Abstract: The present invention relates to compounds of formula IV and their use.

Abstract: The present invention is related to new 3,3-disubstituted indol-2-one derivatives of the general Formula (I) The new compounds are useful for the treatment or prophylaxis of the central nervous system, the gastrointestinal system or the cardiovascular system.

Abstract: The present invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined for formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.

Abstract: The present invention include providing a therapeutically effective amount of a 3-substituted indolin-2-one compositions to protect against neurodegeneration including diseases such as Alzheimer's disease, Parkinson's disease, or Huntington's disease, and conditions such as ischemic stroke

Abstract: Methods for preparing oxindole and thio-oxindole compounds are provided, which compounds are useful as precursors to useful pharmaceutical compounds. Specifically provided are methods for preparing 5-pyrrole-3,3-oxindole compounds and 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile. Also provided are methods for preparing iminobenzo[b]thiophene and benzo[b]thiophenone compounds.

Abstract: Novel compounds of structural formula (I) are disclosed. As modulators of the Cannabinoid-1 (CB1) receptor, these compounds are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. As such, compounds of the present invention are useful as in the treatment, prevention and suppression of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders (e.g., multiple sclerosis, Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis), cerebral vascular accidents, head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, particularly to opiates, alcohol, and nicotine. The compounds are also useful for the treatment of obesity or eating disorders associated with excessive food intake and complications associated therewith.

Abstract: The present invention is directed to compounds that are allosteric inhibitors of tumor necrosis factor receptor I, compositions comprising such compounds, and methods of using such compounds and compositions thereof in the treatment of TNF-? mediated conditions.

Abstract: Transglutaminase inhibitors and methods of use thereof are provided.

Abstract: The present invention relates to drug delivery systems comprising ocular implant, which include organic molecules, capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation, in combination with a polymer, which polymer serves to control, modify, modulate and/or slow the release of the therapeutic component into the environment of the eye in which said composite is placed.

Abstract: The invention describes compounds of the general formula I or the pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are herein described, a process for their manufacture, medicaments containing them as well as the use of these compounds as pharmaceutically active agents. The compounds show activity as antiproliferative agents and may be especially useful for the treatment of cancer.

Abstract: The present invention relates to indolinone derivatives, substituted in the 6-position, of the formula in which R1 to R6 and X are as defined in Claim 1, to their tautomers, enantiomers, diastereomers, to their mixtures and to their salts, in particular their physiologically acceptable salts, which have useful pharmacological properties, in particular in inhibiting action on various receptor tyrosine kinases and on the proliferation of endothelial cells and various tumour cells, to medicaments comprising these compounds, to their use and to processes for their preparation.

Abstract: Methods and compositions to treat edematous ocular, otic and nasal conditions are described.

Abstract: Provided herein are isolated compounds of formula 1: processes for their preparation and isolation, as well as pharmaceutical compositions which comprise these therapeutic agents, and methods of use therefore the treatment and/or control of conditions associated with or mediated by effects of histone deacetylase.

Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.

Abstract: The present invention relates to alkyl-containing 5-acylindolinones of general formula wherein R1 to R3 are defined herein, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on protein kinases, particularly an inhibiting effect on the activity of glycogen synthase kinase (GSK-3).

Abstract: This invention is directed to indolone derivatives which are antagonists or the GALR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier.

Abstract: The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders.

Abstract: This invention relates to selenophene compounds of formula (I) shown below: Each variable in formula (I) is defined in the specification. These compounds can be used to treat cancer.

Abstract: The present invention relates to indolinone derivatives, substituted in the 6-position, of the formula in which R1 to R6 and X are as defined in claim 1, to their tautomers, enantiomers, diastereomers, to their mixtures and to their salts, in particular their physiologically acceptable salts, which have useful pharmacological properties, in particular in inhibiting action on various receptor tyrosine kinases and on the proliferation of endothelial cells and various tumour cells, to medicaments comprising these compounds, to their use and to processes for their preparation.

Abstract: The present invention relates to substituted indoles of Formula (I) useful as pharmaceutical compounds for treating respiratory disorders.

Abstract: The present invention is directed to the prevention, reversal and medical treatment of dystonia and dyskinesia as well as other diseases related to movement disorders, both in human beings and animals by administering a neuronal potassium channel opener such as flupirtine, retigabine or maxipost.

Abstract: The present invention relates to the use of specific benzimidazolone analogues and derivatives to inhibit the cytokine or biological activity of macrophage migration inhibitory factor (MIF), and diseases or conditions wherein MIF cytokine or biological activity is implicated. Novel benzimidazole analogues and derivatives are also provided.

Abstract: N-arylsulfonyl-3-aminoalkoxyindoles indole compounds, radioisotopes, stereoisomers, geometric forms, N-oxides, polymorphs and pharmaceutically acceptable salts.

Abstract: Disclosed is a compound represented by the formula (1) below, a prodrug thereof or a pharmaceutically acceptable salt of either, which is useful as a therapeutic, preventive or ameliorating agent for diabetes and the like. (In the formula, R3 represents an optionally substituted carbamoyl group or the like; X represents a hydroxyl group or the like; W1 and W2 independently represent a single bond or methylene; R7 and R8 independently represent a hydrogen atom, an optionally substituted alkyl group or the like; and Ar represents an optionally substituted aryl group or the like.

Abstract: The present invention relates to oxindoles of the formula I, their use as protein kinase activators or inhibitors, a method for their manufacture, their use for the preparation of a medicament for the treatment of diseases and their use for the manufacture of a pharmaceutical composition.

Abstract: Certain 1H-indole-2-carboxylates and -2-carboxamides are HIV reverse transcriptase inhibitors. These indole compounds and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Abstract: The use of an arylidene 2-indolinone derivative for treating tumors involving Met, PDGF-R, FGF-RI, FGF-R3 or Kit tyrosine kinases, or a Ret oncoprotein which includes a MEN2-associated mutation is disclosed.

Abstract: The present invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined for formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.

Abstract: The present invention encompasses compounds of general formula (1) wherein R1, R2, R3 and X are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.

Abstract: The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

Abstract: Compounds of the general formula (I): pharmaceutical compositions comprising a compound of general formula (I); and methods of treating disease conditions caused by overactivation of the VR1 receptor by administering a compound of general formula (I) to a subject.

Abstract: The present invention discloses and claims methods for the treatment of a patient suffering from a disease or disorder ameliorated by inhibition of casein kinase I? activity comprising the administration of a compounds of formula (I) and formula (II) as inhibitors of human casein kinase I?, and methods of using said compounds of formula (I) and formula (II) for treating central nervous system diseases and disorders including mood disorders and sleep disorders. The R-group substituents are defined herein and pharmaceutical compositions comprising compounds of formula (I) or formula (II) useful in the claimed methods of treatment are also disclosed.

Abstract: The present application describes deuterium-enriched ropinirole, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.

Abstract: The present invention a method of treating anxiety by administering compounds that are active on the GABAB receptor, having formula I: wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification and claims.

Abstract: The present invention provides a new medical use for the compounds of the formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prodrugs thereof, as MAO-A inhibitors. Also included is a method for prophylaxis and treatment of mental disorders such as depression, in a mammal, comprising administering an effective amount of a compound of formula (I). These compounds are also effective in treating a disease, condition or disorder such as weight loss, obesity, bulimia, depression, bipolar disorders, psychoses, schizophrenia, behaviors, alcoholism, tobacco abuse, memory loss, Alzheimer's disease, dementia of aging, seizure disorders, epilepsy, attention deficit disorder, and Parkinson's disease, which is modulated by a cannabinoid receptor antagonist.

Abstract: The novel sustained release dosage form comprising an active agent and a combination of a non-swelling pH dependent release retardant and a non swelling pH independent release retardant polymer which provides pH-independent drug release for a considerable period of time after administration.

Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, and Pichinde), Filoviridae (Ebola and Marburg viruses), Flaviviridae (yellow fever, Omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).

Abstract: The present invention is directed to pesticidal compositions comprising indole derivatives. These indole derivatives are especially active against phytopathogenic fungi. Furthermore, the invention relates to the use of indole derivatives for the production of pesticides and the use of the compositions according to the invention as pesticides. The present invention is also directed to a process for producing a pesticidal composition and to pesticidal compositions prepared by this process. In addition, the invention relates to a process for preventing or combating pests and to a process for protecting plants against pests, especially against phytopathogenic fungi. Further, the invention is directed to plants or seeds as well as objects or materials which have been protected against pests by treatment with a composition according to the invention. Further, the invention is directed to a method for identifying a substance having pesticidal activity.

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.

Abstract: The present invention relates to indolone derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

Abstract: The present invention relates to a method of treating cellular proliferative diseases, in particular cancer, which comprises administering a modulator of the activity of the mitotic kinesin KSP, wherein the activity of the KSP modulator is dependent on the presence of microtubules. It is believed that the KSP modulators utilized in the instant method bind to the KSP protein in a previously unreported manner, since the compounds do not bind competitively with respect to either microtubules or ATP, the substrates of KSP. The modulators useful in the instant methods are furthermore not active against the non-microtubule stimulated activity of KSP. Cellular proliferative diseases that may be treated using the method disclosed herein are, for example cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation.

Abstract: The present invention relates to novel tyrosine derivatives of formula (I), their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention more particularly provides novel tyrosine derivatives of the general formula (I).

Abstract: A medicament having inhibitory activity against NF-?B activation, which comprises a compound represented by the following general formula (I) or a pharmacologically acceptable salt as an active ingredient: wherein X represents a connecting group, A represents hydrogen atom or acetyl group, E represents an aryl group or a heteroaryl group, and ring X represents an arene or a heteroarene.

Abstract: This invention is directed to pyrimidine and indolone derivatives which are selective antagonists for the GAL3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety.

Abstract: Provided herein is a method of protecting a neuron from dysfunction induced by an HIV neurotoxin, comprising contacting the cell with a therapeutically effective dose of a dopamine D1 receptor agonist. Also provided is a method of treating or preventing HIV-1 associated dementia (HAD) in a subject in need of such treatment or prevention, comprising administering to the subject a therapeutically effective dose of a dopamine D1 receptor agonist and estrogenic compound.

Abstract: This invention pertains to a multi-layered tablet for a triple combination release of active agents to an environment of use. More particularly, the invention pertains to a multi-layered tablet (1) comprising two external drug-containing layers (2 and 3) in stacked arrangement with respect to and on opposite sides of an oral dosage form (4) that provides a triple combination release of at least one active agent. In one embodiment of the invention the dosage form is an osmotic device. In another embodiment of the invention the dosage form is a gastro-resistant coated core. In yet another embodiment of the invention the dosage form is a matrix tablet. In a different embodiment the dosage form is a hard capsule.

Abstract: Disclosed herein is a method for preventing ovarian hyperstimulation syndrome in a subject by administering an effective amount of a dopamine agonist in a pharmaceutically acceptable carrier. Also disclosed herein is a method for treating ovarian hyperstimulation syndrome by administering an effective amount of a dopamine agonist in a pharmaceutically acceptable carrier.

Abstract: Novel compounds of structural formula (I) are disclosed. As modulators of the Cannabinoid-1 (CB1) receptor, these compounds are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. As such, compounds of the present invention are useful as in the treatment, prevention and suppression of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders (e.g., multiple sclerosis, Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis), cerebral vascular accidents, head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, particularly to opiates, alcohol, and nicotine. The compounds are also useful for the treatment of obesity or eating disorders associated with excessive food intake and complications associated therewith.

Abstract: Compounds of formula Ia or Ib wherein P; R1; R2; m; and n are as defined in the application, salts thereof, processed for their preparation, new intermediates used therein, pharmaceutical formulations containing said compounds and the use of said compounds in therapy.