Derivatives of benzofuran or benzodioxazole compounds
    5.
    发明授权
    Derivatives of benzofuran or benzodioxazole compounds 失效
    苯并呋喃或苯并恶唑化合物的衍生物

    公开(公告)号:US06716987B1

    公开(公告)日:2004-04-06

    申请号:US10023091

    申请日:2001-12-20

    IPC分类号: C07D41300

    摘要: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)— C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z represents CONH, CONHCH2, or a bond), or N], or (iii) a bond; and R5 represents aryl, an aromatic heterocyclic group, cycloalkyl, pyridine-N-oxide, cyano, or lower alkoxycarbonyl; or pharmaceutically acceptable salts thereof.

    摘要翻译: 由下式(I)表示的含氧杂环化合物:其中R 1和R 2独立地表示氢,低级烷基,氰基, - (CH 2)nE 1 -CO-G 1(其中 E 1表示键,O或NH;且G 1表示氢,取代或未取代的低级烷基,OR 6或NR 7 R 8; n表示0〜 4)等; R 1和R 2相互结合形成饱和碳环和与其相邻的碳原子。 或R 2,以及下述R 11或R 13组合形成单键; R 3表示氢,苯基或卤素; R 4表示羟基,低级烷氧基等; A表示-C(R 9)(R 10) - 或O; B表示O,NR 11,-C(R 12)(R 13) - 或-C(R 14)(R 15)-C(R 16)(R 16) <17>) - ; D表示(i)-C(R 18)(R 19)-X-(其中X表示-C(R 21)(R 22) - ,S或NR 23) ,(ii)-C(R 19)= Y- [Y表示-C(R 24) - Z-(其中Z表示CONH,CONHCH 2或键)或N]或(iii) 一个债券 R 5表示芳基,芳香族杂环基,环烷基,吡啶-N-氧化物,氰基或低级烷氧基羰基; 或其药学上可接受的盐。

    Derivatives of benzofuran or benzodioxole
    6.
    发明授权
    Derivatives of benzofuran or benzodioxole 失效
    苯并呋喃或苯并间二氧杂环戊烯的衍生物

    公开(公告)号:US06514996B2

    公开(公告)日:2003-02-04

    申请号:US08974739

    申请日:1997-11-19

    IPC分类号: A61K3144

    摘要: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)—C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z represents CONH, CONHCH2, or a bond), or N], or (iii) a bond; and R5 represents aryl, an aromatic heterocyclic group, cycloalkyl, pyridine-N-oxide, cyano, or lower alkoxycarbonyl; or pharmaceutically acceptable salts thereof.

    摘要翻译: 由下式(I)表示的含氧杂环化合物:其中R1和R2独立地表示氢,低级烷基,氰基, - (CH2)n-E1-CO-G1(其中E1表示键,O或NH; 并且G 1表示氢,取代或未取代的低级烷基,OR 6或NR 7 R 8; n表示0〜4的整数)等。 R 1和R 2组合​​在一起,与邻近的碳原子一起代表饱和碳环; 或R 2,R 11或R 13组合形成单键; R3表示氢,苯基或卤素; R4代表羟基,低级烷氧基等; A表示-C(R 9)(R 10) - 或O; B表示O,NR 11,-C(R 12)(R 13) - 或-C(R 14)(R 15)-C(R 16)(R 17) - ; D表示(i)-C(R 18)(R 19)-X-(其中X表示-C(R 21)(R 22) - ,S或NR 23),(ⅱ)-C(R 19a)= Y- [Y -C(R 24)-Z-(其中Z表示CONH,CONHCH 2或键)或N]或(iii)键; R5表示芳基,芳香族杂环基,环烷基,吡啶-N-氧化物,氰基或低级烷氧基羰基; 或其药学上可接受的盐。

    Imidazoquinolone derivatives
    10.
    发明授权
    Imidazoquinolone derivatives 失效
    咪唑喹啉酮衍生物

    公开(公告)号:US4994468A

    公开(公告)日:1991-02-19

    申请号:US489025

    申请日:1990-03-05

    IPC分类号: C07D471/04

    CPC分类号: C07D471/04

    摘要: Novel imidazoquinolone derivative represented by the formula (I); ##STR1## wherein R.sup.1 represents hydrogen, alkyl, cycloalkyl, alkenyl aralkyl, aralkenyl or substituted or unsubstituted aryl; X represents nitrogen or ##STR2## where R.sup.2 is hydrogen, hydroxyl, alkyl, cycloalkyl, alkenyl, aralkyl, aralkenyl, substituted or unsubstituted aryl, thiol, halogen, substituted or unsubstituted aromatic heterocyclic group, or --(CH.sub.2).sub.m CO.sub.2 R.sup.6 where R.sup.6 is hydrogen or lower alkyl and m is an integer of 0 to 3; Y represents oxygen or sulfur; R.sup.3 represents alkyl, cycloalkyl, alkoxyalkly, alkenyl, aralkyl, aralkenyl, --(CH.sub.2).sub.n -- Het where Het is substituted or unsubstituted aromatic heterocyclic group and n is an integer of 1 to 3 or --(CH.sub.2).sub.n CO.sub.2 R.sup.6a where n has the same meaning as defined above and R.sup.6a has the same meaning as defined as to R.sup.6 ; each of R.sup.4 and R.sup.5 independently represents hydrogen, lower alkyl, trifluoromethyl, cycloalkyl, halogen, hydroxyl, lower alkoxyl, lower alkylthio, nitro, amino, lower alkylamino, lower alkanoylamino, aroylamino, lower alkanoyl or aroyl; and a pharmaceutically acceptable salt thereof. The Compound (I) and a pharmaceutically acceptable salt thereof show bronchodilatory and antiallergic activities, and are useful for treating respiratory disorders such as bronchial asthma.