公开(公告)号：US20110190492A1

公开(公告)日：2011-08-04

申请号：US13086710

申请日：2011-04-14

Applicant: Yukitsuka KUDO ,  Hiroyuki ARAI ,  Nobuyuki OKAMURA ,  Masahiro MARUYAMA ,  Syozo FURUMOTO ,  Katsumi DOH-URA

Inventor： Yukitsuka KUDO ,  Hiroyuki ARAI ,  Nobuyuki OKAMURA ,  Masahiro MARUYAMA ,  Syozo FURUMOTO ,  Katsumi DOH-URA

IPC: C07D417/14

CPC classification number: C07D417/06 ,  A61K51/04 ,  A61K51/0431 ,  A61K51/0446 ,  A61K51/0453 ,  A61K51/0455 ,  A61K51/0459 ,  A61K51/0463 ,  A61K51/0465 ,  A61K51/0468

Abstract: The invention provides a probe compound useful for early diagnosis of conformation disease, a composition and a kit comprising it for diagnosis for conformation disease, and a medical composition for treatment and/or prevention of conformation disease.

Abstract translation: 本发明提供了可用于构象疾病早期诊断的探针化合物，组合物和包含其用于构象疾病诊断的试剂盒，以及用于治疗和/或预防构象疾病的医药组合物。

公开(公告)号：US20100278733A1

公开(公告)日：2010-11-04

申请号：US12301805

申请日：2007-05-22

Applicant: Morio Nakayama ,  Mamoru Haratake ,  Masahiro Ono

Inventor： Morio Nakayama ,  Mamoru Haratake ,  Masahiro Ono

IPC: A61K49/00 ,  A61K51/00 ,  A61P43/00 ,  C07D213/61 ,  C07D333/22 ,  C07C211/00 ,  C07D277/30 ,  C07D233/54

CPC classification number: C07D213/61 ,  A61K51/04 ,  A61K51/0431 ,  A61K51/0455 ,  C07D213/60 ,  C07D233/64 ,  C07D277/24 ,  C07D307/42 ,  C07D333/28 ,  C07D333/36 ,  C07D409/06

Abstract: There is provided a composition comprising a compound represented by general formula (I), wherein Rl represents a 5-iodothiophen-2-yl group or the like, and R2 represents a 4-dimethylaminophenyl group or the like. This composition is useful for diagnosis of an amyloid-related disease such as Alzheimer's disease because the compound has high binding specificity to amyloid β protein, high permeability through the blood-brain barrier, and a property of being rapidly eliminated from sites other than senile plaques in the brain.

Abstract translation: 提供了包含由通式（I）表示的化合物的组合物，其中R1表示5-碘代噻吩-2-基等，R2表示4-二甲基氨基苯基等。 该组合物可用于淀粉样蛋白相关疾病如阿尔茨海默病的诊断，因为该化合物对淀粉样蛋白和bgr具有高结合特异性; 蛋白质，通过血脑屏障的高渗透性，以及从脑中除老年斑之外的部位迅速消除的性质。

公开(公告)号：US08216547B2

公开(公告)日：2012-07-10

申请号：US12500334

申请日：2009-07-09

Applicant: Paul D. Acton ,  Dennis J. Hlasta ,  Jay M. Matthews ,  James J. McNally

Inventor： Paul D. Acton ,  Dennis J. Hlasta ,  Jay M. Matthews ,  James J. McNally

IPC: A61K51/00 ,  A61M36/14

CPC classification number: A61K51/0431

Abstract: The present invention is directed to radiolabelled ligands, useful for the labeling and imaging of TRP M8 (transient receptor potential M8 channel) functionality. The present invention is further directed to pharmaceutical compositions comprising the radiolabelled ligands and methods for the preparation of the radiolabelled ligands.

Abstract translation: 本发明涉及用于标记和成像TRP M8（瞬时受体电位M8通道）功能的放射性标记的配体。 本发明还涉及包含放射性标记的配体的药物组合物和用于制备放射性标记的配体的方法。

公开(公告)号：US20080299041A1

公开(公告)日：2008-12-04

申请号：US12128005

申请日：2008-05-28

Applicant: Jae Min JEONG ,  Dong Soo LEE ,  June-Key CHUNG ,  Myung Chul LEE

Inventor： Jae Min JEONG ,  Dong Soo LEE ,  June-Key CHUNG ,  Myung Chul LEE

IPC: A61K51/04 ,  C07D277/62 ,  C07D263/54 ,  A61P25/28 ,  C07D333/52 ,  C07D307/87

CPC classification number: C07D307/87 ,  A61K51/0419 ,  A61K51/0431 ,  A61K51/0453 ,  C07D263/57 ,  C07D277/66 ,  C07D333/72

Abstract: The invention is directed to heterocyclic indene derivatives useful for β-amyloid plaque imaging, their radiolabeled compounds and their preparation methods. The compounds of the invention are easily labeled with radioisotopes and have high affinities to β-amyloid depositions, thus they facilitate diagnosis of Alzheimer's disease by imaging the distribution of β-amyloid depositions.

Abstract translation: 本发明涉及可用于β-淀粉样蛋白斑块成像的杂环茚衍生物，其放射性标记的化合物及其制备方法。 本发明的化合物容易用放射性同位素标记，并且对β-淀粉样蛋白沉积具有高亲和力，因此它们通过成像β-淀粉样蛋白沉积的分布来促进阿尔茨海默病的诊断。

公开(公告)号：US20140275539A1

公开(公告)日：2014-09-18

申请号：US14211975

申请日：2014-03-14

Applicant: Ground Fluor Pharmaceuticals, Inc.

Inventor： Stephen G. DiMagno

IPC: A61K51/04

CPC classification number: A61K51/0402 ,  A61K51/04 ,  A61K51/0406 ,  A61K51/0419 ,  A61K51/0431 ,  A61K51/0446 ,  A61K51/0453 ,  A61K51/0455 ,  A61K51/0459

Abstract: Provided herein are stabilized radioiodinated and astatinated compounds, and to methods for their preparation.

Abstract translation: 本文提供了稳定的放射性碘化和消食化合物，以及其制备方法。

公开(公告)号：US20130084245A1

公开(公告)日：2013-04-04

申请号：US13580866

申请日：2011-02-25

Applicant: Ronald Black ,  Michael Grundman

Inventor： Ronald Black ,  Michael Grundman

IPC: A61K51/04

CPC classification number: A61K51/04 ,  A61K51/041 ,  A61K51/0431 ,  A61K51/0453 ,  A61K51/0455

Abstract: The present invention provides methods of monitoring Aβ-directed immunotherapy. The methods involve administering a PET ligand that binds to amyloid deposits and detecting the PET ligand in the brain to provide an indication of the level and/or distribution of amyloid deposits. Surprisingly, the data in the present application show that a statistically significant reduction in amyloid deposits occurs early and consistently among patients following initiation of treatment before statistically significant effects of most if not all other markers are detectable. In consequence, the present methods allow early detection of whether a patient is responding to the Aβ-directed immunotherapy and if necessary adjustment of the immunotherapy regime.

Abstract translation: 本发明提供了监测免疫治疗的方法。 所述方法包括施用结合淀粉样沉积物的PET配体并检测脑中的PET配体以提供淀粉样沉积物的水平和/或分布的指示。 令人惊讶的是，本申请中的数据显示，在大多数（如果不是全部）其他标记物可检测到的统计学显着影响之前，淀粉样蛋白沉积物的统计学显着降低在治疗开始后的患者中早期和始终发生。 因此，本方法允许早期检测患者是否对A＆bgr指导的免疫治疗作出反应，如果需要调整免疫治疗方案。

公开(公告)号：US20080292547A1

公开(公告)日：2008-11-27

申请号：US12096387

申请日：2006-12-07

Applicant: Helge Tolleshaug ,  Ben Newton ,  Anna Rydbeck ,  Salah Chettibi ,  Morten Eriksen

Inventor： Helge Tolleshaug ,  Ben Newton ,  Anna Rydbeck ,  Salah Chettibi ,  Morten Eriksen

IPC: A61K49/00 ,  A61K51/04

CPC classification number: A61K49/0002 ,  A61K51/0431 ,  A61K51/0459

Abstract: The present invention provides a novel imaging agent suitable for the non-invasive visualization of fibrosis. A method for the preparation of the imaging agent is also provided by the invention, as well as a precursor for use in said method. Also provided is a pharmaceutical composition comprising the imaging agent and a kit for the preparation of the pharmaceutical. In a further aspect, use of the imaging agent for in vivo imaging and in the preparation of a medicament for the diagnosis of a condition in which LOX is upregulated is provided.

Abstract translation: 本发明提供了适用于纤维化的非侵入性可视化的新型成像剂。 本发明还提供了用于制备显影剂的方法，以及用于所述方法的前体。 还提供了包含成像剂和用于制备药物的试剂盒的药物组合物。 在另一方面，提供了用于体内成像和用于诊断LOX上调的病症的药物的成像剂的用途。

公开(公告)号：US5135735A

公开(公告)日：1992-08-04

申请号：US573007

申请日：1990-12-14

Applicant: Jurgen Schrader

Inventor： Jurgen Schrader

IPC: G01N33/60 ,  A61K51/00 ,  A61K51/04

CPC classification number: A61K51/0406 ,  A61K51/0431 ,  A61K2123/00

Abstract: The invention relates to a method of localizing and quantifying regional energy metabolism, in particular regional ischemia, in a warm-blooded living being, comprising administering to said being a diagonstically effective quantity of a radiolabelled L-homocysteine or a radiolabelled functional derivative thereof. The invention further relates to a pharmaceutical composition to be used for performing the above method.

Abstract translation: PCT No.PCT / NL89 / 00030 Sec。 371 1990年12月14日第 102（e）1990年12月14日的PCT日期1989年4月27日提交PCT本发明涉及一种在温血生活中定位和量化区域能量代谢特别是区域缺血的方法，包括： 一种对角线有效量的放射性标记的L-高半胱氨酸或其放射性标记的功能性衍生物。 本发明还涉及用于进行上述方法的药物组合物。

公开(公告)号：US20120251448A1

公开(公告)日：2012-10-04

申请号：US13411403

申请日：2012-03-02

Applicant: Franz F. Hefti ,  Geoffrey Golding ,  Ximin Li ,  Seok-Rye Choi ,  Luke Esposito ,  Marisa-Claire Yadon ,  Joel Cummings ,  F. Michael Hudson ,  Thomas Lake ,  Alan D. Snow

Inventor： Franz F. Hefti ,  Geoffrey Golding ,  Ximin Li ,  Seok-Rye Choi ,  Luke Esposito ,  Marisa-Claire Yadon ,  Joel Cummings ,  F. Michael Hudson ,  Thomas Lake ,  Alan D. Snow

IPC: A61K51/04 ,  A61K49/00

CPC classification number: A61K51/0431 ,  A61K51/0453

Abstract: Provided are the use of the disclosed compounds as imaging agents and methods for in vivo imaging and detection of pathological characteristics unique to synuclein diseases, such as Parkinson's disease.

Abstract translation: 提供了所公开的化合物作为成像剂的用途和用于体内成像和检测突触核蛋白疾病如帕金森病特有的病理特征的方法。

公开(公告)号：US20100015053A1

公开(公告)日：2010-01-21

申请号：US12500334

申请日：2009-07-09

Applicant: Paul D. Acton ,  Dennis J. Hlasta ,  Jay M. Matthews ,  James J. McNally

Inventor： Paul D. Acton ,  Dennis J. Hlasta ,  Jay M. Matthews ,  James J. McNally

IPC: A61K51/04 ,  C07D333/66 ,  C12Q1/02 ,  C07C29/14

CPC classification number: A61K51/0431

Abstract: The present invention is directed to radiolabelled ligands, useful for the labeling and imaging of TRP M8 (transient receptor potential M8 channel) functionality. The present invention is further directed to pharmaceutical compositions comprising the radiolabelled ligands and methods for the preparation of the radiolabelled ligands.

Abstract translation: 本发明涉及用于标记和成像TRP M8（瞬时受体电位M8通道）功能的放射性标记的配体。 本发明还涉及包含放射性标记的配体的药物组合物和用于制备放射性标记的配体的方法。