Brian J Moulton

US Patent:

7927613, Apr 19, 2011

Filed:

Sep 11, 2003

Appl. No.:

10/660202

Inventors:

Magali Bourghol Hickey - Medford MA, US
Matthew L. Peterson - Framingham MA, US
Michael J. Zaworotko - Tampa FL, US
Brian Moulton - Providence RI, US

Assignee:

University of South Florida - Tampa FL
The Regents of the University of Michigan - Ann Arbor MI
Transform Pharmaceuticals, Inc. - Lexington MA

International Classification:

A61K 9/00
A01N 43/46
A01N 43/56

US Classification:

424400, 514217, 514403

Abstract:

A pharmaceutical composition comprising a co-crystal of an API and a co-crystal former; wherein the API has at least one functional group selected from ether, thioether, alcohol, thiol, aldehyde, ketone, thioketone, nitrate ester, phosphate ester, thiophosphate ester, ester, thioester, sulfate ester, carboxylic acid, phosphonic acid, phosphinic acid, sulfonic acid, amide, primary amine, secondary amine, ammonia, tertiary amine, sp2 amine, thiocyanate, cyanamide, oxime, nitrile diazo, organohalide, nitro, s-heterocyclic ring, thiophene, n-heterocyclic ring, pyrrole, o-heterocyclic ring, furan, epoxide, peroxide, hydroxamic acid, imidazole, pyridine and the co-crystal former has at least one functional group selected from amine, amide, pyridine, imidazole, indole, pyrrolidine, carbonyl, carboxyl, hydroxyl, phenol, sulfone, sulfonyl, mercapto and methyl thio, such that the API and co-crystal former are capable of co-crystallizing from a solution phase under crystallization conditions.

US Patent:

20070059356, Mar 15, 2007

Filed:

Feb 26, 2004

Appl. No.:

10/546963

Inventors:

Magali Bourghol Hickey - Medford MA, US
Matthew Peterson - Hopkinton MA, US
Michael Zaworotko - Tampa FL, US
Brian Moulton - Providence RI, US

International Classification:

A61K 31/551
A61K 31/55
A61K 31/496
A61K 31/415
A61K 31/455

US Classification:

424464000, 514220000, 514221000, 514406000, 514356000, 514217000, 514254070, 514574000

Abstract:

A pharmaceutical composition comprising a co-crystal of an API and a co-crystal former; wherein the API has at least one functional group selected from ether, thioether, alcohol, thiol, aldehyde, ketone, thioketone, nitrate ester, phosphate ester, thiophosphate ester, ester, thioester, sulfate ester, carboxylic acid, phosphinic acid, phosphonic acid, sulfonic acid, amide, primary amine, secondary amine, ammonia, tertiary amine, imine, thiocyanate, cyanamide, oxime, nitrile diazo, organohalide, nitro, S-heterocyclic ring, thiophene, N-heterocyclic ring, pyrrole, 0-heterocyclic ring, furan, epoxide, peroxide, hydroxamic acid, imidazole, pyridine and the co-crystal former has at least one functional group selected from amine, amide, pyridine, imidazole, indole, pyrrolidine, carbonyl, carboxyl, hydroxyl, phenol, sulfone, sulfonyl, mercapto and methyl thio, such that the API and co-crystal former are capable of co-crystallizing from a solution phase under crystallization conditions.

US Patent:

20090209046, Aug 20, 2009

Filed:

May 21, 2007

Appl. No.:

12/227471

Inventors:

Brian Douglas Moulton - Somerville MA, US
Zhenbo Ma - Providence RI, US

International Classification:

G01N 33/566
C07F 19/00

US Classification:

436501, 546 6, 544225

Abstract:

The invention comprises neutral multi-functionality assemblies of pharmaceuticals comprising an active medicinal functionality, a transition metal functionality, and an ancillary ligand functionality. An exemplary series of mixed-ligand coordination complexes comprised of copper(II), a drug and an ancillary ligand were made and tested. It is demonstrated that the judicious choice of an ancillary ligand affords a large degree of control over die relative lipophilicity/hydrophilicity of the complex in relation to the uncomplexed drug molecule. The important factors to be considered in the design of such complexes, such as the additive-constitutive nature of the partition coefficient of the ancillary ligand and the relative size of the two types of ligands are disclosed, and methods of designing neutral multi-functionality assemblies of pharmaceuticals are disclosed.