Abstract: The present invention relates to tricarbonyl technetium-99m or rhenium-188 labeled cyclic RGD derivatives, a preparation method thereof, and a pharmaceutical composition containing the derivative as an active ingredient for use in the diagnosis or treatment (radiotherapy) of angiogenesis-related diseases. The tricarbonyl technetium-99m or rhenium-188 labeled cyclic RGD derivatives of the present invention has a high subnanomolar affinity to integrin ?v?3 (also called as a vitronectin receptor) that is activated in an angiogenic action induced by a tumor, and acts exclusively upon cancer cells having selectively activated integrin ?v?3 because of a substantially low intake into the liver and intestines.
Type:
Grant
Filed:
May 24, 2011
Date of Patent:
September 13, 2016
Assignee:
BIO IMAGING KOREA CO., LTD.
Inventors:
Byung Chul Lee, Sang Eun Kim, Ji Sun Kim, Byung Seok Moon, Jae Ho Jung
Abstract: Disclosed is the synthesis of [18F]flumazenil that is useful in imaging epileptic lesions by PET (positron emission tomography). A method for preparing [18F]flumazenil by reacting a diaryliodonium salt precursor with the positron-emitting radionuclide fluorine-18. [18F]flumazenil can be prepared from the diaryliodonium salt precursor in the presence of kryptofix2.2.2./potassium carbonate(K2.2.2./K2CO3) and TEMPO in dimethylformamide (DMF) at a high yield.
Type:
Grant
Filed:
November 22, 2013
Date of Patent:
November 25, 2014
Assignee:
Bio Imaging Korea Co., Ltd.
Inventors:
Byung Chul Lee, Byung Seok Moon, Ji Sun Kim
Abstract: Disclosed is the synthesis of [18F]flumazenil that is useful in imaging epileptic lesions by PET (positron emission tomography). A method for preparing [18F]flumazenil by reacting a diaryliodonium salt precursor with the positron-emitting radionuclide fluorine-18. [18F]flumazenil can be prepared from the diaryliodonium salt precursor in the presence of kryptofix2.2.2./potassium carbonate(K2.2.2./K2CO3) and TEMPO in dimethylformamide (DMF) at a high yield.
Type:
Application
Filed:
November 22, 2013
Publication date:
March 20, 2014
Applicant:
BIO IMAGING KOREA CO., LTD.
Inventors:
Byung Chul Lee, Byung Seok Moon, Ji Sun Kim