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1. (WO2018144101) RADIOLABELING AGENTS, METHODS OF MAKING, AND METHODS OF USE THEREOF
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Pub. No.: WO/2018/144101 International Application No.: PCT/US2017/060838
Publication Date: 09.08.2018 International Filing Date: 09.11.2017
IPC:
C07B 47/00 (2006.01) ,C07B 59/00 (2006.01) ,C07D 261/18 (2006.01) ,C07F 1/08 (2006.01) ,C07C 17/10 (2006.01) ,C07C 29/38 (2006.01) ,C07C 41/30 (2006.01) ,C07C 201/12 (2006.01) ,C07C 213/08 (2006.01) ,C07C 319/14 (2006.01) ,C07C 45/68 (2006.01) ,C07C 231/12 (2006.01) ,C07D 261/08 (2006.01) ,C07C 253/30 (2006.01) ,C07C 17/32 (2006.01) ,C07C 17/361 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
B
GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
47
Formation or introduction of functional groups not provided for in groups C07B39/-C07B45/126
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
B
GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
59
Introduction of isotopes of elements into organic compounds
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
261
Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
02
not condensed with other rings
06
having two or more double bonds between ring members or between ring members and non-ring members
10
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
18
Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
F
ACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
1
Compounds containing elements of the 1st Group of the Periodic System
08
Copper compounds
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
17
Preparation of halogenated hydrocarbons
093
by replacement by halogens
10
of hydrogen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
29
Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring
36
increasing the number of carbon atoms by reactions with formation of hydroxy groups, which may occur via intermediates being derivatives of hydroxy groups, e.g. O-metal
38
by reaction with aldehydes or ketones
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
41
Preparation of ethers; Preparation of compounds having groups, groups or groups
01
Preparation of ethers
18
by reactions not forming ether-oxygen bonds
30
by increasing the number of carbon atoms, e.g. by oligomerisation
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
201
Preparation of esters of nitric or nitrous acid or of compounds containing nitro or nitroso groups bound to a carbon skeleton
06
Preparation of nitro compounds
12
by reactions not involving the formation of nitro groups
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
213
Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
08
by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
319
Preparation of thiols, sulfides, hydropolysulfides or polysulfides
14
of sulfides
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
45
Preparation of compounds having CO groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
61
by reactions not involving the formation of CO groups
67
by isomerisation; by change of size of the carbon skeleton
68
by increase in the number of carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
231
Preparation of carboxylic acid amides
12
by reactions not involving the formation of carboxamide groups
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
261
Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
02
not condensed with other rings
06
having two or more double bonds between ring members or between ring members and non-ring members
08
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
253
Preparation of carboxylic acid nitriles
30
by reactions not involving the formation of cyano groups
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
17
Preparation of halogenated hydrocarbons
26
by reactions involving an increase in the number of carbon atoms in the skeleton
32
by introduction of halogenated alkyl groups into ring compounds
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
17
Preparation of halogenated hydrocarbons
361
by reactions involving a decrease in the number of carbon atoms
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 Bethesda, Maryland 20892-7660, US
Inventors:
PIKE, Victor William; US
HASKALI, Mohammad Baqir; US
YANG, Bo Yeun; US
TELU, Sanjay; US
Agent:
LECUYER, Karen A.; US
Priority Data:
62/420,84011.11.2016US
Title (EN) RADIOLABELING AGENTS, METHODS OF MAKING, AND METHODS OF USE THEREOF
(FR) AGENTS DE MARQUAGE ISOTOPIQUE, LEURS PROCÉDÉS DE FABRICATION ET PROCÉDÉS D'UTILISATION
Abstract:
(EN) Described herein are labeling agents, specifically [11C]fluoroform, [11C]difluoromethane, [11C]fluoromethyl iodide, [11C]fluoromethyl bromide, [11C]fluoromethyl chloride, [11C]fluoromethyl trifluoromethansulfonate, [11C]difluoromethyl iodide, [11C]difluoromethyl bromide, [11C]difluoromethyl chloride, [11C]difluoromethyl trifluoromethansulfonate, [11C]trifluoromethyl iodide, [11C]trifluoromethyl bromide, [11C]trifluoromethyl chloride, [11C]trifluoromethyl trifluoromethansulfonate, [18F]fluoroform, [18F]difluoromethane, [18F]difluoromethyl bromide or [18F]trifluoromethyl bromide. Also included are methods of labeling precursors to provide labeled fluoroalkanes and imaging methods.
(FR) La présente invention concerne des agents de marquage, plus particulièrement du [11C]fluoroforme, du [11C]difluorométhane, de l'iodure de [11C]fluorométhyle, du bromure de [11C]fluorométhyle, du chlorure de [11C]fluorométhyle, du trifluorométhansulfonate de [11C]fluorométhyle, de l'iodure de [11C]difluorométhyle, du bromure de [11C]difluorométhyle, du chlorure de [11C]difluorométhyle, du trifluorométhansulfonate de [11C]difluorométhyle, de l'iodure de [11C]trifluorométhyle, du bromure de [11C]trifluorométhyle, du chlorure de [11C]trifluorométhyle, du trifluorométhansulfonate de [11C]trifluorométhyle, du [18F]fluoroforme, du [18F]difluorométhane, du bromure de [18F]difluorométhyle ou du bromure de [18F]trifluorométhyle. L'invention concerne également des procédés de marquage de précurseurs visant à fournir des fluoroalcanes marqués et des procédés d'imagerie.
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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 Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (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)