发明名称 Benzazole derivatives as histamine H4 receptor ligands
摘要 The present patent application concerns new ligands of the H4-receptor of formula (I), their process of preparation and their therapeutic use.;
申请公布号 US8802664(B2) 申请公布日期 2014.08.12
申请号 US201113825989 申请日期 2011.09.27
申请人 Bioproject 发明人 Berrebi-Bertrand Isabelle;Billot Xavier;Calmels Thierry;Capet Marc;Danvy Denis;Krief Stephane;Labeeuw Olivier;Lecomte Jeanne-Marie;Levoin Nicolas;Ligneau Xavier;Robert Philippe;Schwartz Jean-Charles
分类号 C07D417/12;C07D401/12;C07D401/14;A61K31/5377;A61K31/454;A61K31/428 主分类号 C07D417/12
代理机构 Stites & Harbison, PLLC. 代理人 Weyer, Esq. Stephen J.;Stites & Harbison, PLLC.
主权项 1. A compound of formula (I):wherein: X represents NR′, S or O; HetAr represents a phenyl or heteroaryl, optionally substituted with one or more substituents chosen from halogen, OR″ alkyl, cyano, NR″R′″, —COR″, —COOR″, —CONR″R′″, aryl, -alkylaryl; R represents a lower alkyl or H R′ represents H, lower alkyl, alkoxyalkyl or alkoxycarbonyl; R″, R′″ identical or different independently represent H or alkyl; HET representing a non aromatic monocyclic heterocycle containing at least one nitrogen atom, which is linked to R; B represents a single bond or an -alkyl- group; A represents O, NH or S; Ar is a mono or polycyclic aromatic or a mono or polycyclic heteroaromatic which can be optionally substituted with one or more of: halo; azido; cyano; hydroxy; nitro;alkyl; alkoxy; alkylsulfanyl; alkenyl; alkynyl; alkenyloxy; alkenyloxy; alkenylsulfanyl; alkynylsulfanyl; cycloalkoxy; cyloalkylalkyl; whose alkyl, alkenyl, alkynyl or cycloalkyl part can be substituted with one or more of halo, hydroxy, polyhydroxy, alkoxy, hydroxyalkoxy, cyano, amino, aminoalkyl, alkylamino, dialkylamino, aminoalkylamino, aminoalkylaminocarbonyl, alkoxycarbonylamino, diarylmethylimino (where aryl is optionally substituted with one or more of hydroxy or halo), cycloalkenylimino (where cylalkenyl is optionally substituted with one or more of alkyl, OH), alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, cycloalkyl, polycycloalkyl, cycloalkenyl, polycycloalkenyl, guanidino, alkylcarbonylguanidino, acylguanidino, cyanoguanidino, alkoxycarbonylguanidino, alkoxycarbonyl, alkoxycarbonylalkylamino, alkoxycarbonylalkylcycloalkyl, alkoxycarbonylheterocyclyl, aminocarbonyl, alkylaminocarbonyl, alkylcarbonyl, alkylcarbonylalkoxy, aryloxy, arylsulfanyl, arylsulfinyl, arylsulfonyl, heteroaryl, heterocyclyl (heterocyclyl being optionally substituted with one or more of oxo, amino, imino), heteroaryloxy, heterocyclyloxy, heteroarylamino, heterocyclylamino, hydrazinocarbonyl, hydroxyalkylcycloalkyl, N-alkyl(thioureido), phtalimido, ureido, oxocycloalkenylamino substituted with amino, carbamimidoylheterocyclyl;amino; alkylamino; alkylcarbonyl; alkoxycarbonyl; alkylsulfanyl; alkylsulfinyl; alkylsulfonyl; alkylsulfonyloxy whose alkyl can be substituted with one or more of halo; aminocarbonyl which can be N-substituted with one or two of alkyl, aryl, arylalkyl;aryl; arylalkyl; aryloxy; arylalkoxy; arylalkylamino; arylalkylsulfanyl; heteroaryl; heteroaryloxy whose aryl part can be substituted with one or more of amino, halo, alkyl, (poly)haloalkyl, hydroxyalkyl, alkoxy, (poly)haloalkoxy, alkoxycarbonylamino, alkylcarbonyl, alkylsulfanyl, alkylsulfinyl, alkylsulfonyl, nitro, cyanoalkyl, or fused with a non aromatic heterocycle;heterocyclyl; heterocyclyloxy; heterocyclylalkoxy whose heterocycle can be substituted with one or more of halogenoalkyl, acylamino, acyloxy, amino, alkyl, alkylamino, dialkylamino, aminoalkyl, oxo, carbamimidoyl, halo, hydroxy, hydroxyalkyl, hydroxymethyl, alkoxcarbonyl; or fused with a non aromatic heterocycle (optionally substituted with one or more of halogens) or carbocycle; as well as their enantiomers, diastereomers, mixtures thereof and pharmaceutically acceptable salts, tautomers, hydrates and solvates.
地址 Paris FR