公开(公告)号：US20180028695A1

公开(公告)日：2018-02-01

申请号：US15219745

申请日：2016-07-26

Applicant: LABORATOIRES CYCLOPHARMA

Inventor： Gilles VIOT

IPC: A61K51/04 ,  C07J1/00

CPC classification number: A61K51/0493 ,  C07B59/007 ,  C07B63/00 ,  C07B2200/05 ,  C07J1/007 ,  C07J71/0089

Abstract: The present invention relates to a method for the synthesis of a radioactive agent composition comprising at least a purification step carried out in the presence of an antioxidant, to the composition obtained by this method comprising radioactive agent and excipient, and to the method for preventing radiolysis of radioactive agent composition comprising the synthesis of said radioactive agent according to the method of the invention.

公开(公告)号：US09550704B2

公开(公告)日：2017-01-24

申请号：US14401790

申请日：2013-05-24

Applicant: Futurechem Co., LTD.

Inventor： Dae Yoon Chi ,  Byoung Se Lee ,  Jae Hak Lee ,  So Young Chu ,  Woon Jung Jung

IPC: A61K51/04 ,  A61K51/08 ,  C07B59/00 ,  C07H5/02 ,  C07H19/06 ,  C07D451/02 ,  C07J1/00 ,  C07D233/91 ,  C07D417/04 ,  C07C213/08

CPC classification number: C07B59/007 ,  A61K51/0453 ,  A61K51/0455 ,  A61K51/0491 ,  A61K51/0493 ,  A61K51/082 ,  C07B59/00 ,  C07B59/001 ,  C07B59/002 ,  C07B59/004 ,  C07B59/005 ,  C07B2200/05 ,  C07C213/08 ,  C07D233/91 ,  C07D417/04 ,  C07D451/02 ,  C07H5/02 ,  C07H19/06 ,  C07J1/00 ,  C07J1/007 ,  C07J71/0089

Abstract: The present invention relates to a method for synthesizing a radiopharmaceutical using a cartridge, which makes it possible to carry out several steps of reaction required for synthesizing a radiopharmaceutical in the cartridge filled with a polymer. A method for synthesizing a radiopharmaceutical according to the present invention enables each step's reaction to be carried out with the solution confined in the cartridge so as not to flow out, thus being simplified compared to the conventional methods for synthesizing radiopharmaceuticals, and expediting the synthesis thereof.

Abstract translation: 本发明涉及一种使用药筒合成放射性药物的方法，其使得可以在填充有聚合物的药筒中进行合成放射性药物所需的几个反应步骤。 根据本发明的合成放射性药物的方法能够使限制在药筒中的溶液进行每个步骤的反应，从而不会流出，因此与用于合成放射性药物的常规方法相比，简化了其加速合成 。

公开(公告)号：US20150258223A1

公开(公告)日：2015-09-17

申请号：US14571524

申请日：2014-12-16

Applicant: Algeta ASA

Inventor： Roy H. LARSEN ,  Gjermund HENRIKSON

IPC: A61K51/10 ,  A61K51/04 ,  C07B59/00 ,  C07K16/30

CPC classification number: A61K51/1045 ,  A61K51/0459 ,  A61K51/0493 ,  A61K51/1093 ,  C07B59/008 ,  C07K16/30 ,  C07K2317/21 ,  C07K2317/40 ,  C07K2317/76

Abstract: The present invention relates to a receptor binding conjugate which consists of an antibody, a radionuclide and folate or a folate derivative, wherein or not the conjugate possesses dual binding ability. The present invention also relates to a method and a kit to prepare, as well as a method to use, such conjugates. Furthermore, the use of a conjugate according to the present invention to prepare a pharmaceutical solution is disclosed.

Abstract translation: 本发明涉及由抗体，放射性核素和叶酸或叶酸衍生物组成的受体结合结合物，其中所述缀合物具有双重结合能力。 本发明还涉及制备这种缀合物的方法和试剂盒以及使用这种共轭物的方法。 此外，公开了根据本发明的缀合物用于制备药物溶液的用途。

公开(公告)号：US20120269725A1

公开(公告)日：2012-10-25

申请号：US13512966

申请日：2010-12-23

Applicant: Janine Baranowska-Kortylewicz ,  Zbigniew P. Kortylewicz

Inventor： Janine Baranowska-Kortylewicz ,  Zbigniew P. Kortylewicz

IPC: A61K51/04 ,  A61P35/00 ,  A61K31/7072 ,  A61K49/10 ,  C07J43/00

CPC classification number: A61K51/0491 ,  A61K31/7072 ,  A61K47/554 ,  A61K49/10 ,  A61K51/0493 ,  A61K51/0497

Abstract: Method of using androgen receptor and/or butyrylcholinesterase targeted radiolabeled compounds, e.g., cycloSalingenyl pyrimidine nucleoside monophosphates, for the treatment and diagnosis of cancer.

Abstract translation: 使用雄激素受体和/或丁酰胆碱酯酶靶向放射性标记化合物的方法，例如环辛烯基嘧啶核苷单磷酸酯，用于治疗和诊断癌症。

公开(公告)号：US08084016B2

公开(公告)日：2011-12-27

申请号：US12173784

申请日：2008-07-15

Applicant: Marc K. Hellerstein

Inventor： Marc K. Hellerstein

IPC: C12Q1/00 ,  A61K49/00 ,  A61K33/00

CPC classification number: A61K51/0493 ,  G01N33/5091 ,  G01N33/58 ,  G01N33/60 ,  G01N33/6842 ,  G01N33/6848 ,  G01N2800/52 ,  Y10T436/24 ,  Y10T436/25

Abstract: Methods of determining rate of biosynthesis or breakdown of biological molecules from metabolic derivatives and catabolic products are disclosed herein. In particular, methods of measuring the rates of biosynthesis and breakdown of biological molecules inaccessible or not easily accessible to direct sampling by sampling metabolic derivatives and catabolic products in accessible biological samples are disclosed herein.

Abstract translation: 本文公开了鉴定代谢衍生物和分解代谢产物的生物合成或分解生物分子的速率的方法。 特别地，本文公开了测量生物分子的速率的方法，其不可访问或不易于通过在可及的生物样品中取样代谢衍生物和分解代谢产物直接取样。

公开(公告)号：US07048907B2

公开(公告)日：2006-05-23

申请号：US10060652

申请日：2002-01-30

Applicant: Ernest V. Groman ,  Christopher P. Reinhardt

Inventor： Ernest V. Groman ,  Christopher P. Reinhardt

IPC: A61K49/00

CPC classification number: A61K51/0493 ,  A61K33/24 ,  A61K41/009 ,  A61K47/60 ,  A61K51/0497 ,  A61K51/065 ,  A61K51/1255

Abstract: Stable isotope labeling and neutron activation to measure biological functions are provided, as are the use and method of adding a chemical monitor to correct for neutron flux to sample vials prior to the addition of sample is presented, and the use of stable isotopes as a chemical bar code for vials and other items. Methods are provided also for measuring glomerular filtration rate and glomerular sieving function in a subject, and for measuring other physiological functions.

公开(公告)号：US20050069495A1

公开(公告)日：2005-03-31

申请号：US10671376

申请日：2003-09-25

Applicant: Janina Baranowska-Kortylewicz ,  Zbigniew Kortylewicz

Inventor： Janina Baranowska-Kortylewicz ,  Zbigniew Kortylewicz

IPC: A61K51/04 ,  C07H19/048 ,  A61K51/00

CPC classification number: A61K51/0493 ,  A61K51/0491 ,  C07H19/048

Abstract: Radiolabeled conjugates are disclosed which have a component that is effective to target tumor cells, which cells selectively take up and degrade the conjugate, thereby delivering to the tumor cell nucleus a radioisotope capable of being incorporated into the nuclear material, so as to produce a cytotoxic effect and/or to render the cell detectable by radioimaging.

Abstract translation: 公开了放射性标记的缀合物，其具有有效靶向肿瘤细胞的组分，该组分选择性地吸收和降解缀合物，从而将能够并入核材料的放射性同位素递送至肿瘤细胞核，从而产生细胞毒性 效应和/或通过放射成像使细胞可检测。

公开(公告)号：US4541957A

公开(公告)日：1985-09-17

申请号：US529908

申请日：1983-09-07

Applicant: Iwao Nakatsuka ,  William Eckelman ,  Waclaw J. Rzeszotarski

Inventor： Iwao Nakatsuka ,  William Eckelman ,  Waclaw J. Rzeszotarski

IPC: A61K51/00 ,  A61K51/04 ,  C07J1/00 ,  C07J7/00 ,  C07J13/00 ,  C07J51/00 ,  A61K49/00 ,  A61K43/00 ,  C07J3/00

CPC classification number: A61K51/0493 ,  C07J1/0081 ,  C07J51/00 ,  A61K2123/00

Abstract: 17.alpha.-[(E)-2-Iodovinyl]-estra-1,3,5(10)-triene-3,17.beta.-diol wherein the iodine atom is radioactive can be produced from (E)-[3-acyloxy-17.beta.-hydroxyestra-1,3,5(10)-triene-17.alpha.-yl]vinyl dihydroxyborane in an excellent yield by iodinating the same and hydrolyzing the resulting 3-acyloxy-17.alpha.-[(E)-2-iodovinyl]-estra-1,3,5(10)-triene-17.beta.-ol.

Abstract translation: 17α-[（E）-2-碘乙烯基] - 雌-1,3,5（10） - 三烯-3,17β-二醇，其中碘原子是放射性的，可由（E） - [3-酰氧基 -17β-羟基雌-1,3,5（10） - 三烯-17α-基]乙烯基二羟基硼烷以优异的产率进行碘化，水解所得3-酰氧基-17α-[（E）-2- 碘乙烯基] - 雌-1,3,5（10） - 三烯-17β-醇。

公开(公告)号：US4430321A

公开(公告)日：1984-02-07

申请号：US339265

申请日：1982-01-15

Applicant: Richard J. Flanagan ,  Leonard I. Wiebe

Inventor： Richard J. Flanagan ,  Leonard I. Wiebe

IPC: A61K51/04 ,  C07J9/00 ,  A61K49/02 ,  A61K43/00

CPC classification number: A61K51/0493 ,  C07J9/00 ,  A61K2123/00

Abstract: Novel 6-bromo derivatives of cholesterol have the formula ##STR1## Such compounds are prepared from the known 6-iodocholesterol by treatment with cuprous bromide.These compounds, labelled with radioisotopes of Br-82 or Br-77, are localized in the adrenal, mammary and ovary tissue of female mammals and in the adrenal or prostate tissue of males when administered to such individuals. This provides a method for imaging adrenal, ovary or prostate tissue which is superior to use of the prior art 6-iodo-cholesterol.

Abstract translation: 胆固醇的新型6-溴衍生物具有下式：通过用溴化亚铜处理，已知的6-碘胆固醇制备这些化合物。这些用Br-82或Br-77的放射性同位素标记的化合物定位于肾上腺， 雌性哺乳动物的乳腺和卵巢组织以及雄性哺乳动物的肾上腺或前列腺组织。 这提供了用于成像肾上腺，卵巢或前列腺组织的方法，其优于使用现有技术的6-碘胆固醇。

公开(公告)号：US4202876A

公开(公告)日：1980-05-13

申请号：US866853

申请日：1978-01-04

Applicant: Reginald Monks ,  Anthony L. M. Riley

Inventor： Reginald Monks ,  Anthony L. M. Riley

IPC: A61K51/00 ,  A61K51/04 ,  C07J7/00 ,  C07J9/00 ,  C07J51/00 ,  A61K29/00 ,  A61K43/00

CPC classification number: A61K51/0493 ,  C07J51/00 ,  C07J7/0005 ,  C07J9/00 ,  C07J9/005 ,  A61K2123/00

Abstract: Body function of a mammal is investigated using a .gamma.-emitting .sup.75 Se or .sup.123m Te labelled derivative of a bile acid or bile salt. Thus bowel function may be investigated by oral administration of the labelled compound followed, after a suitable period of time, by either a whole body count or a faecal count of radioactivity. Preferred bile acids and salts are substituted either at the 19-position or in the C-17 side chain.

Abstract translation: 哺乳动物的身体功能使用伽马发射的75Se或123mTe标记的胆汁酸或胆汁盐衍生物进行研究。 因此，可以通过口服给予标记的化合物，在适当的时间段之后，通过全身计数或粪便计数的放射性来研究肠功能。 优选的胆汁酸和盐在19位或C-17侧链中被取代。