BINQING WEI,JOHN A FLYGARE,PHILIP WILSON HOWARD,THOMAS PILLOW
申请号：
BR112015023070
公开号：
BR112015023070A2
申请日:
2014.03.13
申请国别(地区):
BR
年份:
2017
代理人:
摘要：
summary "pyrrolbenzodiazepines and conjugates thereof" conjugated compounds of the general formula (a): wherein: r2 is, where r36a and r36b are independently selected from h, f, C1-4 saturated alkyl, c2-3 alkenyl, whose alkyl and alkenyl groups is optionally substituted by a group selected from C1-C4-alkyl-starch alkyl and C1-4-alkyl ester； or, when one of r36a and r36b is h, the other is selected from a nitril and C1-4 alkyl ester； r6 and r9 are independently selected from h, r, oh, or, sh, sr, nh2, nhr, nrr ', no2, me3sn and halo； r7 is independently selected from h, r, oh, or, sh, sr, nh2, nhr, nrr ', no2, me3sn and halo； y is selected from formulas a1, a2, a3, a4, a5 and a6: 1 is a binder bound to a cell binding agent； cba is the cell binding agent； n is an integer selected from 0 to 48； ra4 is a C1-6 alkylene group； or (a) r10 is h, and r11 is oh, well, where ra is aikyl c 1-4； or (b) r10 and r11 form a carbon-nitrogen double bond between the nitrogen and carbon atoms to which they are attached； or (c) r10 is h and r11 is osozm, where z is 2 or 3, and m is a pharmaceutically acceptable monovalent cation； rer 'are each independently selected from optionally substituted C1-12 alkyl, c3-20 heterocyclyl and c5-20 aryl groups, and optionally with respect to the group nrr', rer 'together with the nitrogen atom to which they are linked form a 4-, 5-, 6- or optionally substituted 7-membered heterocyclic ring； wherein r16, r17, r19, r20, r21 and r22 are as defined for r6, r7, r9, r10, r11 and r2, respectively； wherein z is ch or n； wherein tet 'are independently selected from a single bond or a C1-9 alkylene, wherein the chain may be interrupted by one or more heteroatoms, for example o, s, n (h), nme, provided that the number of atoms in the shortest chain of atoms from x and x is from 3 to 12 atoms of； and x and x 'are independently selected from o, s and n (h).resumo “pirrolbenzodiazepinas e conjugados das mesmas” compostos conjugados de fórmula geral (a): em que: r2
