摘要:
Non-peptide compounds that act as antagonists of the intestinal hormone glucagon-like peptide 1 (GLP-1) have a 9H-β-carboline central motif. The compounds exhibit advantageous physical, chemical and biological properties and inhibit GLP-1 peptide binding to the GLP-1 receptor and/or prevent activation of the receptor by bound GLP-1. The invention further relates to a method of inhibiting the binding of GLP-1 to the GLP-1 receptor and a method of inhibiting the activation of the GLP-1 receptor. Intermediate compounds useful for making non-peptide GLP-1 receptor antagonists are also described.
摘要:
A perinone compound represented by the formula
wherein R represents arylene; R and R, which may be the same or different, each represents alkoxyalkyl, hydroxyalkyl, N,N-dialkylaminoalkyl. cycloalkyl or aralkyl; and X represents oxygen or sulfur. Preparation methods are by reaction of a compound having the essential structure with either X=C-NHRNHR' to replace 2 halogen atoms, or with a carbonylating or thiocarbonylating agent, in an inert solvent. The compounds fluoresce yellowish green to orange in color and are useful for dyeing fibers, textiles, synthetic plastics molding and films.
wherein A is a radical selected from the group consisting of formulae A 1 to A 8 :
wherein the arrow denotes the point of attachment to the radical B; and B is a radical selected from the group consisting of formulae B 1 to B 11 :
wherein the arrow denotes the point of attachment to the radical A; and wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as insecticides and can be prepared in a manner known per se.