Abstract: The present invention relates to the use of indolinones of general formula substituted in the 6 position, wherein R1 to R5 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof, as a medicament for the prevention or treatment of specific fibrotic diseases.

Abstract: Some embodiments include compositions and methods of using or identifying compounds that modulate the activity of the granulocyte colony-stimulating factor receptor (GCFR). Some embodiments include use of compounds to treat certain disorders, such as hematopoietic or neurological disorders.

Abstract: Indolyl or indolinyl compounds of formula (I): wherein bond, n, R1, R2, R3, R4, R5, and R6, are defined herein. Also disclosed is a method for treating cancer with these compounds.

Abstract: The present invention provides compounds of formula (I), as well as pharmaceutically acceptable salt thereof, wherein R1 to R7 have the significance given herein. The compounds are useful in the treatment of prophylaxis of diseases that are related to AMPK regulation.

Abstract: Compositions and methods are provided that utilize an injectable ropinirole having a therapeutically effective amount of ropinirole in an aqueous solvent, the composition having a pH of from about 3.0 to about 6.5. The compositions and methods provided contain less than 3% by weight of impurities and are suitable for administration by infusion pumps. In some embodiments, the compositions are made in an oxygen free environment and/or are made with an antioxidant to reduce impurities and improve stability. In some embodiments, the compositions provided are utilized to treat Parkinson's disease.

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.

Abstract: Treating Sonic Hedgehog-Associated Medulloblastoma comprises inhibiting the synthesis or biologic activity of leukotrienes that drive Nestin expression in cancerous or precancerous granule neuron precursors and that further drive growth and proliferation of medulloblastoma cells through Nestin-mediated aberrant Sonic Hedgehog signaling.

Abstract: The present invention provides a method of using indole-ketone or indolidone to treat or prevent a neurodegenerative disease or disorder. In one embodiment, the neurodegenerative disease is Parkinson's disease. In another embodiment, the neurodegenerative disease or disorder is associated with excessive neuronal Nitric Oxide Synthase (nNOS) activity. Examples of indole-ketone include, but are not limited to, SU4312, SU5416, SU11248 (Sunitinib), and indirubin-3-oxime.

Abstract: Provided herein are inhibitors of HDAC3, as well as methods of treatment comprising administering those compounds to a subject in need thereof.

Abstract: The disclosure relates to TAK1 inhibitors, compositions, and uses related thereto. In certain embodiments, the disclosure relates to compounds of formula (I), pharmaceutical compositions having a compound of formula (I), and methods of treating or preventing cancer by administering an effective amount of a pharmaceutical composition having a compound of formula (I) to a subject in need thereof.

Abstract: The present invention provides a method of inhibiting, suppressing or preventing levodopa-induced dyskinesia in a patient suffering from Parkinson's Disease, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention. The present invention further provides a method of inhibiting, suppressing or preventing Parkinson's Disease in a patient, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention.

Abstract: Biodegradable implants comprising dopamine modulating compounds are described.

Abstract: The present invention relates to a composition comprising a maxi-K potassium channel opener the use in the treatment of fragile X syndrome. More specifically the present invention relates to a composition comprising a fluoro-oxindole or a chloro-oxindole for use in the treatment of fragile X syndrome.

Abstract: Some embodiments of this invention include methods for treating disease and methods for administering a compound of Formula (I). In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of Formula (I). Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I).

Abstract: The present invention provides compounds of formula (I), as well as pharmaceutically acceptable salt thereof, wherein R1 to R7 have the significance given herein. The compounds are useful in the treatment of prophylaxis of diseases that are related to AMPK regulation.

Abstract: The invention describes anti-cancer therapies comprising using dual Aurora kinase/MEK inhibitors as described herein.

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: There are provided substituted 3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide derivatives (I) which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.

Abstract: The present invention relates to the C-13 molecule (methyl 2-{5-[(3-benzyl-4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]-2-furyl}-benzoate) and to organic molecules functionally equivalent to the C-13 molecule, capable of inhibiting the binding of an antibody or antibody fragment with the human Syk protein tyrosine kinase, to the use of these molecules for the production of medicaments for the prevention or treatment of diseases dependent on metabolic pathways involving Syk, and also to a method for identifying such molecules.

Abstract: Methods for restoring normal patterns of activity in a subject suffering from Parkinson's Disease are disclosed that include administering an effective steady state concentration of a dopamine modulating compound continuously for a prolonged period of time such that normal patterns of activity are substantially restored in the subject.

Abstract: A ropinirole-containing patch comprises an adhesive agent layer and a support layer, the adhesive agent layer containing ropinirole and/or a pharmaceutically acceptable salt thereof, wherein a content of the ropinirole and/or the pharmaceutically acceptable salt thereof in terms of free ropinirole in the adhesive agent layer satisfies the following two conditions: 5 to 13.2% by mass relative to a total mass of the adhesive agent layer, and 0.12 to 2.7 mg/cm2 per unit area of the adhesive agent layer.

Abstract: Biodegradable implants comprising dopamine modulating compounds are described.

Abstract: The present invention relates to the use of indolinones of general formula substituted in the 6 position, wherein R1 to R6 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof, as a medicament for the prevention or treatment of specific fibrotic diseases.

Abstract: The present invention relates to an amide compound or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition comprising the same. The inventive amide compound facilitates bone formation and inhibits bone loss, and is therefore useful for preventing and treating bone disorders such as osteoporosis, osteodystrophy, bone fracture, periodontal disease, Paget's disease, bone metastasis, and rheumatoid arthritis.

Abstract: Disclosed herein are methods of treating cancer by administering to a patient a small molecule inhibitor of Survivin. Also disclosed herein are methods of inhibiting Survivin dimerization in a patient by administering a compound of formula (I), (II), (III), or (IV). Methods of inducing cell cycle arrest in cancer cells, comprising G2/M stage arrest, in a patient by administering a compound of formula (I), (II), (III), or (IV) are also disclosed. Further disclosed herein are methods of inducing apoptosis in cancer cells in a patient by administering a compound of formula (I), (II), (III), or (IV).

Abstract: The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, or especially of amides of the formula II, wherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.

Abstract: A ropinirole-containing patch comprises an adhesive agent layer and a support layer, the adhesive agent layer containing ropinirole and/or a pharmaceutically acceptable salt thereof, wherein a content of the ropinirole and/or the pharmaceutically acceptable salt thereof in terms of free ropinirole in the adhesive agent layer is 5 to 13.2% by mass relative to a total mass of the adhesive agent layer.

Abstract: Methods for treating cancer using compounds that inhibit human DNA ligases. Methods for using compounds that inhibit human DNA ligases to provide insights into the reaction mechanisms of human DNA ligases, for example to identify the human DNA ligase involved in different DNA repair pathways. Screening methods for compounds that inhibit human DNA ligases.

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: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerization inhibitors.

Abstract: A polymer comprising at least one type of repeat unit comprising at least one type of an optionally substituted indolocarbazole moiety and at least one divalent linkage.

Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R5 and R6 are as defined in the specification.

Abstract: Composition for controlling phytopathogens comprising compound of the formula: wherein: R1 represents H, or a CO—R? acyl group; R2, the same or different when n is equal to 2, is a halogen, optionally selected from fluorine, chlorine, bromine or iodine; a C1-C9 alkyl group; a C1-C9 haloalkyl group; a C1-C9 alkoxyl group; a C1-C9 haloalkoxyl group; a C1-C9 thioalkyl group; a C1-C9 halothioalkyl group; a C3-C9 cycloalkyl group; a C2-C10 carboalkoxyl group; a cyano group; a hydroxyl group; R? represents a hydrogen; a C1-C9 alkyl group; a C1-C9 haloalkyl group; a C1-C9 alkoxyl group; a C1-C9 haloalkoxyl group; a C2-C10 carboalkoxyl group; a phenyl group; n is a number ranging from 0 to 2; X represents an oxygen atom, a nitrogen or sulfur atom in combination with a fungicide; method for controlling phytopathogens with compound of formula (1) with or without another fungicide.

Abstract: The invention describes dual Aurora kinase/MEK inhibitors and their use in therapy.

Abstract: A crystalline form of 3-{3-[1-(4-Dimethylaminomethyl-phenylamino)-1-phenyl-meth-(Z)-ylidene]-2-oxo-2,3-dihydro-1H-indol-6-yl}-propynoic acid ethylamide.

Abstract: The present invention relates to methods for preventing the development of cancer or neurodegenerative diseases by administering N-Acetylcysteine (NAC), melatonin, or a combination thereof. The present invention also relates to methods for diagnosing cancer and/or neurdegenerative disease by detecting or determining the amount of dopamine metabolites, 4-CE, 2-CE, methylation of CE or CE-Q conjugates.

Abstract: This disclosure relates to compounds and compositions for forming bone and methods related thereto. In certain embodiments, the disclosure relates to methods of forming bone comprising implanting a bone graft composition comprising a growth factor such as BMP in a subject at a site of desired bone growth or enhancement in combination with a JAB1 blocker.

Abstract: Compounds of Formula I wherein the substituents are as defined in Claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as agrochemical active ingredients and can be prepared in a manner known per se.

Abstract: A novel class of indoline-2-one derivatives are disclosed. These compounds are protein kinase inhibitors which are useful for treating hyperproliferative diseases such as cancer.

Abstract: The present invention includes compositions and methods for treating disorders of the skin or mucosa resulting from cancer therapies comprising: identifying a patient receiving cancer treatment; and administering to said patient an effective dose of a treated organic/inorganic complex material with an organic dye molecule or derivative thereof, in a pharmaceutically acceptable carrier.

Abstract: The invention relates to new 3?-, 7-substituted-indirubins of formula (I) wherein R represents N—OH, N—O-alkyl or N—O—CO-alkyl, NO—(Ra)n1-Het, N—O—(Y)n1—N Ra Rb, N—O—CO—N(Rb Rc), radical with Het representing an aliphatic nitrogeneous heterocycle, Y being an optionally substituted —CH2— radical, n1 being 1 to 3, and X is an halogen atom selected in the group comprising F, Cl, Br, I, and Z is H or CH3 and the salts thereof.

Abstract: Described herein are methods for improving engraftment of hematopoietic cells in an individual following hematopoietic progenitor cell transplantation (e.g., via bone marrow or cord blood transplantation). Methods for increasing hematopoietic progenitor cell proliferation in individuals with bone marrow aplasia are also described. The methods involve administering an agent that inhibits adipogenesis, adipocyte growth, adipocyte differentiation and/or adipocyte proliferation.

Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R5 to R10, A, L1, B, m and p are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and their use as medicaments.

Abstract: One aspect of the invention relates to novel isatin derivative compounds and the pharmaceutical composition thereof. Another aspect of the invention relates to methods of using the isatin derivative compounds disclosed herein and the pharmaceutical compositions thereof. In certain embodiments, the method is used to treat a cancer or a tumor in a subject including, without limitation, prostate cancer, melanoma, pancreatic cancer, ovarian cancer, and lymphoma. In certain embodiment, the method is used to treat a condition in a subject that can be regulated by the activation of one or more proteins such as EGFR, Erk1/2, Her2/Neu, Jak2, Src, Stat3, Akt, Cyclin B1, and Cdc25C. In certain embodiment, the method is used to treat a condition in a subject that can be regulated by the disruption of microtubule formations.

Abstract: Biocompatible intraocular implants include a tyrosine kinase inhibitor and a biodegradable polymer that is effective to facilitate release of the tyrosine kinase inhibitor into an eye for an extended period of time. The therapeutic agents of the implants may be associated with a biodegradable polymer matrix, such as a matrix that is substantially free of a polyvinyl alcohol. The implants may be placed in an eye to treat or reduce the occurrence of one or more ocular conditions.

Abstract: The present invention relates to novel trifluoromethoxyphenyl-substituted tetramic acid derivatives of the formula (I), in which J, X, Y, A, B, D and G have the meanings given above, to a number of processes for their preparation, and to their use as pesticides and/or herbicides. The invention further provides selective herbicidal compositions which comprise, firstly, trifluoromethoxyphenyl-substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention further relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the additions of ammonium salts or phosphonium salts and optionally penetrants.

Abstract: The present invention comprises compositions, methods and kits for delivering drugs. The invention provides an implantable device for delivery of a pharmaceutical substance to a patient, comprising a core comprising a core polymeric material optionally containing a core pharmaceutical substance, surrounded by a first layer comprising a first-layer pharmaceutical substance and a first-layer polymeric material, optionally surrounded by one or more additional layers comprising an additional pharmaceutical substance and an additional polymeric material, where the core, first, and optional additional polymeric materials may be the same or different, and where the optional core pharmaceutical substance, first-layer pharmaceutical substance, and optional additional pharmaceutical substances are the same or different. Implantation of the device allows a controlled release of drug for an extended period of time. The device may be implanted subcutaneously in an individual in need of continuous treatment with a drug.

Abstract: Drug compositions comprising the compound HT-2157 and their therapeutic uses, including the treatment of CNS disorders and cognitive impairments and the modulation of cognitive function, are disclosed. More particularly, the present invention relates to enteric-coated formulations comprising HT-2157 that reduce the appearance of clinically relevant methemoglobinemia relative to administration of non-enteric-coated formulations comprising HT-2157.

Abstract: Methods and compositions are provided for preventing or reversing loss of the therapeutic effect of a drug, where the loss is associated with the repeated administration of the drug to a patient. The method includes administering to the patient a dopamine receptor agonist or partial agonist or a drug that increases the extracellular level of dopamine by enhancing release of dopamine, decreasing the removal of dopamine from the extracellular space, enhancing the synthesis of dopamine within the brain, or decreasing metabolic degradation of dopamine; and also administering to the patient an opioid receptor antagonist in an ultra-low dose amount, wherein the ultra-low dose amount is effective to prevent or reverse loss of therapeutic effects associated with the repeated administration of the drug to the patient. The methods are useful for various treatments, including treating Parkinson's Disease, Restless Leg Syndrome, depression, schizophrenia, psychostimulant drug abuse, or attention deficit disorder.

Abstract: Hydrazone compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.