Merck Sharp + Dohme Corp.

Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa

Msd Italia S.r.l.

Irbm-science Park S.p.a.

C.n.c.c.s. Scarl Collezione Nazionale Dei Composti Chimici E Centro Screening

Merck + Co., Inc.

Instituto Di Ricerche Di Biologia Molecolare P. Angeletti S.p.a.

Retrophin, Inc.

Istituto Di Ricerche Di Biologia P. Angeletti S.p.a.

Insituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa

Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.r.l.

Steven Harper

Vincenzo Summa

Nigel J Liverton

John A McCauley

Cristina Gardelli

Michael T Rudd

Jesus Maria Ontoria Ontoria

Emanuela Nizi

Simona Ponzi

Maria Emilia Di Francesco

Marco Ferrara

Alessia Petrocchi

Frank Narjes

Uwe Koch

Marco Poma

Paola Pace

Victor Giulio Matassa

Savina Malancona

Barbara Pacini

Joseph J Romano

Ian Stansfield

Federica Ferrigno

Malcolm MacCoss

Samuel Chackalamannil

Yongxin Han

Srikanth Venkatraman

Daniel Elbaum

David Brian Olsen

Michael Rowley

John W Butcher

Francisco Velazquez

M Katharine Holloway

Monica Donghi

Unmesh G Shah

Charles J McIntyre

Ester Muraglia

Benoit Bachand

Kevin F Gilbert

Edith Monteagudo

Alberto Bresciani

Ilaria Biancofiore

Ester Murgalia

Ralph Laufer

Sergio Altamura

Giacomo Paonessa

Roberto Gambari

Helmi Zaghdane

Benedetta Crescenzi

Stefania Colarusso

Virender Singh Aulakh

Patrick Beaulieu

Claudio Giuliano

Malte Meppen

Marco Pompei

Vicenzo Summa

Benjamin Gerlach

Maria Beconi

Marcello Di Filippo

Danilo Fabbrini

Sylvie Charron

Giulia Breveglieri

Marie-Christine Brochu

Christiane Grisé-Bard

Maria Veneziano

Alina Ciammaichella

Maria Vittoria Orsale

Johh A Mccauley

John A Mccauley

Charles A Mcintyre

Charles J Mcintyre

John Mccauley

The present invention relates to a class of novel heterocyclic compounds, to pharmaceutical compositions containing the compounds and their use in the treatment of kinetoplastid infections.

Compounds for use in the treatment of kinetoplastid infection

Compounds having the following formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, D, E and Rare as defined herein, are provided. Methods comprising the use of such compounds for the treatment of neurological disorders, such as pantothenate kinase-associated neurodegeneration, and pharmaceutical compositions containing such compounds, and their use in the treatment of neurological disorders, also are provided. 

Cyclic phosphates and cyclic phosphoramidates for the treatment of neurologic disorders

The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections. 

HCV NS3 protease inhibitors

The present invention relates to compounds of formula (I) and (IV), and pharmaceutically acceptable salts, tautomers, stereoisomers thereof, which are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are for use in the treatment of disorders that are ameliorated by inhibition of HDAC such as cancer and hemoglobinopathies like &#x3b2;-thalassemia or sickle cell anemia. 

Compounds for use in the treatment of disorders that are ameliorated by inhibition of HDAC

The present invention relates to compounds useful for treating parasitic diseases, which are infectious diseases caused or transmitted by a parasite. Compounds of the invention are particularly active against the causative pathogens in malaria. Such compounds are selective inhibitors of parasitic histone deacetylase (PfHDAC) and suppress the growth of parasites, such as, at a lower concentration than the concentration required for the inhibition of the growth of mammalian cells.

Compounds for use in the treatment of parasitic diseases

A class of macrocyclic compounds of formula (I), wherein R, R, R, R, R, A, Z, Y, X, M, W, n and m are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also provided are processes 5 for the synthesis and use of such macrocyclic compounds for treating or preventing HCV infection. Formula (I): 

Macrocyclic compounds as antiviral agents

A class of macrocyclic compounds of formula (I), wherein R, R, R, R, R, A, B, Z, M, W and n are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also provided are processes for the synthesis and use of such macrocyclic compounds for treating or preventing HCV infection. 

Therapeutic compounds

The present invention relates to macrocyclic compounds of formula (I): wherein W, n, m, R, R, R, R, R, R, M, Z and ring B are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus. 

The present invention relates to macrocyclic a compound of formula (I) and its use as inhibitors of the hepatitis C virus (HCV) NS3 protease, and in treating or preventing HCV infections. 

Macrocyclic quinoxaline compounds as HCV NS3 protease inhibitors

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. 

Nucleoside aryl phosphoramidates for the treatment of RNA-dependent RNA viral infection

4,5-Dihydroxypyrimidine-6-carboxamides of formula:  are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R, R, Rand Rare defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

Dihydroxypyrimidine carboxamide inhibitors of HIV integrase

4,5-Dihydroxypyrimidine-6-carboxamides of formula (I); are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R, R, Rand Rare defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described 

Compounds of formula (I), and pharmaceutically acceptable salts and esters thereof: (I); wherein Q, R2, X, Y and Z are as defined herein; are inhibitors of the hepatitis C virus (HCV) NS3 protease 

Peptides and their use as inhibitors of hepatitis C virus ns3 protease

Growing community of inventors

Rome, Italy

Steven Harper