Abstract: The invention provides compounds, methods, pharmaceutical compositions, and kits for the treatment of proliferative disorders such as cancer. In one aspect, the methods comprise compounds that inhibit the activity of protein kinases, such as cell division cycle (Cdc) kinase. In another aspect, the methods comprise compounds that inhibit Cdc7 and/or Dbf4 activity. In another aspect, the methods comprise compounds that exhibit anti-proliferative properties useful in treating diseases such as cancer. Compounds useful for any of the methods include compounds of the Formula (A) or (B): or pharmaceutically acceptable salts thereof. Exemplary compounds of Formula (A) or (B) include granaticin A, granaticin B, dihydrogranaticin A, dihydrogranaticin B, medermycin, and actinorhodin.

Abstract: A preparation method of drug-loaded micelles of an absorbable vascular stent coating for angiostenosis in an infant is provided, including the following steps: S1: dissolving a drug to be encapsulated in an appropriate amount of an emulsifying agent, adding a chitosan-poly(p-dioxohone) amphiphilic block copolymer (chitosan-b-PPDO copolymer), and thoroughly mixing to obtain a drug-copolymer solution; S2: adding the drug-copolymer solution obtained in S1 dropwise to an emulsifying agent aqueous solution prepared in advance, and continuously stirring to obtain a stable drug-loaded micellar solution; and S3: removing the emulsifying agent from the micellar solution obtained in S2 through vacuum evaporation, stirring a resulting concentrate, and centrifuging the concentrate to obtain a supernatant; and filtering the supernatant to obtain a filtrate, and subjecting the filtrate to dialysis to obtain the drug-loaded micelles.

Abstract: A 12-bromo-2,16-dioxapentacyclo[7.7.5.01,21.03,8.010,15]henicosa3(8),10,12,14-tetraene-7,20-dione compound, its synthesis, and its use as an antimicrobial agent.

Abstract: Disclosed are bruceolides for the treatment of cancer, and other diseases, selectively targeting unwanted cells. The disclosed bruceolides may include a site specific cleavable moiety inhibiting the chemotoxic activity until cleaved, i.e., removed, within and/or near a cancer to be treated. As to facilitate selective delivery to cancer tumors, the disclosed bruceolides may be loaded into, attached to or otherwise carried by nanoparticles.

Abstract: The subject invention pertains to compositions and methods for treating neurodegenerative diseases, including Alzheimer's disease (AD), Parkinson's disease (PD), amyotrophic lateral sclerosis (ALS), Huntington's disease (HD), multiple sclerosis, epilepsy, stroke, alcohol withdrawal, progressive supranuclear palsy (PSP), Pick's disease (PiD), corticobasal degeneration (CBD), frontotemporal dementia or parkinsonism linked to chromosome 17 (FTDP-17). The methods of the subject invention further relate to methods of fermentation of bacterial cells and methods of tautomerization of the subject compounds.

Abstract: The invention relates to compounds for treating and/or preventing obesity and obesity-related disorders. Particularly, the invention provides chromanone derivatives used as ATF3 inducer and for treating and/or preventing obesity and obesity-related disorders such as heart disease, hypertension, hyperlipidemia and diabetes.

Abstract: Provided herein are timosaponin compounds of Formula I, II, III, I?, II? and III?, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are uses of said timosaponin compounds for preparing medicament for the treatment of diseases associated with beta-amyloid in hosts or subjects in need thereof.

Abstract: The present invention relates to a combination of ivermectin and brimonidine for use in the treatment and/or the prevention of moderate to severe rosacea, preferably by topical administration of a 1% ivermectin cream and 0.33% brimonidine gel.

Abstract: Provided is a method for producing a concentrated oil-based polyphenol composition for human consumption. The unique combination of polyphenols in a biologic oil-based formulation may be administered for optimal effects on human platelets, lipids, and inflammatory markers. These physiologic changes have beneficial effects for human health and longevity.

Abstract: Compounds of formula I are disclosed. The compounds are useful for promoting skeletal muscle hypertrophy or treating skeletal muscle atrophy.

Abstract: Formulations comprising compounds obtainable from a neem extract and/or biomass and at least one water-soluble organosilicone surfactant, and methods of making and using such formulations are provided.

Abstract: Embodiments of the invention involve treating skin afflictions by the topical or oral use of acetylcholinesterase inhibitor. By effectively reducing or eliminating the population of Demodex mites in affected skin areas and areas where Demodex mites may exist, this treatment achieves a more complete remission of clinical signs and symptoms of the skin afflictions than any previously described method. Embodiments of the invention are useful for treating skin afflictions including common acne, seborrheic dermatitis, perioral dermatitis, an acneform rash, transient acantholytic dermatosis, acne necrotica milliaris, psoriasis, steroid induced dermatitis, primary irritation dermatitis and rosacea.

Abstract: The invention refers to novel dermatic and cosmetic compositions to protect against impaired pigmentation of the skin. Locally caring Ginkgoloides are selected out of pure, high quality products comprising phospholipids and lecithins to antagonize alkyl-acyl GPC. The Ginkgoloides are bound to one or more transport proteins, carrier proteins, peptides, amino acids and these carriers contain at least one acetyl group and/or Acetyl CoA. The entire transdermal compositions then endocrinologically equilibrate the skin and the skin cells whereby acetylating compounds locally act as sun screening agent.

Abstract: The present disclosure is directed, at least in part, to disease-modifying treatments for neurodegenerative disorders. In one embodiment, a method of delaying worsening of one or more symptoms and/or progression of a neurodegenerative disorder is provided. In one embodiment, a method of treating or ameliorating one or more symptoms of a neurodegenerative disorder is provided. In one embodiment, the methods of the present invention comprise administering to a subject in need thereof, a compound having the structure of Formula (1a); Formula (1a); and/or a pharmaceutically acceptable salt thereof. In one embodiment, the the compound of (1a) and/or a pharmaceutically acceptable salt thereof is administered in combination with one or more pharmacologically active agents.

Abstract: The invention relates to products comprising an antibiotic agent and a second agent being a dispersant or an anti-adhesive agent, in particular a mucolytic dispersant or a mucolytic anti-adhesive agent, which are useful in relation to the prevention and treatment of bacterial infections.

Abstract: The present disclosure is directed, at least in part, to disease-modifying treatments for neurodegenerative disorders. In one embodiment, a method of delaying worsening of one or more symptoms and/or progression of a neurodegenerative disorder is provided. In one embodiment, a method of treating or ameliorating one or more symptoms of a neurodegenerative disorder is provided. In one embodiment, the methods of the present invention comprise administering to a subject in need thereof, a compound having the structure of Formula (1a); Formula (1a); and/or a pharmaceutically acceptable salt thereof. In one embodiment, the the compound of (1a) and/or a pharmaceutically acceptable salt thereof is administered in combination with one or more pharmacologically active agents.

Abstract: Use of pycnidione, epolone A, and epolone B as anti-dandruff actives either alone or in combination in anti-dandruff compositions, particularly shampoos and conditioners. The actives are particularly effective against Malassezia yeasts and Malassezia furfur. A method of obtaining pycnidione, epolone A, and epolone B from culturing of Neosetophoma samarorum is also described.

Abstract: The invention relates to a method for on-demand contraception, which method comprises administering a progestogen agent or progesterone receptor modulator, such as 17a-acetoxy-11b-[4-N, N-dimethylamino-phenyl)-19-norpregna-4, 9-diene-3, 20-dione (ulipristal acetate) in a woman, within 72 hours before an intercourse or within 120 hours after the intercourse.

Abstract: Embodiments of the invention involve treating skin afflictions by the topical or oral use of organophosphates. By effectively reducing or eliminating the population of Demodex mites in affected skin areas and areas where Demodex mites may exist, this treatment achieves a more complete remission of clinical signs and symptoms of the skin afflictions than any previously described method. Embodiments of the invention are useful for treating skin afflictions including common acne, seborrheic dermatitis, perioral dermatitis, an acneform rash, transient acantholytic dermatosis, acne necrotica milliaris, psoriasis, steroid induced dermatitis, primary irritation dermatitis, rosacea and for diagnositic methods thereof.

Abstract: The present invention relates to a composition for inhibiting the formation of a SNARE complex, containing myricetin derivatives, and having novel structures and obtained by the acylation of myricetin, laricitrin, combretol, or syringetin. The myricetin derivatives are considered to exhibit an effect of being bioconverted into myricetin in a cell. The myricetin derivatives lost the dark color of conventional myricetin and properties thereof were changed such that the myricetin derivatives have properties of photostability and fat solubility. Therefore, since stable form myricetin derivatives are absorbed into a cell such that an activity, possessed by normal myricetin, of inhibiting the formation of a SNARE complex are exhibited, the present invention can exhibit an excellent function as a SNARE targeting prodrug, and as a composition for inhibiting the formation of a SNARE complex, containing the same.

Abstract: Compositions including a compound of the family of avermectins, preferably ivermectin, and an agonist compound for at least one of the retinoic acid receptors are described. The compositions are in particular used in the treatment of acne.

Abstract: Embodiments of the invention involve treating skin afflictions by the topical or oral use of acetylcholinesterase inhibitor. By effectively reducing or eliminating the population of Demodex mites in affected skin areas and areas where Demodex mites may exist, this treatment achieves a more complete remission of clinical signs and symptoms of the skin afflictions than any previously described method. Embodiments of the invention are useful for treating skin afflictions including common acne, seborrheic dermatitis, perioral dermatitis, an acneform rash, transient acantholytic dermatosis, acne necrotica milliaris, psoriasis, steroid induced dermatitis, primary irritation dermatitis and rosacea.

Abstract: The present description provides oligourea catalysts, a polar helical oligomeric strands, and methods for catalyzing reactions with polar helical oligomeric strands and oligourea catalysts. In particular, the invention relates to a polar helical oligomeric strand of at least 4 residues selected from the formula (I) and which can be used as a catalyst.

Abstract: A quinonemethide triterpenoid is administered to subjects with multidrug-resistant cancer, in particular a cancer with enhanced expression and/or functional activity of ABC transporter proteins such as P-glycoprotein and/or an apoptosis-deficient, in particular p53-, Bax- or Bak-deficient, cancer, i.e. specific subgroups of subjects with cancer. The quinonemethide triterpenoid is suitable to treat cancer allowing for an accumulation of cytotoxic or therapeutic compounds in the cells while having exceptionally increased cytotoxic activity towards the multidrug-resistant cancer cells and while allowing for an increased activity of chemotherapeutic compounds. Methods for specifically targeting cancer cells with multidrug-resistance and methods for potentiating the activity of a chemotherapeutic compound in those cancer cells are also disclosed. A kit including a quinonemethide triterpenoid and a chemotherapeutic compound is also provided.

Abstract: The present invention discloses the novel coumarin derivative of formula (1): its synthesis, pharmaceutical composition, preparation and use thereof. The pharmaceutical composition including: (1) the novel coumarin derivative of formula (1) as active pharmaceutical ingredient; and (2) one or more pharmaceutical excipients, required to yield final dosage forms suitable for therapeutic administration. The composition is safe and efficient therapeutic agent for viral diseases including the acquired immunodeficiency syndrome (AIDS).

Abstract: The invention relates to a method for on-demand contraception, which method comprises administering a progestogen agent or progesterone receptor modulator, such as 17a-acetoxy-11b-[4-N,N-dimethylamino-phenyl)-19-norpregna-4,9-diene-3,20-dione (ulipristal acetate) in a woman, within 72 hours before an intercourse or within 120 hours after the intercourse.

Abstract: ?9-THC acid is extracted from cannabis flowers using a first organic solvent, then separated using a second aqueous solvent. ?9-THC acid is converted to ?9-THC carboxylic salt before being extracted by a third organic solvent and converted back to ?9-THC carboxylic acid. Using a solvent swap, ?9-THC carboxylic acid is decarboxylated and extracted again with an organic solvent prior to purification to give ?9-THC.

Abstract: A method of treating acne in a human in need thereof comprising administering systemically to said human a tetracycline compound in an amount that is effective to treat acne but has substantially no antibiotic activity, without administering a bisphosphonate compound.

Abstract: The present invention aims to provide a pharmaceutical agent for the prophylaxis and/or treatment of Alzheimer's disease, which has a novel action mechanism and shows less side effects. A polyphenol derivative having liposolubility enhanced by the introduction of at least one kind of a liposoluble group selected from the group consisting of a chain saturated hydrocarbon group, a chain unsaturated hydrocarbon group, a cyclic saturated hydrocarbon group, a cyclic unsaturated hydrocarbon group, an aromatic hydrocarbon group, a liposoluble vitamin residue and a sterol residue has an action to potentiate neprilysin activity, and is useful as a pharmaceutical agent for the prophylaxis and/or treatment of Alzheimer's disease.

Abstract: The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: Certain embodiments are directed to oridonin analogs or derivatives. In certain aspects, the derivatives are used as anticancer or anti-inflammatory agents.

Abstract: The invention relates to compositions, such as pharmaceuticals, foods, food additives, or dietary supplements, containing A-type procyanidins, and methods of use thereof, for prophylactic or therapeutic treatment of a human or a veterinary animal to treat or prevent NO-responsive health conditions, treat hypertension, cardiovascular disease, coronary artery disease and/or vascular circulation disorders, prevent or reduce the risk of heart attack, stroke, congestive heart failure and/or kidney failure, or to improve blood flow, for example renal blood flow. The composition may optionally contain an additional NO modulating agent and/or a cardiovascular-protective or therapeutic agent, or may be administered in combination with such an agent.

Abstract: Crystalline solid forms of methyl {(2S)-1-[(2S,5S)-2-(9-{2-[(2S,4S)-1-{(2R)-2-[(methoxycarbonyl)amino]-2-phenylacetyl}-4-(methoxymethyl)pyrrolidin-2-yl]-1H-imidazol-5-yl}-1,11-dihydroisochromeno[4?,3?:6,7]naphtho[1,2-d]imidazol-2-yl)-5-methylpyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl}carbamate (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using these crystalline forms.

Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein X and R are as defined herein. The compounds of formula (I) are useful as gyrase and/or topoisomerase IV inhibitors for treating bacterial infections. The compounds of formula (I) either possess a broad range of anti-bacterial activity and advantageous toxicological properties or are prodrugs of compounds having said activity.

Abstract: The invention relates to agents and to pharmaceutical compositions for reducing the formation of amyloid and/or for promoting the disaggregation of amyloid proteins. The compositions may also be used to detect amyloid.

Abstract: The invention relates to compositions and methods (with regard to animals and humans) for utilizing an extract and/or one or more natural spiro triterpenoids and derivatives thereof alone or as a supplement. Certain materials utilized are from the blazeispirol family, obtainable from Agaricus species. Treatments include the prophylactic and/or therapeutic treatment of a disease, disorder or condition that responds to the modulation of Liver X receptor, as well as corresponding methods of treatment, the manufacture of a pharmaceutical and nutraceutical formulation for said treatment. The invention also relates to the use of the extract and compound(s) in the treatment or in the preparation of a medicament (e.g. a nutraceutical) for the prophylactic and/or therapeutic treatments, as well as their preparation. It also relates to pharmaceutical or nutraceutical formulations described herein which are useful in prophylactic and therapeutic treatments. They can also be used for non-therapeutic, e.g.

Abstract: The present invention relates to a cosmetic composition comprising compounds or salts of formula (I) or formula (II), wherein R1 and R2 are both independently hydrogen (H), or a saturated, straight or branched C1-C8 alkyl group. More particularly, the present invention also relates to the use of said cosmetic composition for the prevention of the graying of hair and/or for restoration and/or maintenance of the natural hair color.

Abstract: Methods and compositions are provided for alleviating and/or preventing one or more side effects associated with exposure to radiation in a subject exposed to radiation or at risk for exposure to radiation comprising oral administration to the subject of an amount of an edible source of melanin effective to alleviate a side effect associated with radiation.

Abstract: The invention relates to the use of 4,6,4?-trimethylangelicin (TMA) and structural analogs thereof to prepare a medicament for the treatment of cystic fibrosis with the primary objective of correcting the defective CFTR in a sub-group of cystic fibrosis patients consisting of patients carrying the F508del-CFTR mutation.

Abstract: The invention relates to a method for on-demand contraception, which method comprises administering a progestogen agent or progesterone receptor modulator, such as 17a-acetoxy-11b-(4-N,N-dimethylamino-phenyl)-19-norpregna-4,9-diene-3,20-dione (ulipristal acetate) in a woman, within 72 hours before an intercourse or within 120 hours after the intercourse.

Abstract: A therapy system includes a diagnostic image scanner (12) that acquires a diagnostic image of a target region to be treated. A planning processor (70) is configured to generate a patient specific adaptive radiation therapy plan based on patient specific biomarkers before and during therapy. A first set of patient specific biomarkers is determined then used for the determination of a first normal tissue complication probability (NTCP) model and a first tumor control probability (TCP) model. A radiation therapy device (40) administers a first dose of radiation to the target region with a protocol based on the first NTCP model and the first TCP model. A second set of patient specific biomarkers is determined. A relationship between the first set and second set of patient specific biomarkers is used to determine a second NTCP model and a second TCP model.

Abstract: Compounds and their pharmaceutically acceptable salts for treatment of synucleinopathies, such as Parkinson's disease and tauopathies.

Abstract: The present invention refers to the use of sodium channel blockers such as tetrodotoxin or saxitoxin, its analogues/derivatives as well as their acceptable salts, for the production of a medicament for the treatment of neuropathic pain resulting from chemotherapy.

Abstract: Provided are an attractant for bone marrow stem cells containing at least one of cinnamtannin B1 and pentagalloylglucose, and a method for attracting bone marrow stem cells in which bone marrow stem cells are attracted by the attractant.

Abstract: Use of sparstolonin B in inhibition of growth and/or viability of human neuroblastoma cells is described. The sparstolonin B can be naturally derived from the Chinese herb Sparganium stoloniferum or can be synthetic. The sparstolonin B is shown to be effective both in vitro and in vivo in inhibition of growth and/or viability of neuroblastoma cells of multiple different genetic backgrounds including N-myc amplified with wild p53 neuroblastoma cells, N-myc amplified with mutated p53 neuroblastoma cells, and N-myc nonamplified neuroblastoma cells.

Abstract: New pharmaceutical compositions extracted from Ferula assa-foetida are confirmed to effectively treat influenza A (H1N1) virus. The extraction method of the new pharmaceutical compositions mainly includes steps of: (a) extracting F. assa-foetida with methanol to obtain a crude extract; (b) fractioning the crude extract with n-hexane-methanol to obtain a methanol extract; (c) fractioning the methanol extract with chloroform-water to obtain a chloroform extract; and (d) chromatographing the chloroform extract to obtain the pharmaceutical compositions, which can be further fractioned and chromatographed to obtain various sesquiterpene coumarins.

Abstract: The invention relates to Simalikalactone E (SkE) to be used for preventing and/or treating cancers.

Abstract: In one embodiment, the present application discloses synthetic LDL nanoparticles comprising mixtures of components selected from the group consisting of phospholipids, triglycerides, cholesterol ester and free cholesterol; optionally further comprising an agent selected from the group consisting of natural antioxidants, ubiquinol and vitamin E, and methods for preparing the synthetic nanoparticles. The disclosed synthetic LDL nanoparticles are capable of selectively delivering lipophilic drugs and prodrugs to cellular targets expressing LDL receptors after intra venous injection.

Abstract: A composition comprising a high purity cannabinoid, an acid, and a pharmaceutically-acceptable solvent achieves room temperature stability for over 24 months. The acid improves the stability of the composition and the solvent enhances the solubility of the acid, thereby allowing the acid to have an improved stabilizing effect on the highly pure cannabinoid. Preferably, the solvent is an alcohol and, more preferably, the composition contains an oil. A method for making the composition includes combining the cannabinoid and the solvent and evaporating a portion of the solvent, along with adding an acid to the composition, before, during, or after the evaporating step. A method for making and storing the composition includes storing the composition in a manner adapted to maintain its stability. Pharmaceutical dosage forms include a formulated composition, such as having the oil. A method of treating a subject comprises administering to the subject the dosage form.

Abstract: A highly bioavailable, water soluble, sustained release nanoformulation comprising a hydrophobic plant derived compound(s) in an emulsifier phase, and aqueous phase. The formulation provides sustained release of the hydrophobic plant derived compound(s) over a 24 hr time period. A process for preparation of the water soluble nanoformulation is described.