Abstract: The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumour, which comprises the administration of ZD6474 in combination with androgen ablation; to a pharmaceutical composition comprising ZD6474 and an antiandrogen; to a combination product comprising ZD6474 and an antiandrogen for use in a method of treatment of a human or animal body by therapy; to a kit comprising ZD6474 and an antiandrogen; to the use of ZD6474 and an antiandrogen in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation.

Abstract: The present invention is directed to polyphosphorylated and pyrophosphate derivatives of cyclitols. More particularly, the invention relates to polyphosphorylated and pyrophosphate derivatives of inositols. The invention also relates to compositions of the polyphosphorylated and pyrophosphate derivatives of inositol and other similar, more lipophilic derivatives, and their use as allosteric effectors, cell-signaling molecule analogs, and therapeutic agents.

Abstract: Methods of treating various autoimmune diseases, such as multiple sclerosis, peripheral neuritis, optical neuritis, amylotrophic lateral sclerosis, and uveitis utilizing specific amino alcohol derivatives are provided herein.

Abstract: Methods and compositions are provided for modulating myocyte BK channel activity and for screening for modulators of BK channel activity. The methods and compositions are useful in the treatment of disorders where increasing myocyte BK channel activity can attenuate, revert or prevent the disorder. For example, the methods and compositions are useful for treating disorders ameliorated by increasing vasodilation and blood flow in a subject, in particular, increasing cerebral blood flow.

Abstract: The present invention relates to progesterone receptor antagonists of general formula I: in which R1 can be a hydrogen atom and R2 a hydroxyl group or R1 and R2 together can be an oxo group.

Abstract: Selective estrogen receptor modulators, as well their related pharmaceutical compositions and methods of use, are provided herein. These estrogen receptor modulators include compounds that primarily exhibit estrogen receptor antagonist activity or primarily exhibit selective estrogen receptor antagonist and agonist activity, i.e., SERM activity, in specific tissue types. Particular embodiments provide compounds that behave as NeuroSERMs promoting neurotrophism and neuroprotection in brain tissue. These NeuroSERMs represent a subset of the modulators compounds provided herein that can cross the blood-brain-barrier and exert estrogen receptor agonist-like effects in the brain. The compounds should be useful for treating a variety of diseases, particularly estrogen receptor-mediated diseases and disorders, such as osteoporosis, breast and endometrial cancers, atherosclerosis and Alzheimer's disease.

Abstract: Compositions for treating, reducing, ameliorating, or preventing infection of an ear or upper respiratory tract comprise a fluroquinolone having Formula I, II, or III. Methods for treating, reducing, ameliorating, or preventing such infection use such compositions. Such compositions and methods can be effective against certain antibiotic-resistant microbial pathogens found in such infection.

Abstract: The present invention relates to the use of zinc complexes of natural amino acids, especially L-arginine, L-lysine, L-ornithine, and other natural amino acids, in a molar ratio of about 1:2 (metal:amino acid), and formulations thereof. These pharmaceutical compositions offer better tolerated and faster acting regimens than common zinc salts (i.e., acetate, sulfate, etc.) for long term maintenance therapy of diseases caused by abnormal elevated copper levels, such as in Wilson's disease, inflammatory and fibrotic diseases and Alzheimer's disease.

Abstract: Disclosed are urea compounds of formula I, stereoisomer, or pharmaceutical acceptable salts thereof, and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, pulmonary, and diabetic-related diseases.

Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula 1.

Abstract: The present invention provides compounds represented by the structural formula (I): or pharmaceutically acceptable isomers, salts, solvates or esters of the compound of Formula (I), wherein each of the substituents is as specified herein, formulations including the above compounds, processes for preparing the same and methods for treating atherosclerosis, hypercholesterolemia, or sitosterolemia, and for lowering plasma levels of sterols and/or stanols.

Abstract: Administration of ?-Lactam compounds, including ?-lactam antibiotics and ?-lactamase inhibitors provides significant neurotropic effects in warm-blooded vertebrates evidence inter alia by anxiolytic and anti-aggressive behavior modification and enhanced cognition. Therapeutic methods for using such compounds and their pharmaceutical formulations are described.

Abstract: The present invention relates to certain new pyridin analogues of Formula (I) to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-trombotic agents etc, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.

Abstract: Treprostinil can be administered using a metered dose inhaler. Such administration provides a greater degree of autonomy to patients. Also disclosed are kits that include a metered dose inhaler containing a pharmaceutical formulation containing treprostinil.

Abstract: Use of ivabradine, or 3-{3-[{[(7S)-3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]-methyl}-(methyl)-amino]-propyl}-7,8-dimethoxy-1,3,4,5-tetrahydro-2H-3-benzazepin-2-one, its addition salts with a pharmaceutically acceptable acid and their hydrates, for obtaining a medicament intended for the treatment of endothelial dysfunction.

Abstract: Compounds of the formula (I), in which W, R, R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.

Abstract: Film-form, single-layered, cavity-free preparation free of surfactants, effervescent additive and taste masker and comprising one or more film former(s), one or more gel former(s) and one or more active ingredient(s) from the group of neuroleptics.

Abstract: The present invention is directed to a method of simultaneously treating hypertension, hypertriglyceridemia, a pro-inflammatory state, a pro-coagulative state, and insulin resistance (with or without treating obesity or endothelial dysfunction), associated with or independent from Metabolic Syndrome, as well as vascular disease such as cardiovascular, cerebrovascular, or peripheral vascular disease comprising the step of administering to a patient suffering from such disorders a therapeutically effective amount of a central acting dopamine agonist. In one embodiment, the central acting dopamine agonist is bromocriptine, optionally combined with a pharmaceutically acceptable carrier.

Abstract: Carbon-linked tetrahydro-pyrazolo-pyridine compounds are described, which are useful as cathepsin S modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by cathepsin S activity, such as psoriasis, pain, multiple sclerosis, atherosclerosis, and rheumatoid arthritis.

Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.

Abstract: The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.

Abstract: The present invention relates to 1,2,3 -thiadiazole compounds represented by formula (I): wherein R1, R2, R3, R4 and R5 each represents H, halogen, CN, alkyl, alkoxyalkyl, aryl, arylalkyl, alkylcarbonyl or the like; R6 represents —C?(W1)YR7 in which R7 reresents H, alkyl, alkenyl, phenylcarbonyl, heterocyclic ring-carbonyl, arylsulfonyl or the like; Y represents O, S, —N(R11), —N(R11)O— in which R11 represents H, alkyl, cycloalkyl, substituted phenyl, or the like; W1 represents O or S; and symbols in the formula are defined in detail in the specification or salts thereof, and to a plant disease control agent for agricultural and horticultural use which contains the compound as an active ingredient.

Abstract: This invention relates to methods of treating, managing and preventing body composition disorders, and to compounds and pharmaceutical compositions useful in such methods.

Abstract: The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the general Formula I: including all prodrugs, pharmaceutically acceptable salts and stereoisomers, R1, R2, R3, n, and Z are described herein.

Abstract: Compounds of formula (I): wherein: when X is NR5, Y is absent or is CH2; when X is CH2, Y is absent, CH2, NR6, O, S, S(O) or S(O)2; Z is a 5- or 6-membered heterocyclyl ring; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).

Abstract: The present invention provides compounds of formula I: along with methods of use thereof for the control of agricultural pests, particularly fungal pests, weedy pests and insect pests, as well as use as pharmaceuticals, particularly the treatment of obesity, metabolic syndrome, atherosclerosis, cardiovascular disease and insulin resistance, e.g.

Abstract: Disclosed are new substituted pyrazole and triazole compounds of Formula (I) and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses thereof:

Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.

Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: The present invention is related to methods of treating viral and protozoan infections in mammals using antipathogenic benzamide compounds having the formula wherein at least one of the R1 groups is F, Cl, CN or CF3 and R2, R3, Y, Z, m, and n are as defined herein.

Abstract: Compounds of formula (I) in free or pharmaceutically acceptable salt form, where R1, R2, R3, R4, R5, R6, R7, m, n, w, X, and Y have the meanings as indicated in the specification, are useful for treating conditions mediated by the CRTh2 receptor, especially inflammatory or obstructive airways diseases.

Abstract: Disclosed are alpha keto amide and alpha hydroxy amide compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, pulmonary, and diabetic-related diseases.

Abstract: Therapeutically active heteroaryl carboxylic acid derivatives of Formula (I) wherein R1, R2, W, X, Y and Z are as defined in the specification, processes for the preparation of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, particularly in the treatment of diseases in which under-activation of the HM74A receptor contributes to the disease or in which activation of the receptor will be beneficial, are disclosed.

Abstract: Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X=NRX then n is 1 or 2 and if X=CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.

Abstract: The present invention relates to certain derivatives of cycloalkanediones invariably substituted with a chroman-2-yl, 2-quinolyl or —O-phenyl residue which are serotonin (5-hydroxytryptamine, 5-HT) 5-HT1A receptor subtype agonists modulators, to their stereochemical isomers and to their use in the preparation of a medicament for the treatment of pathological states for which an agonist a modulator of these receptors is indicated.

Abstract: The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein R1—R4 A, B, D, E, and G are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.

Abstract: A compound of formula: wherein X is S or O and A, R1, R2, R3, R4, n, and m are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Pyridazinylpiperazine Compound”), compositions comprising a Pyridazinylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD and IBS in an animal comprising administering to an animal in need thereof an effective amount of a Pyridazinylpiperazine Compound are disclosed herein.

Abstract: The present invention relates to novel imidazo[1,2-a]pyridine compounds of general formula (I): as well as pharmaceutically acceptable salts thereof; wherein R1, R2, R3 and R4 are as defined in the claims. The compounds have specific affinity for GABAA receptor and are therefore useful in the treatment and prevention of diseases modulated by ?1- and ?2-GABAA receptors.

Abstract: Disclosed herein are novel salts of flunarizine with improved properties. Also described herein are novel pharmaceutical compositions comprising such flunarizine salts, methods of making, and related methods of treatment.

Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: (I) wherein A1, A2, A3, A4, A5, A6, A7, A8, X4, X6, R2a, Rx, R4, R5, and R6 are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.

Abstract: The present invention features a composition including (i) a retinoid, and (ii) an interleukin-8 inhibitor. The composition provides reduced irritation to human skin.

Abstract: This invention comprises antineoplastic curcumin derivatives and methods of preparation and use thereof. Particular reference is made to the following isomeric compounds wherein R1, R2, and R3 are selected from the group consisting of H, OH, OCH3, and COOH.

Abstract: The invention relates to new salts of ocaperidone and uses thereof, particularly in the pharmaceutical industry. The invention discloses specific salts of ocaperidone having increased water solubilities, as well as therapeutic methods by administering said salts, in particular for treating various diseases of the central or peripheral nervous system, especially central nervous system. It further deals with pharmaceutical compositions comprising said salts and methods for preparing the same.

Abstract: 6-Phenyltriazolopyrimidinylamines of the formula I, in which the substituents are defined according to the description, processes for preparing these compounds, compositions comprising them and their use for controlling phytopathogenic harmful fungi.

Abstract: Myocardial infarction in a mammal is treated by administering to the mammal a therapeutically effective amount of a chemical Src family tyrosine kinase protein inhibitor and the use of such inhibitor compounds for the preparation of a medicament for treating myocardial infarction. Myocardial infarction can be prevented by administering to the mammal a prophylactic amount of the inhibitor. The inhibitor preferably is an inhibitor of Src protein selected from the group consisting of a pyrazolopyrimidine class Src family tyrosine kinase inhibitor, a macrocyclic dienone class Src family tyrosine kinase inhibitor, a pyrido[2,3-d]pyrimidine class Src family tyrosine kinase inhibitor, a 4-anilino-3-quinolinecarbonitrile class Src family tyrosine kinase inhibitor, and a mixture thereof. The Src family tyrosine kinase inhibitors can be used to prepare medicaments for the treatment of myocardial infarction. Also disclosed are articles of manufacture containing a chemical Src family tyrosine kinase inhibitor.

Abstract: (EN) The invention relates to the use of a partially neutralized, anionic (meth)acrylate copolymer comprising radically polymerized units of 25 to 95 percent by weight of C1 to C4 alkyl esters of acrylic or methacrylic acid and 5 to 75 percent by weight of (meth)acrylate monomers with an anionic group, at least 4 percent of which are neutralized by means of a base, for producing a medicament that is provided with an active substance-containing core and is coated with the partially neutralized, anionic (meth)acrylate copolymer. Said medicament releases at least 30 percent of the active substance contained therein in 30 minutes at a pH at which the active substance is sufficiently soluble and stable and at which the corresponding medicament that is coated with the non-neutralized anionic (meth)acrylate polymer releases less than 10 percent of the active substance contained therein.

Abstract: Compounds of formula I in free or salt form, wherein R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine A2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.

Abstract: The present invention relates to pharmaceutical compositions comprising at least one multifunctional phosphodiesterase inhibitor (MPDEI) and at least one adenosine uptake inhibitor. The present invention also relates to compositions comprising cilostazol and dipyridamole and their use.

Abstract: Disclosed are protein kinase inhibitors, compositions comprising such inhibitors, and methods of use, thereof. More particularly, disclosed are inhibitors of Aurora-2 (Aurora-A) protein kinase. Also disclosed are methods of treating diseases associated with protein kinases, especially diseases associated with Aurora-2, such as cancer.