Tibotec Pharmaceuticals Ltd.

Janssen Pharmaceutica Nv

Koenraad Jozef Lodewijk Andries

Jean-François Bonfanti

Frans E Janssens

Anil Koul

Christophe Meyer

Philippe Muller

Frédéric Marc Maurice Doublet

Rudy Edmond Willebrords

Philip Maria Martha Bern Timmerman

Tom Valerius Josepha Gevers

Jérôme Michel Claude Fortin

Jean Fernand Armand Lacrampe

Jerôme Emile Georges Guillemont

Magali Madeleine Simone Motte

François Maria Sommen

Jérome Michel Claude Fortin

Jérome Emile Georges Guillemont

David Francis Alain LANÇOIS

Frans Eduard Janssens

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

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

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 wherein G is a direct bond or optionally substituted Calkanediyl; Ris Aror a monocyclic or bicyclic heterocycle Q is R, pyrrolidinyl substituted with R, piperidinyl substituted with Ror homopiperidinyl substituted with R; 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(=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. It further concerns the preparation thereof and compositions comprising these compounds, as well as the use thereof as a medicine.

The present invention concerns piperidine-amino-benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula their prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms wherein Q is Calkyl optionally substituted with trifluoromethyl, Ccycloalkyl, Ar, hydroxy, Calkoxy, Calkylthio, Ar-oxy-, Ar-thio-, Ar(CH)oxy, Ar(CH)thio, hydroxycarbonyl, aminocarbonyl, Calkyl-carbonyl, Arcarbonyl, Calkoxycarbonyl, Ar(CH)carbonyl, aminocarbonyloxy, Calkylcarbonyloxy, Arcarbonyloxy, Ar(CH)carbonyloxy, Calkoxy-carbonyl(CH)oxy, mono- or di(Calkyl)aminocarbonyl, mono- or di(Calkyl)-aminocarbonyloxy, aminosulfonyl, mono- or di(Calkyl)aminosulfonyl or a heterocycles selected from the group consisting of pyrrolidinyl, pyrrolyl, dihydropyrrolyl, imidazolyl, triazolyl, piperidinyl, homopiperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, pyridyl and tetrahydropyridyl, wherein each of said heterocycle may optionally be substituted with oxo or Calkyl; G is a direct bond or optionally substituted Calkanediyl; Ris Aror a monocyclic or bicyclic heterocycle; one of Rand Ris Calkyl and the other one of Rand Ris hydrogen; in case Ris different from hydrogen then Ris hydrogen or Calkyl, and Ris hydrogen; in case Ris different from hydrogen then Ris hydrogen or Calkyl, and Ris hydrogen; t is 1, 2 or 3; Aris phenyl or substituted phenyl; and Aris phenyl or substituted phenyl. It further concerns their preparation and compositions comprising them, as well as their use as a medicine.

Piperdine-amino-benzimidazole derivatives as inhibitors of respiratory syncytial virus replication

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Beerse, Belgium

Koenraad Jozef Lodewijk Andries