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吡咯并苯并二氮呯及其共軛物
专利权人:
SPIROGEN SARL;GENENTECH, INC.
发明人:
HOWARD, PHILIP WILSON,霍华 菲利浦 威尔森,霍華 菲利浦 威爾森,FLYGARE, JOHN A.,费洛加 约翰A,費洛加 約翰A,PILLOW, THOMAS,皮洛 汤玛斯,皮洛 湯瑪斯,WEI, BINQING,魏斌清,霍华 菲利浦 威尔森,霍華 菲利浦 威爾森,费洛加 约翰A,費洛加 約翰A,皮洛 汤玛斯,皮洛 湯瑪斯
申请号:
TW103109209
公开号:
TW201532615A
申请日:
2014.03.13
申请国别(地区):
TW
年份:
2015
代理人:
摘要:
Conjugate compounds of formula (A): wherein: R2 is , where R36a and R36b are independently selected from H, F, C1-4 saturated alkyl, C2-3 alkenyl, which alkyl and alkenyl groups are optionally substituted by a group selected from C1-4 alkyl amido and C1-4 alkyl ester; or, when one of R36a and R36b is H, the other is selected from nitrile and a 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 formulae A1, A2, A3, A4, A5 and A6: L is a linker connected to a cell binding agent; CBA is the cell binding agent; n is an integer selected in the range of 0 to 48; RA4 is a C1-6 alkylene group; either (a) R10 is H, and R11 is OH, ORA, where RA is C1-4 alkyl; or (b) R10 and R11 form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are bound; or (c) R10 is H and R11 is OSOzM, where z is 2 or 3 and M is a monovalent pharmaceutically acceptable cation; R and R’ are each independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups, and optionally in relation to the group NRR', R and R’ together with the nitrogen atom to which they are attached form an optionally substituted 4-, 5-, 6- or 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 T and T’ are independently selected from a single bond or a C1-9 alkylene, which chain may be interrupted by one or more heteroatoms e.g. O, S, N(H), NMe, provided that the number of atoms in the shortest chain of atoms between X and X’ is 3 to 12 atoms; and X and X’ are independently selected from O, S and N(H).本發明係關於式(A)之共軛化合物:其中:R2為,其中R36a及R36b係獨立地選自H、F、C1-4飽和烷基、C2-3烯基,該等烷基及烯基視情況經選自C1-4烷基醯胺基及C1-4烷基酯基之基團取代;或當R36a及R36b中之一者為H時,另一者係選自腈及C1-4烷基酯基;R6及R9係獨立地選自H、R、OH、OR、SH、SR、NH2、
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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