公开(公告)号：US20220305013A1

公开(公告)日：2022-09-29

申请号：US17619837

申请日：2020-06-18

申请人： THE GOVERNING COUNCIL OF THE UNIVERSITY OF TORONTO ,  THE REGENTS OF THE UNIVERSITY OF CALIFORNIA

发明人： Molly S. SHOICHET ,  Ahil N. GANESH ,  Eric N. DONDERS ,  Brian K. SHOICHET ,  Hayarpi TOROSYAN

IPC分类号： A61K31/506 ,  A61K9/10 ,  A61K47/42 ,  A61K31/4174 ,  A61K31/438 ,  A61K47/28 ,  A61K47/34 ,  A61K31/566 ,  A61K31/44

摘要： The present application provides a colloid drug aggregate composition and methods of use and manufacture thereof. While the formation of colloidal aggregates leads to artifacts in early drug discovery, their composition makes them attractive as nanoparticle formulations for targeted drug delivery. The present application provides an acid-responsive composition comprising: a colloidal aggregate of one or more drugs and a stabilizing agent, wherein the colloidal aggregate disrupts, dissolves or disassembles when the acid-responsive composition is in an acid environment having a pH of less than 7.4. The colloidal aggregate of the composition will disassemble upon contact with acid or upon introduction to an acidic environment, such as is found in the endosomes of cells. This approach makes this composition an attractive vehicle for drug delivery to a target site in a subject or to cells.

公开(公告)号：US20170283437A1

公开(公告)日：2017-10-05

申请号：US15622972

申请日：2017-06-14

申请人： Wisconsin Alumni Research Foundation ,  The Regents of the University of California

发明人： Laura L. KIESSLING ,  Virginia A. KINCAID ,  Nir LONDON ,  Brian K. SHOICHET

IPC分类号： C07D513/04 ,  C07D417/04

CPC分类号： C07D513/04 ,  C07D417/04

摘要： Compounds and salts thereof which inhibit microbial growth or attenuate the virulence of pathogenic microorganisms and which inhibit UDP-galactopyranose mutase (UGM). Compounds of the invention include triazolothiadiazines, particularly 3, 6, 7-substituted-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines, and 4-(1H-pyrrol-3-yl) thiazoles, particularly 4-(1,2,5-substituted-1H-pyrrol-3-yl)-2-substituted thiazoles, and salts thereof. Methods for inhibiting growth or attenuating virulence of microbial pathogens including mycobacterium, for example, M. tuberculosis and M. smegmatis and Klebsiella, for example, Klebsiella pneumoniae. Methods for inhibiting eukaryotic human and animal pathogens, and fungi and nematodes in particular. Methods for treatment of infections by prokaryotic and eukaryotic pathogens employing compounds of the invention.