Abstract: The present invention relates to methods for controlling or preventing infestation of soybean by phytopathogenic microorganisms, in particular of the Fusarium genus, Sclerotinia sclerotiorum, Microsphaera diffusa, Septoria glycines and Cercospora sojina, more particularly Fusarium virguliforme, Fusarium solani, Fusarium oxysporum, Fusarium acuminatum, Fusarium chlamydosporum, Fusarium compactum, Fusarium culmorum, Fusarium equiseti, Fusarium graminearum, Fusarium merismoides, Fusarium proliferatum, Fusarium pseudograminearum, Fusarium semitectum, Fusarium subglutinans and Fusarium verticilliodes, comprising applying to a crop of plants, the locus thereof, or propagation material thereof, a compound according to formula (I), wherein R1, R2, R3, R4, R5, Y, A, B are as defined herein.

Abstract: Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (II): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2a, R2b, R2c, R3, R4, R5, R6a, R6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: This invention relates to a resolution process for the preparation of fluoroleucine alkyl esters.

Abstract: The present invention relates to compounds of the formula (I), wherein the residues R1 to R6, V, G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present, or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.

Abstract: The present invention relates to a process for the preparation of compounds endowed with phosphodiesterase (PDE4) inhibitory activity having formula (I). The invention also relates to the process for the isolation by crystallization of the compound (I) and to its use for the preparation of pharmaceutical compositions for inhalation in combination with suitable carriers or vehicles. The present invention also relates to solvates and crystal forms of a compound of formula (I). The synthesized product is suitable for use in pharmaceutical applications for instance in the treatment of respiratory diseases.

Abstract: In one aspect, the invention relates to substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: A dual thyrointegrin antagonist and a method for treating an angiogenesis-mediated disorder and/or a hyperthyroidism disorders by introducing the dual thyrointegrin antagonist into animals (e.g., mammals, human beings). The dual thyrointegrin antagonist includes a chemical structure having a thyroid hormone antagonist and ?v?3 integrin antagonist in the same molecule.

Abstract: Disclosed herein are methods and pharmaceutical compositions for reducing the pain associated with parenterally administering a therapeutic agent. The methods and compositions comprise a dispersion comprising microparticles of an analgesic agent in an amount effective to reduce the pain, inflammation, and/or immunological reaction associated with parenterally administering a primary therapeutic agent, wherein the microparticles of the analgesic agent have an effective particle size of less than 20 micrometers.

Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.

Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.

Abstract: Disclosed are sulfonamide compounds of Formula (I): or stereoisomers, N-oxides, prodrugs, or pharmaceutically acceptable salts thereof, wherein ring A, R1, R2, R3, R4 and R5 are defined herein. Also disclosed are methods of using such compounds in the treatment of conditions related to CYP17 enzyme, such as cancer, and pharmaceutical compositions comprising such compounds.

Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropiomc acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).

Abstract: The present invention relates to novel depot formulations (prodrugs) comprising an immobility promoting unit linked via an ester to an active pharmaceutical ingredient, i.a. common NSAIDs. The novel depot formulations are suitable for intra-articular injections and are soluble at slightly acidic pH to facilitate ease of injection, and sparingly soluble at physiological pH thereby precipitating at the site of administration. The precipitate will slowly dissolve and the active drug is released from dissolved depot formulation following esterase mediated cleavage of the ester link between the immobility promoting unit and the active pharmaceutical agent.

Abstract: Process for the preparation of a N-[2-(2-pyridinyl)ethyl]carboxamide derivative of general formula (I) or a salt thereof Intermediate of general formula (II) Intermediate of general formula (III)

Abstract: A dual thyrointegrin antagonist and a method for treating an angiogenesis-mediated disorder and/or a hyperthyroidism disorders by introducing the dual thyrointegrin antagonist into animals (e.g., mammals, human beings). The dual thyrointegrin antagonist includes a chemical structure having a thyroid hormone antagonist and ?v?3 integrin antagonist in the same molecule.

Abstract: Embodiments provided herein relate to molecules, compositions, and methods for light absorption. In some embodiments, the molecules and/or compositions can be used to absorb ultraviolet light. In some embodiments, the ultraviolet light absorption compound can be used in a sunscreen composition. In some embodiments, the compound includes an azobenzene group for the absorption of ultraviolet light.

Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.

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: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

Abstract: The present disclosure relates to novel compounds, compositions containing same and methods for treating or preventing a condition associated with a deficient insulin secretion such as diabetes and metabolic syndrome in a subject in need thereof.

Abstract: Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ?CH— or ?N—; W is —CH?CH— Or —CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R2 and R3 are selected from the side chains of a natural or non-natural alpha amino acid, provided that neither R2 nor R3 is hydrogen, or R2 and R3, taken together with the carbon to which they are attached, form a 3-6 membered saturated cycloalkyl or heterocyclyl ring; Y is a bond, —C(C?O)—, —S(?O)2—, —C(C?O)O—, —C(C?O)NR?—, —C(?S)—NR?, —C(?NH)NR? or —S(?O)2NR— wherein R? is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)(Alk2)p— wherein in, n, p, Q, AIk1 and AIk2 are as defined in the claims; X1 represents a bond; —C(?O); or —S(?O)2—; —NR4C(?O)—, —C(C?O)NR4—, —NR4C(?O)NR5—, —NR4S(?O)2—, or —S(?O)2NR4— wherein R4 and R5 are independently hydrogen or optionally substituted C1

Abstract: Compounds of formula (I) described herein are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and are useful for the prevention and/or treatment of an allergic disease state or a disease of the respiratory tract characterized by airway obstruction.

Abstract: Disclosed are sulfonamide compounds of Formula (I): or stereoisomers, N-oxides, prodrugs, or pharmaceutically acceptable salts thereof, wherein ring A, R1, R2, R3, R4 and R5 are defined herein. Also disclosed are methods of using such compounds in the treatment of conditions related to CYP17 enzyme, such as cancer, and pharmaceutical compositions comprising such compounds.

Abstract: The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.

Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.

Abstract: The present invention pertains to an electrode layer comprising a porous film made of oxide semiconductor fine particles sensitized with certain methin dyes. Moreover the present invention pertains to a photoelectric conversion device comprising said electrode layer, a dye sensitized solar cell comprising said photoelectric conversion device and to novel methin dyes.

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, ester or stereoisomer thereof, wherein R1 to R3 and X have the significances given herein. The present invention is also directed to processes for making said compounds and uses of said compounds, in particular their use as medicaments, more particularly their use as medicaments in the treatment of cancer.

Abstract: The present application relates to novel substituted 8-alkoxy-2-aminotetraline derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders.

Abstract: This invention relates to novel 4-trimethylammoniobutyrates of the formula wherein A1, R1, m and n are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit carnitine palmitoyl transferase (CPT) activity, in particular CPT2 activity, and can be used as medicaments.

Abstract: The present invention relates to novel triazole derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests wherein A1, A2, A3, A4, A5, A6, G1, G2, R1, R2, R3, L, Q1, Q2, R4, R5, R6, R7, Q2, Y1, Y2, Y3, Y4, Y5, Y6, Y7, Y8, and Y9 are as defined in claim 1; or salts or N-oxides thereof.

Abstract: Small molecule inhibitors of AGBL2 are provided, as well as methods of using the inhibitors to treat or prevent cancer and neurologic disorders.

Abstract: The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs).

Abstract: Novel biaromatic compounds having the general formula (I): and cosmetic/pharmaceutical compositions comprised thereof are useful in human or veterinary medicine (in dermatology and also in the fields of cardiovascular diseases, of immune diseases and/of diseases related to the metabolism of lipids), or, alternatively, in cosmetic compositions.

Abstract: Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ?CH— or ?N—; W is —CH?CH—Or —CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R2 and R3 are selected from the side chains of a natural or non-natural alpha amino acid, provided that neither R2 nor R3 is hydrogen, or R2 and R3, taken together with the carbon to which they are attached, form a 3-6 membered saturated cycloalkyl or heterocyclyl ring; Y is a bond, —C(?O)—, —S(?O)2—, —C(?O)O—, —C(?O)NR?—, —C(?S)—NR?, —C(?NH)NR? or —S(?O)2NR— wherein R? is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n, p, Q.

Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.

Abstract: An object of the present invention is to provide a medicament and method for treating lissencephaly patients. The present invention provides a lissencephaly therapeutic or preventive agent comprising a compound represented by the general formula (I): wherein R1 is lower alkyl substituted with lower alkoxy, lower alkyl substituted with a heterocyclic group, a heterocyclic group, or a group represented by the formula (IIa): wherein R4 is lower alkyl, R5 is lower alkylene, and m is an integer of 1 to 6; R2 is lower alkyl optionally substituted with phenyl; and R3 is lower alkyl optionally substituted with halogen, lower alkoxy, or phenyl; condensed polycyclic hydrocarbon; or hydrogen.

Abstract: In one aspect, the invention relates to substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.

Abstract: The present application relates to novel substituted 8-alkoxy-2-aminotetraline derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders.

Abstract: Compounds of formula (I) inhibit HDAC activity: wherein A, B and D independently represent ?C— or ?N—; W is a divalent radical —CH?CH— or CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; z is 0 or 1; and Y, L1, and X1 are as defined in the claims.

Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.

Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino 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: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.

Abstract: Heteroaryl(alkyl)dithiocarbamate compounds represented by general formula (I) or their pharmaceutically acceptable salts, their preparing methods, and their uses for preparing antitumor medicines are disclosed, wherein each said substituent is defined as in the description. The compounds are new tyrosine kinase inhibitors useful as an anti-tumor agents, preferably useful in the preparation of medicines for treating breast cancer, liver cancer, non-small cell lung cancer, gastric cancer, colon cancer, leukaemia or nasal cancer.

Abstract: The present invention features compounds of formula I or pharmaceutically acceptable salts, solvates or prodrugs thereof, and methods of using the same to inhibit the metabolizing activities of CYP enzymes. The present invention also features methods of using these compounds, salts, solvates or prodrugs to improve the pharmacokinetics of drugs that are metabolized by CYP enzymes.

Abstract: Process for the preparation of a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R1 and R2 represent H; or either R1 represents ethyl and R2 represents n-hexyloxycarbonyl that applies to industrial scale, novel intermediates useful for the preparation thereof, and processes of preparing said intermediates.

Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.

Abstract: The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.

Abstract: The invention provides a novel class of compounds viz. generally lipopeptides like Pam3CSK4, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 2. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness a vaccine.

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.