Janssen Pharmaceutica Nv

Janssen Sciences Ireland Unlimited Company

Global Alliance for Tb Drug Development

Other

Janssen Pharmaceutica

Hanssen Pharmaceutica, N.v.

Janssen Pharmacatica, N.v.

Koenraad Jozef Lodewijk Marcel Andries

Jérôme Emile Georges Guillemont

Anil Koul

Frans E Janssens

Lucien Maria Henricus Koymans

Jean Fernand Armand Lacrampe

Jan Heeres

Donald William Ludovici

Paul Adriaan Jan Janssen

Michael Joseph Kukla

Chih Yung Ho

Koen Jeanne Alfons Van Aken

Bart L De Corte

François Maria Sommen

Kathleen Petrus Marie-José Meersman

David Francis Alain Lançois

Marc René De Jonge

Marcel August Constant Janssen

Magali Madeleine Simone Motte

Elisabeth Thérèse Jeanne Pasquier

Ismet Dorange

Lieven Meerpoel

Marc Gaston Venet

Zhenkun Ma

Robert William Kavash

Leo Jacobus Jozef Backx

Brian Desmond Palmer

Christopher Blair Cooper

Jean-Marc Edmond Fernand Marie Neefs

Marc Ren&eacute; De Jonge

Esther Dina Guido Basstanie

Maristella Bernini

Peter Karel Maria Verhasselt

Johann Winkler

Walter Marcel Mathilde Van Den Broeck

Anna Marie Upton

Maria Cristina Villellas Arilla

Elisabeth Therese Jeanne Pasquier

Fran&ccedil;ois Maria Sommen

Frank Xavier Jozef Herwig Arts, Legal Representative

Marc Rene De Jonge

Yvan René Ferdinand Simonnet

Hinrich Wilhelm Helmut Gohlmann

Kathleen Petrus Marie-Jos&eacute; Meersman

Jerome Emile Geroges Guilemont

Elisabeth Thérèse Jeanne

Hinrich Wilhelm Helmut Göhlmann

David Francis Alain LANÇOIS

J E G Guillemont

E T J Pasquier

José Manuel Villalgordo-Soto

Paul Andriaan Jan Janssen

Bart De Cort

This invention concerns pharmaceutical compositions for administration via intramuscular or subcutaneous injection, comprising micro- or nanoparticles of the anti-TB compound bedaquiline, suspended in an aqueous pharmaceutically acceptable carrier, and the use of such pharmaceutical compositions in the treatment and prophylaxis of a pathogenic mycobacterial infection.

Long-acting formulations

The present invention relates to novel combinations, which are useful in the treatment of tuberculosis.

PZA and cytochrome Bc1 inhibitor combination treatment

PZA and cytochrome bc1 inhibitor combination treatment

The present invention relates to compounds of formula (I) including any stereochemically isomeric form thereof, or pharmaceutically acceptable salts thereof, for the treatment of tuberculosis. 

Antibacterial compounds and uses thereof

Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (Ia) or (Ib) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, a tautomeric form thereof or a N-oxide form thereof, wherein Ris hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1, 2, 3 or 4; Ris hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula; Ris alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is 1, 2 or 3; Rand Rare hydrogen, alkyl or benzyl; or Rand Rtogether and including the N to which they are attached may form a ring; Ris hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkythioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal Rradicals may be taken together to form a bivalent radical of formula &#x2014;CH&#x2550;CH&#x2014;CH&#x2550;CH&#x2014;; r is 1, 2, 3, 4 or 5; Ris hydrogen, alkyl, Ar or Het; Ris hydrogen or alkyl; Ris oxo; or Rand Rtogether form the radical &#x2014;CH&#x2550;CH&#x2014;N&#x2550;. 

Quinoline derivatives as antibacterial agents

Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (I) a pharmaceutically acceptable acid or base addition salt, a quaternary amine, a stereochemically isomeric form, a tautomeric form or a N-oxide form thereof, wherein Ris hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1 to 3; s is 0 to 4; Ris hydrogen; halo; alkyl; hydroxy; mercapto; optionally substituted alkyloxy; alkyloxyalkyloxy; alkylthio; mono or di(alkyl)amino wherein alkyl may optionally be substituted; Ar; Het or a radical of formula Ris alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is 0 to 4; Rand Reach independently are hydrogen, alkyl or benzyl; or Rand Rmay be taken together including the N to which they are attached; Ris hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal Rradicals may be taken together to form together with the phenyl ring to which they are attached a naphthyl; r is 1 to 5; Ris hydrogen, alkyl, Ar or Het; Ris hydrogen, alkyl, hydroxyl, aminocarbonyl, mono- or di(alkyl)aminocarbonyl, Ar, Het, alkyl substituted with one or two Het, alkyl substituted with one or two Ar, Het-C(&#x2550;O)&#x2014; or Ar&#x2014;C(&#x2550;O)&#x2014;; provided that when the Rbearing radical is placed in position 3 of the quinoline moiety; Ris placed in position 4 and Ris placed in position 2 and represents hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula then s is 1 to 4.

Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of Formula (Ia) or (Ib) a pharmaceutically acceptable acid or base addition salt thereof, a quaternary amine thereof, a stereochemically isomeric form thereof, a tautomeric form thereof or a N-oxide form thereof, wherein Ris hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1, 2, 3 or 4; Ris hydrogen, hydroxy, thio, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula Ris alkyl, Ar, Ar-alkyl, Het or Het-alkyl; Ris hydrogen, alkyl or benzyl; Ris hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal Rradicals may be taken together to form together with the phenyl ring to which they are attached a naphthyl; r is 1, 2, 3, 4 or 5; Ris hydrogen, alkyl, Ar or Het; Ris hydrogen or alkyl; Ris oxo; or Rand Rtogether form the radical &#x2014;CH&#x2550;CH&#x2014;N&#x2550;; Z is CHor C(&#x2550;O).

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 replication inhibiting pyrimidines

The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof,a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.

Antibacterial quinoline derivatives

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

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

Growing community of inventors

Beerse, Belgium

Koenraad Jozef Lodewijk Marcel Andries