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And (pirrolobenzodiacepinas
专利权人:
SPIROGEN SÀRL;GENENTECH, INC.
发明人:
申请号:
ARP140100974
公开号:
AR096287A1
申请日:
2014.03.13
申请国别(地区):
AR
年份:
2015
代理人:
摘要:
Conjugated compounds of formula (1) wherein: R u00b2 is a remainder of the formula (2), where r u00b3 u2076 u1d43 are selected independently and r u00b3 u2076 u1d47 h, F, c u2081 u208b u2084 saturated alkyl, alquenilo c u2082 u208b u2083, where groups are optionally substituted by alkyl and alquenilo a Select Group Or alquilamido c u2081 u208b u2084 and alquil u00e9ster c u2081 u208b u2084; or when one of r u00b3 u2076 u1d43 and r u00b3 u2076 u1d47 is H,The other is selected from Nitrile and a alquil u00e9ster c u2081 u208b u2084; r u2076 and r u2079 are selected independently of H, Oh, o, S, sh, nh u2082, NHR, NRR, no u2082, me u2083sn and Halo; r u2077 is selected regardless of H, Oh, o, S, sh, nh u2082, NHR, NRR no u2082 me u2083sn Halo,, and; and is selected from the f u00f3rmulas (3), (4), (5), (6),(7) and (8); a Connector connected to a cell Binding Agent is the agent of Union; CBA Cell; n is an integer selected within the range of 0 to 48; ra u2074 is a group alquileno c u2081 u208b u2086; either (a) r u00b9 u2070 is H, and r u00b9 u00b9 is Oh, ora,Where ra is c u2081 u208b u2084 alkyl; or (b) r u00b9 u2070 r u00b9 u00b9 and form a carbon nitrogen Double Bond between Carbon and Nitrogen Atoms which are United; or (c) r u00b9 u2070 is H and r u00b9 u00b9 is oso u1dbbm, where z is 2 or 3 and M is a monovalent cation pharmaceutically acceptable; R and R Selection An, each group independently, optionally substituted alkyl and aryl c u2081 u208b u2081 u2082, heterociclilo c u2083 u208b u2082 u2080 c u2085 u208b u2082 u2080,In connection with the group and optionally NRR, R and R, together with the nitrogen Atom to which they are United to form a Heterocyclic Ring of 4, 5, 6 or 7 members optionally substituted; where r u00b9 u2076, r u00b9 u2077, r u00b9 u2079, r u00b2 u2070, r u00b2 u00b9 and r u00b2 u00b2 are as defined for r u2076, r u2077, r u2079, r u00b9 u2070, R u00b9 u00b9 and R u00b2,Respectively, where z is CH or N; where t and T are selected independent
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