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    PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF
    31.
    发明申请
    PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF 审中-公开
    。。。。。。。。。。。。

    公开(公告)号：US20130266595A1

    公开(公告)日：2013-10-10

    申请号：US13650277

    申请日：2012-10-12

    Applicant: Genentech, Inc. ,  SPIROGEN DEVELOPMENTS SARL

    Inventor： John A. Flygare ,  Janet L. Gunzner-Toste ,  Thomas Pillow ,  Philip Wilson Howard ,  Luke Masterson

    IPC: A61K47/48

    CPC classification number: A61K47/6803 ,  A61K47/6849 ,  C07D487/04 ,  C07D519/00

    Abstract: A conjugate of formula (A): where Y is selected from a single bond, and a group of formulae A1 or A2: where N shows where the group binds to the N10 of the PBD moiety; RL1 and RL2 are independently selected from H and methyl, or together with the carbon atom to which they are bound form a cyclopropylene group; CBA represents a cell binding agent; Q is independently selected from O, S and NH; R11 is either H, or R or, where Q is O, SO3M, where M is a metal cation.

    Abstract translation: 式（A）的缀合物：其中Y选自单键，并且具有式A1或A2的基团：其中N表示该基团与PBD部分的N10结合的位置; RL1和RL2独立地选自H和甲基，或与它们所结合的碳原子一起形成环亚丙基; CBA代表细胞结合剂; Q独立地选自O，S和NH; R 11是H或R，或其中Q是O，SO 3 M，其中M是金属阳离子。

    Methods for preparing antibody drug conjugates
    34.
    发明授权
    Methods for preparing antibody drug conjugates 有权

    公开(公告)号：US11547762B2

    公开(公告)日：2023-01-10

    申请号：US16354905

    申请日：2019-03-15

    Applicant: Genentech, Inc.

    Inventor： Thomas Pillow ,  Peter Dragovich

    IPC: A61K47/68 ,  C07K16/28 ,  C07K16/22 ,  A61K47/65

    Abstract: The subject matter described herein is directed to methods of preparing certain antibody-drug conjugates (ADCs) wherein the antibody is linked to the drug through a linker, wherein the drug contains a heteroaryl group having a secondary nitrogen, and the linker is attached to the drug via the secondary nitrogen. The resulting conjugates are useful in treating various diseases and conditions.

    Pyrrolobenzodiazepines and conjugates thereof
    36.
    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

    Applicant: MedImmune Limited ,  Genentech, Inc.

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

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

    Abstract: 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).

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