Abstract: The present invention provides a new prodrug technology and new prodrugs in order to increase the solubility, to modulate plasma protein binding or to enhance the biovailability of a drug. In the present invention the prodrugs are conjugates of a therapeutic compound and a peptide (eg tetrapeptide or hexapeptide) wherein the conjugate is cleavable by dipeptidyl-peptidases, more preferably by CD26, also known as DPPIV (dipeptidyl aminodipeptidase IV). The present invention furthermore provides a method of producing the prodrugs, to enhance brain and lymphatic delivery of drugs and/or to extend drug half-lives in plasma.
Type:
Grant
Filed:
May 10, 2004
Date of Patent:
August 7, 2012
Assignees:
Consejo Superior de Investigaciones Clentificas (CSIC), K.U. Leuven Research & Development
Inventors:
Jan Balzarini, Maria José Camarasa Ríus, Sonsoles Velázquez Díaz
Abstract: The invention relates to a method of preparing an alkylated aromatic compound. The inventive method is characterized in that it comprises an alkylation reaction of an aromatic compound with an alkylating agent which is selected from an olefin, an alcohol and a polyalkylated aromatic compound, in the presence of a catalyst which is a porous crystalline material with the following chemical composition in the calcined form: X2O3:n YO2:m ZO2, wherein (n+m) is at least 5, X is at least a trivalent element, Z is Ge, Y is at least a tetravalent element different from Ge and the n/m ratio is at least 1. Said method is particularly suitable for obtaining cumene.
Type:
Grant
Filed:
January 11, 2005
Date of Patent:
October 21, 2008
Assignees:
Consejo Superior de Investigaciones Clentificas, Universidad Politecnica de Valencia
Inventors:
Avelino Corma Canós, Fernando Rey García, María José Díaz Cabañas