A compound obtained by reaction of one or more amines of the general formula NHR.sup.6R.sup.7 with a compound of the following general formula (IX): ##STR00001## wherein, PI is a photoinitiator derivative, G is linker comprising a number p' of unreacted hydroxyl groups, M is a group comprising a number z of (meth)acrylate groups equal to at least one, as well as inks, coating compositions and adhesives comprising the same.
A method for producing a 1,2,4-triazole compound involves reacting an amide compound represented by formula (2) with a hydrazide compound represented by formula (3) in a solvent in the presence of a Lewis acid and a Lewis base, thereby obtaining a 1,2,4-triazole compound represented by formula (1): ##STR00001## R.sup.1 represents an alkyl group, a cycloalkyl group, an alkoxy group, a cycloalkoxy group, an aryl group, an aryloxy group, a monovalent heterocyclic group or a substituted amino group, R.sup.2 and R.sup.3 each independently represent a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group, a monovalent heterocyclic group or a substituted amino group, and Ring A and Ring B each independently represent an aromatic hydrocarbon ring or an aromatic heterocyclic ring.
Inducible HSP70 is overexpressed in a wide spectrum of human tumors and its expression correlates with metastasis and poor outcomes to radiation and chemotherapy in patients. Identification of small molecule inhibitors of HSP70 pose a new therapy to cancer treatment. HS72, a benzimidazole piperidinyl carboxamide has been identified as an allosteric inhibitor for HSP70 and has demonstrated good tumor growth inhibition in vivo.
The present invention is directed to indazole derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.
This application features pyrazol-3-one compounds that activate pro-apoptotic BAX. Also featured are methods of using such compounds, e.g., for the treatment or prevention of diseases, disorders, and conditions associated with deregulated apoptosis of cells (e.g., insufficient apoptosis of diseased or damaged cells or essentially the absence of apoptosis of diseased or damaged cells).
The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the compounds of Formula (I) or (II), or compositions thereof, for treating or preventing a wide range of diseases (e.g., proliferative diseases (e.g., cancers, benign neoplasms, angiogenesis, inflammatory diseases, autoimmune diseases) and metabolic diseases (e.g., diabetes (e.g., type 2 diabetes, gestational diabetes)) in a subject. Treatment of a subject with a disease using a compound of Formula (I) or (II), or compositions thereof, may downregulate the expression and/or inhibit the activity of a kinase (e.g., a tyrosine kinase, such as a Tec kinase, in particular, bone marrow on X chromosome kinase (BMX)), and therefore, suppress tyrosine kinase singling in the subject.
The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula IA or Formula IB, as well as stereoisomers, tautomers or pharmaceutically acceptable salts thereof. ##STR00001## For Formula IA and Formula IB compounds A.sup.1, A.sup.2, A.sup.3, A.sup.4, W.sup.1, W.sup.2, Y, X, R.sup.1, R.sup.2, R.sup.3, R.sup.4a, R.sup.4b, R.sup.5a, R.sup.5b, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.9a, R.sup.9b, R.sup.10 and subscript n are as defined in the specification. The inventive Formula IA and Formula IB compounds are inhibitors of Mnk and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.
A series of fused bicyclic heteroaromatic derivatives of formula (I), as defined herein, being selective inhibitors of phosphatidylinositol-4-kinase III.beta. (PI4KIII.beta.) activity, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases and malaria; and organ and cell transplant rejection. ##STR00001##