[发明专利]聚芳族钠通道阻断剂

权利要求书

1.式(I)代表的化合物：

及其外消旋体、对映异构体、非对映异构体、互变异构体、多晶型物、假多晶型物和可药用盐，其中：

X为氢、卤素、三氟甲基、低级烷基、未取代或取代的苯基、低级烷基-硫基、苯基-低级烷基-硫基、低级烷基-磺酰基或苯基-低级烷基-磺酰基；

Y为氢、羟基、巯基、低级烷氧基、低级烷基-硫基、卤素、低级烷基、未取代或取代的单核芳基，或-N(R²)₂；

R¹为氢或低级烷基；

每个R²独立地为-R⁷、-(CH₂)_m-OR⁸、-(CH₂)_m-NR⁷R¹⁰、-(CH₂)_n(CHOR⁸)(CHOR⁸)_n-CH₂OR⁸、-(CH₂CH₂O)_m-R⁸、-(CH₂CH₂O)_m-CH₂CH₂NR⁷R¹⁰、-(CH₂)_n-C(＝O)NR⁷R¹⁰、-(CH₂)n-(Z)_g-R⁷、-(CH₂)_m-NR¹⁰-CH₂(CHOR⁸)(CHOR⁸)_n-CH₂OR⁸、-(CH₂)_n-CO₂R⁷或

R³和R⁴各自独立地为氢、低级烷基、羟基-低级烷基、苯基、(苯基)-低级烷基、(卤代苯基)-低级烷基、((低级烷基)苯基)-低级烷基、((低级烷氧基)苯基)-低级烷基、(萘基)-低级烷基或(吡啶基)-低级烷基，或者式A或式B代表的基团，前提是R3和R4中至少一个是式A或式B代表的基团；

式A：-(C(R^L)₂)_o-x-(C(R^L)₂)_pA¹

式B：-(C(R^L)₂)_o-x-(C(R^L)₂)_pA²

A¹是被至少一个R⁵所取代的C₇-C₁₅元芳香族碳环，并且其余取代基为R⁶；

A²是被至少一个R⁵所取代的七至十五元芳香族杂环，并且其余取代基为R⁶，其中所述芳香族杂环包含1-4个选自O、N和S的杂原子；

每个R^L独立地为-R⁷、-(CH₂)_n-OR⁸、-O-(CH₂)_m-OR⁸、

-(CH₂)_n-NR⁷R¹⁰、-O-(CH₂)_m-NR⁷R¹⁰、

-(CH₂)_n(CHOR⁸)(CHOR⁸)_n-CH₂OR⁸、

-O-(CH₂)_m(CHOR⁸)(CHOR⁸)_n-CH₂OR⁸、-(CH₂CH₂O)_m-R⁸、

-O-(CH₂CH₂O)_m-R⁸、-(CH₂CH₂O)_m-CH₂CH₂NR⁷R¹⁰、

-O-(CH₂CH₂O)_m-CH₂CH₂NR⁷R¹⁰、-(CH₂)_n-C(＝O)NR⁷R¹⁰、

-O-(CH₂)_m-C(＝O)NR⁷R¹⁰、-(CH₂)_n-(Z)_g-R⁷、-O-(CH₂)_m-(Z)_g-R⁷、

-(CH₂)_n-NR¹⁰-CH₂(CHOR⁸)(CHOR⁸)_n-CH₂OR⁸、

-O-(CH₂)_m-NR¹⁰-CH₂(CHOR⁸)(CHOR⁸)_n-CH₂OR⁸、-(CH₂)_n-CO₂R⁷、

-O-(CH₂)_m-CO₂R⁷、-OSO₃H、-O-葡糖苷酸、-O-葡萄糖、

每个o独立地为0至10的整数；

每个p独立地为0至10的整数；

前提是在每个连续链中o和p的总和为1至10；

每个x独立地为O、NR¹⁰、C(＝O)、CHOH、C(＝N-R¹⁰)、CHNR⁷R¹⁰或单键；

每个R⁵独立地为OH、-(CH₂)_m-OR⁸、-O-(CH₂)_m-OR⁸、

-(CH₂)_n-NR⁷R¹⁰、-O-(CH₂)_m-NR⁷R¹⁰、

-(CH₂)_n(CHOR⁸)(CHOR⁸)_n-CH₂OR⁸、

-O-(CH₂)_m(CHOR⁸)(CHOR⁸)_n-CH₂OR⁸、-(CH₂CH₂O)_m-R⁸、

-O-(CH₂CH₂O)_m-R⁸、-(CH₂CH₂O)_m-CH₂CH₂NR⁷R¹⁰、

-O-(CH₂CH₂O)_m-CH₂CH₂NR⁷R¹⁰、-(CH₂)_n-C(＝O)NR⁷R¹⁰、

-O-(CH₂)_m-C(＝O)NR⁷R¹⁰、-(CH₂)_n-(Z)_g-R⁷、-O-(CH₂)_m-(Z)_g-R⁷、

-(CH₂)_n-NR¹⁰-CH₂(CHOR⁸)(CHOR⁸)_n-CH₂OR⁸、

-O-(CH₂)_m-NR¹⁰-CH₂(CHOR⁸)(CHOR⁸)_n-CH₂OR⁸、-(CH₂)_n-CO₂R⁷、

-O-(CH₂)_m-CO₂R⁷、-OSO₃H、-O-葡糖苷酸、-O-葡萄糖、

-(CH₂)_n-CO₂R¹³、-Het-(CH₂)_m-CO₂R¹³、-(CH₂)_n-(Z)_g-CO₂R¹³、

-Het-(CH₂)_m-(Z)_g-CO₂R¹³、-(CH₂)_n-NR¹⁰-(CH₂)_m(CHOR⁸)_n-CO₂R¹³、

-Het-(CH₂)_m-NR¹⁰-(CH₂)_m(CHOR⁸)_n-CO₂R¹³、

-(CH₂)_n-(CHOR⁸)_m-CO₂R¹³、-Het-(CH₂)_m-(CHOR⁸)_m-CO₂R¹³、

-(CH₂)_n-(CHOR⁸)_m(Z)_g-CO₂R¹³、-Het-(CH₂)_n-(CHOR⁸)_m-(Z)_g-CO₂R¹³、

-(CH₂)_n-(Z)_g-(CH₂)_m-CO₂R¹³、-(CH₂)_n-(Z)_g-(CH₂)_m-CO₂R¹³、

-(CH₂)_n-(Z)_g(CHOR⁸)_m-(Z)_g-CO₂R¹³、

-Het-(CH₂)_n-(Z)_g-(CHOR⁸)_m-(Z)_g-CO₂R¹³、

-(CH₂)_n-CONH-C(＝NR¹³)-NR¹³R¹³、

-Het-(CH₂)_n-CO-NH-C(＝NR¹³)-NR¹³R¹³、

-(CH₂)_n-(Z)_g-CONH-C(＝NR¹³)-NR¹³R¹³、

-Het-(CH₂)_n-(Z)_g-CONH-C(＝NR¹³)-NR¹³R¹³、

-(CH₂)_n-NR¹⁰-(CH₂)_m(CHOR⁸)_n-CONH-C(＝NR¹³)-NR¹³R¹³、

-Het-(CH₂)_n-NR¹⁰-(CH₂)_m(CHOR⁸)_n-CONH-C(＝NR¹³)-NR¹³R¹³、

-(CH₂)_n-(CHOR⁸)_m-CONH-C(＝NR¹³)-NR¹³R¹³、

-Het-(CH₂)_n-(CHOR⁸)_m-CONH-C(＝NR¹³)-NR¹³R¹³、

-(CH₂)_n-(CHOR⁸)_m-(Z)_g-CONH-C(＝NR¹³)-NR¹³R¹³、

-Het-(CH₂)_n-(CHOR⁸)_m-(Z)_g-CONH-C(＝NR¹³)-NR¹³R¹³、

-(CH₂)_n-(Z)_g-(CH₂)_mCONH-C(＝NR¹³)-NR¹³R¹³、

-Het-(CH₂)_n-(Z)_g-(CH₂)_mCONH-C(＝NR¹³)-NR¹³R¹³、

-(CH₂)_n-(Z)_g-(CHOR⁸)_m-(Z)_g-CONH-C(＝NR¹³)-NR¹³R¹³、

Het-(CH₂)_n-(Z)_g-(CHOR⁸)_m-(Z)_g-CONH-C(＝NR¹³)-NR¹³R¹³、

-(CH₂)_n-CONR⁷-CONR¹³R¹³、-Het-(CH₂)_n-CONR⁷-CONR¹³R¹³、

-(CH₂)_n-(Z)_g-CONR⁷-CONR¹³R¹³、-(CH₂)_n-(Z)_g-CONR⁷-CONR¹³R¹³、

-(CH₂)_n-NR¹⁰-(CH₂)_m(CHOR⁸)_n-CONR⁷-CONR¹³R¹³、

-Het-(CH₂)_n-NR¹⁰-(CH₂)_m(CHOR⁸)_n-CONR⁷-CONR¹³R¹³、

-(CH₂)_n-(CHOR⁸)_m-CONR⁷-CONR¹³R¹³、

Het-(CH₂)_n-(CHOR⁸)_m-CONR⁷-CONR¹³R¹³、

-(CH₂)_n-(CHOR⁸)_m-(Z)_g-CONR⁷-CONR¹³R¹³、

-Het-(CH₂)_n-(CHOR⁸)_m-(Z)_g-CNR⁷-CONR¹³R¹³、

-(CH₂)_n-(Z)_g-(CH₂)_mCONR⁷-CONR¹³R¹³、

-Het-(CH₂)_n-(Z)_g-(CH₂)_mCONR⁷-CONR¹³R¹³、

-(CH₂)_n-(Z)_g(CHOR⁸)_m-(Z)_g-CONR⁷-CONR¹³R¹³、

-Het-(CH₂)_n-(Z)_g(CHOR⁸)_m-(Z)_g-CONR⁷-CONR¹³R¹³、

-(CH₂)_n-CONR7SO₂NR¹³R¹³、-Het-(CH₂)_m-CONR⁷SO₂NR¹³R¹³、

-(CH₂)_n-(Z)_g-CONR⁷SO₂NR¹³R¹³、-Het-(CH₂)_m-(Z)_g-CONR⁷SO₂NR¹³R¹³、

-(CH₂)_n-NR¹⁰-(CH₂)_m(CHOR⁸)_n-CONR⁷SO₂NR¹³R¹³、

-Het-(CH₂)_m-NR¹⁰-(CH₂)_m(CHOR⁸)_n-CONR⁷SO₂NR¹³R¹³、

-(CH₂)_n-(CHOR⁸)_m-CONR⁷SO₂NR¹³R¹³、

-Het-(CH₂)_m-(CHOR⁸)_m-CONR⁷SO₂NR¹³R¹³、

-(CH₂)_n-(CHOR⁸)_m-(Z)_g-CONR⁷SO₂NR¹³R¹³、

-Het-(CH₂)_n-(CHOR⁸)_m-(Z)_g-CONR⁷SO₂NR¹³R¹³、

-(CH₂)_n-(Z)_g-(CH₂)_mCONR⁷SO₂NR¹³R¹³、

-Het-(CH₂)_n-(Z)_g-(CH₂)_mCONR⁷SO₂NR¹³R¹³、

-(CH₂)_n-(Z)_g-(CHOR⁸)_m-(Z)_g-CONR⁷SO₂NR¹³R¹³、

-Het-(CH₂)_n-(Z)_g-(CHOR⁸)_m-(Z)_g-CONR⁷SO₂NR¹³R¹³、

-(CH₂)_n-SO₂NR¹³R¹³、-Het-(CH₂)_m-SO₂NR¹³R¹³、

-(CH₂)_n-(Z)_g-SO₂NR¹³R¹³、-Het-(CH₂)_m-(Z)_g-SO₂NR¹³R¹³、

-(CH₂)_n-NR¹⁰-(CH₂)_m(CHOR⁸)_n-SO₂NR¹³R¹³、

-Het-(CH₂)_m-NR¹⁰-(CH₂)_m(CHOR⁸)_n-SO₂NR¹³R¹³、

-(CH₂)_n-(CHOR⁸)_m-SO₂NR¹³R¹³、-Het-(CH₂)_m-(CHOR⁸)_m-SO₂NR¹³R¹³、

-(CH₂)_n-(CHOR⁸)_m-(Z)_g-SO₂NR¹³R¹³、

-Het-(CH₂)_n-(CHOR⁸)_m-(Z)_g-SO₂NR¹³R¹³、

-(CH₂)_n-(Z)_g-(CH₂)_mSO₂NR¹³R¹³、-Het-(CH₂)_n-(Z)_g-(CH₂)_mSO₂NR¹³R¹³、

-(CH₂)_n-(Z)_g-(CHOR⁸)_m-(Z)_g-SO₂NR¹³R¹³、

-Het-(CH₂)_n-(Z)_g-(CHOR⁸)_m-(Z)_g-SO₂NR¹³R¹³、-(CH₂)_n-CONR¹³R¹³、

-Het-(CH₂)_m-CONR¹³R¹³、-(CH₂)_n-(Z)_g-CONR¹³R¹³、

-Het-(CH₂)_m-(Z)_g-CONR¹³R¹³、

-(CH₂)_n-NR¹⁰-(CH₂)_m(CHOR⁸)_n-CONR¹³R¹³、

-Het-(CH₂)_m-NR¹⁰-(CH₂)_m(CHOR⁸)_n-CONR¹³R¹³、

-(CH₂)_n-(CHOR⁸)_m-CONR¹³R¹³、-Het-(CH₂)_m-(CHOR⁸)_m-CONR¹³R¹³、

-(CH₂)_n-(CHOR⁸)_m-(Z)_g-CONR¹³R¹³、

-Het-(CH₂)_n-(CHOR⁸)_m-(Z)_g-CONR¹³R¹³、

-(CH₂)_n-(Z)_g-(CH₂)_mCONR¹³R¹³、-Het-(CH₂)_n-(Z)_g-(CH₂)_mCONR¹³R¹³、

-(CH₂)_n-(Z)_g-(CHOR⁸)_m-(Z)_g-CONR¹³R¹³、

-Het-(CH₂)_n-(Z)_g-(CHOR⁸)_m-(Z)_g-CONR¹³R¹³、-(CH₂)_n-CONR₇COR¹³、

-Het-(CH₂)_m-CONR⁷COR¹³、-(CH₂)_n-(Z)_g-CONR⁷COR¹³、

-Het-(CH₂)_m-(Z)_g-CONR⁷COR¹³、

-(CH₂)_n-NR¹⁰-(CH₂)_m(CHOR⁸)_n-CONR⁷COR¹³、

-Het-(CH₂)_m-NR¹⁰-(CH₂)_m(CHOR⁸)_n-CONR⁷COR¹³、

-(CH₂)_n-(CHOR⁸)_m-CONR⁷COR¹³、

-Het-(CH₂)_m-(CHOR⁸)_m-CONR⁷COR¹³、

-(CH₂)_n-(CHOR⁸)_m-(Z)_g-CONR⁷COR¹³、

-Het-(CH₂)_n-(CHOR⁸)_m-(Z)_g-CONR⁷COR¹³、

-(CH₂)_n-(Z)_g-(CH₂)_mCONR⁷COR¹³、-(CH₂)_n-(Z)_g-(CH₂)_mCONR⁷COR¹³、

-Het-(CH₂)_n-(Z)_g-(CHOR⁸)_m-(Z)_g-CONR⁷COR¹³、

-(CH₂)_n-CONR⁷CO₂R¹³、-(CH₂)_n-(Z)_g-CONR⁷CO₂R¹³、

-Het-(CH₂)_m-(Z)_g-CONR⁷CO₂R¹³、

-(CH₂)_n-NR¹⁰-(CH₂)_m(CHOR⁸)_n-CONR⁷CO₂R¹³、

-Het-(CH₂)_m-NR¹⁰-(CH₂)_m(CHOR⁸)_n-CO NR⁷CO₂R¹³、

-(CH₂)_n-(CHOR⁸)_m-CONR⁷CO₂R¹³、

-Het-(CH₂)_m-(CHOR⁸)_m-CONR⁷CO₂R¹³、

-(CH₂)_n-(CHOR⁸)_m-(Z)_g-CONR⁷CO₂R¹³、

-Het-(CH₂)_n-(CHOR⁸)_m-(Z)_g-CONR⁷CO₂R¹³、

-(CH₂)_n-(Z)_g-(CH₂)_mCONR⁷CO₂R¹³、

-Het-(CH₂)_n-(Z)_g-(CH₂)_mCONR⁷CO₂R¹³、

-(CH₂)_n-(Z)_g-(CHOR⁸)_m-(Z)_g-CONR⁷CO₂R¹³、

-Het-(CH₂)_n-(Z)_g-(CHOR⁸)_m-(Z)_g-CONR⁷CO₂R¹³、

-(CH₂)_n-NH-C(＝NR¹³)-NR¹³R¹³、-Het-(CH₂)_m-NH-C(＝NR¹³)-NR¹³R¹³、

-(CH₂)_n-(Z)_g-NH-C(＝NR¹³)-NR¹³R¹³、

-Het-(CH₂)_m-(Z)_g-NH-C(＝NR¹³)-NR¹³R¹³、

-(CH₂)_n-NR¹⁰-(CH₂)_m(CHOR⁸)_n-NH-C(＝NR¹³)-NR¹³R¹³、

-Het-(CH₂)_m-NR¹⁰-(CH₂)_m(CHOR⁸)_n-NH-C(＝NR¹³)-NR¹³R¹³、

-(CH₂)_n-(CHOR⁸)_m-NH-C(＝NR¹³)-NR¹³R¹³、

-Het-(CH₂)_m-(CHOR⁸)_m-NH-C(＝NR¹³)-NR¹³R¹³、

-(CH₂)_n-(CHOR⁸)_m-(Z)_g-NH-C(＝NR¹³)-NR¹³R¹³、

-Het-(CH₂)_n-(CHOR⁸)_m-(Z)_g-NH-C(＝NR¹³)-NR¹³R¹³、

-(CH₂)_n-(Z)_g-(CH₂)_mNH-C(＝NR¹³)-NR¹³R¹³、

-Het-(CH₂)_n-(Z)_g-(CH₂)_mNH-C(＝NR¹³)-NR¹³R¹³、

-(CH₂)_n-(Z)_g-(CHOR⁸)_m-(Z)_g-NH-C(＝NR¹³)-NR¹³R¹³、

-Het-(CH₂)_n-(Z)_g-(CHOR⁸)_m-(Z)_g-NH-C(＝NR¹³)-NR¹³R¹³、

-(CH₂)_n-C(＝NR¹³)-NR¹³R¹³、Het-(CH₂)_m-C(＝NH)-NR¹³R¹³、

-(CH₂)_n-(Z)_g-C(＝NH)-NR¹³R¹³、Het-(CH₂)_m-(Z)_g-C(＝NH)-NR¹³R¹³、

-(CH₂)_n-NR¹⁰-(CH₂)_m(CHOR⁸)_n-C(＝NR¹³)-NR¹³R¹³、

Het-(CH₂)_m-NR¹⁰-(CH₂)_m(CHOR⁸)_n-C(＝NR¹³)-NR¹³R¹³、

-(CH₂)_n-(CHOR⁸)_m-C(＝NR¹³)-NR¹³R¹³、

-Het-(CH₂)_m-(CHOR⁸)_m-C(＝NR¹³)-NR¹³R¹³、

-(CH₂)_n-(CHOR⁸)_m-(Z)_g-C(＝NR¹³)-NR¹³R¹³、

-Het-(CH₂)_n-(CHOR⁸)_m-(Z)_g-C(＝NR¹³)-NR¹³R¹³、

-(CH₂)_n-(Z)_g-(CH₂)_m-C(＝NHC(＝NR¹³)-NR¹³R¹³、

Het-(CH₂)_n-(Z)_g-(CH₂)_m-C(＝N R¹³)-NR¹³R¹³、

-(CH₂)_n-(Z)_g-(CHOR⁸)_m-(Z)_g-C(＝NR¹³)-NR¹³R¹³、

-Het-(CH₂)_n-(Z)_g-(CHOR⁸)_m-(Z)_g-C(＝NR¹³)-NR¹³R¹³、-(CH₂)_n-NR¹²R¹²、

-O-(CH₂)_m-NR¹²R¹²、-O-(CH₂)_n-NR¹²R¹²、-O-(CH₂)_m(Z)_gR¹²、

-(CH₂)_nNR¹¹R¹¹、-O-(CH₂)_mNR¹¹R¹¹、-(CH₂)_n-(Z)_g-(CH₂)_m-NR¹⁰R¹⁰、

-O-(CH₂)_m-(Z)_g-(CH₂)_m-NR¹⁰R¹⁰、-(CH₂CH₂O)_m-CH₂CH₂NR¹²R¹²、

-O-(CH₂CH₂O)_m-CH₂CH₂NR¹²R¹²、-(CH₂)_n-(C＝O)NR¹²R¹²、

-O-(CH₂)_m-(C＝O)NR¹²R¹²、-O-(CH₂)_m-(CHOR⁸)_mCH₂NR¹⁰-(Z)_g-R¹⁰、

-(CH₂)_n-(CHOR⁸)_mCH₂-NR¹⁰-(Z)_g-R¹⁰、

-(CH₂)_nNR¹⁰-O(CH²)_m(CHOR⁸)_nCH₂NR¹⁰-(Z)_g-R¹⁰、

-O(CH₂)_m-NR¹⁰-(CH₂)_m-(CHOR⁸)_nCH₂NR¹⁰-(Z)_g-R¹⁰、

-(Het)-(CH₂)_m-OR⁸、-(Het)-(CH₂)_m-NR⁷R¹⁰、

-(Het)-(CH₂)_m(CHOR⁸)(CHOR⁸)_n-CH₂OR⁸、-(Het)-(CH₂CH₂O)_m-R⁸、

-(Het)-(CH₂CH₂O)_m-CH₂CH₂NR⁷R¹⁰、-(Het)-(CH₂)_m-C(＝O)NR⁷R¹⁰、

-(Het)-(CH₂)_m-(Z)_g-R⁷、

-(Het)-(CH₂)_m-NR¹⁰-CH₂(CHOR⁸)(CHOR⁸)_n-CH₂OR⁸、

-(Het)-(CH₂)_m-CO₂R⁷、-(Het)-(CH₂)_m-NR¹²R¹²、-(Het)-(CH₂)_n-NR¹²R¹²、

-(Het)-(CH₂)_m-(Z)_gR¹²、-(Het)-(CH₂)_mNR¹¹R¹¹、

-(Het)-(CH₂)_m-(Z)_g-(CH₂)_m-NR¹⁰R¹⁰、

-(Het)-(CH₂CH₂O)_m-CH₂CH₂NR¹²R¹²、-(Het)-(CH₂)_m-(C＝O)NR¹²R¹²、

-(Het)-(CH₂)_m-(CHOR⁸)_mCH₂NR¹⁰-(Z)_g-R¹⁰、

-(Het)-(CH₂)_m-NR¹⁰-(CH₂)_m-(CHOR⁸)_nCH₂NR¹⁰-(Z)_g-R¹⁰、

-(CH₂)_n(CHOR⁸)(CHOR⁸)_n-CH₂OR⁸、

-O-(CH₂)_m(CHOR⁸)(CHOR⁸)_n-CH₂OR⁸、

-(CH₂)_n-NR¹⁰-CH₂(CHOR⁸)(CHOR⁸)_n-CH₂OR⁸、

-O-(CH₂)_m-NR¹⁰-CH₂(CHOR⁸)(CHOR⁸)_n-CH₂OR⁸、Link-(CH₂)_n-CAP、

Link-(CH₂)_n(CHOR⁸)(CHOR⁸)_n-CAP、Link-(CH₂CH₂O)_m-CH₂-CAP、

Link-(CH₂CH₂O)_m-CH₂CH₂-CAP、Link-(CH₂)_n-(Z)_g-CAP、

Link-(CH₂)_n(Z)_g-(CH₂)_m-CAP、

Link-(CH₂)_n-NR¹³-CH₂(CHOR⁸)(CHOR⁸)_n-CAP、

Link-(CH₂)_n-(CHOR⁸)_mCH₂-NR¹³-(Z)_g-CAP、

Link-(CH₂)_nNR¹³-(CH₂)_m(CHOR⁸)_nCH₂NR¹³-(Z)_g-CAP、

-Link-(CH₂)_m-(Z)_g-(CH₂)_m-CAP、Link-NH-C(＝O)-NH-(CH₂)_m-CAP、

Link-(CH₂)_m-C(＝O)NR¹³-(CH₂)_m-C(＝O)NR¹⁰R¹⁰、

Link-(CH₂)_m-C(＝O)NR¹³-(CH₂)_m-CAP、Link-(CH₂)_m-C(＝O)NR¹¹R¹¹、

Link-(CH₂)_m-C(＝O)NR¹²R¹²、Link-(CH₂)_n-(Z)_g-(CH₂)_m-(Z)_g-CAP、

Link-(Z)g-(CH₂)_m-Het-(CH₂)_m-CAP、Link-(CH₂)_n-CR¹¹R¹¹-CAP、

Link-(CH₂)_n(CHOR⁸)(CHOR⁸)_n-CR¹¹R¹¹-CAP、

Link-(CH₂CH₂O)_m-CH₂-CR¹¹R¹¹-CAP、

Link-(CH₂CH₂O)_m-CH₂CH₂-CR¹¹R¹¹-CAP、

Link-(CH₂)_n-(Z)_g-CR¹¹R¹¹-CAP、

Link-(CH₂)_n(Z)_g-(CH₂)_m-CR¹¹R¹¹-CAP、

Link-(CH₂)_n-NR¹³-CH₂(CHOR⁸)(CHOR⁸)_n-CR¹¹R¹¹-CAP、

Link-(CH₂)_n-(CHOR⁸)_mCH₂-NR¹³-(Z)_g-CR¹¹R¹¹-CAP、

Link-(CH₂)_nNR¹³-(CH₂)_m(CHOR⁸)_nCH₂NR¹³-(Z)_g-CR¹¹R¹¹-CAP、

Link-(CH₂)_m-(Z)_g-(CH₂)_m-CR¹¹R¹¹-CAP、

Link NH-C(＝O)-NH-(CH₂)_m-CR¹¹R¹¹-CAP、

Link-(CH₂)_m-C(＝O)NR¹³-(CH₂)_m-CR¹¹R¹¹-CAP、

Link-(CH₂)_n-(Z)_g-(CH₂)_m-(Z)_g-CR¹¹R¹¹-CAP或

Link-(Z)_g-(CH₂)_m-Het-(CH₂)_m-CR¹¹R¹¹-CAP；

每个R⁶独立地为R⁵、-R⁷、-OR¹¹、-N(R⁷)₂、-(CH₂)_m-OR⁸、

-O-(CH₂)_m-OR⁸、-(CH₂)_n-NR⁷R¹⁰、-O-(CH₂)_m-NR⁷R¹⁰、

-(CH₂)_n(CHOR⁸)(CHOR⁸)_n-CH₂OR⁸、

-O-(CH₂)_m(CHOR⁸)(CHOR⁸)_n-CH₂OR⁸、-(CH₂CH₂O)_m-R⁸、

-O-(CH₂CH₂O)_m-R⁸、-(CH₂CH₂O)_m-CH₂CH₂NR⁷R¹⁰、

-O-(CH₂CH₂O)_m-CH₂CH₂NR⁷R¹⁰、-(CH₂)_n-C(＝O)NR⁷R¹⁰、

-O-(CH₂)_m-C(＝O)NR⁷R¹⁰、-(CH₂)_n-(Z)_g-R⁷、-O-(CH₂)_m-(Z)_g-R⁷、

-(CH₂)_n-NR¹⁰-CH₂(CHOR⁸)(CHOR⁸)_n-CH₂OR⁸、

-O-(CH₂)_m-NR¹⁰-CH₂(CHOR⁸)(CHOR⁸)_n-CH₂OR⁸、-(CH₂)_n-CO₂R⁷、

-O-(CH₂)_m-CO₂R⁷、-OSO₃H、-O-葡糖苷酸、-O-葡萄糖、

其中当两个R⁶为-OR¹¹且彼此相邻位于芳香族碳环或芳香族杂环上时，这两个OR¹¹可形成亚甲基二氧基；

每个R⁷独立地为氢、低级烷基、苯基、取代的苯基或-CH₂(CHOR⁸)_m-CH₂OR⁸；

每个R⁸独立地为氢、低级烷基、-C(＝O)-R¹¹、葡糖苷酸、2-四氢吡喃基或

每个R⁹独立地为-CO₂R⁷、-CON(R⁷)₂、-SO₂CH₃、-C(＝O)R⁷、-CO₂R¹³、-CON(R¹³)₂、-SO₂CH₂R¹³或-C(＝O)R¹³；

每个R¹⁰独立地为-H、-SO₂CH₃、-CO₂R⁷、-C(＝O)NR⁷R⁹、-C(＝O)R⁷或-CH₂-(CHOH)_n-CH₂OH；

每个Z独立地为-(CHOH)-、-C(＝O)-、-(CHNR⁷R¹⁰)-、-(C＝NR¹⁰)-、-NR¹⁰-、-(CH₂)_n-、-(CHNR¹³R1³)-、-(C＝NR¹³)-或-NR¹³-；

每个R¹¹独立地为氢、低级烷基、苯基低级烷基或取代的苯基低级烷基；

每个R¹²独立地为-SO₂CH₃、-CO₂R⁷、-C(＝O)NR⁷R⁹、-C(＝O)R⁷、-CH₂(CHOH)_n-CH₂OH、-CO₂R¹³、-C(＝O)NR¹³R¹³或-C(＝O)R¹³；

每个R¹³独立地为R⁷、R¹⁰、-(CH₂)_m-NR⁷R¹⁰、-(CH₂)_m-NR⁷R⁷、-(CH₂)_m-NR¹¹R¹¹、-(CH₂)_m-(NR¹¹R¹¹R¹¹)⁺、-(CH₂)_m-(CHOR⁸)_m-(CH₂)_mNR¹¹R¹¹、-(CH₂)_m-(CHOR⁸)_m-(CH₂)_mNR⁷R¹⁰、-(CH₂)_m-NR¹⁰R¹⁰、-(CH₂)_m-(CHOR⁸)_m-(CH₂)_m-(NR¹¹R¹¹R¹¹)⁺、-(CH₂)_m-(CHOR⁸)_m-(CH₂)_mNR⁷R⁷、

前提是在结构部分-NR¹³R¹³中，两个R¹³与它们所连接的氮一起可任选地形成选自下述的环：

每个V独立地为-(CH₂)_m-NR⁷R¹⁰、-(CH₂)_m-NR⁷R⁷、-(CH₂)_m-(NR¹¹R¹¹R¹¹)+、-(CH₂)_n-(CHOR⁸)_m-(CH₂)_mNR⁷R¹⁰、-(CH₂)_n-NR¹⁰R¹⁰-(CH₂)_n-(CHOR⁸)_m-(CH₂)_mNR⁷R⁷、-(CH₂)_n-(CHOR⁸)_m-(CH₂)_m-(NR¹¹R¹¹R¹¹)⁺，

前提是当V直接连接到氮原子时，则V也可以独立地为R⁷、R¹⁰或(R¹¹)₂；

每个R¹⁴独立地为H、R¹²、-(CH₂)_n-SO₂CH₃、-(CH₂)_n-CO₂R¹³、-(CH₂)_n-C(＝O)NR¹³R¹³、-(CH₂)_n-C(＝O)R¹³、-(CH₂)_n-(CHOH)_n-CH₂OH、-NH-(CH₂)_n-SO₂CH₃、NH-(CH₂)_n-C(＝O)R¹¹、NH-C(＝O)-NH-C(＝O)R¹¹、-C(＝O)NR¹³R¹³、-OR¹¹、-NH-(CH₂)_n-R¹⁰、-Br、-Cl、-F、-I、SO₂NHR¹¹、-NHR¹³、-NH-C(＝O)-NR¹³R¹³、-(CH₂)_n-NHR¹³或-NH-(CH₂)_n-C(＝O)-R¹³；

每个g独立地为1至6的整数；

每个m独立地为1至7的整数；

每个n独立地为0至7的整数；

每个-Het-独立地为-N(R⁷)-、-N(R¹⁰)-、-S-、-SO-、-SO₂-、-O-、-SO₂NH-、-NHSO₂-、-NR⁷CO-、-CONR⁷-、-N(R1³)-、-SO₂NR¹³-、-NR¹³CO-或-CONR¹³-；

每个Link独立地为-O-、-(CH₂)_n-、-O(CH₂)_m-、-NR¹³-C(＝O)-NR¹³-、-NR¹³-C(＝O)-(CH₂)_m-、-C(＝O)NR¹³-(CH₂)_m、-(CH₂)_n-(Z)_g-(CH₂)_n-、-S-、-SO-、-SO₂-、-SO₂NR⁷-、-SO₂NR¹⁰-或-Het-；

每个CAP独立地为噻唑烷二酮、噁唑烷二酮、-杂芳基-C(＝O)NR¹³R¹³、杂芳基-W、-CN、-O-C(＝S)NR¹³R¹³、-(Z)_gR¹³、-CR¹⁰((Z)_gR¹³)((Z)_gR¹³)、-C(＝O)OAr、-C(＝O)NR¹³Ar、咪唑啉、四唑、四唑酰胺、-SO₂NHR¹³、-SO₂NH-C(R¹³R¹³)-(Z)_g-R¹³、环状糖或低聚糖、环状氨基糖、低聚糖、-CR¹⁰(-(CH₂)_m-R⁹)(-(CH₂)_m-R⁹)、-N(-(CH₂)_m-R⁹)(-(CH₂)_m-R⁹)、-NR¹³(-(CH₂)_m-CO₂R¹³)、

每个Ar独立地为苯基、取代苯基，或者是杂芳基，其中所述取代苯基的取代基为1-3个独立地选自下述的取代基：OH、OCH₃、NR¹³R¹³、Cl、F和CH₃；和

每个W独立地为噻唑烷二酮、噁唑烷二酮、杂芳基-C(＝O)NR¹³R¹³、-CN、-O-C(＝S)NR¹³R¹³、-(Z)_gR¹³、-CR¹⁰((Z)_gR¹³)((Z)_gR¹³)、-C(＝O)OAr、-C(＝O)NR¹³Ar、咪唑啉、四唑、四唑酰胺、-SO₂NHR¹³、-SO₂NH-C(R¹³R¹³)-(Z)_g-R¹³、环状糖或低聚糖、环状氨基糖、低聚糖、

前提是当任一个-CHOR⁸-或-CH₂OR⁸基团相对于彼此位于1，2-或1，3-位时，则R⁸基团可以任选地一起形成环状单-或二-取代的1，3-二氧环己环或1，3-二氧环戊烷。