Abstract: The present disclosure relates to compounds, cosmetic or dermopharmaceutical compositions comprising the same, and methods for using the compounds or compositions for treating, protecting, and/or improving the condition and/or aesthetic appearance of skin, for example, treating, preventing, ameliorating, reducing and/or eliminating fine lines and/or wrinkles of skin, or improving the appearance of fine lines and/or or wrinkles of skin comprising application of the compounds or compositions disclosed.

Abstract: [Problem] Provided is a non-peptide compound which can be used as a GAPDH aggregation inhibitor. [Solution] Provided is a GAPDH aggregation inhibitor including as an active ingredient a compound represented by the chemical formula 1 wherein R1, R2, and R3 are each independently a hydrogen atom, a halogen atom, or an aliphatic hydrocarbon group having a carbon number of from 1 to 10, a polysulfurized derivative thereof, or a pharmaceutically acceptable salt thereof. The present compound has a GAPDH aggregation inhibitory activity to suppress intracerebral aggregation of various proteins involved in cerebral neurodegenerative diseases, thereby contributing to improvement in various brain neurological diseases associated with aggregation of these proteins such as Alzheimer's disease, Parkinson's disease, and cerebral infarction, and prevention of advanced seriousness of these diseases.

Abstract: Provided are compositions and methods for modulating quorum sensing in microbes. The compounds are AI-2 analogs and as such have structures similar to 4,5-dihydroxy-2,3-pentanedione that can act as agonists/antagonists of quorum sensing. The compounds are useful for modulating quorum sensing in bacteria and can be used in methods for prophylaxis or therapy of bacterial infections and for reduction of biofilms.

Abstract: A method is provided for the treatment of vision problems in a subject suffering from one of various forms of albinism, including, for example, oculocutaneous albinism types OCA1a and OCA1b, as well as ocular albinism type 1, resulting from mutations in the GPR143 gene, as well as the OCA2, OCA3 or OCA4 genes, by administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of the compound (2-[2-nitro-4-(trifluoromethyl)benzoyl]cyclohexane-1,3-dione), also known as NTBC for a sufficient period of time. The administration of NTBC is believed to increase the amount of pigmentation in the subject and alleviate certain symptoms caused by lack of pigmentation in the eye tissues. Also described are methods of use of NTBC for increasing the pigmentation of a subject for cosmetic purposes, by administering to the subject a therapeutically effective amount of NTBC.

Abstract: The invention relates to a pharmaceutical composition comprising a compound of formula (1) wherein R1 is optionally substituted phenyl, optionally substituted pyridyl or optionally substituted indolyl; R2 is (CH2)n wherein n is 0, 1, 2, 3 or 4; R3 is (CH2)mR3A wherein m is 0, 1, 2, 3 or 4, and R3A is methyl, isopropyl, tert-butyl, OCH3, OH, optionally substituted phenoxy, C?CH, C?N, optionally substituted phenyl, furanyl or thienyl; A is a ring containing X1 with the meaning O, S, NH, N(CH3) or CH2; and X2 is O, S or NH; and a compound of formula (2) wherein R4 is optionally substituted phenyl, optionally substituted pyridyl, optionally substituted indolyl, —NR7R8; or —NH—N?CH—R9; and substituents R5 to R9 have the meanings indicated in the description, in particular ethionamide. The pharmaceutical composition is useful, e.g., in the treatment of multidrug-resistant tuberculosis.

Abstract: The present invention relates to nitric oxide donor compounds having a quinone based structure, to processes for their preparation and to their use in the treatment of pathological conditions where a deficit of NO plays an important role in their pathogenesis.

Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic pain.

Abstract: It is provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of trans-thyretin-associated amyloidosis. It is also provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of transthyretin-associated amyloidosis in combination therapy with another COMT inhibitor, a benzoxazole derivative, iododiflunisal, diflunisal, resveratrol, tauroursodeoxycholic acid, doxocycline, or epigallocatechin-3-gallate.

Abstract: The present disclosure provides polymer conjugates comprising a polymer and an agent, the agent linked to the polymer via a linking group containing a cleavable moiety.

Abstract: The invention relates to novel arylamide derivatives having formula (I) and stereoisomers and pharmaceutically acceptable salts thereof, where R1-R11, R?, R?, z and X are as defined in the claims. The arylamide derivatives of formula (I) have antiandrogenic properties. The invention also relates to compounds of formula (I) for use as a medicament and to pharmaceutical compositions comprising them and to their preparation.

Abstract: The invention concerns a liquid pharmaceutical formulation suitable for oral administration, comprising a suspension of an effective amount of micronized 2-(2-nitro-4-trifluoromethylbenzoyl)-1,3-cyclohexanedione (nitisinone); and citric acid buffer having a pH in the range of 2.5 to 3.5. The formulation is useful in the treatment of disorders and diseases in which inhibition of 4-hydroxyphenylpyruvate dioxygenase (HPPD) is desirable, e.g. in hereditary tyrosinaemia type I.

Abstract: Disclosed are compounds which are nuclear receptor modulators that can act as antagonists to the androgen receptor, for example, a compound of Formula I: wherein R1 to R5 and X1 to X5 are as described herein, as well as pharmaceutically acceptable salts, solvates, and stereoisomers thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment for cancers, including prostate cancers, other nuclear receptor mediated cancers, and other conditions, are also disclosed.

Abstract: A method of treating rheumatoid arthritis using a water-soluble cocrystal composition contains a quantity of acetylsalicylic acid and a quantity of a theanine enantiomer selected from an alpha variant of theanine or a beta variant of theanine or other form of theanine.

Abstract: The present invention provides methods and compositions for treating cancer metastasis by cyclohexenone compounds.

Abstract: The present invention provides the compounds of formula (I): The present invention relates to imidazo[4,5-c]quinoline derivatives of formula (I), process for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases mediated by phosphatidylinositol-3-kinase (PBK) and/or mammalian target of rapamycin (mTOR) and/or tumor necrosis factor-? (TNF-oc) and/or interleukin-6 (IL-6), particularly in the treatment of cancer and inflammation.

Abstract: The present invention identifies the cholesterol biosynthetic pathway, including the enzyme oxidosqualene cyclase, as new protein targets for anti-tumor therapeutics. The present invention further provides a class of oxidosqualene cyclase inhibitors containing a tertiary amine linked with aromatic ring structures, as a new class of anticancer agents. Compounds disclosed herein have been tested in 19 cell lines including breast cancer, prostate cancer, lung cancer (including drug-resistant lung cancer H69AR), colon cancer, ovarian cancer (including drug-resistant OVCAR-3), and pancreatic cancer cells, as wells as in human breast and prostate xenograft tumor growth in nude mice, and have been shown to be active.

Abstract: The invention provides methods for treating impulse control disorders in patients with catechol-o-methyl-transferase inhibitors. The invention also provides methods for treating patients with obsessive compulsive disorders and substance addictions with catechol-o-methyl-transferase inhibitors.

Abstract: The invention relates to methods and compositions for promoting cognitive function and/or treating cognitive function disorders and impairments. In particular the methods are accomplished by administering to a subject CI-994 or dinaline or a pharmaceutically acceptable salt, ester, prodrug or metabolite thereof.

Abstract: The present invention relates to a theanine derivative, a preparation method thereof, and a use thereof for anti-acne treatment, having a selective inhibitory effect on Propionibacterium acnes in the skin.

Abstract: Antimitotic agents comprising a modified chalcone or modified chalcone derivative are disclosed. The modified chalcone or modified chalcone derivative compounds are of the general formula CHAL-LIN-COV, wherein CHAL is a chalcone or chalcone derivative portion, LIN is an optional linker portion, and COV is a covalent bonding portion (e.g., an ?,?-unsaturated thiol ester group). The modified chalcone or modified chalcone derivative compounds provide an improved method of interference with tubulin polymerization, for example by covalent (and essentially irreversible) bonding between tubulin and the covalent bonding portion, potentially resulting in a decrease in tumor size and/or disappearance of the cancer, to the benefit of cancer patients.

Abstract: A bacterial autoinducer, CAI-1, was purified and its structure identified. Methods for synthesis of the autoinducer and its analogues were elucidated. Methods of using the autoinducer or its analogues for treating bacterial pathogenicity and bio film formation are described. Methods for prevention and treatment of cholera are described. Synthetic (S)-3-hydroxytridecan-4-one functions as well as natural CAI-1 in repressing production of the virulence factor toxin co-regulated pilus (TCP). Strategies are described to manipulate bacterial quorum sensing in the clinical arena.

Abstract: A method of treatment using a water-soluble cocrystal composition contains a quantity of acetylsalicylic acid and a quantity of a theanine enantiomer selected from an alpha variant of theanine or a beta variant of theanine or other form of theanine.

Abstract: The present disclosure relates to methods of using fatty acid amide hydrolase (FAAH) inhibitors to treat aspects of Parkinson's disease (PD), restless legs syndrome (RLS) and periodic limb movement disorder (PLMD), the use of FAAH inhibitors for the manufacture of medicaments for use in the treatment of PD, RLS and PLMD, as well as pharmaceutically acceptable compositions comprising FAAH inhibitors for use in the treatment of PD, RLS and PLMD.

Abstract: Topical compositions and methods of use to treat symptoms of reduced skin elasticity are provided comprising desthiobiotin and certain desthiobiotin analogues. These compounds are effective in stimulating LOXL-1 activity and can thus increase elastin remodeling and improve appearance of fine lines, wrinkles, skin sagging and other symptoms of reduced elastin function.

Abstract: The present invention provides methods of preventing or inhibiting tumor metastasis in a subject by administering a therapeutically effective amount of (1) a compound from a group of enumerated compounds, or a pharmaceutically acceptable salt thereof; (2) an agent that covalently modifies at least one cysteine residue of S100A4 protein; or (3) an agent that inhibits the interaction between S100A4 and myosin-IIA.

Abstract: A method is provided for the treatment of vision problems in a subject suffering from one of various forms of albinism, including, for example, oculocutaneous albinism types OCA1a and OCA1b, as well as ocular albinism type 1, resulting from mutations in the GPR143 gene, as well as the OCA2, OCA3 or OCA4 genes, by administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of the compound (242-nitro-4-(trifluoromethyl)benzoyl]cyclohexane-1,3-dione), also known as NTBC for a sufficient period of time. The administration of NTBC is believed to increase the amount of pigmentation in the subject and alleviate certain symptoms caused by lack of pigmentation in the eye tissues. Also described are methods of use of NTBC for increasing the pigmentation of a subject for cosmetic purposes, by administering to the subject a therapeutically effective amount of NTBC.

Abstract: Provided are compositions and methods for modulating quorum sensing in microbes. The compounds are AI-2 analogs and as such have structures similar to 4,5-dihydroxy-2,3-pentanedione that can act as agonists/antagonists of quorum sensing. The compounds are useful for modulating quorum sensing in bacteria and can be used in methods for prophylaxis or therapy of bacterial infections and for reduction of biofilms.

Abstract: Compounds that cause reversible night blindness may be used to treat ophthalmic conditions associated with the overproduction of waste products that accumulate during the course of the visual cycle. We describe methods and compositions using such compounds and their derivatives to treat, for example, the macular degenerations and dystrophies or to alleviate symptoms associated with such ophthalmic conditions. Such compounds and their derivatives may be used as single agent therapy or in combination with other agents or therapies.

Abstract: The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent.

Abstract: An aspirin-theanine cocrystal composition including a quantity of acetylsalicylic acid and a quantity of a theanine enantiomer combined with the quantity of acetylsalicylic acid in a mixture. The theanine enantiomer may be L-theanine, D-theanine, or DL-theanine.

Abstract: The present invention provides methods and compounds for inhibiting HEC1 activity for the treatment of diseases involving cell hyperproliferation, e.g. cancer. The present invention also provides methods of identifying compounds for inhibiting HEC1 activity.

Abstract: The present invention is directed to pest-controlling compositions comprising as active ingredients one or more ?-diones, particularly ?-diketones and ?-triketones, and to the use of these compositions inter alia for preventing, eradicating, destroying, repelling or mitigating harmful, annoying or undesired pests including insects, arachnids, helminths, molluscs, protozoa and viruses. The present invention is further directed to processes of preparing ?-diones by de novo synthesis or from natural sources such as volatile oil-bearing plants from families including Alliaceae, Apiaceae, Asteraceae, Cannabinaceae, Lamiaceae, Pteridaceae, Myrtaceae, Myoporaceae, Proteaceae, Rutaceae and Zingiberaceae.

Abstract: The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders comprising administration of novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent.

Abstract: The present invention relates generally to formulations comprising paracetamol. More particularly, the present invention provides a swallow formulation comprising paracetamol which facilitates the rapid delivery of paracetamol into the circulatory system following oral administration. The present invention further relates to methods for inducing efficient pain relief including an analgesic effect by the administration of the paracetamol formulation.

Abstract: The invention provides organonitro compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat non-Hodgkin's lymphoma and certain leukemias in a patient. The compounds, compositions, kits, and methods are contemplated to provide a therapeutic benefit in treating non-Hodgkin's lymphoma, chronic lymphocytic leukemia, acute myelogenous leukemia, chronic myelogenous leukemia, and acute lymphoblastic leukemia. Exemplary organonitro compounds described herein include alkyl-substituted and acyl-substituted di-nitroheterocycles.

Abstract: The invention concerns the combinations of an mGluR modulator, e.g. an mGluR5 modulator and at least one of L-dopa, a dopamine modulator, e.g. a dopamine agonist, a dopa decarboxylase inhibitor or a catechol-O-methyl transferase inhibitor.

Abstract: A water-soluble aspirin-theanine cocrystal composition which includes a quantity of acetylsalicylic acid and a quantity of a theanine enantiomer associated with the quantity of acetylsalicylic acid. The composition may be created by a method including the steps of: (i) providing a quantity of acetylsalicylic acid; (ii) adding a quantity of a theanine enantiomer to the quantity of acetylsalicylic acid to form a mixture comprising the quantity of acetylsalicylic acid and the enantiomer of theanine; (iii) wetting the mixture; and (iv) grinding the mixture for a length of time sufficient to produce a dried crystalline mass. The water-soluble cocrystal composition is suitable for intravenous administration, preferably to humans.

Abstract: This invention relates to a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. The ligands comprise a class of ketones.

Abstract: Provided herein are skin substitutes suitable for use in a living subject for purpose of repairing damaged tissues, methods of producing the skin substitutes and their uses. A biocomposite membrane comprising poly(?-caprolactone) (PCL) and at least one material selected from collagen and gelatin is provided. In one embodiment, the biocomposite is a 2-component membrane of PCL and gelatin. In another embodiment, the biocomposite is a 3-component membrane of PCL, collagen and gelatin. The bio-composite membrane may be used directly in vivo as a wound dressing, or as a support for cell growth on each side of the membrane to produce an in vitro cultivated artificial skin for future in vivo and/or in vitro applications.

Abstract: The invention provides methods for treating disorders in patients with catechol-o-methyl-transferase inhibitors, such as impulse control disorders and cognitive disorders, such as attention deficit hyperactivity disorder. The invention also provides methods for treating patients with obsessive compulsive disorders and substance addictions with catechol-o-methyl-transferase inhibitors.

Abstract: The invention provides methods for treating impulse control disorders in patients with catechol-o-methyl-transferase inhibitors. The invention also provides methods for treating patients with obsessive compulsive disorders and substance addictions with catechol-o-methyl-transferase inhibitors.

Abstract: Compounds of the general formula (I) or its salt or a compound in which one or more atoms are replaced by their stable, nonradio-active isotopes, in particular its pharmaceutically acceptable salt; in which X is —CH2—; R is a mono- to tetra-substituted, mono- or bicyclic, unsaturated heterocyclic radical having 1 to 4 nitrogen atoms, R2 is C1-6alkyl or C3-6cycloalkyl; R3 is independently of one another H, C1-6alkyl, C1-6alkoxycarbonyl or C1-6alkanoyl; R4 is C2-6alkenyl, C1-6alkyl, unsubstituted or substituted aryl-C1-6alkyl or C3-8cycloalkyl; R5 is -Lm-R6; L is C1-6alkylene which is optionally substituted by 1-4 halogen, or a linker: formula (II) n=0, 1 or 2; m=0 or 1; R6 is a radical composed of 2 cyclic systems selected from bicyclo[x.y.z]alkyl, spiro[o.p]alkyl, mono- or bioxabicyclo[x.y.z]alkyl or mono- or bioxaspiro[o.

Abstract: The present invention provides 4-substituted-2-azetidinone compounds, bicyclic 2-5-diketopiperazine compounds, and pharmaceutical compositions thereof that are potent, safe and effective neuroprotective agents. Due to their strong central nervous system (CNS) activity, the compounds can be used to enhance memory and to treat a variety of neurological disorders. The compounds are particularly useful for treating neurological disorders caused by, or associated with, CNS trauma.

Abstract: A pharmaceutical composition comprises (a) a CETP inhibiting compound, or a pharmaceutically acceptable salt thereof; (b) a concentration-enhancing polymer, and (c) optionally one or more surfactants; wherein the compound has the structure shown as Formula I below. The composition raises HDL-cholesterol and lowers LDL-cholesterol.

Abstract: This invention relates, inter alia, to detecting and/or measuring succinylacetone and one or more additional biological analytes using mass spectrometry.

Abstract: A composition comprising a compound of formula (I) CH3CH(OH)C(?O)NR1R2 where R1 and R2 are each independently hydrogen; or C1-6 alkyl, C2-6 alkenyl or C3-6 cycloalkyl, each of which is optionally substituted by up to three substituents independently selected from phenyl, hydroxy, C1-5 alkoxy, morpholinyl and NR3R4 where R3 and R4 are each independently C1-3 alkyl; or phenyl optionally substituted by up to three substituents independently selected from C1-3 alkyl; or R1 and R2 together with the nitrogen atom to which they are attached form a morpholinyl, pyrrolidinyl, piperidinyl or azepanyl ring, each of which is optionally substituted by up to three substituents independently selected from C1-3 alkyl; and at least one biologically active compound, which comprises at least one aromatic five and/or six membered ring wherein the ring contains at least one nitrogen as a ring member, with the provisos (i) that the composition does not contain cyproconazole when the compound of formula (1) is selected from the gro

Abstract: The invention provides novel compounds according to formula I relates to compounds with the general formula I said compounds being useful, e.g. in the treatment of inflammatory, ophthalmic diseases or cancer.

Abstract: Methods for concomitant administration of colchicine together with one or more macrolide antibiotics, e.g., clarithromycin, are disclosed. Such methods reduce the dangers commonly associated with such concomitant administration and provide additional benefits.

Abstract: The invention relates to novel compounds of the formula (I) in which X, Y, Z, A, B and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, the phenyl-substituted bicyclooctane-1,3-dione derivates 33 and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to increasing the activity of crop protection compositions comprising in particular phenyl-substituted bicyclooctane-1,3-dione derivates by adding ammonium salts or phosphonium salts and, if appropriate, penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as insecticides and/or acaricides and/or for preventing unwanted plant growth.

Abstract: The present invention is based on the discovery that the administration of at least one immunoconjugate and at least one chemotherapeutic agent provides an unexpectedly superior treatment for cancer. The present invention is directed to compositions comprising at least one immunoconjugate and at least one chemotherapeutic agent and to methods of treating cancer using at least one immunoconjugate and at least one chemotherapeutic agent. The present invention also provides methods of modulating the growth of selected cell populations, such as cancer cells, by administering a therapeutically effective amount of at least one chemotherapeutic agent and at least one immunoconjugate.