Abstract: This invention relates to tryptophan hydroxylase inhibitors, compositions comprising them, and methods of their use for the treatment, management and/or prevention of metastatic bone disease.

Abstract: The present invention provides compounds that are inhibitors of voltage-gated sodium channels (Nav), in particular Nav 1.7, and are therefore useful for the treatment of diseases treatable by inhibition of these channels, in particular, chronic pain disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Abstract: The present invention is directed to pyridazinone compounds of formula (I) and furan compounds of formula (II), pharmaceutical compositions of compounds of formula (I) and (II), kits containing these compounds, methods of syntheses, and a method of treatment of a proliferative disease in a subject by administration of a therapeutically effective amount of a compound of formulae (I) or (II). Both classes of compounds were identified through screening of a collection of small molecule libraries.

Abstract: The present invention relates to triazine derivatives of Formula I for their use in the treatment of Type 2 diabetes, and to compositions comprising said triazine derivatives.

Abstract: The present invention relates to triazine derivatives of formula (I) for their use in the treatment of type 1 diabetes mellitus, and to compositions comprising said triazine derivatives.

Abstract: The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

Abstract: This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly(ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization from” approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling to” that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonal” chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

Abstract: The present invention is related to novel compounds of formula (I) having antibacterial activity against Clostridium bacteria, in particular Clostridium perfringens, pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.

Abstract: The present invention relates to a compound of the following general formula (I): wherein: R1 is notably H, a halogen or an aryl group, R2 is notably a halogen or an aryl group, R3 is notably a halogen, or an aryl or heteroaryl group, as well as to its pharmaceutically acceptable salts, its hydrates or its polymorphic crystalline structures, its racemates, diastereoisomers or enantiomers, except the compound 1-(2,4-diaminopyrido[3,2-d]pyrimidin-7-yl)-3,6,6-trimethyl-6,7-dihydro-1H-indol-4(5H)-one.

Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.

Abstract: The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. As a result of extensive and intensive studies on compounds having an inhibitory effect against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins, the inventors of the present invention have found that the di(arylamino)aryl compound of the present invention has inhibitory activity against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. This finding led to the completion of the present invention.

Abstract: The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

Abstract: Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.

Abstract: This document discloses molecules having the following formula (“Formula I”):

Abstract: The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and reducing the risk of microbial infections in humans and animals.

Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents.

Abstract: The present invention relates to disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted triazine derivatives as inhibitors for a protein kinase.

Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.

Abstract: Anytime obtained is uniform crystal of N-(4-fluorophenyl)-N?-phenyl-N?-(pyrimidin-2-ylmethyl)-1,3,5-triazine-2,4,6-triamine (compound A) and/or N,N?-bis (4-fluorophenyl)-N?-(pyrimidin-2-ylmethyl)-1,3,5-triazine-2,4,6-triamine (compound B) as a medicament or a starting material for the preparation of the medicament, and provided are a fumarate of the compound A and/or the compound B having excellent stability and a novel crystal thereof. A salt of the compound A and/or the compound B with fumaric acid enables uniform crystal to be anytime obtained, and thus, it is a compound that is very useful as a medicament or a starting material for the preparation of the medicament having excellent stability.

Abstract: Alterations of certain metabolite concentrations and fluxes that occur in response to viral infection are described. Host cell enzymes in the involved metabolic pathways are selected as targets for intervention; i.e., to restore metabolic flux to disadvantage viral replication, or to further derange metabolic flux resulting in “suicide” of viral-infected cells (but not uninfected cells) in order to limit viral propagation. While any of the enzymes in the relevant metabolic pathway can be selected, pivotal enzymes at key control points in these metabolic pathways are preferred as candidate antiviral drug targets. Inhibitors of these enzymes are used to reverse, or redirect, the effects of the viral infection. Drug candidates are tested for antiviral activity using screening assays in vitro and host cells, as well as in animal models. Animal models are then used to test efficacy of candidate compounds in preventing and treating viral infections. The antiviral activity of enzyme inhibitors is demonstrated.

Abstract: This invention relates to topical compositions for combating ectoparasites and endoparasites in animals, comprising at least one isoxazoline active agent and a pharmaceutically acceptable carrier, optionally in combination with one or more additional active agents. This invention also provides for an improved methods for eradicating, controlling, and preventing parasite infections and infestations in an animal comprising administering the compositions of the invention to the animal in need thereof.

Abstract: Provided are crystals of compound A which have properties suitable for industrial production. MEANS FOR SOLVING As the results of intensive studies to provide crystals of compound A having an inhibitory activity on the kinase activity of an EML4-ALK fusion protein and a mutant EGFR protein, crystals of compound A were found. Moreover, it was found that A04-type crystal of compound A, from among the aforesaid crystals of compound A, unexpectedly have preferred properties as a drug substance.

Abstract: The present invention describes novel triazines, their related pyrimidines and their use in controlling insects. This invention also includes new synthetic procedures, intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects using the compounds.

Abstract: The invention relates to compounds of formula wherein R1, R2, R3, R4, and Ar are as defined in the specification and claims, or to pharmaceutically active acid addition salts of such compounds. Compounds of formula I are modulators for amyloid beta and may be useful for the treatment or prevention of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.

Abstract: Compounds having the formula I wherein wherein R1, R2 and R3 are as defined herein are Hepatitis C virus NS5b polymerase inhibitors with improved bioavailability. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.

Abstract: There is provided an antifouling coating composition capable of forming an antifouling coating film which has stable coating film consumption degree on ships, underwater structures and the like and which exhibits excellent antifouling property over a long term. The antifouling coating composition includes a hydrolyzable copolymer (A) and an antifouling agent (B), wherein the hydrolyzable copolymer (A) is, e.g., a metal salt bond-containing copolymer having a component unit derived from a monomer (a21) represented by the general formula (II): CH2?C(R2)—COO-M-O—CO—C(R2)?CH2??(II) [In the formula (II), M is zinc or copper, and R2 is a hydrogen atom or a methyl group], and a component unit derived from other unsaturated monomer (a22) copolymerizable with the monomer (a21), and wherein the antifouling agent (B) includes at least medetomidine.

Abstract: The invention relates to methods of treatment and prevention of aquatic mold infections in aquatic organisms and methods of disinfecting equipment used in raising aquatic organisms. The methods comprise use of one or more stilbene derivatives, including 4,4?-bis-(1,3,5-triazinylamino)stilbene-2,2?-disulfonic acid derivatives.

Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.

Abstract: The present invention provides a novel class of compounds that have the activity of inhibiting HSP90 enzyme and are useful as anti-cancer agents or such, and compounds that are useful as synthetic intermediates thereof. Specifically, the present invention provides compounds represented by the following formula (1), and pharmaceutically acceptable salts thereof: wherein X, R1, R2, R3, R4, R5, R6, R7, L1, L2, and L3 are as defined in the specification.

Abstract: The present invention comprises inter alia triazine compounds as shown in formula (I) and pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single agent or in combination with one or more additional pharmaceutical agents, such as, an inhibitor of DPP-IV, a biguanide, an SGLT2 inhibitor, or an alpha-glucosidase inhibitor, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.

Abstract: The present invention provides for, inter alia, novel topical formulations comprising at least one 1-N-arypyrazole derivative and amitraz and to methods for treating, controlling, or preventing parasite infestations on mammals or birds The inventive formulations include spot-on, pour-on or spray formulations and may include a further ectoparasiticide, such as an IGR compound, an avermectin or milbemycin derivative, or a pyrethroid insecticides, and anthelmintics, such as benzimidazoles and imidazothiazoles. The inventive formulation provides a larger duration of parasite control at a faster rate of control. The inventive formula remains effective up to three months from the first application. Moreover, the inventive formulations prevent tick attachment to the animal, thereby providing protection against tick borne diseases. The ectoparasites which may be controlled, treated or prevented by the present invention includes ticks, fleas, mites, mange, lice, mosquitoes, flies and cattle grubs.

Abstract: A series of fused bicyclic pyridine and pyrazine derivatives, substituted directly on the pyridine or pyrazine ring by a functional group attached via a sulphur-containing linkage, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.

Abstract: This invention relates to certain unsaturated fatty acid derivatives of therapeutically active 1,3-dioxolane nucleoside analogues and to pharmaceutical formulations containing them. The said derivatives fall within formula (I). Compounds of formula (I) can be used in the treatment of a cancerous disease, including solid tumors and haematological cancers such as leukaemias, lymphomas and multiple myelomas.

Abstract: Methods for preserving technical products such as fuels and lubricants with a microbicidal composition. The composition is made up of at least one formaldehyde donor compound and at least one antioxidant. The antioxidant is either a gallic ester, a phenol derivative, a L-ascorbic acid, including salts and derivatives thereof, a tocopherol or one of its associated derivatives.

Abstract: Compounds of the formulae and selected hindered nitroxyl, hydroxylamine and hydroxylamine salt compounds such as the compound of the formula wherein G1 is hydrogen; C1-C22alkyl; C1-C22alkylthio; C2-C22alkylthioalkyl; C5-C7cycloalkyl; phenyl; C7-C9-phenylalkyl; or SO3M; G2 is C1-C22alkyl; C5-C7cycloalkyl; phenyl; or C7-C9-phenylalkyl; E is oxyl or hydroxyl; V is —O—; or —NH—; a is 0 or 1 or 2; b, c and d and g are each independently of one another 0 or 1; e is an integer from 1 to 4; f, m, n and p are each independently of one another an integer from 1 to 3; q is 0 or an integer from 1 to 3; Q, T and G3 are as defined in claim 1; G4 and G5 are each independently of the other hydrogen; or C1-C22alkyl; exhibit marked antiinflammatory action.

Abstract: The present invention relates to the field of therapeutic methods to screen for compounds on the basis of their ability to influence Wnt activity. The screening process is applied to both a physical library of a series of compounds and a virtual library of compounds that affect Wnt activity. In one aspect, the virtual screening process could be carried out where a permutational library of small peptides is substituted for the small organic molecules. The inventive methods may be used to empirically test for effects on Wnt activity and may also be applied to any pair of proteins involved in protein-protein interactions.

Abstract: Novel hetarylaminonaphthyridine derivatives of formula (I) wherein X, R1, R2, R3, R4, W1, W2, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.

Abstract: The present invention relates to synergistic mixtures comprising, as active components, one insecticidal compound I selected from the group of insect growth regulators comprising chitin synthesis inhibitors, moulting disruptors and ecdysone receptor agonists; and one fungicidal compound II selected from the group of strobilurine fungicides in synergistic effective amounts.

Abstract: Methods and compositions for the treatment and/or management of cancer are disclosed, which comprise the use of tryptophan hydroxylase inhibitors.

Abstract: The present invention provides a composition having an excellent controlling activity on plant disease. The composition comprising the compound represented by the formula (1) and one or more heterocyclic fungicidal compound selected from the group (A) shows an excellent controlling activity on a plant disease.

Abstract: The present invention provides hydrophobic prodrugs of bases, nucleosides, and nucleotides as well as methods of using the prodrugs as antiviral and anti-cancer chemotherapeutic agents.

Abstract: The present invention provides a method for treating a corneal disease by administering to a patient in need of such treatment an effective amount of ozagrel or a salt thereof.

Abstract: The present invention includes compositions that are useful in the treatment of breathing control diseases or disorders in a subject in need thereof. The present invention also includes a method of treating a respiratory disease or disorder in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a pharmaceutical formulation of the invention. The present invention further includes a method of preventing destabilization or stabilizing breathing rhythm in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a pharmaceutical formulation of the invention.

Abstract: The present application relates to novel azabicyclic compounds, processes for their preparation, their use alone or in combinations for the treatment and/or prevention of diseases, and their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular disorders.

Abstract: A novel heterocyclic compound belonging to ‘triazine-aryl-bis-indoles’, useful for the treatment of asthma. The pathway by which this compound inhibits asthma is also demonstrated. The present invention also provides a process for the preparation of above compounds and their derivatives are presented.

Abstract: Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2?-diindolylmethane, 2?,3-diindolylmethane, and 3,3?-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.

Abstract: A composition comprising at least one physiologically tolerated film forming agent, at least one physiologically tolerated solvent, at least one plasticizer and a compound of the formula I or a stereoisomeric form or a physiologically tolerated salt of any of the foregoing. The composition is suitable for treatment of androgenic alopecia or hirsutism, that is, for avoiding undesirable hair growth, and for treatment of seborrhea and acne, and can furthermore be employed in cosmetics.

Abstract: The invention provides pyridyl-triazine derivatives to inhibit the hedgehog signaling pathway and the use of such compounds in the treatment of hyperproliferative diseases and angiogenisis mediated diseases.

Abstract: A method of inhibiting matrix metalloproteinase 9 (MMP-9) dimerization without substantially inhibiting the catalytic activity of MMP-9, comprising contacting the MMP-9 with a small molecule compound of the structure wherein A is a ring structure which is substituted by R2, R3 and R4; X is present or absent and when present is NH, O, ester or N-monosubstituted amide; Z is S, O, or N; n is an integer from 0-5; R1 is alkyl, aryl, heteroalkyl, or heteroaryl, each with or without substitution; and R2, R3, and R4 is each present or absent, and is each independently H, alkyl, aryl, heteroalkyl, heteroaryl, each with or without substitution, or a pharmaceutically acceptable salt thereof.