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1. (WO2019070236) CHEMICAL CONJUGATES OF EVANS BLUE DERIVATIVES AND THEIR USE AS RADIOTHERAPY AND IMAGING AGENTS
Latest bibliographic data on file with the International BureauSubmit observation

Pub. No.: WO/2019/070236 International Application No.: PCT/US2017/054863
Publication Date: 11.04.2019 International Filing Date: 03.10.2017
IPC:
C07D 403/12 (2006.01) ,C07D 307/60 (2006.01) ,C07D 257/02 (2006.01) ,A61K 31/4015 (2006.01) ,A61K 31/395 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
307
Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
02
not condensed with other rings
34
having two or three double bonds between ring members or between ring members and non-ring members
56
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
60
Two oxygen atoms, e.g. succinic anhydride
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
257
Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
02
not condensed with other rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
40
having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
4015
having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
Applicants:
THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES [US/US]; National Institutes of Health Office of Technology Transfer 6011 Executive Boulevard Suite 325, MSC 7660 Bethesda, Maryland 20892-7660, US
Inventors:
CHEN, Xiaoyuan; US
WEISS, Orit Jacobson; US
Agent:
GARABEDIAN, Todd E.; US
Priority Data:
Title (EN) CHEMICAL CONJUGATES OF EVANS BLUE DERIVATIVES AND THEIR USE AS RADIOTHERAPY AND IMAGING AGENTS
(FR) CONJUGUÉS CHIMIQUES DE DÉRIVÉS DU BLEU D'EVANS ET LEUR UTILISATION COMME AGENTS DE RADIOTHÉRAPIE ET D'IMAGERIE
Abstract:
(EN) The present invention is directed to a compound of Formula III or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt: Formula III wherein the definitions of R1-R12 and L1-L4 are provided in the disclosure, wherein R13 is a chelating group comprising 177Lu, and wherein R14 is a peptide. The compounds of Formula I may be covalently bonded to a peptide via a linker to provide a compound of Formula III and thereby extend the half-life of the therapeutic compound. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use in the diagnosis or treatment of diseases.
(FR) La présente invention concerne un composé de formule III ou un ester, amide, solvate ou sel pharmaceutiquement acceptable de celui-ci, ou un sel d'un tel ester ou amide ou un solvate d'un tel ester, amide, ou sel : formule III, dans laquelle les définitions de R1 à R12 et L1 à L4 sont telles que définis dans la description, R13 étant un groupe chélateur comprenant 177Lu, et R14 étant un peptide. Les composés de formule I peuvent être liés de manière covalente à un peptide par l'intermédiaire d'un lieur afin de fournir un composé de formule III et prolonger ainsi la demi-vie du composé thérapeutique. L'invention concerne également des compositions pharmaceutiques de composés selon l'invention, ainsi que leur utilisation dans le diagnostic ou le traitement de maladies.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)