HRP20201372T1 - Radioaktivno označeni pet mglur2/3 ligandi - Google Patents
Radioaktivno označeni pet mglur2/3 ligandi Download PDFInfo
- Publication number
- HRP20201372T1 HRP20201372T1 HRP20201372TT HRP20201372T HRP20201372T1 HR P20201372 T1 HRP20201372 T1 HR P20201372T1 HR P20201372T T HRP20201372T T HR P20201372TT HR P20201372 T HRP20201372 T HR P20201372T HR P20201372 T1 HRP20201372 T1 HR P20201372T1
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- Croatia
- Prior art keywords
- compound
- formula
- image
- pharmaceutically acceptable
- solvate
- Prior art date
Links
- 239000003446 ligand Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 19
- 150000003839 salts Chemical class 0.000 claims 8
- 239000012453 solvate Substances 0.000 claims 8
- 238000003384 imaging method Methods 0.000 claims 6
- 239000012442 inert solvent Substances 0.000 claims 6
- 239000000825 pharmaceutical preparation Substances 0.000 claims 5
- 101001071429 Homo sapiens Metabotropic glutamate receptor 2 Proteins 0.000 claims 4
- 102100036837 Metabotropic glutamate receptor 2 Human genes 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 102000005962 receptors Human genes 0.000 claims 4
- 108020003175 receptors Proteins 0.000 claims 4
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims 3
- 241000124008 Mammalia Species 0.000 claims 3
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 claims 3
- 238000006243 chemical reaction Methods 0.000 claims 3
- 230000002285 radioactive effect Effects 0.000 claims 3
- 230000015572 biosynthetic process Effects 0.000 claims 2
- 239000003153 chemical reaction reagent Substances 0.000 claims 2
- IZDROVVXIHRYMH-UHFFFAOYSA-N methanesulfonic anhydride Chemical compound CS(=O)(=O)OS(C)(=O)=O IZDROVVXIHRYMH-UHFFFAOYSA-N 0.000 claims 2
- 230000000269 nucleophilic effect Effects 0.000 claims 2
- 238000003786 synthesis reaction Methods 0.000 claims 2
- GETQZCLCWQTVFV-UHFFFAOYSA-N trimethylamine Chemical compound CN(C)C GETQZCLCWQTVFV-UHFFFAOYSA-N 0.000 claims 2
- 239000002872 contrast media Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000002600 positron emission tomography Methods 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 238000011002 quantification Methods 0.000 claims 1
- 239000008174 sterile solution Substances 0.000 claims 1
Classifications
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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
- A61K51/041—Heterocyclic compounds
- A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
- A61K51/0459—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- General Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Physics & Mathematics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Optics & Photonics (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (15)
1. Spoj prema Formuli (I)
[image]
pri čemu R1 je -CH2F i R2 je -H, ili R1 je -H i R2 je -CH2F, i pri čemu je najmanje jedan atom radioaktivan, ili njegova farmaceutski prihvatljiva sol ili solvat, naznačen time što je za uporabu za slikanje ili kvantificiranje mGlu2 i 3 receptora.
2. Spoj za uporabu u skladu s patentnim zahtjevom 1, naznačen time što ima Formulu
[image]
ili farmaceutski prihvatljiva sol njegovog solvata.
3. Spoj za uporabu u skladu s patentnim zahtjevom 1, naznačen time što ima Formulu
[image]
ili farmaceutski prihvatljiva sol njegovog solvata.
4. Radioaktivno označen spoj Formule
[image]
ili farmaceutski prihvatljiva sol njegovog solvata.
5. Radioaktivno označen spoj Formule
[image]
ili farmaceutski prihvatljiva sol njegovog solvata.
6. Sterilni farmaceutski pripravak naznačen time što sadrži spoj Formule (I) kako je definiran u bilo kojem od patentnih zahtjeva 1 do 5, ili njegovu farmaceutski prihvatljivu sol ili solvat, i farmaceutski prihvatljiv nosač ili razrjeđivač.
7. Sterilni farmaceutski pripravak prema patentnom zahtjevu 6, naznačen time što je takav pripravak sterilna otopina.
8. Sterilni farmaceutski pripravak kako je definiran u patentnom zahtjevu 6 ili 7, naznačen time što je za uporabu za slikanje ili kvantificiranje mGlu2 i 3 receptora.
9. Sterilni farmaceutski pripravak for use kako je definiran u patentnom zahtjevu 8, naznačen time što slikanje uključuje određivanje popunjenosti mGlu2 i 3 receptorskog mjesta s drugim ne-radioaktivno označenim spojevima.
10. Spoj prema bilo kojem od patentnih zahtjeva 1 do 5, ili farmaceutski pripravak prema patentnom zahtjevu 6 ili 7, naznačen time što je za uporabu kao kontrastno sredstvo za slikanje tkiva, stanica ili sisavca.
11. Postupak slikanja tkiva, stanica ili sisavca, obuhvaća dovođenje u kontakt ili osiguravanje odredive količine spoja Formule (I) ili njegove farmaceutski prihvatljive soli ili solvata kako je definirano u bilo kojem od zahtjeva 1 do 5, u tkivo, stanice ili sisavca i otkrivanje obilježenog spoja povezanog s mGlu2 i 3 receptorom.
12. Postupak prema patentnom zahtjevu 11 naznačen time što je tehnika slikanja pozitronsko-emisijska tomografija.
13. Spoj naznačen time što je odabran iz skupine koja sadrži
[image]
ili njihovu farmaceutski prihvatljivu sol ili solvat.
14. Postupak za sintezu spoja definiranog u patentnom zahtjevu 2, naznačen time što sadrži
(a) korake (a-1) reakcije spoja s Formulom (P-1) s metansulfonskim anhidridom u prisutnosti baze i inertnog otapala, i (a-2) reakciju spoja dobivenog u koraku (a-1) s [18F]F- u prisutnosti baze u inertnom otapalu
[image]
(b) korak reakcije spoja s Formulom (P-2) s [18F]F- u prisutnosti baze u inertnom otapalu
[image]
15. Postupak za sintezu spoja definiranog u patentnom zahtjevu 3, naznačen time što sadrži
(a) korake (a-1) reakcije spoja s Formulom (P-3) s metansulfonskim anhidridom u prisutnosti baze i inertnog otapala, na primjer, trimetilaminom ili trietilaminom i diklorometanom, i (a-2) reakciju spoja dobivenog u koraku (a-1) s nukleofilnim radioaktivnim fluorirajućim reagensom [18F]F- u prisutnosti baze u inertnom otapalu
[image]
(b) korak reakcije spoja s Formulom (P-4) s nukleofilnim radioaktivnim fluorirajućim reagensom [18F]F- u prisutnosti baze u inertnom otapalu
[image]
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15201240 | 2015-12-18 | ||
| EP16812961.7A EP3389727B1 (en) | 2015-12-18 | 2016-12-16 | Radiolabelled mglur2/3 pet ligands |
| PCT/EP2016/081542 WO2017103182A1 (en) | 2015-12-18 | 2016-12-16 | Radiolabelled mglur2/3 pet ligands |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20201372T1 true HRP20201372T1 (hr) | 2020-11-27 |
Family
ID=55023944
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20201372TT HRP20201372T1 (hr) | 2015-12-18 | 2020-08-28 | Radioaktivno označeni pet mglur2/3 ligandi |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US11033641B2 (hr) |
| EP (1) | EP3389727B1 (hr) |
| JP (1) | JP6927974B2 (hr) |
| AU (1) | AU2016374571B2 (hr) |
| CA (1) | CA3003998A1 (hr) |
| CY (1) | CY1124935T1 (hr) |
| DK (1) | DK3389727T3 (hr) |
| ES (1) | ES2828976T3 (hr) |
| HR (1) | HRP20201372T1 (hr) |
| HU (1) | HUE050665T2 (hr) |
| LT (1) | LT3389727T (hr) |
| PL (1) | PL3389727T3 (hr) |
| PT (1) | PT3389727T (hr) |
| RS (1) | RS60981B1 (hr) |
| SI (1) | SI3389727T1 (hr) |
| WO (1) | WO2017103182A1 (hr) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JOP20150179B1 (ar) | 2014-08-01 | 2021-08-17 | Janssen Pharmaceutica Nv | مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2 |
| JOP20150177B1 (ar) | 2014-08-01 | 2021-08-17 | Janssen Pharmaceutica Nv | مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2 |
| US10967078B2 (en) | 2014-12-03 | 2021-04-06 | Janssen Pharmaceutica Nv | Radiolabelled mGluR2 PET ligands |
| CA2967153A1 (en) | 2014-12-03 | 2016-06-09 | Janssen Pharmaceutica Nv | 6,7-dihydropyrazolo[1,5-.alpha.]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglur2 receptors |
| AU2016374568B2 (en) * | 2015-12-18 | 2020-08-27 | Janssen Pharmaceutica Nv | Radiolabelled mGluR2/3 PET ligands |
| RS60981B1 (sr) | 2015-12-18 | 2020-11-30 | Janssen Pharmaceutica Nv | Radiooznačeni mglur2/3 pet ligandi |
| KR20200090843A (ko) | 2017-11-24 | 2020-07-29 | 다이닛본 스미토모 세이야꾸 가부시끼가이샤 | 6, 7-디히드로 피라졸로[1, 5-a]피라지논 유도체 및 그 의약 용도 |
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| JOP20150179B1 (ar) | 2014-08-01 | 2021-08-17 | Janssen Pharmaceutica Nv | مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2 |
| EP3174884B1 (en) | 2014-08-01 | 2018-09-26 | Janssen Pharmaceutica NV | 6,7-dihydropyrazolo[1,5- ]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglu2 receptors |
| JO3601B1 (ar) * | 2014-08-01 | 2020-07-05 | Janssen Pharmaceutica Nv | مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2 |
| AU2015295300B2 (en) | 2014-08-01 | 2019-05-02 | Janssen Pharmaceutica Nv | 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mGluR2 receptors |
| US10967078B2 (en) | 2014-12-03 | 2021-04-06 | Janssen Pharmaceutica Nv | Radiolabelled mGluR2 PET ligands |
| CA2967153A1 (en) | 2014-12-03 | 2016-06-09 | Janssen Pharmaceutica Nv | 6,7-dihydropyrazolo[1,5-.alpha.]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglur2 receptors |
| JP2016124810A (ja) * | 2014-12-26 | 2016-07-11 | 大日本住友製薬株式会社 | 新規縮合ピラゾール誘導体およびその医薬用途 |
| RS60981B1 (sr) | 2015-12-18 | 2020-11-30 | Janssen Pharmaceutica Nv | Radiooznačeni mglur2/3 pet ligandi |
| AU2016374568B2 (en) * | 2015-12-18 | 2020-08-27 | Janssen Pharmaceutica Nv | Radiolabelled mGluR2/3 PET ligands |
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2016
- 2016-12-16 RS RS20201288A patent/RS60981B1/sr unknown
- 2016-12-16 JP JP2018531628A patent/JP6927974B2/ja active Active
- 2016-12-16 AU AU2016374571A patent/AU2016374571B2/en active Active
- 2016-12-16 ES ES16812961T patent/ES2828976T3/es active Active
- 2016-12-16 PL PL16812961T patent/PL3389727T3/pl unknown
- 2016-12-16 EP EP16812961.7A patent/EP3389727B1/en active Active
- 2016-12-16 SI SI201630916T patent/SI3389727T1/sl unknown
- 2016-12-16 PT PT168129617T patent/PT3389727T/pt unknown
- 2016-12-16 HU HUE16812961A patent/HUE050665T2/hu unknown
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| ES2828976T3 (es) | 2021-05-28 |
| HUE050665T2 (hu) | 2020-12-28 |
| CA3003998A1 (en) | 2017-06-22 |
| CY1124935T1 (el) | 2022-07-22 |
| JP6927974B2 (ja) | 2021-09-01 |
| LT3389727T (lt) | 2020-10-12 |
| JP2019502700A (ja) | 2019-01-31 |
| US11033641B2 (en) | 2021-06-15 |
| AU2016374571B2 (en) | 2021-05-06 |
| WO2017103182A1 (en) | 2017-06-22 |
| US20200306389A1 (en) | 2020-10-01 |
| SI3389727T1 (sl) | 2020-10-30 |
| PT3389727T (pt) | 2020-10-30 |
| RS60981B1 (sr) | 2020-11-30 |
| EP3389727B1 (en) | 2020-08-12 |
| EP3389727A1 (en) | 2018-10-24 |
| PL3389727T3 (pl) | 2021-02-08 |
| DK3389727T3 (da) | 2020-11-02 |
| AU2016374571A1 (en) | 2018-05-17 |
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