NOVEL QUINUCLIDINE DERIVATIVES AND MEDICINAL COMPOSITIONS CONTAINING THE SAME

    公开(公告)号:US20100234333A1

    公开(公告)日:2010-09-16

    申请号:US12787772

    申请日:2010-05-26

    摘要: A compound according to formula (I) wherein: {circle around (C)} is a phenyl ring, a C4 to C9 heteroaromatic compound containing one or more heteroatoms, or a naphthalenyl, 5,6,7,8-tetrahydronaphthalenyl or biphenyl group; R1, R2 and R3 each independently represent a hydrogen or halogen atom, or a hydroxy group, or a phenyl, —OR4, —SR4, —NR4R5, —NHCOR4, —CONR4R5, —CN, —NO2, —COOR4 or —CF3 group, or a straight or branched lower alkyl group which may optionally be substituted, for example, with a hydroxy or alcoxy group, wherein R4 and R5 each independently represent a hydrogen atom, straight or branched lower alkyl group, or together form an alicyclic ring; or R1 and R2 together form an aromatic, alicyclic or heterocyclic ring; n is an integer from 0 to 4; A represents a —CH2—, —CH═CR6, —CR6═CH—, —CR6R7—, —CO—, —O—, —S—, —S(O)—, SO2 or —NR6— group, wherein R6 and R7 each independently represent a hydrogen atom, straight or branched lower alkyl group, or R6 and R7 together form an alicyclic ring; m is an integer from 0 to 8; provided that when m=0, A is not —CH2—; p is an integer from 1 to 2 and the substitution in the azoniabicyclic ring may be in the 2, 3 or 4 position including all possible configurations of the asymmetric carbons; B represents a group of formula i) or ii): wherein R10 represents a hydrogen atom, a hydroxy or methyl group; and R8 and R9 each independently represents wherein R11 represents a hydrogen or halogen atom, or a straight or branched lower alkyl group and Q represents a single bond, —CH2—, —CH2—CH2—, —O—, —O—CH2—, —S—, —S—CH2— or —CH═CH—, and when i) or ii) contain a chiral centre they may represent either configuration; X represents a pharmaceutically acceptable anion of a mono or polyvalent acid, which shows high affinity for muscarinic M3 receptors (Hm3).

    Quinuclidine derivatives and medicinal compositions containing the same
    4.
    发明授权
    Quinuclidine derivatives and medicinal compositions containing the same 有权
    奎宁环衍生物和含有它们的药物组合物

    公开(公告)号:US07109210B2

    公开(公告)日:2006-09-19

    申请号:US10740264

    申请日:2003-12-17

    IPC分类号: A61K31/439 C07D453/02

    摘要: Compounds of the formula wherein: {circle around (C)} is phenyl, C4 to C9 heteroaromatic, naphthalenyl, 5,6,7,8-tetrahydronaphthalenyl or biphenyl; R1, R2 and R3 are hydrogen or a substituent; n is 0 to 4; A represents —CH2—, —CH═CR6, —CR6═CH—, —CR6R7—, —CO—, —O—, —S—, —S(O)—, SO2 or —NR6—, wherein R6 and R7 are hydrogen or lower alkyl, or R6 and R7 together form an alicyclic ring; m is 0 to 8; (when m=0, A is not —CH2—); p is 1 or 2; B represents a group of the formula ii): wherein R10 is hydrogen, hydroxy or methyl; and Q represents a single bond, —CH2—, —CH2—CH2—, —O—, —O—CH2—, —S—, —S—CH2— or —CH═CH—, and x represents an anion and wherein the compounds show high affinity for muscarinic M3 receptors (Hm3).

    摘要翻译: 下式的化合物其中:{环绕(C为苯基,C 4至C 9 - 杂芳基,萘基,5,6,7,8-四氢萘基或联苯基; R R 1,R 2和R 3是氢或取代基; n是0-4; A代表-CH 2, CH 3,-CH-CR 6,-CR 6 -CH-,-CR 6,R 7, - , - CO - , - O - , - S - , - S(O) - ,SO 2 - 或-NR 6 - ,其中R 6, R 1和R 2分别为氢或低级烷基,或R 6和R 7一起形成脂环族; m为0至8 ;(当m = 0时,A不是-CH 2 - ); p为1或2; B表示式II)的基团:其中R 10为 氢,羟基或甲基; 且Q表示单键,-CH 2 - , - CH 2 -CH 2 - , - O - , - O-CH -S-,-S-CH 2 - 或-CH-CH-,x表示阴离子,并且其中所述化合物对毒蕈碱M 3受体(Hm3)。

    Quinuclidine carbamate derivatives and their use as M3 antagonists
    9.
    发明授权
    Quinuclidine carbamate derivatives and their use as M3 antagonists 失效
    奎宁环氨基甲酸酯衍生物及其作为M3拮抗剂的用途

    公开(公告)号:US07312231B2

    公开(公告)日:2007-12-25

    申请号:US10404395

    申请日:2003-03-31

    IPC分类号: A61K31/44

    CPC分类号: C07D471/08 C07D453/02

    摘要: A compound which is a carbamate of formula: wherein R1 represents R2 represents a benzyl, phenethyl, furan-2-ylmethyl, furan-3-ylmethyl, thiophen-2-ylmethyl or thiophen-3-ylmethyl group or a straight or branched alkyl group having 3 to 8 carbon atoms, an alkenyl group having 3 to 8 carbon atoms, or a cycloalkyl group of 3 to 6 carbon atoms; p is 1 or 2 and the substitution in the azoniabicyclic ring may be in the 2, 3 or 4 position including all possible configurations of the asymmetric carbons; or a pharmaceutically acceptable salt thereof. The pharmaceutically acceptable salt may be of formula:

    摘要翻译: 化合物,其为下式的氨基甲酸酯:其中R1表示R2表示苄基,苯乙基,呋喃-2-基甲基,呋喃-3-基甲基,噻吩-2-基甲基或噻吩-3-基甲基或直链或支链烷基 具有3至8个碳原子,具有3至8个碳原子的烯基或3至6个碳原子的环烷基; p是1或2,氮杂双环中的取代可以在2,3或4位,包括不对称碳的所有可能构型; 或其药学上可接受的盐。 药学上可接受的盐可以具有下式: