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1. WO2020139012 - CARBOXYLIC ACID-INTRODUCED PSMA-TARGETING COMPOUND AND USE THEREOF

Publication Number WO/2020/139012
Publication Date 02.07.2020
International Application No. PCT/KR2019/018594
International Filing Date 27.12.2019
IPC
C07D 249/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
249Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
02not condensed with other rings
041,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
A61K 31/4192 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
41921,2,3-Triazoles
C07C 275/12 2006.1
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
06of an acyclic and saturated carbon skeleton
12being further substituted by doubly-bound oxygen atoms
C07D 213/56 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
24with substituted hydrocarbon radicals attached to ring carbon atoms
54Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
56Amides
A61P 35/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
G01N 33/574 2006.1
GPHYSICS
01MEASURING; TESTING
NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
33Investigating or analysing materials by specific methods not covered by groups G01N1/-G01N31/131
48Biological material, e.g. blood, urine; Haemocytometers
50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
53Immunoassay; Biospecific binding assay; Materials therefor
574for cancer
CPC
A61K 31/4192
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
41921,2,3-Triazoles
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07C 275/12
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
06of an acyclic and saturated carbon skeleton
12being further substituted by doubly-bound oxygen atoms
C07D 213/56
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
24with substituted hydrocarbon radicals attached to ring carbon atoms
54Radicals substituted by carbon atoms having three bonds to heteroatoms, with at the most one to halogen, e.g. ester or nitrile radicals
56Amides
C07D 249/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
249Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
02not condensed with other rings
041,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
G01N 33/574
GPHYSICS
01MEASURING; TESTING
NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
33Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
48Biological material, e.g. blood, urine
50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
53Immunoassay; Biospecific binding assay; Materials therefor
574for cancer
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
  • 이교철 LEE, Kyo Chul
  • 이용진 LEE, Yong Jin
  • 박지애 PARK, Ji Ae
  • 강충모 KANG, Choong Mo
  • 임상무 LIM, Sang Moo
Agents
  • 이원희 LEE, Won Hee
Priority Data
10-2018-017077027.12.2018KR
Publication Language Korean (KO)
Filing Language Korean (KO)
Designated States
Title
(EN) CARBOXYLIC ACID-INTRODUCED PSMA-TARGETING COMPOUND AND USE THEREOF
(FR) COMPOSÉ CIBLANT PSMA INTRODUIT PAR ACIDE CARBOXYLIQUE ET UTILISATION ASSOCIÉE
(KO) 카르복시산이 도입된 PSMA-표적 화합물 및 그의 용도
Abstract
(EN)
The present invention relates to a 18F-labeled compound for diagnosing prostate cancer and a use thereof. The carboxylic acid-introduced compound of the present invention forms strong ion-pair bonds (salt-bridge interactions) with arginine residues present at PSMA protein-binding sites, and thus has high binding affinity, and has rapid background radiation removal effects in vivo due to the hydrophilic properties of carboxylic acid, and less non-specific binding.
(FR)
La présente invention concerne un composé marqué par 18F pour le diagnostic d'un cancer de la prostate et une utilisation associée. Le composé introduit par un acide carboxylique selon la présente invention forme de fortes liaisons à paires d'ions (interactions en pont salin) avec des résidus d'arginine présents au niveau des sites de liaison à la protéine PSMA, et présente ainsi une affinité de liaison élevée, et a des effets d'élimination de rayonnement d'arrière-plan rapides in vivo en raison des propriétés hydrophiles d'acide carboxylique, et moins de liaisons non spécifiques.
(KO)
본 발명은 전립선암 진단을 위한 18F-표지된 화합물 및 그의 용도에 관한 것으로, 본 발명의 카르복실산이 도입된 화합물들은 PSMA 단백질 결합부위에 있는 아르기닌(arginine) 잔기와의 강한 이온쌍 결합(Salt Bridge Interaction)을 형성하여 결합친화력이 높고, 카르복실산의 친수성 성질로 생체 내 빠른 배경방사능 제거 효과와 낮은 비특이적 결합을 갖는 특징이 있다.
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