Abstract: The present invention relates to fluorinated and alkylated bile acids.

Abstract: A hydrophobic cationic steroidal anti-microbial (ceragenin) compound forms an amphiphilic compound having a hydrophobic sterol face and a hydrophilic cationic face. The hydrophobic CSA also includes a hydrophobic substituent that gives the ceragenin compound a C Log P value of at least 6.0, 6.25, 6.5, 7.5, 8.5, or 10.

Abstract: The present invention relates to the synthesis and use of a novel trifluorinated bile acid analogue, that being, CA-sar-TFMA which is useful as an imaging probe, diagnostic agent or contrast agent and is resistant to bacterial deconjugation, wherein the trifluorinated bile acid analogue can be used as a 19F MRI tracer exhibiting an increased half-life due to its resistance to choloylglycine hydrolase.

Abstract: The present invention relates in one aspect to radiolabeled compounds comprising the structure of Formula 1. The radiolabeled compounds are preferably bile acids or bile acid derivatives. Further aspects of the invention relates to use of the compounds comprising the structure of Formula 1 in imaging methods such as for example PET, imaging method using a compound comprising the structure of Formula 1, administering said compound to an individual and making a radiographic image of a region of interest from said individual.

Abstract: A method of reducing heart failure or preventing sudden cardiac death in a subject in need thereof is carried out by administering a composition comprising a compound that increases cellular level of Sarco/endoplasmic reticulum Ca2+-ATPase 2a (SERCA2a). The invention represents a significant breakthrough in the treatment or prevention of chronic heart failure. The invention is based upon the discovery that a Mifepristone molecule increases the cellular level of SERCA2a protein.

Abstract: Described herein are aqueous and substantially non-aqueous oral compositions comprising a cationic steroidal compound and methods of making and using the same.

Abstract: The present invention relates to compounds of formula I, or a pharmaceutically acceptable salt thereof, for use in the treatment or prevention, suppression or amelioration of a disease mediated by the ROR gamma receptor in a subject in need thereof, in particular diabetes and diabetes-related disorders, specifically type II diabetes, methods of their production, as well as methods of treatment or prevention of such diseases.

Abstract: Polymorphic forms of onapristone and methods of making and using such polymorphic forms are provided. Crystalline polymorphic forms can be characterized by their X-ray powder diffraction patterns and other properties.

Abstract: The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compound that will yield or generate 3APS, either in vitro or in vivo.

Abstract: Provided herein are bile acid analogues and derivatives, methods of synthesizing bile acid analogues and derivatives and their use in treating diabetes and liver disease.

Abstract: Disclosed are compounds having the general formula: wherein R1-R4 and X are as defined herein, pharmaceutical compositions including such compounds, and a method of treating a patient involving antagonizing the endogenous progesterone, such as in inducing menses and treating endometriosis, dysmenorrhea, endocrine hormone-dependent tumors, meningiomas, uterine leiomyomas, or uterine fibroids, inhibiting uterine endometrial proliferation, inducing cervical ripening, inducing labor, and in contraception.

Abstract: The invention relates to compounds of formula (I): wherein R is ethyl, propyl or allyl, and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists.

Abstract: The invention relates to fatty acid statin conjugates and fatty acid FXR agonist conjugates; compositions comprising an effective amount of a fatty acid statin conjugate or a fatty acid FXR agonist conjugate; and methods for treating or preventing a metabolic disease comprising the administration of an effective amount of a fatty acid statin conjugate or a fatty acid FXR agonist conjugate.

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 a compound of formula (I): for its use as progesterone receptor antagonist, in particular for its use for the prevention and/or the treatment of cancer or uterine pathologies.

Abstract: This invention is directed to a process for the preparation of high yield alkyl or aryl iodide from its corresponding carboxylic acid using N-iodo amides.

Abstract: Described herein are compounds which either act as pure antiprogestins or as antiprogestins with partial agonistic activity and methods of treating cancer using such compounds.

Abstract: This invention relates to methods of preserving the integrity of peptides in the gut. In particular it concerns the use of certain compounds as inhibitors of gut proteases. Compounds identified as having gut protease inhibitory activity are biguanides, certain bile acids and pharmaceutically acceptable salts of these compounds. This activity makes these compounds useful for co-administration with prophylactic or therapeutic peptides. This invention relates to methods of inhibiting gut proteases and peptide formulations comprising these gut protease inhibitor.

Abstract: A process for the preparation of cholyl-L-lysine comprising the steps of: —(a) reacting N-?-CBZ-cholyl-L-lysine with a hydrogen source in the presence of a catalyst in a solvent comprising one or more alkanols; (b) removing the catalyst; (c) optionally diluting the resulting reaction mixture with water and optionally adjusting the pH of the resultant reaction mixture to a pH less than or equal to about 4; (d) removing the bulk of the alkanol whilst ensuring that the alkanol content of the resultant mixture is maintained above about 3% w/w of the remaining mixture; (e) extracting the resultant mixture from step (d) with an organic solvent; (f) adjusting the pH of the aqueous layer to a pH of about 4.5 or greater to precipitate cholyl-L-lysine; (g) isolate the precipitate.

Abstract: Methods of detecting at least one analyte and at least one nucleic acid in a sample are provided. Reagents for carrying out the methods are also provided.

Abstract: New methods are provided for synthesis of photoacid generator compounds (“PAGs”), new photoacid generator compounds and photoresist compositions that comprise such PAG compounds. In a particular aspect, sulfonium-containing (S+) photoacid generators and methods of synthesis of sulfonium photoacid generators are provided.

Abstract: A delivery agent for delivering a biologically active agent to a warm-blooded animal includes a hydrophobic moiety covalently bonded to a hydrophilic moiety. The hydrophobic moiety can include bile acids, sterols, or hydrophobic small molecules. The hydrophilic moiety can include ?-amino acids, dipeptides or tripeptides, or hydrophilic small molecules. An illustrative delivery agent is N?-deoxycholyl-L-lysine-methylester. The delivery agent and the biologically active agent are mixed together to form a complex, which is then administered to the animal. These complexes are particularly useful for oral administration of biologically active agents, but other routes of administration may be used.

Abstract: The present invention relates to a polymer comprising a cholane core having at least one derivatizable group covalently bonded thereto and a hydrophilic polymer chain covalently bonded to derivatizable group(s) and a process for producing it The present invention also relates to micellar aggregate formed from the polymer of the present.

Abstract: The present invention relates to compounds of formula (I) wherein: R1 is hydrogen or an alkyl group; R2 is hydrogen or a halogen, nitro, alkyloxy, amino or carboxy group; Y is CH2, oxygen or sulfur; n is an integer from 1 to 4, and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof for the treatment of FXR-mediated diseases or conditions.

Abstract: Described herein are compounds which exhibit progesterone antagonistic effects and methods of treating cancer using such compounds.

Abstract: A method of treating a disorder related to a high cholesterol concentration, comprising administering to a subject in need thereof a compound of formula (I): Also disclosed are methods, kits, combinations, and compositions for treating a disorder in a subject where an activator of liver X alpha is indicated, such as in, for example, treating a high cholesterol disease.

Abstract: Disclosed are methods for providing enhanced systemic blood concentrations of orally delivered drugs that are incompletely translocated across the intestinal wall of an animal. Also disclosed are methods for the sustained release of drugs, whether poorly or readily bioavailable via oral delivery to animals. Still further, disclosed are compounds and pharmaceutical compositions that are used in such methods.

Abstract: The present invention relates to compounds of formula (I) wherein: R1 is hydrogen or an alkyl group; R2 is hydrogen or a halogen, nitro, alkyloxy, amino or carboxy group; Y is CH2, oxygen or sulfur; n is an integer from 1 to 4, and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof for the treatment of FXR-mediated diseases or conditions.

Abstract: GPBAR1 for use as a target for selective inhibition of Th1 mediated immune responses.

Abstract: The invention provides novel compounds, methods for treating or preventing a condition related to ER-stress, e.g. hypercholesterolemia, atherosclerosis and related conditions, and pharmaceutical compositions related thereto.

Abstract: The present invention involves intermediates, including a 7?-substituted steroid (II), and processes which are used to prepare eplerenone, a useful pharmaceutical agent.

Abstract: The present invention involves intermediates, including a 7?-substituted steroid (II), and processes which are used to prepare eplerenone, a useful pharmaceutical agent.

Abstract: The invention describes new compounds as pharmaceutical active ingredients, which have in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo a preferential action on bone rather than the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The new compounds are 16?- and 16?-hydroxy-estra-1,3,5(10)-estratrienes, which carry additional substituents on the steroid skeleton and can have one or more additional double bonds in the B-, C- and/or D-rings.

Abstract: This invention relates to methods for treating asthma or allergy in a mammal by administering a 3-aminosteroid compound to a mammal in need thereof. The 3-aminosteroid compound being capable of down regulating the IL-9 pathway and alleviating asthmatic responses to allergen. Exemplary 3-aminosteroid compounds used in the methods of the invention include compounds having the chemical formula (I), wherein X, R1, R2, R3, and R4 groups are as defined herein. The invention also relates to certain novel compounds of formula (I). Moreover, the invention also provides methods for identifying an immunomodulatory 3-aminosteroid compound.

Abstract: A conjugated prodrug of an estradiol compound conjugated to a biological activity modifying agent.

Abstract: This invention is directed to methods for providing sustained systemic concentrations of therapeutic or prophylactic agents such as GABA analogs following oral administration to animals. This invention is also directed to compounds and pharmaceutical compositions that are used in such methods.

Abstract: A food additive useful for lowering serum cholesterol in humans contains a sterol or stanol ester of a fatty acid or a dicarboxylic acid ester of a sterol or stanol made by reacting a sterol, stanol and a carboxylic acid in the presence of an effective amount of a catalyst selected from the group consisting of calcium oxide, calcium hydroxide, a calcium salt of a carboxylic acid, magnesium hydroxide and combinations thereof described herein below.

Abstract: The invention relates to compounds of formula (I) 1

Abstract: Steroid derivatives of this invention interact with nuclear liver X receptor (LXR) and ubiquitous receptor (UR) and can be used to treat a variety of LXR- or UR-mediated disorders.

Abstract: A method of treating a disorder related to a high cholesterol concentration, comprising administering to a subject in need thereof a compound of formula (I): 1

Abstract: Substituted acylguanidines and their pharmaceutically tolerable salts and physiologically functional derivatives. Compounds of the formula I in which the radicals have the meanings indicated, and their physiologically tolerable salts, physiologically functional derivatives and a process for their preparation are described. The compounds are suitable, for example, as medicaments for the prophylaxis or treatment of gallstones.

Abstract: The invention relates to 17-methylene steroids, process for their production and pharmaceutical compositions that contain these compounds.

Abstract: Novel sterol/stanol esters of a conjugated fatty acid are provided through the esterification or transesterification of a sterol such as beta-sitosterol or a hydrogenated form thereof (stanol). Such novel esters exhibit the combined properties normally possess by the sterol/stanol compound and the conjugated fatty acid and as such are excellent additives for dietetic foods and supplements.

Abstract: A method for preparing at least one hydroxycholesterol chosen from the group consisting of 25-hydroxycholesterol, 17,25-dihydroxycholesterol and 25,26-dihydroxycholesterol by biological hydroxylation of cholesterol, and the aforementioned dihydroxycholesterols. In the above biological hydroxylation, a microorganism is used which has the abovementioned hydroxylation capacity and which belongs to the genus Amycolata and the genus Sphingomonas.

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: The present invention relates to bile acid or bile salt fatty acid conjugates (hereinafter called “BAFAC), to their use in dissolving cholesterol gallstones in bile, preventing their occurrence or recurrence, to their use in reducing or preventing arteriosclerosis and to methods for the treatment of said diseases. The conjugates are of the formula W—X—G in which G is a bile acid or bile salt radical, W stands for one or two saturated fatty acid radicals and X is either a direct bond or a bonding member between said bile acid or bile salt and the fatty acid(s). The conjugation is advantageously performed at a position selected among the 3, 6, 7, 12 and 24 positions of the bile acid or bile salt nucleus.

Abstract: A compound having the general formula: 1

Abstract: A series of novel steroid derivatives are described. The steroid derivatives are antibacterial agents. The steroid derivatives also act to sensitize bacteria to other antibiotics including erythromycin and novobiocin.

Abstract: Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering derivatives of 2-methoxyestradiol of the general formula: 1

Abstract: Multiple reaction schemes, process steps and intermediates are provided for the synthesis of epoxymexrenone, useful as a diuretic, and other compounds of Formula I wherein the variables are as defined by the specification.