Michael Joseph Palte

US Patent:

20130196433, Aug 1, 2013

Filed:

Jan 18, 2013

Appl. No.:

13/745737

Inventors:

Ronald T. Raines - Madison WI, US
Gregory Ellis - Madison WI, US
Michael Palte - Madison WI, US

International Classification:

C07K 19/00

US Classification:

435375, 530300, 530350, 562443, 564 8

Abstract:

Methods for enhancing cellular uptake of cargo molecules by boronating the cargo molecule, particularly with one or more phenylboronic acid groups. Cellular uptake includes at least partial uptake into the cytosol. Boronation includes ligating, crosslinking or otherwise bonding one or more phenylboronic acids substituted to contain a reactive group to a cargo molecule. Boronation also includes ligating, crosslinking or otherwise bonding a phenylboronated oligopeptide to a cargo molecule. The phenylboronate groups are optionally conjugated to the cargo molecule via linking moieties that can be selectively cleaved, such cleavable linkers can allow the phenylboronate groups to be removed from the cargo molecule after the boronated cargo molecule is introduced into the cell. The invention includes certain phenylboronates which are boronation reagents, certain boronated oligopeptides and certain boronated peptides and proteins. The invention also includes kits for enhancing cellular uptake of cargo molecules by boronation with one or more phenylboronates or boronated oligopeptides.

US Patent:

20130178617, Jul 11, 2013

Filed:

Sep 27, 2012

Appl. No.:

13/629588

Inventors:

Ronald Raines - Madison WI, US
Benjamin Caes - West Des Moines IA, US
Michael Palte - Madison WI, US

International Classification:

C07D 307/50
B01J 27/20

US Classification:

536124, 549489, 502172, 502169

Abstract:

Methods and catalyst compositions for formation of furans from carbohydrates. A carbohydrate substrate is heating in the presence of a 2-substituted phenylboronic acid (or salt or hydrate thereof) and optionally a magnesium or calcium halide salt. The reaction is carried out in a polar aprotic solvent other than an ionic liquid, an ionic liquid or a mixture thereof. Additional of a selected amount of water to the reaction can enhance the yield of furans.

US Patent:

20170327517, Nov 16, 2017

Filed:

Jul 28, 2017

Appl. No.:

15/662813

Inventors:

- Madison WI, US
Ian WINDSOR - Wisconsin Rapids WI, US
Michael PALTE - Melrose MA, US
John LUKESH - Madison WI, US

International Classification:

C07F 5/02
A61K 31/427
A61K 31/34
A61K 31/69
A61K 31/00

Abstract:

Protease inhibitors, particularly aspartyl protease inhibitors, and more particularly HIV protease inhibitors which are boronated to enhance activity or to enhance entry into cells. Compounds, prodrugs and salts thereof of this invention contain phenylboronate groups, in particular p-B(OH)-phenyl groups, benzoxaborole groups or borono-pyridyl groups or analogous groups in which the boronate group is protected. Methods for treating AIDS and ARC as well as providing a method for treating or preventing HIV infection

US Patent:

20160122366, May 5, 2016

Filed:

Oct 29, 2015

Appl. No.:

14/927390

Inventors:

- Madison WI, US
Ian Windsor - Wisconsin Rapids WI, US
Michael Palte - Melrose MA, US
John Lukesh - Madison WI, US

International Classification:

C07F 5/02
A61K 31/427
A61K 31/69

Abstract:

Protease inhibitors, particularly aspartyl protease inhibitors, and more particularly HIV protease inhibitors which are boronated to enhance activity or to enhance entry into cells. Compounds, prodrugs and salts thereof of this invention contain phenylboronate groups, in particular p-B(OH)-phenyl groups, benzoxaborole groups or borono-pyridyl groups or analogous groups in which the boronate group is protected. Methods for treating AIDS and ARC as well as providing a method for treating or preventing HIV infection

US Patent:

20160083706, Mar 24, 2016

Filed:

Dec 2, 2015

Appl. No.:

14/957040

Inventors:

- Madison WI, US
Gregory Ellis - Madison WI, US
Michael Palte - Madison WI, US

International Classification:

C12N 9/36
C12N 9/22

Abstract:

Cargo molecules carrying one or more phenylboronate moieties useful for cellular uptake of the cargo molecules. Phenylboronate can be ligated, crosslinked or otherwise bonded to the cargo molecules. Cargo molecules include peptides and proteins. The phenylboronate groups are optionally conjugated to the cargo molecule via linking moieties that can be selectively cleaved, such cleavable linkers can allow the phenylboronate groups to be removed from the cargo molecule after the boronated cargo molecule is introduced into the cell. The invention includes certain phenylboronates which are boronation reagents, certain boronated oligopeptides and certain boronated peptides and proteins. The invention also includes kits for enhancing cellular uptake of cargo molecules by boronation with one or more phenylboronates or boronated oligopeptides.