Abstract: Pharmaceutical compositions for the topical administration of a drug to the pilosebaceous unit and methods for administering the same. As disclosed herein, the inventors of the present invention have made the surprising discovery that pharmaceutical compositions comprising small particles of an active pharmaceutical ingredient can be administered to the pilosebaceous unit. The pharmaceutical composition can comprise SHR0302 or spironolactone as an active pharmaceutical ingredient.

Abstract: Anti-cancer treatment and therapeutic methods are provided in which an antibody that binds specifically to glycosylated PD-L1 relative to unglycosylated PD-L1 and blocks binding of PD-L1 to PD-1 is administered to a subject in need in combination with an antibody that binds specifically to glycosylated PD-L1 relative to unglycosylated PD-L1, blocks binding of PD-L1 to PD-1 and also promotes internalization and degradation of PD-L1. The anti-cancer methods utilize antibodies that recognize specific epitopes on glycosylated PD-L1 protein, as well as antibodies that exhibit the IPD function of both blocking the binding of PD-L1 to PD-1 and also facilitating the internalization of PD-L1 on cells expressing PD-L1. Methods in which such antibody combinations are especially useful include cancer and tumor treatments and therapies in which the cancer or tumor is a PD-L1 positive cancer or tumor.

Abstract: Pharmaceutical compositions for the topical administration of a drug to the pilosebaceous unit and methods for administering the same. As disclosed herein, the inventors of the present invention have made the surprising discovery that pharmaceutical compositions comprising small particles of an active pharmaceutical ingredient can be administered to the pilosebaceous unit. The pharmaceutical composition can comprise SHR0302 or spironolactone as an active pharmaceutical ingredient.

Abstract: A formulation includes a nanostructured lipid carrier (NLC) matrix and spironolactone as an active ingredient loaded within the NLC matrix, forming a spironolactone-loaded NLC (SP-NLC) gel or lotion.

Abstract: Disclosed herein is a stable, ready-to-use liquid formulation comprising spironolactone and its method of use.

Abstract: The present invention relates to pharmaceutical compositions and kits comprising pharmaceutical compositions, and methods for administering pharmaceutical compositions comprising active contraceptive drugs in a patient. Specifically, the pharmaceutical compositions may comprise progestogen-only contraceptive (“POC”), such as Drosphirenone.

Abstract: Chemical entities that are bufalin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.

Abstract: Compounds and pharmaceutical compositions are contemplated that inhibit N-acyl-ethanolamine-hydrolyzing acid amidase (NAAA) to so increase the concentration of the substrate of NAAA, palmitoylethanolamide (PEA). NAAA inhibition is contemplated to be effective to alleviate conditions associated with a reduced concentration of PEA. Among other uses, various NAAA inhibitors are especially contemplated as therapeutic agents in the treatment of inflammatory diseases.

Abstract: Chemical entities that are bufalin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.

Abstract: The present invention relates to method and pharmaceutical compositions for preventing glucocorticoid-induced corneal or skin thinning. In particular, the present invention relates to a mineralocorticoid receptor antagonist for topical use in a method for preventing or reducing glucocorticoid-induced corneal or skin thinning in a subject in need thereof. The invention also relates to a topical pharmaceutical composition comprising an amount of at least one glucocorticoid and an amount of at least one mineralocorticoid receptor antagonist or inhibitor of MR expression for use in a method for treating an inflammatory skin disease or an inflammatory disease of the cornea or of the anterior segment of the eye in a subject in need thereof.

Abstract: The present invention relates to method and pharmaceutical compositions for preventing glucocorticoid-induced corneal or skin thinning. In particular, the present invention relates to a mineralocorticoid receptor antagonist for topical use in a method for preventing or reducing glucocorticoid-induced corneal or skin thinning in a subject in need thereof. The invention also relates to a topical pharmaceutical composition comprising an amount of at least one glucocorticoid and an amount of at least one mineralocorticoid receptor antagonist or inhibitor of MR expression for use in a method for treating an inflammatory skin disease or an inflammatory disease of the cornea or of the anterior segment of the eye in a subject in need thereof.

Abstract: The present invention relates to a very low-dosed dosage form for hormone replacement therapy (HRT). More particularly, the present invention concerns a solid oral dosage form comprising about 0.5 mg estradiol and about 0.25 mg drospirenone, and at least one pharmaceutically acceptable excipient. Despite the very low E2 and DRSP doses it has surprisingly been found that a high proportion of the women suffering from moderate to severe hot flushes actually respond to this treatment. Accordingly, the dosage form of the invention may be used as maintenance HRT or may be used already when HRT is initiated.

Abstract: The present invention relates to a method and compositions for the treatment of cystic fibrosis.

Abstract: Compounds and pharmaceutical compositions are contemplated that inhibit N-acyl-ethanolamine-hydrolyzing acid amidase (NAAA) to so increase the concentration of the substrate of NAAA, palmitoylethanolamide (PEA). NAAA inhibition is contemplated to be effective to alleviate conditions associated with a reduced concentration of PEA. Among other uses, various NAAA inhibitors are especially contemplated as therapeutic agents in the treatment of inflammatory diseases.

Abstract: The present invention relates generally to methods of inhibiting the onset and progression of Alzheimer's disease (AD), mild cognitive impairment (MCI), and related neurodegenerative disorders involving amyloidosis. The methods involve administering a composition comprising a therapeutically effective amount of D-pinitol to individuals who are at risk of developing the disease or have one or more symptoms of the disease. The invention also relates to methods of treating or preventing Alzheimer's disease or MCI that involve the use of such compositions. The invention further provides methods to promote the general health of the nervous system through administration of active ingredient compositions. The invention further relates to animal and cellular systems for the study of AD, MCI, and related disorders, and the identification of reagents useful in treating amyloidosis. The invention further provides methods to inhibit AD or MCI in an individual based on reducing caloric intake by the individual.

Abstract: Chemical entities that are bufalin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.

Abstract: A method for treating cancer by using an agent which is capable of inhibiting the functionality of the MCM complex, a heterohexameric ring formed from six subunits, in the process of DNA replication and a method of screening for such agents by detecting the locations and functions of the MCM subunits, such as hMcm2 and hMcm6, in cells treated with candidate compounds.

Abstract: Chemical entities that are bufalin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.

Abstract: A compound of general formula (I), wherein R1-R17 and the - - - - - - line take various meanings for use in the treatment of cancer.

Abstract: Methods of inhibiting the onset and progression of Alzheimer's disease (AD), mild cognitive impairment (MCI), and related neurodegenerative disorders involving amyloidosis are provided. The methods involve administering a composition comprising a therapeutically effective amount of D-pinitol to individuals who are at risk of developing the disease or have one or more symptoms of the disease. Also provided are methods of treating or preventing Alzheimer's disease or MCI that involve the use of such compositions. Also provided are methods of using D-pinitol to promote a healthy nervous system and as a food supplement.

Abstract: This process relates to a pharmaceutical composition of an Na—K-ATPase ligand which will stimulate Na/K-ATPase signaling in a pharmaceutically acceptable vehicle. In one embodiment, the composition may be used to treat a skin disorder. In another embodiment, the composition may be used to inhibit cardiac fibrosis.

Abstract: The invention provides epoxytaccalonolide microtubule stabilizers and their use as anti-proliferative microtubule stabilizing agents.

Abstract: There is provided a novel compound having neurite-outgrowing activity that is useful for the prevention or the treatment of a neurodegenerative disease. A compound of Formula (I) [where X is OR or NR1R2, Y is OH, NR3R4, —NHC(?NH)NHR5, or —NHC(?NH)R5, and Z is a hydrogen atom, a linear or branched C1-5 alkyl group, or a 5- or 6-membered ring aryl group optionally having 1 or 2 nitrogen atom(s), sulfur atom(s), or oxygen atom(s)], or a pharmaceutically or veterinary-medically acceptable salt of the compound.

Abstract: The present invention describes novel single drug entities, formed by direct linkage of an antibiotic to a steroidal drug. Upon topical application to the eye, the conjugate would undergo enzymatic and/or hydrolytic cleavage to release the individual drugs. The antibiotic is coupled directly to the steroid drug.

Abstract: The present invention describes steroid antibiotic conjugates. These single drug entities are formed connecting a steroid moiety and two same antibiotics moieties, or a steroid moiety and two different antibiotics moieties. Upon topical application to the eye, the conjugate hybrid would undergo enzymatic and/or hydrolytic cleavage to release the individual drugs.

Abstract: The present disclosure is generally directed to neuroactive 13,17-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: Known or suspected traumatic brain injuries may be treated therapeutically by administering a therapeutically effective dose of resibufogenin. A preferred method for determining if a patient has a traumatic brain injury includes obtaining a body specimen from the patient, determining the concentration of marinobufagenin in the body specimen, comparing the concentration of marinobufagenin to the concentration in such body specimens in normal patients, and if the marinobufagenin concentration is substantially above the concentration of a normal patient, concluding traumatic brain injury exists. In a preferred embodiment, a substantial elevation is deemed to be an increase of about 30 percent above the marinobufagenin concentration of a normal patient. The body specimen may be blood, urine, or cerebrospinal fluid.

Abstract: The invention provides 11?-hydroxyandrosta-4-ene-3-one compounds of Formula I, or physiologically acceptable salts or solvates thereof: wherein R4 represents a moiety selected from a group consisting of (A), (B) and (C), with a proviso that when R4 represents moiety (C), Z is S:

Abstract: The present invention relates to a method for manufacturing uniform size polymeric nanoparticles containing poorly soluble drugs, and more particularly, to a method for manufacturing uniform size polymeric nanoparticles containing poorly soluble drugs, including a first step of dissolving a biodegradable polymer in a non-volatile polar organic solvent, a second step of adding poorly soluble drugs to water and the biodegradable polymer solution to produce a dispersion, and a third step of adding the dispersion to emulsifier solutions in a batch under the condition of low mechanical energy level stirring.

Abstract: Several ursolic acid derivatives and pharmaceutical compositions thereof are provided. The ursolic acid derivatives and the pharmaceutical compositions thereof have at least one of an anticancer and an anti-inflammatory effects. A method for increasing a reactive oxygen species in a cell is also provided. The method comprises a step of providing the cell with a pharmaceutical composition including an ursolic acid derivative.

Abstract: Methods and compositions for detecting, treating, characterizing, and diagnosing interstitial lung and/or fibrotic diseases are described.

Abstract: The invention provides for a method of inhibiting interferon-beta gene expression and/or reducing the level of interferon-beta in a cell by contacting the cell with a Na+, Ca2+, or K+ ion-channel modulator. The invention also provides for a method of treating a disease or disorder characterized by elevated interferon beta levels or elevated levels of interferon-beta gene expression. Additionally, the invention provides a method for treating pathogenic or non-pathogenic infections.

Abstract: Disclosed is a cucurbitane-triterpenoid compound for activating estrogen receptor activity, and a pharmaceutical composition, use and preparation method thereof. The cucurbitane-triterpenoid compound is presented as formula (I): wherein a single bond or a double bond is formed between C5 and C10, and a single bond or a double bond is fromed between C8 and C9; when a single bond is formed between C5 and C10, the R1 is oxygen; while a single bond is formed between C8 and C9, R2 is carbonyl group (—C?O), methyl hydroxyl group (—CH(OH)), methyl ketone or methyl dimethoxy group (—CH(OCH3)2); and wherein while R1 is oxygen (—O—) and R2 is carbonyl group (—C?O) or methyl hydroxyl group (—CH(OH)), a single bond is formed between R1 (—O—) and C19 of R2 such that R1 and R2 are formed tetrahydro-2H-pyran-2-one or hemiacetal ring.

Abstract: Compounds and compositions, and methods of use thereof, for treatment and/or prevention of multiple sclerosis, including symptoms associated with multiple sclerosis, and/or treatment and/or prevention of other disease/disorder affecting the nervous system (e.g. central, peripheral) or muscle including symptoms thereof, comprising administering to a subject in need thereof daptomycin and/or daptomycin-related lipopeptide.

Abstract: The invention provides methods for promoting weight loss by an animal, promoting weight loss by an animal while preventing or minimizing loss of lean body mass by the animal preventing a reduction in energy metabolism by an animal reducing the risk of regaining weight by an animal after weight loss, and ameliorating undesirable animal behaviors associated with reduced caloric intake by intermittently feeding an animal a first diet containing calories that meet the animal's maintenance energy requirements and a second diet containing calories that do not meet the animal's maintenance energy requirements. In preferred embodiments, the described feeding pattern and diets are ted in conjunction with one or more weight loss agents.

Abstract: A series cardenolide derivatives including structure of formula I from the root of Reevesia formosana have provided. In formula (1) and (2), where R3, R5, R10 and R16 are as defined in the specification. The derivatives compounds showed potent cytotoxicity against MCF-7, NCI-H460, and HepG2 cancer cell lines.

Abstract: The invention provides methods for treating inflammatory and autoimmune diseases by administering to the subject an effective amount of a cardiac glycoside, where the dose is effective to suppress or prevent initiation, progression, or relapses of the disease, including the progression of established disease. In some embodiments, the methods of the invention comprise administering to a subject determined to have rheumatoid arthritis or systemic lupus, or a pre-clinical disease state thereof, an effective amount of a cardiac glycoside, to suppress or prevent activity of the disease. In other embodiments, the methods of the invention comprise administering to a subject determined to have insufficient endogenous cardiac glycosides, an effective amount as a supplement to counteract the effects of cardiac glycoside deficiency.

Abstract: Chemical entities that are novel compounds, pharmaceutical compositions and methods of treatment of cancer are described.

Abstract: The present invention relates to a biomarker for characterizing prostate cancer and method of using the same. More particularly, the invention relates to method of using a membrane-associated C family G protein-coupled receptor GPRC6A as biomarker of characterizing prostate cancer progression. The present invention also provides a kit for detecting prostate cancer in a subject.

Abstract: A method of inhibiting the secretion of IL-8 and other pro-inflammatory cytokines from cells secreting elevated levels of these compounds is provided. The method includes contacting the cell with a composition comprising a cardiac glycoside such as oleandrin. The cardiac glycoside can be used to treat cystic fibrosis and other IL-8 dependent disorders by lowering levels of spontaneously secreted IL-8 and other pro-inflammatory cytokines. Oleandrin was found to suppress the secretion of IL-8 from cultured CF lung epithelial cells in the nanomolar concentration range. Structure-activity relationships (SARs) for cardiac glycosides are also elucidated.

Abstract: [Problem] To provide a prophylactic/therapeutic agent against, for example, nerve diseases and the like such as ischemic brain disease and neurodegenerative disease, or a prophylactic/therapeutic agent against diseases against which antioxidant action is effective, as a cell protecting agent, in particular as an inhibitor of brain cell damage or brain cell death.

Abstract: Glucono-delta-lactone (GDL) can be used to mediate the human blood coagulation process. In particular, GDL can be used in an assay to determine an individual's risk potential for accelerated blood clotting or as a treatment for conditions related to accelerated clotting potential and/or inflammatory states.

Abstract: The invention relates to processes for obtaining steroids with a spirolactone group in position 17, particularly to industrially obtaining 6?,7?; 15?,16?-dimethylene-3-oxo-17?-pregn-4-ene-21,17-carbolactone, commonly known as Drospirenone, as well as to intermediates useful in said process.

Abstract: The present invention provides a Withania somnifera fraction rich in withanolides and a vaccine comprising a “Withania somnifera fraction” as an adjuvant.

Abstract: The present invention relates to an improved transdermal hydroalcoholic testosterone gen formulation that provides, among other things, a desirable pharmacokinetic hormone profile, and methods of use.

Abstract: A hair treatment composition comprising at least one lactone in combination with at least one disaccharide.

Abstract: The present invention relates to methods and compositions for stimulating reepithelialisation during wound healing. More particularly, the present invention relates to a mmeralocorticoid receptor antagonist or an inhibitor of mineralocorticoid receptor gene expression for use in a method for stimulating reepithelialisation of the skin or of the cornea during wound healing.

Abstract: Chemical entities that are bufalin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.

Abstract: A method of inhibiting cell migration or treating an inflammatory condition, comprising administering a compound disclosed herein to the subject, is provided. The compound can be administered systemically, locally, or a combination thereof. For example, the compound can be locally delivered from a temporary device or an implant, such as a vascular prosthesis.

Abstract: The present invention relates to a method of treating plant(s) against larval pests by the use of terreulactone. It also relates to a process for producing meroterpenoid from fungus Aspergillus terreus strain MTCC5390.