Team Lead, Chem Modeling & Informatics at Merck & Co., Inc.
Location:
Greater Boston Area
Industry:
Pharmaceuticals
Work:
Merck & Co., Inc. since Mar 2000
Team Lead, Chem Modeling & Informatics
Education:
Universität Basel 1994 - 1997
D.Phil., Physical chemistry
University of Chicago 1991 - 1993
M.Sc., Organic chemistry
Stanford University 1987 - 1991
B.S., Chemistry
Balkrishen Bhat - Carlsbad CA, US Anne Eldrup - Encinitas CA, US Steven Carroll - Yardley PA, US David Olsen - Lansdale PA, US Daniel McMasters - New York NY, US Malcolm MacCoss - Freehold NJ, US Jie Xia - Carlsbad CA, US
International Classification:
A61K031/7072 A61K031/513 C 07D 4 9/04
US Classification:
514/050000, 514/269000, 536/028100, 544/317000
Abstract:
The present invention provides nucleoside compounds and certain derivatives thereof 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 inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds 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 compounds of the present invention.
Ribonucleoside Cyclic Acetal Derivatives For The Treatment Of Rna-Dependent Rna Viral Infection
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
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 pre-cursors 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.
Novel Tricyclic Compounds As Inhibitors Of Mutant Idh Enzymes
- Rahway NJ, US Stephane L. Bogen - Rahway NJ, US Matthew L. Childers - Boston MA, US Francesc Xavier Fradera Llinas - Boston MA, US Michael J. Ellis - Boston MA, US Sara Esposite - Neptune NJ, US Qingmei Hong - Kenilworth NJ, US Chunhui Huang - Kenilworth NJ, US Alexander J. Kim - Rahway NJ, US John W. Lampe - Cary NC, US Michelle R. Machacek - Boston MA, US Daniel R. McMasters - Boston MA, US Ryan D. Otte - Boston MA, US Michael H. Reutershan - Boston MA, US Nunzio Sciammetta - Boston MA, US Patrick Pengcheng Shao - Kenilworth NJ, US David L. Sloman - Boston MA, US Feroze Ujjainwalla - Kenilworth NJ, US Catherine White - Boston MA, US Zhicai Wu - Kenilworth NJ, US Yang Yu - Kenilworth NJ, US Kake Zhao - Kenilworth NJ, US Craig R. Gibeau - Boston MA, US
The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
Novel Tricyclic Compounds As Inhibitors Of Mutant Idh Enzymes
- Rahway NJ, US Stephane L. Bogen - Rahway NJ, US Matthew Lloyd Childers - Boston MA, US Francesc Xavier Fradera Llinas - Boston MA, US Alexander J. Kim - Rahway NJ, US John W. Lampe - Cary NJ, US Michelle R. Machacek - Boston MA, US Daniel R. McMasters - Boston MA, US Nunzio Sciammetta - Boston MA, US Patrick Pengcheng Shao - Kenilworth NJ, US David L. Sloman - Boston MA, US Wanying Sun - Kenilworth NJ, US Feroze Ujjainwalla - Kenilworth NJ, US
The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I); wherein A is —C(R1)= or —N═; and X is selected from the group consisting of: (II-i), (II-ii), (I) (II-iii), and (II-iv). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
Novel Tricyclic Compounds As Inhibitors Of Mutant Idh Enzymes
- Rahway NJ, US Stephane L. Bogen - Rahway NJ, US Matthew L. Childers - Boston MA, US Francesc Xavier Fradera Llinas - Boston MA, US Michael J. Ellis - Boston MA, US Sara Esposite - Neptune NJ, US Dawn M. Hoffman - Boston MA, US Chunhui Huang - Kenilworth NJ, US Solomon D. Kattar - Boston MA, US Alexander J. Kim - Rahway NJ, US John W. Lampe - Cary NJ, US Michelle R. Machacek - Boston MA, US Daniel R. McMasters - Boston MA, US Michael H. Reutershan - Boston MA, US Nunzio Sciammetta - Boston MA, US Patrick Pengcheng Shao - Kenilworth NJ, US David L. Sloman - Boston MA, US Wanying Sun - Kenilworth NJ, US Feroze Ujjainwalla - Kenilworth NJ, US Zhicai Wu - Kenilworth NJ, US Yang Yu - Kenilworth NJ, US Craig R. Gibeau - Boston MA, US
Assignee:
Merck Sharp & Dohme Corp. - Rahway NJ
International Classification:
C07D 471/04 C07D 519/00 C07D 471/14
Abstract:
The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes (I); wherein A is —C(R)═ or —N═; and X is selected from the group consisting of: (II-i), and (II-ii). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.