David OlsenUnion Center, NJ

6369208, Apr 9, 2002

Mar 30, 1998

08/973137

James L. Cole - Rahway NJ
Lawrence C. Kuo - Rahway NJ
David B. Olsen - Rahway NJ
Fritz Benseler - Rahway NJ

Merck Co., Inc. - Rahway NJ

C07H 2102

536 231, 536 243, 536 2432, 435196, 4352351

A method is provided for making synthetic capped RNAs. These compounds serve as substrates for the virally encoded endonuclease associated with influenza virus. We are able to assay for this unique and specific viral activity of cleavage of a capped RNA in vitro. Therefore, screening of inhibitors of this activity is possible. In addition, short non-extendible (due to their length or because of the modification of the 3â-end of the oligo, i. e. 3â-dA) RNAs are potent inhibitors of the cleavage of capped RNAs by influenza endonuclease. Finally, these compounds may be used to investigate viral and cellular mechanisms of transcription/translation or mRNA maturation.

7632821, Dec 15, 2009

Aug 4, 2006

11/990051

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

Merck & Co., Inc. - Rahway NJ

A01N 43/04
A61K 31/70

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

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.

7879815, Feb 1, 2011

Feb 12, 2007

12/223940

Malcolm MacCoss - Freehold NJ, US
David B. Olsen - Lansdale PA, US
Monica Donghi - Rome, IT
Cristina Gardelli - Rome, IT
Steven Harper - Rome, IT
Malte Meppen - Rome, IT
Frank Narjes - Rome, IT
Barbara Pacini - Rome, IT

Merck Sharp & Dohme Corp. - Rahway NJ
Istituto di Ricerche di Biologia Molecolare P. Angeletti S.p.A. - Pomezia, Rome

A01N 43/04
A61K 31/70

514 49, 514 43

The present invention provides nucleoside aryl phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to 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 to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside aryl phosphoramidates 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 nucleoside aryl phosphoramidates of the present invention.

2007026, Nov 15, 2007

Jun 20, 2005

11/628934

Malcolm MacCoss - Freehold NJ, US
David Olsen - Lansdale PA, US

A61K 31/7076
A61P 1/16
A61P 31/12
C07H 19/16

514045000, 536026700

The present invention provides nucleoside aryl phosphoramidates which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to 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 to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside aryl phosphoramidates 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 nucleoside aryl phosphoramidates of the present invention.

2008028, Nov 13, 2008

Oct 17, 2005

11/664564

Malcolm MacCoss - Freehold NJ, US
David B. Olsen - Lansdale PA, US
Joseph Leone - Tinton Falls NJ, US
Philippe L. Durette - New Providence NJ, US

MERCK & CO., INC. - Rahway NJ

A61K 31/7064
C07H 19/04
A61P 31/12

514 43, 536 272

The present invention provides fluorinated pyrrolo[2,3,d]pyrimidine nucleoside compounds which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are 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 to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such fluorinated pyrrolo[2,3-d]pyrimidine nucleoside 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 fluorinated pyrrolo[2,3-d]pyrimidine nucleoside of the present invention.

2013000, Jan 3, 2013

Dec 17, 2010

13/518613

Sheo Singh - Edison NJ, US
Jon D. Polishook - Old Bridge NJ, US
Deborah L. Zink - Manalapan NJ, US
Olga Genilloud - Madrid, ES
Michael Goetz - Scotch Plains NJ, US
Francisca Vicente - Madrid, ES
David Brian Olsen - Lansdale PA, US
Scott Knoble Smith - San Jose CA, US

C07H 15/26
C12P 19/46
A61P 31/04
C12N 1/20
A61K 31/706
A61K 31/7056

514 35, 536 168, 4352521, 435 79

The present invention relates to novel compounds of formulae (I) and (II) and pharmaceutically acceptable salts thereof that are useful in the treatment and/or prevention of human and animal bacterial infections and associated diseases and conditions; compositions containing such compounds; derivation of such compounds by fermentation and isolation, partial synthesis and total synthesis; methods of inhibiting bacterial growth; methods of treating, preventing or controlling bacterial infection; biologically pure cultures of bacterial strains from which such compounds may be produced; and processes for preparing compositions containing such compounds.

2022033, Oct 20, 2022

Jul 21, 2020

17/633655

- Rahway NJ, US
- Parkville, Victoria, AU
- Beijing, AU
Paola Favuzza - Melbourne, AU
Zhuyan Guo - Scotch Plains NJ, US
Bin Hu - Shanghai, CN
Zhiyu Lei - Shanghai, CN
David B. Olsen - Lansdale PA, US
Brad Sleebs - Bundoora, Victoria, AU
Jennifer K. Thompson - Melbourne, AU
Tony Triglia - Melbourne, AU
Dongmei Zhan - Shanghai, CN
Cailing Zhang - Shanghai, CN
Lianyun Zhao - Shanghai, CN

Merck Sharp & Dohme Corp. - Rahway NJ
The Walter and Eliza Hall Institute of Medical Research - 1G Royal Parade
MSD R & D (China) Co. LTD. - Beijing

A61K 31/513
C07D 405/14
C07D 493/10
C07D 491/052
C07D 409/14
C07D 239/22
C07D 405/12
C07D 409/04
A61P 33/06
A61K 45/06

Methods of treating malaria comprising administration of compounds of Formula (I′) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables are as defined herein. It also provides uses of the compounds of Formula (I), as defined herein, for inhibiting plasmepsin X, plasmepsin IX or plasmepsin X and IX activity, for treating a infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.

2016012, May 5, 2016

Jun 16, 2014

14/899008

- Rahway NJ, US
Vinay Girijavallabhan - Denville NJ, US
Quang Truong - Morganville NJ, US
Ping Chen - Edison NJ, US
Frank Bennett - Cranford NJ, US
Angela Kerekes - Plainfield NJ, US
Qun Dang - Westfield NJ, US
David B. Olsen - Lansdale PA, US
Ian Davies - Princeton NJ, US

Merck Sharp & Dohme Corp. - Rahway NJ

C07H 19/10
A61K 45/06
A61K 31/7072

The present invention relates to Cyclic Phosphonate Substituted Nucleoside Derivatives of Formula (I): (structure) and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3 are as defined herein, as well as to compositions and methods of using the Cyclic Phosphonate Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.