Abstract: Novel mutant ESR1 molecules and uses are disclosed.

Abstract: The present disclosure describes treatment compositions and methods for preventing and/or treating microbial infections of ciliated tissues, such as tissues of the trachea, lungs, and sinuses. The method utilizes a treatment composition that includes a cationic steroidal antimicrobial (CSA) compound, a poloxamer, and a carrier, which is administered to ciliated tissue, such as lung tissue, in order to prevent or treat a microbial infection by killing microbes associated with the ciliated tissue. The poloxamer forms micelles that encapsulate the CSA compound, the poloxamer being included in the treatment composition in an amount, by weight, that is about 100 to 1000 times the amount of the CSA compound.

Abstract: This invention relates to the use of the combination of 25-hydroxyvitamin D3 (“25-OH D3”) and antioxidants/anti-inflammatories (ascorbic acid vitamin E and canthaxanthin) to make a premix or feed which can ameliorate various problems observed in poultry which have been subject to overfeeding. Feeds containing the 25-OH D3 and antioxidants/anti-inflammatories and premixes are also provided.

Abstract: Described are oxysterols, pharmaceutical compositions including the oxysterols, and methods of using the oxysterols and compositions for treating diseases and/or disorders related to myelin injury, such as neonatal brain injury, traumatic brain injury, spinal cord injury, cerebral palsy, seizures, cognitive delay, multiple sclerosis, stroke, autism, leukodystrophy, schizophrenia and bipolar disorder.

Abstract: Disclosed is a method and an oral composition for treating CNS disorders. An embodiment of the invention comprises orally administering an allopregnanolone containing composition to a subject having a CNS disorder. Exemplary CNS disorders include sleep disorders, mood disorders, dysthymic disorders, bipolar disorders, anxiety disorders, stress disorders, compulsive disorders, schizophrenia spectrum disorders, convulsive disorders, memory disorders, cognition disorders, movement disorders, personality disorders, autism spectrum disorders, substance abuse disorders, dementia, pain, traumatic brain injury (TBI), vascular disease, withdrawal syndrome, and tinnitus. The composition and methods disclosed herein exhibit effective oral absorption/bioavailability.

Abstract: Provided is a composition for prevention or treatment of an allergic disease, the composition including an inotodiol compound and a chaga mushroom (Inonotus obliquus) extract including an inotodiol compound as an active ingredient. More particularly, it was found that when an inotodiol compound or a chaga mushroom extract containing an inotodiol compound as one of the active ingredients is administered to a mouse model in which a food allergy was induced, symptoms induced by the allergy were alleviated and cured. Thus, the inotodiol compound or the chaga mushroom extract containing an inotodiol compound as an active ingredient is expected to be useful as a composition for prevention or treatment of an allergic disease.

Abstract: The present invention relates to the use of Nor-UDCA in the treatment of hepatic steatosis in patients having a hepatic fat fraction of greater than 10%.

Abstract: Methods of treating, reducing, or preventing lung infections or lung inflammation include identifying a patient in need of treatment and administering a therapeutically effective amount of at least one cationic steroid antimicrobial (CSA), or a pharmaceutically acceptable salt thereof. Treatment of cystic fibrosis lung infections, COPD lung infections, inflammation of the lungs in these patient populations, and lung scarring in these patient populations is also described.

Abstract: The invention features methods of treating disorders related to increased levels of myeloid derived suppressor cells such as cancer or infections. The disclosure also provides methods of treating cancer including combinations of LXR? agonists and immunotherapies such as PD1 inhibitors, PDL1 inhibitors, and adoptive T-cell transfer therapy.

Abstract: This disclosure provides pharmaceutical compositions for delivering estradiol to a subject in need thereof, as well as methods of administering the compositions, and methods of using them.

Abstract: The invention relates to compounds, compositions and polymers comprising a first component adapted to promote germination of Clostridium difficile (C. diff) and a second component which acts as an antimicrobial agent. Said compounds, compositions and polymers are useful for destroying C. diff where conventional antimicrobial agents are unsuccessful. The compositions can be formulated as coating or materials which actively destroy C. diff which come into contact with it. The germination promotion is induced by bile salts. The invention also relates to the use of such materials as a treatment for C. diff associated diseases and toxic megacolon.

Abstract: The present invention relates to solid pharmaceutical compositions, in particular to oral contraceptives, comprising a progestogen, such as drospirenone; an estrogen, such as ethinylestradiol; a tetrahydrofolic acid or a pharmaceutically acceptable salt thereof, such as calcium 5-methyl-(6S)-tetrahydrofolate; and at least one pharmaceutical acceptable excipient or carrier. The compositions of the invention provide good stability of the tetrahydrofolic acid upon storage while still ensuring a fast and reliable release of the estrogen and the progestogen present in the composition.

Abstract: Methods of preventing and/or treating ischemia, organ dysfunction and/or organ failure, including multiple organ dysfunction syndrome (MODS), and necrosis and apoptosis associated with organ dysfunction/failure, are provided. For instance, the methods involve contacting organ(s) with an oxygenated cholesterol sulfate (OCS), e.g. 5-cholesten-3,25-diol, 3-sulfate (25H-C3S). The organ(s) may be in vivo (e.g. in a patient that is treated with the OCS) or ex vivo (e.g. an organ that has been harvested from a donor and is to be transplanted).

Abstract: A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

Abstract: The present disclosure provides methods of treating breast cancer including administering aqueous suspensions comprising solubilized fulvestrant, non-solubilized fulvestrant particles having one or more of an LD Dv(10) between about 1.5 and about 2.1 microns, an LD Dv(50) between about 5.5 and about 9.0 microns, and an LD Dv(90) between about 15 and about 35 microns, with the aqueous suspensions further including a surfactant, a polyvinylpyrrolidone, and a sugar alcohol, and a water-soluble excipient. The water-soluble excipient can be an aryl-Ci-6alk-OH, a Ci-6alkyl-OH, a buffering salt, a polysorbate, a polyalkylene glycol, a Ci-i2alkylene glycol, a phosphatidylcholine, or a combination thereof.

Abstract: Methods for treating or reducing the likelihood of acquiring estrogen-related (e.g. estrogen-exacerbated) diseases including endometriosis include administering to a patient a selective estrogen receptor modulator (SERM), in combination with inhibiting ovarian secretions, e.g., by administering an LHRH agonist or antagonist. In some embodiments, a precursor of sex steroids, said precursor being selected from the group consisting of dehydroepiandrosterone (DHEA), dehydroepiandrosterone sulfate (DHEA-S), androst-5-ene-3?,17?-diol (5 diol), and androstenedione or a compound transformed into one of these, is also administered.

Abstract: Compositions comprising bile acids or their salts and methods of use thereof for the treatment of residual lesions of vascular anomalies.

Abstract: Disclosed herein are methods of treating, reducing, or preventing a disease such as oral mucositis, gastric mucositis, or inflammatory fibrosis, comprising identifying a patient in need of treatment and administering a therapeutically effective amount of at least one cationic steroid antimicrobial (CSA), or a pharmaceutically acceptable salt thereof. Kits comprising such compositions and instructions on such methods are also contemplated herein.

Abstract: The presently claimed invention relates to a color developer, a process for its manufacture and its use as a component in heat sensitive recording material. The heat sensitive recording material is useful for thermographic printing.

Abstract: The present invention generally relates to a specific pregnenolone derivative for its use for the treatment of a Cannabinoids-Related Disorder. More particularly, the invention relates to a compound of Formula (I) for its use in the treatment of a Cannabinoids-Related Disorder. Indeed, the compound of the invention is in vivo very potent in inhibiting the effects of THC, and is able to inhibit both unconditioned and conditioned effects of THC including THC self-administration and reinstatement in THC seeking in non-human primates.

Abstract: A combination storage and sterilization device for fake eyelashes is a portable device that houses and disinfects all types of fake eyelashes including eyelash extensions and eyelash tools. The device includes a casing, a drawer, a cover, and a sterilization mechanism. The sterilization mechanism may include a UV bulb, a power source such as batteries, and a control circuit with a timer to automatically turn on and off the sterilization mechanism. The device may further include additional compartments for storing tools and accessories associated with fake eyelashes.

Abstract: The invention provides corticosteroids that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the corticosteroid not attached to the water-soluble oligomer.

Abstract: Described are oxysterols, pharmaceutical compositions including the oxysterols, and methods of using the oxysterols and compositions for treating diseases and/or disorders related to myelin injury, such as neonatal brain injury, traumatic brain injury, spinal cord injury, cerebral palsy, seizures, cognitive delay, multiple sclerosis, stroke, autism, leukodystrophy, schizophrenia and bipolar disorder.

Abstract: The present invention pertains to an oral preparation having exceptional elutability, the oral preparation containing obeticholic acid or a pharmacologically acceptable salt thereof, a water-soluble excipient, a disintegrating agent, and a water-soluble polymer binder, wherein the oral preparation is a quick-release tablet.

Abstract: Compositions comprising 2-((5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenyloxy)butanoic acid, an ester derivative, or a pharmaceutically acceptable salt thereof; a triglyceride; and a surfactant, as well as methods for their use. The present disclosure further relates to self-emulsifying drug delivery systems, such as SEDDS, SMEDDS, or SNEDDS comprising 2-((5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenyloxy)butanoic acid.

Abstract: Described herein are synthetic progestogens, such as 6?,7?:15?,16?-Dimethylene-3-oxo-17?-pregn-4-ene-21,17-carbolactone, as well as pharmaceutical compositions comprising the same. Also described are methods of use.

Abstract: Described herein are synthetic progestogens, such as 6?,7?:15?,16?-Dimethylene-3-oxo-17?-pregn-4-ene-21,17-carbolactone, as well as pharmaceutical compositions comprising the same. Also described are methods of use.

Abstract: Novel mutant ESR1 molecules and uses are disclosed.

Abstract: Disclosed herein is, among other things, a soft gel vaginal pharmaceutical composition and dosage form containing solubilized estradiol for the treatment of vulvovaginal atrophy (VVA) and female sexual dysfunction (FSD).

Abstract: Disclosed are a pentacyclic triterpene compound as shown in general formula (I) and a preparation method therefor. The compound has an effective antagonistic effect on FXR receptors.

Abstract: The present invention relates to a composition for preventing, treating, or alleviating ischemia-reperfusion injury, containing bile acid. According to the present invention, bile acid increases intranuclear beta-catenin levels, interferes with the opening of a mitochondria permeable transition pore (mPTP), and has excellent effects, in ischemia-reperfusion injury animal models, of alleviating tissue injury and reducing the size of infarcts, thereby being usable in the prevention, treatment, or alleviation of ischemia-reperfusion injury.

Abstract: Described herein are synthetic progestogens, such as 6?,7?:15?,16?-Dimethylene-3-oxo-17?-pregn-4-ene-21,17-carbolactone, as well as pharmaceutical compositions comprising the same. Also described are methods of use.

Abstract: The present disclosure provides methods for stabilizing a colloidal dispersion during transport for low defect tolerance applications. The methods involve eliminating fluid interfaces within a dispersion, storing the dispersion in an environment of inert gas, and degassing the dispersion. Several bottle closure devices are described which may be ideal for use with these methods, being able to seal a container filled with a dispersion, permit the removal of headspace and rapidly empty the contained dispersion. In one aspect, the device includes a vented cap and semi-permeable membrane, which allows the passage of gas into and out of the container, and a dispenser nozzle integrated with the device to allow a stored dispersion to be dispensed without removing the device from the container. In another aspect, the bottle closure device includes an attachment point for a removable downtube and dispenser nozzle.

Abstract: Compounds are provided according to Formula (A): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, R3, R4, R5, R6, and RG are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

Abstract: The present invention relates to the use of non-bioconvertible C3-substituted pregnenolone derivatives of formula (I), with no significant affinity for hormonal receptors or receptors of the central nervous system, in the treatment of substance use disorders, and in particular of alcohol use disorder.

Abstract: The present invention relates to methods and novel intermediates useful in the preparation of a compound of formula (A) or a pharmaceutically acceptable salt thereof, comprising converting the aldehyde of a compound of formula (B) with a reducing agent to prepare a compound of formula (C) and converting the compound of formula (C) with a sulfating reagent to prepare a compound of formula (A). An objective of the present invention is to provide methods of preparing bile acid derivatives and novel intermediates. A use of the methods and intermediates described relates to the synthesis of bile acid derivatives which activate both FXR and TGR5.

Abstract: The invention refers to a process for preparing sterile active pharmaceutical ingredients (APIs) useful in the preparation of sterile product for ophthalmic use. The process comprises the gamma-ray sterilization treatment of the APIs powder in a protective atmosphere.

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds which inhibit Hedgehog signaling. Also described herein are methods for using such Hedgehog signaling inhibitors, alone or in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of Hedgehog signaling.

Abstract: Compositions and kits including an agent that inhibits the interaction between Disabled-2 and mutant CFTR proteins, optionally in combination with a CFTR corrector, CFTR potentiator, CAL inhibitor, mucolytic, anti-inflammatory agent or a combination thereof are provided as are methods for preventing or treating cystic fibrosis.

Abstract: The present invention provides a process for preparation of deoxycholic acid or salt thereof; the process comprises the steps of reacting the compound of formula II to obtain a compound of formula III; the compound of formula III is converted to a compound of formula IV and the compound of formula IV is converted to deoxycholic acid. The present invention also provides a process for the purification of deoxycholic acid or salt thereof.

Abstract: Compounds of formula (I), wherein Ar is an aryl group optionally further substituted with one or more groups R3; A is a lipophilic, hydrophobic moiety; R1 is a phosphodiester, phosphotriester, thioether or amide group; X is an unsubstituted or substituted C6 to C24 alkylene or alkenylene group, which is optionally interrupted by one or more —NR9—, —O— or —S— linkages, R2 is —YC(R4)(R5)CO2R6; and pharmaceutically acceptable salts or solvates thereof are useful as endosomolytic agents particularly for the delivery of nucleic acids useful in gene therapy.

Abstract: Methods of reducing hepatitis delta virus (HDV) viral loads in a patient are provided. In some embodiments, the method comprises treating the patient with lonafarnib-ritonavir co-therapy. In some embodiments, the method further comprises treating the patient with an interferon.

Abstract: The present application provides Compound 1: or a pharmaceutically acceptable salt or amino acid conjugate thereof. The present invention relates to an FXR activator and to methods of making and using said compound.

Abstract: A topical application formulation of estrogen and estrogen analogs or other estrogen receptor modulators is disclosed for the treatment of primary or secondary dry eye syndrome (also known as keratoconjunctivitis sicca (KCS)). Preferred formulations include 17-?-estradiol and its derivatives in lipid, liposomes, polymers, or aqueous or non-aqueous vehicles for the topical treatment of the ocular surface tissues particularly as time-release or micro-dose formulations. These formulations may also be useful in treating other conditions where KCS may occur, such as post-operative refractive surgery and corneal transplant patients.

Abstract: The application relates to compounds of formula A: or a salt, solvate, ester, tautomer, amino acid conjugate, or metabolite thereof. The compounds of formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.

Abstract: Compounds are provided according to Formula (I): Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein R1, R2, R3, R6, R7, R8, and n are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

Abstract: The disclosure relates to obeticholic acid formulations with improved stability, dissolution, and/or solubility, methods of preparing the same for use and methods of treating various diseases and conditions.

Abstract: The present invention relates to processes for preparing compounds of Formula (I) and compounds of Formula (II): These compounds are useful as FXR or TGR5 modulators.

Abstract: Capsicum compositions are described that include biologically active constituents non-capsaicinoids and capsaicinoids in a specific ratio are useful for the treatment and management of cardiometabolic syndrome and associated risk factors, in a subject in need thereof. The capsicum compositions include a capsicum extract which is prepared by extracting capsicum pods by using suitable polar and non-polar solvents. Capsicum compositions include non-capsaicinoid components like saponins and polyphenols such as flavonoids, which along with capsaicinoids effectively reduce risk factors of cardiometabolic syndrome and also reduce oxidative stress on vital body organs by reducing inflammatory and/or oxidative markers. The capsicum compositions inhibit pancreatic lipase enzyme and enhance lipolysis, when administered in an effective amount to a subject in need thereof. Capsicum compositions as described herein are prepared by human intervention and are safe for consumption.

Abstract: The present invention relates to tricyclic compounds of formula (I) and formula (II), or a pharmaceutically acceptable salt thereof. The present tricyclic compounds are useful non-systemic TGR5 agonists that can be used to treat diabetic diseases in human. The present invention provides a pharmaceutical composition containing tricyclic compounds of formula (I) and formula (II) and a method of making as well as a method of using same in treating patients inflicted with metabolic disorders by administering same. The compounds of the present invention may be used in combination with additional anti-diabetic drugs.