Abstract: Compositions and methods are provided for modulating the physiological activation of tissue transglutaminase (TG2); which methods can include inhibiting the activity of TG2 associated with inflammatory disorders, which disorders may include, without limitation, sepsis, ischemic reperfusion injury, renal fibrosis, and the like.

Abstract: The present invention provides a process for the hydrogenation of the levulinic acid to ?-valerolactone in a single step with a single Pt supported on hydrotalcite catalyst. The process provides conversion of ?-valerolactone over Pt supported hydrotalcite catalyst at room temperature (25° C.). The process provides a levulinic acid conversion of 34-100% with 20-50 bar hydrogen pressure to give ?-valerolactone selectivity up to 99%.

Abstract: A compound represented by formula (4) is produced by a step A of reacting a compound represented by formula (2): wherein R1 represents an ethyl group or the like, R represents a halogen atom or the like, n represents 0, 1, 2, or 3, and M represents potassium or the like, with thionyl chloride to obtain a compound represented by formula (1): a step B of reacting the compound represented by formula (1) with a compound represented by formula (5): wherein A1 represents a nitrogen atom or ?CH—, R5 represents a trifluoromethyl group or the like, and m represents 1 or 2, to produce a compound represented by formula (3): or an acid salt thereof; and a step C of reacting the compound represented by formula (3) or an acid salt thereof in the presence of acid at 100° C. to 180° C.

Abstract: The invention relates to inhibitors of mutant isocitrate dehydrogenase (mt-IDH) proteins with neomorphic activity useful in the treatment of cell-proliferation disorders and cancers, having the Formula: where A, B, W1, W2, W3, and R1-R8 are described herein.

Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols A, X, Y, L1, L2, G, Q, p, R1, R2 and R10 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).

Abstract: The present invention relates to tetrahydroisoquinolinone derivatives, a pharmaceutical composition comprising the same and the use of these derivatives in the inhibition of the Hsp70 protein. The compounds are useful in the treatment or inhibition of cancer, autoimmune disease, rheumatoid arthritis, inflammatory bowel disease and psoriasis.

Abstract: The present invention is directed to polymorphic forms of Pitavastatin sodium and processes for preparation of the same.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts, esters, amides, or radiolabelled forms thereof, wherein R1, R2, and R3 are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by voltage-gated sodium channels, e.g., Nav 1.7 and/or Nav 1.8. Methods for making the compounds are disclosed. Also disclosed are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.

Abstract: The present invention provides compounds of Formula 1, or a pharmaceutically acceptable salts, thereof, where R, X, A, E, and G are as described herein, methods of preparing the compounds, and use of the compounds to treat pain and/or inflammation.

Abstract: The present invention provides novel, non-covalently bound complexes of serum albumin and analogs of poorly soluble drugs, such as camptothecin. The novel complexes are significantly more water-soluble than the camptothecin analogs and are useful as prodrug forms of the camptothecin analogs for the treatment of mammalian cell proliferative diseases, such as cancer.

Abstract: Disclosed are alpha-aryl-beta-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing isoquinoline amide compounds.

Abstract: The present invention relates to novel polymorphic forms of ivacaftor, process for its preparation and pharmaceutical compositions comprising the same.

Abstract: The invention relates to a process for preparing substituted quinolin-4-ol compounds useful for preparing protein tyrosine kinase (PTK) inhibitors which are useful in treating cancer.

Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof, for use in the treatment of multiple myeloma.

Abstract: Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.

Abstract: Isoquinoline compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an isoquinoline compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

Abstract: This invention involves the field of biomedicine, and reveals naphthyridine compounds, medical combinations and use thereof. The naphthyridine compounds has the structure as shown by Formula (I), or its stereoisomers, geometric isomers, tautomers, nitrogen oxides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or their prodrugs. The naphthyridine compounds of this invention has anti-tumor efficacy significantly superior to that of prior art. Moreover, the naphthyridine compounds of this invention can treat diseases mediated by protein kinases.

Abstract: It is intended to provide: a compound useful as an amyloid oxidation catalyst which is applicable in vivo and is applicable not only to A? peptides but to other amyloids; and a prophylactic or therapeutic drug for an amyloid-related disease, comprising the same. The present invention provides a benzothiazole compound represented by the following formula (1) wherein X represents a halogen atom; R1 represents an optionally substituted hydrocarbon group; R2 represents a hydrogen atom or an optionally substituted hydrocarbon group; R3 and R4 are the same or different and each represent a hydrogen atom, an optionally substituted hydrocarbon group, an alkoxy group, a halogen atom, an amino group, a nitro group, or a cyano group; R2 and R4 optionally together form an alkylene group; and R5 represents an anion.

Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.

Abstract: Provided are a quinacridone pigment having a low content of a primary aromatic amine, a method for producing the same, and also a gravure and flexo ink, a colorant for plastic, a paint, a lithographic ink, a toner, or an ink-jet ink using the pigment. The quinacridone pigment having a low primary aromatic amine content is provided by washing a quinacridone pigment with at least one solvent selected from water and an organic solvent, or by adding an oxidizing agent to a pigment slurry including a quinacridone pigment and at least one solvent selected from water and an organic solvent to oxidatively decompose the aromatic amine.