Janssen Pharmaceutica Nv

Tibotec Pharmaceuticals Ltd.

Tibotec Bvba

Janssen-Cilag S.a.

Jan Heeres

Jerome Emile Georges Guillemont

Paul Adriaan Jan Janssen

Patrice Palandjian

Marc Rene De Jonge

Frederik Frans Desire Daeyaert

Paulus Joannes Lewi

Koen Jeanne Alfons Van Aken

Hendrik Maarten Vinkers

Lucien Maria Henricus Koymans

Marc René De Jonge

Frederik Frans Desiré Daeyaert

Jérôme Emile Georges Guillemont

Frederik Frans Daeyaert

Lucien Maria Koymans

Paul Adriaan Janssen

Frank Xavier Jozef Herwig Arts, Legal Representative

Jerome Emile Guillemont

Elisabeth Therese Pasquier

Jerôme Emile Georges Guillemont

Amuri Kilonda

Kurt Hertogs

Ruben Gerardus George Leenders

Eva Bettens

Elisabeth Thérese Jeanne Pasquier

Ruben Gerardus Leenders

Georges Joseph Hoornaert

Eddy Jean Edgard Freyne

Donald William Ludovici

Werner Constant Johan Embrechts

Marc Willems

Gaston Stanislas Marcella Diels

Christopher John Love

Peter Jacobus Johannes Antonius Buijnsters

Elisabeth Therese Jeanne Pasquier

Georges Joseph Cornelius Hoornaert

Frank Xavier Jozef Herwig Arts

Frank Xavier Jozef Herwig, Legal Representative

Frank Xavier Josef Herwig Arts, Legal Representative

Jéròme Emile Georges Guillemont

Patrice Palandijian

Dirk Alfons Leo Vandenput

Frank Jozef Herwig Arts, Legal Representative

Georges Joseph Cornelius Hoomaert

Paul Adrian Janssen

Dirk Alfons Vandenput

Patrice Palandijan

Frederik F D Daeyaert

Georges J C Hoornaert

Lucien Maria H Koymans

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

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

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

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

The present invention relates to HIV replication inhibitors of formula (I) as defined in the specification their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them. 

HIV inhibiting 1,2,4-triazines

This invention concerns HIV replication inhibitors of formula (I), the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

HIV replication inhibiting pyrimidines and triazines

This invention concerns a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A is a 6-membered heterocycle; Ris hydrogen; aryl; formyl; Calkylcarbonyl; optionally substituted Calkyl; Calkyloxycarbonyl; optionally substituted CalkyloxyCalkylcarbonyl; X is a direct bond or a linker atom or group; Z is a direct bond or a linker atom or group; Ris hydrogen, Calkyl, Calkenyl, Calkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; Ris hydrogen; hydroxy; halo; optionally substituted Calkyl or Calkenyl or Calkynyl; Calkyloxy; Calkylthio; Calkyloxycarbonyl; Calkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(Calkyl)amino; polyhaloCalkyl; polyhaloCalkyloxy; polyhaloCalkylthio; R; R&#x2014;Calkyl; R&#x2014;O&#x2014;; R&#x2014;S&#x2014;; R&#x2014;C(&#x2550;O)&#x2014;; R&#x2014;S(&#x2550;O)&#x2014;; R&#x2014;S(&#x2550;O)&#x2014;; R&#x2014;S(&#x2550;O)&#x2014;NH&#x2014;; R&#x2014;S(&#x2550;O)&#x2014;NH&#x2014;; R&#x2014;C(&#x2550;O)&#x2014;; &#x2014;NHC(&#x2550;O)H; &#x2014;C(&#x2550;O)NHNH; R&#x2014;C(&#x2550;O)&#x2014;NH&#x2014;; R&#x2014;C(&#x2550;O)&#x2014;NH&#x2014;; &#x2014;C(&#x2550;NH)R&#x2014;C(&#x2550;NH)R; Ris an optionally substituted heterocycle provided that &#x2014;X&#x2014;Rand/or Ris other than hydrogen; their use, pharmaceutical compositions comprising them and processes for their preparation.

Heteroaryl amines as glycogen synthase kinase 3&#x3b2;  inhibitors (GSK3 inhibitors)

This invention concerns HIV replication inhibitors of formula (I), The N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them. 

This invention concerns HIV replication inhibitors of formula (I) the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing &#x2212;a=a&#x2212;a=a&#x2014;and &#x2212;b=b&#x2212;b=brepresents pheynl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; Ris hydrogen; aryl; formyl; Calkylcarbonyl; Calkyl; Calkyloxycarbonyl, substituted Calkyl, Calkylcarbonyl; 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?2?, &#x2014;NHC(&#x2550;O)R, &#x2014;C(&#x2550;NH)Ror a 5-membered hetrocycl; 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; substituted Calkylenyl; 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 

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Antwerp, Belgium

Hendrik Maarten Vinkers