Abstract: The invention relates to cyclopentathiophene carboxamides of formula (I.0) wherein R1, R2, R3, R4, and n are as defined herein, and pharmaceutically acceptable salts thereof. The invention also relates to the use of the cyclopentathiophene carboxamides of formula (I.0) for the treatment of diseases which can be influenced by antagonizing the activity mediated by the platelet activating factor receptor.

Abstract: A method of preparing a Senna obtusifolia seed extract rich in anthraquinones and a galactomannan extract includes the following steps: (1) crushing Senna obtusifolia seeds into a Senna obtusifolia seed powder; (2) extracting the Senna obtusifolia seed powder with 40-85% ethanol, filtering to obtain an extract solution and a residue; (3) concentrating the extract solution under vacuum to obtain a concentrated extract solution, spray-drying the concentrated extract solution to obtain the Senna obtusifolia seed extract; (4) extracting the residue with membrane filtered water, conducting a centrifugation to obtain a supernatant; (5) adding ammonium sulfate and ethanol to the supernatant to form a two-phase aqueous system, collecting a bottom layer of the two-phase aqueous system; and (6) conducting an ultrafiltration of the bottom layer with a cut-off molecular weight of 50 k-200 k to obtain a galactomannan extract solution, drying the galactomannan extract solution under vacuum to obtain the galactomannan extra

Abstract: A number of triterpene saponin variants with different modifications on their central glycosyl ester linkage are described. Also described are methods of making and method of using such triterpene saponin variants.

Abstract: The present invention relates to novel aqueous N-acyl glycinate compositions wherein the said compositions are free-flowing, pumpable, phase-stable on long-term storage, and processable at sub-zero temperatures; more specifically below ?5° C. The present invention also relates to the use of these aqueous N-acyl glycinate compositions in preparing isotropic aqueous skin and hair cleansing formulations such as body wash, shower gels, shampoos, and other.

Abstract: Compounds described herein are mithramycin (MTM) oxide (OX) derivatives and MTM Hydrazine (HY) derivatives. These compounds are useful for treatment of cancers and neuro-diseases.

Abstract: The present invention relates to methods of treating subjects having heart failure with preserved ejection fraction (HFpEF) with a sustained-delivery formulation of cardiotonic 5-(pyridinyl)-2(1H)-pyridinone compounds.

Abstract: A use of noreugenin glycoside derivatives of formulas I, II and III as a self-tanning substance or to increase the synthesis of melanin, improve melanin transport and/or improve the distribution of melanin in suprabasal layers, preparations containing noreugenin glycoside derivatives of formulas I, II and III, and noreugenin glycoside derivatives of formulas I, II and III.

Abstract: The invention relates to stable vancomycin hydrochloride powder for oral liquid formulations. Also provided herein are methods of using vancomycin oral liquid formulations for the treatment of certain diseases such as Clostridium difficile pseudomembranous colitis and Staphylococcal enterocolitis as well as kits and related products thereof.

Abstract: 2-pyrrolino-13-deoxyanthracycline derivatives, medical uses thereof, and a process for making them. A 2-pyrrolino-13-deoxyanthracycline and a 13-deoxyanthracycline can be administered to a patient simultaneously or sequentially in amounts to produce a synergistic therapeutic effect with increased potency and efficacy, compared to the sum of the effects of each drug when administered alone. A composition or preparation of a 2-pyrrolino-13-deoxyanthracycline and a 13-deoxyanthracycline for producing a potent anticancer therapeutic effect is also provided.

Abstract: The invention disclosed herein relates to the use of an extract of Dodonaea viscosa in breast cancer therapy, either alone or in combination with other breast cancer therapies.

Abstract: A composition that is useful in a skin function improving agent includes at least a sapogenol, and a collagen hydrolysate. This composition can be used in a skin function improving agent and is particularly useful in a skin function improving agent for inhibiting transdermal moisture loss and/or for retaining the moisture in the stratum corneum.

Abstract: This invention provides compositions, methods and process of producing extracts from Xanthoceras sorbifolia. The extract comprises alkaloids, coumarins, saccharides, proteins, polysaccharides, glycosides, saponins, tannins, acid, flavonoids and others. The composition can be used for treating cancer, arthritis, rheumatism, poor circulation, arteriosclerosis, Raynaud's syndrome, angina pectoris, cardiac disorder, coronary heart disease, headache, dizziness, kidney disorder, impotence and premature ejaculation; for preventing cerebral aging; for improving memory, cerebral functions; or for curing enuresis, frequent micturition, urinary incontinence, dementia, weak intelligence and Alzheimer's disease, autism, brain trauma, Parkinson's disease or other diseases caused by cerebral dysfunctions, and treating arthritis, rheumatism, poor circulation, arteriosclerosis, Raynaud's syndrome, angina pectoris, cardiac disorder, coronary heart disease, headache, dizziness, kidney disorder.

Abstract: This invention relates to the compound extracted from husk and fruit stem of Xanthoceras Sobifolia and its extracting method and use thereof.

Abstract: Disclosed herein are compositions comprising lopinavir alone or in combination with ritonavir for use as a medicament in the treatment of cancer or benign proliferative disorders (warts) or in the prevention of the development of cancer. Pharmaceutical compositions formulated for topical application comprising a therapeutically effective amount of lopinavir or a therapeutically effective amount lopinavir and ritonavir in a pharmaceutically acceptable vehicle are also provided. Also disclosed are methods of treating a patient having an HPV related dysplasia of the cervix comprising administering to said patient a therapeutically effective dose of the disclosed pharmaceutical compositions.

Abstract: Methods of treatment or prevention of a cancerous or pre-cancerous condition, of slowing or preventing growth of a cancerous condition, of stimulating a cell-mediated immune response, stimulating a Th1 helper T cell response against a pathogen in a mammal and of treating or preventing inflammatory diseases or disorders that involve administration of N-methyl pyrrolidone (NMP) or a physiologically acceptable salt, solvate, tautomer or prodrug thereof are provided. Also provided are formulations of an active agent.

Abstract: The present invention relates to an oridonin functionalized selenium nanoparticle, method of preparing and use thereof for anti-cancer and anti-inflammatory treatments. The present invention provides oridonin functionalized selenium nanoparticle that is stable, water soluble and storable.

Abstract: The invention relates generally to formulations having one or more ingredients segregated from other constituents of the same formulation. The formulations are typically for topical application to an integument.

Abstract: The present invention pertains to novel uses of glycyrrhetinic acid (GA), glycyrrhizic acid (GLA) and related compounds for prevention and/or treatment of pulmonary fibrosis, in particular, irradiation-induced pulmonary fibrosis. Also embodied are therapeutic uses of prodrugs, metabolites, derivatives (e.g., acids, esters and ethers), and salts of glycyrrhetinic acid (GA) and glycyrrhizic acid (GLA). The present invention also provides for therapeutic or pharmaceutical compositions comprising a compound of the invention in a form that can be combined with a pharmaceutically acceptable carrier.

Abstract: The invention relates to the use of an oral composition comprising steviol, a steviol precursors or Stevia extract as skin tanning agent. It further relates methods of enhancing the natural skin tan by oral administration of an effective amount of Steviol, a Steviol precursor or Stevia extract.

Abstract: SAPONINS AND CHROMANS DERIVATIVES MIXTURE COMPOSITIONS AGAINST LEISHMANIASIS, TRYPANOSOMIASIS AMERICANA, MALARIA, TRYPANOSOMIASIS AFRICANA AND FASCIOLA HEPATICA, is a composition of saponins and chromans derivatives. The saponins are triterpene types and chromans are hydrazones derivatives. This composition is a therapeutic agent against tropical diseases.

Abstract: The present invention relates to reduced toxicity of functional alcoholic beverage composition comprising distilled alcohol, deionized water, 18?-Glycyrrhizin or 18?-Glycyrrhizin and a sugar alcohol or sugars, having pH in the range of 4.0-9.0. More particularly, alcoholic beverage composition comprises distilled alcohol, deionized water, 18?-Glycyrrhizin or 18?-Glycyrrhizin and a sugar alcohol/sugars as hepato-protectants. The present invention provides an alcoholic beverage for reducing hepatotoxicity caused by its consumption and a process to manufacture the said alcoholic beverage.

Abstract: The present disclosure encompasses QS-21-based structurally-defined adjuvants to address the need for stronger, safer, and easier-to-access adjuvants. The new compositions can provide tools for addressing long-standing mechanistic questions concerning saponin immune-potentiation through structure-activity-relationship (SAR) studies. Most advantageously, the compounds of the disclosure may be formulated into pharmaceutically acceptable compositions, including vaccines that may be delivered to a subject human or animal subject. The compounds can then act as, for example, an adjuvant to augment an immunological response to a vaccine immunogen.

Abstract: The invention provides methods and compositions for the diagnosis, prognosis and treatment of respiratory tract diseases. Specifically, the invention provides diagnosis, prognosis and treatment of respiratory infections using bitter and sweet taste signal transduction pathways. In one aspect, the invention relates to a method for treating a respiratory infection by administering a composition to the respiratory tract of a subject in an amount capable of activating bitter taste signaling and/or inhibiting sweet taste signaling. The composition comprises at least a bitter receptor agonist and, optionally, a pharmaceutically acceptable carrier for delivering the composition to the respiratory tract. In another aspect, the invention relates to a composition for treatment of a respiratory infection. Such composition comprises at least a bitter receptor agonist and, optionally, a pharmaceutically acceptable carrier for delivering the composition to the respiratory tract.

Abstract: The present invention relates to conjugates of therapeutically useful anthracyclines with carriers such as polyclonal and monoclonal antibodies, proteins or peptides of natural or synthetic origin; methods for their preparation, pharmaceutical composition containing them and use thereof in treating certain mammalian tumors.

Abstract: The present invention relates to triterpene glycoside saponin-derived adjuvants, syntheses thereof, intermediates thereto, and uses thereof. QS-7 is a potent immuno-adjuvant that is significantly less toxic than QS-21, a related saponin that is currently the favored adjuvant in anticancer and antiviral vaccines. Tedious isolation and purification protocols have hindered the clinical development of QS-7. A novel semi-synthetic method is provided wherein a hydrolyzed prosapogenin mixture is used to synthesize QS-7, QS-21, and related analogs, greatly facilitating access to QS-7 and QS-21 analogs for preclinical and clinical evaluation.

Abstract: Described herein are compositions and methods for treating or preventing a sexually transmitted infection in a subject

Abstract: The present invention relates to a topical pharmaceutical composition of thiocolchicoside and methylsulfonylmethane comprising at least one penetration enhancer and one or more gelling agent. Furthermore, the invention relates to process for preparing the said topical pharmaceutical composition and its use for the treatment of pain and inflammatory symptoms associated with muscle-skeletal system and osteoarthritis.

Abstract: This invention is a novel pharmaceutical composition comprising flurbiprofen or a pharmaceutically acceptable salt thereof in combination with an ?-2 adrenergic receptor agonist or a gamma-aminobutiric acid receptor agonist with anti-inflammatory, analgesic and myorelaxant activity.

Abstract: The present invention describes a formulation comprising a prune and/or plum concentrate, and one or more water-soluble, non-digestible, prebiotic oligosaccharides. Optionally, one or more low calorie sweeteners, an antioxidant, calcium sennosides, or sennosides extract, PEG-3350, licorice, cocoa, coffee, tea flavors; fruit flavorings and spice flavorings, gelatin, agar-agar, carrageenan, pectin or cocoa powder are added. Other ingredients may be present as dietary supplements such as water-soluble vitamins, lipid-soluble vitamins; amino acids, maltodextrin, resveratrol, caffeine, mineral supplements, or natural sleep aids for use as a laxative, A variety of formulations are possible, such as premix, a laxative+energy power drink or power bar, or as a prebiotic supplement in probiotic yogurts, or in the form of gummies, chocolates, candies, and desserts such as red beans Japanese desserts.

Abstract: An agent for preventing or ameliorating skin aging, which exhibits a more excellent effect on the suppression of formation, or the amelioration, of wrinkles on the skin or sagging skin. An agent for preventing or ameliorating skin aging, containing triterpenoid saponins represented by the following formula (1) as an active ingredient, wherein at least one of R1 and R2 is a tigloyl group and the other represents a tigloyl group or an angeloyl group; R3 represents a methyl group or a hydroxymethyl group; and R4 represents Glc, Xyl or Gal.

Abstract: This invention provides a composition comprising a triterpenoid saponin, comprising two side groups attached to carbons 21, and 22 of the triterpenoid saponin backbone, for inhibiting skin or ovarian tumor cell growth.

Abstract: The invention aims at finding a highly-safe natural product having glutathione production-enhancing activity, and providing a glutathione production enhancer and a prophylactic/therapeutic agent for diseases caused by glutathione deficiency using that natural product as an active ingredient. The glutathione production enhancer or the prophylactic/therapeutic agent for diseases caused by glutathione deficiency contains, as an active ingredient, a licorice extract composition that contains liquiritin, liquiritigenin, isoliquiritin and isoliquiritigenin but contains substantially no glycyrrhizic acid.

Abstract: The present invention relates to new aminopyrimidine inhibitors of tyrosine kinase activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Provided herein are bitter taste receptor ligands, related agents, combinations, compositions, methods and systems for modulating release of a metabolic hormone in vitro or in vivo from cells of the GI tract of an individual.

Abstract: This invention provides a method of synthesizing new active compounds for pharmaceutical uses including cancer treatment, wherein the cancers comprise breast, leukocytic, liver, ovarian, bladder, prostatic, skin, bone, brain, leukemia, lung, colon, CNS, melanoma, renal, cervical, esophageal, testicular, spleenic, kidney, lymphatic, pancreatic, stomach and thyroid cancers. This invention is an anti adhesion therapy which uses the compound as a mediator or inhibitor of adhesion proteins and angiopoietins. It inhibits excess adhesion and inhibits cell attachment. It modulates angiogenesis. The compounds also use as mediator of cell adhesion receptor, cell circulating, cell moving and inflammatory diseases.

Abstract: Aureolic acid derivatives, process for obtaining them and uses thereof. This invention provides a bacterial strain that produces compound belonging to the family of aureolic acids useful in the treatment of cancer or nervous system diseases.

Abstract: Disclosed herein are novel cytoprotective derivatives of avicin D, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising these derivative compounds. Methods and intermediates useful for making the derivatives, and methods of using the derivatives and compositions thereof, including for the treatment of cancer, are also provided.

Abstract: The present invention provides hydroxyl, keto, and glucuronide derivatives of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile.

Abstract: The present invention relates to a patch for the transdermal release of diclofenac or a pharmaceutically acceptable salt thereof, in particular diethylamine salt, and thiocolchicoside.

Abstract: This invention relates, e.g., to a method for designing or selecting on a computer a candidate small molecule amyloid binder or inhibitor, comprising: a) docking test compounds to the binding site or binding surface determined from the three-dimensional structure of a co-crystal of a protofilament of an amyloid protein bound to a small molecule which is known to bind to the amyloid protein, and (b) selecting test compounds which exhibit an energy below that of the small molecule used to form the co-crystal made in a), as candidate amyloid binders.

Abstract: This invention provides methods, processes, compounds and compositions for modulating the gene expression and modulating the secretion, expression, or synthesis of adhesion proteins or their receptors to cure disease, wherein the modulating comprises positive and negative regulating; wherein comprises inhibiting cancer growth, wherein the adhesion proteins or receptors comprise fibronectin, integrins family, Myosin, vitronectin, collagen, laminin, Glycosylation cell surface proteins, polyglycans, cadherin, heparin, tenascin, CD 54, CAM, elastin and FAK; wherein the methods, processes, compounds and compositions are also for anti-angiogenesis; wherein the cancers comprise breast cancer, leukocyte cancer, liver cancer, ovarian cancer, bladder cancer, prostate cancer, skin cancer, bone cancer, brain cancer, leukemia cancer, lung cancer, colon cancer, CNS cancer, melanoma cancer, renal cancer or cervix cancer.

Abstract: A silicone surfactant-based synergistic agricultural formulation contains a combination of a first defined silicone surfactant and a second defined silicone surfactant in a concentration sufficient to cause a knockdown level on treated arthropods, even in the absence of known pesticidally active ingredients.

Abstract: Acaciaside-B (Ac-B) has emerged as a prospective candidate molecule for prevention of HIV infection along with potential for use as/in vaginal contraceptive/formulation. It possesses anti-HIV property at a tolerably low concentration, is non-mutagenic and does not harm the niche of Lactobacilli. Thus Ac-B appears to be a superior ingredient for formulations of a chemical barrier against HIV-1 infection wherein its spermicidal property is superfluous.

Abstract: This application provides compositions and methods useful in the treatment of certain cancers. In part, this application is based on the recognition that certain molecules that target abasic lesions or AP sites in DNA improve, augment, or potentiate the chemotherapeutic efficacy of certain anticancer agents.

Abstract: Wash compositions for topical application are described. The compositions can be stable and well tolerated. Also described, are methods of using such compositions as cosmetic or pharmaceutical products. For example, the compositions can be used for cleansing the skin, preferably of acne patients, without compromising the skin barrier or resulting in over-compensation of sebum production. A topical wash composition is also described that can include: a) at least one surfactant; b) a zinc salt of gluconic acid; and c) a salt or derivative of glycyrrhizic acid or of glycyrrhetinic acid.

Abstract: A soy saponin composition is provided high bodily absorption characteristics. In an embodiment, a soyasapogenol composition comprises soyasapogenol B and 3-O-D-glucuronopyranosyl soyasapogenol B. The weight ratio (B/A) of the 3-O-D-glucuronopyranosyl soyasapogenol B to the soyasapogenol B is in the range of 0.001-10. The composition can be produced by partial decomposition of a sugar chain residue of a soy saponin B group glycoside utilizing an acid.

Abstract: A topical pharmaceutical gel includes flurbiprofen or a pharmaceutically acceptable salt of flurbiprofen, thiocolchicoside or a pharmaceutically acceptable salt of thiocolchicoside, and menthol. Pharmaceutical combinations of flurbiprofen, thiocolchicoside, and menthol in the form of topical gels with anti-inflammatory, analgesic, and myorelaxant activities are described.

Abstract: The invention relates to the preparation of phenolics derivatives by enzymatic condensation of phenolics selected among pyrocatechol or its derivatives with the glucose moiety of sucrose. The production of said phenolics derivatives is achieved with a glucosyltransferase (EC 2.4.1.5). These O-?-glucosides of selected phenolics are new, have a solubility in water higher than that of their parent polyphenol and have useful applications in cosmetic and pharmaceutical compositions, such as antioxidative, antiviral, antibacterial, immune-stimulating, antiallergic, antihypertensive, antiischemic, antiarrythmic, antithrombotic, hypocholesterolemic, antilipoperoxidant, hepatoprotective, anti-inflammatory, anticarcinogenic, antimutagenic, antineoplastic, anti-thrombotic and vasodilatory formulations, or in any other field of application.

Abstract: A method for producing a pharmaceutical composition comprising a combination of phospholipid and glycyrrhizic acid or a pharmaceutically acceptable salt thereof, which composition is hydratable to produce an injectable medicinal form, said method comprising subjecting a mixture of phospholipid and an aqueous solution of glycyrrhizic acid or a pharmaceutically acceptable salt thereof and a carbohydrate to homogenization, for example at 800-1200 bar pressure at a temperature of less than 90° C., and subjecting the product of the homogenization to a sublimation drying step to produce said composition. Compositions obtainable using this method, and hydrated forms of these ready for administration by injection form further aspects of the invention.

Abstract: Herein, methods of modulating inclusion formation and stress granules in cells are described. The methods comprise contacting a cell with an inclusion inhibitor. Methods for screening for modulators of TDP-43 aggregation are also described.