公开(公告)号：WO2012040133A2

公开(公告)日：2012-03-29

申请号：PCT/US2011052239

申请日：2011-09-20

Applicant: GE HEALTHCARE LTD ,  IMPERIAL COLLEGE ,  MEDI PHYSICS INC ,  ABOAGYE ERIC OFORI ,  ROBINS EDWARD GEORGE ,  SMITH GRAHAM ,  ZHAO YONGJUN

Inventor： ABOAGYE ERIC OFORI ,  ROBINS EDWARD GEORGE ,  SMITH GRAHAM ,  ZHAO YONGJUN

IPC: C07C213/00 ,  C07C213/02 ,  C07C213/06 ,  C07C215/08 ,  C07C217/10

CPC classification number: C07C215/08 ,  C07B2200/05 ,  C07C217/10 ,  C07C309/73

Abstract: Novel radiotracer(s) for Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) imaging of disease states related to altered choline metabolism (e.g., tumor imaging of prostate, breast, brain, esophageal, ovarian, endometrial, lung and prostate cancer - primary tumor, nodal disease or metastases). The present invention also describes intermediate(s), pre-cursor(s), pharmaceutical composition(s), methods of making, and methods of use of the novel radiotracer(s).

Abstract translation: 用于正电子发射断层扫描（PET）或单光子发射计算机断层扫描（SPECT）的新型放射性示踪剂与改变的胆碱代谢相关的疾病状态（例如，前列腺，乳腺，脑，食管，卵巢，子宫内膜，肺和 前列腺癌 - 原发性肿瘤，淋巴结转移或转移）。 本发明还描述了新型放射性示踪剂的中间体，前体，药物组合物，制备方法和使用方法。

公开(公告)号：WO2012040133A3

公开(公告)日：2012-03-29

申请号：PCT/US2011/052239

申请日：2011-09-20

Applicant: GE HEALTHCARE LIMITED ,  IMPERIAL COLLEGE ,  MEDI-PHYSICS, INC. ,  ABOAGYE, Eric, Ofori ,  ROBINS, Edward George ,  SMITH, Graham ,  ZHAO, Yongjun

Inventor： ABOAGYE, Eric, Ofori ,  ROBINS, Edward George ,  SMITH, Graham ,  ZHAO, Yongjun

IPC: C07C213/00 ,  C07C213/02 ,  C07C213/06 ,  C07C215/08 ,  C07C217/10

Abstract: The present invention describes intermediate (s), pre-cursor (s), for the preparation of radialabelled choline analogs to be used as radiotracers for Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) imaging of diseases.

公开(公告)号：WO2012040138A3

公开(公告)日：2012-03-29

申请号：PCT/US2011/052253

申请日：2011-09-20

Applicant: GE HEALTHCARE LIMITED ,  IMPERIAL COLLEGE ,  MEDI-PHYSICS, INC. ,  ABOAGYE, Eric, Ofori ,  ROBINS, Edward, George ,  SMITH, Graham ,  ZHAO, Yongjun ,  LEYTON, Julius ,  TURTON, David ,  WILSON, Anthony ,  BHALLA, Rajiv ,  BRICKUTE, Diana

Inventor： ABOAGYE, Eric, Ofori ,  ROBINS, Edward, George ,  SMITH, Graham ,  ZHAO, Yongjun ,  LEYTON, Julius ,  TURTON, David ,  WILSON, Anthony ,  BHALLA, Rajiv ,  BRICKUTE, Diana

IPC: C07C213/00 ,  C07C213/02 ,  C07C213/06 ,  C07C215/08 ,  C07C217/10

Abstract: Novel radiotracer(s) for Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) imaging of disease states related to altered choline metabolism (e.g., tumor imaging of prostate, breast, brain, esophageal, ovarian, endometrial, lung and prostate cancer - primary tumor, nodal disease or metastases). The present invention also describes intermediate(s), pre-cursor(s), pharmaceutical composition(s), methods of making, and methods of use of the novel radiotracer(s).

公开(公告)号：WO2010026388A1

公开(公告)日：2010-03-11

申请号：PCT/GB2009/002132

申请日：2009-09-04

Applicant: IMPERIAL INNOVATIONS LIMITED ,  HAMMERSMITH IMANET LIMITED ,  ABOAGYE, Eric, Ofori ,  SMITH, Graham ,  NGUYEN, Quang-Dé ,  ARSTAD, Erik ,  GLASER, Matthias, Eberhard

Inventor： ABOAGYE, Eric, Ofori ,  SMITH, Graham ,  NGUYEN, Quang-Dé ,  ARSTAD, Erik ,  GLASER, Matthias, Eberhard

IPC: C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  A61K31/404 ,  A61K51/00 ,  A61P25/28

CPC classification number: C07D403/12 ,  C07D403/14 ,  C07D405/14

Abstract: The present invention provides isatin 5-sulfonamide derivatives, pharmaceutical compositions comprising said derivatives, their use as molecular imaging agents, their use for the diagnosis or treatment of diseases or disorders associated with dysregulation of apoptosis, methods for synthesizing said derivatives, methods for the molecular imaging of caspase activity and apoptosis, and methods of assessing the therapeutic effect of a test substance on caspase activity.

Abstract translation: 本发明提供靛红5-磺酰胺衍生物，包含所述衍生物的药物组合物，其作为分子显像剂的用途，其用于诊断或治疗与凋亡失调相关的疾病或病症的用途，用于合成所述衍生物的方法，所述衍生物的方法 半胱氨酸蛋白酶活性和凋亡的成像以及评估测试物质对胱天蛋白酶活性的治疗效果的方法。

公开(公告)号：WO2012040151A3

公开(公告)日：2012-03-29

申请号：PCT/US2011/052275

申请日：2011-09-20

Applicant: GE HEALTHCARE LIMITED ,  IMPERIAL COLLEGE ,  MEDI-PHYSICS, INC. ,  ABOAGYE, Eric, Ofori ,  ROBINS, Edward George ,  SMITH, Graham ,  LUTHRA, Sajinder

Inventor： ABOAGYE, Eric, Ofori ,  ROBINS, Edward George ,  SMITH, Graham ,  LUTHRA, Sajinder

IPC: C07C213/00 ,  C07C213/02 ,  C07C213/06 ,  C07C215/08 ,  C07C217/10

Abstract: Novel choline - derived radiotracer (s) having an isotopic carbon for Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) imaging of disease states related to altered choline metabolism (e.g., tumor imaging of prostate, breast, brain, esophageal, ovarian, endometrial, lung and prostate cancer - primary tumor, nodal disease or metastases).

公开(公告)号：WO2012040138A2

公开(公告)日：2012-03-29

申请号：PCT/US2011052253

申请日：2011-09-20

Applicant: GE HEALTHCARE LTD ,  IMPERIAL COLLEGE ,  MEDI PHYSICS INC ,  ABOAGYE ERIC OFORI ,  ROBINS EDWARD GEORGE ,  SMITH GRAHAM ,  ZHAO YONGJUN ,  LEYTON JULIUS ,  TURTON DAVID ,  WILSON ANTHONY ,  BHALLA RAJIV ,  BRICKUTE DIANA

Inventor： ABOAGYE ERIC OFORI ,  ROBINS EDWARD GEORGE ,  SMITH GRAHAM ,  ZHAO YONGJUN ,  LEYTON JULIUS ,  TURTON DAVID ,  WILSON ANTHONY ,  BHALLA RAJIV ,  BRICKUTE DIANA

IPC: C07C213/00 ,  C07C213/02 ,  C07C213/06 ,  C07C215/08 ,  C07C217/10

CPC classification number: A61K51/04 ,  C07B59/001 ,  C07B2200/05 ,  C07C213/08 ,  C07C215/08 ,  C07C215/40 ,  Y10T428/13

Abstract: Novel radiotracer(s) for Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) imaging of disease states related to altered choline metabolism (e.g., tumor imaging of prostate, breast, brain, esophageal, ovarian, endometrial, lung and prostate cancer - primary tumor, nodal disease or metastases). The present invention also describes intermediate(s), pre-cursor(s), pharmaceutical composition(s), methods of making, and methods of use of the novel radiotracer(s).

Abstract translation: 用于正电子发射断层扫描（PET）或单光子发射计算机断层扫描（SPECT）的新型放射性示踪剂与改变的胆碱代谢相关的疾病状态（例如，前列腺，乳腺，脑，食管，卵巢，子宫内膜，肺和 前列腺癌 - 原发性肿瘤，淋巴结转移或转移）。 本发明还描述了新型放射性示踪剂的中间体，前体，药物组合物，制备方法和使用方法。

公开(公告)号：WO2010023457A1

公开(公告)日：2010-03-04

申请号：PCT/GB2009/002096

申请日：2009-08-28

Applicant: IMPERIAL INNOVATIONS LIMITED ,  ABOAGYE, Eric, Ofori ,  SMITH, Graham

Inventor： ABOAGYE, Eric, Ofori ,  SMITH, Graham

IPC: A61K31/7072 ,  C07H19/073 ,  C07H19/067

CPC classification number: C07H19/073 ,  C07H5/10 ,  C07H23/00

Abstract: The invention provides compounds that comprise a 4'-thio nucleoside that is a derivative of 4'-thiothymidine or 4'-thio-2'-deoxyuridine comprising a positron or single photon emitting radioisotope or corresponding non-radioactive isotope attached via a triazole link to the N-3 position. Methods for preparing such compounds and uses of the compounds in medicine are also provided.

Abstract translation: 本发明提供了包含4'-硫代胸苷或4'-硫代-2'-脱氧尿苷衍生物的4'-硫代核苷的化合物，其包含通过三唑连接物连接的正电子或单光子发射放射性同位素或相应的非放射性同位素 到N-3位置。 还提供了制备这些化合物的方法和该化合物在医药中的用途。

公开(公告)号：WO2012118909A1

公开(公告)日：2012-09-07

申请号：PCT/US2012/027168

申请日：2012-03-01

Applicant: GE HEALTHCARE LIMITED ,  IMPERIAL COLLEGE ,  MEDI-PHYSICS, INC. ,  LUTHRA, Sajinder Kaur ,  LEYTON, Julius ,  ABOAGYE, Eric, Ofori ,  IDDON, Lisa ,  INDREVOLL, Bard ,  GLASER, Matthias Eberhard ,  CUTHBERTSON, Alan

Inventor： LUTHRA, Sajinder Kaur ,  LEYTON, Julius ,  ABOAGYE, Eric, Ofori ,  IDDON, Lisa ,  INDREVOLL, Bard ,  GLASER, Matthias Eberhard ,  CUTHBERTSON, Alan

IPC: A61K51/08 ,  A61K101/02 ,  C07B59/00

CPC classification number: A61K51/08 ,  A61K51/083 ,  A61K51/088 ,  C07B59/002 ,  C07B59/008

Abstract: Novel radiotracer(s) for Positron Emission Tomography (PET) imaging are described. Novel radiotracer(s) for Positron Emission Tomography (PET) imaging of neuorendocrine tumors are described. Specifically the present invention describes novel [18F]Fluoroethyltriazol-[Tyr3]Octreotate analogs; in particular those that target somatostatin receptors found on the cell surface of gastroenteropancreatic neuorendocrine tumors. The present invention also describes intermediate(s), precursor(s), pharmaceutical composition(s), methods of making, and methods of use of the novel radiotracer(s).

Abstract translation: 描述了用于正电子发射断层扫描（PET）成像的新型放射性示踪剂。 描述了用于神经内分泌肿瘤的正电子发射断层扫描（PET）成像的新型放射性示踪剂。 具体地说，本发明描述了新颖的[18 F]氟乙基三唑 - [Tyr 3] Octreotate类似物; 特别是在胃肠胰腺内分泌肿瘤的细胞表面上发现的生长抑素受体的那些。 本发明还描述了新型放射性示踪剂的中间体，前体，药物组合物，制备方法和使用方法。

公开(公告)号：WO2012040151A2

公开(公告)日：2012-03-29

申请号：PCT/US2011052275

申请日：2011-09-20

Applicant: GE HEALTHCARE LTD ,  IMPERIAL COLLEGE ,  MEDI PHYSICS INC ,  ABOAGYE ERIC OFORI ,  ROBINS EDWARD GEORGE ,  SMITH GRAHAM ,  LUTHRA SAJINDER

Inventor： ABOAGYE ERIC OFORI ,  ROBINS EDWARD GEORGE ,  SMITH GRAHAM ,  LUTHRA SAJINDER

IPC: C07C213/00 ,  C07C213/02 ,  C07C213/06 ,  C07C215/08 ,  C07C217/10

CPC classification number: A61K51/04 ,  C07B59/001 ,  C07B2200/05 ,  C07C215/08 ,  C07C215/40

Abstract: Novel radiotracer(s) for Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) imaging of disease states related to altered choline metabolism (e.g., tumor imaging of prostate, breast, brain, esophageal, ovarian, endometrial, lung and prostate cancer - primary tumor, nodal disease or metastases). The present invention also describes intermediate(s), pre-cursor(s), pharmaceutical composition(s), methods of making, and methods of use of the novel radiotracer(s).

Abstract translation: 用于正电子发射断层扫描（PET）或单光子发射计算机断层扫描（SPECT）的新型放射性示踪剂与改变的胆碱代谢相关的疾病状态（例如，前列腺，乳腺，脑，食管，卵巢，子宫内膜，肺和 前列腺癌 - 原发性肿瘤，淋巴结转移或转移）。 本发明还描述了新型放射性示踪剂的中间体，前体，药物组合物，制备方法和使用方法。

公开(公告)号：WO2008050125A1

公开(公告)日：2008-05-02

申请号：PCT/GB2007/004069

申请日：2007-10-24

Applicant: IMPERIAL INNOVATIONS LTD. ,  ABOAGYE, Eric, Ofori

Inventor： ABOAGYE, Eric, Ofori

IPC: C07C311/44 ,  A61K31/18 ,  A61P35/00

CPC classification number: C07C311/44

Abstract: There is provided a compound of formula (I) wherein R 1a , R 2a , R 3 , X 1 to X 6 , a, b and c have meanings given in the description, which compounds are useful as, or are useful as prodrugs of, inhibitors of HDAC enzyme activity, and thus, in particular, in the treatment of conditions where inhibition of HDAC enzyme activity is required.

Abstract translation: 提供了式（I）的化合物，其中R 1a，R 2a，R 3，X 3，X 1， a，b和c具有说明书中给出的含义，哪些化合物可用作或用作HDAC酶活性抑制剂的前药，因此特别是在 治疗需要抑制HDAC酶活性的条件。