Janssen Pharmaceutica Nv

Janssen Sciences Ireland Uc

Tibotec Pharmaceuticals Ltd.

Other

Universiteit Antwerpen

Janssen Sciences Ireland Unlimited Company

Janssen R&d Ireland

Tibotec Bvba

Shakturana Cv

Janssen-Cilag S.a.

Lucien Maria Henricus Koymans

Hendrik Maarten Vinkers

Koen Jeanne Alfons Van Aken

Paulus Joannes Lewi

Frederik Frans Desire Daeyaert

Jan Heeres

Paul Adriaan Jan Janssen

Marc René De Jonge

Frederik Frans Desiré Daeyaert

Jerôme Emile Georges Guillemont

Jérôme Emile Georges Guillemont

Mikaël Paugam

Patrice Palandjian

Bruno Francois Marie Delest

Frank Xavier Jozef Herwig Arts, Legal Representative

Amuri Kilonda

Eddy Jean Edgard Freyne

Donald William Ludovici

Werner Constant Johan Embrechts

Marc Willems

Peter Jacobus Johannes Antonius Buijnsters

Kurt Hertogs

Ruben Gerardus George Leenders

Georges Joseph Cornelius Hoornaert

Marc Rene De Jonge

Eva Bettens

Elisabeth Thérese Jeanne Pasquier

Michael Joseph Kukla

Jean Fernand Armand Lacrampe

Gaston Stanislas Marcella Diels

Lieven Elvire Colette Baert

Christopher John Love

Elisabeth Therese Jeanne Pasquier

Pieter Van Der Veken

Koen Augustyns

Jurgen Joossens

Frans Josef Cornelius Compernolle

Bruno François Marie Delest

Frederik Frans Daeyaert

Lucien Maria Koymans

Jerome Emile Guillemont

Paul Adriaan Janssen

Elisabeth Therese Pasquier

Georges Joseph Hoornaert

Ruben Gerardus Leenders

Patrice Palandijian

Dirk Alfons Leo Vandenput

Kevin Karel Florentina Arien

Guido Louis Emile Vanham

Frank Jozef Herwig Arts, Legal Representative

Georges Joseph Cornelius Hoomaert

Frank Xavier Jozef Herwig Arts

Venkatraj Muthusamy

Frank Xavier Jozef Herwig, Legal Representative

Jerome Emile Georges Guillemont

Herwig Josephus Margareta Janssen, Legal Representative

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

Marc Hubert Mercken

Frank Xavier Josef Herwig Arts, Legal Representative

Jéròme Emile Georges Guillemont

Koen Jeanne Van Aken

Paul Adrian Janssen

Frans Josef Compernolle

Dirk Alfons Vandenput

Mikael Paugam

Bruno Francois Delest

Rudolf Leemans

Patrice Palandijan

Maroussia Godelieve Frank Janssen

Jasmin Josee Werner Janssen

Jean Fernand Armand Janssen-Cilag Lacrampe

Graziella Maria Constantina Janssen

Herwig Josephus Margareta Janssen

Paul Peter Maria Janssen

Donald William Janssen Pharmac Inc Ludovici

Frederik F D Daeyaert

Georges J C Hoornaert

Lucien Maria H Koymans

Luc Jozef Raphael Moens

Luc Jozef Moens

Lieven Elvire Baert

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

HIV inhibiting bicyclic pyrimdine derivatives

HIV replication inhibitors having formula (I) defined herein are disclosed. Pharmaceutical compositions containing the HIV replication inhibitors; the use of the HIV replication inhibitors in the treatment of HIV; and processes for preparing the HIV replication inhibitors are also disclosed.

HIV inhibiting pyrimidines derivatives

Growing community of inventors

Turnhout, Belgium

Paulus Joannes Lewi