Tatyana A Dyakonov

US Patent:

6525098, Feb 25, 2003

Filed:

Oct 27, 2000

Appl. No.:

09/697795

Inventors:

Nnochiri Nkem Ekwuribe - Cary NC
Tatyana A. Dyakonov - Greensboro NC

Assignee:

Nobex Corporation - Durham NC

International Classification:

A61K 3119

US Classification:

514569, 514682, 514732

Abstract:

The present invention provides therapeutically effective amounts of 6MNA prodrugs. The pharmaceutical composition comprises wherein R is H or CORâ, wherein Râ is selected from the group consisting of C to C alkyl, (CH ) O(CH ) , (CH ) (OC H ) O(CH ) , (CH ) (OC H ) , (OCH H ) ONO and (OCH H ) O(CH ) wherein m is an integer from 2 to 4, and n and p are integers from 1 to 4. Alternatively, R is a therapeutic moiety.

US Patent:

6713454, Mar 30, 2004

Filed:

Dec 31, 1999

Appl. No.:

09/474915

Inventors:

Nnochiri Ekwuribe - Cary NC
Christopher H. Price - Chapel Hill NC
Tatyana A. Dyakonov - Greensboro NC

Assignee:

Nobex Corporation - Research Triangle Park NC

International Classification:

A61K 31704

US Classification:

514 25, 514468, 536 181, 536 183, 549298

Abstract:

The present invention provides amphiphilic prodrugs comprising a therapeutic compound conjugated to an PEG-oligomer/polymer and methods for using said prodrugs to enable oral drug delivery and/or delivery of drugs across the blood brain barrier into the central nervous system.

US Patent:

7119074, Oct 10, 2006

Filed:

Mar 24, 2004

Appl. No.:

10/808044

Inventors:

Nnochiri Ekwuribe - Cary NC, US
Christopher H. Price - Chapel Hill NC, US
Tatyana A. Dyakonov - Greensboro NC, US

Assignee:

Nobex Corporation - Durham NC

International Classification:

A61K 31/704

US Classification:

514 25

Abstract:

The present invention provides amphiphilic prodrugs comprising a therapeutic compound conjugated to an PEG-oligomer/polymer and methods for using said prodrugs to enable oral drug delivery and/or delivery of drugs across the blood brain barrier into the central nervous system.

US Patent:

7842707, Nov 30, 2010

Filed:

Jul 21, 2005

Appl. No.:

11/571857

Inventors:

Susan Marie Royalty - Cary NC, US
James Ford Burns - Glen Ridge NJ, US
Jan Jozef Scicinski - Sunnyvale CA, US
Robert James Foglesong - Durham NC, US
Kellee Griffin Ring - Garner NC, US
Tatyana Dyakonov - Durham NC, US
David Middlemiss - Hertfordshire, GB

Assignee:

Nuada, LLC - Durham NC

International Classification:

A01N 43/40
A01N 43/78
A01N 43/80
A01N 43/36
A61K 31/44
A61K 31/425
A61K 31/42
A61K 31/40
C07D 401/00
C07D 277/00
C07D 261/00
C07D 295/00

US Classification:

514343, 514365, 514380, 514423, 5462791, 548200, 548243, 548540

Abstract:

The present invention relates to a series of novel compounds having the formula (I) wherein: X is NRor O; n is 1 or 2; A is a bicyclic carbocycle and R1 and R2 are as described herein. The compounds are useful as DPP-IV inhibitors, such as for the treatment of diabetes.

US Patent:

20030069309, Apr 10, 2003

Filed:

Jun 12, 2002

Appl. No.:

10/170800

Inventors:

Nnochiri Ekwuribe - Cary NC, US
Tatyana Dyakonov - Greensboro NC, US

International Classification:

A61K031/235
A61K031/075

US Classification:

514/532000, 514/721000

Abstract:

The present invention provides therapeutically effective amounts of 6MNA prodrugs. The pharmaceutical composition comprises wherein R is H or COR′, wherein R′ is selected from the group consisting of Cto Calkyl, (CH)O(CH), (CH)(OCH)O(CH), (CH)(OCH), (OCHH)ONOand (OCHH)O(CH)wherein m is an integer from 2 to 4, and n and p are integers from 1 to 4. Alternatively, R is a therapeutic moiety.

US Patent:

20040152769, Aug 5, 2004

Filed:

Nov 7, 2003

Appl. No.:

10/703647

Inventors:

Nnochiri Ekwuribe - Cary NC, US
Jennifer Riggs-Sauthier - Raleigh NC, US
Tatyana Dyakonov - Durham NC, US

International Classification:

A61K031/66
A61K031/325
A61K031/16

US Classification:

514/478000, 514/615000, 514/114000

Abstract:

Prodrugs having a hydrolyzable carbamate moiety, compositions including the prodrugs, methods of preparing the prodrugs and methods of treatment using the prodrugs are disclosed. The prodrug has the formula DC(X)XR, where D is a biologically active agent, X is O, S or NR′, and R is a moiety that modifies various properties of the biologically active agent. The biologically active agent either includes a functional group such as an amide, thioamide, imide, thioimide, urea, thiourea, carbamate, thiocarbamate, sulfonamide, or sulfonimide group, or includes a hydroxy, amine, carboxylic acid or thiol group that is modified to include such a group. An NH group from the biologically active agent can be coupled to an activated form the C(X)XR moiety to form the prodrugs described herein. Relative to a conventional carbamate group, the presence of the additional carbonyl or sulfonyl group makes the carbamate group more susceptible to hydrolysis. The prodrugs are more stable in certain environments than the biologically active agent, and can permit the drugs to be administered orally, in those embodiments where the biologically active agent must otherwise be administered by injection or intraveneous administration.

US Patent:

20040253206, Dec 16, 2004

Filed:

Mar 29, 2004

Appl. No.:

10/811760

Inventors:

Nnochiri Ekwuribe - Cary NC, US
Tatyana Dyakonov - Durham NC, US
Christopher Price - Chapel Hill NC, US

International Classification:

A61K038/17
C08G063/48
C08G063/91

US Classification:

424/078270, 525/054100

Abstract:

Drug-oligomer conjugates and pharmaceutical compositions prepared therefrom. Methods of making and using the drug-oligomer conjugates and pharmaceutical compositions.

US Patent:

20050054735, Mar 10, 2005

Filed:

Oct 21, 2004

Appl. No.:

10/970571

Inventors:

Nnochiri Ekwuribe - Cary NC, US
Tatyana Dyakonov - Greensboro NC, US

International Classification:

A61K031/445
A61K031/12
A61K031/075

US Classification:

514681000, 514319000, 514718000

Abstract:

The present invention provides therapeutically effective amounts of MNA prodrugs. The pharmaceutical composition comprises wherein R is H or COR′, wherein R′ is selected from the group consisting of Cto Calkyl, (CH)O(CH), (CH)(OCH)O(CH), (CH)(OCH), (OCHH)ONOand (OCHH)O(CH)wherein m is an integer from 2 to 4, and n and p are integers from 1 to 4. Alternatively, R is a therapeutic moiety.