发明申请
- 专利标题: Novel quinuclidine derivatives and medicinal compositions containing the same
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申请号: US11116777申请日: 2005-04-28
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公开(公告)号: US20050209272A1公开(公告)日: 2005-09-22
- 发明人: Maria Fernandez Forner , Maria Quinones , Maria Buil Albero
- 申请人: Maria Fernandez Forner , Maria Quinones , Maria Buil Albero
- 优先权: ESP9901580 19990714
- 主分类号: A61K31/435
- IPC分类号: A61K31/435 ; A61K31/439 ; A61K31/4745 ; A61P1/00 ; A61P1/04 ; A61P1/06 ; A61P1/12 ; A61P11/00 ; A61P11/02 ; A61P11/06 ; A61P11/08 ; A61P11/14 ; A61P13/00 ; A61P13/02 ; A61P13/06 ; A61P13/10 ; A61P27/16 ; A61P43/00 ; C07D453/02
摘要:
A compound according to formula (I) wherein: {circle over (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).
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