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NEW FLOROGLUCIN DERIVATIVES ACTIVITIES FOR SELECTIN LIGAND

机译:选择素配体的新型叶绿素衍生物活性

摘要

1. Pharmaceutical compositions comprising at least one compound of formula (I) and a pharmaceutically acceptable carrier that is useful in medicine! ! where the symbols and substituents have the following meanings:! -X- represents! (a) ! ! where m is 0, 1; n is an integer from 1 to 3; ! (b)! ! where the "ring" represents! ! in which R1 represents H, NO2, CF3, F, Cl, Br, I, CN, CH3, NH2, NHalkyl, NHaryl, NACyl and k is 0, 1; ! (with) ! ! where T represents O, S or [H, H]; p is 0, 1, 2; ! -Y- represents! (a) ! ! where s is 0 or 1,! R2 is CO2H, CO2alkyl, CO2aryl, CO2NH2, CO2aralkyl, SO3H, SO2NH2, PO (OH) 2, 1-H-tetrazolyl-, CHO, COCH3, CH2OH, NH2, NHalkyl, N (alkyl) alkyl, OCH3, CH2OCH3 SH, F, Cl, Br, I, CH3, CH2CH3, CN, CF3; ! R3, independently of R2, is H, CH3, CH2CH3, CF3, F, Cl, Br, I, CN, NO2 and! R4, independently of R2 and R3, is H, CH3, CH2CH3, CF3, F, Cl, Br, I, CN, NO2, R2,! R5 represents H, NO2, CF3, F, Cl, Br, I, CN, CH3, OCH3, SH, NH2! and -W- represents - (CH2-) V, cis-CH = CH- or trans-CH = CH-, where v is 0, 1, 2,! in the case where -W- is cis-CH = CH- or trans-CH = CH-, R2 should not be NH2 or SH; ! (b)! ! where R6, independently of R2, is H, F, Cl, Me, t-Bu, CN, NH2; ! (c)! ! (e)! ! where t is 0, 1, 2; ! -Z represents! (i)! ! R7, independently of R2, is H, NO2, CF3, F, Cl, Br, I, CN, CH3, OCH3, SH, NH2,! (iv)! ! where K is NH, NMe, O, S,! (v)! ! or pharmaceutically acceptable salts, esters or amides and prodrugs of the above compounds of formula (I). ! 2. The pharmaceutical compositions according to claim 1, where the compounds have the formula (II)! ! where -X'- is X (a) or X (b) and -Y has the meanings indicated in claim 1. ! 3. The pharmaceutical compositions according to claim 2, where the compounds have the formula (A) or (B)! ! where -X'- and -Y have the meanings indicated in clause 2, and where
机译:1.药物组合物,其包含至少一种式(I)的化合物和可药用的药学上可接受的载体! !其中的符号和取代基具有以下含义: -X-代表! (一种) ! !其中m是0,1; n为1至3的整数; ! (b)! ! “环”代表的地方! !其中R1代表H,NO2,CF3,F,Cl,Br,I,CN,CH3,NH2,NH烷基,NH芳基,NACyl,并且k为0、1; ! (带)! !其中T代表O,S或[H,H]; p是0、1、2; ! -Y-代表! (一种) ! !其中s为0或1! R 2是CO 2 H,CO 2烷基,CO 2芳基,CO 2 NH 2,CO 2芳烷基,SO 3 H,SO 2 NH 2,PO(OH)2,1-H-四唑基-,CHO,COCH 3,CH 2 OH,NH 2,NH烷基,N(烷基)烷基,OCH 3,CH 2 OCH 3 SH, F,Cl,Br,I,CH 3,CH 2 CH 3,CN,CF 3; !与R 2无关的R 3为H,CH 3,CH 2 CH 3,CF 3,F,Cl,Br,I,CN,NO 2和! R 4独立于R 2和R 3,是H,CH 3,CH 2 CH 3,CF 3,F,Cl,Br,I,CN,NO 2,R 2! R 5代表H,NO2,CF3,F,Cl,Br,I,CN,CH3,OCH3,SH,NH2! -W-表示-(CH 2-)V,顺式-CH = CH-或反式-CH = CH-,其中v是0、1、2 、!在-W-为顺式-CH = CH-或反式-CH = CH-的情况下,R2不应为NH2或SH; ! (b)! !其中R6独立于R2是H,F,Cl,Me,t-Bu,CN,NH 2; ! (C)! ! (e)! !其中t为0、1、2; ! -Z代表! (一世)! !独立于R 2的R 7为H,NO 2,CF 3,F,Cl,Br,I,CN,CH 3,OCH 3,SH,NH 2! (iv)! !其中K是NH,NMe,O,S! (v)! !或上述式(I)化合物的药学上可接受的盐,酯或酰胺和前药。 ! 2.根据权利要求1的药物组合物,其中所述化合物具有式(II)! !其中-X'-是X(a)或X(b),而-Y具有权利要求1所示的含义。 3.根据权利要求2的药物组合物,其中所述化合物具有式(A)或(B)! !其中-X'-和-Y具有第2节中指示的含义,其中

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