HRP20191482T1 - 18f-označeni psma ciljani pet reagensi - Google Patents
18f-označeni psma ciljani pet reagensi Download PDFInfo
- Publication number
- HRP20191482T1 HRP20191482T1 HRP20191482T HRP20191482T1 HR P20191482 T1 HRP20191482 T1 HR P20191482T1 HR P20191482 T HRP20191482 T HR P20191482T HR P20191482 T1 HRP20191482 T1 HR P20191482T1
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- Prior art keywords
- group
- formula
- nitrobenzyl
- benzyl
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/0489—Phosphates or phosphonates, e.g. bone-seeking phosphonates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/0402—Organic compounds carboxylic acid carriers, fatty acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/06—Phosphorus compounds without P—C bonds
- C07F9/22—Amides of acids of phosphorus
- C07F9/24—Esteramides
- C07F9/2404—Esteramides the ester moiety containing a substituent or a structure which is considered as characteristic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/06—Phosphorus compounds without P—C bonds
- C07F9/22—Amides of acids of phosphorus
- C07F9/24—Esteramides
- C07F9/2404—Esteramides the ester moiety containing a substituent or a structure which is considered as characteristic
- C07F9/2416—Esteramides the ester moiety containing a substituent or a structure which is considered as characteristic of cycloaliphatic alcohols
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/06—Phosphorus compounds without P—C bonds
- C07F9/22—Amides of acids of phosphorus
- C07F9/24—Esteramides
- C07F9/2454—Esteramides the amide moiety containing a substituent or a structure which is considered as characteristic
- C07F9/2458—Esteramides the amide moiety containing a substituent or a structure which is considered as characteristic of aliphatic amines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/576—Six-membered rings
- C07F9/58—Pyridine rings
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Optics & Photonics (AREA)
- Physics & Mathematics (AREA)
- Biophysics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Peptides Or Proteins (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (15)
1. Spoj formule (I):
ili njegova farmaceutski prihvatljiva sol, pri čemu je
L veznik formule -NH-CH2CH2-(OCH2CH2-)y-C(O)- ili skupine formula
pri čemu je
u čemu
y je 1,2, 3, 4, 5, 6, 7, 8, 9, 10, 11 ili 12;
m je 1, 2, 3 ili 4;
svaki nje neovisno 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 ili 12;
R1 je fenil ili piridil; pri čemu je fenil ili piridil supstituiran sa [F] - ili [18F] -fluoro skupinom i opcijski supstituirana s drugom skupinom koja je odabrana od halogena, cijano i nitro;
svaki R2 je nezavisno vodik ili C1-C6 alkil; i
svaki R je neovisno vodik ili zaštitna skupina odabrana iz skupine koja sadrži alkil, alkenil, haloalkil, benzil, trifenilmetil (trtil), difenilmetil, o-nitrobenzil, 2,4,6-trimetilbenzil, p-bromobenzil, p-nitrobenzil, p-metoksibenzil (PMB), 2,6-dimetoksibenzil, 4- (metilsulfinil) benzil, 4-sulfobenzil, 4-azidometoksibenzil, i piperonil, poželjno odabran iz skupine koja sadrži metil, etil, propil, izopropil, terc-butil, alil, trifluorometil, trifluoroetil, benzil, trifenilmetil (tritil), difenilmetil, o-nitrobenzil, 2,4,6- trimetilbenzil, p-bromobenzil, p-nitrobenzil, p-metoksibenzil (PMB), 2,6-dimetoksibenzil, 4- (metilsulfinil) benzil, 4-sulfobenzil, 4-azidometoksibenzil i piperonil;
pod uvjetom da kada je L skupina formule
m (n+2) je veće ili jednako 3 i manje ili jednako 21.
2. Spoj u skladu s patentnim zahtjevom 1, pri čemu je spoj formule (Ic);
ili njegova farmaceutski prihvatljiva sol.
3. Spoj u skladu s patentnim zahtjevom 1 ili 2, pri čemu je svaki R vodik.
4. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-3, pri čemu je svaki R2 vodik.
5. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-4, pri čemu je m 1 ili 2.
6. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-5, pri čemu je spoj formule (Id):
ili njegova farmaceutski prihvatljiva sol.
7. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-6, pri čemu je R1:
pri čemu je
X vodik ili klor; i
Y je N ili CH.
8. Spoj u skladu s patentnim zahtjevom 7, pri čemu je (i) X vodik i Y CH; (ii) X je vodik i Y je N; (iii) X je klor i Y je N; ili (iv) X je klor i Y je CH.
9. Spoj u skladu s patentnim zahtjevom 1 koji je:
ili njegova farmaceutski prihvatljiva sol.
10. Pripravak koji sadrži spoj bilo kojeg od patentnih zahtjeva 1-9, ili njegovu farmaceutski prihvatljivu sol, zajedno s farmaceutski prihvatljivim nosačem, ekscipijensom i/ili razrjeđivačem.
11. Spoj formule (II):
ili njegova farmaceutski prihvatljiva sol, pri čemu je
L veznik formule -NH-CH2CH2-(OCH2CH2-)y-C(O)- ili skupine formula
pri čemu je
y 1,2, 3, 4,5,6, 7, 8, 9, 10, 11 ili 12;
m je 1, 2, 3, ili 4;
svaki nje neovisno 1,2, 3, 4, 5, 6, 7, 8, 9, 10, 11 ili 12;
svaki R2 je neovisno vodik ili C1-C6 alkil; i
svaki R je neovisno vodik ili zaštitna skupina izabrana iz skupine koja sadrži alkil, alkenil, haloalkil, benzil, trifenilmetil (tritil), difenilmetil, o-nitrobenzil, 2,4,6-trimetilbenzil, p-bromobenzil, p-nitrobenzil, p-metoksibenzil (PMB), 2,6-dimetoksibenzil, 4-(metilsulfmil)benzil, 4-sulfobenzil, 4-azidometoksibenzil, i piperonil, preferabilno izabran iz skupine koja sadrži metil, etil, propil, isopropil, tert-butil, alil, trifluorometil, trifluoroetil, benzil, trifenilmetil (tritil), difenilmetil, o-nitrobenzil, 2,4,6-trimetilbenzil, p-bromobenzil, p-nitrobenzil, p-metoksibenzil (PMB), 2,6-dimetoksibenzil, 4-(metilsulfinil)benzil, 4-sulfobenzil, 4-azidometoksibenzil, i piperonil; pod uvjetom da kada je L skupina formule
m (n+2) je veći ili jednak 3 i manji ili jednak 21.
12. Spoj u skladu s patentnim zahtjevom 11 koji je:
ili njegova farmaceutski prihvatljiva sol.
13. Spoj formule (III):
ili njegova farmaceutski prihvatljiva sol, pri čemu je
L veznik formule -NH-CH2CH2-(OCH2CH2-)y-C(O)- ili skupina formule
pri čemu je
y 1,2, 3, 4,5,6, 7, 8, 9, 10, 11 ili 12;
m je 1, 2, 3 ili 4;
svaki nje neovisno 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 ili 12;
R3 je fenil ili piridil; pri čemu je fenil ili piridil supstituiran odlazećom grupom i opcionalno supstituiran s drugom grupom izabranom između halogena, cijano i nitro;
svaki R2 je neovisno vodik ili C1-C6 alkil; i
svaki R je neovisno vodik ili zaštitna skupina izabrana iz grupe koja sadrži alkil, alkenil, haloalkil, benzil, trifenilmetil (tritil), difenilmetil, o-nitrobenzil, 2,4,6-trimetilbenzil, p-bromobenzil, p-nitrobenzil, p-metoksibenzil (PMB), 2,6-dimetoksibenzil, 4-(metilsulfinil)benzil, 4-sulfobenzil, 4-azidometoksibenzil, i piperonil, preferabilno izabran iz skupine koja sadrži metil, etil, propil, izopropil, tert-butil, alil, trifluorometil, trifluoroetil, benzil, trifenilmetil (tritil), difenilmetil, o-nitrobenzil, 2,4,6-trimetilbenzil, p-bromobenzil, p-nitrobenzil, p-metoksibenzil (PMB), 2,6-dimetoksibenzil, 4-(metilsulfinil) benzil, 4-sulfobenzil, 4-azidometoksibenzil i piperonil; pod uvjetom da kada je L skupina formule
m (n+2) je veće ili jednako 3 i manje ili jednako 21.
14. Spoj u skladu s patentnim zahtjevom 13, pri čemu je R3
pri čemu R6 je odlazeća skupina.
15. Spoj u skladu s patentnim zahtjevima 13 ili 14, pri čemu su odlazeća skupina nitro, trimetilstanil, benzotriazol-1-iloksi, halogen, C1-C10alkilsulfonat, C1-C10haloalkilsulfonat, nonaflat, fenilsulfonat pri čemu je fenil opcionalno supstituiran s 1,2 ili 3 skupine koje su svaka neovisno halogene ili C1-C4 alkil ili sol amonijaka formule -[N(Rx)(Ry)(Rz)]+[X]-, pri čemu su Rx, Ry, and Rz neovisno vodik ili alkil i X je konjugirana baza jake kiseline, preferabilno je odlazeća skupina halogen ili trialkilamonijak.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201361798108P | 2013-03-15 | 2013-03-15 | |
PCT/US2014/027820 WO2014143736A1 (en) | 2013-03-15 | 2014-03-14 | 18f-labeled psma-targeted pet imaging agents |
EP14721640.2A EP2970345B1 (en) | 2013-03-15 | 2014-03-14 | 18f-labeled psma-targeted pet imaging agents |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20191482T1 true HRP20191482T1 (hr) | 2019-11-15 |
Family
ID=50639969
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20230109TT HRP20230109T1 (hr) | 2013-03-15 | 2014-03-14 | Postupci pripreme 18f-obilježenih psma-usmjerenih sredstava za pet snimanje i dijagnostički postupci sa njima |
HRP20191482 HRP20191482T1 (hr) | 2013-03-15 | 2014-03-14 | 18f-označeni psma ciljani pet reagensi |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20230109TT HRP20230109T1 (hr) | 2013-03-15 | 2014-03-14 | Postupci pripreme 18f-obilježenih psma-usmjerenih sredstava za pet snimanje i dijagnostički postupci sa njima |
Country Status (17)
Country | Link |
---|---|
US (2) | US11554183B2 (hr) |
EP (3) | EP3560937B1 (hr) |
CN (2) | CN108558939B (hr) |
AU (2) | AU2014228233B2 (hr) |
CA (1) | CA2903131C (hr) |
DK (2) | DK2970345T3 (hr) |
ES (2) | ES2743433T3 (hr) |
FI (1) | FI3560937T3 (hr) |
HR (2) | HRP20230109T1 (hr) |
HU (2) | HUE046194T2 (hr) |
LT (2) | LT3560937T (hr) |
PL (2) | PL2970345T3 (hr) |
PT (2) | PT3560937T (hr) |
RS (1) | RS64011B1 (hr) |
SI (2) | SI3560937T1 (hr) |
SM (1) | SMT202300035T1 (hr) |
WO (1) | WO2014143736A1 (hr) |
Families Citing this family (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US11078166B2 (en) | 2015-08-13 | 2021-08-03 | The Johns Hopkins University | Triazole conjugated ureas, thioureas, carbamates, and reversed carbamates for PSMA-targeted imaging agents and uses thereof |
MX392700B (es) * | 2016-08-10 | 2025-03-11 | Cancer Targeted Tech Llc | Inhibidores de antígeno de la membrana específico para la próstata (psma) quelados. |
CN110418604B (zh) | 2017-03-22 | 2023-04-18 | 赛佛欧普手术有限公司 | 用于检测电生理诱发电位变化的医疗系统和方法 |
WO2018233798A1 (en) | 2017-06-20 | 2018-12-27 | ITM Isotopen Technologien München AG | NOVEL PSMA BINDING AGENTS AND USE THEREOF |
KR20200009091A (ko) | 2017-05-24 | 2020-01-29 | 아이티엠 이소토펜 테크놀로지엔 뮌헨 아게 | 신규 psma-결합제 및 이의 용도 |
WO2020108753A1 (en) | 2018-11-28 | 2020-06-04 | ITM Isotopen Technologien München AG | Novel tumor antigen binding agents and uses thereof |
WO2020224780A1 (en) | 2019-05-08 | 2020-11-12 | ITM Isotopen Technologien München AG | Para-aminohippuric acid (pah) as a renal protective substance |
WO2021046233A1 (en) | 2019-09-03 | 2021-03-11 | Cancer Targeted Technology Llc | Chelate-containing psma inhibitors |
WO2022096103A1 (en) | 2020-11-05 | 2022-05-12 | ITM Isotopen Technologien München AG | Combination of para-aminohippuric acid (pah) and radiolabeled complexes for treating cancer |
WO2022111800A1 (en) | 2020-11-25 | 2022-06-02 | Itm Solucin Gmbh | Stable formulations for radionuclide complexes |
JP2024514293A (ja) | 2021-04-02 | 2024-04-01 | ノバルティス アーゲー | 前立腺がんの診断方法 |
WO2025038752A1 (en) | 2023-08-14 | 2025-02-20 | Cancer Targeted Technology Llc | Psma binding ligand-linker conjugates and methods for use thereof |
Family Cites Families (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7696185B2 (en) * | 2006-03-14 | 2010-04-13 | Cancer Targered Technology LLC | Peptidomimetic inhibitors of PSMA, compounds comprising them, and methods of use |
BRPI0716554A2 (pt) * | 2006-09-08 | 2013-09-24 | Bayer Schering Pharma Ag | compostos de mÉtodos para agentes rotulados de 18f |
RU2494096C2 (ru) * | 2008-08-01 | 2013-09-27 | Дзе Джонс Хопкинс Юниверсити | Агенты, связывающиеся с psma, и их применение |
US9328129B2 (en) * | 2010-11-12 | 2016-05-03 | Washington State University | Peptidomimetic inhibitors of PSMA |
CN107325127B (zh) * | 2011-06-15 | 2020-09-01 | 癌靶技术有限责任公司 | 螯合的psma抑制剂 |
CN102757296B (zh) * | 2012-04-10 | 2014-11-19 | 中国科学院上海应用物理研究所 | 一种对化合物进行[18f]标记的方法 |
WO2013173630A1 (en) * | 2012-05-16 | 2013-11-21 | Cancer Targeted Technology, Llc | Formulation of radiopharmaceuticals containing multiple acidic groups |
WO2013173583A1 (en) * | 2012-05-16 | 2013-11-21 | Cancer Targeted Technology, Llc | Psma inhibitors |
-
2014
- 2014-03-14 PT PT191797588T patent/PT3560937T/pt unknown
- 2014-03-14 SI SI201432018T patent/SI3560937T1/sl unknown
- 2014-03-14 LT LTEP19179758.8T patent/LT3560937T/lt unknown
- 2014-03-14 PL PL14721640T patent/PL2970345T3/pl unknown
- 2014-03-14 EP EP19179758.8A patent/EP3560937B1/en active Active
- 2014-03-14 AU AU2014228233A patent/AU2014228233B2/en active Active
- 2014-03-14 HU HUE14721640A patent/HUE046194T2/hu unknown
- 2014-03-14 DK DK14721640.2T patent/DK2970345T3/da active
- 2014-03-14 CA CA2903131A patent/CA2903131C/en active Active
- 2014-03-14 HU HUE19179758A patent/HUE061402T2/hu unknown
- 2014-03-14 PT PT14721640T patent/PT2970345T/pt unknown
- 2014-03-14 LT LTEP14721640.2T patent/LT2970345T/lt unknown
- 2014-03-14 EP EP14721640.2A patent/EP2970345B1/en active Active
- 2014-03-14 WO PCT/US2014/027820 patent/WO2014143736A1/en active Application Filing
- 2014-03-14 PL PL19179758.8T patent/PL3560937T3/pl unknown
- 2014-03-14 DK DK19179758.8T patent/DK3560937T3/da active
- 2014-03-14 CN CN201810256877.5A patent/CN108558939B/zh active Active
- 2014-03-14 ES ES14721640T patent/ES2743433T3/es active Active
- 2014-03-14 SI SI201431305T patent/SI2970345T1/sl unknown
- 2014-03-14 HR HRP20230109TT patent/HRP20230109T1/hr unknown
- 2014-03-14 ES ES19179758T patent/ES2937955T3/es active Active
- 2014-03-14 US US14/774,371 patent/US11554183B2/en active Active
- 2014-03-14 EP EP22215508.7A patent/EP4180438A1/en active Pending
- 2014-03-14 FI FIEP19179758.8T patent/FI3560937T3/fi active
- 2014-03-14 HR HRP20191482 patent/HRP20191482T1/hr unknown
- 2014-03-14 SM SM20230035T patent/SMT202300035T1/it unknown
- 2014-03-14 RS RS20230089A patent/RS64011B1/sr unknown
- 2014-03-14 CN CN201480021159.XA patent/CN105308056B/zh active Active
-
2019
- 2019-05-22 AU AU2019203610A patent/AU2019203610B2/en active Active
-
2023
- 2023-01-04 US US18/149,981 patent/US20230144322A1/en active Pending
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