申请人:THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
公开号:EP0177202A1
公开(公告)日:1986-04-09
Calcium chelating compounds having a decreased affinity for calcium following illumination and of the formulae
or
wherein:
A is -NO2 or -H;
R' is -H (unless R2 is H), -CH3 or other alkyl, -F, -Cl or -Br;
R2 is -H (unless R' is H), -CH3 or other alkyl, -F, -Cl, -Br, or C1-C4 alkoxy;
R3. R4 and R5 are independently -H, OH, NR6R7, or alkoxy, or
R3 and R4 together are -OCH20- or -OCH2CH20- and R5 is -H, OH, NR6R7, or alkoxy, or
R4 and R5 together are -OCH2O- or OCH2CH2O- and R3 is -H, OH, NR6R7, or alkoxy;
X is -OH, alkoxy, -Cl, -Br, -NR6R7, -OCOCH3, -OCOCF3, -OCOCH2NH2, -OP03H, or -OS02CH3;
R6 and R7 are independently -H, methyl or ethyl;
D is O, N, NH, or N alkyl;
Q is a double bond when D is N and a single bond otherwise;
R8 is H and R9 is H or
R8 and R9, together with heteroatom D, the carbon adjacent R8, and the phenyl ring adjacent to R9, form a quinoline ring system (D=N, Q=double bond); and
W is -H, -OH, alkoxy or -NHR6, the compound optionally being as a physiologically acceptable salt or ester thereof.
光照后对钙的亲和力降低的钙螯合化合物,其式为
或
其中
A 是-NO2 或-H;
R'是-H(除非 R2 是 H)、-CH3 或其他烷基、-F、-Cl 或-Br;
R2 是-H(除非 R' 是 H)、-CH3 或其他烷基、-F、-Cl、-Br 或 C1-C4 烷氧基;
R3.R4 和 R5 独立地为-H、OH、NR6R7 或烷氧基,或
R3 和 R4 同为-OCH20-或-OCH2CH20-,R5 为-H、OH、NR6R7 或烷氧基,或
R4 和 R5 同为-OCH2O- 或 OCH2CH2O-,R3 为-H、OH、NR6R7 或烷氧基;
X 是-OH、烷氧基、-Cl、-Br、-NR6R7、-OCOCH3、-OCOCF3、-OCOCH2NH2、-OP03H 或 -OS02CH3;
R6 和 R7 独立地为-H、甲基或乙基;
D 是 O、N、NH 或 N烷基;
当 D 为 N 时,Q 为双键,否则为单键;
R8 是 H,R9 是 H 或
R8 和 R9 与杂原子 D、与 R8 相邻的碳和与 R9 相邻的苯环一起形成一个喹啉环系统(D=N,Q=双键);以及
W 是-H、-OH、烷氧基或-NHR6,化合物可选为生理上可接受的盐或酯。