Abstract: The present invention provides compositions of matter, kits and methods for their use in the treatment of cancer. In particular, the invention provides compositions and methods for treating cancer in a subject by inhibiting a poly-ADP-ribose polymerase, as well as providing formulations and modes of administering such compositions.

Abstract: In one aspect, the present invention provides a composition and a kit comprising a combination of topoisomerase inhibitor and PARP inhibitor for treatment of cancer. In another aspect, the invention provides a method of treating cancer comprising administering to a subject a combination of topoisomerase inhibitor and PARP inhibitor. In particular, the invention provides compositions and methods for treating cancer in a subject by inhibiting a poly-ADP-ribose polymerase and a topoisomerase, as well as providing formulations and modes of administering such compositions.

Abstract: The present invention relates to coumarins of the formula (I): that are useful as inhibitors of nitric oxide synthase. Pharmaceutical compositions and methods of using these compounds as inhibitors of nitric oxide synthase are described herein.

Abstract: The present invention is directed to therapeutic compositions targeting the NCCa-ATP channel of an astrocyte, neuron or capillary endothelial cell and methods of using same. More specifically, agonists and antagonists of the NCCa-ATP channel are contemplated. The therapeutic compositions are used to treat cancer, more specifically, a metastatic brain tumor, wherein a tumor-brain barrier is present. Such treatments are contemplated in combination with conventional anti-cancer therapies. Alternatively, the compositions are used to prevent cell death and to treat cerebral edema that result from ischemia, due to interruption of blood flow, to tissue trauma or to increased tissue pressure.

Abstract: Novel mercaptan compounds, particularly those including a photolabile protecting group, are described as well as methods of using the compounds for the prevention and treatment of ocular damage and disease.

Abstract: Fungicidal mixtures comprising, as active components 1) the strobilurin derivative of the formula I, and 2) at least one active compound II selected from the group of heterocyclic compounds in a synergistically effective amount, methods for controlling harmful fungi using mixtures of the compound I with active compounds II, the use of the compound I with active compounds II for preparing such mixtures and compositions comprising these mixtures.

Abstract: This invention provides a method of detecting enzyme activity on a solid medium. The enzyme substrate has a chromogenic portion comprising a catechol residue, in which a derivitising moiety is linked to the aromatic ring of the catechol via a bond, and an enzyme cleavable group which is attached via an ester or ether linkage to the oxygen atom derived from a hydroxyl group of the catechol residue. If the enzyme substrate contacts an enzyme capable of cleaving the enzyme cleavable groups and the cleaved compound contacts a chelatable metal ion, a substantially non-diffusable coloured precipitate is formed.

Abstract: The invention provides chroman compounds having formula 1 wherein R1 is (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl, and independently R1 has a cis-orientation in relation to the exocyclic phenyl group at the 2-position of the skeleton; R4 is H, Hal, CF3, OH or (1C-2C)alkyloxy; R2, R3, and R5are independently H, Hal, CF3, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl and prodrugs thereof for the manufacture of a medicine for estrogen-receptor related treatments.

Abstract: A suppressor of the expression of MCP-1 is provided that is excellent in safety and is widely applicable to, for example, foods. The suppressor of the expression of MCP-1 according to the present invention is characterized by containing auraptene. Auraptene is contained in citrus fruits such as Hassaku, Amanatsu, Natsumikan, and grapefruit. Since these citrus fruits have been eaten for a long time, the present invention has no problem in safety. Furthermore, even when added to, for example, foods, auraptene does not impair the flavor thereof because it is substantially tasteless and odorless. Since auraptene has a low calorific value, for example, an obese person or a diabetic patient can ingest it over a long period of time. Auraptene suppresses the expression of MCP-1 at a genetic level (see FIG. 1) and a protein level.

Abstract: The present invention provides compounds having formula (1): wherein R1-R6, A, J, D, E, G, Q, w, x, y, and z are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof in the treatment of cancer and/or inflammatory disorders, and more generally as proteasome inhibitors.

Abstract: Novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups are disclosed. The novel compounds are used as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species and/or excess Zn ions, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds have not only low toxicity but also similar or superior LPO inhibition activity to references. They also effectively inhibit the cerebral neuronal cell death by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.

Abstract: The subject invention provides anticoagulant compounds of formula I: and pharmaceutically acceptable salts thereof, wherein R1, R3, n and Ar are as defined herein. The compounds of the subject invention can be used to treat at-risk populations thereby bringing relief of symptoms, improving the quality of life, preventing acute and long-term complications, reducing mortality and treating accompanying disorders. The invention further comprises pharmaceutical compositions comprising the compounds and salts of the invention, as well as methods of using the compounds, salts, and compositions of the invention.

Abstract: The invention relates to a method of modulating poly(ADP-ribose)polymerase-1 (PARP-1) activity in a mammal comprising administering to a mammal an effective amount of an organic aromatic compound having from 4 to about 35 carbon atoms, wherein said organic aromatic compound is capable of binding the arginine-34 moiety located in Zinc finger-1 of the PARP-1 enzyme and wherein said organic aromatic compound has electron donating capabilities such that it's ?-electron system will interact with the positively charged (cationic) guanidinium moiety of the specific arginine-34 residue of the Zinc-1 finger of PARP-1 and does not contain benzamide or lactam substituents. In particular, substituted benzopyrones and substituted indoles and their pharmaceutical compositions containing such compounds that modulate the activity of PARP-1, are described.

Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.

Abstract: The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen receptor modulator, wherein formula I is: and wherein R1-R5 and Q1 are defined as described herein. Methods of providing hormone replacement therapy and for treating carcinomas, dysfunctional bleeding, uterine leiomyomata, endometriosis, and polycystic ovary syndrome is provided which includes delivering a compound of formula I and a selective estrogen receptor modulator are also described.

Abstract: The present invention easily and efficiently provides a peroxisome proliferator-activated receptor ligand, and a composition for amelioration of insulin resistance or for prevention and/or amelioration of the insulin resistance syndrome containing the same, as an active ingredient. The present invention relates to a peroxisome proliferator-activated receptor ligand which comprises a prenylflavonoid, a chalcone derivative exclusive of prenylflavonoids, a flavonol derivative exclusive of prenylflavonoids, and a salt, a glycoside and/or an esterified substance thereof acceptable as a pharmaceutical preparation or a food or a beverage; a composition containing the above ligand; a plant-derived extract containing the above ligand; and a process for producing the above extract.

Abstract: Compounds of the formula where the variables are as defined in the specification, are useful for preventing or treating emphysema and related pulmonary conditions of mammals and other diseases and conditions which are responsive to RAR? agonist retinoids, such as skin related diseases, including but not limited to acne and psoriasis.

Abstract: This invention is related to novel aminoalkyl- and amidoalkyl-benzopyran derivatives of the following general formula (I) wherein: the group ?is a substituent in position 6 or 7 wherein: R is an aromatic mono- or bi-cyclic carbocyclic ring or a mono- or bi-cyclic heterocyclic ring radical, said rings being optionally substituted by one or two substituents selected from (C1-C5) straight or branched alkyl, (C1-C5) straight or branched alkoxy, hydroxy, halogen and trifluoromethyl; m is zero or an integer from 1 to 3; n, p, R1 and R2 are as herein indicated and R3 and R4 are both hydrogen or taken together represent an oxygen atom, and the pharmaceutically acceptable salts thereof. The compounds that are active as selective and reversible MAO-B inhibitors in vitro and in vivo, are useful as medicaments for the prevention and the treatment of CNS degenerative disorders.

Abstract: The present invention provides compositions of matter, kits and methods for their use in the treatment of cancer. In particular, the invention provides compositions and methods for treating cancer in a subject by inhibiting a poly-ADP-ribose polymerase, as well as providing formulations and modes of administering such compositions.

Abstract: The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one heterocyclic nitric oxide donor group, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension and (n) treating ophthalmic disorders. The cardiovascular compounds are preferably ?-adrenergic antagonists, angiotensin-converting enzyme (ACE) inhibitors, anti-hyperlipidemic compounds, and antithrombotic and vasodilator compounds.

Abstract: The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.

Abstract: Method and systems of treating a patient with at least one of a myocardial infarction, a stroke, and a pulmonary embolism include providing a stimulator coupled to at least one electrode and a catheter, configuring one or more stimulation parameters to treat at least one of a myocardial infarction, a stroke, and a pulmonary embolism, programming the stimulator with the one or more stimulation parameters, delivering with the stimulator via the catheter at least one drug to at least one tissue in accordance with the one or more stimulation parameters, and limiting perfusion of the at least one tissue by delivering electrical stimulation with the stimulator via the at least one electrode to the at least one tissue.

Abstract: The present invention relates to methods of screening for modulators of interleukin 32 (IL-32), to modulators of IL-32 and to their use. Proteinase 3 has been identified as an IL-32 binding protein capable of deavege thereof. Inhibition of PR 3 activity to process IL-32 or neutralization of IL-32 by-inactive PR3 or its fragments may reduce the consequences of IL-32 in immune regulated diseases (e.g. inflammatory diseases).

Abstract: The use of resveratrol, a derivative, metabolite or analogue thereof, in combination with at least one additional component selected from EGCG, coenzyme Q-IO, genistein, lycopene, hydroxytyrosol and polyunsaturated fatty acids in the manufacture of a nutraceutical composition for delaying aging and/or for the treatment or prevention of age-related diseases in animals, in particular in mammals including humans.

Abstract: The present invention relates to the albumin-guided development of coumarin analogs and the analogs developed thereby. The coumarin analogs of the present invention are identified and isolated by the fact that they have binding sites to albumin which are different than the binding sites of conventional coumarin analogs such as sodium warfarin, and as a result will be less prone to be displaced since the binding site of sodium warfarin is shared by numerous drugs such as aspirin. The coumarin analogs of the invention are advantageous because they can achieve the effects of the prior coumarin analogs with a minimum of metabolic complications and undesirable side effects.

Abstract: The invention relates to the synthesis and complete stereochemical assignments of cytotoxic compounds such as compound 28-a and its stereoisomers: The invention further provides processes for making the compounds, their synthetic intermediates, and for methods of using the compounds and their pharmaceutical compositions for the treatment of neoplastic diseases.

Abstract: Accurate means of dosing with a compressed, segmented pharmaceutical tablet, and tablettes formed from said tablets, is disclosed.

Abstract: Truncated thyroid hormone receptors ?TR?1 and ?TR?2 have been discovered to play a role in actin-based endocytosis, e.g., in the nervous system. The invention relates to methods of discovering ligands effective in modulating endocytosis and transgenic mice with altered expression of ?TR?1 and ?TR?2. The invention is useful for the discovery and testing of compounds for treating disorders of the nervous system such as depression.

Abstract: The present invention relates to methods, compositions and their constituents for inhibiting 5-Lipoxygenase (5-LO), 15-Lipoxygenase (15-LO), cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), in living organisms. More particularly, the present invention relates to methods and compositions involving the inhibition of 5-Lipoxygenase (5-LO), 15-Lipoxygenase (15-LO), cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), using processed Morinda citrifolia L. plant products.

Abstract: Certain embodiments in the present invention provide for methods for therapy of lung diseases and other conditions such as infection are provided. In certain embodiments, the methods comprise one or more agents capable of increasing thiol-containing compound transport via a transporter system (i.e., ABC transporters such as MDR-1 or MRP-2) in cells. Other embodiments can include the use of agents to modulate transport of thiol-containing compounds from the cell such as thiocyanate. In certain embodiments, therapeutic methods involve the administration of such agents to a patient afflicted with an inflammatory condition or infection responsive to stimulation of thiol-containing compound transport.

Abstract: This invention is drawn to compounds which are more easily metabolized by the metabolic drug detoxification systems. Particularly, warfarin analogs which have been designed to include esters within the structure of the compounds are taught. The invention teaches methods of reducing the toxicity of drugs comprising the introduction of ester groups into drugs during the synthesis of the drug. This invention is also drawn to methods of treating coagulation disorders comprising the administration of compounds which have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester containing warfarin, analogs are also taught.

Abstract: Compounds of formula I: wherein a, b, c, X, R2, R3, R4, R6 and R7 are defined herein, are useful as inhibitors of HIV replication.

Abstract: The present invention relates to compounds useful for detecting the activity of monoamine oxidases, compounds useful for competitively inhibiting monoamine oxidases, for determining inhibitors of monoamine oxidases and compounds useful for treating monoamine oxidase-related nervous system pathologies, as well as pharmaceutical compositions and methods of manufacture thereof.

Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.

Abstract: A topical composition and method for the reduction of scar tissue and/or improving the appearance of scar tissue after it has formed. The topical composition includes one or more flavonoids formulated in a pharmaceutically acceptable topical carrier. The method includes the step of topically applying a composition including one or more flavonoids formulated in a pharmaceutically acceptable topical carrier to scar tissue to reduce the amount of, or improve the appearance of the scar tissue. The topical compositions and methods of the present invention reduce scar tissue after it has formed as well as improving the appearance of the remaining scar tissue.

Abstract: Novel benzopyran analogs are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions containing one or more of the compounds of the present invention.

Abstract: Certain bis-(coumarin) compounds as well as the products of their intramolecular cyclization including pharmaceutically acceptable salts, hydrates, solvates, clathrates, prodrugs, tautomers and stereoisomers thereof are disclosed. Certain processes and intermediates for the preparation of certain bis-(coumarin) compounds, as well as for the use of these compounds as therapeutically active agents in the prophylaxis and treatment of asthma and other inflammatory diseases and conditions in mammals, especially humans are also disclosed.

Abstract: A process for treating a biological organism, comprising the steps in which a cell cycle arresting drug is administered to the organism to produce synchronized cells, the microtubules within the synchronized cells are stabilized by means of a microtubule stabilizing agent, and the synchronized cells with the stabilized microtubules are then contacted with mechanical vibrational energy.

Abstract: There are provided a novel compound having irreversible inhibitory activity against neuraminidase, a therapeutic agent and a detection agent for a disease involving neuraminidase. A compound represented by the following formula (I) and a salt thereof, a production method thereof, and an application method thereof, wherein: A1 represents an aryl group optionally having a substituent group or a heteroaryl group optionally having a substituent group; A2 represents —CX2R6 or —CHXR6 wherein X represents —F, —Cl, —Br, or —I; R1 represents a hydrogen atom or an alkyl group optionally having a substituent group; R2, R3, R4, and R5 represent each independently —OC(?O)R6, —OR6, —N(R6)2, —N3, —NHC(?NH)NHR6, —NHCOR6, —OSO3R6, —OPO3(R6)2, F, Cl, Br, or I; and R6 represents each independently a hydrogen atom, an alkyl group optionally having a substituent group, an aryl group optionally having a substituent group, or an optionally substituted heteroaryl group.

Abstract: The present invention relates to a noble 6-alkylamino-2-methyl-2?-(N-methyl substituted sulfonamido)methyl-2H-1-benzopyran derivative, a method for preparing the same with high efficiency using a parallel synthetic method, one of combinatorial chemical synthetic techniques, and a use of the novel compound showing a high inhibitory effect to 5-lipoxygenase (5-LO) activity for preventing and treating leukotriene (LTA4, B4, C4, D4) activation-related diseases such as inflammatory diseases, rheumatoid arthritis, colitis, asthma and psoriasis.

Abstract: The present invention relates to a chalcone compound represented by the following general formula: wherein R1 and R2 are taken together with the carbon atom to which they are bound, respectively, to form a hydroxydimethyl hexane ring, or where R1 is a hydroxyl group, R2 is an isohexenyl group, a derivative thereof, or a salt thereof. Also, the present invention relates to a therapeutic agent or prophylactic agent for a disease requiring neuronal protection, suppression for nitrogen monoxide (NO) production, inhibition for aldose reductase or suppression for interleukin production, and a food, beverage or feed for treatment or prevention of the above-mentioned disease, characterized in that each comprises the above-mentioned compound as an effective ingredient.

Abstract: A liver function protecting or improving agent which comprises a compound represented by the formula (I) {in the formula (I), R1, R2, R3, R4, R5, R6, R7, R8 and R9 may be the same or different, and represent hydrogen, halogen, hydroxy, alkoxy or alkyl; and RA represents the formula (II) [in the formula (II), R10 and R11 may be the same or different, and represent hydrogen or halogen, or R10 and R11 together represent a binding] or the formula (III) [in the formula (III), R12 represents hydrogen, halogen, hydroxy, alkoxy, cyano or alkyl, R13 and R14 may be the same or different, and represent hydrogen or halogen, or R13 and R14 together represent a binding]} or a glycoside thereof or a pharmaceutically acceptable salt thereof.

Abstract: Compounds useful as chemotherapeutic, chemopreventive, and antiangiogenic agents are provided. The compounds are flavanoids, including flavanones, flavanols, and chalcones. The compounds have the structure of formula (I) wherein R1 through R3 and R5 through R11 are defined herein, and ?, ?, and ? are optional bonds, providing that when ? is absent, ? is present, and when ? is absent, ? is present. When ? is present, preferred R4 moieties are selected from O, S, NH and CH2, and when ? is absent, preferred R4 groups are selected from OH, SH, NH2 and CH3. When ? is present, the preferred R5 substituent is O, while when ? is absent, the preferred R5 substituent is OH. Pharmaceutical compositions are provided as well, as are methods of synthesis and use.

Abstract: The present invention is directed to methods of treating or preventing the development of cardiovascular disease by administering compounds that stabilize mast cells. In addition, it includes pharmaceutical compositions which have both a mast cell stabilizer and instructions regarding the use of the stabilizer in treating or preventing cardiovascular disease. The methods and compositions will be of particular value for preventing aneurysms of the abdominal aorta in individuals with atherosclerosis, diabetes, hypertension or a family history of aneurysms.

Abstract: A method for accelerating the process of removing ethanol from the blood through the use of certain additives that accelerate the metabolic oxidation of ethanol, and others which in addition act as catalysts or “pseudo” enzymes for the oxidation. These additives include multivalent transition metal ions, as well as complexes thereof, and NAD+ which enhance the oxidation reaction. The method described can act as a sobriety inducer and/or as an effective palliative for the unpleasant effects of overuse of ethanol.

Abstract: This invention relates to compositions, and methods of use thereof, for treating conditions associated with elevated arginase levels and/or activity comprising administering to a subject in need thereof, certain polyphenols such as flavanols, procyanidins, or pharmaceutically acceptable salts or derivatives thereof.

Abstract: There is disclosed a composition comprising at least one of a compound selected from the group consisting of a bioflavonoid, a beta-1,3-beta-1,4-polymer of glucose having a weight average molecular weight (MW) of not greater than 1000 kDa, and a sterol. Moreover, there is disclosed a food or beverage or health supplement product comprising the disclosed composition. Further, there is disclosed a method of lowering blood serum cholesterol levels comprising administering to a patient in need thereof an effective amount of the disclosed composition.

Abstract: The invention provides self-preserving compositions and methods for their production.

Abstract: The subject invention provides anticoagulant compounds of formula I: and pharmaceutically acceptable salts thereof, wherein R1, R3, n and Ar are as defined herein. The compounds of the subject invention can be used to treat at-risk populations thereby bringing relief of symptoms, improving the quality of life, preventing acute and long-term complications, reducing mortality and treating accompanying disorders. The invention further comprises pharmaceutical compositions comprising the compounds and salts of the invention, as well as methods of using the compounds, salts, and compositions of the invention.

Abstract: Disclosed are methods for a treating a disease or condition relating to blood coagulation and fibrinolysis using p38 MAP kinase inhibitors.