DAVID EDWIN THURSTON,KHONDAKER MIRAZUR RAHMAN,PETER WILLIAM TAYLOR,PHILIP WILSON HOWARD
申请号:
BR112014027190
公开号:
BR112014027190A2
申请日:
2013.04.30
申请国别(地区):
BR
年份:
2017
代理人:
摘要:
Summary "Pyrrolobenzodiazepines" The present invention relates to a compound of formula I: (i) or a salt or solvate thereof, wherein: the dotted double bond indicates the presence of a single or double bond between c2 and c3; r 2 is selected from -h, -oh, = o, = ch 2, -cn, -r, or, halo, di-halo, = chr, = chrr ', -o-so 2 -r, co 2 r and color; r7 is selected from h, r, oh, or, sh, sr, nh2, nhr, nrr ', nitro, me3sn and halo; wherein r and r 'are independently selected from optionally substituted C1-7 alkyl, c3-20 heterocyclyl and c5-20 aryl groups; r10 and r11 together form a double bond, or are selected from h and qrq respectively, where q is selected from o, if nh and rq is h or C1-7 alkyl or he soxm, where x is 2 or 3 em is a monovalent pharmaceutically acceptable cation; a is selected from a1, a2, a3, a4 or a5: (a1) (a2) (a3) (a4) (a5) where x1 and y1 are selected from: ch and nh; ch and nme; n and nme; ch and s; n and s; n and o; and ch and o respectively; x2 and y2 are selected from: ch and nh; ch and nme; n and nme; ch and s; n and s; n and o; and ch and o respectively; z1 is selected from o and s; z2 is selected from ch and n; f is selected from a single bond and - (e-f1) m-; each e is independently selected from a single bond, and –c (= o) -nh-; each f1 is independently a c3-20 heteroarylene group; m is 1, 2 or 3; g is selected from hydrogen, C1-4 alkyl group, -c (= o) -o C1-4 alkyl, - (ch2) n-heterocycloalkyl c3-20, and –o- (ch2) n -heterocycloalkyl ; each n is 0-4; provided that a2 is not a2 ': (a2'); wherein x1 and y1 of a2 'are selected from: ch and nme; coh and nme; ch and s; n and nme; n and s respectively; and provided that a3 is not a3 ': (a3') where x2 and y2 of a3 'are selected from: ch and nme; coh and nme; ch and s; n and nme; n and s respectively; b is a simple bond or: where x and y of b1 are selected from: ch and nme; coh and nme; ch and s; n and nme; n and s respectively; and R1 is C1-4 alkyl.resumo “pirrolobenzodiazepinas” a presente invenção