Janssen Pharmaceutica Nv

Other

Tibotec Pharmaceuticals Ltd.

Janssen Pharmaceutica

Tibotec Bvba

Marc René De Jonge

Lucien Maria Henricus Koymans

Jan Heeres

Paul Adriaan Jan Janssen

Koen Jeanne Alfons Van Aken

Paulus Joannes Lewi

Frederik Frans Desiré Daeyaert

Hendrik Maarten Vinkers

Donald William Ludovici

Michael Joseph Kukla

Jérôme Emile Georges Guillemont

Robert William Kavash

Koenraad Jozef Lodewijk Marcel Andries

Bart L De Corte

Patrice Palandjian

Chih Yung Ho

Frank Xavier Jozef Herwig Arts, Legal Representative

Amuri Kilonda

Ruben Gerardus George Leenders

Bart Lieven Daniel De Corte

Alain Krief

Eddy Jean Edgard Freyne

Werner Constant Johan Embrechts

Jerôme Emile Georges Guillemont

Marc Willems

Peter Jacobus Johannes Antonius Buijnsters

Kurt Hertogs

Georges Joseph Cornelius Hoornaert

Marcel August Constant Janssen

Eva Bettens

Elisabeth Thérese Jeanne Pasquier

Jean Fernand Armand Lacrampe

Gaston Stanislas Marcella Diels

Christopher John Love

Elisabeth Therese Jeanne Pasquier

Jean-Marc Edmond Fernand Marie Neefs

Frans Josef Cornelius Compernolle

Johann Winkler

Peter Karel Maria Verhasselt

Marc Hubert Mercken

Frank Xavier Josef Herwig Arts, Legal Representative

Rony Maria Nuydens

Hugo Alfons Gabriel Geerts

Theodora Joanna Francisca Arts

Maroussia Godelieve Frank Janssen, Legal Representative

Jasmine Josée Werner Janssen, Legal Representative

Paul Peter Maria Janssen, Legal Representative

Herwig Josephus Margareta Janssen, Legal Representative

Graziella Maria Constantina Janssen, Legal Representative

Jéròme Emile Georges Guillemont

Hinrich Wilhelm Helmut Göhlmann

Patrice Palandijian

Dirk Alfons Leo Vandenput

Frank Jozef Herwig Arts, Legal Representative

Georges Joseph Cornelius Hoomaert

Frank Xavier Jozef Herwig Arts

Frank Xavier Jozef Herwig, Legal Representative

Frans J C KULeuven Res&Dev Compernolle

Lucien Maria H Koymans

Frederik Frans D Janssen Pharm NV Daeyaert

Amuri KULeuven Research & Development Kilonda

Georges J C KULeuven Res & Dev Hoornaert

Lucien Maria H Janssen Pharm NV Koymans

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

Paul A J Janssen Pharmaceutica NV Janssen

KJLM Janssenpharmaceutica NV Andries

Peter KM Janssen Pharmaceutica NV Verhasselt

Johann Janssen Pharmaceutica NV Winkler

Hinrich WH Janssen Pharmaceutica NV GÖHLMANN

Lucien Maria Henricus Molmo Services Bvba Koymans

J-MEFM Janssen Pharmaceutica NV Neefs

Paul Adriaan Jan Janssen Pharm NV Janssen

Donald W Janssen Pharmaceutica Inc Ludovici

Koen J A Janssen Pharmaceutica NV Van Aken

Alain Université Notre-Dame De La Paix Krief

Lucien M H Janssen Pharmaceutica NV Koymans

Jan Janssen Pharmaceutica NV Heeres

Robert W Janssen Pharmaceutica Inc Kavash

Bart L D Janssen Pharmaceutical Inc De Corte

Paulus Joannes Janssen Pharmaceutica NV Lewi

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

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.

This invention provides an isolated mutant atpE protein and departing from said mutant atpE protein the identification of an ATPase binding domain. This invention also provides related nucleic acids, vectors, host cells, pharmaceutical compositions and articles of manufacture. This invention further provides methods for determining whether a test compound interacts with an atpE protein, i.e. with the ATPase binding domain of the present invention, as well as pharmaceuticals compositions comprising said test compound, in particular as antimicrobials, more particular as antimycobacterial agent, even more particular for treating tuberculosis in a subject.

Bacterial ATP synthase binding domain

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

This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CRor N; n is 0 to 4; Q is hydrogen or &#x2014;NRR; Rand Rare selected from hydrogen, hydroxy, Calkyl, Calkyloxy, Calkylcarbonyl, Calkyloxycarbonyl, aryl, amino, mono- or di(Calkyl)-amino, mono- or di(Calkyl)aminocarbonyl wherein each Calkyl may optionally be substituted; or Rand Rtaken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(Calkyl)aminoCalkylidene; Ris hydrogen, aryl, Calkylcarbonyl, optionally substituted Calkyl, Calkyloxy-carbonyl; and Ris hydroxy, halo, optionally substituted Calkyl, Calkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; Ris hydrogen or Calkyl; L is optionally substituted Calkyl, Calkenyl, Calkynyl, Ccycloalkyl; or L is &#x2014;X&#x2014;Ror &#x2014;X-Alk-Rwherein Rand Rare optionally substituted phenyl; Xand Xare &#x2014;NR&#x2014;, &#x2014;NH&#x2014;NH&#x2014;, &#x2014;N&#x2550;N&#x2014;, &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;S(&#x2550;O)&#x2014; or &#x2014;S(&#x2550;O)&#x2014;; Alk is Calkanediyl; aryl is optionally substituted phenyl; Het is an optionally substituted aliphatic or aromatic heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and compositions comprising them.

HIV inhibiting pyrimidine 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.

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 concerns compounds of formula (A)(A)N&#x2014;R(I), the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein Ris substituted Calkyl; &#x2014;S(&#x2550;O)&#x2014;R; &#x2014;S(&#x2550;O)&#x2014;R; Calkylcarbonyl; optionally substituted CalkyloxycarbonylCalkylcarbonyl; with Rbeing Calkyl, arylor Het; (A)(A)N&#x2014; is the covalently bonded form of the corresponding intermediate of formula (A)(A)N&#x2014;H, which is a HIV replication inhibiting pyrimidine of formula 

Prodrugs of HIV replication inhibiting pyrimidines

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

Growing community of inventors

Tilburg, Netherlands

Marc René De Jonge