申请人：——
公开号：US20040072863A1
公开（公告）日：2004-04-15
A compound of formula (I), wherein B is a phenyl ring, a 5 to 10 membered heteroaromatic group containing one or more heteroatoms, or a naphthalenyl, 5,6,7,8-tetrahydronaphthalenyl, benzo[1,3]dioxolyl, or biphenyl group; R
1
, R
2
and R
3
each independently represent a hydrogen or halogen atom, or a hydroxy group, a phenyl group, —OR
7
, —SR
7
, —NR
7
R
8
, —NHCOR
7
, —CONR
7
R
8
, —CN, —NO
2
, —COOR
7
or CF
3
group, or a strait or branched, substituted or unsubstituted lower alkyl group, wherein R
7
and R
8
each independently represent a hydrogen atom, a straight or branched lower alkyl group, or together form an alicyclic ring; or R
1
and R
2
together form an aromatic or alicyclic ring or a heterocyclic group. n is an integer from 0 to 4; A represents a group selected from —CH
2
—, —CH═CR
9
—, —CR
9
═CH—, —CR
9
R
10
—, —CO—, —O—, —S—, —S(O)—, —S(O)
2
— and NR
9
, wherein R
9
and R
10
each independently represent a hydrogen atom, a straight or branched lower alkyl group, or together form an alicyclic ring; m is an integer from 0 to 8, provided that when m=0, A is not —CH
2
—; p is an integer from 1 to 2 and the substitution in the azonia bicyclic ring may be in the 2, 3 or 4 position including all possible configurations of the asymmetric carbons; R
4
represents a group of structure: (Formulae II) wherein R
11
represents a hydrogen or halogen atom, a hydroxy group, an alkoxy group, a nitro group, a cyano group, —CO
2
R
12
or —NR
12
R
13
, wherein R
12
and R
13
are identical or different and are selected from hydrogen and straight or branched lower alkyl groups, or a straight or branched, substituted or unsubstituted lower alkyl group; R
5
represents an alkyl group of 1 to 7 carbon atoms, an alkenyl group containing 2 to 7 carbon atoms, or a group of formula (III) wherein q=1 or 2 and R
11
iss a defined above; R
6
represents a hydrogen atom, a hydroxy group, a methyl group or a —CH
2
OH group; and X
−
represents a pharmaceutically acceptable anion of a mono or polyvalent acid.
1
式(I)的化合物，其中B是苯环、含有一个或多个杂原子的5至10元杂芳香族基团，或
萘基、5,6,7,8-四氢
萘基、苯并[1,3]二氧杂环戊基或
联苯基团；R1、R2和R3各自独立地表示氢或卤素原子，或羟基、苯基、—OR7、—SR7、—NR7R8、—NHCOR7、—CONR7R8、—CN、—
NO2、—COOR7或
CF3基团，或直链或支链、取代或未取代的低级烷基基团，其中R7和R8各自独立地表示氢原子、直链或支链的低级烷基基团，或一起形成脂环族环；或者R1和R2一起形成芳香族或脂环族环或杂环基团。n是0至4的整数；A表示选自—
CH2—、—CH═CR9—、—CR9═CH—、—CR9R10—、—CO—、—O—、—S—、—S(O)—、—S(O)2—和NR9的基团，其中R9和R10各自独立地表示氢原子、直链或支链的低级烷基基团，或一起形成脂环族环；m是0至8的整数，条件是当m=0时，A不是— —；p是1至2的整数，并且
氮杂双环环上的取代可以在2、3或4位，包括所有可能的不对称碳构型；R4表示具有结构：(式II)的基团，其中R11表示氢或卤素原子、羟基、烷氧基、硝基、
氰基、—CO2R12或—NR12R13，其中R12和R13相同或不同，并选自氢和直链或支链的低级烷基基团，或直链或支链、取代或未取代的低级烷基基团；R5表示1至7个碳原子的烷基基团、含有2至7个碳原子的烯基基团，或具有式(III)的基团，其中q=1或2，且R11如上定义；R6表示氢原子、羟基、甲基或— OH基团；X-表示药物上可接受的单或多元酸的阴离子。
