利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

77 条记录 (耗时 0.072 秒)

    Pyrrolobenzodiazepines and conjugates thereof
    54.
    发明授权
    Pyrrolobenzodiazepines and conjugates thereof 有权

    公开(公告)号：US10576164B2

    公开(公告)日：2020-03-03

    申请号：US15786055

    申请日：2017-10-17

    申请人： MedImmune Limited ,  Genentech, Inc.

    发明人： Philip Wilson Howard ,  John A. Flygare ,  Thomas Pillow ,  Binqing Wei

    IPC分类号： A61K47/68 ,  A61P35/00 ,  C07D498/14 ,  C07D519/00 ,  A61K31/5517 ,  C07D487/04 ,  C07D487/16

    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).

    Pyrrolobenzodiazepines
    56.
    发明授权
    Pyrrolobenzodiazepines 有权

    公开(公告)号：US10392393B2

    公开(公告)日：2019-08-27

    申请号：US16072116

    申请日：2017-01-26

    申请人： Medimmune Limited

    发明人： Philip Wilson Howard ,  Thaïs Cailleau

    IPC分类号： C07D487/04 ,  C07D403/12 ,  A61P35/00 ,  A61K47/60 ,  A61K47/65

    摘要： A compound with the formula I, wherein R2 is of formula II, where A is a C5-7 aryl group, X is selected from the group consisting of: OH, SH, CO2H, COH, N═C═O, NHNH2, CONHNH2, (III), (IV), and NHRN, wherein RN is selected from H and C1-4 alkyl, and either: (i) Q1 is a single bond, and Q2 is selected from a single bond and —Z—(CH2)n—, where Z is selected from a single bond, O, S and NH and n is from 1 to 3; or (ii) Q1 is —CH═CH—, and Q2 is a single bond; and its conjugates.