Janssen Pharmaceutica Nv

Tibotec Pharmaceuticals Ltd.

Frank Xavier Jozef Herwig Arts, Legal Representative

Jan Heeres

Paul Adriaan Jan Janssen

Lucien Maria Henricus Koymans

Paulus Joannes Lewi

Marc René De Jonge

Frederik Frans Desiré Daeyaert

Hendrik Maarten Vinkers

Koen Jeanne Alfons Van Aken

Jérôme Emile Georges Guillemont

Donald William Ludovici

Koenraad Jozef Lodewijk Marcel Andries

Michael Joseph Kukla

Chih Yung Ho

Jerôme Emile Georges Guillemont

Robert William Kavash

Bart L De Corte

Amuri Kilonda

Ruben Gerardus George Leenders

Mikaël Paugam

Georges Joseph Cornelius Hoornaert

Bruno Francois Marie Delest

Patrice Palandijian

Dirk Alfons Leo Vandenput

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

The present invention relates to the use of a compound of formula (I) for the manufacture of a medicament for the prevention or the treatment of HIV infection wherein the compound of formula (I) is a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein A and B each represents a radical of formula and wherein &#x2014;C-D- represents a bivalent radical of formula&#x2014;N&#x2550;CH&#x2014;NR&#x2014;&#x2003;&#x2003;(c-1); or&#x2014;NR&#x2014;CH&#x2550;N&#x2014;&#x2003;&#x2003;(c-2);provided that when A represents a radical of formula (a) then B represents a radical of formula (b) and when A represents a radical of formula (b) then B represents a radical of formula (a).

HIV replication inhibiting purine derivatives

This invention concerns the use of compounds of formula the N-oxides, pharmaceutically acceptable addition salts, quaternary amines, stereochemically isomeric forms thereof, wherein -a=a-a=a- forms phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl with the attached vinyl group; n is 0 to 5; Ris hydrogen, aryl, formyl, Calkylcarbonyl, Calkyl, Calkyloxycarbonyl, substituted Calkyl, substituted CalkyloxyCalkylcarbonyl; Ris hydroxy, halo, optionally substituted Calkyl, Calkenyl or Calkynyl, Ccycloalkyl, 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)R, 5-membered heterocyclic ring; L is optionally substituted Calkyl, Calkenyl, Calkynyl or Ccycloalkyl; or &#x2014;X&#x2014;R; Q is hydrogen, Calkyl, halo, polyhalo-Calkyl, 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, 13 NHC(&#x2550;O)R,&#x2014;C(&#x2550;NH)R, aryl; for the treatment of subjects suffering from HIV infection.

HIV replication inhibiting pyrimidines

The present invention relates to HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein ring A and ring B represent phenyl, pyridyl, pyridazinyl, pyrimidinyl or pyrazinyl; n and m are 1 to 4; Rrepresents hydrogen; aryl; formyl; Calkylcarbonyl; Calkyloxycarbonyl; optionally substituted Calkyl; CalkyloxyCalkylcarbonyl substituted with Calkyloxycarbonyl; Ror Rrepresents hydrogen; hydroxy; halo; optionally substituted Calkyl; optionally substituted Calkenyl; optionally substituted Calkynyl; Ccycloalkyl; Calkyloxy; Calkyloxycarbonyl; Calkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(Calkyl)amino; polyhaloCalkyl; polyhaloCalkyloxy; polyhaloCalkylthio; &#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; NHC(&#x2550;O)R; C(&#x2550;NH)R; or R; Ror Rrepresents cyano; aminocarbonyl; amino; halo; 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; optionally substituted Calkyl; optionally substituted Calkyloxy; optionally substituted CalkyloxyCalkyl; optionally substituted Calkenyl; optionally substituted Calkynyl; &#x2014;C(&#x2550;N&#x2014;O&#x2014;R)&#x2014;Calkyl; Ror &#x2014;X&#x2014;R; Xor Xrepresents &#x2014;NR&#x2014;; &#x2014;NH&#x2014;NH&#x2014;; &#x2014;N&#x2550;N&#x2014;; &#x2014;O&#x2014;; &#x2014;C(&#x2550;O)&#x2014;; &#x2014;Calkanediyl-; &#x2014;CHOH&#x2014;; &#x2014;S&#x2014;; &#x2014;S(&#x2550;O)&#x2014;; &#x2014;X&#x2014;Calkanediyl-; &#x2014;Calkanediyl-X&#x2014;; or &#x2014;Calkanediyl-X&#x2014;Calkanediyl-; their use as a medicine, their use for the manufacture of a medicament for the treatment or the prevention of HIV infection; their processes for preparation and pharmaceutical compositions comprising them.

HIV inhibiting 1,2,4-triazin-6-one derivatives

Growing community of inventors

Brasschaat, Belgium

Frank Xavier Jozef Herwig Arts, Legal Representative