Kenneth Alan Koeplinger

US Patent:

6653331, Nov 25, 2003

Filed:

Mar 17, 1999

Appl. No.:

09/147469

Inventors:

Zhiyang Zhao - Westerly RI
Alfredo G. Tomasselli - Kalamazoo MI
Kenneth A. Koeplinger - Portage MI
Tillie Peterson - Portage MI

Assignee:

Pharmacia Upjohn Company - Kalamazoo MI

International Classification:

A61K 3118

US Classification:

514344, 514347, 514367, 514603, 514604, 546288, 546293, 548166, 564 87, 564 92

Abstract:

The present invention relates to Glutathione S-transferase (GST)/Reduced Glutathione (GSH) as a means for the in-vivo release of a drug that has been conjugated to specific electrophilic moieties via a sulfonamide bond. The drug may be an anticancer agent (or one with other therapeutic properties) carrying a free âNHâ which has been derivatized by the attachment of an electrophile containing a moiety, such as p-CNâ or p-NO -pyridinylsulfonyl groups, or p-NO - or 2,4 dinitrophenylsulfonyl groups, or suitable derivatives thereof, to make a prodrug. Optionally, the sulfonamide moiety may have attached to it a targeting molecule. The present invention also provides Glutathione S-transferase (GST)/Reduced Glutathione (GSH) as a means for the release of a protected amino derivative that has been conjugated to specific electrophilic moieties via a sulfonamide bond. The precursor is a synthetic intermediate carrying a free âNHâ which has been derivatized by the attachment of an electrophile via a sulfonamide bond.

US Patent:

7632821, Dec 15, 2009

Filed:

Aug 4, 2006

Appl. No.:

11/990051

Inventors:

Gabor Butora - Martinsville NJ, US
Kenneth Alan Koeplinger - Lansdale PA, US
Malcolm MacCoss - Freehold NJ, US
Daniel R. McMasters - New York NY, US
David B. Olsen - Lansdale PA, US
Lihu Yang - Edison NJ, US

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A01N 43/04
A61K 31/70

US Classification:

514 43, 514 45, 514 48, 514 49, 514 50, 514 51, 536 271, 536 2713, 536 281

Abstract:

The present invention provides ribonucleoside 2′,3′-cyclic acetals of structural formula I which are precursors or prodrugs of inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors of inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors or prodrugs of inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors or prodrugs of inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such ribonucleoside 2′,3′-cyclic acetals alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the ribonucleoside 2′,3′-cyclic acetals of the present invention.

US Patent:

20020045205, Apr 18, 2002

Filed:

May 22, 2001

Appl. No.:

09/862915

Inventors:

Robert Heinrikson - Plainwell MI, US
Alfredo Tomasselli - Kalamazoo MI, US
Kenneth Koeplinger - Kalamazoo MI, US

International Classification:

C12P021/06
C07H021/04
C12N009/64
C12N005/06
C12P021/02

US Classification:

435/068100, 435/069100, 435/325000, 435/226000, 435/320100, 536/023200

Abstract:

A novel recombinant procaspase 8 protein lacking the death effector domains and a method for converting said novel procaspase protein to full active human caspase 8 by concentration of the procaspase 8 on a collection device.

US Patent:

63033291, Oct 16, 2001

Filed:

Jul 23, 1999

Appl. No.:

9/360017

Inventors:

Robert Leroy Heinrikson - Plainwell MI
Alfredo Giuseppe Tomasselli - Kalamazoo MI
Kenneth A. Koeplinger - Kalamazoo MI

Assignee:

Pharmacia & Upjohn Company - Kalamazoo MI

International Classification:

C12Q 137
C12N 950
C12P 2106

US Classification:

435 681

Abstract:

A novel recombinant procaspase 8 protein lacking the death effector domains and a method for converting said novel procaspase protein to full active human caspase 8 by concentration of the procaspase 8 on a collection device.