122results about How to "Potent activity" patented technology

This invention relates to the use of monoclonal and polyclonal antibodies that specifically bind to and have the ability in the alternative to become internalized by cells expressing folate receptor alpha (FRA) and to induce an immune effector activity such as antibody-dependent cellular cytotoxicity. The antibodies are useful in specific delivery of pharmacologic agents to FRA-expressing cells as well as in eliciting an immune-effector activity particularly on tumor cells and precursors. The invention is also related to nucleotides encoding the antibodies of the invention, cells expressing the antibodies; methods of detecting cancer cells; and methods of treating cancer using the antibodies.

Novel compounds, their methods of preparation and use in therapies related to cancer and inflammation are provided. Compounds comprise esters of cinnamic acid, vanillic acid and 4-hydroxy cinnamic acid and derivatives and salts thereof. Compounds with novel benzofuran lignan structure as a potent antimitotic agent and inducer of apoptosis are provided. Formulations and methods for treatment of diseases mediated by NF-kappaB are also provided.

Disclosed are novel compounds useful for the control of harmful organisms, harmful organism control agents using the same, and processes for producing the novel compounds. The useful novel compounds according to the present invention include compounds represented by formula (1). The compounds represented by formula (1) have potent activity against harmful organisms, and do not have phytotoxicity against agricultural and gardening plants, as objects to which the compounds of the present invention are applied for preventive and exterminating purposes, and human beings and beastswherein A represents a bond or an optionally substituted alkylene chain; R1 represents one or more groups, which may be the same or different, selected from the group consisting of a hydrogen atom, alkoxy, and haloalkoxy; R2 represents a hydrogen atom, benzyl, alkyl or alkanoyl, in which the groups other than the hydrogen atom may be substituted; and R3 represents a hydrogen atom, cycloalkyl, cycloalkenyl, aryl or a heterocyclic group, in which the groups other than the hydrogen atom may be substituted, excluding the case where R1 represents a hydrogen atom, A represents a bond or a methylene chain, and R3 represent phenyl or cyclohexyl, and the case where A represents an alkylene chain and R3 represents a hydrogen atom.

The disclosed invention is a bicyclo[4.2.1]nonane and its pharmaceutically acceptable salt or prodrug, and its composition and method of use to treat Flaviviridae (Hepacivirus, Flavivirus, and Pestivirus) infections in a host, including animals, and especially humans.

The invention provides compounds of the formula:wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 and R3 are independently hydrogen atom or an optionally substituted hydrocarbon group; n is an integer of 0-3; or salts thereof, which are useful as medicines having an osteogenesis promoting effect and chondrogensis promoting effect.The present invention relates to an amine compound having an excellent effect of inhibiting production and / or secretion of amyloid-b protein, a production and use thereof. Especially, it is effective for preventing and / or treating, for example, neurodegenerative diseases, amyloid angiopathy, neurological disorders caused by cerebrovascular disorders, and so forth.

Methods of preparing, and compositions comprising, derivatives of (-)-venlafaxine are disclosed. Also disclosed are methods of treating and preventing diseases and disorders including, but not limited to, affective disorders such as depression, bipolar and manic disorders, attention deficit disorder, attention deficit disorder with hyperactivity, Parkinson's disease, epilepsy, cerebral function disorders, obesity and weight gain, incontinence, dementia and related disorders.

Methods of preparing, and compositions comprising, derivatives of venlafaxine are disclosed. Also disclosed are methods of treating and preventing diseases and disorders including, but not limited to, affective disorders such as depression, bipolar and manic disorders, attention deficit disorder, attention deficit disorder with hyperactivity, Parkinson's disease, epilepsy, cerebral function disorders, obesity and weight gain, incontinence, dementia and related disorders.

The subject invention provides novel compounds and compositions for the safe and effective treatment of gastroesophageal reflux and related conditions. In a preferred embodiment, the compositions of the subject invention comprise esterified cisapride derivatives. These compositions possess potent activity in treating gastroesophageal reflux disease and substantially reduce adverse effects associated with the administration of cisapride. These adverse effects include, but are not limited to, diarrhea, abdominal cramping and elevations of blood pressure and heart rate.

Methods of preparing, and compositions comprising, derivatives of venlafaxine are disclosed. Also disclosed are methods of treating and preventing diseases and disorders including, but not limited to, affective disorders such as depression, bipolar and manic disorders, attention deficit disorder, attention deficit disorder with hyperactivity, Parkinson's disease, epilepsy, cerebral function disorders, obesity and weight gain, incontinence, dementia and related disorders.

This invention is directed to the treatment of cancer, particularly ocular melanoma, with a dual inhibitor of MET and VEGF such as Compound 1.

There is provided an imidazole derivative useful as a thrombosis treating agent, which is represented by the formula (I): wherein R represents an optionally substituted cyclic hydrocarbon group or an optionally substituted heterocyclic group, W represents a bond or an optionally substituted divalent linear hydrocarbon group, X represents an optionally substituted divalent hydrocarbon group, Y represents —CO—, —S(O)—, —S(O)2— or a bond, ring A represents an optionally substituted pyrrolidine ring, an optionally substituted piperidine ring or an optionally substituted perhydroazepine ring, Z1 and Z3 independently represent a bond or an optionally substituted divalent linear hydrocarbon group, Z2 represents —N(R1)—, —O—, —S(O)—, —S(O)2—, —CO—, —CH(R1)— or a bond, ring B represents an optionally substituted imidazole ring, wherein a substituent which the optionally substituted imidazole ring represented by ring B may have may be taken together with R1 to form an optionally substituted ring, and a represents 0, 1 or 2.

Flavivirus, rhabdovirus and paramyxovirus infections may be treated by administering an inhibitor of the enzyme dihydroorotate dehydrogenase such as 6-fluoro-2-(2′-fluoro-1,1′-biphenyl-4-yl)-3-methyl-4-quinolinearcarboxylic acid sodium salt (Brequinar). A synergistic effect can be obtained if an interferon such as interferon α2, interferon α8 or interferon β, or an inhibitor of a second enzyme selected from inosine monophosphate dehydrogenase, guanosine monophosphate synthetase, cytidine triphosphate synthetase and S-adenosylhomocysteine hydrolase, is also administered.

The disclosed invention is a bicyclo[4.2.1]nonane and its pharmaceutically acceptable salt or prodrug, and its composition and method of use to treat Flaviviridae (Hepacivirus, Flavivirus, and Pestivirus) infections in a host, including animals, and especially humans.

Methods are disclosed using Trospium Chloride, an antimuscarinic smooth muscle relaxant, for the treatment of urinary incontinence, and other disorders, while avoiding the concomitant liability of adverse side effects associated with other antimuscarinic drugs.

This invention is directed to the treatment of cancer, particularly ocular melanoma, with a dual inhibitor of MET and VEGF such as Compound 1.

This invention relates to a process for manufacturing a fraction of cacao bean husk having an inhibitory activity against glucosyltransferase in the prevention of tooth decay and more particularly, to the process for manufacturing a fraction of cacao bean husk having more potent activity against glucosyltransferase in the prevention of tooth decay, while providing an economically feasible recovery process designed to treat enormous wastes of cacao bean husk, wherein it comprises the steps in which: an extract of cacao bean husk, which has already proven to exhibit an excellent inhibitory activity against glucosyltransferase, is formed from cacao bean husk; and, the extract is again added to an adsorption resin and fractioned by 50% thanol aqueous solution.

Methods are disclosed using trospium, an antimuscarinic smooth muscle relaxant, for the treatment of smooth muscle disorders, while avoiding the concomitant liability of adverse side effects associated with conventional antimuscarinic treatment.

This application discloses phosphoramidate and phosphonoamidate prodrugs of alcohol-based therapeutic agents, such as nucleosides, nucleotides, acyclonucleosides, C-nucleosides, and C-nucleotides, and use of these prodrugs for treatment of diseases or disorders, including infectious diseases and cancers. This application also discloses a general method for enhancing bioavailability and / or liver-targeting property of alcohol drugs through converting the alcohol drugs to phosphoramidate or phosphonoamidate prodrugs, and methods of preparation of these prodrugs.

The present invention provides a compound of Formula I, all of its related stereoisomers, and their pharmaceutically acceptable salts, wherein A—B, K, Q, X, Y, Z, R and R1 are as defined in Claim 1. The present invention also provides processes for the preparation thereof, the use thereof in treating immune mediated disease and conditions, and pharmaceutical compositions for use in such therapy

The object of the present invention is to provide a compound useful for the prevention and treatment of viral infectious diseases, and particularly liver diseases caused by HCV infection due to its having a high degree of replication inhibitory activity against HCV, its production method, an intermediate compound useful for its production and a pharmaceutical composition containing these compounds, and the present invention relates to a compound represented by the formula (I): (wherein A represents —(CH2)n—, etc.; B represents —(C═O)—, etc.; D represents —(CH2)m—R′, etc.; E represents a hydrogen atom, etc.; G represents —(CH2)p-J, etc.; bond Q represents a single bond or double bond; and R1, R2 and R3 may be the same or different and each represent a hydrogen atom, etc.), a prodrug thereof or a pharmaceutically acceptable salt thereof.

The present invention includes a formulation which comprises an antibacterial substance and an antiulcer substance, wherein at least either of them is formulated into a gastrointestinal mucosa-adherent solid preparation. The formulation of the present invention shows long retention time in the gastrointestinal tract because of adhesion to the gastrointestinal tract mucosa, synergetically enhances the pharmaceutical effects of an antibacterial substance, specially antibiotic against Helicobacter pylori (HP) and an antiulcer substance, with very low doses of active ingredients, particularly the anti-HP antibiotic with low prevalence of side effects. The present agent is useful as an antiulcer agent, showing potent anti-HP activity.

Human Valpha24<+> natural killer T cells are expanded by culturing a mononuclear cell fraction obtainable from human peripheral blood in which hemopoietic stem cells are mobilized by granulocyte colony-stimulating factor, in the presence of a cytokine, such as interleukin 2, effecting proliferation and / or activation of lymphocytes and alpha-glycosylceramide. A cell fraction comprising human Valpha24<+> natural killer T cells expanded by the method, is useful as a cancer-treating agent.

This invention relates to long-acting injectable formulations for combating parasites in animals, comprising at least one isoxazoline active agent, a poloxamer, and a co-solvent. This invention also provides for improved methods for eradicating, controlling, and preventing parasite infections and infestations in an animal comprising administering the long-acting injectable formulations of the invention to the animal in need thereof.

Certain 3,6-disubstituted and 2, 4, 5-trisubstituted pyran derivatives that exhibit potent activity on monoamine transport systems are provided. The 3, 6 and 2, 4, 5 pyrans are useful in probing the effects of their binding to monoamine transporter systems and the corresponding relationships to various afflictions affecting the CNS, or as a treatment for various CNS-related disorders in which the monoamine transport and related systems are implicated.

A method for the prevention or treatment of Kaposi's sarcoma or Kaposi's sarcoma-associated herpes virus infection by administering an effective amount of a cyclopropanated carbocyclic 2′-deoxynucleoside to an individual in need thereof is provided.

Template-fixed β-hairpin peptidomimetics of the general formulaewherein Z is a chain of 11 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or Pro(4NHCOPhe), or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to inhibit proteases, in particular serine proteases, especially Cathepsin G or Elastase or Tryptase. These β-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.

The novel C7-modified camptothecin analogs, and pharmaceutically-acceptable salts thereof, of the present invention: (i) possess potent antitumor activity (i.e., in nanomolar or subnanomolar concentrations) for inhibiting the growth of human and animal tumor cells in vitro; (ii) are potent inhibition of Topoisomerase I; (iii) lack of susceptibility to MDR / MRP drug resistance; (iv) require no metabolic drug activation: (v) lack glucuronidation of the A-ring or B-ring; (vi) reduce drug-binding affinity to plasma proteins; (vii) maintain lactone stability; (viii) maintain drug potency; and (ix) possess a low molecular weight (e.g., MW<600).