Abstract: The compounds of Formula I described herein regulate activity of JAK2 by specifically binding to the JAK2 pseudokinase domain, JH2, and are useful as therapeutic agents in the treatment or amelioration of myeloproliferative disorders. Also provided herein are methods of treating myeloproliferative disorders, and methods of making compounds of Formula I.

Abstract: An methyl 4-((5-(3-fluorophenyl)-4-phenyl-4H-1,2,4-triazol-3-ylthio)methyl)benzoate compound, its synthesis, and its use as an antimicrobial agent.

Abstract: A mass spectrometer including an entrance slit, an energy filter, a momentum filter and a detector array, the entrance slit, energy filter and momentum filter being configured to provide molecular analyte ions to the detector array at a mass resolution of about 20,000 or greater. A method for determining the isotopic composition of an analyte in a sample includes converting the analyte to molecular analyte ions, separating the molecular analyte ions using an entrance slit, separating the molecular analyte ions according to their energy levels, separating the molecular analyte ions according to their momenta, detecting two or more of the molecular analyte ions at a mass resolution of about 20,000 or greater to produce molecular analyte ion data; and analyzing the molecular analyte data to determine the isotopic composition of at least a portion of the analyte.

Abstract: Cyclohexyl sulfonamide compounds which are platelet-activating factor (PAF) receptor antagonists. Said compounds may be useful, for example, for the treatment of atherosclerosis or other PAF-mediated disorders, including inflammatory, cardiovascular, and immune disorders.

Abstract: This document discloses molecules having the following formulas (“Formula One” & “Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.

Abstract: Formula (I) and (II). The present invention relates to the use of a new lupane derivative of general formula (I) or (II), or a pharmaceutically acceptable salt, crystal form, complex, hydrate, or hydrolysable ester thereof, for preventing and/or inhibiting tumor growth and for treating cancer and other proliferative diseases, more particularly for treating leukemia, liver, cervical, colon and prostate cancer. The present invention also relates to the synthesis of these compounds and to pharmaceutical compositions which contain them.

Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, and G are defined herein.

Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.

Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with the compounds.

Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.

Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.

Abstract: Tetrazol-5-yl- and triazol-5-yl-aryl compounds of the general formula (I) as herbicides are described. In this formula (I), X, Z, W and R are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. A and B are N and CY. Q is cyanoalkylcarbonyl or isoxazolyl.

Abstract: The present invention relates to compounds of formula (IA) wherein QA is QA1 or QA2 P is P1, heterocycyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, Z, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (IA), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (IA) and to methods of using the compounds of formula (IA) to control insect, acarine, nematode and mollusc pests.

Abstract: The invention relates to novel compounds of the formula (I) in which X, Y and CKE have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. The invention also relates to selective herbicidal compositions comprising, firstly, the 1,2,4-triazolyl-substituted ketoenols and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising, in particular, 1,2,4-triazolyl-substituted ketoenols, through the addition of ammonium salts or phosphonium salts and optionally penetrants, to the corresponding compositions, to processes for producing them and to their application in crop protection as insecticides and/or acaricides and/or for preventing unwanted plant growth.

Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as pain, neurological disorders, psychiatric disorders, and neuromuscular disorders. Compounds provided herein modulate the activity of opioid receptor (e.g., ?-opioid receptor) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.

Abstract: Processes are described for the preparation of PI3K inhibitor, GDC-0032, Formula I, having the structure: and intermediates useful for the preparation of I.

Abstract: This document discloses molecules having the following formulas (“Formula One” & “Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.

Abstract: This document discloses pesticidal compostions comprising molecules having the following formulas: and processes related thereto.

Abstract: A condensed cyclic compound represented by Formula 1 below and an organic light-emitting device (OLED) including the condensed cyclic compound are presented. Ar1 and Ar2 in Formula 1 are each independently one of a hydrogen atom, an aryl or heteroaryl group and an arylamino group, at least one of Ar1 and Ar2 being a substituted or unsubstituted 1,2.4-triazol-4-yl group; L1 and L2 in Formula 1 are linking groups, each independently one of a cyclic or noncyclic, saturated or unsaturated hydrocarbon group and a heteroarylene group; a and b in Formula 1 are each independently one of 0 or 1; and R1 to R8 in Formula 1 being each independently one of a variety of inorganic and organic substituents including cyclic or noncyclic, saturated or unsaturated and aromatic, nonaromatic or heteraromatic groups. The OLED may have a low driving voltage, a high emission efficiency and long lifespan characteristics.

Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.

Abstract: The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).

Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.

Abstract: Methods and compositions for treating degenerative muscle conditions are disclosed. The compositions disclosed herein include S1P promoting compositions that include an S1P promoting agent. Embodiments of the methods disclosed herein include administering therapeutically effective amounts to subjects suffering from a degenerative muscle condition, such as, for example, subjects suffering from sarcopenia and subjects suffering from muscular dystrophy, including subjects suffering from Duchenne Muscular Dystrophy and Becker Muscular Dystrophy.

Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which have excellent insecticidal activity and which can thus be used as an insecticide.

Abstract: Novel crystalline salts of 3-[4-(3-ethanesulfonyl-propyl)-bicyclo[2.2.2]oct-1-yl]-4-methyl-5-(2-trifluoromethyl-phenyl)-4H-1,2,4-triazole are potent inhibitors of 11?-hydroxysteroid dehydrogenase Type 1 and are useful for the treatment of conditions associated with Metabolic Syndrome as well as cognitive impairment. The invention also relates to pharmaceutical compositions containing these novel salts, processes to prepare these salts and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes, hyperglycemia, obesity, dyslipidemia, hypertension, and cognitive impairment.

Abstract: Compounds of the general structure: Z-A-(S—B)n where A represents a linear aromatic molecular core, S represents a flexible spacer unit, B represents a crosslinking group such as a methacrylate group, n equals 1 to 3, and Z represents any entity compatible with the B groups, and in which A is a substantially aromatic nucleus containing fluorene ring structures substituted at the 9-position and in which the 9-positions of the fluorenes are not susceptible to oxidation.

Abstract: Disclosed herein are novel antifungal compounds of Formula 1, containing fluconazole pharmacophore moieties coupled with other moieties including aryl enones and chalcones and pharmaceutically acceptable salts thereof, methods for preparing these compounds and pharmaceutical preparations containing these novel compounds for prevention and treatment of fungal infections.

Abstract: A bisazole-based compound is represented by formula (I): wherein X represents C—R3 or nitrogen, R1 and R2 independently represent a haloalkyl group, R3 represents H or F. A transition metal complex is represented by formula (II): ML1L2L3??(II) wherein M is a transition metal, L1 represents in which X represents C—R31 or nitrogen, R11 and R21 independently represent a haloalkyl group, and R31 represents H or F; and L2 and L3 independently represent a dipyridine-based ligand.

Abstract: The present invention relates to novel compounds of formula (A): in the form of a free base or of an addition salt with an acid. The invention also relates to process of preparation of compounds of formula (A), to composition comprising them and to their application in therapeutics and in particular in cancers.

Abstract: Compounds of the general structure: Z-A-(S—B)n where A represents a linear aromatic molecular core, S represent a flexible spacer unit, B represents a crosslinking group such as a methacrylate group, n equals 1 to 3, and Z represents any entity compatible with the B groups, and in which A is a substantially aromatic nucleus containing fluorene ring structures substituted at the 9-position and in which the 9-positions of the fluorenes are not susceptible to oxidation.

Abstract: Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.

Abstract: This invention provides compounds of formula I: wherein R1, R2, CY, Y1, Y2, X1, X2, and X3 are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

Abstract: [Problem] Provided is a pharmaceutical, in particular, a pharmaceutical composition which is useful for the treatment of pain. [Means for Solution] The present inventors have made extensive studies using model animals with pain for the purpose of providing a therapeutic agent for pain. As a result, they have found that 11?-hydroxydehydrogenase type 1 (11?-HSD1) inhibitor, in particular, a triazole compound having a cyclic group at the 3-position (or 5-position) of a triazole ring has a good effect of ameliorating chronic pain. That is, according to the present invention, a pharmaceutical composition comprising an 11?-HSD1 inhibitor, in particular, the triazole compound of the present invention, as an active ingredient, is useful for the treatment of pain (particularly, neuropathic pain or fibromyalgia).

Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts thereof, wherein R1, R2, and R3 are as defined herein, are useful for treating flaviviridae viral infections.

Abstract: A compound represented by formula [I] and a pharmaceutically accepted salt of said compound are a novel compound and a pharmaceutically accepted salt thereof which exert antagonistic activity against group II metabotropic glutamate (mGlu) receptors, and are effective as a novel preventive or therapeutic agent for disorders such as mood disorders (depressive disorder, bipolar disorder, etc.), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, a specific phobic disorder, acute stress disorder, etc.), schizophrenia, Alzheimer's disease, cognitive impairment, dementia, drug dependence, convulsions, shivering, pain, sleep disorders, and the like.

Abstract: The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.

Abstract: [Problem] A compound, which can be used for preventing or treating diseases, in which 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1) is concerned, in particular, diabetes, insulin resistance, dementia, schizophrenia and depression, is provided. [Means for Solution] It was found that a triazole derivative, in which one of the 3- and 5-positions of the triazole ring has (di)alkylmethyl or cycloalkyl, each of which is substituted with —O— (aryl or a heterocyclic group, each of which may be substituted, or lower alkylene-cycloalkyl), and the other thereof has aryl, a heterocyclic group or cycloalkyl, each of which may be substituted, or a pharmaceutically acceptable salt thereof exhibits potent 11?-HSD1 inhibitory action. From the above, the triazole derivative of the present invention can be used for preventing or treating diabetes, insulin resistance, dementia, schizophrenia and depression.

Abstract: The present invention relates to compounds of formula (I) wherein Q is Q1 or Q2 P is P1, heterocyclylor heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, Y1, Z, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.

Abstract: A class of topomimetic calixarene-based peptide mimetics is described. Calixarene-based peptide mimetics have various biological activities such as, for example, bactericidal activity, antiangiogenic activity, and/or antitumor activity. Methods of use and methods of designing calixarene-based peptide mimetics are described.

Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, and Z are as defined herein, are useful for treating flaviviridae viral infections.

Abstract: The present invention provides heterocyclic derivatives of formula I that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.

Abstract: The invention relates to methods for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome which comprise administering a therapeutically effective amount of a compound of formula I wherein R1, R2, R3, V, W, Y, and Z are as defined herein or a pharmaceutically active acid addition salt of such compounds. The invention also relates to a subgenus of such compounds and pharmaceutical compositions containing them, as well as methods for their manufacture.

Abstract: A process for preparing 7-[2-[4-(6-fluoro-3-methyl-1,2-benzisoxazol-5-yl)-1-piperazinyl]ethyl]-2-(1-propynyl)-7H-pyrazolo-[4,3-e]-[1,2,4]-triazolo[1,5-c]pyrimidin-5-amine, intermediates useful in that process, and processes for preparing said intermediates are disclosed.

Abstract: This document discloses molecules having the following formulas (“Formula One” & “Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.

Abstract: This invention provides compounds of formula I: wherein R1, R2, CY, Y1, Y2, X1, X2, and X3 are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

Abstract: The present invention concerns novel heteroaryl-N-aryl carbamates and their use in pest control, as insecticides and acaricides This invention also includes preparation of the pesticide compositions containing the compounds, and methods of controlling insects using the compounds.

Abstract: The present disclosure provides 2,4-disubstituted thiazoles of the general structure shown below that are agonists of G-protein coupled receptor (IC-GPCR2). Also, provided are compositions comprising these compounds as well as methods for using these compounds in a variety of applications including diabetes and metabolic disorders.

Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, Y1, and Z are as defined herein, are useful for treating flaviviridae viral infections.

Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists.