82846-28-4Relevant articles and documents
BTK protein kinase inhibitors
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Page/Page column 59, (2009/05/29)
This application discloses pyridine and pyrimidine compounds according to formula I wherein R1, R2, R3, R4, R5, X1 and A are as described herein which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of formula I and at least one carrier, diluent or excipient.
3-Nitro-4-amino benzoic acids and 6-amino nicotinic acids are highly selective agonists of GPR109b
Skinner, Philip J.,Cherrier, Martin C.,Webb, Peter J.,Sage, Carleton R.,Dang, Huong T.,Pride, Cameron C.,Chen, Ruoping,Tamura, Susan Y.,Richman, Jeremy G.,Connolly, Daniel T.,Semple, Graeme
, p. 6619 - 6622 (2008/04/02)
A series of 3-nitro-4-substituted-aminobenzoic acids were prepared and found to act as potent and highly selective agonists of the orphan human GPCR GPR109b, a low affinity receptor for niacin. No activity was observed at the closely homologous high affinity niacin receptor, GPR109a. A second series, comprising 6-amino-substituted nicotinic acids was, also prepared and several analogues showed comparable activity to the nitroaryl series.
Synthesis of N-acetylglucosaminyl and diacetylchitobiosyl amides of heterocyclic carboxylic acids as potential chitinase inhibitors
Rottmann,Synstad,Eijsink,Peter
, p. 2293 - 2297 (2007/10/03)
2-(Dimethylammo)oxazoline-4-carboxylic acids 5 were prepared by condensation of binucleophilic amino acids 4 and O-ethyl-N,N-dimethyhsourea 3. New heterocyclic N-acetylglucosaminyl amides and chitobiosyl amides 8 were obtained by the coupling of tetraacetylglucosamine 6a or heptaacetylchitobiosylamine 6b with acid chlorides of heterocyclic carboxylic acids 2 or 5a and subsequent deacetylation. Based on their substitution patterns, compounds 8 were expected to have inhibitory activity towards chitinases. Enzyme assays showed that glycosyl amides 8 indeed were moderate inhibitors of chitinases, the diacetylchitobiosyl amides 8d-f generally having higher inhibitory activities than the N-acetylglucosaminyl amide derivatives 8a-c. Inhibitory activities depended on the chitinase tested.
