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1. WO2019190266 - PSMA-TARGETED RADIOPHARMACEUTICAL FOR DIAGNOSING AND TREATING PROSTATE CANCER

Publication Number WO/2019/190266
Publication Date 03.10.2019
International Application No. PCT/KR2019/003716
International Filing Date 29.03.2019
IPC
C07D 403/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
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
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
CPC
A61K 51/0402
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 ; , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
04Organic compounds
0402carboxylic acid carriers, fatty acids
A61K 51/0474
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 ; , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
04Organic compounds
0474complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group
A61K 51/0487
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 ; , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
04Organic compounds
0474complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group
0487Metallocenes, i.e. complexes based on a radioactive metal complexed by two cyclopentadienyl anions
A61K 51/0497
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 ; , i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
04Organic compounds
0497conjugates with a carrier being an organic compounds
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07D 257/02
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
257Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
02not condensed with other rings
Applicants
  • (주)퓨쳐켐 FUTURECHEM CO., LTD [KR]/[KR]
Inventors
  • 지대윤 CHI, Dae Yoon
  • 이병세 LEE, Byoung Se
  • 추소영 CHU, So Young
  • 정현진 JEONG, Hyeon Jin
  • 김민환 KIM, Min Hwan
Agents
  • 이원희 LEE, Won Hee
Priority Data
10-2018-003722630.03.2018KR
Publication Language Korean (KO)
Filing Language Korean (KO)
Designated States
Title
(EN) PSMA-TARGETED RADIOPHARMACEUTICAL FOR DIAGNOSING AND TREATING PROSTATE CANCER
(FR) AGENTS RADIOPHARMACEUTIQUES CIBLÉS SUR PSMA POUR LE DIAGNOSTIC ET LE TRAITEMENT DU CANCER DE LA PROSTATE
(KO) 전립선암 진단 및 치료를 위한 PSMA-표적 방사성의약품
Abstract
(EN)
The present invention relates to a pharmaceutical composition for diagnosing and treating prostate cancer, capable of targeting PSMA, and a compound provided by one aspect of the present invention has a glutamine-urea-lysine compound to which a radioactive metal-coupled chelator is structurally coupled and to which an aryl group that can additionally bind to PSMA protein is coupled.Coupling between the glutamine-urea-lysine compound and the chelator includes a polar spacer so as to serve the role of reducing in vivo nonspecific coupling and exhibit an effect of being rapidly removed from vital organs, but not from prostate cancer. These characteristics lower the radiation exposure, which is caused by a therapeutic radioisotope-coupled compound, to normal tissue and organs, and thus reduce side effects. In addition, a compound that contains a phenyl group having a coupling force with albumin has an increased residence time in the blood, thereby becoming more accumulated in prostate cancer.
(FR)
La présente invention concerne une composition pharmaceutique pour le diagnostic et le traitement du cancer de la prostate, capable de cibler PSMA; un aspect de l'invention concerne aussi un composé comprenant un composé glutamine-urée-lysine auquel un chélateur couplé à un métal radioactif est couplé de manière structurelle et auquel un groupe aryle qui peut en outre se lier à la protéine PSMA est couplé. Le couplage entre le composé glutamine-urée-lysine et le chélateur comprend un espaceur polaire ayant un rôle dans la réduction de couplage non spécifique in vivo et pouvant présenter un effet d'être rapidement éliminé des organes vitaux, mais pas du cancer de la prostate. Ces caractéristiques réduisent l'exposition au rayonnement, qui est provoquée par un composé couplé à un radio-isotope thérapeutique, à un tissu normal et à des organes, et réduisent ainsi les effets secondaires. De plus, un composé qui contient un groupe phényle ayant une force de couplage avec de l'albumine a un temps de séjour accru dans le sang, ce qui lui permet de rester plus accumulé dans le cancer de la prostate.
(KO)
PSMA-표적이 가능한 전립선암 진단 및 치료용 약학적 조성물에 관한 것으로, 본 발명의 일 측면이 제공하는 화합물은 구조적으로 글루타민-유레아-리신 화합물에 방사성금속이 결합된 킬레이터가 결합되어 있고,PSMA 단백질과의 추가적인 결합을 할 수 있는 아릴기가 결합되어 있는 특징이 있다. 글루타민산-유레아-리신 화합물과 킬레이터간의 결합은 극성의 스페이서로 되어 있어 생체내 비특이적 결합을 감소시키는 역할을 하고,전립선암 이외의 주요 장기에서 빠르게 제거되는 효과를 나타낸다. 이러한 특징은 치료용 방사성 동위원소가 결합된 화합물에 의한 정상조직 및 장기의 방사성 피폭을 낮추어 부작용을 감소시키는 장점이 있다. 또한 알부민에 결합력을 갖는 페닐기를 포함하는 화합물은 혈액 내 체류시간이 증가하여 전립선암에 보다 많이 축적되는 효과가 있다.
Also published as
PH12020551471
TH2001005633
AEP6001378/2020
MXMX/a/2020/010266
ZA2020/06008
JP2021502679
Latest bibliographic data on file with the International Bureau