Abstract: Oxidation resistant bioprosthetic tissues and oxidation resistant bioprosthetic heart valve leaflets are described. Also provided are methods for preparing the oxidation resistant bioprosthetic tissues and bioprosthetic heart valve leaflets, and methods for preventing oxidative degeneration in bioprosthetic tissues, including immobilizing covalently an effective amount of an antioxidant to the bioprosthetic tissue.

Abstract: The present invention relates to a method of treating or preventing the visual function loss in optic nerve in a subject after crush injury by using 4-(Phenylsulfanyl)butane-2-one (4-PSB-2). The present invention has the ability of enhancing the protection effect of RGCs, preserving the visual function in optic nerve after crush injury, recovering the visual function loss, attenuating apoptosis in optic nerve after injury, and inhibiting the inflammatory responses in optic nerves after ON injury.

Abstract: A method of improving the appearance of aging skin that includes applying an effective amount of artichoke leaf extract and carob fruit extract in combination to a target area of skin that exhibits a sign of aging skin. The composition is applied for a period of time sufficient to improve the appearance of the aging skin.

Abstract: Green tea polyphenol compositions and methods of their use in treating herpes simplex virus (HSV) are provided. Representative green tea polyphenols include, but are not limited to (?)-epigallocatechin-3-gallate as well as green tea polyphenols with one on more ester-linked fatty acids.

Abstract: The embodiments herein provide a long-acting injectable drug (insulin) delivery nano-carrier system and a method of synthesizing the same. The insulin entrapped nanoparticles are prepared using a lipid/phospholipid core which is coated by a polymer. The lipid and phospholipid are dissolved in organic solvent. This solution is transferred into an aqueous phase consisting of distilled water or a buffer and dissolved insulin. A solution of polymer is added drop wise. The drug entrapped nanoparticle formation is achieved by diffusion of the organic solvent within the aqueous solvent to obtain the nanoparticles. The drug gets entrapped within the formed nanoparticles via the anti-solvency effect of the aqueous matrix. The resulting drug nanocarriers are capable of releasing the drug in a slow rate upon injection. The synthesized drug carrying nanoparticles are cryopreserved stored for future administration. For better storage the nanodispersion is dried to form a powder.

Abstract: The present invention relates to methods and compositions for treating a subject suffering from a sclerosing disorder, comprising administering, to the subject, an effective amount of an estrogen receptor antagonist (“ERANT”), wherein said ERANT has essentially no estrogen receptor agonist activity under physiologic conditions.

Abstract: It is an object of the present invention to provide a method for improving the solubility of a poorly-soluble substance, which is capable of increasing the solubility of substantially all poorly-soluble substances. This is a method comprising coating the surface of a poorly-soluble substance particle with microparticles of a calcium compound such as calcium phosphate or calcium carbonate, and at least one selected from a pH adjuster and a surfactant, by applying mechanical energy thereto.

Abstract: The present invention relates to a compound of the general formula (I) where: X?S, SO or SO2; and one of the radicals R1 and R2 is a hydrogen atom and the other is a radical: a C1 to C18 linear or branched alkyl, optionally substituted by one or more halogen atom(s); a C2 to C18 linear or branched alkenyl, optionally substituted by one or more halogen atom(s); an aralkyl, optionally substituted by one or more C1 to C6 alkoxy group(s); or a COR3 or CONHR3, but not simultaneously, where R3 is a radical: a C1 to C18 linear or branched alkyl, optionally substituted by one or more halogen atom(s); a C2 to C18 linear or branched alkenyl, optionally substituted by one or more halogen atom(s); an aralkyl, optionally substituted by one or more C1 to C6 alkoxy group(s); an aralkenyl, optionally substituted by one or more C1 to C6 alkoxy groups and/or one or more OH group(s); or an aryl radical, optionally substituted by one or more C1 to C6 alkoxy group(s).

Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.

Abstract: Treatment of cancer includes administering a compound of formula (I) to a subject. In particular, treatment of colorectal cancer is described.

Abstract: The present disclosure relates to lipid compounds of formula (I): wherein: R1 is chosen from a C10-C21 alkyl, a C10-C21 alkenyl having 1-6 double bonds, and a C10-C21 alkynyl having 1-6 triple bonds; R2 and R3 are the same or different and are chosen from hydrogen and a C1-C6 alkyl; X is chosen from O, S, SO, SO2, Si, and Se; n=1 or 3; and P1 is chosen from hydrogen; a C10-C21 alkyl, a C10-C21 alkenyl having 1-6 double bonds, a C10-C21 alkynyl having 1-6 triple bonds, optionally substituted; a group of formula (II) or formula (III), wherein P2, P3, and P4 are chosen from hydrogen, an alkyl, an alkenyl, and an alkynyl, optionally substituted; and a group of formula (IV) or formula (V), wherein P5 is chosen from hydrogen and a C1-C6 alkyl; or a pharmaceutically acceptable salt, complex, or solvate thereof.

Abstract: This invention pertains to methods and compositions for the diagnosis and treatment of cardiovascular conditions. More specifically, the invention relates to isolated molecules that can be used to diagnose and/or treat cardiovascular conditions including cardiac hypertrophy, myocardial infarction, stroke, arteriosclerosis, and heart failure.

Abstract: The invention relates to a sulfur-containing compound and the preparation thereof. The invention also relates to the uses of the sulfur-containing compound in inhibiting inducible nitric oxide synthase and/or cyclooxygenase-2 and in treating the diseases associated with inducible nitric oxide synthase and/or cyclooxygenase-2. This invention also describes a series of chemical analogues of the said sulfur-containing compound and the preparation of these compounds.

Abstract: This invention provides methods of inhibiting replication of a poxvirus by contacting a poxvirus with a compound having formula I, formula XXI, formula XXXII, or formula XLI which in turn reduce, inhibit, or abrogate poxvirus DNA polymerase activity and/or its interaction with its processivity factor. Formula I, formula XXI, formula XXXII, or formula XLI can be utilized to treat humans and animals suffering from a poxvirus infection. Pharmaceutical compositions for treating poxvirus infected subjects are also provided.

Abstract: A personal care composition which contains 25-200 ppm of 2-methyl-4-isothiazolin-3-one and at least one hydroquinone radical scavenger, and a method for reducing odor arising in personal care compositions containing 2-methyl-4-isothiazolin-3-one.

Abstract: The present invention relates to the use of polyols of formula (I): or a salt thereof, for preventing the hair from breaking. The invention also relates to a cosmetic composition comprising at least one such polyol or a salt thereof, in a cosmetically acceptable medium, and also to a cosmetic hair treatment process using the said composition.

Abstract: The presently disclosed and claimed inventive concept(s) provides new estrogenic compounds of the general formula and pharmaceutical compositions containing them. The compounds of the presently disclosed and claimed inventive concept(s) are useful, for example, in hormone replacement therapies (HRT/ERT), and as contraceptives, and estrogenic hormone therapies. Also provided is a process for synthesizing the compounds of the presently disclosed and claimed inventive concept(s).

Abstract: This invention pertains to methods and compositions for the diagnosis and treatment of cardiovascular conditions. More specifically, the invention relates to isolated molecules that can be used to diagnose and/or treat cardiovascular conditions including cardiac hypertrophy, myocardial infarction, stroke, arteriosclerosis, and heart failure.

Abstract: The present invention relates to the use of one or more compounds selected from the following classes of biologically active agents: an a-adrenergic antagonist, an anthelmintic agent, an antifungal agent, an antimalarial agent, an antineoplastic agent, an antipsychotic agent, an antioxidant, a vasodilator and/or a vitamin, or a pharmaceutically acceptable derivative thereof, for use in the treatment of a microbial infection and in particular for killing multiplying, non-multiplying and/or clinically latent microorganisms associated with such an infection.

Abstract: Disclosed is a substance which has a low molecular weight, can be applied in a simpler manner, and has an immunopotentiating activity against cancer and/or a microorganism-mediated infectious disease. An EP4 agonist exhibits an immunopotentiating activity through the activation of a cytotoxic T cell, and is therefore useful for the prevention and/or treatment of cancer or a microorganism-mediated infection disease.

Abstract: The present invention relates to allosteric binding compounds of formula (I), especially for the treatment of CNS disorders, together with pharmaceutical compositions and methods of treatment including these compounds.

Abstract: This invention provides compounds having a structure of Formula (I). Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provided.

Abstract: This invention relates to compounds which selectively bind to the survival protein MCL-1 with high affinity and selectivity, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for modulating MCL-1 activity and for treating hyperproliferative disorders, angiogenesis disorders, cell cycle regulation disorders, autophagy regulation disorders, inflammatory disorders, and/or infectious disorders and/or for enhancing cellular engraftment and/or wound repair, as a sole agent or in combination with other active ingredients.

Abstract: The present disclosure relates generally to treating or preventing diseases associated with angiogenesis by administering to a patient certain compounds found to inhibit or substantially reduce angiogenesis. Compounds employed according to the present disclosure exhibit good anti-angiogenic activity as well as demonstrate a prophylactic effect for preventing and substantially reducing angiogenesis. Examples of such compounds include Ritanserin, Amiodarone, Terfenadinc, Perphenazine, Bithionol, and Clomipramine.

Abstract: Therapeutic agents for treatment of Galactosemia and disorders thereof, and other enzyme related disorders thereof are identified. The compounds inhibit galactokinase (GALK) and other kinase activity and are identified by a high throughput screening assay.

Abstract: Compositions and methods for managing or treating chronic pain are provided. More particularly, methods are provided for managing or treating chronic pain by administering to a patient in need thereof an effective amount of propofol or a propofol derivative having limited anesthetic properties. Methods of modulating HCN channel gating are also provided. Pharmaceutically acceptable compositions for, e.g., modulating HCN channel gating are further provided.

Abstract: Compounds of the formulae and selected hindered nitroxyl, hydroxylamine and hydroxylamine salt compounds such as the compound of the formula wherein G1 is hydrogen; C1-C22alkyl; C1-C22alkylthio; C2-C22alkylthioalkyl; C5-C7cycloalkyl; phenyl; C7-C9-phenylalkyl; or SO3M; G2 is C1-C22alkyl; C5-C7cycloalkyl; phenyl; or C7-C9-phenylalkyl; E is oxyl or hydroxyl; V is —O—; or —NH—; a is 0 or 1 or 2; b, c and d and g are each independently of one another 0 or 1; e is an integer from 1 to 4; f, m, n and p are each independently of one another an integer from 1 to 3; q is 0 or an integer from 1 to 3; Q, T and G3 are as defined in claim 1; G4 and G5 are each independently of the other hydrogen; or C1-C22alkyl; exhibit marked antiinflammatory action.

Abstract: This invention provides methods of inhibiting replication of a poxvirus by contacting a poxvirus with a compound having formula I, formula XXI, formula XXXII, or formula XLI which in turn reduce, inhibit, or abrogate poxvirus DNA polymerase activity and/or its interaction with its processivity factor. Formula I, formula XXI, formula XXXII, or formula XLI can be utilized to treat humans and animals suffering from a poxvirus infection. Pharmaceutical compositions for treating poxvirus infected subjects are also provided.

Abstract: The present invention relates to compositions and methods for treating, preventing and improving the condition and/or aesthetic appearance of skin, particularly, treating, preventing, ameliorating, reducing and/or eliminating fine lines and/or wrinkles of skin, where the compositions include active agents which increase expression levels of genes associated with the dermatological signs of aging. The compositions of the invention are topically applied to the skin, or are delivered by directed means to a site in need thereof, once daily in an amount effective in improving the condition and/or aesthetic appearance of skin.

Abstract: Methods of treating cancer by administering effective amounts of a Ras antagonist comprising FTS, or analogs thereof, or a pharmaceutically acceptable salt, and 2-deoxyglucose (2DG) to a patient are disclosed. Pharmaceutical compositions useful in treating cancer containing a Ras antagonist comprising FTS, or analogs thereof, or a pharmaceutically acceptable salt, and 2DG are also disclosed.

Abstract: Disclosed are methods of treating ovarian cancer by administering an effective amount of FTS (farnesylthiosalicylic acid), or various analogs thereof, or a pharmaceutically acceptable salt, optionally with, a platinum-based chemotherapy drug to a human diagnosed with ovarian cancer.

Abstract: The present invention provides a medical device for placement into a lumen such as a stent and a catheter whose surface is uniformly and sufficiently coated with a drug, and a process thereof with easy way and with low cost. The medical device is coated with mixed particles of drug particles whose surface is modified with positive-charge and biocompatible nanoparticles. In the invention, a drug can be taken into a cell through the dissolution of the drug particle together with the biocompatible nanoparticle after a DES is placed in a biological body.

Abstract: A therapeutic agent for the treatment of diabetic neuropathy which comprises (±)-[2-[4-(3-ethoxy-2-hydroxypropoxy)phenylcarbamoyl]-ethyl]dimethylsulfonium p-toluenesulfonate of the formula (1) as an active ingredient.

Abstract: There is provided an organic sulfur compound having an excellent controlling effect on harmful arthropods represented by the formula (I): wherein, R1 represents a C3-C10 alkenyl group optionally substituted with at least one halogen atom, a C3-C10 alkynyl group optionally substituted with at least one halogen atom, or the like, R2 represents a cyano group or the like, R3 represents a hydrogen atom, a halogen atom or a C1-C4 alkyl group, R4 represents a C1-C5 fluoroalkyl group, and n represents 0, 1 or 2.

Abstract: The present invention relates to methods and compositions for treating a subject suffering from a sclerosing disorder, comprising administering, to the subject, an effective amount of an estrogen receptor antagonist (“ERANT”), wherein said ERANT has essentially no estrogen receptor agonist activity under physiologic conditions.

Abstract: The present invention relates to allosteric binding compounds of formula (I), especially for the treatment of CNS disorders, together with pharmaceutical compositions and methods of treatment including these compounds.

Abstract: The present invention relates to a compound of the general formula (I) where: X?S, SO or SO2; and one of the radicals R1 and R2 is a hydrogen atom and the other is a radical: a C1 to C18 linear or branched alkyl, optionally substituted by one or more halogen atom(s); a C2 to C18 linear or branched alkenyl, optionally substituted by one or more halogen atom(s); an aralkyl, optionally substituted by one or more C1 to C6alkoxy group(s); or a COR3 or CONHR3, but not simultaneously, where R3 is a radical: a C1 to C18 linear or branched alkyl, optionally substituted by one or more halogen atom(s); a C2 to C18 linear or branched alkenyl, optionally substituted by one or more halogen atom(s); an aralkyl, optionally substituted by one or more C1 to C6alkoxy group(s); an aralkenyl, optionally substituted by one or more C1 to C6 alkoxy groups and/or one or more OH group(s); or an aryl radical, optionally substituted by one or more C1 to C6 alkoxy group(s).

Abstract: Provided are compounds for inhibiting Snail-p53 binding and therapeutic agents for cancer including the compounds as an effective component. The Snail-p53 binding inhibitors induce expression of p53 in K-Ras mutant cell lines, thereby enabling effective treatment or prevention of K-Ras mutant cancer, such as, pancreatic cancer, lung cancer, cholangioma, and colon cancer, of which diagnosis or treatment is not easy.

Abstract: Methods and compositions for the treatment or prophylaxis of a disorder associated with platelet activation or enhanced thrombin activity are provided, that include the administration of an effective amount of a compound of the formula: or its pharmaceutically acceptable salt, ester or prodrug, wherein the substituents are defined herein, optionally in the appropriate pharmaceutically acceptable carrier for the route of administration selected.

Abstract: Therapeutic agents for treatment of Galactosemia and disorders thereof, and other enzyme related disorders thereof are identified. The compounds inhibit galactokinase (GALK) and other kinase activity and are identified by a high throughput screening assay.

Abstract: The present invention provides new estrogenic compounds of the general formula in which the substituents have the meanings that are explained in more detail in the description, and pharmaceutical compositions containing them. The compounds of the invention are useful, for example, in hormone replacement therapies (HRT/ERT) and as contraceptives and estrogenic hormone therapies. Also provided is a process for synthesizing the compounds of the invention.

Abstract: A composition for use in inhibiting the binding of a Norovirus to the histo-blood group antigen on the surface of epithelia. The composition contains a therapeutically effective amount of a binding-inhibiting compound selected from Compounds 1 through 15, and at least one diluent, carrier or excipient. The Compounds competitively bind a Norovirus that has the capability of binding with the histo-blood group antigens of secretor blood type, including A, B, AB, and O blood types. The compositions can be administered to a human prior to or after infection by a Norovirus, to prevent or ameliorate an infection.

Abstract: Autotaxin (ATX) is a prometastatic enzyme initially isolated from the conditioned media of human melanoma cells that stimulates a myriad of biological activities including angiogenesis and the promotion of cell growth, survival, and differentiation through the production of lysophosphatidic acid (LPA). ATX increases the aggressiveness and invasiveness of transformed cells, and ATX levels directly correlate with tumor stage and grade in several human malignancies. To study the role of ATX in the pathogenesis of malignant melanoma, we developed antibodies and small molecule inhibitors against recombinant human protein. Immunohistochemistry of paraffin embedded human tissue demonstrates that ATX levels are markedly increased in human primary and metastatic melanoma relative to benign nevi. Chemical screens identified several small molecule inhibitors with binding constants ranging from nanomolar to low micromolar.

Abstract: The present invention includes a group of chemical compounds useful as modulators of calcium ion (Ca2+) channels, especially for T-type, N-Type and L-type channels. The present invention also includes pharmaceutical compositions comprising these calcium ion channel modulating agents and methods of using these calcium ion channel modulating agents for the treatment diseases and conditions associated with the calcium ion channels.

Abstract: Treatment of cancer includes administering a compound of formula (I) to a subject. In particular, treatment of colorectal cancer is described.

Abstract: The present disclosure relates to lipid compounds of formula (I): wherein: R1 is chosen from a C10-C21 alkyl, a C10-C21 alkenyl having 1-6 double bonds, and a C10-C21 alkynyl having 1-6 triple bonds; R2 and R3 are the same or different and are chosen from hydrogen and a C1-C6 alkyl; X is chosen from O, S, SO, SO2, Si, and Se; n=1 or 3; and P1 is chosen from hydrogen; a C10-C21 alkyl, a C10-C21 alkenyl having 1-6 double bonds, a C10-C21 alkynyl having 1-6 triple bonds, optionally substituted; a group of formula (II) or formula (III), wherein P2, P3, and P4 are chosen from hydrogen, an alkyl, an alkenyl, and an alkynyl, optionally substituted; and a group of formula (IV) or formula (V), wherein P5 is chosen from hydrogen and a C1-C6 alkyl; or a pharmaceutically acceptable salt, complex, or solvate thereof.

Abstract: Processes for synthesizing resveratrol-based oligomers are provided. In addition, resveratrol-based oligomer compounds free of plant extract are provided.

Abstract: The present invention provides a method for treating a disease or condition in a mammal associated with influx of extracellular calcium via T type calcium channels, which comprises administering to the mammal a therapeutically effective amount of a T type calcium channel inhibitor, a prodrug thereof, or a pharmaceutically acceptable salt of said inhibitor or prodrug, wherein the T type calcium channel inhibitor has a structure represented by Formula (I): Formula (I), wherein R1 is selected from the group consisting of C1-C4 alkyl, hydroxy and C1-C4 alkoxy; X is selected from the group consisting of N and CH; Z is selected from the group consisting of NH, O, S and CH2; R2 is selected from the group consisting of H, halo, NH2, C1-C4 alkyl, hydroxy and C1-C4 alkoxy; and R3 is selected from the group consisting of H, halo, NH2, C1-C4 alkyl, hydroxy and C1-C4 alkoxy.

Abstract: Disclosed is a substance which has a low molecular weight, can be applied in a simpler manner, and has an immunopotentiating activity against cancer and/or a microorganism-mediated infectious disease. An EP4 agonist exhibits an immunopotentiating activity through the activation of a cytotoxic T cell, and is therefore useful for the prevention and/or treatment of cancer or a microorganism-mediated infection disease.

Abstract: The present invention provides a method and compositions for synthesizing an oligopeptide or polypeptide by convergent assembly of a plurality of pairs of oligopeptides in chemical ligation reactions. An important aspect of the present invention is an oligopeptide having a C-terminal disulfide-protected carboxythioester group that can be deprotected to spontaneously generate a free C-terminal thioester moiety. This allows a single precursor to participate in a succession of chemical ligation reactions, thereby making the convergent synthesis approach possible. The present invention is useful in methods for chemical synthesis of oligopeptides, polypeptides and proteins, and improves the efficiency of native chemical ligation reactions, particularly where four or more peptide fragments are used to assemble an oligopeptide, polypeptide or protein product.