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Pyrrolbenzodiazepine
专利权人:
СПИРОГЕН САРЛ;СИЭТЛ ДЖЕНЕТИКС, ИНК.
发明人:
Филип Уилсон,Арно,Скотт,Патрик
申请号:
EA201490535
公开号:
EA201490535A1
申请日:
2012.10.12
申请国别(地区):
EA
年份:
2014
代理人:
摘要:
The compound of the formula I, where R is the formula II, where X is selected from the group consisting of OH, SH, COH, COH, N = C = O, NHNH, CONHNH, NHR, where R is selected from the group consisting of H and C1-6 alkyl; R, R and R are independently selected from H and unsubstituted C1-6 alkyl; and either R is selected from the group consisting of (ia) a Caryl group optionally substituted by one or more substituents selected from the group consisting of halogen, nitro, cyano, ether, C1-6 alkyl, Cheterocyclyl, and bis-hydroxy-C1-6 alkylene; (ib) C saturated aliphatic alkyl; (ic) Saturated cycloalkyl; (id) where each of R, R and R is independently selected from H, C saturated alkyl, Salkenyl, Salkinyl and cyclopropyl, where the total number of carbon atoms in the group R is not more than 5; (ie) where one of R1 and R1 is H and the other is selected from phenyl, where phenyl is optionally substituted with a group selected from halogen, methyl, methoxy; pyridyl and thiophenyl; and (if) where R is selected from H; C saturated alkyl; Salkenil; Calkinilla; cyclopropyl; phenyl, where phenyl is optionally substituted with a group selected from halogen, methyl, methoxy; pyridyl and thiophenyl; and R and R are independently selected from H, R, OH, OR, SH, SR, NH, NHR, NRR ', nitro, MeSn, and halogen; where R and R 'are independently selected from the optionally substituted C1-6 alkyl, C2 heterocyclyl and Saryl groups; R is selected from H, R, OH, OR, SH, SR, NH, NHR, NHRR ', nitro, MeSn and halogen; either (a) R 5 is H and R is OH, OR, where R 2 is C1-6 alkyl; (b) R and R form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are attached; or (c) R 2 is H and R 3 is SOM, where z is 2 or 3 and M is a monovalent pharmaceutically acceptable cation; R "is a C1-6 alkylene group whose chain may be interrupted by one or more heteroatoms and / or aromatic rings; Y and Y 'are selected from O, S or NH;Соединение формулы Iгде R2 имеет формулу IIгде X выбр
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