Janssen Sciences Ireland Uc

Tibotec Pharmaceuticals Ltd.

Janssen Sciences Ireland Unlimited Company

Janssen Pharmaceutica Nv

Janssen R&d Ireland

Frédéric Marc Maurice Doublet

Jean-François Bonfanti

Jérôme Michel Claude Fortin

Philippe Muller

Pierre Jean-Marie Bernard Raboisson

Eric Pierre Alexandre Arnoult

Christophe Meyer

Rudy Edmond Willebrords

Tom Valerius Josepha Gevers

David Craig McGowan

Werner Embrechts

Nacer Lounis

David Craig Mc Gowan

Koenraad Jozef Lodewijk Andries

Philip Maria Martha Bern Timmerman

Jérome Michel Claude Fortin

This invention relates to macrocyclic deaza-purinones derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.

Macrocyclic deaza-purinones for the treatment of viral infections

The present invention relates to purine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.

Purine derivatives for the treatment of viral infections

This invention relates macrocyclic purine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.

Macrocyclic purines for the treatment of viral infections

The present invention relates to novel compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein the integers are as defined in the description. 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.

Pyrimidine derivatives for the treatment of bacterial diseases

The present invention relates to purine derivatives of formula (I), processes for their preparation, pharmaceutical compositions, and their use in treating viral infections. 

The present invention concerns morpholinyl containing benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula a prodrug, N-oxide, addition salt, quaternary amine, metal complex or stereochemically isomeric form thereof. It further concerns the preparation thereof and compositions comprising these compounds, as well as the use thereof as a medicine.

Morpholinyl containing benzimidazoles as inhibitors of respiratory syncytial virus replication

The present invention concerns 5- or 6-substituted-benzimidazole derivatives having inhibitory activity on the replication of the respiratory syncytial virus and having the formula a prodrug, N-oxide, addition salt, quaternary amine, metal complex or stereochemically isomeric form thereof wherein Q is Ar, R, pyrrolidinyl substituted with R, piperidinyl substituted with Ror homopiperidinyl substituted with R, G is a direct bond or optionally substituted Calkanediyl; Ris Aror a monocyclic or bicyclic heterocycle; one of Rand Ris cyanoCalkyl, cyanoCalkenyl, ArCalkyl, HetCalkyl, N(RR)Calkyl, ArCalkenyl, HetCalkenyl, AraminoCalkyl, HetaminoCalkyl, ArthioCalkyl, HetthioCalkyl, ArsulfonylCalkyl, HetsulfonylCalkyl, Araminocarbonyl, Hetaminocarbonyl, Ar(CH)amino-carbonyl, Het(CH)aminocarbonyl, Arcarbonylamino, Hetcarbonylamino, Ar(CH)carbonylamino, Het(CH)carbonylamino, and the other one of Rand Ris hydrogen; in case Ris hydrogen, then Ris hydrogen;in case Ris hydrogen, the Ris hydrogen or Calkyl. It further concerns their preparation and compositions comprising them, as well as their use as a medicine.

5- or 6-substituted benzimidazole derivatives as inhibitors of respiratory syncytial virus replication

Heterocyclylaminoalkyl Substituted Benzimidazoles Inhibitors of RSV replication of formula (I): The salts and stereochemically isomeric forms thereof, wherein Q is hydrogen, C1-6alkyl optionally substituted with a heterocycle or Q is C1-6alkyl substituted with both &#x2014;OR4 and a heterocycle; wherein said heterocycle is oxazolidine, thiazolidine, 1-oxo-thiazolidine, 1,1-dioxothiazolidine, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, hexahydrooxazepine, hexahydrothiazepine, 1-oxo-hexahydrothiazepine, 1,1-dioxo-hexahydrothiazepine, pyrrolidine, piperidine, homopiperidine, piperazine; which heterocyle may be substituted with 1-2 substituents; each Alk is C1-6alkanediyl; R1 is Ar or optionally substituted piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, furanyl, tetrahydrofuranyl, thienyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, isothiazolyl, pyrazolyl, isoxazo lyl, oxadiazolyl, quinolinyl, quinoxalinyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzthiazolyl, pyridopyridyl, naphthiridinyl, 1H-imidazo[4,5-b]pyridinyl, 3H-imidazo[4,5-b]pyridinyl, imidazo[1,2-a]pyridinyl or 2,3-dihydro-1,4-dioxino[2,3-b]pyridyl; R3 is hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, cyanoC1-6alkyl, aminocarbonyl-C1-6-alkyl, mono- or di(C1-6alkyl)aminocarbonyl-C1-6-alkyl, carboxyl-C1-6-alkyl, C1-6alkoxycarbonyl-C1-6 alkyl; R2, R4 and R5 are hydrogen or C1-6alkyl; Het is pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, furanyl, tetrahydrofuranyl, thienyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, isothiazolyl, pyrazolyl, isoxazolyl, oxadiazolyl, quinolinyl, quinoxalinyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazo lyl, benzthiazolyl, pyridopyridyl, naphthiridinyl, 1H-imidazo[4,5-b]-pyridinyl, 3H-imidazo[4,5-b]pyridinyl, imidazo[1,2-a]pyridinyl and 2,3-dihydro-1,4-dioxino[2,3-b]pyridyl; Ar is optionally substituted phenyl; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). 

Heterocyclylaminoalkyl substituted benzimidazoles

Aminobenzimidazoles and benzimidazoles having inhibitory activity on RSV replication and having the formula the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; wherein G is a direct bond or Calkanediyl optionally substituted with one or more hydroxy, Calkyloxy, ArCalkyloxy, Calkylthio, ArCalkylthio, HO(&#x2014;CH&#x2014;CH&#x2014;O)&#x2014;, Calkyloxy(&#x2014;CH&#x2014;CH&#x2014;O)&#x2014; or ArCalkyloxy(&#x2014;CH&#x2014;CH&#x2014;O)&#x2014;; Ris Aror a monocyclic or bicyclic heterocycle; Q is hydrogen, amino or mono- or di(Calkyl)amino; one of Rand Ris selected from halo, optionally mono- or polysubstituted Calkyl, optionally mono- or polysubstituted Calkenyl, nitro, hydroxy, Ar, N(RR), N(RR)sulfonyl, N(RR)carbonyl, Calkyloxy, Aroxy, ArCalkyloxy, carboxyl, Calkyloxycarbonyl, or &#x2014;C(&#x2550;Z)Ar; and the other one of Rand Ris hydrogen; in case Ris different from hydrogen then Ris hydrogen, Calkyl or halogen and Ris hydrogen; in case Ris different from hydrogen then Ris hydrogen, Calkyl or halogen and Ris hydrogen. Compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.

Aminobenzimidazoles and benzimidazoles as inhibitors of respiratory syncytial virus replication

Inhibitors of RSV replication of formula (I) which can be represented by formula (I) the salts and stereochemically isomeric forms thereof, wherein 

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Isneauville, France

Frédéric Marc Maurice Doublet