公开(公告)号：US20190201561A1

公开(公告)日：2019-07-04

申请号：US16050453

申请日：2018-07-31

Applicant: Genentech, Inc.

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

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

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：US08771966B2

公开(公告)日：2014-07-08

申请号：US13692888

申请日：2012-12-03

Applicant: Genentech, Inc.

Inventor： Mark Dennis ,  Jan Marik ,  Paul Polakis ,  Bonnee Rubinfeld ,  Simon Williams

IPC: G01N33/53

CPC classification number: C07K16/40 ,  A61K47/6811 ,  A61K47/6871 ,  A61K51/1072 ,  A61K51/1075 ,  A61K51/1093 ,  A61K51/1096 ,  A61K2039/505 ,  C07B59/008 ,  C07B2200/05 ,  C07K16/3069 ,  C07K2317/24 ,  C07K2317/565 ,  C07K2317/92 ,  G01N33/534 ,  G01N33/57492 ,  G01N33/60 ,  G01N33/6893

Abstract: Anti-STEAP-1 antibodies and immunoconjugates thereof are provided. Methods of using anti-STEAP-1 antibodies and immunoconjugates thereof are provided. Methods of detecting or determining the presence of STEAP-1 proteins are provided.

Abstract translation: 提供抗STEAP-1抗体及其免疫偶联物。 提供了使用抗STEAP-1抗体及其免疫偶联物的方法。 提供检测或确定STEAP-1蛋白存在的方法。

公开(公告)号：US10675367B2

公开(公告)日：2020-06-09

申请号：US16050453

申请日：2018-07-31

Applicant: Genentech, Inc.

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

IPC: A61K51/04 ,  C07B59/00 ,  C07D487/04 ,  C07D513/04

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：US20160002121A1

公开(公告)日：2016-01-07

申请号：US14814734

申请日：2015-07-31

Applicant: Genentech, Inc.

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

IPC: C07B59/00 ,  C07D207/404 ,  C07D207/452

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。

公开(公告)号：US20130216475A1

公开(公告)日：2013-08-22

申请号：US13855126

申请日：2013-04-02

Applicant: Genentech, Inc.

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

IPC: A61K51/10 ,  A61K51/08 ,  C07K19/00 ,  C07D403/12 ,  C07D249/04

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：US20130156700A1

公开(公告)日：2013-06-20

申请号：US13687441

申请日：2012-11-28

Applicant: Genentech, Inc.

Inventor： Jan Marik ,  Zachary Kevin Sweeney ,  Bryan K. Chan ,  Anthony Estrada

IPC: C07D403/12 ,  C07D239/48

CPC classification number: C07D403/12 ,  A61K51/0453 ,  A61K51/0455 ,  A61K51/0459 ,  C07D239/48

Abstract: A method for positron emission tomography (PET) imaging of LRRK2 in tissue of a subject, the method comprising: administering a compound of formula I, formula II or formula III, or a pharmaceutically acceptable salt thereof to the subject, wherein the compound includes at least one C11 or F18 label thereon; allowing the compound to penetrate into the tissue of the subject; and collecting a PET image of the CNS or brain tissue of the subject

Abstract translation: 一种用于受试者组织中LRRK2的正电子发射断层摄影（PET）成像的方法，所述方法包括：向受试者施用式I，式II或式III化合物或其药学上可接受的盐，其中所述化合物包括 在其上至少有一个C11或F18标签; 允许化合物渗透到受试者的组织中; 并收集受试者的CNS或脑组织的PET图像

公开(公告)号：US11504440B2

公开(公告)日：2022-11-22

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：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：US12214058B2

公开(公告)日：2025-02-04

申请号：US18056856

申请日：2022-11-18

Applicant: Genentech, Inc.

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