Kenneth A James

US Patent:

6593492, Jul 15, 2003

Filed:

Oct 25, 2000

Appl. No.:

09/695884

Inventors:

Nnochiri Nkem Ekwuribe - Cary NC
Kenneth D. James - Mebane NC

Assignee:

Nobex Corporation - Durham NC

International Classification:

C07C 6702

US Classification:

560250

Abstract:

A methods of preparing a substantially pure enantiomer of an acylanilide such as Casodex (bicalutamide) and/or its derivatives includes resolving an intermediate compound having the structure of Formula I: wherein R is alkyl or haloalkyl having up to 4 carbons; R is alkyl having up to 6 carbon atoms; R is a direct link or alkyl having up to 6 carbon atoms; R is alkyl, alkenyl, hydroxyalkyl or cycloalkyl each of up to 6 carbons; or R is phenyl which bears one, two or three substituents independently selected from hydrogen, halogen, nitro, carboxy, carbamoyl and cyano, and alkyl, alkoxy, alkanoyl, alkylthio, alkylsulphinyl, alkylsulphonyl, perfluoroalkyl, perfluoroalkylthio, perfluoroalkylsulphinyl, perfluoroalkylsulphonyl, alkoxycarbonyl and N-alkylcarbamoyl each of up to 4 carbon atoms, and phenyl, phenylthio, phenylsulphinyl and phenylsulphonyl; or R is naphthyl; or R is a 5- or 6-membered saturated or unsaturated heterocyclic which contains one, two or three heteroatoms selected from oxygen, nitrogen and sulfur, which heterocyclic may be a single ring or may be fused to a benzo-ring, and which heterocyclic is unsubstituted or bears one or two halogen, cyano or amino, or alkyl, alkoxy, alkylthio, alkylsulphinyl or alkylsulphonyl each of up to 4 carbon atoms, or oxy or hydroxy substituents, or which if sufficiently saturated may bear one or two oxo substituents; and X is oxygen, sulfur, sulphinyl (âSOâ), sulphonyl (âSO â), imino (âNHâ) or alkylimino (âNR â) where R is alkyl having up to 6 carbon atoms. The resolved intermediate compound of Formula I is then treated under conditions sufficient to provide a substantially pure enantiomer of an acylanilide such as Casodex (bicalutamide) and/or its derivatives.

US Patent:

7605123, Oct 20, 2009

Filed:

Jul 19, 2005

Appl. No.:

11/184528

Inventors:

Balasingam Radhakrishnan - Chapel Hill NC, US
Diti Aggarwal - Raleigh NC, US
Michelle Ferro - Raleigh NC, US
Kenneth D. James - Mebane NC, US
Navdeep B. Malkar - Cary NC, US
Mark A. Miller - Raleigh NC, US
Leo Pavliv - Morrisville NC, US
Karen Polowy - Raleigh NC, US
Monica Puskas - Spring Hope NC, US
Nnochiri N. Ekwuribe - Cary NC, US

Assignee:

Biocon Ltd.

International Classification:

A61K 38/28

US Classification:

514 3, 514 2, 514 4, 530303, 530345

Abstract:

Fatty acid compositions for administration of of pharmaceutical agents, such as proteins and peptides, protein and peptide conjugates, and/or cation-polypeptide conjugate complexes. In particular, the invention provides a solid pharmaceutical composition formulated for oral administration by ingestion, having from about 0. 1 to about 75% w/w fatty acid component, where the fatty acid component comprises saturated or unsaturated C4, C5, C6, C7, C8, C9, C10, C11, or C12 fatty acids and/or salts of such fatty acids; and a therapeutic agent. Further, the invention provides a liquid pharmaceutical composition formulated for oral administration by ingestion, comprising: from about 0. 1 to about 10% w/v fatty acid component, where the fatty acid component comprises saturated or unsaturated C4, C5, C6, C7, C8, C9, C10, C11, or C12 fatty acids and/or salts of such fatty acids; and a therapeutic agent.

US Patent:

7648962, Jan 19, 2010

Filed:

Nov 30, 2004

Appl. No.:

10/999761

Inventors:

Kenneth D. James - Mebane NC, US
Balasingham Radhakrishnan - Chapel Hill NC, US
Navdeep B. Malkar - Cary NC, US
Mark A. Miller - Raleigh NC, US
Nnochiri N. Ekwuribe - Cary NC, US

Assignee:

Biocon Limited

International Classification:

A61K 38/16
C07K 14/00
A61K 47/48
A61K 9/00

US Classification:

514 12, 530324, 424400

Abstract:

Modified natriuretic compounds and conjugates thereof are disclosed in the present invention. In particular, conjugated forms of hBNP are provided that include at least one modifying moiety attached thereto. The modified natriuretic compound conjugates retain activity for stimulating cGMP production, binding to NPR-A receptor, and in some embodiments an improved half-life in circulation as compared to unmodified counterpart natriuretic compounds. Oral, parenteral, enteral, subcutaneous, pulmonary, and intravenous forms of the compounds and conjugates may be prepared as treatments and/or therapies for heart conditions particularly congestive heart failure. Modifying moieties comprising oligomeric structures having a variety of lengths and configurations are also disclosed. Analogs of the natriuretic compound are also disclosed, having an amino acid sequence that is other than the native sequence.

US Patent:

7662773, Feb 16, 2010

Filed:

Nov 26, 2003

Appl. No.:

10/723933

Inventors:

Kenneth D. James - Mebane NC, US
Balasingam Radhakrishnan - Chapel Hill NC, US
Navdeep B. Malkar - Cary NC, US
Mark A. Miller - Raleigh NC, US
Nnochiri N. Ekwuribe - Cary NC, US

Assignee:

Biocon Limited

International Classification:

A61K 38/03
A61K 8/64

US Classification:

514 2

Abstract:

Modified natriuretic compounds and conjugates thereof are disclosed in the present invention. In particular, conjugated forms of hBNP are provided that include at least one modifying moiety attached thereto. The modified natriuretic compound conjugates retain activity for stimulating cGMP production, binding to NPR-A receptor, and in some embodiments an improved half-life in circulation as compared to unmodified counterpart natriuretic compounds. Oral, parenteral, subcutaneous, and intravenous forms of the compounds and conjugates may be prepared as treatments and/or therapies for heart conditions particularly congestive heart failure. Modifying moieties comprising oligomeric structures having a variety of lengths and configurations are also disclosed. Analogs of the natriuretic compound are also disclosed, having an amino acid sequence that is other than the native sequence.

US Patent:

7872095, Jan 18, 2011

Filed:

Jul 19, 2005

Appl. No.:

11/184594

Inventors:

Balasingam Radhakrishnan - Chapel Hill NC, US
Diti Aggarwal - Raleigh NC, US
Michelle Ferro - Raleigh NC, US
Kenneth D. James - Mebane NC, US
Navdeep B. Malkar - Cary NC, US
Mark A. Miller - Raleigh NC, US
Monica Puskas - Spring Hope NC, US
Nnochiri N. Ekwuribe - Cary NC, US

Assignee:

Biocon Limited

International Classification:

C07K 14/62

US Classification:

530303, 514 3, 530345

Abstract:

An insulin compound coupled to a modifying moiety having a formula:—X—R—Y-PAG-Z—R  (Formula VI).

US Patent:

7875700, Jan 25, 2011

Filed:

Jul 19, 2005

Appl. No.:

11/184668

Inventors:

Balasingam Radhakrishnan - Chapel Hill NC, US
Diti Aggarwal - Raleigh NC, US
Michelle Ferro - Raleigh NC, US
Kenneth D. James - Mebane NC, US
Navdeep B. Malkar - Cary NC, US
Mark A. Miller - Raleigh NC, US
Monica Puskas - Spring Hope NC, US
Nnochiri N. Ekwuribe - Cary NC, US

Assignee:

Biocon Limited

International Classification:

A61K 38/28

US Classification:

530304, 530303, 530345, 514 2, 514 3, 514 4

Abstract:

The invention provides a complex including a cation and an insulin compound conjugate. The insulin compound conjugate includes insulin compound, such as human insulin or an analog thereof, conjugated to a modifying moiety, such as a polyethylene glycol moiety. The invention also includes solids and pharmaceutical compositions including such complexes, methods of making such complexes, and methods of using such complexes in the treatment of insulin compound deficiencies and other ailments. Further, the invention includes novel insulin compound conjugates and modifying moieties for use in making novel insulin compound conjugates. The invention also includes fatty acid compositions for administration of pharmaceutical agents, such as the novel insulin compound conjugates, and/or the cation-insulin compound conjugate complexes of the invention.

US Patent:

8563685, Oct 22, 2013

Filed:

Oct 20, 2009

Appl. No.:

12/581953

Inventors:

Balasingam Radhakrishnan - Chapel Hill NC, US
Diti Aggarwal - Raleigh NC, US
Michelle Ferro - Raleigh NC, US
Kenneth D. James - Mebane NC, US
Navdeep B. Malkar - Cary NC, US
Mark A. Miller - Raleigh NC, US
Leo Pavliv - Morrisville NC, US
Karen Polowy - Raleigh NC, US
Monica Puskas - Spring Hope NC, US
Nnochiri N. Ekwuribe - Cary NC, US

Assignee:

Biocon Limited

International Classification:

C07K 14/62

US Classification:

530303, 530345, 514 59, 514 69

Abstract:

Fatty acid compositions for administration of of pharmaceutical agents, such as proteins and peptides, protein and peptide conjugates, and/or cation-polypeptide conjugate complexes. In particular, the invention provides a solid pharmaceutical composition formulated for oral administration by ingestion, having from about 0. 1 to about 75% w/w fatty acid component, where the fatty acid component comprises saturated or unsaturated C4, C5, C6, C7, C8, C9, C10, C11, or C12 fatty acids and/or salts of such fatty acids; and a therapeutic agent. Further, the invention provides a liquid pharmaceutical composition formulated for oral administration by ingestion, comprising: from about 0. 1 to about 10% w/v fatty acid component, where the fatty acid component comprises saturated or unsaturated C4, C5, C6, C7, C8, C9, C10, C11, or C12 fatty acids and/or salts of such fatty acids; and a therapeutic agent.

US Patent:

20020165406, Nov 7, 2002

Filed:

May 2, 2001

Appl. No.:

09/847229

Inventors:

Nnochiri Ekwuribe - Cary NC, US
Kenneth James - Mebane NC, US

International Classification:

C07C255/49
C07C235/32

US Classification:

558/418000, 564/199000

Abstract:

Methods of synthesizing an acylanilide include contacting a compound having the structure of Formula I: with a compound having the structure of Formula II: under conditions sufficient to provide a compound having the structure of Formula III: and treating the compound of Formula III under conditions sufficient to provide an acylanilide. The compound of Formula III may be addition reacted with a compound having the structure of Formula IV: under conditions sufficient to provide an acylanilide having the structure of Formula V: