Abstract: The invention relates to isoindolones of formula, (I) with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

Abstract: The invention relates to novel 2,4,6-phenyl-substituted cyclic ketoenols of the formula (I), in which CKE, W, X and Y are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising firstly the 2,4,6-phenyl-substituted cyclic ketoenols and secondly at least one compound which improves crop plant tolerance.

Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.

Abstract: The present invention relates to compounds of formula (I) comprising a lactam or a lactam derivative moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as pharmaceuticals.

Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.

Abstract: This invention is directed to spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.

Abstract: The present invention provides spirolactam derivatives of formula (I): wherein R1-R7 are as defined herein; or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and uses of the same.

Abstract: The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts thereof. The are useful as HSL inhibitors and may, for example, be used in treatment of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis, and obesity.

Abstract: The present invention relates to novel 4?4?-dioxaspiro-spirocyclically substituted tetramates of the formula (I) in which A, B, G, m, n, W, X, Y and Z to a plurality of processes for their preparation and to their use as pesticides and/or herbicides. The invention also provides selectively herbicidal compositions comprising firstly the 4?4?-dioxaspiro-spirocyclically substituted tetramates and secondly a crop plant compatibility-improving compound. The present invention also relates to novel water-soluble concentrates of 4?4?-dioxaspiro-spirocyclically substituted tetramates and their enols, to processes for preparing these formulations and to their use as pesticides and/or herbicides.

Abstract: This invention is directed to pharmaceutical compositions for oral administration to a mammal, wherein the pharmaceutical compositions comprise a spiro-oxindole compound, as a single stereoisomer or as a mixture thereof, or a pharmaceutically acceptable salt thereof. These pharmaceutical compositions are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

Abstract: The present invention relates to novel C2-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y, Z and CKE are as defined in the description, to processes for their preparation and to their use as pesticides and herbicides.

Abstract: The present invention relates to the use of known cyclic ketoenols against phytopathogenic bacteria.

Abstract: The present invention relates to compounds of the following formula (I) that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).

Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and Q have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the Al adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurological disease or injury; sleep disorder; epilepsy; and depression.

Abstract: The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The novel active compound combinations comprising a compound of the formula (I) or (II) and the active compounds (1) to (6) listed in the description have very good insecticidal and acaricidal properties.

Abstract: This invention provides a progesterone receptor antagonist of formula 1 having the structure wherein, T is O, S, or absent; R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl; or R1 and R2 are taken together form a ring and together contain —CH2(CH2)nCH2—, —CH2CH2CMe2CH2CH2—, —O(CH2)pCH2—, —O(CH2)qO—, —CH2CH2OCH2CH2—, or —CH2CH2NR7CH2CH2—; n=1-5; p=1-4; q=1-4; R3 is hydrogen, OH, NH2, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or CORA; RA is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R4 is hydrogen, halogen, CN, NH2, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R5 is hydrogen, alkyl, or substituted alkyl; R6 is hydrogen, alkyl, substituted alkyl, or CORB; RB is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R7 is hydrogen or alkyl; or a pharmaceutically acceptable salt thereof.

Abstract: This invention is directed to spiroheterocyclic compounds of formula (I): wherein k, j, p, Q, R1, R3a, R3b, R3e, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, that are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of using the compounds are also disclosed.

Abstract: The invention relates to the use of compounds which exhibit an affinity for the ?-opioid receptor of at least 100 nM (Ki value, human) and an affinity for the ORL-1 receptor, wherein the ratio between the affinities ORL1/?defined as 1/[Ki(ORL1)/Ki(?)] is from 0.1 to 30, for the treatment of pain.

Abstract: Novel oil-based suspension concentrates consisting of at least one compound, solid at room temperature, of the formula (I), at least one penetrant, at least one vegetable oil, at least one nonionic surfactant and/or at least one anionic surfactant and optionally one or more additives from the groups of the emulsifiers, the antifoams, the preservatives, the antioxidants, the colorants and/or the inert fillers, a process for preparing these suspension concentrates and their use for applying the active compounds comprised therein to plants and/or their habitat and for controlling insects.

Abstract: This invention is directed to the (S)-enantiomer of the compound of formula (I): or a pharmaceutically acceptable solvate or prodrug thereof. This (S)-enantiomer is useful for the treatment of diseases or conditions, such as pain, which are ameliorated or alleviated by the modulation of voltage-gated sodium channels.

Abstract: Compounds of formula (I), pharmaceutical compositions thereof, and methods for treatment using the same.

Abstract: An object of the present invention is to provide a novel and excellent agent for treating or preventing dementia, schizophrenia and the like, based on the 5-HT5A receptor modulating action. It was confirmed that a compound characterized by a structure that a tricyclic hetero ring having a pyrrole ring at the center and guanidine are bonded via a carbonyl group has a potent 5-HT5A receptor modulating action and an excellent pharmacological action based thereon, and thus, it was found that the compound can be an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder, or attention deficit hyperactivity disorder, particularly for memory-related functional disorders such as cognitive impairments including dementia and schizophrenia, thereby completing the present invention.

Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).

Abstract: The invention relates to a method for improving the utilization of the production potential of transgenic plants. In the last years, there has been a marked increase in the proportion of transgenic plants in agriculture, even if regional differences are still noticeable to date. Thus, for example, the proportion of transgenic maize in the USA has doubled from 26% to 52% since 2001, while transgenic maize has hardly been of any practical importance in Germany. However, in other European countries, for example in Spain, the proportion of transgenic maize is already about 12%.

Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.

Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, for treating diseases and conditions of the central nervous system (CNS), in particular sleep disorders.

Abstract: The novel active compound combinations comprising compounds of the formulae (I) and (II) have very good insecticidal and acaricidal properties.

Abstract: The present application relates to the use of tetramic acid derivatives for controlling soil-dwelling nematodes.

Abstract: Methods for promoting osteogenesis to accelerate or enhance bone fracture healing, treat bone defects, and enhance bone formation are disclosed. The methods modulate an arachidonic acid metabolic or signaling pathway in general, and, in particular, utilize 5-lipoxygenase inhibitors. These molecules can be delivered alone or in combination with one or more agents that inhibit bone resorption, regulate calcium resorption from bone, enhance bone accumulation, enhance bone formation, induce bone formation, impair growth of microorganisms, reduce inflammation, and/or reduce pain.

Abstract: The invention relates to novel haloalkoxyspirocyclic tetramic and tetronic acid derivatives of the formula (I) in which W, X, Y, Z, A, D, Q1, Q2, m and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. Moreover, the invention provides selective herbicidal compositions comprising, firstly, haloalkoxyspirocyclic tetramic and tetronic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to increasing the action of crop protection compositions comprising compounds of the formula (I) through the addition of ammonium salts or phosphonium salts and optionally penetrants.

Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.

Abstract: The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention.

Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).

Abstract: Compounds of the formulae (I) and (II) for controlling pathogens by drenching or drip application.

Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.

Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A, B and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. The invention also provides selective herbicidal compositions comprising, firstly, geminally alkoxy/alkylspirocyclically substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the addition of ammonium salts or phosphonium salts and optionally penetrants.

Abstract: Briefly described, embodiments of this disclosure include compositions, pharmaceutical compositions, methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of identifying a candidate agent for the treatment of hepatitis C virus (HCV) infection, and the like.

Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.

Abstract: The present invention relates to the use of tetramic acid derivatives on their own and also of active compound combinations comprising, firstly, known tetramic acid derivatives and, secondly, further known insecticidal active compounds for controlling viroses transferred by insects.

Abstract: The invention relates to quaternary ?-aminocarboxyamide derivatives of formula (I), wherein R1, R2, R3, R4, R5, R6, X, q and n are as defined in claim 1, for treating diseases and conditions mediated by modulation of voltage-gated sodium channels.

Abstract: The present invention relates to novel intermediates used in the preparation of substituted spirocyclic ketoenols of the formula (I) in which W, X, Y, Z, A, B, D and G are as defined in the disclosure.

Abstract: The invention provides for compositions and methods of reducing pain in a subject by administering a combination of mu-opioid receptor agonist, kappa1-opioid receptor agonist and a nonselective opioid receptor antagonist in amounts effective to reduce pain and ameliorate an adverse side effect of treatment combining opioid-receptor agonists. The invention also provides for methods of enhancing an analgesic effect of treatment with an opioid-receptor agonist in a subject suffering from pain while reducing an adverse side effect of the treatment. The invention also provides for methods of reducing the hyperalgesic effect of treatment with an opioid-receptor agonist in a subject suffering from pain while reducing an adverse side effect of the treatment. The invention further provides for methods of promoting the additive analgesia of pain treatment with an opioid-receptor agonist in a subject in need while reducing an adverse side effect of the treatment.

Abstract: A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum (Cmin) and maximum (Cmax) blood levels of about 0.5-2.5 ng/ml and about 2.0-6.0 ng/ml, respectively.

Abstract: A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum (Cmin) and maximum (Cmax) blood levels of about 0.5-2.5 ng/ml and about 2.0-6.0 ng/ml, respectively.

Abstract: The present invention is directed to novel tetracyclic heteroatom containing derivatives, pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more sex steroid hormone receptors and processes for their preparation.

Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.

Abstract: The novel active compound combinations comprising a compound of the formula (I-1) or (I-2) and the active compounds (1) to (26) listed in the description have very good insecticidal and acaricidal properties.

Abstract: The present invention provides methods of treating rheumatoid arthritis. The methods generally involve an intermittent dosing strategy for administering Atiprimod alone or in combination with a second therapeutic agent wherein the second therapeutic agent is selected from the group consisting of Methotrexate, gold compounds, antimalarials, cyclosporine A, leflunomide, azathioprine, sulfasalazine d-penicillamine, aurothioglucose, auranofin, or a TNF inhibitor.