Abstract: The present invention relates to heteroarylylmethyl sulfonamides of formula I wherein B, E, Ra, n, R, A, Y and Cy are as defined in the claims, to the N-oxides, and salts thereof and their use for combating harmful fungi, and also to compositions and seed comprising at least one such compound. The invention also relates to a process and intermediates for preparing these compounds.

Abstract: The present invention provides methods and compositions for modulating levels of amyloid-? peptide (A?) exhibited by cells or tissues. The invention also provides pharmaceutical compositions and methods of screening for compounds that modulate A? levels. The invention also provides modulation of A? levels via selective modulation (e.g., inhibition) of ATP-dependent ?-secretase activity. The invention also provides methods of preventing, treating or ameliorating the symptoms of a disorder, including but not limited to an A?-related disorder, by administering a modulator of ?-secretase, including, but not limited to, a selective inhibitor of ATP-dependent ?-secretase activity or an agent that decreases the formation of active (or optimally active) ?-secretase. The invention also provides the use of inhibitors of ATP-dependent ?-secretase activity to prevent, treat or ameliorate the symptoms of Alzheimer's disease.

Abstract: Use of chemical compounds obtained in silico for the preparation of pharmaceutical compositions to attenuate or inhibit Dengue virus infection. Particularly, through the interference or the modulation of several stages of viral replication cycle related with the entry of virus into host cells and the assembly of mature progeny virions. The invention also comprises the use of such pharmaceutical compositions for prophylactic and/or therapeutic treatment of infection caused by all four serotypes of Dengue virus and other flaviviruses.

Abstract: Certain noel N-(heteroarylalkyl)alkanediamine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula I: wherein Ar, a, r, R, Ra, Rb, Rc, Rd, b, c, Re, Rf, Rg, Rh, R5, d, e, U, V, X, WR6 and R7 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.

Abstract: The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A2 and R1, R2, R3, R4a, R4b, R5, R6, Ar, X1, X2, X4, X4 and X5 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.

Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, and W are as defined in the specification. Such compounds are MEK inhibitors and are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, and inflammatory conditions in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative and inflammatory diseases in mammals and pharmaceutical compositions containing such compounds.

Abstract: The invention relates to a compound of formula (I) wherein A1 and R1 to R5 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

Abstract: Compounds of the formula (I) or a pharmaceutically acceptable salt or solvate thereof is disclosed. The compounds are useful for treating diabetes, inflammation, atherosclerosis, hypertension, pain and the like. Pharmaceutical compositions and methods of use are also included.

Abstract: The present invention pertains to a combination for simultaneous, separate or sequential use which comprises (a) a cyclin-dependent kinase inhibitor and (b) 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide and to its use for the treatment of cancer, especially of Bcr/Abl+ leukemia resistant to compound of formula I.

Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising novel diamine compositions for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.

Abstract: Phenylalanine derivatives of the following formula, analogues thereof and pharmaceutically acceptable salts thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning ?4 integrin in which ?4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection. wherein R1 is a methyl group and R2 is a methoxy group.

Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein the variables A, L1, L2, R2, R11, and M are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Abstract: Benzenesulfonamide derivative compounds corresponding to the general formula (I): and their pharmaceutically acceptable addition salts; a process for preparation of such compounds; pharmaceutical compositions containing such compounds, and the use of such compounds as a pharmacologically active substance, in particular in the treatment of neurodegenerative diseases, cardiovascular diseases, inflammatory diseases; hypercholesterolemia, and diabetes.

Abstract: The invention concerns the use of ketoconazole and derivatives having a corresponding biological activity, and combinations thereof, in the treatment of abdominal obesity, hypertension, hyperinsulinemia, and elevated blood lipids.

Abstract: The present invention discloses compounds of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Phenylene Compound”); compositions comprising an effective amount of a Phenylene Compound; and methods for treating or preventing pain and other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Phenylene Compound.

Abstract: The invention discloses methods and compositions useful for facilitating neuronal regeneration and functional recovery in neurodegenerative diseases. The methods and compositions utilize ligands for the sigma receptor, wherein the ligand is preferably SA-4503, or salts, or solvates thereof. These molecules can be delivered alone or in combination with agents which treat or prevent neurodegenerative diseases such as those caused by ischemic stroke, diabetic peripheral neuropathy, cancer therapy induced neuropathy, multiple sclerosis, amyotrophic lateral sclerosis, traumatic brain injury, spinal cord injury, Huntington's disease or Parkinson's disease. In other methods, the sigma receptor ligands are administered after stroke to facilitate functional recovery. The administration of the sigma receptor ligands effects faster functional recovery.

Abstract: A novel class of pyridazine compositions and related methods of use.

Abstract: The novel active compound combinations comprising compounds of the formulae (I) and (II) have very good insecticidal and acaricidal properties.

Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: The present invention encompasses compounds of Formula I which are antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.

Abstract: A method for the treatment of chronic valvular disease (CVD) in animals, particularly dogs, comprising administering to a subject in need thereof an effective amount of levosimendan or a pharmaceutically acceptable salt thereof. Levosimendan was shown to significantly reduce mortality and to significantly improve quality of life in dogs suffering from chronic valvular disease.

Abstract: The invention discloses methods and compositions useful for facilitating neuronal regeneration and functional recovery in neurodegenerative diseases. The methods and compositions utilize ligands for the sigma receptor, wherein the ligand is preferably AGY-94806, or salts, or solvates thereof. These molecules can be delivered alone or in combination with agents which treat or prevent neurodegenerative diseases such as those caused by multiple sclerosis. In other methods, the sigma receptor ligands are administered after MS to facilitate functional recovery. The administration of the sigma receptor ligands causes faster functional recovery.

Abstract: The present invention relates to prokineticin 1 receptor antagonists and methods of using the same to modulate intestine epithelial functions and to treat inflammation in the intestine in a mammal.

Abstract: The invention relates to the use of a phosphodiesterase type III (PDE III) inhibitor or Ca2+-sensitizing agent or a pharmaceutically acceptable derivative thereof for the preparation of a medication for the prolongation of time until onset of clinical symptoms in patents having an asymptomatic (occult) heart failure or for the reduction of heart size in patients having an asymptomatic (occult) heart failure of a patient suffering from asymptomatic heart disease.

Abstract: Compounds having the formula I wherein R1, R2, R3, R4, R5a, R5b, R5c and R6 are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.

Abstract: The present invention relates to novel pyridazine derivatives of formula (I) as active ingredients which have microbiocidal activity, in particular fungicidal activity: formula (I) wherein R1 is C1-C6alkyl, C1-C6haloalkyl or C3-C6cycloalkyl; R2 is hydrogen or an optionally substituted alkyl, aryl or heteroaryl; R3 is hydrogen, C1-C6alkyl or C1-C6haloalkyl; R4 is hydrogen, C1-C6alkyl or C1-C6haloalkyl; or R3 and R4 together can be part of a carbocyclic or heterocyclic 3- to 8-membered ring; R5 is optionally substituted aryl or heteroaryl; and R6 is hydroxy, halogen, C1-C6alkoxy, C1-C6haloalkoxy, C1-C6alkylthio or C1-C6haloalkylthio; or an agrochemically usable salt form thereof.

Abstract: The present invention is related substituted enaminones represented by a compound of Formula I that are novel allosteric modulators of ?7 nAChRs. The invention also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on ?7 nAChRs in a mammal by administering an effective amount of a compound of Formula I.

Abstract: The present invention provides an integrin expression inhibitor, and an agent for treating arterial sclerosis, psoriasis, cancer, retinal angiogenesis, diabetic retinopathy or inflammatory diseases, an anticoagulant, or a cancer metastasis suppressor on the basis of an integrin inhibitory action.

Abstract: Conventional many fungicidal compositions have had practical problems such that either a preventive effect or a curing effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired.

Abstract: The invention provides novel arylamino N-heteroaryl MEK inhibitors of Formula (I): Such compounds are MEK inhibitors that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation. Also disclosed is the treatment of a hyperproliferative disease in mammals, and pharmaceutical compositions containing such compounds.

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as obesity, hyperlipidemia, hypercholesterolemia and diabetes and other related disorders and diseases, and may be useful for other diseases such as NASH, atherosclerosis, cardiovascular diseases, hypothyroidism, thyroid cancer and other disorders and diseases related thereto.

Abstract: The present invention provides compositions and methods of use thereof to prevent and/or treat pathogenic infection. In particular, the present invention provides the use of kinase inhibitors to inhibit kinases that involve in pathogen-host cell interactions that are associated with or cause pathogenic infections, therefore, to effectively prevent and/or treat pathogenic infections with far less likely to engender resistance as compared to conventional antibiotics and anti-viral drugs. The present invention further provides the use of kinase inhibitors for the treatment of acute pathogenic infections for a short period of time to avoid toxicities that may caused by long term use of these kinase inhibitors.

Abstract: A combination of a levosimendan compound or a pharmaceutically acceptable salt thereof and an angiotensin II receptor antagonist or an angiotensin converting enzyme (ACE) inhibitor shows synergistic effect in the prevention of stroke. Pharmaceutical compositions and medical kits comprising as a first active ingredient a levosimendan compound or a pharmaceutically acceptable salt thereof and as a second active ingredient an angiotensin II receptor antagonist or an angiotensin converting enzyme (ACE) inhibitor are provided.

Abstract: Pyridazinyl compounds, compositions and related methods of use.

Abstract: A pyridazine compound represented by formula (1): wherein R1 and R2 are same or different and represent a C1-C4 alkyl group; R3 represents a halogen atom, a nitro group, a cyano group, a C1-C4 alkyl group optionally substituted by at least one halogen atom, a C1-C4 alkoxy group optionally substituted by at least one halogen atom or a C1-C4 alkylthio group optionally substituted by at least one halogen atom; R4 and R5 each represents a halogen atom, a nitro group, a cyano group, a C1-C4 alkyl group optionally substituted by at least one halogen atom or a C1-C4 alkoxy group optionally substituted by at least one halogen atom; and m and n each represents an integer.

Abstract: The present invention is directed to methods and agents that are useful in the prevention and amelioration of signs and symptoms associated with neuropathic conditions. More particularly, the present invention discloses the use of angiotensin II receptor 2 (AT2 receptor) antagonists for the treatment, prophylaxis, reversal and/or symptomatic relief of neuropathic pain, including mechanical hyperalgesia, thermal or mechanical allodynia, diabetic pain and entrapment pain, in vertebrate animals and particularly in human subjects. The AT2 receptor antagonists may be provided alone or in combination with other compounds such as those that are useful in the control of neuropathic conditions.

Abstract: Conventional fungicidal compositions have had practical problems such that either a preventive effect or a curative effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired. The present invention provides a fungicidal composition containing a carboxylic acid amide derivative of the formula (I) or a salt thereof, as an active ingredient: wherein A is phenyl which may be substituted, benzodioxolanyl which may be substituted, or benzodioxanyl which may be substituted; B is 2- or 3-pyridyl which may be substituted; each of R1 and R2 is alkyl, or R1 and R2 may together form a 3- to 6-membered saturated carbon ring, provided that when B is 3-pyridyl which may be substituted, A is phenyl substituted by at least two substituents.

Abstract: The present invention provides compositions and methods for administering florfenicol to mammals. The compositions contain a prodrug of florfenicol in a pharmaceutically acceptable carrier. In one embodiment the prodrug is an esterized form of florfenicol. Examples of suitable prodrugs include one or a combination of one or a combination of the following: florfenicol acetate, florfenicol propionate, florfenicol butyrate, florfenicol pentanoate, florfenicol hexanoate, florfenicol heptanoate, florfenicol octanoate, florfenicol nanoate, florfenicol decanoate, florfenicol undecanoate, florfenicol dodecanoate, and florfenicol phthalate. In another embodiment the prodrug is converted into the florfenicol in vivo by the action of one or more endogenous esterases. The invention also provides new compounds, pharmaceutical compositions containing the compounds, and methods for their administration.

Abstract: The present invention relates to the use of active substance combinations which consist firstly of a known dihydrofuranone derivative and secondly of further known pesticidal active substances, which active substance combinations are used for controlling animal pests, in particular from the order of the mites.

Abstract: The present invention is directed to pyridazinone compounds of formula (I) and furan compounds of formula (II), pharmaceutical compositions of compounds of formula (I) and (II), kits containing these compounds, methods of syntheses, and a method of treatment of a proliferative disease in a subject by administration of a therapeutically effective amount of a compound of formulae (I) or (II). Both classes of compounds were identified through screening of a collection of small molecule libraries.

Abstract: The present invention relates to therapeutic and/or prophylactic uses of pyridazine compounds and to pharmaceutical compositions containing one or more of these compounds as an active component for treating a disorder characterized by conduction disturbances, electroconvulsions and/or seizures, in particular epilepsy, more particularly pediatric epilepsy. In an aspect of the invention, the pyridnsine compound has the Formula (Ia) or (Ib) wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the description.

Abstract: The present invention relates to an improved method of formation of disulfide bridges in substances bearing SH groups, in particular peptides, for example by formation of intramolecular disulfide bridges, in which a heterocyclic compound having at least one nitrogen atom (e.g. caffeine or a caffeine-like substance) is used for catalysis of the reaction. It was found, surprisingly, that addition of the heterocyclic substance increases both the yield and the purity of the product bearing disulfide bridges.

Abstract: The novel active compound combinations comprising a compound of the formula (I-1) or (I-2) and the active compounds (1) to (26) listed in the description have very good insecticidal and acaricidal properties.

Abstract: The present invention relates to novel N-sulfamoyl-piperidineamides of Formula I and their physiologically acceptable acid addition salts, to pharmaceutical compositions comprising them, processes for their preparation, and their use for the treatment of obesity and its concomitant and/or secondary diseases and related or other conditions.

Abstract: The present invention is directed to compounds of formula I: Wherein R1 to R5, X and Z are further defined in the description. The invention also relates to processes for the preparation of the compounds and to intermediates used in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.

Abstract: The invention provides novel arylamino N-heteroaryl MEK inhibitors of Formula (I): Such compounds are MEK inhibitors that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation. Also disclosed is the treatment of a hyperproliferative disease in mammals, and pharmaceutical compositions containing such compounds.

Abstract: To find a compound having a tissue fibrinosis-inhibitory activity and a fibrinolytic activity, and to provide a novel compound that is useful for preventing and/or treating tissue fibrinosis diseases (pulmonary fibrosis, renal fibrosis etc.), diseases caused by pathological blood clots such as ischemic heart diseases (myocardial infarction, angina), intraatrial thrombus, pulmonary embolism, deep venous thrombosis, disseminated intravascular coagulation, ischemic cerebral diseases (cerebral infarction, cerebral bleeding) and arteriosclerosis and the like. To provide a pharmaceutical drug comprising a 5-phenyl-3-pyridazinone derivative represented by the following general formula (I): and an optical isomer thereof, or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, useful for preventing and/or treating disease conditions or symptoms mediated by plasminogen activator inhibitor-1.

Abstract: The invention relates to compounds of formula wherein Het, A1, A2, A3, A4, D, W, T, Q, Y, X1, X2, R1, R2, R3, R4, k and m are as defined hereinabove, and, where applicable, to possible E/Z isomers, mixtures of E/Z isomers and/or tautomers thereof, in each case in free form or in salt form, to a process for the preparation of and to the use of those compounds, E/Z isomers, mixtures of E/Z isomers and/or tautomers, to pesticidal compositions in which the active ingredient has been selected from those compounds, E/Z isomers, mixtures of E/Z isomers and/or tautomers, in each case in free form or in agrochemically usable salt form, to a process for the preparation of and to the use of those compositions, to plant propagation material treated with those compositions, to a method of controlling pests, to intermediates and, where applicable, to possible E/Z isomers, mixtures of E/Z isomers and/or tautomers thereof, in each case in free form or in salt form, for the preparation of those compounds, E/Z isomers, m

Abstract: The invention relates to methods of treating patients who have suffered an acute myocardial infarction (AMI) with a therapeutic that has anti-fibrotic effects, for example, pirfenidone and analogs thereof.

Abstract: Compounds of the formula I, in which R1, R2, R3, R4, R5 and X have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.