NOVEL QUINUCLIDINE DERIVATIVES AND MEDICINAL COMPOSITIONS CONTAINING THE SAME

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专利权人:

ALMIRALL; S.A.

发明人:

Maria Dolors FERNANDEZ FORNER,Maria PRAT QUINONES,Maria Antonia BUIL ALBERO

申请号：

US14311102

公开号：

US20140303126A1

申请日:

2014.06.20

申请国别(地区):

US

年份:

2014

代理人:

摘要：

A compound according to formula (I) wherein z© 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； in 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 formulae (a), (b), (c), (d) and 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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