Abstract: This document relates to inhibitors of G protein coupled receptor 6 kinase (GRK6) polypeptides as well as methods and materials for using such inhibitors to treat hematological malignancies, inflammation diseases, and autoimmune disorders.

Abstract: This disclosure relates to a novel class of compounds having the structure of formula I as defined herein and pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof. This disclosure also comprises methods of treating a subject by administering a therapeutically effective amount of a compound of formula I or a pharmaceutically acceptable salt thereof to the subject. These compounds are useful for the conditions disclosed herein. This disclosure further comprises methods for making the compounds of formula I and corresponding intermediates.

Abstract: The present invention relates to novel oxazolidinone compounds of general formula (I) having antibiotic activity also against multiresistant bacterial strains.

Abstract: In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate.

Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R5, A1, A2, and are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein the syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.

Abstract: The invention relates to the compounds of formula I, formula II, formula III and formula IV or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II, formula III or formula IV and methods for the treatment of mucositis may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, oral solution, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of mucositis and oral mucosal inflammatory or oral infectious diseases.

Abstract: The present invention relates to compounds of formula (I) and to compositions comprising the same and to the use of the compounds and their compositions in treatment, for example in the treatment of inflammatory diseases, in particular respiratory inflammatory disease. The invention also extends to methods of making said compounds.

Abstract: Compounds of the formula where the variables have the meaning defined in the specification have analgesic and/or immunostimulant effect in mammals.

Abstract: A tetrazolinone compound represented by formula (1): wherein R1 and R2 each independently represents a hydrogen atom, a C1-C4 alkyl group optionally having one or more halogen atoms, etc.; R3 represents a hydrogen atom, a C1-C4 alkyl group optionally having one or more halogen atoms, etc.; R4 represents a halogen atom, a C1-C4 alkyl group optionally having one or more halogen atoms, etc.; h represents any one of integers of 0 to 4; X represents a nitrogen atom or CR5; and R5 represents a hydrogen atom, a halogen atom, etc.; has excellent control activity against pests.

Abstract: This invention generally relates to substituted imidazopyridine compounds, particularly substituted 4-(imidazo[1,2-a]pyridin-2-yl)benzamide compounds and salts thereof. This invention also relates to pharmaceutical compositions and kits comprising such a compound, uses of such a compound (including, for example, treatment methods and medicament preparations), processesor making such a compound, and intermediates used in such processes.

Abstract: The purification method of an aldehyde compound of the present invention includes a step of neutralizing a reaction solution containing an aldehyde compound by adding water and a base compound to the reaction solution, and a step of distilling the neutralized reaction solution, in which the reaction solution is obtained by reacting a compound represented by the following Formula (a1) or (a2) with hydrogen and carbon monoxide in the presence of a metal compound of groups 8 to 10 and a phosphorus compound, the phosphorus compound is represented by Formula (R1O)3P, and the base compound is at least one kind selected from among carbonate and hydrogen carbonate of metals of group I on the periodic table and carbonate and hydrogen carbonate of metals of group II on the periodic table.

Abstract: The invention provides methods of treating or preventing malaria comprising administering to an animal an effective amount of a compound of formula I: Q-Y—R1—R2??(I), wherein Q, Y, R1, and R2 are as described herein. Methods of inhibiting a plasmodial surface anion channel of a parasite in an animal are also provided. The invention also provides pharmaceutical compositions comprising a compound represented by formula I in combination with any one or more compounds represented by formulas II, V, and VI. Use of the pharmaceutical compositions for treating or preventing malaria or for inhibiting a plasmodial surface anion channel in animals including humans are also provided. Also provided by the invention are clag3 amino acid sequences and related nucleic acids, vectors, host cells, populations of cells, antibodies, and pharmaceutical compositions.

Abstract: The present, invention relates to a process for large scale production of N-[4-(1-Cyclobutyl piperidin-4-yloxy) phenyl]-2-(morpholin-4-yl) acetamide dihydrochloride of formula (I).

Abstract: By either forming a triaryl acid halide or a triaryl mixed anhydride and subsequently treating with aqueous sodium azide, triaryl acyl azides are prepared in high yield using inexpensive reagents in a process in which by-products are easily removed from the triaryl acyl azide.

Abstract: Isoindoline sigma-2 receptor antagonist compounds, pharmaceutical compositions comprising such compounds, and methods for inhibiting Abeta-associated synapse loss or synaptic dysfunction in neuronal cells, modulating an Abeta-associated membrane trafficking change in neuronal cells, and treating cognitive decline associated with Abeta pathology are provided.

Abstract: A pest control agent comprising an aromatic compound represented by formula (1) wherein R1 represents a halogen atom, etc.; R3 represents a hydrogen atom, etc.; R7 represents a C1-C3 alkyl group optionally having one or more halogen atoms, etc.; Z2 represents a halogen atom, etc.; Z3 represents a C1-C3 alkyl group optionally having one or more halogen atoms, etc.; and Q represents the following group Q1, Q2, or Q3 has excellent control activity.

Abstract: Using a morpholino nucleotide wherein 5?-hydroxy group or a hydroxy group present on the substituent of the 5?-hydroxy group is protected by a protecting group having an alkyl group having not less than 10 and not more than 300 carbon atoms and/or an alkenyl group having not less than 10 and not more than 300 carbon atoms as a starting material, a method capable of efficiently producing the morpholino oligonucleotide in a high yield by a liquid phase synthesis can be provided.

Abstract: The present invention relates to compounds of formula of formula I wherein X, L and R1 are as described herein, compositions containing compounds of formula I, methods of manufacture of compounds of formula I and methods of treating psychiatric, metabolic, cardiovascular or sleep disorders with compounds of formula I.

Abstract: The invention relates to a process for the manufacture of diastereomerically and enantiomerically enriched triazole compounds isavuconazole and ravuconazole, comprising a Reformatsky reaction between a ketone and a 2-halozincpropionate ester, followed by a resolution step, preferably an enzymatic resolution with an esterase enzyme.

Abstract: The invention relates to new bicyclic heterocycle compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of diseases, e.g. cancer.