for producing 1,1-bis-H-phosphinates and 1,1-bis-H-phosphinate conjugates. These compounds and conjugates are used as precursors of bisphosphonates and bisphosphonate conjugates, respectively, or as prodrugs directly for treating bone-related and various other diseases.

Abstract: This invention features conjugates, degradable linkers, compositions, methods of synthesis, and applications thereof, including cholesterol, folate, galactose, galactosamine, N-acetyl galactosamine, PEG, phospholipid, peptide and human serum albumin (HSA) derived conjugates of biologically active compounds, including antibodies, antivirals, chemotherapeutics, peptides, proteins, hormones, nucleosides, nucleotides, non-nucleosides, and nucleic acids including enzymatic nucleic acids, DNAzymes, allozymes, antisense, dsRNA, siNA, siRNA, triplex oligonucleotides, 2,5-A chimeras, decoys and aptamers.

Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16&agr;-bromo-3&bgr;-hydroxy-5&agr;-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% 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&agr;-bromo-3&bgr;-hydroxy-5&agr;-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.

Abstract: The present invention comprises compounds, compositions thereof, and methods capable of delivering a broad range of anionic molecules to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, and methods that enhance the ability of mammalian red blood cells to deliver oxygen, by delivering a ligand for the allosteric site of hemoglobin to the cytoplasm of the red blood cells.

Abstract: A compound of formula (I) and pharmaceutical acceptable salts, solvates, stereoisomers and prodrugs thereof, in isolation or in mixture, wherein, independently at each occurrence: R1 and R2 are selected from hydrogen, oxygen so as to form nitro or oxime, amino, sulfate, and sulfonic acid, and organic groups having 1-30 carbons and optionally containing 1-6 heteroatoms selected from nitrogen, oxygen, phosphorous, silicon, and sulfur, where R1 and R2 may, together with the N to which they are both bonded, form a heterocyclic structure that may be part of an organic group having 1-30 carbons and optionally containing 1-6 heteroatoms selected from nitrogen, oxygen and silicon, and where R1 may be a 2, or 3 atom chain to numeral 2 so that —N—R1— forms part of a fused bicyclic structure to ring A; R3 and R4 are selected from direct bonds to 6 and 7 respectively so as to form carbonyl groups, hydrogen, or a protecting group such that R3 and/or R4 is part of hydroxyl or carbonyl protecting group; nu

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: There is provided a compound comprising a steroidal ring system and a group R1 selected from any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein the D ring of the steroidal ring system is substituted by a group R2 of the formula —L—R3, wherein L is an optional linker group and R3 is an aromatic hydrocarbyl group.

Abstract: Certain novel sterol derivatives can be used for regulating the meiosis in oocytes and in male germ cells.

Abstract: Disclosed are novel bicyclic tris(anhydride)s useful as intermediates in the synthesis of biologically active compounds, and the compounds which may be synthesized from such intermediates.

Abstract: Bile-acid conjugates useful for sustained release of L-DOPA, inhibitors of catechol O-methyl transferase and/or inhibitors of L-aromatic amino acid decarboxylase are provided.

Abstract: Methods of treating a fungal or yeast infection and of killing or inhibiting fungi or yeast are disclosed. The methods use derivatives of triterpenes that are abundant in birch bark and other plants. The triterpenes include betulin, allobetulin, and lupeol.

Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.

Abstract: Newly isolated aminosterol compounds and pharmaceutical compositions based on the aminosterol compounds are described. Methods for the treatment of various disorders, for example, a microbial infection, are also described.

Abstract: A composition and method of preventing or inhibiting tumor growth and, more particularly, of treating a malignant tumor, using prodrugs of plant-derived compounds and derivatives is disclosed. In the method, a composition containing betulinic acid or a betulinic acid derivative is administered in a prodrug form to release betulinic acid or a betulinic acid derivative in vivo at the tumor site.

Abstract: The invention consists of a compound of the general formula (I) below: 1

Abstract: Bisphosphonate derivatives of hydroxy steroids which are bone resorption inhibitors or bone formation stimulators, the derivatives having at least one group A in place of a hydroxy group on the steroid molelcule, where A is a group of forumla (A) where X is: (i) St--O--CO-- where St is the residue of the hydroxy steroid given by removal of an OH group; or (ii) R.sup.1 --O--CO-- where R.sup.1 is an alkyl, alkenyl, cycloalkyl, aralkyl or aryl group, any of which may optionally be substituted, and the salts and solvates of these compounds. The steroid is typically 17.beta.-oestradiol, oestrone, testosterone, norethindrone, androsterone, norethandrolone or nandrolone. The derivatives can be used in the treatment of bone disorders such as osteoporosis.

Abstract: Steroid sulphatase inhibitors and pharmaceutical compositions containing them for use in the treatment of oestrone dependent tumors, especially breast cancer. The steroid sulphatase inhibitors are phosphonate esters of formula (I) ##STR1## where R is alkyl, alkenyl, cycloalkyl or aryl; and --O--polycycle represents the residue of a polycyclic alcohol such as a sterol, preferably a 3-sterol.

Abstract: A Chrysosporium strain No. CBS 123.95, mutants and derivatives thereof, and a method for preparing non-peptide compounds using said strain, are disclosed. Novel compounds of general formula (I), pharmaceutical compositions containing same, and the use of said compounds in anticancer treatments, are also disclosed.

Abstract: Compounds having a broad range of antimicrobial activity generally have a structure including asteroid nucleus with a cationic, preferably polyamine, side chain (X) and an anionic side chain (Y). The invention is also directed to compounds of the Formula III: ##STR1## preferably where the steroid ring nucleus is saturated; the steroid ring substituent Z.sub.5 is .alpha.-H; one Z.sub.7 is .beta.-H and the other is .alpha.-H or .alpha.-OH; both substituents Z.sub.12 are hydrogen; X' is a polyamine side chain of the formula --NH--(CH.sub.2).sub.p --NH--(CH.sub.2).sub.q --N(R.sup.II)(R.sup.III) where p and q are each independently 3 or 4, and R.sup.II and R.sup.III are each independently hydrogen or methyl; R' is methyl; and Y' is (C.sub.1 -C.sub.10)-alkyl substituted with a group such as --CO.sub.2 H or --SO.sub.3 H.

Abstract: Monomeric bile acid derivatives, processes for their preparation and the use of these compounds as medicamentsMonomeric bile acid derivatives of the formula IZ--X--GS I,in which GS, X and Z have the meanings given, and processes for their preparation are described. The compounds have useful pharmacological properties and can therefore be used as medicaments.

Abstract: The invention relates to substituted 17.alpha.-acyl steroidal 5.alpha.-reductase inhibiting compounds. The invention also relates to pharmaceutical compositions containing these compounds and their use for reducing prostate size and treating prostate adenocarcinoma. Further, the invention describes a process for making these compounds by heating the corresponding substituted 17.beta.-acyl steroid in a solvent, such as ethylene glycol or dimethyl sulfoxide (DMSO), in a base, such as sodium or potassium hydroxide.