公开(公告)号：US20150017094A1

公开(公告)日：2015-01-15

申请号：US14300630

申请日：2014-06-10

Applicant: Genentech, Inc.

Inventor： Herman Gill ,  Jagath R. Junutula ,  Henry B. Lowman ,  Jan Marik ,  Jeff Tinianow ,  Simon Williams

IPC: A61K51/10

CPC classification number: A61K51/1093 ,  A01K2267/0331 ,  A61K51/1027 ,  A61K51/1051 ,  C07C259/06 ,  C07C323/60 ,  C07C2601/14 ,  C07K16/00 ,  C07K16/32 ,  C07K2317/21 ,  C07K2317/51 ,  C07K2317/52 ,  C07K2317/55 ,  C07K2317/624

Abstract: Antibodies are engineered by replacing one or more amino acids of a parent antibody with non cross-linked, highly reactive cysteine amino acids. Antibody fragments may also be engineered with one or more cysteine amino acids to form cysteine engineered antibody fragments (ThioFab). Methods of design, preparation, screening, and selection of the cysteine engineered antibodies are provided. Cysteine engineered antibodies (Ab) are conjugated with one or more zirconium complex (Z) labels through a linker (L) to form cysteine engineered zirconium-labeled antibody conjugates having Formula I: Ab-(L-Z)p  I where p is 1 to 4. Imaging methods and diagnostic uses for zirconium-radiolabeled, cysteine engineered antibody conjugate compositions are disclosed.

Abstract translation: 通过用非交联的高反应性半胱氨酸氨基酸替代亲本抗体的一个或多个氨基酸来设计抗体。 抗体片段也可以用一个或多个半胱氨酸氨基酸进行工程化以形成半胱氨酸改造的抗体片段（ThioFab）。 提供了设计，制备，筛选和选择半胱氨酸改造的抗体的方法。 半胱氨酸改造的抗体（Ab）通过接头（L）与一个或多个锆络合物（Z）标记物缀合以形成具有式I：Ab-（LZ）p I的半胱氨酸改造的锆标记的抗体缀合物，其中p为1至4 公开了用于放射性标记的半胱氨酸改造的抗体缀合物组合物的成像方法和诊断用途。

公开(公告)号：US08865122B2

公开(公告)日：2014-10-21

申请号：US13855126

申请日：2013-04-02

Applicant: Genentech, Inc.

Inventor： Herman Gill ,  Jan Marik ,  Jeff Tinianow ,  Simon Williams

IPC: A61K51/00 ,  A61M36/14 ,  A61K51/10 ,  A61K51/08 ,  C07K1/13 ,  C07D249/04 ,  C07D403/12 ,  C07K19/00

CPC classification number: A61K51/10 ,  A61K51/08 ,  A61K51/103 ,  C07D249/04 ,  C07D403/12 ,  C07K1/13 ,  C07K19/00

Abstract: A modular platform is provided for rapid preparation of various water-soluble prosthetic groups capable to efficiently introduce 18F into proteins with 18F labelling reagents.

Abstract translation: 提供了一个模块化平台，用于快速制备能够使18F标记试剂有效地将18F引入蛋白质的各种水溶性辅基。

公开(公告)号：US20200297875A1

公开(公告)日：2020-09-24

申请号：US16895352

申请日：2020-06-08

Applicant: Genentech, Inc.

Inventor： Jan Marik ,  Joseph P. Lyssikatos ,  Simon Williams

IPC: A61K51/04 ,  C07B59/00 ,  C07D487/04

Abstract: The present invention relates to deuterated and optionally detectably labeled compounds of formula (I) and formula (V): and salts thereof, wherein R1, R2, A, and X10-X19 have any of the values defined in the specification. Also included are pharmaceutical compositions comprising such compounds and salts, and methods of using such compounds and salts as imaging agents.

公开(公告)号：US10076581B2

公开(公告)日：2018-09-18

申请号：US15006997

申请日：2016-01-26

Applicant: Genentech, Inc.

Inventor： Jan Marik ,  Joseph P. Lyssikatos ,  Simon Williams

IPC: A61K51/04 ,  C07B59/00 ,  C07D487/04

Abstract: The present invention relates to deuterated and optionally detectably labeled compounds of formula (I) and formula (V): and salts thereof, wherein R1, R2, A, and X10-X19 have any of the values defined in the specification. Also included are pharmaceutical compositions comprising such compounds and salts, and methods of using such compounds and salts as imaging agents.

公开(公告)号：US20160250358A1

公开(公告)日：2016-09-01

申请号：US15006997

申请日：2016-01-26

Applicant: Genentech, Inc.

Inventor： Jan Marik ,  Joseph P. Lyssikatos ,  Simon Williams

IPC: A61K51/04 ,  C07D487/04 ,  C07B59/00

CPC classification number: A61K51/0459 ,  C07B59/002 ,  C07B2200/05 ,  C07D487/04

Abstract: The present invention relates to deuterated and optionally detectably labeled compounds of formula (I) and formula (V): and salts thereof, wherein R1, R2, A, and X10-X19 have any of the values defined in the specification. Also included are pharmaceutical compositions comprising such compounds and salts, and methods of using such compounds and salts as imaging agents.

Abstract translation: 本发明涉及氘化和任选可检测地标记的式（I）和式（Ⅴ）化合物及其盐，其中R1，R2，A和X10-X19具有说明书中定义的任何值。 还包括包含这些化合物和盐的药物组合物，以及使用这些化合物和盐作为成像剂的方法。

公开(公告)号：US20140170064A1

公开(公告)日：2014-06-19

申请号：US14132252

申请日：2013-12-18

Applicant: Genentech, Inc.

Inventor： Charles Andrew Boswell ,  Leslie A. Khawli ,  Jan Marik ,  Simon Williams

IPC: A61K49/16 ,  C07K5/02 ,  C07K16/28

CPC classification number: A61K49/16 ,  A61K51/0482 ,  A61K51/08 ,  A61K51/088 ,  A61K51/103 ,  A61K51/1051 ,  A61K51/1093 ,  C07B59/002 ,  C07D207/404 ,  C07D207/452 ,  C07K1/13 ,  C07K5/02 ,  C07K16/28

Abstract: Methods and compositions are provided for labeling proteins with radiohalogen-label reagents. Radiohalogen-labeled proteins may be used for imaging studies, as therapeutics and in diagnostic tests. The [125I] HIP-DOTA label reagent 6 is prepared by an efficient and convenient process.

Abstract translation: 提供了用放射性卤素标记试剂标记蛋白质的方法和组合物。 放射性卤素标记的蛋白质可用作成像研究，作为治疗剂和诊断测试。 [125I] HIP-DOTA标签试剂6通过有效和方便的方法制备。