Abstract: The invention relates to the novel N?-nitroxyalkylnicotinamide derivatives represented by the general formula I wherein R1 is C1-C4 alkyl; R2 is hydrogen. C1-C4 alkyl, CH2OH or CH2ONO2; R3 is ONO2, CH2ONO2 or OH; provided that when R3 is OH, R2 is CH2ONO2; and X? is an organic or inorganic anion; as well as pharmaceutical compositions thereof and their use as a medicament, in particular, in the treatment of diseases of the cardiovascular system.

Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein G, L, Q, Z, R6, R7, and R8 are defined herein.

Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.

Abstract: There is provided compounds of formula I, wherein ring A, D1, D2a, D2b, D3, L1, Y1, L3 and Y3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.

Abstract: The present invention is concerned with novel arylalkyl carboxylic acid derivatives, more specifically, with acylates of arylalkyl carboxylic acids with naturally occurring, non-toxic hydroxy, sulfhydryl, amino or imino compounds, and to compositions containing them. The compositions are preferably cosmetic preparations.

Abstract: Viruses, and particularly RNA viruses, have high mutation rates. Hence, antiviral agents that have been developed to date targeting protease or reverse transcriptase of viruses have quickly lost their effectiveness and resistant viruses have emerged. Also, in recent years, viral diseases caused by various new viruses such as SARS, avian influenza, and the hepatitis C have become social menaces. Therefore, the development of a novel antiviral agent that can cope with a virus resistant to an existing drug or a new virus and has a wide range of applications has been demanded. The present invention provides a novel anti-RNA viral agent and a method for use thereof. The present invention further provides an anti-RNA viral agent that is also effective against a new virus or a drug-resistant virus, and a method for use thereof.

Abstract: The invention relates to fatty acid niacin conjugates; compositions comprising an effective amount of a fatty acid niacin conjugate; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a fatty acid niacin conjugate.

Abstract: A process for preparing arylcarboxamides of the formula (I) where Ar =a mono- to trisubstituted phenyl, pyridyl or pyrazolyl ring, where the substituents are selected from halogen, Ci-C4-alkyl and C1-C4-haloalkyl; M =thienyl or phenyl, which may bear a halogen substituent; Q =direct bond, cyclopropylene, fused bicycio[2.2.1]heptane or bicyclo[2.2.1]heptene ring; R1 =hydrogen, halogen, C1-C6-alkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, mono- to trisubstituted phenyl, where the substituents are selected from halogen and trifluoromethylthio, or cyclopropyl; by reacting an acid chloride of the formula (II) with an arylamine (III) in a suitable nonaqueous solvent, wherein, in the absence of an auxiliary base, a) the acid chloride (II) is initially charged, b) a pressure of from 0 to 700 mbar is established, c) the arylamine (III) is metered in in an approximately stoichiometric amount and d) the product of value is isolated.

Abstract: The present invention is directed to the amphiphilic pyridinium compounds, such as for suppressing IL-8 secretion and production. The present invention further provides methods of making and using such compounds for the treatment of the IL-8 related diseases, such as cystic fibrosis.

Abstract: The present invention relates to a combination, such as a combined preparation or pharmaceutical composition comprising: (a) compound of formula (I), and/or (II) or a pharmaceutically acceptable salt thereof; (b) at least one therapeutic agent selected from the group consisting of: an antihypertensive agent; an antidiabetics agent; a hypolipidemic agent; an antiplatelet agent; an antiobesity agent; an antithrombotic agent; an agent for diabetic vascular complications; and an agent for treatment of heart failure; or a pharmaceutically acceptable salts thereof, optionally in presence of a pharmaceutically acceptable carrier for separate, simultaneous or sequential use. The present invention also relates to a use of such combination for the treatment of mammal including human being. R1, R2, R3, R1, R2, R3, R4, R5, X, Y, A and B and m are as defined in the specification.

Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.

Abstract: The invention relates to a composition comprising at least one aminobenzamide compound or a salt thereof for controlling animal parasites, veterinary pharmaceutical compositions comprising at least one aminobenzamide of formula (I) for preventing infection with diseases transmitted through parasites, its use for the preparation of a veterinary pharmaceutical for controlling animal parasites, and a method for preventing infection with diseases transmitted through parasites.

Abstract: Compounds of the formula (II) and (IV) are provided, which may be employed as intermediates for making compounds useful in treating respiratory diseases.

Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].

Abstract: The present invention relates to a process for preparing substituted biphenylanilides of the formula I which comprises reacting a compound of formula II in the presence of a base and of a palladium catalyst selected from the group of: a) palladium-triarylpliosphine or -trialkylphosphine complex with palladium in the zero oxidation state, b) salt of palladium in the presence of triarylphospine or trialkylphosphine as a complex ligand or c) metallic palladium, optionally applied to support, in the presence of triarylphosphine or trialkylphosphine, in a solvent, with a diphenylborinic acid according to formula (III)

Abstract: The mechanism by which the high bone mass (HBM) mutation (G171V) of the Wnt coreceptor LRP5 regulates the canonical Wnt signaling was investigated. The mutation was previously shown to reduce Dkk protein-1-mediated antagonism, suggesting that the first YWTD repeat domain where G171 is located may be responsible for Dkk protein-mediated antagonism. However, we found that the third YWTD repeat, but not the first repeat domain, is required for DKK1-mediated antagonism. Instead, we found that the G171V mutation disrupted the interaction of LRP5 with Mesd, a chaperon protein for LRP5/6 that is required for the coreceptors' transport to cell surfaces, resulting in less LRP5 molecules on the cell surface. Although the reduction in the level of cell surface LRP5 molecules led to a reduction in Wnt signaling in a paracrine paradigm, the mutation did not appear to affect the activity of coexpressed Wnt in an autocrine paradigm.

Abstract: Disclosed are certain complexes of AFC compounds and binding agents. Such complexes are useful, among other things, in the treatment of inflammatory diseases or disorders.

Abstract: The present invention relates to compounds of the formula wherein R1 to R8 are 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 the modulation of CB1 receptors.

Abstract: The present invention is directed to pyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin 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 orexin receptors are involved.

Abstract: A fungicidal compound of formula (1): where Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, the ring being substituted by groups R7, R8 and R9; R1 is hydrogen, optionally substituted (C1-4)alkylC(?O), optionally substituted (C1-4)alkylC(?O)O, optionally substituted (C1-4)alkoxy(C1-4)alkyl, optionally substituted allyl, optionally substituted propargyl or optionally substituted allenyl; R2, R3, R4and R5 are each, independently, hydrogen, halogen, optionally substituted (C1-4)alkoxy(C1-4)alkoxy or optionally substituted (C1-4)alkoxy(C1-4)alkyl; R6 is an organic group containing three to thirteen carbon atoms and at least one silicon atom and, optionally, one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, and is optionally substituted by one to four independently selected halogen atoms; R7, R8 and R9are each, independently, hydrogen, halogen, C1-3alkyl, C1-3haloalkyl, C1-3alkoxy(C

Abstract: Nicotinamide compounds of the formula (1) and processes for the preparation thereof are described.

Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-+related disease.

Abstract: The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are defined herein, to compositions containing such compounds and to the uses of such compounds for the treatment of allergic and respiratory conditions.

Abstract: Compounds of Formula (I): in which R1, R2, R7, R8, R9, R10 and A have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.

Abstract: Non-peptidic renin inhibitors nitroderivatives of general formula (I): A1-(Xa—ONO2)j ??(I) having wider pharmacological activity and enhanced tolerability. They can be employed for treating or preventing cardiovascular, renal and chronic liver diseases, inflammatory processes and metabolic syndrome.

Abstract: A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1?) (wherein R1 and R2 are each hydrogen atom or optionally substituted aryl, etc.; X is —COO— or —CON(R10)—; R3 and R4 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R5, R6 and R7 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R9 and R9 are each independently hydrogen atom, C1-C6 alkyl, —CON(R18) (R19) or —COO(R20), etc.; ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; Alk1 and Alk2 are each independently alkanediyl, etc.; l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.

Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.

Abstract: The invention relates to a fungicidally active compound of the general Formula (I): where Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, the ring being substituted by the groups R3, R4 and R5; R1 and R2 are independently H, halo, C1-4 alkyl or C1-4 haloalkyl; and R3, R4 and R5 are each, independently, H, halo, C1-4 alkyl, C1-4 haloalkyl or C1-4 haloalkoxy, provided that at least one of R3, R4 and R5 is not H; to the preparation of these compounds, to novel intermediates used in their preparation, to agrochemical compositions which comprise at least one of the novel compounds as an active ingredient, to the preparation of the compositions and to the use of the active ingredients or compositions in agriculture or horticulture for controlling or preventing infestations of plants by phytopathogenic microorganisms, especially fungi.

Abstract: Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.

Abstract: Compounds of formula (I): or pharmaceutically acceptable salts and esters thereof, are useful for the treatment of obesity, type II diabetes and the metabolic syndrome.

Abstract: A compound of general formula (I): A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.

Abstract: The invention concerns benzamide derivatives of Formula (I) wherein R1a, R1b, R1c, R2, R3, R4, W, m and n have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of histone deacetylase (HDAC).

Abstract: The present invention relates to the use of a compound of formula (I): in which R1 represents a radionuclide, Ar represents an aromatic nucleus, m is an integer varying from 2 to 4, R2 and R3 represent, independently of one another, a hydrogen atom, a (C1-C6)alkyl group, a (C1-C6)alkenyl group or an aryl group chosen from a phenyl, benzyl, imidazolyl, pyridyl, pyrimidinyl, pyrazinyl, indolyl, indazolyl, furyl and thienyl group, and their addition salts with pharmaceutically acceptable acids, in the preparation of a radiopharmaceutical composition intended for the diagnosis and/or treatment of melanoma.

Abstract: Disclosed are nicotinanilide-N-oxide compounds, methods for their production, pharmaceutical compositions which include these compounds, and methods for their use in various therapies.

Abstract: Novel phenyl compounds, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the compounds are agonists and/or ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, genitourinary disorders, inflammation, glaucoma, auto-immune diseases, ischemic conditions, immune-related disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, and as an appetite stimulant.

Abstract: This invention relates aryl substituted pyridines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Ar and R1-R4 are set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

Abstract: The invention provides certain well-defined benzamides that are useful as sphingosine-1-phosphate antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.

Abstract: 3,4(,5)-substituted tetrahydropyridine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4(,5)-substituted tetrahydropyridine compound, and/or a method of treatment comprising administering a 3,4(,5)-substituted tetrahydropyridine compound, a method for the manufacture of a 3,4(,5)-substituted tetrahydropyridine compound, and novel intermediates and partial steps for its synthesis. The 3,4(,5)-substituted tetrahydropyridine compounds have the formula I wherein the substituents and symbols are as described in the specification.

Abstract: The present invention relates to modulators of metalloproteinase activity.

Abstract: An electron donor-acceptor dyad is provided that can provide a charge-separated state with longevity and not only high oxidizing power but also high reducing power. A compound of the present invention is a quinolinium ion derivative represented by the following formula (I), a stereoisomer or tautomer thereof, or a salt thereof: where R1 is a hydrogen atom or an alkyl group, and Ar1 to Ar3 each are a hydrogen atom or an electron-donating group. The compound of the present invention has the above-mentioned structure and therefore can provide a charge-separated state with longevity and not only high oxidizing power but also high reducing power and can be used for various products such as photocatalysts, photosensitizers, dyes, oxidants, reductants, dye-sensitized solar cells, and organic EL devices.

Abstract: Compounds of the formula: are described in which Z, Q, X, L, m and n assume the meanings stated in the description. The compounds (I) inhibit the production of TNF ? and may thus be useful in the treatment of inflammation and pathological conditions involving overproduction of said cytokine. They furthermore exhibit significant inhibitory activity on the proliferation of tumour cells and may thus be used for the treatment and/or prevention of tumorous, neurodegenerative or autoimmune disorders.

Abstract: A compound of general formula (I): A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.

Abstract: The present invention is concerned with novel arylalkyl carboxylic acid derivatives, more specifically, with acylates of arylalkyl carboxylic acids with naturally occurring, non-toxic hydroxy, sulfhydryl, amino or imino compounds, and to compositions containing them. The compositions are preferably cosmetic preparations.

Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, R4, and X are as defined herein or to pharmaceutically acceptable acid addition salts thereof, with the exception of 4-methoxy-N-[2-oxo-2-(phenylamino)ethyl]-N-phenyl-benzamide, 4-chloro-N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-chloro-N-[2-[5-chloro-2-methoxyphenyl)amino]-2-oxoethyl]-N-benzamide, 4-methyl-N-(2-oxo-2-[(2,4,6-trichlorophenyl)amino]ethyl]-N-benzamide, N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-methyl-N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-chloro-N-(2-oxo-2-[(2,4,6-trichlorophenyl)amino]ethyl]-N-benzamide and N-[2-[(2,4-dimethoxyphenyl)amino]-2-oxoethyl]-N-[(2-fluorophenyl)methyl]-benzeneacetamide. The compounds are useful in the treatment of neurological and neuropsychiatric disorders.

Abstract: The present invention is related to alkynyl aryl carboxamides of Formula (I?) and use thereof for the treatment and/or prevention of an inflammatory disorder, obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia-hypercholesterolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of alkynyl aryl carboxamides of Formula (I?) to modulate, notably to inhibit the activity of PTPs. (I?) A is a C2-C15 alkynyl, C2-C6-alkynyl aryl, C2-C6-alkynyl heteroaryl. Cy is an aryl, heteroaryl, cycloalkyl or heterocycle group; n is either 0 or 1. Cy? is an aryl, which may optionally be fused by a 3-8 membered cycloalkyl. R1 and R2 are independently from each other is selected from the group consisting of hydrogen or (C1-C6)alkyl. R4 and R5 are each independently from each other selected from the group consisting of H, hydroxy.

Abstract: The invention describes compositions and kits comprising at least one organic nitric oxide enhancing salt of an angiotensin ? antagonist, 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; (n) treating ophthalmic disorders; (o) treating metabolic syndrome; and (p) treating hyperlipidemia.

Abstract: Novel 3-acylaminobenzanilides of the formula (I) wherein R1 represents phenyl which may be substituted or a 5-member or 6-member heterocyclic ring group, which may be substituted, containing at least one hetero-atom selected from the group consisting of N, O, and S; R2 represents halogen, C1-6 alkyl, or C1-6 haloalkyl; R3 represents C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 haloalkylthio, C1-6 haloalkylsulfinyl, or C1-6 haloalkylsulfonyl; R4 represents halogen, C1-6 alkyl, or C1-6 haloalkyl; X represents halogen, C1-6 alkyl, or C1-6 haloalkyl; and n represents 0 or 1 and the compounds are used as insecticides, and a use of the new compounds as insecticides.

Abstract: The invention is concerned with novel pyridopyrimidinone derivatives of formula (I): wherein R1 to R8, X, Y, m and n are as defined in the description and in the claims. The compounds of the present invention are HM74A agonists with improved properties compared to niacin and can be used for the treatment and/or prevention of diseases such as dyslipidemia, atherosclerosis, diabetes, metabolic syndrome, and other related diseases associated with HM74A.

Abstract: 2-amino-2-phenyl-alkanol ester derivatives of general formula (I) in which: R1 is H, straight or branched 1 to 4C alkyl, straight or branched 2 to 4C alkyl substituted by OH, alkoxy, alkylthio, acyloxy, NH2, alkylamino, dialkylamino, alkylcarbamoyloxy, alkoxycarbonylamino, ureido or alkylureido, R2 is a —CO—R radical in which R is H, alkyl, aryl, heterocyclyl, benzyl or heterocyclylmethyl, or R2 is a —CO—Y—R4 radical for which Y is —O—, —S—, —NH—, -Nalk- for which alk is straight or branched (1 to 4C) alkyl, and R4 is alkyl, aryl, aralkyl or heterocyclylalkyl, capable of being substituted by one or more halogen atoms or OH radicals, straight or branched (1 to 4C) alkyl, alkoxy, alkylthio, acylaminoalkylthio, alkoxycarbonyl or acylamino (1 to 4C) straight or branched, or oxo, or capable of being substituted by R5COO— in which R5 is alkyl optionally substituted by benzyloxycarbonylamino, acylamino or by an amino acid residue, or represents an heterocyclyl radical, or R2 is alkyl (2 to 4C) substituted by OH, alk

Abstract: A compound of formula (I): Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, the ring being substituted by groups R4, R5 and R6; R1 is hydrogen or halo; R2 is hydrogen or halo; R3 is optionally substituted C2-12 alkyl, optionally substituted C2-12 alkenyl, optionally substituted C2-12 alkynyl, optionally substituted C3-12 cycloalkyl, optionally substituted phenyl or optionally substituted heterocyclyl; and R4, R5 and R6 are, independently, selected from hydrogen, halo, cyano, nitro, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy(C1-4)alkyl and C1-4 haloalkoxy(C1-4)alkyl, provided that at least one of R4, R5 and R6 is not hydrogen. The compounds of formula (I) have plant-protective properties and are suitable for protecting plants against infestations by phytopathogenic microorganisms.