Merck Sharp + Dohme Corp.

Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa

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

Istituto Di Richerche Di Biologia Molecolare P. Angeletti S.p.a.

Merck Sharpe & Dohme Corp.

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

Merck & Dohme Limited

Michael Rowley

Paul D Leeson

Ian James Collins

Vincenzo Summa

Giovanna Pescatore

Benedetta Crescenzi

Ester Muraglia

Federica Orvieto

Rita Scarpelli

Christopher Richard Moyes

Cristina Gardelli

Jose Luis Castro Pineiro

William Robert Carling

Alessia Petrocchi

Marco Poma

Paola Pace

Emanuela Nizi

Timothy Harrison

Angus Murray MacLeod

Martin Richard Teall

Frank Narjes

Paul David Leeson

Olaf Kinzel

Janusz Jozef Kulagowski

Leslie Joseph Street

Raymond Baker

Monique Bodil Van Niel

Stephen Robert Fletcher

David James Hallett

Kevin William Moore

Alan John Nadin

Ian Stansfield

Howard Barff Broughton

Timothy Jason Sparey

Ian M Mawer

Caterina Ercolani

Barbara Attenni

Philip Jones

Andrew Pate Owens

Tamara Ladduwahetty

Marco Ferrara

Graham A Showell

Uwe Koch

Steven Harper

Simon Charles Goodacre

Adrian Leonard Smith

Jesus Maria Ontoria Ontoria

Joerg Habermann

Raffaele Ingenito

Graeme Irvine Stevenson

Stephen John Lewis

Federica Ferrigno

Robert James Maxey

Alexander Richard Guiblin

Simona Ponzi

Immacolata Conte

Savina Malancona

Laura Llauger Bufi

Monica Donghi

Jose Ignacio Martin Hernando

Marco Pompei

Karl Richard Gibson

James Michael Crawforth

Steven Michael Hutchins

Graeme I Sevenson

Paul David Lesson

Jesus Maria Ontoria

Carsten Schultz

William Barnaby Davey

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. 

Macrocyclic compounds as antiviral agents

Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds of Formula A: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein n is an integer equal to zero, 1, 2 or 3, and R, R, R, R, R, R, 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.

Tetrahydro-4H-pyrido[1,2-a] pyrimidines useful as HIV integrase inhibitors

The present invention relates to compounds of formula I: or pharmaceutically acceptable salts or tautomers thereof, which are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.

Heterocycle derivatives as histone deacetylase (HDAC) inhibitors

N-substituted 5-hydroxypyrimidin-6-one-4-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.

N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase

The present invention relates to tetracyclic indole compounds of formula (I): wherein R, R, A, Ar, W, X, Y and Z 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.

Tetracyclic indole derivatives as antiviral agents

The present invention relates to thienopyrrole compounds of formula (I); wherein A, B, Y, Ar, n, Z and Xare as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections. 

Thienopyrroles as antiviral agents

The present invention relates to tetracyclic indole compounds of formula (I); wherein R, R, R, R, A, Ar, Y and Z 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. 

Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds of Formula (A): are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein n is an integer equal to zero, 1, 2 or 3, and R, R, R, R, R, R, 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. 

Substituted pyrimido[1,2-a]azepines useful as HIV integrase inhibitors

N-substituted 5-hydroxypyrimidin-6-one-4-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.

N-substituted 5-hydroxypyrimidin-6-one-4-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 

A class of 3-phenylimidazo[1,2-a]pyridine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a &#x2014;NH-linkage, are selective ligands for GABAreceptors, in particular having high affinity for the &#x3b1;2 and/or &#x3b1;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.

Imidazo-pyridine derivatives as ligands for GABA receptors

The present invention is directed to 3-phenylimidazol&lsqb;4,5-b&rsqb;pyridine derivatives, that are selective ligands for GABA receptors. These compounds are useful in the treatment and prevention of disorders of the central nervous system, including anxiety and convulsions.

A class of substituted 1,2,4-triazolo&lsqb;4,3-&rsqb;pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position, a substituted alkoxy moiety at the 6-position, and an optionally substituted bicycloalkyl ring system at the 7-position, are selective ligands for GABA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.

Imidazo-triazine derivatives as ligands for GABA receptors

A class of tryptamine analogues bearing an optionally substituted phenyl nucleus at the 2-position are selective antagonists of the human 5-HT receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse neurological conditions, including psychotic disorders such as schizophrenia.

Phenylindole derivatives as 5-HT2A receptor ligands

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Axa, Italy

Michael Rowley