Merck Frosst Canada, Inc.

Boehringer Ingelheim (canada) Ltd.

Boehringer Ingelheim International Gmbh

Bio-mega/boehringer Ingelheim Research Inc.

Gilead Sciences, Inc.

Biomega, Inc.

Merck + Co., Inc.

Boehringer Ingelheim Gmbh

Boehringer Ingelheim Pharma Gmbh & Co Kg

Boehringer Ingelheim International Gmbh & Co., Kg

Christiane Yoakim

Paul Cates Anderson

Yvan Guindon

William W. Ogilvie

Robert Deziel

Jeffrey O'Meara

Rejean Fortin

Bruno Simoneau

Joshua Rokach

William W Ogilvie

Yves Girard

Cheuk K Lau

John W Gillard

Peter White

Howard E Morton

Bounkham Thavonekham

Sebastien Morin

Patrick Deroy

Nathalie Goudreau

Anne-Marie Faucher

Serge R Landry

Paul C Anderson

Alexandre Gagnon

Pierre Louis Beaulieu

Stephen Kawai

Robert D&eacute;ziel

Eric Malenfant

Francedillaois Soucy

Youla S Tsantrizos

Murray D Bailey

Patrice C Belanger

Martin Duplessis

Lee Fader

Carl Thibeault

Simon Surprenant

Rebekah J Carson

Francois Bilodeau

Robert Déziel

Steven R Laplante

Teddy Halmos

Dale R Cameron

Clint A James

Claudio F Sturino

Paul John Edwards

Sylvie Goulet

Pierre Lavallee

Julie Naud

Catherine Chabot

Oliver Hucke

Jean-Eric Lacoste

Martin Tremblay

Louis Morency

Yong Wang

Jacques Archambault

Pierre Lavall Ee

Simon Suprenant

Joannie Minville

Pierre Bonneau

Vida Gorys

Thomas R Jones

Christopher Lemke

Bruno Hache

Bruno Hach&eacute;

Jeffrey O′Meara

Steven LaPlante

Claudio Sturino

Paul J Edwards

Jeffrey O'MEARA

Compounds of formula I: wherein a, R, R, R, R, Rand Rare defined herein, are useful as inhibitors of HIV replication.

Inhibitors of human immunodeficiency virus replication

Compounds of formula (I): wherein R, R, A, A, A, A, X and Y are as defined herein, are useful as inhibitors of HIV replication.

Inhibitors of HIV replication

Compounds of formula (I): wherein Ar, X, R, R, Rand Rare as defined herein. The compounds are useful as reverse transcriptase inhibitors against wild type and single or double mutant strains of HIV.

Non-nucleoside reverse transcriptase inhibitors

The present invention relates to compounds of formula (I) wherein R, R, Rand Rare as defined herein, compositions and uses thereof for treating human immunodeficiency virus (HIV) infection. In particular, the present invention provides novel inhibitors of HIV replication, pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HIV infection. 

A compound of formula (I) or its enantiomers or diastereoisomers thereof: wherein: A,; X, W, R, Y; R; and Rare as defined herein. The compounds of the invention may be used as inhibitors of the papilloma virus E1-E2-DNA complex. The invention further provides a method of treating or preventing human papilloma virus infection.

Inhibitors of papilloma virus

Disclosed herein are compounds of formula Ar&#x2014;X&#x2014;W&#x2014;Arwherein Arand Arrepresent aryl groups characterized generally as aromatic heterocycles (e.g. imidazolyl or tetrazolyl) or carbocycles (e.g. phenyl or naphthalenyl); the aryl groups are optionally substituted or fused with other heterocycles or carbocycles; the aryl groups can bear substituents such as alkyl, halo or O-alkyl. X is a heteroatom, a valence bond or an optionally substituted divalent methylene, and W represents a spacer; typical spacers include divalent alkylene or alkylene-amido, -amido or -oxy radicals, which may optionally be substituted (e.g. hydroxyl or oxo). A typical compound is a derivative of 2-(N-napthalenyltetrazolylthio)-N-(2-nitrophenyl)acetamide. The compounds have inhibitory activity against Wild Type and single or double mutant strains of HIV.

Compounds of formula (I): wherein R, R, R, R, Rand Rare as defined herein. The compounds are useful as reverse transcriptase inhibitors against HIV. In particular, the compounds are active against wild type and single or double mutant strains of HIV.

Benzoic acid derivatives as non nucleoside reverse-transcriptase inhibitors

A compound of formula (I) or its enantiomers or diastereoisomers thereof: wherein: A, X, W, R, Y; R; and Rare as defined herein. The compounds of the invention may be used as inhibitors of the papilloma virus E1-E2-DNA complex. The invention further provides a method of treating or preventing human papilloma virus infection.

Non nucleoside reverse transcriptase inhibitors

Inhibitors of HIV reverse transcriptase which are useful for the treatment of HIV infection. Exemplars of the invention are compounds of the formula wherein the substituents are as defined in the following table 

Alkynyl compounds as non nucleoside reverse transcriptase inhibitors

Compounds represented by formula 1: wherein Ris H, halogen, (C)alkyl, O(C)alkyl, and haloalkyl; Ris H or methyl; Ris H or (C)alkyl; Ris H or (C)alkyl; Ris (C)alkyl, (C)alkyl(C)cyclo-alkyl or (C)cycloalkyl; and W is a fused phenyl-5 or 6-membered heterocycle having one or two heteroatoms selected from N or S; or W is phenyl, 1,1'-biphenyl, 2,3-dihydro-1H-indene, 1,2,3,4-tetrahydronaphthyl, or naphthyl; said W being optionally substituted with (C)alkyl, which in turn can be optionally substituted with a carboxy or (C)alkoxycarbonyl, or a salt or ester thereof. The compounds have inhibitory activity against Wild Type, single and double mutant strains of HIV.

A crystallizable composition, comprising an human papillomavirus (HPV-11) E2 transactivation domain (TAD)-like polypeptide of SEQ ID NO. 2 complexed with an inhibitor L (sodium (2R,3R,4S,5R)-5-(3,4-dichlorophenyl)-5'-methyl-1&#x2032;,3&#x2032;-dioxo-4-({[4-(1,2,3-thiadiazol-4-yl)phenyl]amino}carbonyl)-1&#x2032;,3&#x2032;,4,5-tetrahydro-3H-spiro[furan-2,2&#x2032;-indene]-3-carboxylate). The invention also provides a method for producing the crystallized HPV E2 TAD-inhibitor complex (HPV E2 TAD-L) comprising: a) mixing purified HPV E2 TAD, contained in a purification buffer, with solublized inhibitor L to generate a complex solution containing the HPV E2 TAD-L complex; and b) crystallizing the complex from a) in a crystallization buffer. The invention also provides a method for producing crystallized apo HPV E2 TAD, comprising: a) mixing apo HPV E2 TAD, contained in a purification buffer, with a crystallization buffer. X-ray crystal structure coordinates the HPV E2 TAD-L complex, are also provided, which define an inhibitor binding pocket. The inhibitor binding pocket is useful for screening potential small molecule inhibitors that bind to the pocket that may be inhibitors of papillomavirus infection.

Method of identifying potential inhibitors of human papillomavirus protein E2 using x-ray atomic coordinates

Compounds represented by formula I: wherein Ris H, halogen, (C)alkyl, O(C)alkyl, and haloalkyl; Ris H or (C)alkyl; Ris H or (C)alkyl; Ris (C)alkyl, (C)alkyl(C)cycloalkyl, or (C)cycloalkyl; and Q is a fused phenyl-5 or 6-membered saturated heterocycle having one to two heteroatoms selected from O and N, said Q being optionally substituted with hydroxy, or (C)alkyl which in turn maybe optionally substituted with pyridinyl-N-oxide or C(O)OR wherein R is H or (C)alkyl; or a salt thereof. The compounds have inhibitory activity against Wild Type, and single and double mutants strains, of HIV.

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Laval, Canada

Christiane Yoakim