发明名称 Respiratory syncytial virus replication inhibitors
摘要 The present invention concerns compounds of formula (I), prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof wherein -a<SUP>1</SUP>=a<SUP>2</SUP>-a<SUP>3</SUP>=a<SUP>4</SUP>- represents a radical of formula -CH-CH-CH-CH-; -N-CH-CH-CH-; -CH-N-CH-CH-; -CH-CH-N-CH-; CH-CH-CH-N-; wherein each hydrogen atom may optionally be substituted; Q is a radical of formulae (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), wherein Alk is C<SUB>1-6</SUB>alkanediyl; Y<SUP>1 </SUP>is a bivalent radical of formula -NR<SUP>2</SUP>- or -CH(NR<SUP>2</SUP>R<SUP>4</SUP>); X<SUP>1 </SUP>is NR<SUP>4</SUP>, S, S(-O), S(-O)<SUB>2</SUB>, O, CH<SUB>2</SUB>, C(-O), CH(-CH<SUB>2</SUB>), CH(OH), CH(CH<SUB>3</SUB>), CH(OCH<SUB>3</SUB>), CH(SCH<SUB>3</SUB>), CH(NR<SUP>5a</SUP>R<SUP>5b</SUP>), CH<SUB>2</SUB>-NR<SUP>4 </SUP>or NR<SUP>4</SUP>-CH<SUB>2</SUB>; X<SUP>2 </SUP>is a direct bond, CH<SUB>2</SUB>, C(-O), NR<SUP>4</SUP>, C<SUB>1-4</SUB>alkyl-NR<SUP>4</SUP>, NR<SUP>4</SUP>-C<SUB>1-4</SUB>alkyl, t is 2 to 5; u is 1 to 5; v is 2 or 3; and whereby each hydrogen in Alk and in (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), may optionally be replaced by R<SUP>3</SUP>; provided that when R<SUP>3 </SUP>is hydroxy or C<SUB>1-6</SUB>alkyloxy, then R<SUP>3 </SUP>cannot replace a hydrogen atom in the alpha position relative to a nitrogen atom; G is a direct bond or optionally substituted C<SUB>1-10</SUB>alkanediyl; R<SUP>1 </SUP>is an optionally substituted bicyclic heterocycle; R<SUP>2 </SUP>is hydrogen, formyl, C<SUB>1-6</SUB>alkylcarbonyl, Hetcarbonyl, pyrrolidinyl, piperidinyl, homopiperidinyl, C<SUB>3-7</SUB>cycloalkyl or C<SUB>1-10</SUB>alkyl substituted with N(R<SUP>6</SUP>)<SUB>2 </SUB>and optionally with another substituent; R<SUP>3 </SUP>is hydrogen, hydroxy, C<SUB>1-6</SUB>alkyl, C<SUB>1-6</SUB>alkyloxy, arylC<SUB>1-6</SUB>alkyl or arylC<SUB>1-6</SUB>alkyloxy, R<SUP>4 </SUP>is hydrogen, C<SUB>1-6</SUB>alkyl or arylC<SUB>1-6</SUB>alkyl; R<SUP>5a</SUP>, R<SUP>5b</SUP>, R<SUP>5c </SUP>and R<SUP>5d </SUP>are hydrogen or C<SUB>1-6</SUB>alkyl; or R<SUP>5a </SUP>and R<SUP>5b</SUP>, or R<SUP>5c </SUP>and R<SUP>5d </SUP>taken together from a bivalent radical of formula -(CH<SUB>2</SUB>)<SUB>S</SUB>- wherein S is 4 or 5; R<SUP>6 </SUP>is hydrogen, C<SUB>1-4</SUB>alkyl, formyl, hydroxyC<SUB>1-6</SUB>alkyl, C<SUB>1-6</SUB>alkylcarbonyl or C<SUB>1-6</SUB>alkyloxycarbonyl; aryl is optionally substituted phenyl; Het is pyridyl, pyrimidinyl, pyryzinyl, pyridazinyl; as respiratory syncytial virus replication inhibitors; their preparation, compositions containing them and their use as a medicine.
申请公布号 US7407969(B2) 申请公布日期 2008.08.05
申请号 US20050247392 申请日期 2005.10.11
申请人 JANSSEN PHARMACEUTICA, N.V. 发明人 JANSSENS FRANS EDUARD;LACRAMPE JEAN FERNAND ARMAND;GUILEMONT JEROME EMILE GEROGES;VENET MARC G;ANDRIES KOENRAAD JOZEF LODEWIJK MARCEL
分类号 A61P11/00;C07D491/056;A61K31/436;A61K31/4365;A61K31/437;A61K31/4375;A61K31/4409;A61K31/4439;A61K31/454;A61K31/4709;A61K31/496;A61K31/498;A61P31/12;A61P43/00;C07B61/00;C07D401/06;C07D401/14;C07D409/14;C07D413/14;C07D417/14;C07D471/04 主分类号 A61P11/00
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