Abstract: The present invention relates to diarylpyridazinone derivatives that block the potassium Kv channels (specifically the Kv1.5, Kv4.3, and Kv11.1 channels) and to the use thereof for the treatment of humans. Said compounds have the general formula (I), where R1 and R2 are simultaneously or independently one or more groupings such as: halogen, such as F, Br, Cl, a straight or branched C1-C4 alkyl, hydroxy, a straight or branched C1-C4 alkoxy, arylsulfonamido, in which the aryl is optionally replaced with a straight or branched C1-C4 alkyl, or nitrile, as well as the various enantiomers and the mixtures thereof in any proportion, and the pharmaceutically acceptable salts thereof.

Abstract: This invention relates to novel 1,2-pyridazines, 1,6-pyridazines or pyrimidines of the formula wherein B1 to B3 and R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may therefore be useful as medicaments for the treatment of diseases such as type II diabetes.

Abstract: Briefly described, embodiments of this disclosure include compounds as described herein, labeled compounds as described herein, pharmaceutical composition including compounds described herein, methods of imaging, method of forming a compound as described herein, and the like. In particular, embodiments of the disclosure include a series of triamino-pyridine derivatives and labeled triamino-pyridine derivatives, methods of synthesizing these compounds, intermediate compounds, methods of treatment using these compounds, methods of imaging, diagnosing, localizing, monitoring, and/or assessing a condition (e.g., corticotropin releasing factor type-1 (CRF1)) and/or related biological events, using triamino-pyridine derivatives, and the like. In addition, the present disclosure includes compositions (e.g., labeled triamino-pyridine derivatives that are ligands for the CRF1 receptor) used in and methods relating to non-invasive imaging (e.g., positron emission tomography (PET) imaging or SPECT imaging).

Abstract: Pyridine and pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.

Abstract: The present invention provides a compound of the Formula I, or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2, R3, m and are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions that comprise the above compounds, and methods of treating cancer using the same.

Abstract: Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.

Abstract: The present invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist. In addition, the invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist having Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof. These compositions are useful in pharmaceutical compositions whose use includes the treatment of obesity.

Abstract: The present invention relates to new therapies to treat pain and related diseases, as well as pharmaceutical compounds for use in said therapies.

Abstract: The invention relates to the combination of an endothelin receptor antagonist of formula (I) with paclitaxel, and in particular to this combination for therapeutic use, simultaneously, separately or over a period of time, in the treatment of ovarian cancer.

Abstract: The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and pro-drugs of said compounds, wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.

Abstract: A pyridazinone compound represented by the formula (I) has excellent effect on weed control and is useful as an active ingredient of herbicides.

Abstract: This invention relates to pyridazine derivatives, compositions comprising therapeutically effective amounts of those pyridazine derivatives and methods of using those derivatives or compositions in treating central nervous system (CNS) disorders with cognitive impairment that are responsive to agonists of ?5 subunit containing GABAA receptor, e.g., age-related cognitive impairment, Mild Cognitive Impairment (MCI), dementia, Alzheimer's Disease (AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia and cancer-therapy-related cognitive impairment.

Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, L1, L2, U and B are as defined in the application, which have valuable pharmacological properties, and in particular modulate the activity of the MCH receptor.

Abstract: The present invention relates to ethynyl derivatives of formula I wherein U, V, W, Y, R, R1, R2, R3 and R3? are as described herein. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).

Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).

Abstract: A compound of the formula (I) where, for example, W, X and Y are each CH; R1 and R6 together with the adjacent nitrogen forms a 3 to 10-membered saturated ring, wherein the ring may contain, in addition to the nitrogen and carbon ring members, 1, 2 or 3 heteroatoms and/or heteroatom groups as ring members, independently of one another, selected from the group consisting of sulfur, CO, SO, SO2 and N—R7 and/or the ring may carry 1, 2 or 3 radicals, independently of one another, each selected, for example, from the group consisting of halogen, cyano, nitro, amino, and C1-C6-alkyl. R2 is, for example, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy or C1-C6-alkoxy-C1-C6-alkoxy, and R7 is for example, R10C(?O), C1-C6 alkyl or C1-C6-haloalkyl; and/or salts thereof; and their use as pesticidal agents.

Abstract: The present invention relates to inhibitors of HCV replication of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein R1; R3; and R4 have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.

Abstract: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having a P2X3 and/or P2X2/3 receptor antagonistic effect comprising a compound of the formula (I): wherein ring A is substituted or unsubstituted 5 to 7-membered cycloalkane, substituted or unsubstituted 5 to 7-membered cycloalkene or the like; C is a carbon atom; —X— is —N(R16)— or the like; R16 is hydrogen, substituted or unsubstituted alkyl or the like; R7 is substituted or unsubstituted 5- or 6-membered heteroaryl, substituted or unsubstituted 6 to 10 membered aryl; Q1 and Q2 are each independently a carbon atom or a nitrogen atom; -L- is —O—, —S— or the like; R6 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl or the like; R2 is hydrogen, hydroxy or the like, or its pharmaceutically acceptable salt or a solvate thereof.

Abstract: The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by LRRK2 kinase activity, for example Parkinson's disease or Alzheimer's disease.

Abstract: This invention relates to a pharmaceutical composition for preventing and curing myocardium ischemia and reducing area of myocardial infarction, its pharmaceutical preparation and applications. The composition includes (a) levocarnitine or its derivatives, and (b) trimetazidine or its medicative salts. The quantity of levocarnitine or its derivatives, and trimetazidine or its medicative salts in the composition is effective amount for treating myocardial ischemia and reducing the area of myocardial infarction.

Abstract: The present disclosure provides indole/indazole-pyrimidinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, having the structure of Formula (I): wherein W, X, R1, R2, R3, R4, R5 and R6 are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for treating p38 kinase mediated diseases using the compound.

Abstract: A pharmaceutical composition, especially capsules, comprising granules containing nilotinib or a salt thereof with at least one pharmaceutically acceptable excipient. The granules may be produced by a wet granulation process.

Abstract: The present invention provides a compound represented by the formula (I): wherein R1, R2, R3, Z1, Z2, Ra, Rb, q, A and n are as defined in the description, a pharmaceutically acceptable salt or solvate thereof. The compound is useful as P2X3 and/or P2X2/3 receptor antagonist.

Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here.

Abstract: Compositions and methods for making a pharmaceutical dosage form include making a pharmaceutical composition that includes one or more active pharmaceutical ingredients (API) with one or more pharmaceutically acceptable excipients by thermokinetic compounding into a composite. Compositions and methods of preprocessing a composite comprising one or more APIs with one or more excipients include thermokinetic compounding, comprising thermokinetic processing the APIs with the excipients into a composite, wherein the composite can be further processed by conventional methods known in the art, such as hot melt extrusion, melt granulation, compression molding, tablet compression, capsule filling, film-coating, or injection molding.

Abstract: The present invention relates to the use of novel triazolopyridine derivatives of formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.

Abstract: The present invention relates to a pyridazinone derivative which can be used as a caspase inhibitor, process for the preparation thereof, and pharmaceutical composition for inhibiting caspase comprising the same.

Abstract: The present invention relates to substituted benzo-pyrimido-tetrazolo-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo-pyrimido-tetrazolo-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

Abstract: New phenylamidines are described, having general formula (I): and their use for the control of phytopathogenic fungi.

Abstract: The present invention relates to pyridazinthione derivatives that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

Abstract: The invention discloses a previously unidentified subset of mammalian non-small cell lung carcinomas (NSCLC) in which platelet-derived growth factor receptor alpha (PDGFR?) is expressed and is driving the disease, and provides methods for identifying a mammalian NSCLC tumor that belongs to a subset of NSCLC tumors in which PDGFR? is expressed, and for identifying a NSCLC tumor that is likely to respond to a PDGFR?-inhibiting therapeutic. The invention also provides methods for inhibiting the progression of a mammalian NSCLC tumor in which PDGFR? is expressed, and for determining whether a compound inhibits the progression of a PDGFR?-expressing mammalian NSCLC tumor.

Abstract: Novel compositions and methods of using substituted pyrimidines which have the general formula: (I).

Abstract: The present invention discloses methods of use of facially amphiphilic polymers and oligomers, including pharmaceutical uses of the polymers and oligomers as antimicrobial agents and antidotes for hemorrhagic complications associated with heparin therapy. The present invention also discloses novel facially amphiphilic polymers and oligomers and their compositions, including pharmaceutical compositions. The present invention further discloses the design and synthesis of facially amphiphilic polymers and oligomers.

Abstract: The present invention provides compounds of Formula (I) that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase.

Abstract: A plant disease controlling composition containing a pyridazine compound represented by formula (I): wherein R1 represents a chlorine atom, a bromine atom, a cyano group, or a methyl group, and R2 represents a hydrogen atom or a fluorine atom; and at least one QoI compound selected from the group consisting of dimoxystrobin, azoxystrobin, fluoxastrobin, pyraclostrobin, famoxadone, kresoxim-methyl, picoxystrobin, trifloxystrobin, N-methyl-?-methoxyimino-2-[(2,5-dimethylphenoxy)methyl]phenylacetamide, and fenamidone.

Abstract: A plant disease controlling composition containing a pyridazine compound represented by formula (I): wherein R1 represents a chlorine atom, a bromine atom, a cyano group, or a methyl group, and R2 represents a hydrogen atom or a fluorine atom; and at least one carboxamide compound selected from the group consisting of bixafen, isopyrazam, boscalid, fluopyram, fluxapyroxad, sedaxane, penflufen, flutolanil, mepronil, carboxin, thifluzamide, penthiopyrad, and furametpyr.

Abstract: A plant disease controlling composition is provided containing a pyridazine compound represented by formula (I): wherein R1 represents a chlorine atom, a bromine atom, a cyano group or a methyl group, and R2 represents a hydrogen atom or a fluorine atom; and at least one azole compound selected from the group consisting of propiconazole, prothioconazole, triadimenol, prochloraz, penconazole, tebuconazole, flusilazole, diniconazole, bromuconazole, epoxiconazole, difenoconazole, cyproconazole, metconazole, triflumizole, tetraconazole, myclobutanil, fenbuconazole, hexaconazole, fluquinconazole, triticonazole, bitertanol, imazalil, ipconazole, simeconazole, and flutriafol.

Abstract: The invention relates to compounds of formula (I): in which: n is equal to 0 or 1; D represents an oxygen atom or a bond; W represents a nitrogen atom or a —CH— group; X1 represents a nitrogen atom or a —CH?CH— group; X2 represents an oxygen atom or a nitrogen atom; X3 represents an oxygen atom or a nitrogen atom; one of X1, X2, X3 being other than a nitrogen atom, X2 and X3 not being an oxygen atom at the same time; R1, R2 are absent or represent, (i) independently of one another, a hydrogen atom or a (C1-C4)alkyl group, (ii) R1 and R2 may form, with the carbon atom to which they are attached, a —(C3-C10)cycloalkyl- group; Y represents a —(C3-C10)cycloalkyl-, aryl or aryloxy group, said groups being optionally substituted with one or more substituents chosen from a halogen atom or a (C1-C6)alkoxy group; Z1 is absent or represents an —NH— function; Z2 and Z3 are as defined in the description.

Abstract: The invention provides compounds of formula I or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for inducing apoptosis or treating cancer using compounds of formula I.

Abstract: Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Formula (I) Wherein Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.

Abstract: Molecules having a spacer unit, linker and recognition unit(s) are used for the treatment of various diseases, disorders and conditions. The compounds are useful in treating infectious diseases and diseases, disorders or conditions related thereto. Further, the methods for treating diseases, disorders or conditions involve recognition and binding of carbohydrate structures.

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: A plant disease controlling composition, containing a carboxamide compound represented by formula (I): wherein R1 represents a hydrogen atom or a methyl group and R2 represents a methyl group, a difluoromethyl group or a trifluoromethyl group; and a pyridazine compound represented by formula (II) wherein A1 represents a chlorine atom, a bromine atom, a cyano group or a methyl group, and A2 represents a hydrogen atom or a fluorine atom.

Abstract: This invention relates to 1-pyridazinyl-hydroxyimino-3-phenyl-propanes of the formula wherein R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may therefore be useful as medicaments for the treatment of diseases such as type II diabetes.

Abstract: Novel pyridazinone compounds of formula (I), which inhibit the purinergic P2X7 receptor and are useful for prevention, therapy and improvement of inflammatory and immunological diseases.

Abstract: To provide a radiation therapy potentiator, which, when employed in combination with cancer radiation therapy, can reduce radiation dose and can mitigate adverse effects. The invention provides a radiation therapy potentiator containing, as an effective ingredient, a uracil derivative represented by formula (1) (wherein R1 represents a halogen atom or a cyano group; and R2 represents a 4- to 8-membered heterocyclic group having 1 to 3 nitrogen atoms and optionally having as a substituent a lower alkyl group, an imino group, a hydroxyl group, a hydroxymethyl group, a methanesulfonyloxy group, or an amino group; an amidinothio group in which a hydrogen atom attached to a nitrogen atom may be substituted by a lower alkyl group; a guanidino group in which a hydrogen atom attached to a nitrogen atom may be substituted by a lower alkyl group or a cyano group; a lower alkylamidino group; or a 1-pyrrolidinylmethyl group) or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfon-amide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein X, Ar1, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.

Abstract: The invention relates to ring-annulated dihydropyrrolo[2,1-a]isoquinoline compounds according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.

Abstract: Disclosed are compounds of the Formulas III and IV and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9, and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

Abstract: The present invention relates to ethynyl derivatives of formula I wherein U, V, W, Y, R, R1, R2, R3 and R3? are as described herein. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).