Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with the compounds.

Abstract: The present invention relates to novel compounds, their use in the prevention or treatment of symptoms and disorders associated with the bradykinin B1 pathway and pharmaceutical compositions containing them.

Abstract: The present invention relates to compounds of formula (IA) wherein QA is QA1 or QA2 P is P1, heterocycyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, Z, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (IA), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (IA) and to methods of using the compounds of formula (IA) to control insect, acarine, nematode and mollusc pests.

Abstract: The present invention provides compounds having the general structural Formula (I): and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis or dysproliferation.

Abstract: Provided herein are new N-,C-disubstituted azoles and derivatives thereof that exhibit nematicidal activity and are useful, for example, in methods for the control of unwanted nematodes.

Abstract: The present application relates to new, substituted 2-acetamido-5-aryl-1,2,4-triazolones, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.

Abstract: Compounds represented by Formula I and II, or pharmaceutically acceptable salts thereof: inhibit bacterial 2-epimerase and are useful anti-infective agents.

Abstract: Sterically hindered imidazole ligands are described, along with their synthesis, which are capable of coordinating to Group 2 metals, such as: calcium, magnesium, strontium, in an eta-5 coordination mode which permits the formation of monomeric or dimeric volatile complexes. A compound comprising one or more polysubstituted imidazolate anions coordinated to a metal selected from the group consisting of barium, strontium, magnesium, radium or calcium or mixtures thereof. Alternatively, one anion can be substituted with and a second non-imidazolate anion. Synthesis of the novel compounds and their use to form BST films is also contemplated.

Abstract: Imidazole derivatives of formula (I): wherein R1, R2a, R2b, A, V and W are as defined in the description, as inhibitors of fructose-1,6-bisphosphatase, their preparation process and their use in the prevention or treatment of diabetes, and other diseases where the inhibition of gluconeogenesis, control of blood glucose levels, reduction in glycogen stores, or reduction in insulin levels is beneficial and diseases related to the insulin resistance syndrome.

Abstract: The invention relates to compounds of formula (I) wherein R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.

Abstract: The present invention relates to novel derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.

Abstract: The invention relates to the compounds of the general formula (I): in which A, D, R, R1 and X are as defined in the description, to a process for the preparation thereof and to the therapeutic use thereof in the treatment of pathologies associated with insulin resistance syndrome.

Abstract: The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds.

Abstract: Presently provided are IDO inhibitors of general formulae (VII), (VIII) as shown below and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.

Abstract: The present invention relates to novel derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: Sterically hindered imidazole ligands are described, along with their synthesis, which are capable of coordinating to Group 2 metals, such as: calcium, magnesium, strontium, in an eta-5 coordination mode which permits the formation of monomeric or dimeric volatile complexes. A compound comprising one or more polysubstituted imidazolate anions coordinated to a metal selected from the group consisting of barium, strontium, magnesium, radium or calcium or mixtures thereof. Alternatively, one anion can be substituted with and a second non-imidazolate anion.

Abstract: [Object] To provide a pharmaceutical product (chemotherapeutic agent) effective in the prevention and treatment of hyperlipidemia, obesity, etc. [Solving Means] A phenylimidazole compound represented by the following General Formula (1): wherein, R1 represents a hydrogen atom, a phenyl lower alkyl group optionally having a substituent, or a pyridyl lower alkyl group optionally having a substituent, and the benzene ring and the pyridine ring are optionally substituted with 1 or 2 substituents selected from the group consisting of halogen atoms, cyano group and halogen-substituted lower alkyl groups. One of R2 and R3 represents a hydrogen atom and the other represents a lower alkoxy group. R4 represents a phenyl group optionally having a substituent. R5 and R6 are the same or different, and represent a hydrogen atom or a lower alkyl group. R7 and R8 are the same or different, and represent a hydrogen atom or a lower alkoxy group.

Abstract: Disclosed are compounds and compositions of the formula (I) as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula (I).

Abstract: This invention relates to novel imidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.

Abstract: The invention relates to compounds of formula (I) wherein R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.

Abstract: The present invention relates to new imidazole modulators of M3 muscarinic acetylcholine receptor activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The invention is in general directed to acid-sensitive linkers, and methods of use thereof, such as, for example, in drug delivery methods.

Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.

Abstract: The present invention relates to 4,5-bis(4-methoxyphenyl)imidazole compound inducing differentiation of myoblasts or muscle fibers into neuron cells, a pharmaceutical composition including said compound, a method of inducing neuron cells differentiation and a screening method for identifying additional compound useful for inducing neuron cells differentiation. More specifically, it relates to 2-{2-[5-(3-chlorophenyl)]furanyl}-4,5-bis(4-methoxyphenyl)imidazole that induces differentiation of myoblasts or muscle fibers into neuron cells, all pharmaceutically acceptable isomers, salts, and a pharmaceutical composition including said compound, a method of inducing neuron cells differentiation and a screening method for identifying additional compound useful for inducing neuron cells differentiation.

Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of ?-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.

Abstract: The present invention relates to novel imidazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). The compounds are represented by the general formula (I) wherein R1, R2, R3 and R4 are as defined in the description. For example, R1 may be phenyl, R2 may be dimethylamino pyrrolidin-1-yl, R3 may be alkoxy and R4 may be alkyl, ai arylalkyl, aryloxyalkyl, aryloxy or heterocyclylalkyl.

Abstract: The present invention relates to 4,5-bis(4-methoxyphenyl)imidazole compound inducing differentiation of myoblasts or muscle fibers into neuron cells, a pharmaceutical composition including said compound, a method of inducing neuron cells differentiation and a screening method for identifying additional compound useful for inducing neuron cells differentiation. More specifically, it relates to 2-{2-[5-(3-chlorophenyl)]furanyl}-4,5-bis(4-methoxyphenyl)imidazole that induces differentiation of myoblasts or muscle fibers into neuron cells, all pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug thereof, and a pharmaceutical composition including said compound, a method of inducing neuron cells differentiation and a screening method for identifying additional compound useful for inducing neuron cells differentiation.

Abstract: An ophthalmic solid pharmaceutical preparation for external use is disclosed which can be used to continuously administer with ease a pharmacologically active agent to ocular local tissues. The pharmaceutical preparation is a solid pharmaceutical preparation containing a pharmacologically active ingredient in a base, which may comprise an oily base, and designed to be applied by being rubbed on the surface of the skin including the surface of either of the eyelids to deliver, through the skin of the eyelids, the pharmacologically active ingredient to the local tissues of the eye located on the backside of the eyelids.

Abstract: The invention relates to the use of imidazole derivatives of the formula (1): in which A, R?1, R?2 and R?3 are as defined in the description, as AMPK activators. The invention also relates to processes for the preparation of the said compounds, to their uses for the preparation of medicaments for the treatment of insulin resistance, diabetes and related pathologies, and also obesity, and to the pharmaceutical compositions comprising them. Certain compounds of the formula (1) are novel and, in this respect, also form part of the invention.

Abstract: The present invention relates to a compound of the formula (1): wherein R1 is group of the formula (2): (wherein X is nitrogen atom or C(R5), Y is nitrogen atom or C(R6), R5 and R6 are each independently hydrogen atom, etc.) etc., m is 1 to 6, L1 is single bond, etc., R2 is hydrogen atom, substituted or unsubstituted alkyl group, etc., R3 is hydrogen atom, etc., L2 is single bond, etc., R4 is hydrogen atom, substituted or unsubstituted aryl group, etc., or pharmaceutically acceptable salt thereof, being useful for preventing or treating Alzheimer's disease.

Abstract: The present invention relates to a process for preparing optionally substituted aromatic or heteroaromatic nitriles starting from haloaromatics. These are reacted in a copper-catalysed reaction with potassium hexacyanoferrate(II) or potassium hexacyanoferrate(III) in the presence of heteroaromatic amines.

Abstract: Imidazole derivatives of formula (I) wherein R1, R2a, R2b, A, V and W are as defined in the description, as inhibitors of fructose-1,6-bisphosphatase, their preparation process and their use in the prevention or treatment of diabetes, and other diseases where the inhibition of gluconeogenesis, control of blood glucose levels, reduction in glycogen stores, or reduction in insulin levels is beneficial and diseases related to the insulin resistance syndrome.

Abstract: The present application relates to novel phenylthioacetic acid derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders, in particular dyslipidaemias and arteriosclerosis.

Abstract: An improved process for preparing arylethanoldiamines is described. Compounds of this type are known to be useful as agonists at a typical beta-adrenoceptors (also known as beta-3-adrenoceptors).

Abstract: The invention relates to the compounds of the general formula (I): in which A, D, R, R1 and X are as defined in the description, to a process for the preparation thereof and to the therapeutic use thereof in the treatment of pathologies associated with insulin resistance syndrome.

Abstract: The present invention relates to novel compounds and methods that are useful in treating members of the Flaviviridae family of viruses. Compounds of the present invention will have a structure according to Formulas (I)-(VI) as recited throughout the application.

Abstract: The present invention provides bradykinin-B1 antagonists of the formula in which A, Ar, G, Q, R1 and R4 are as defined in claim 1, their enantiomers, their diastereomers, their mixtures and their salts, in particular their physiologically acceptable salts with organic or inorganic acids or bases having useful properties, their preparation, medicaments comprising the pharmacologically effective compounds, their preparation and their use.

Abstract: The present invention relates to novel compounds and methods that are useful in treating members of the Flaviviridae family of viruses. Compounds of the present invention will have a structure according to Formulas (I)–(VI) as recited throughout the application.

Abstract: The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein L, Z0, R1, R4, R5, and R11 are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.

Abstract: The present invention provides novel 5-substituted tetralones of Formulas I, II, III, and IV and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof, which are useful for treating and preventing uncontrolled or abnormal proliferation of tissues, such as cancer, atherosclerosis, restenosis, and psoriasis.

Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts thereof, are useful for modulating mitochondrial F1F0 ATPase activity and treating ischemic conditions including myocardial infarction, congestive heart failure, and cardiac arrhythmias.

Abstract: This invention relates to low molecular weight, non-peptidic, non-peptidomimetic, organic molecules that act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also to such ligands that act as antagonists or inverse agonists of complement C5a receptors. Preferred compounds of the invention possess some or all of the following properties in that they are: 1) multi-aryl in structure, 2) heteroaryl in structure, 3) a pharmaceutically acceptable oral dose can provide a detectable in vitro effect, 4) comprise fewer than four or preferably no amide bonds, and 5) capable of inhibiting leukocyte chemotaxis at nanomolar or sub-nanomolar concentrations. This invention also relates to pharmaceutical compositions comprising such compounds and the use of such compounds in treating a variety of inflammatory and immune system disorders. Additionally, this invention relates to the use such compounds as probes for the localization of C5a receptors.

Abstract: The present invention provides antibacterial agents having the formula I described herein.

Abstract: Hydantoin compounds which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.

Abstract: The present invention provides antibacterial agents having the formula I described herein.

Abstract: Nobel PDF inhibitors and novel methods for their use are provided.

Abstract: This invention relates to low molecular weight, non-peptidic, non-peptidomimetic, organic molecules that act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also to such ligands that act as antagonists or inverse agonists of complement C5a receptors, preferably human C5a receptors, Preferred compounds of the invention possess one or more, and preferably two or more, three or more, four or more, or all of the following properties in that they are; 1) multi-aryl in structure (having a plurality of un-fused or fused aryl groups), 2) heteroaryl in structure, 3) orally available in vivo (such that a sub-lethal or preferably a pharmaceutically acceptable oral dose can provide a detectable in vitro effect such as a reduction of C5a-induced neutropenia), 4) comprised of fewer than four, preferably fewer than three, or fewer than two, or no amide bonds, and 5) capable of inhibiting leukocyte chemotaxis at nanomolar concentrations and preferably at

Abstract: The present invention relates to a c-Jun N-terminal kinase inhibitor containing an azole compound (I) substituted by a nitrogen-containing aromatic group having substituent(s)(except a compound represented by the formula: 1

Abstract: Nucleic acid labeling compounds containing heterocyclic derivatives are disclosed. The heterocyclic derivative containing compounds are synthesized by condensing a heterocyclic derivative with a cyclic group (e.g. a ribofuranose derivative). The labeling compounds are suitable for enzymatic attachment to a nucleic acid, either terminally or internally, to provide a mechanism of nucleic acid detection.