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1. WO2021080352 - RADIOISOTOPE LABELED COMPOUND FOR IMAGING OR TREATMENT OF PROSTATE CANCER

Publication Number WO/2021/080352
Publication Date 29.04.2021
International Application No. PCT/KR2020/014501
International Filing Date 22.10.2020
IPC
C07C 275/24 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
275Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups
04having nitrogen atoms of urea groups bound to acyclic carbon atoms
20of an unsaturated carbon skeleton
24containing six-membered aromatic rings
C07F 1/08 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
1Compounds containing elements of Groups 1 or 11 of the Periodic System
08Copper compounds
A61K 51/04 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51Preparations containing radioactive substances for use in therapy or testing in vivo
02characterised by the carrier
04Organic compounds
A61K 47/22 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
22Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
A61K 47/02 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
02Inorganic compounds
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
Applicants
  • 서울대학교 산학협력단 SEOUL NATIONAL UNIVERSITY R&DB FOUNDATION [KR]/[KR]
Inventors
  • 정재민 JEONG, Jae Min
  • 로디나딤아메드 LODHI, Nadeem Ahmed
  • 이윤상 LEE, Yun-Sang
Agents
  • 이원희 LEE, Won Hee
Priority Data
10-2019-013298424.10.2019KR
Publication Language Korean (KO)
Filing Language Korean (KO)
Designated States
Title
(EN) RADIOISOTOPE LABELED COMPOUND FOR IMAGING OR TREATMENT OF PROSTATE CANCER
(FR) COMPOSÉ MARQUÉ PAR UN RADIOISOTOPE DESTINÉ À L'IMAGERIE OU AU TRAITEMENT D'UN CANCER DE LA PROSTATE
(KO) 전립선 암의 영상 또는 치료를 위한 동위원소 표지 화합물
Abstract
(EN)
The present invention relates to: a derivative in which glutamate-urea-Lysine (GUL) and isonitril are linked by a linker; a radioisotope labeled compound comprising the derivative; and a pharmaceutical composition for treating and diagnosing prostate cancer, containing the derivative as an active ingredient. A derivative according to the present invention has high binding capacity for PSMA, which is expressed in prostate cancer, by acting as a multi-ligand through the binding of three or six derivatives to one atom of technetium or rhenium, has excellent stability in human serum when administered in vivo, and is excreted into the kidney rather than the hepatobiliary tract because of high water solubility so that a clear image of a prostate cancer tumor site can be obtained, and thus the present invention can be effectively usable as a pharmaceutical composition for treating or diagnosing prostate cancer.
(FR)
La présente invention concerne : un dérivé dans lequel de la glutamate-urée-lysine (GUL) et de l'isonitrile sont liés par un lieur ; un composé marqué par un radioisotope comprenant le dérivé ; et une composition pharmaceutique dans le traitement et le diagnostic d'un cancer de la prostate, contenant le dérivé en tant que principe actif. Le dérivé selon la présente invention a une grande capacité de liaison du PSMA, qui est exprimé dans le cancer de la prostate, en agissant comme un multi-ligand par l'intermédiaire de la liaison de trois ou six dérivés à un atome de technétium ou de rhénium, il a une excellente stabilité dans le sérum humain lorsqu'il est administré in vivo, et est extrait dans le rein plutôt que dans le tractus hépatobiliaire, en raison de sa grande solubilité dans l'eau, de façon à pouvoir obtenir une image claire du site tumoral d'un cancer de la prostate, de sorte que la présente invention peut être efficacement utilisée comme composition pharmaceutique dans le traitement ou le diagnostic d'un cancer de la prostate.
(KO)
본 발명은 Glumate -urea-Lysine (GUL)과 이소니트릴을 링커로 연결한 유도체 및 이를 포함하는 방사성동위원소 표지 화합물 및 이를 유효 성분으로 함유하는 전립선암 치료 및 진단용 약학적 조성물에 관한 것이다. 본 발명에 따른 유도체는 테크네튬이나 레늄 한 원자에 3개 혹은 6개가 결합하여 다중 리간드로 작용하여 전립선암에서 발현되는 PSMA에 결합력이 크고, 체내에 투여될 경우 인혈청 내에서 안정성이 우수하고, 수용성이 높아 간담도가 아닌 신장으로 배설이 되어 전립선암 종양 부위의 선명한 영상을 얻을 수 있어서, 전립선암 치료 또는 진단용 약학적 조성물로 유용하게 사용될 수 있다.
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