Abstract: The present invention relates to combinations of 4-bromo-2-(4-chloro-phenyl)-5-(trifluoromethyl)-1H-pyrrole-3-carbonitrile, or a salt thereof, and a biocidal compound which provide an improved protecting effect against fouling organisms.

Abstract: Solid pharmaceutical compositions containing atorvastatin are disclosed. The compositions include a solid dispersion of amorphous atorvastatin and one or more optional pharmaceutically acceptable excipients. The solid dispersion is prepared by mixing crystalline atorvastatin with a melt-processable polymer and an optional stabilizer at a temperature sufficiently high to soften or melt the polymer and to melt or dissolve the crystalline atorvastatin in the polymer, thereby forming a dispersion of amorphous atorvastatin.

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 present invention provides new method of treatment of epilepsy with non-imidazole alkylamine derivatives that constitute antagonists of the H3-receptors of histamine.

Abstract: A therapeutic combination, useful in a co-therapy method for improving cardiovascular performance and/or treating cardiovascular diseases, is provided comprising a first agent and a second agent, wherein the first agent comprises a histone deacetylase inhibiting agent and the second agent comprises at least one nuclear hormone receptor ligand.

Abstract: Medical devices and methods for delivering a therapeutic agent to a heart valve.

Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted biaryl-methanesulfinyl acetamides of Formula (I): wherein Ar, Y, R1, R2, R4, R5, q and x are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness associated with narcolepsy, obstructive sleep apnea, or shift work disorder; Parkinson's disease; Alzheimer's disease; attention deficit disorder; attention deficit hyperactivity disorder; depression; or fatigue associated with a neurological disease; as well as the promotion of wakefulness.

Abstract: The present invention provides an azolylacylquanidine compound of formula I The present invention also provides methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tangles.

Abstract: Described herein are compositions and methods for using these compositions in the treatment of cancer, tumors, and tumor-related disorders in a subject.

Abstract: The present invention provides novel compounds of the general Formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is (CH2)n where n is 0, 1 or 2; R1, R2, R3, R4 and R5 may be the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, alkylsulphonyloxy, cyano, nitro, trihaloalkyl, sulpho or one of the structures given in Scheme 1; or two of R1, R2, R3, R4 and R5 may together form a methylenedioxy or ethylenedioxy moiety; R6, R7, R8 and R9 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, amines (primary, secondary or tertiary) having 0, 1 or 2 carbon atoms, cyano, nitro, trihaloalkyl, amide or sulpho, and z where shown represents the point of attachment of the residue to the phenyl or pyrrole ring; and the pharmacologically active salts thereof.

Abstract: It has now been found that certain novel heterocyclic derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): R Preferred are those compounds of formula (I) where R2 and R3 taken together is ?NCH(R6)CH(R7)N(R8)—, ?NC(R6)=C(R7)N(R8)-, or ?CHN?C(R7)N(R8)—, and tautomers thereof, and where R4 and R5 taken together is —C(R11)=C(R12)C(R13)=C(R14) 112, -, where R, R, R6, R7, R8, R11, R R13, R14, and X are described. 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: Heterocyclic arylsulfonamidobenzylic compounds are provided which are useful in treating lipid disorders, metabolic disorders and cell-proliferative diseases.

Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.

Abstract: A method of inhibiting NF-?B activation in a mammal including a human, which comprises the step of administering an effective dose of a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof:

Abstract: An encapsulated composition of (a) a pesticide at least active via ingestion that is photolabile, and (b) at least one photoprotectant, wherein the encapsulating polymeric barrier is base triggerable is disclosed. A method for controlling damage of a material by a pest by the use of such encapsulated compositions is likewise disclosed. The composition as disclosed gives protection for beneficial arthropods and reduces workers exposure.

Abstract: It relates to an endogenous repair factor production accelerator which comprises one or at least two selected from prostaglandin (PG) 12 agonist, EP2 agonist and EP4 agonist. Since prostaglandin (PG) 12 agonist, EP2 agonist or EP4 agonist has various endogenous repair factor production accelerating action, angiogenesis acceleration action and stem cell differentiation induction action, it is useful as preventive and/or therapeutic agents for ischemic organ diseases (e.g., arteriosclerosis obliterans, Buerger disease, Raynaud disease, myocardial infarction, angina pectoris, diabetic neuropathy, spinal canal stenosis, cerebrovascular accidents, cerebral infarction, pulmonary hypertension, bone fracture, Alzheimer disease, etc.) and various cell and organ diseases.

Abstract: The present invention provides an azolylacylquanidine compound of formula I The present invention also provides methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tangles.

Abstract: The invention relates to a compound represented by general formula (I) wherein Z represents N, O or S, and A represents a CH group, a nitrogen atom or an NL+ group wherein L represents a straight-chained or branched C1-C12 alkyl group. The invention also relates to a method for the preparation thereof and the use thereof as an antimitotic.

Abstract: Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, B, D, Z, R1, R2a, R2b, and Rx are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.

Abstract: The invention describes new compounds derived from formula I pyrroles, methods for obtaining them and their application as drugs in pharmaceutical compositions for the treatment of cancer due to their inhibitory activity on certain histone deacetylases.

Abstract: Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid or solvates or hydrates thereof, as well as crystalline salts characterized by their X-ray powder diffraction pattern are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.

Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.

Abstract: Novel pyrrole derivatives are disclosed as A?42-lowering agents for the treatment and prevention of neurodegenerative disorders characterized by the formation or accumulation of amyloid plaques comprising the A?42 peptide.

Abstract: This invention relates to a combination product or medicament comprising at least one novel substituted pyrrole derivative and one or more dyslipidemic agents, antiobesity agents, antihyperglycaemic agents, anti-inflammatory agents or mixture thereof.

Abstract: A medicament for preventive and/or therapeutic treatment of neurodegenerative diseases such as Alzheimer's disease or the like which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein A represents hydrogen atom or acetyl group, E represents a 2,5-di-substituted or a 3,5-di-substituted phenyl group, or a monocyclic or a fused polycyclic heteroaryl group which may be substituted, provided that the compound wherein said heteroaryl group is {circle around (1)} a fused polycyclic heteroaryl group wherein the ring which binds directly to —CONH— group in the formula (I) is a benzene ring, {circle around (2)} unsubstituted thiazol-2-yl group, or {circle around (3)} unsubstituted benzothiazol-2-yl group is excluded, ring Z represents an arene which may have one or more substituents in addition to the group represented by

Abstract: Aminophosphonate and amino bisphosphonate compounds and methods for their preparation are provided. Also provided are pharmaceutical and agricultural compositions containing the compounds. The compounds and compositions are useful in methods for treatment of various diseases, including, inflammation, autoimmune disease, cardiovascular disease, bacterial infection, viral disease, abnormal cell proliferation, bone resorption disease, osteoporosis, or parasitic disease and in various agricultural methods, including, methods of eradicating weeds.

Abstract: The invention concerns compounds of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. The invention also concerns the method for preparing said compounds including the intermediates therefor and their therapeutic use.

Abstract: The present invention relates to compounds of formula (I) wherein R1 is as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP-IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.

Abstract: The present invention relates to novel substituted pyrrole compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel substituted pyrrole compounds of the general formula (I), their analogs, their derivatives, their polymorphs, their tautomeric forms, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. This invention also relates to the process for preparing such compounds, a composition containing such a compound and the use of such a compound and composition in medicine.

Abstract: The invention relates to compounds having formula (I): Wherein X, R1, R2, R3, R4 and R5 are as defined herein. The invention also relates to the preparation method thereof and the use of same in therapeutics.

Abstract: The present invention provides a novel pyrrole derivative having excellent androgen receptor antagonism, which is represented by the formula: wherein R1 represents a hydrogen atom, a cyano group or a group represented by the formula COORA (wherein RA represents an optional substituted C1-6 alkyl group), R2 and R4 are the same or different, and each represents a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a trifluoromethyl group, an amino-C1-6 alkyl group, a mono- or di-substituted amino-C1-6 alkyl group, an optionally halogenated C1-6 alkyl group substituted with an optionally substituted hydroxyl group, a C2-6 alkenyl group substituted with an optionally substituted hydroxyl group, a C1-6 alkyl group substituted with an optionally substituted and optionally oxidized thiol group, an optionally substituted with and optionally oxidized thiol group, a cyano group, an acyl group, an optionally substituted oxazolyl group or a 1,3-dioxolan-2-yl group, R3 represents a group represented by the for

Abstract: A regime or regimen for promoting and/or inducing and/or stimulating the pigmentation of keratin materials and/or for preventing and/or limiting the depigmentation and/or bleaching and/or for preventing and/or limiting the canities thereof, more particularly of human keratin fibers such as the hair, beard hair, moustache hair, the eyelashes and the eyebrows, includes administering to an individual in need of such treatment at least one 2-oxyacetamide compound of formula (I), or a salt and/or solvate thereof:

Abstract: The invention relates to the use of substituted 2-aminotetralins of general formula (I) as a medicament for the preventive treatment of Parkinson's disease.

Abstract: The present invention relates to a composition for noxious organisms-controlling agent having a synergistic effect and a method for using said composition, which comprises, as active ingredients thereof, one or more compounds selected from the phthalamide derivatives represented by general formula (I) being useful as an insecticide or acaricide and one or more compounds selected from the compounds having insecticidal, acaricidal or nematocidal activity: wherein R1, R2 and R3 may be the same or different and each represent hydrogen atom, C3-C6 cycloalkyl, -A1-Qp, etc., each of X and Y may be the same or different and represents hydrogen atom, halogen atom, etc., n is an integer of 1 to 4, m is an integer of 1 to 5, and each of Z1 and Z2 represents O or S.

Abstract: The invention relates to aqueous insecticidal compositions embodied in the form of an aqueous polymer fine particle dispersion containing at least one type of organic insecticidal active substance whose water solubility is equal to or less than 5 g/l at 25° C./1013 mbar and a polymer particle average size, determined by dynamic light scattering, is equal to or less than 300 nm, wherein the polymer particles containing at least one insecticidal active substance exhibit a cationic surface charge and the aqueous dispersion of active substance containing polymer particles is obtained by radical aqueous emulsion polymerisation of an ethylenically unsaturated monomer composition M, in which said ethelenycally unsaturated monomer M contains at least one type of insecticidal active substance in a dissolved form. The use of the inventive aqueous insecticidal compositions for protecting lignocellulose-containing materials, in particular wood, against infest pest attacks is also disclosed.

Abstract: Aminomethyl substituted tetracycline compounds, pharmaceutical compositions, and methods of use thereof are discussed.

Abstract: The invention provides pyrrole-containing compounds and methods of use thereof. Kits and pharmaceutical compositions comprising the pyrrole compounds of the invention are also provided. The compounds and compositions disclosed herein are preferably used in the treatment of neurodegenerative diseases, cardiovascular diseases, proliferative diseases, and visual disorders. In particular, methods and compositions for the treatment of stroke are disclosed herein.

Abstract: The present invention relates to novel substituted pyrrole compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel substituted pyrrole compounds of the general formula (I), their analogs, their derivatives, their polymorphs, their tautomeric forms, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them This invention also relates to the process for preparing such compounds, a composition containing such a compound and the use of such a compound and composition in medicine.

Abstract: Compounds of the formula (I) wherein m, n, A, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds and using the compounds for treatment of diseases or conditions mediated by Cathepsin K.

Abstract: Progesterone receptor modulators of formula I, or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein. These compounds are useful for contraception and hormone replacement therapy. Also provided are products containing these compounds.

Abstract: Progesterone receptor modulators of formula I, or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein, are useful for contraception and hormone replacement therapy are described. Also provided are products containing these compounds.

Abstract: The present invention relates to a method for treating a disorder selected from depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R1, R2, Q, W, X, Y, m, and n are as defined in the specification d or not; and their pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers and tautomeric forms.

Abstract: HMGCo-A reductase inhibitor compounds useful as hypocholesterolemic and hypolipidemic compounds are provided. Also provided are pharmaceutical compositions of the compounds. Methods of making and methods of using the compounds are also provided.

Abstract: The present invention is directed to water-soluble derivatives of 2,6-diisopropylphenol (Propofol). The compounds act as prodrugs of 2,6-diisopropylphenol and metabolize rapidly to Propofol thereby providing an alternative to the water-insoluble 2,6-diisopropylphenol. Pharmaceutical compositions comprising these compounds, methods of induction and maintenance of anesthesia or sedation as well as methods of treating neurodegenerative diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.

Abstract: A group of compounds that inhibit HIV replication by blocking HIV entry was identified. Two representative compounds, designated NB-2 and NB-64, inhibited HIV replication (p24 production) with IC50 values <0.5 ?g/ml.

Abstract: The present invention is related to anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations containing them. The compounds act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. The compounds are therefore suitable for use as novel antiarrhythmic agents for the treatment and prophylaxis of atrial arrhythmias (e.g., atrial fibrillation (AF) or atrial flutter).

Abstract: The present invention provides novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups and the use of the novel compounds 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 of the invention 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: N-(2-aminoaryl-propionyl)-amides of formula (1) are described. The process for their preparation and pharmaceutical preparations thereof are also described. The amides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbate recruitment of polymorphonuclear neutrophils (leukocytes PMN) at the inflammatory sites. In particular, the invention relates to the R enantiomers of 2-(aminoaryl)-propionyl amides of formula (1) for use in the ihibition of the chemotaxis of neutrophils induced by IL-8. The compounds of the invention are used in the treatment of psoriasis, ulcerative cholitis, glomerular nephritis, acute respiratory insufficiency, idiopathic fibrosis, and rheumatoid arthritis.

Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) specified agonists or antagonists of nicotinic acetylcholine receptors.

Abstract: The present invention provides novel compounds of the general Formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is (CH2)n where n is 0, 1 or 2; R1, R2, R3, R4 and R5 may be the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, alkylsulphonyloxy, cyano, nitro, trihaloalkyl, sulpho or one of the structures given in Scheme 1; or two of R1, R2, R3, R4 and R5 may together form a methylenedioxy or ethylenedioxy moiety; R6, R7, R8 and R9 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, amines (primary, secondary or tertiary) having 0, 1 or 2 carbon atoms, cyano, nitro, trihaloalkyl, amide or sulpho, and z where shown represents the point of attachment of the residue to the phenyl or pyrrole ring; and the pharmacologically active salts thereof.