Janssen Pharmaceutica Nv

Other

Janssen Sciences Ireland Uc

Tibotec Pharmaceuticals Ltd.

Janssen Pharmaceutica

Universiteit Antwerpen

Janssen Sciences Ireland Unlimited Company

Janssen R&d Ireland

Tibotec Bvba

Janssen Pharmacuetica N.v.

Shakturana Cv

Janssen-cilag S.a.

Lucien Maria Henricus Koymans

Hendrik Maarten Vinkers

Koen Jeanne Alfons Van Aken

Jan Heeres

Paul Adriaan Jan Janssen

Leo J Backx

Paulus Joannes Lewi

Marc René De Jonge

Joseph H Mostmans

Donald William Ludovici

Michael Joseph Kukla

Frederik Frans Desiré Daeyaert

Bart L De Corte

Robert William Kavash

Raymond A Stokbroekx

Chih Yung Ho

Jerôme Emile Georges Guillemont

Jérôme Emile Georges Guillemont

Robert Jozef Hendrickx

Lieven Meerpoel

Koenraad Jozef Lodewijk Marcel Andries

Ruben Gerardus George Leenders

Louis J Van Der Veken

Marc Willems

Mikaël Paugam

Patrice Palandjian

Bruno Francois Marie Delest

Marc Ren&eacute; De Jonge

Frank Xavier Jozef Herwig Arts, Legal Representative

Elisabeth Therese Jeanne Pasquier

Frank Christopher Odds

Marcel August Constant Janssen

Luc Alfons Van Der Eycken

Paul A J Janssen

Henri E L Moereels

Marcel J Van Der Aa

Paul A Janssen

Jean Louis Mesens

Amuri Kilonda

Didier Robert De Chaffoy De Courcelles

Bart Lieven Daniel De Corte

Didier Philippe Robert Schils

Robert Jozef Maria Hendrickx

Bart Petrus Anna Maria Jozef Medaer

Marc Rene De Jonge

Joannes Josephus Maria Willems

Alain Krief

Adolf Hubele

Eddy Jean Edgard Freyne

Elmar Sturm

Werner Constant Johan Embrechts

Leo Jacobus Jozef Backx

Peter Jacobus Johannes Antonius Buijnsters

Hubert K Hermans

Kurt Hertogs

Jozef Peeters

Willy Joannes Van Laerhoven

Georges Joseph Cornelius Hoornaert

Lourens Wals

Gustaaf Van Reet

Eva Bettens

Frederik Frans Desir&eacute; Daeyaert

Louis Jozef Elisabeth Van Der Veken

Elisabeth Thérese Jeanne Pasquier

Jerome Emile Georges Guillemont

Robert Nyfeler

Jean Fernand Armand Lacrampe

Gaston Stanislas Marcella Diels

Lieven Elvire Colette Baert

Christopher John Love

Pieter Van Der Veken

Koen Augustyns

Jurgen Joossens

Jean P Van Wauwe

Frans Josef Cornelius Compernolle

Alfonsus G Knaeps

Robert Franciscus Van Ginckel

Bruno François Marie Delest

Paul Peter Maria Janssen, Legal Representative

Graziella Maria Constantina Janssen, Legal Representative

Jasmine Josée Werner Janssen, Legal Representative

Maroussia Godelieve Frank Janssen, Legal Representative

Theodora Joanna Francisca Arts

Hugo Alfons Gabriel Geerts

Rony Maria Nuydens

Jéròme Emile Georges Guillemont

Marc Hubert Mercken

Frank Xavier Josef Herwig Arts, Legal Representative

Mark Arthur Josepha Van Der Flaas

Hugo Florent Adolf Vanden Bossche

Paul August Clement Luyts

Frederik Frans Daeyaert

Lucien Maria Koymans

Venkatraj Muthusamy

Kevin Karel Florentina Arien

Patrice Palandijian

Johan R Beetens

Guido Louis Emile Vanham

Dirk Alfons Leo Vandenput

This invention relates to the use of a parenteral formulation comprising the NNRTI TMC278 for the long term prevention of HIV infection in a subject at risk of being infected by HIV, which comprises the intermittent administration of the said formulation at long time intervals.

Prevention of HIV-infection

This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a=a-a=a- and -b=b-b=b- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; Ris hydrogen; aryl; formyl; Calkylcarbonyl; Calkyl; Calkyloxycarbonyl; substituted Calkyl, Calkylcarbonyl, Calkyloxycarbonyl, Calkylcarbonyloxy; substituted CalkyloxyCalkylcarbonyl; Ris hydroxy, halo, optionally substituted Calkyl, Ccycloalkyl, optionally substituted Calkenyl, optionally substituted Calkynyl, Calkyloxy, Calkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(Calkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, &#x2014;S(&#x2550;O)R, &#x2014;NH&#x2014;S(&#x2550;O)R, &#x2014;C(&#x2550;O)R, &#x2014;NHC(&#x2550;O)H, &#x2014;C(&#x2550;O)NHNH, &#x2014;NHC(&#x2550;O)R, &#x2014;C(&#x2550;NH)Ror a 5-membered heterocycle; Xis &#x2014;NR&#x2014;, &#x2014;NH&#x2014;NH&#x2014;, &#x2014;N&#x2550;N&#x2014;, &#x2014;O&#x2014;, &#x2014;C(&#x2550;O)&#x2014;, Calkanediyl, &#x2014;CHOH&#x2014;, &#x2014;S&#x2014;, &#x2014;S(&#x2550;O)&#x2014;, &#x2014;X&#x2014;Calkanediyl- or &#x2014;Calkanediyl-X&#x2014;; Ris NHR; NRR; &#x2014;C(&#x2550;O)&#x2014;NHR; &#x2014;C(&#x2550;O)&#x2014;NRR; &#x2014;C(&#x2550;O)&#x2014;R; &#x2014;CH&#x2550;N&#x2014;NH&#x2014;C(&#x2550;O)&#x2014;R; substituted Calkyl; optionally substituted CalkyloxyCalkyl; substituted Calkenyl; substituted Calkynyl; Calkyl substituted with hydroxy and a second substituent; &#x2014;C(&#x2550;N&#x2014;O&#x2014;R)&#x2014;Calkyl; R; or &#x2014;X&#x2014;R; Ris halo, hydroxy, Calkyl, Ccycloalkyl, Calkyloxy, cyano, nitro, polyhaloCalkyl, polyhaloCalkyloxy, aminocarbonyl, Calkyloxycarbonyl, Calkylcarbonyl, formyl, amino, mono- or di(Calkyl)amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

HIV replication inhibiting pyrimidines

HIV replication inhibitors of formula wherein

HIV inhibiting bicyclic pyrimidine derivatives

HIV replication inhibitors of formula N-oxides, pharmaceutically acceptable addition salts, quaternary amines or stereoisomeric forms thereof, wherein

The present invention relates to the field of HIV-1 infections, and in particular provides novel compounds containing triazine rings and suitable spacers. The compounds according to this invention are very suitable for the prevention and/or treatment of HIV-1 infection and in particular show improved activity against NNRTI-resistant viruses of HIV-1.

Triazines with suitable spacers for treatment and/or prevention of HIV infections

HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein

HIV inhibiting 5-substituted pyrimidines

This invention concerns the use of a compound for the manufacture of a medicament for the prevention of HIV infection via sexual intercourse and related intimate contact between partners, wherein the compound is a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein the ring containing -a=a-a=a- and -b=b-b=b- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; Ris hydrogen; aryl; formyl; Calkylcarbonyl; Calkyl; Calkyloxycarbonyl; substituted Calkyl, Calkylcarbonyl, Calkyloxycarbonyl, Calkylcarbonyloxy; substituted CalkyloxyCalkylcarbonyl; Ris hydroxy, halo, optionally substituted Calkyl, Ccycloalkyl, optionally substituted Calkenyl, optionally substituted Calkynyl, Calkyloxy, Calkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(Calkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, &#x2014;S(&#x2550;O)R, &#x2014;NH&#x2014;S(&#x2550;O)R, &#x2014;C(&#x2550;O)R, &#x2014;NHC(&#x2550;O)H, &#x2014;C(&#x2550;O)NHNH, &#x2014;NHC(&#x2550;O)R, &#x2014;C(&#x2550;NH)Ror a 5-membered heterocycle; Xis &#x2014;NR&#x2014;, &#x2014;NH&#x2014;NH&#x2014;, &#x2014;N&#x2550;N&#x2014;, &#x2014;O&#x2014;, &#x2014;C(&#x2550;O)&#x2014;, Calkanediyl, &#x2014;CHOH&#x2014;, &#x2014;S&#x2014;, &#x2014;S(&#x2550;O)&#x2014;, &#x2014;X&#x2014;Calkanediyl- or &#x2014;Calkanediyl-X&#x2014;; Ris NHR; NRR; &#x2014;C(&#x2550;O)&#x2014;NHR; &#x2014;C(&#x2550;O)&#x2014;NRR; &#x2014;C(&#x2550;O)&#x2014;R; &#x2014;CH&#x2550;N&#x2014;NH&#x2014;C(&#x2550;O)&#x2014;R; substituted Calkyl; optionally substituted CalkyloxyCalkyl; substituted Calkenyl; substituted Calkynyl; Calkyl substituted with hydroxy and a second substituent; &#x2014;C(&#x2550;N&#x2014;O&#x2014;R)&#x2014;Calkyl; R; or &#x2014;X&#x2014;R; Ris halo, hydroxy, Calkyl, Ccycloalkyl, Calkyloxy, cyano, nitro, polyhaloCalkyl, polyhaloCalkyloxy, aminocarbonyl, Calkyloxycarbonyl, Calkylcarbonyl, formyl, amino, mono- or di(Calkyl)amino; and pharmaceutical compositions comprising them.

Pyrimidine derivatives for the prevention of HIV infection

Compounds of formula (I), N-oxides, pharmaceutical acceptable salts, quaternary amines or stereoisomeric forms thereof, and their use as HIV replication inhibitors, In the formula, -a=a-a=a- and -b=b-b=b- may be &#x2014;C&#x2550;C&#x2014;C&#x2550;C&#x2014;; X1 may be O, NR1, etc.;R, R, R, R, Rand Rare assorted substituents as defined in the specification.

HIV inhibiting 5-heterocyclyl pyrimidines

This invention concerns the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a=a-a=a- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; Ris hydrogen, aryl, formyl, Calkylcarbonyl, Calkyl, Calkyloxycarbonyl, substituted Calkyl, or substituted CalkyloxyCalkylcarbonyl; each Rindependently is hydroxy, halo, optionally substituted Calkyl, Calkenyl or Calkynyl, Ccycloalkyl, Calkyloxy, Calkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(Calkylamino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, &#x2014;S(&#x2550;O)R, &#x2014;NH&#x2014;S(&#x2550;O)R, &#x2014;C(&#x2550;O)R, &#x2014;NHC(&#x2550;O)H, &#x2014;C(&#x2550;O)NHNH, &#x2014;NHC(&#x2550;O)R, &#x2014;C(&#x2550;NH)Ror a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted Calkyl, Calkenyl, Calkynyl or Ccycloalkyl; or L is &#x2014;X&#x2014;Rwherein Ris optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is &#x2014;NR&#x2014;, &#x2014;NH&#x2014;NH&#x2014;, &#x2014;N&#x2550;N&#x2014;, &#x2014;O&#x2014;, &#x2014;C(&#x2550;O)&#x2014;, &#x2014;CHOH&#x2014;, &#x2014;S&#x2014;, &#x2014;S(&#x2550;O)&#x2014; or &#x2014;S(&#x2550;O)&#x2014;; Q is hydrogen, Calkyl, halo, polyhalo-Calkyl or an optionally substituted amino group; Y represents hydroxy, halo, Ccycloalkyl, optionally substituted Calkyl, Calkenyl or Calkynyl, Calkyloxy, Calkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(Calkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, &#x2014;S(&#x2550;O)R, &#x2014;NH&#x2014;S(&#x2550;O)R, &#x2014;C(&#x2550;O)R, &#x2014;NHC(&#x2550;O)H, &#x2014;C(&#x2550;O)NHNH, &#x2014;NHC(&#x2550;O)R, &#x2014;C(&#x2550;NH)Ror aryl; aryl is optionally substituted phenyl; Het is an optionally substituted heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.

HIV inhibiting bicyclic pyrimdine derivatives

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Vosselaar, Belgium

Jan Heeres