公开(公告)号：US08410312B2

公开(公告)日：2013-04-02

申请号：US12063470

申请日：2006-08-11

Applicant: Anthony Eamon Storey ,  Clare Louise Jones ,  Denis Raymond Christophe Bouvet ,  Nicolas Lasbistes ,  Steven Michael Fairway ,  Lorenzo Williams ,  Alexander Mark Gibson ,  Robert James Nairne ,  Farhad Karimi ,  Bengt Langstrom

Inventor： Anthony Eamon Storey ,  Clare Louise Jones ,  Denis Raymond Christophe Bouvet ,  Nicolas Lasbistes ,  Steven Michael Fairway ,  Lorenzo Williams ,  Alexander Mark Gibson ,  Robert James Nairne ,  Farhad Karimi ,  Bengt Langstrom

IPC: C07C211/46

CPC classification number: A61K51/0453 ,  B01J19/24 ,  B01J2219/24 ,  C07D277/66 ,  Y02P20/55

Abstract: The invention relates to a process for preparation of a compound of formula (I): R1 is selected from C1-6alkyl, C2-6alkenyl, and C2-6alkynyl; which comprises: (i) reaction with fluoride, suitably [18F]fluoride, of a corresponding compound of formula (II): wherein R2 is selected from hydrogen, C1-10alkyl, C1-10haloalkyl, C6-14aryl, C6-14arylalkyl, —(CH2CH2O)q—CH3 wherein q is an integer of from 1 to 10; R1 is as defined for the compound of formula (I); and R3 is a leaving group. Certain novel precursors of formula (II) and radiopharmaceutical kits containing such precursors are also claimed.

Abstract translation: 本发明涉及制备式（I）化合物的方法：R1选自C 1-6烷基，C 2-6烯基和C 2-6炔基; 其包括：（i）与氟化物，适当的[18 F]氟化物反应，相应的式（II）化合物：其中R 2选自氢，C 1-10烷基，C 1-10卤代烷基，C 6-14芳基，C 6-14芳烷基， （CH 2 CH 2 O）q -CH 3，其中q是1至10的整数; R1如式（I）化合物所定义; R3是离去基团。 还要求具有式（II）的某些新型前体和含有这些前体的放射性药物试剂盒。

公开(公告)号：US08226927B2

公开(公告)日：2012-07-24

申请号：US12301648

申请日：2007-05-21

Applicant: Farhad Karimi ,  Bengt Langstrom

Inventor： Farhad Karimi ,  Bengt Langstrom

IPC: A61K51/00

CPC classification number: C07B59/002 ,  C07D471/04 ,  C07D491/04

Abstract: The present invention relates to new 11C/18F-labeled inhibitor compounds for over-expressed GSK-3 prepared from the GMP synthesis method. The present invention provides novel 11C/18F inhibitor compounds for over-expressed GSK-3 that are suitable for use as an in vivo imaging agent. A pharmaceutical comprising the compound and a kit for the preparation of the pharmaceutical are also provided.

Abstract translation: 本发明涉及由GMP合成方法制备的用于过表达的GSK-3的新的11C / 18F标记的抑制剂化合物。 本发明提供适用于体内显像剂的过表达GSK-3的新型11C / 18F抑制剂化合物。 还提供了包含该化合物的药物和用于制备药物的试剂盒。

公开(公告)号：US07928210B2

公开(公告)日：2011-04-19

申请号：US12074538

申请日：2008-03-03

Applicant: Hartmuth C. Kolb ,  Joseph C. Walsh ,  Robert M Yeh ,  Kai Chen ,  Umesh Gangadharmath ,  Brian Duclos ,  Vani P. Mocharla ,  Farhad Karimi ,  Henry C. Padgett ,  Qianwa Liang ,  Tieming Zhao

Inventor： Hartmuth C. Kolb ,  Joseph C. Walsh ,  Robert M Yeh ,  Kai Chen ,  Umesh Gangadharmath ,  Brian Duclos ,  Vani P. Mocharla ,  Farhad Karimi ,  Henry C. Padgett ,  Qianwa Liang ,  Tieming Zhao

IPC: C07H21/02 ,  C07H21/04

CPC classification number: C07H19/073 ,  A61K51/0491 ,  C07H19/06 ,  C07H19/067

Abstract: Disclosed herein are novel radiolabeled nucleosides and methods for detecting cellular proliferation in a mammal, the method comprising administrating an effective amount of a radiolabeled nucleoside; the method comprising: a) administering to the mammal a diagnostically effective amount of the nucleoside to the mammal; b) allowing the nucleoside to distribute into the effective tissue; and c) imaging the tissue, wherein an increase in binding of the compound to tissue compared to a normal control level of binding indicates that the mammal is suffering from a disease involving cellular proliferation.

Abstract translation: 本文公开了新型放射性标记核苷和用于检测哺乳动物细胞增殖的方法，该方法包括施用有效量的放射性标记的核苷; 所述方法包括：a）向哺乳动物施用诊断有效量的核苷; b）允许核苷分布到有效组织中; 和c）对所述组织进行成像，其中与正常对照结合水平相比，所述化合物与组织的结合增加指示所述哺乳动物患有涉及细胞增殖的疾病。

公开(公告)号：US20090142264A1

公开(公告)日：2009-06-04

申请号：US12159016

申请日：2006-12-27

Applicant: Bengt Langstrom ,  Farhad Karimi

Inventor： Bengt Langstrom ,  Farhad Karimi

IPC: A61K51/04 ,  C07C233/00

CPC classification number: C07B59/001

Abstract: The present invention provides novel 18F-labeled phenoxyphenyl N-benzyl alkanamid derivative compounds that are suitable for use as an in vivo imaging agent. A pharmaceutical comprising the compound and a kit for the preparation of the pharmaceutical are also provided. Methods of use and use of claims for novel 18F-labeled phenoxyphenyl N-benzyl alkanamid derivative compounds are provided as well.

Abstract translation: 本发明提供了适合用作体内成像剂的新颖的18F标记的苯氧基苯基N-苄基烷酰胺衍生物。 还提供了包含该化合物的药物和用于制备药物的试剂盒。 也提供了新的18F标记的苯氧基苯基N-苄基烷酰胺衍生物化合物的权利要求书的使用和使用方法。

公开(公告)号：US20090016958A1

公开(公告)日：2009-01-15

申请号：US12074538

申请日：2008-03-03

Applicant: Hartmuth C. Kolb ,  Joseph C. Walsh ,  Robert M. Yeh ,  Kai Chen ,  Umesh Gangadharmath ,  Brian Duclos ,  Vani P. Mocharla ,  Farhad Karimi ,  Henry C. Padgett ,  Qianwa Liang ,  Tieming Zhao

Inventor： Hartmuth C. Kolb ,  Joseph C. Walsh ,  Robert M. Yeh ,  Kai Chen ,  Umesh Gangadharmath ,  Brian Duclos ,  Vani P. Mocharla ,  Farhad Karimi ,  Henry C. Padgett ,  Qianwa Liang ,  Tieming Zhao

IPC: A61K51/04 ,  C07H19/06 ,  G01N33/53

CPC classification number: C07H19/073 ,  A61K51/0491 ,  C07H19/06 ,  C07H19/067

Abstract: Disclosed herein are novel radiolabeled nucleosides and methods for detecting cellular proliferation in a mammal, the method comprising administrating an effective amount of a radiolabeled nucleoside; the method comprising: a) administering to the mammal a diagnostically effective amount of the nucleoside to the mammal; b) allowing the nucleoside to distribute into the effective tissue; and c) imaging the tissue, wherein an increase in binding of the compound to tissue compared to a normal control level of binding indicates that the mammal is suffering from a disease involving cellular proliferation.

Abstract translation: 本文公开了新型放射性标记核苷和用于检测哺乳动物细胞增殖的方法，该方法包括施用有效量的放射性标记的核苷; 所述方法包括：a）向哺乳动物施用诊断有效量的核苷; b）允许核苷分布到有效组织中; 和c）对所述组织进行成像，其中与正常对照结合水平相比，所述化合物与组织的结合增加指示所述哺乳动物患有涉及细胞增殖的疾病。

公开(公告)号：US20080213175A1

公开(公告)日：2008-09-04

申请号：US11901704

申请日：2007-09-17

Applicant: Hartmuth C. Kolb ,  Kai Chen ,  Joseph C. Walsh ,  Umesh Gangadharmath ,  Dhanalakshmi Kasi ,  Bing Wang ,  Brian Duclos ,  Qianwa Liang ,  Henry Clifton Padgett ,  Farhad Karimi

Inventor： Hartmuth C. Kolb ,  Kai Chen ,  Joseph C. Walsh ,  Umesh Gangadharmath ,  Dhanalakshmi Kasi ,  Bing Wang ,  Brian Duclos ,  Qianwa Liang ,  Henry Clifton Padgett ,  Farhad Karimi

IPC: A61K51/08 ,  C07K5/12 ,  A61K38/12 ,  A61K38/14

CPC classification number: C07K7/56

Abstract: The present application is directed to radiolabeled cyclic peptidomimetics, pharmaceutical compositions comprising radiolabeled cyclic peptidomimetics, and methods of using the radiolabeled cyclic peptidomimetics. Such peptidomimetics can be used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT).

Abstract translation: 本申请涉及放射性标记的环肽模拟物，包含放射性标记的环肽模拟物的药物组合物，以及使用放射性标记的环肽模拟物的方法。 这种肽模拟物可用于成像研究，例如正电子发射断层扫描（PET）或单光子发射计算机断层扫描（SPECT）。

公开(公告)号：US08741261B2

公开(公告)日：2014-06-03

申请号：US11086632

申请日：2005-03-22

Applicant: Bengt Langstrom ,  Julien Barletta ,  Hisashi Doi ,  Masaaki Suzuki ,  Ryoji Noyori ,  Yasuyoshi Watanabe ,  Farhad Karimi

Inventor： Bengt Langstrom ,  Julien Barletta ,  Hisashi Doi ,  Masaaki Suzuki ,  Ryoji Noyori ,  Yasuyoshi Watanabe ,  Farhad Karimi

IPC: A61K51/00 ,  A61M36/14 ,  C07D345/00 ,  C07D205/00 ,  C07D213/46

CPC classification number: C07C333/04 ,  A61K51/04 ,  A61K51/0453 ,  A61K51/0455 ,  C07B59/00 ,  C07B2200/05 ,  C07C231/10 ,  C07C269/02 ,  C07C273/1827 ,  C07C333/08 ,  C07D205/08 ,  C07D207/263 ,  C07D207/267 ,  C07D213/64 ,  C07C233/07 ,  C07C271/28 ,  C07C275/28 ,  C07C275/64

Abstract: Methods and reagents for transition metal-promoted carbonylation via isocyanate using carbon-isotope labeled carbon monoxide are provided. The resultant carbon-isotope labeled compounds are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). Associated kits for PET studies are also provided.

Abstract translation: 提供了使用碳同位素标记的一氧化碳通过异氰酸酯过渡金属促进羰基化的方法和试剂。 所得碳同位素标记的化合物可用作放射性药物，特别用于正电子发射断层扫描（PET）。 还提供了用于PET研究的相关工具包。

公开(公告)号：US20110002850A1

公开(公告)日：2011-01-06

申请号：US12836926

申请日：2010-07-15

Applicant: Thomas Lee Collier ,  Brian A. Duclos ,  Umesh B. Gangadharmath ,  Zhiyong Gao ,  Farhad Karimi ,  Dhanalakshmi Kasi ,  Hartmuth C. Kolb ,  Qianwa Liang ,  Henry Clifton Padgett ,  Joseph C. Walsh ,  Tieming Zhao

Inventor： Thomas Lee Collier ,  Brian A. Duclos ,  Umesh B. Gangadharmath ,  Zhiyong Gao ,  Farhad Karimi ,  Dhanalakshmi Kasi ,  Hartmuth C. Kolb ,  Qianwa Liang ,  Henry Clifton Padgett ,  Joseph C. Walsh ,  Tieming Zhao

IPC: A61K51/04 ,  A61P35/00 ,  A61K31/4178 ,  C07D403/06

CPC classification number: C07D403/06 ,  C07B59/002 ,  C07D403/12

Abstract: The present invention relates to novel radioactively labeled bioreducible tracers of Formula I useful for detecting hypoxic tumors or ischemic tissue in vivo. In one embodiment, the tracers consist of a 2-nitroimidazole moiety, a triazole, metabolically stable linker with pharmacokinetics enhancing substituents, and a radioisotope. The preferred in vivo imaging modality is positron emission tomography.

Abstract translation: 本发明涉及用于体内检测缺氧性肿瘤或缺血组织的式I的新型放射性标记的生物可降解示踪剂。 在一个实施方案中，示踪剂由2-硝基咪唑部分，三唑，具有药代动力学增强取代基的代谢稳定接头和放射性同位素组成。 优选的体内成像模式是正电子发射断层摄影。

公开(公告)号：US20090123372A1

公开(公告)日：2009-05-14

申请号：US12099135

申请日：2008-04-07

Applicant: Hartmuth C. Kolb ,  Joseph C. Walsh ,  Dhanalakshmi Kasi ,  Vani P. Mocharla ,  Bing Wang ,  Umesh B. Gangadharmath ,  Brian A. Duclos ,  Kai Chen ,  Wei Zhang ,  Gang Chen ,  Henry Clifton Padgett ,  Farhad Karimi ,  Peter J. H. Scott ,  Zhiyong Gao ,  Qianwa Liang ,  Thomas Lee Collier ,  Tieming Zhao ,  Chunfang Xia

Inventor： Hartmuth C. Kolb ,  Joseph C. Walsh ,  Dhanalakshmi Kasi ,  Vani P. Mocharla ,  Bing Wang ,  Umesh B. Gangadharmath ,  Brian A. Duclos ,  Kai Chen ,  Wei Zhang ,  Gang Chen ,  Henry Clifton Padgett ,  Farhad Karimi ,  Peter J. H. Scott ,  Zhiyong Gao ,  Qianwa Liang ,  Thomas Lee Collier ,  Tieming Zhao ,  Chunfang Xia

IPC: C07D249/04 ,  C07D413/12 ,  A61K49/04 ,  A61K51/04

CPC classification number: C07D417/04 ,  C07D249/04 ,  C07D249/06 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14 ,  C12Q1/485 ,  G01N2500/04 ,  G01N2500/10

Abstract: The present application discloses methods for identifying inhibitors with high binding-affinity for the carbonic anhydrase-IX (CA-IX) enzyme using click chemistry and uses the candidates thereof as positron emission tomography (PET) imaging agents.

Abstract translation: 本申请公开了使用点击化学法鉴定对碳酸酐酶IX（CA-IX）酶具有高结合亲和力的抑制剂的方法，并将其候选用作正电子发射断层摄影（PET）成像剂。

公开(公告)号：US08506932B2

公开(公告)日：2013-08-13

申请号：US12094172

申请日：2006-11-20

Applicant: Erik Arstad ,  Ian Wilson ,  Sajinder Kaur Luthra ,  Frank Brady ,  Bengt Langstrom ,  Farhad Karimi ,  Edward George Robins ,  Bo Shan

Inventor： Erik Arstad ,  Ian Wilson ,  Sajinder Kaur Luthra ,  Frank Brady ,  Bengt Langstrom ,  Farhad Karimi ,  Edward George Robins ,  Bo Shan

IPC: A61K49/00

CPC classification number: C07D209/80 ,  C07D495/04

Abstract: The present invention provides novel tetracyclic indole compounds of Formula (I) either as in vivo imaging agents or as therapeutic agents. A method for the preparation of the in vivo imaging agent compound is also provided by the invention, as well as a precursor for use in said method. Pharmaceutical compositions comprising the compounds of the invention are additionally provided. Where the pharmaceutical composition comprises a compound suitable for in vivo imaging, a kit is provided for the preparation of the pharmaceutical composition. In a further aspect, use of the compound for in vivo imaging or treatment of conditions associated with PBR is provided.

Abstract translation: 本发明提供作为体内显像剂或治疗剂的式（I）的新型四环吲哚化合物。 本发明还提供了制备体内显像剂化合物的方法，以及用于所述方法的前体。 另外提供包含本发明化合物的药物组合物。 当药物组合物包含适于体内成像的化合物时，提供用于制备药物组合物的试剂盒。 在另一方面，提供了该化合物用于体内成像或治疗与PBR相关的病症的用途。