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    C8, c8' linked 5-oxo-1,2,3,11a-tetrahydro-5h-pyrrolo[2,1-c][1,4] benzodiazepine dimers with 1h-pyrrole-dicarboxylic acid amide linkers and oligomeric analogs therof as well as related compounds for the treatment of proliferative diseases
    4.
    发明申请
    C8, c8' linked 5-oxo-1,2,3,11a-tetrahydro-5h-pyrrolo[2,1-c][1,4] benzodiazepine dimers with 1h-pyrrole-dicarboxylic acid amide linkers and oligomeric analogs therof as well as related compounds for the treatment of proliferative diseases 审中-公开
    C8，c8'连接的5-氧代-1,2,3,11a-四氢-5H-吡咯并[2,1-c] [1,4]苯并二氮杂二聚体与1h-吡咯二羧酸酰胺接头和低聚类似物 以及用于治疗增殖性疾病的相关化合物

    公开(公告)号：US20070191349A1

    公开(公告)日：2007-08-16

    申请号：US10598470

    申请日：2005-03-01

    申请人： Philip Howard ,  Stephen Gregson ,  Arnaud Tiberghien

    发明人： Philip Howard ,  Stephen Gregson ,  Arnaud Tiberghien

    IPC分类号： A61K31/551 ,  C07D487/14

    CPC分类号： C07D487/04

    摘要： Compounds of formula (I): PBD-A-Y—X—(Het)na-L-(Het)nb-L-(Het)nc-T-(Het′)nd-L-(Het′)ne-L-(Het′)nf—X′—Y′- A′-PBD′ and salts, solvates and chemically protected forms thereof, are disclosed wherein the PBD units have the formulae (PBD) (PBD′) with the bonds at the 8 position on each molecule bond to the A and A′ groups respectively; A is selected from O, S, NH or a single bond, and each Het and Het′ is respectively an amino-heteroarylene-carbonyl group; X and X′ are both either NH or C (═O)-Q—C(═O)— wherein Q is a divalent group such that HY═R; in a second aspectm the invention comprises compounds of the general formula (II): PBD-A-Y—X—(Het)ng-[L-(Het)nh]nj-X′—Y′-A′-PBD′. Wherein: PBD and PBD′ are as defined above, X and X′ are either NH and C(═O) respectively or C(O) and NH respectively; the other substitutents are defined in the claims. Further aspects of the present invention relate to their use in the manufacture of a medicament for the treatment of a proliferative disease.

    摘要翻译： 式（I）的化合物：PBD-AYX-（Het）-Na -L-（Het）N b -L-（Het）nc < -T-（Het'） -L-（Het'） -L-（Het'）Nf -X'-Y 公开了“--A'-PBD'及其盐，溶剂合物和化学保护形式，其中PBD单元具有式（PBD）（PBD'），每个分子上的8位的键与A和A' 分别; A选自O，S，NH或单键，每个Het和Het'分别为氨基 - 亚杂芳基 - 羰基; X和X'都是NH或C（-O）-Q-C（-O） - ，其中Q是二价基团，使得HY-R; 在第二方面，本发明包括通式（II）的化合物：PBD-AYX-（Het）N - [L-（Het）nh] nj -X'-Y'-A'-PBD'。 其中：PBD和PBD'如上所定义，X和X'分别是NH和C（-O）或C（O）和NH; 其他替代物在权利要求中定义。 本发明的其它方面涉及其在制备用于治疗增殖性疾病的药物中的用途。

    11-Hydroxy-5h-pyrrolo[2,1-c][1,4] benzodiazepin-5-one derivatives as key intermediates for the preparation of c2 substituted pyrrolobenzodiazepines
    5.
    发明申请
    11-Hydroxy-5h-pyrrolo[2,1-c][1,4] benzodiazepin-5-one derivatives as key intermediates for the preparation of c2 substituted pyrrolobenzodiazepines 有权
    11-羟基-5H-吡咯并[2,1-c] [1,4]苯并二氮杂-5-酮衍生物作为制备c2取代的吡咯并苯并二氮杂的关键中间体

    公开(公告)号：US20070173497A1

    公开(公告)日：2007-07-26

    申请号：US10598518

    申请日：2005-03-01

    申请人： Philip Howard ,  Stephen Gregson

    发明人： Philip Howard ,  Stephen Gregson

    IPC分类号： A61K31/54

    CPC分类号： C07D487/04 ,  Y02P20/55

    摘要： The present inventors have developed a key intermediate for the production of C2 substituted PBDs, which has a leaving group at the C2 position, a carbamate protecting group at the N10 position and a protected hydroxy group at the C11 position. In a first aspect, the present invention comprises a compound with a the formula (I), wherein: R10 is a carbamate-based nitrogen protecting group; R11 is an oxygen protecting group; and R2 is a labile leaving group. In a further aspect, the present invention comprises a method of synthesising a compound of formula (III), or a solvate thereof, from a compound of formula (I) as defined in the first aspect, R16 is either O—R11, wherein R11 is as defined in the first aspect, or OH, or R10 and R16 together form a double bond between N10 and C11; and R15 is R. The other substituents are defined in the claims. Further aspects of the present invention relate to compounds of formula (III) (including solvates thereof when R10 and R16 form a double bond between N10 and C11, and pharmaceutical salts thereof), pharmaceutical compositions comprising these, and their use in the manufacture of a medicament for the treatment of a proliferative disease.

    摘要翻译： 本发明人已经开发了用于生产在C2位具有离去基团的C2取代的PBD的关键中间体，N10位的氨基甲酸酯保护基和C11位的被保护的羟基。 在第一方面，本发明包括具有式（I）的化合物，其中：R 10是氨基甲酸酯基氮保护基; R 11是氧保护基; R 2是不稳定的离去基团。 在另一方面，本发明包括由第一方面定义的式（I）化合物合成式（III）化合物或其溶剂化物的方法，其中R 16， 是O-R 11，其中R 11如在第一方面中所定义，或OH或R 10和R 16一起形成 N10和C11之间的双键; 并且R 15是R.其它取代基在权利要求中限定。 本发明的其它方面涉及式（III）的化合物（当R 10和R 16在N 10和C 11之间形成双键时，包括其溶剂合物，以及药物盐 ），包含它们的药物组合物及其在制备用于治疗增殖性疾病的药物中的用途。