Abstract: An N-acyl anthranilic acid derivative represented by general formula (1) or a salt thereof is useful for prevention or treatment of diseases associated with excessive production of collagen. (In the formula, R1 represents a carboxyl group or the like; R2 represents a hydrogen atom or the like; R3 represents an optionally substituted aryl group or the like; X1 represents a carbonyl group; X2 represents a bonding hand; X3 represents a bonding hand; X4 represents a bonding hand or the like; and A represents an optionally substituted phenyl group or the like.

Abstract: The present invention relates to the use of compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, Y, X, and G have the meanings given above as insecticides and/or acaricides and/or fungicides.

Abstract: Disclosed herein are novel benzophenone derivatives represented by formula I, a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof, a pharmacological composition containing the same, and a use of the composition as therapeutic drugs. The benzophenone derivatives have an inhibition activity of microtubule formation and can be used to treat a normal proliferative state of a malignant tumor by killing the actively proliferating cells.

Abstract: The invention relates to substituted aryl-sulphonylglycine derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as in the specification and claims, which are suitable for preparing a pharmaceutical composition for the treatment of metabolic disorders, particularly type 1 or type 2 diabetes mellitus.

Abstract: Tetrahydropyrimidines of the formula where R is a hydrogen atom or a hydrocarbon radical comprising up to eight carbon atoms, R? is hydrogen, OH or OR? and R? is R or COR, with R having the above described significance for use in the prevention or treatment of post-operative inflammatory stresses and pain.

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

Abstract: The present invention relates to compounds of general formula I wherein n, R1, R2, R3, R4, R5, R6, R7 and R8 are defined as stated hereinafter, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.

Abstract: The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer.

Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.

Abstract: The present invention provides a compound of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R9, R10, A and B are as defined in the specification. The present invention also provides pharmaceutical compositions containing the compound of this invention, and methods of treatment using the compound of this invention. The invention also relates to the use of a combination of a compound of this invention and one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus (HIV). The invention further relates to the use of a compound of this invention, alone or in combination with another agent, in the treatment of solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis.

Abstract: The present invention relates to compounds that inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.

Abstract: Chiral liquid crystal compounds of the general formula (1): in which at least one of R1 and R2 is a chiral substituent, K may be a single bond or the same as K1-5 and K1-5 denote a six-membered ring system which rings may be at least partially unsaturated, wherein the number of atoms in these rings or ring systems between the two atoms forming a part of the link to the next ring, or to one of the substituents R1 and R2, does not differ by more than one if counted in the clockwise, and in the counter-clockwise sense, starting from the same atom in each case, X1-20 denote alkyl, or alkoxy, or fluorinated alkyl, or fluorinated alkoxy groups, or atom H, or halogen atoms, mixtures comprising such chiral liquid crystal compounds, and liquid crystal displays comprising such mixtures as active ingredients

Abstract: Compounds are provided according to formula (I), where A, B, W, X?, L, R1, R3, R4b, and m? are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.

Abstract: The present invention relates to the synthesis of a series of ionone and curcumin derivatives as multi-targeting agents effective against both hormone-sensitive and hormone-independent cancers. In particular, the present invention is directed to a distinct class of bifunctional antiandrogens, which inhibit both AR and IKBkinases (IKK). A series of ionone-based chalcones were synthesised and their in vitro cytotoxicity against prostate cancer cell lines were demonstrated. A series of derivatives formed by reacting ionone-based chalcones and hydrazines demonstrate substantial antiproliferative activities in prostate cancer, breast cancer and lung cancer cell lines.

Abstract: The present invention is directed to 4,4-di-substituted piperidine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.

Abstract: This invention relates to sulfur functionalized ionic liquid compounds that are useful in methods of carbon dioxide or sulfur dioxide removal to which they may be applied.

Abstract: Disclosed are highly convergent processes for preparing compounds of formula (I), which compounds are potent active agents for the treatment of hepatitis C virus (HCV) infection: The disclosed processes use SNAr-type coupling reactions between peptidic compounds having a hydroxyproline moiety of the following formula: and halogenated or sulfonated bromoquinoline compounds.

Abstract: Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules. Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition.

Abstract: This invention provides compounds of formula (I): wherein ring A, X1, X2, X3, R2, R4b, R10, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.

Abstract: Cannabinoid derivatives according to formula (I) are disclosed wherein, X, Y, R1, R2, and W can have the definitions provided herein. Without limitation, use of such compounds, their salts or pro-drug, or compositions containing the compounds, salts, or pro-drug, to modify the activity of CB1 and CB2 receptors and treat conditions mediated by these receptors.

Abstract: The present disclosure is generally directed to compounds that can inhibit DAGL? and/or ? activity, compositions comprising such compounds, and methods for inhibiting DAGL? and/or ? activity.

Abstract: The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

Abstract: Provided is a liquid crystal compound having general physical properties necessary for a compound, stability to heat, light or the like, a wide liquid crystal phase temperature range, a high clearing point, an excellent compatibility with other liquid crystal compounds, a large refractive index anisotropy and a large dielectric anisotropy. Provided are a liquid crystal composition including the liquid crystal compound, and a liquid crystal display device containing the liquid crystal composition. The compound is represented by formula (1): wherein, for example, R1 is alkyl having 1 to 20 carbons; at least one of the rings A1 to A6 is pyrimidine-2,5-diyl or pyridine-2,5-diyl and the others are 1,4-cyclohexylene or 1,4-phenylene; Z1 to Z6 are a single bond; L1 to L4 is hydrogen or halogen; X1 is hydrogen, halogen, —C?N or alkyl having 1 to 10 carbons; and l, m, n, o, p and q are 0 or 1 and l+m+n+o+p+q=3.

Abstract: The invention relates to a fungicidally active compound of 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, provided that the ring is not 1,2,3-triazole, the ring being substituted by groups R8, R9 and R10; X is a single or double bond; Y is O, S, N(R11) or (CR12R13)(CR14R15)m(CR16R17)n; m is 0 or 1; n is 0 or 1; and R1 to R17 each, independently, have a range of values; to the preparation of these compounds, to novel intermediates used in the preparation of these compounds, to agrochemical compositions which comprise at least one of the novel compounds as active ingredient, to the preparation of the compositions mentioned and to the use of the active ingredients or compositions in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.

Abstract: The present invention relates to compounds defined by formula I wherein the groups R1 to R3, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.

Abstract: The present invention discloses novel compounds of Formula (I), or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.

Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II); and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B. L1-L4 A, B, R1-R4 and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.

Abstract: The invention relates to an innovative method for synthesis of cyclic amidines. The synthesis starts from a ?-, ?- or ?-lactone which is twofold brominated. After esterification of the carboxyl function, the bromine atoms are nucleophilically substituted and the corresponding diamino compound is obtained. The ring closure to the cyclic amidine is accomplished subsequently by reaction with orthoester, imidate or thioimidate. Owing to interposing additional steps for recovery of the diamino compound in enantiomerically pure form, the enantiomers of the cyclic amidines can be stereoselectively synthesized.

Abstract: The present invention provides compounds and methods for antagonizing the anticoagulant effect of an anticoagulant agent that is selected from UFH, LMWH, and a heparin/LMWH derivative in a patient comprising administering to the patient a compound of the invention or a salt thereof, or a composition comprising the same.

Abstract: The invention relates to substituted phenoxyacetic acids (I) as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.

Abstract: The invention relates to novel compounds which comprise, as cationic or as anionic component, a pyrimidinecarboxylic acid derivative, in particular a derivative of ectoin or hydroxyectoin, to a process for the preparation thereof, and to the use thereof as ionic liquid or to the use thereof in pharmaceutical, cosmetic and dermatological formulations.

Abstract: The invention relates to compounds of the formula (I) where: R is a (C1-C6)alkyl group, a halo(C1-C6)alkyl group; R1 is a hydrogen atom; R2 is a heteroaromatic group or a heteroaromatic(C1-C4)alkyl group, said groups being optionally substituted; R3 and R4 represent independently from each other an optionally substituted phenyl group; Y is a hydrogen atom, a halogen, a cyano, a (C1-C6)alkyl group, a halo(C1-C6)alkyl group, a (C1-C6)alkoxy group, a halo(C1-C6)alkoxy group or a (C1-C6)alkylS(O)p group; and p is 0 to 2. Said compounds can be in the form— of a base or a salt for addition to an acid. The invention also relates to a method for preparing same and to the therapeutic application thereof.

Abstract: Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.

Abstract: Indoles that have activity as inhibitors of FAAH are described as are indoles and indole derivatives that have activity as inhibitors of DAO.

Abstract: The present invention is directed to immune adjuvants containing IAP inhibitors, including Smac mimetics. The invention further provides pharmaceutical compositions and vaccines containing an IAP inhibitor and an antigen. Methods of enhancing an immune response by administration of an IAP inhibitor, methods of treating or preventing cancer, methods of treating or preventing infections, methods of treating autoimmune disorders, and methods of potentiating cytokine or antibody production are also provided.

Abstract: Aspects of the present invention relate to compounds and methods useful in modulating angiogenesis and methods of treating or preventing diseases associated with angiogenesis by administering a polycationic compound. The present invention relates to methods of use and compositions for inhibiting angiogenesis-mediated disorders in mammals including animals and humans. Additionally, this invention relates to the combined use of polycations with other anti-angiogenesis agents for the treatment of different angiogenesis-mediated disorders. Additionally, those polycationic compounds can be used with various anti-inflammatory and cytotoxic agents as well as with radio-therapeutic agents in cancer patients to prevent and treat tumor growth and metastasis.

Abstract: The present invention relates to novel derivatives of substituted benzylamines, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.

Abstract: There is provided a fluorine-containing organosulfur compound having an excellent control effect on harmful arthropods, which is represented by the formula (I): wherein m represents 0 or 1; n represents 0, 1 or 2; A represents an optionally substituted 6-membered aromatic heterocyclic group; R1 to R4 are the same or different and represent a hydrogen atom, a C1-C4 chain hydrocarbon group optionally substituted with a halogen atom, etc.; and Q represents a C1-C5 haloalkyl group containing at least one fluorine atom, or a fluorine atom.

Abstract: Disclosed are compounds of formula (I) and compositions of the present invention which are inhibitors of the sodium proton exchanger isoform-1 (NHE-I). Also disclosed are methods of using and making the same.

Abstract: Novel 3?-deoxy-3?-acylaminospectinomycin compounds are described. Also described are methods of using the 3?-deoxy-3-acylaminospectinomycin compounds and other spectinomycin analogs in treating tuberculosis and in treating microbial infections.

Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.

Abstract: The invention provides a liquid crystal compound which has stability to heat, light and so forth, a nematic phase in a wide temperature range, a small viscosity, a large optical anisotropy, and a suitable elastic constant K33, and further has a suitable and negative dielectric anisotropy and an excellent compatibility with other liquid crystal compounds. Moreover, the invention provides a liquid crystal composition comprising this liquid crystal compound and a liquid crystal display device containing this liquid crystal composition. A liquid crystal compound represented by formula (a): for example, R1 and R2 are alkyl having 1 to 10 carbons, alkenyl having 2 to 10 carbons or alkoxy having 1 to 9 carbons; ring A1 and ring A2 are 1,4-phenylene or trans-1,4-cyclohexylene; L1 and L2 are hydrogen or fluorine, and at least one of L1 and L2 is fluorine; and Z1 and Z2 are a single bond, —(CH2)2—, —CH?CH—, —CH2O— or —OCH2—.

Abstract: The present invention relates to substituted pyrimidine derivatives of as well as N-oxides and agriculturally acceptable salts thereof, and their use to control undesired plant growth, in particular in crops of useful plants. The invention extends to herbicidal compositions comprising such compounds, N-oxides and/or salts as well as mixtures of the same with one or more further active ingredient (such as, for example, an herbicide, fungicide, insecticide and/or plant growth regulator) and/or a safener.

Abstract: Compounds are provided according to formula 1: where A, B, W, X?, L, R1, R3, R4b, and m? are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.

Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof, processes for preparing such compounds, their use as GPR119 modulators, methods for their therapeutic use, particularly in the treatment of obesity and diabetes mellitus, and pharmaceutical compositions containing them.

Abstract: Topical cream, ointment, lotion, gel, foam formulations and slow release formulations or devices are provided including certain CCR5 antagonists as prophylactics for the prevention, retardation or inhibition of transmission of Human Immunodeficiency Virus (HIV) infection from one human to another.

Abstract: Carboxylic acid derivatives where R-R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.

Abstract: Carboxylic acid derivatives where R-R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.

Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.