HRP20220401T4 - Nova vizualizacijska sredstva za detektiranje neurološke disfunkcije - Google Patents
Nova vizualizacijska sredstva za detektiranje neurološke disfunkcije Download PDFInfo
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- HRP20220401T4 HRP20220401T4 HRP20220401TT HRP20220401T HRP20220401T4 HR P20220401 T4 HRP20220401 T4 HR P20220401T4 HR P20220401T T HRP20220401T T HR P20220401TT HR P20220401 T HRP20220401 T HR P20220401T HR P20220401 T4 HRP20220401 T4 HR P20220401T4
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- 6alkyl
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- 239000012216 imaging agent Substances 0.000 title 1
- 230000009251 neurologic dysfunction Effects 0.000 title 1
- 208000015015 neurological dysfunction Diseases 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 20
- 241000124008 Mammalia Species 0.000 claims 6
- 210000005013 brain tissue Anatomy 0.000 claims 5
- 208000024827 Alzheimer disease Diseases 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- 239000000835 fiber Substances 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 230000008499 blood brain barrier function Effects 0.000 claims 2
- 210000001218 blood-brain barrier Anatomy 0.000 claims 2
- 210000004556 brain Anatomy 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 229920000642 polymer Polymers 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000006652 (C3-C12) cycloalkyl group Chemical group 0.000 claims 1
- LRCFGRPTVXBTCM-UHFFFAOYSA-N 4-methyl-3-(9h-pyrimido[4,5-b]indol-6-yl)aniline Chemical compound CC1=CC=C(N)C=C1C1=CC=C(NC=2C3=CN=CN=2)C3=C1 LRCFGRPTVXBTCM-UHFFFAOYSA-N 0.000 claims 1
- 208000037259 Amyloid Plaque Diseases 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 125000005914 C6-C14 aryloxy group Chemical group 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 claims 1
- 206010034912 Phobia Diseases 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical group 0.000 claims 1
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 1
- 230000000971 hippocampal effect Effects 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 238000003384 imaging method Methods 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- 238000010253 intravenous injection Methods 0.000 claims 1
- 238000012544 monitoring process Methods 0.000 claims 1
- 210000002682 neurofibrillary tangle Anatomy 0.000 claims 1
- 231100000189 neurotoxic Toxicity 0.000 claims 1
- 230000002887 neurotoxic effect Effects 0.000 claims 1
- -1 nitro, hydroxyl Chemical group 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 208000019899 phobic disease Diseases 0.000 claims 1
- 238000002600 positron emission tomography Methods 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 230000002285 radioactive effect Effects 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 238000002603 single-photon emission computed tomography Methods 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 238000012800 visualization Methods 0.000 claims 1
- 238000007794 visualization technique Methods 0.000 claims 1
Classifications
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- 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
-
- 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
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Neurology (AREA)
- General Health & Medical Sciences (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Anesthesiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Child & Adolescent Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Indole Compounds (AREA)
- Quinoline Compounds (AREA)
- Pyrane Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (10)
1. Spoj sljedeće Formule I:
[image]
,
i njegove farmaceutski prihvatljive soli, naznačen time što:
A je N ili CR1; B je N ili CR2, J je N ili CR3, K je N ili CR4; L je N ili CR5; M je N; P je N ili CR7; i Q je N ili CR8; uz uvjet da najviše dva od A, B, J, K, L, M, P, te Q mogu biti N;
X je veza;
svaki od R1, R2, R4, R5, R7, te R8 je neovisno vodik ili se svakog od neovisno bira iz skupine koju čine C1-6-alkil, C3-6cikloalkil, C3-12cikloalkilC1-5alkil, heteroarilC2-5alkoksi, C6-14aril, C6-10arilC1-4alkil, heteroaril, C3-6cikloalkoksi, C3-12cikloalkilC1-5alkoksi, C6-14ariloksi, C6-10arilC1-4alkoksi, heteroariloksi, C1-5alkilNR10C(O)-, (C1-6alkil)2NC(O)CH(C1-5alkil)-, C1-5alkilNR10C(O)O-, C1-5alkilC(O)-, C1-5alkilC(O)O-, C6-10arilC(O)-, te C6-10arilC(O)O-, a R3 se bira iz skupine koju čine C3-6cikloalkil, C3-12cikloalkilC1-5alkil, heteroarilC2-5alkoksi, C6-14aril, C6-10arilC1-4alkil, heteroaril, C3-6cikloalkoksi, C3-12cikloalkilC1-5alkoksi, C6-14ariloksi, C6-10arilC1-4alkoksi, heteroariloksi, C1-5alkilNR10C(O)-, (C1-6alkil)2NC(O)CH(C1-5alkil)-, C1-5alkilNR10C(O)O-, C1-5alkilC(O)-, C1-5alkilC(O)O-, C6-10arilC(O)-, te C6-10arilC(O)O-;
najmanje četiri od R1, R2, R4, R5, R7, te R8 su vodici;
R9 je vodik;
svaki R10 je neovisno H ili C1-6alkil; i
supstituenti na R1, R2, R3, R4, R5, R7 R8 i R10 mogu biti dodatno supstituirani supstituentima koje se bira iz skupine koju čine amino, halogen, cijano, nitro, hidroksil, -SH, -SC1-6alkil, -C(O)NH2, -C(S)NH2, halogenC1-6alkil, perhalogenC1-6alkil, C1-6alkil, C3-6cikloalkil, C3-12cikloalkil, C6-14aril i heteroaril, uz uvjet da spoj Formule I nije 4-metil-3-(9H-pirimido[4,5-b]indol-6-il)anilin.
2. Spoj u skladu s patentnim zahtjevom 1 koji je radioaktivno obilježen, naznačen time što radioaktivni biljeg sadrži radionuklid kojeg se bira iz skupine koju čine 11C, 13N, 15O, 18F, 123I, 124I, 125I, 131I i 77Br, te njegove farmaceutski prihvatljive soli.
3. Spoj u skladu s patentnim zahtjevom 1 ili 2, naznačen time što je namijenjen upotrebi u liječenje bolesti ili stanja kod sisavca kojem je to potrebno, koje se bira iz skupine koju čine anksioznost, depresija, shizofrenija, Alzheimerova bolest, bolesti povezane sa stresom, panika, fobija, opsesivno-kompulzivni poremećaj, pretilost, posttraumatski stresni sindrom ili epilepsija.
4. Farmaceutski pripravak namijenjen vizualizaciji in vivo amiloidnih naslaga, naznačen time što sadrži:
spoj u skladu s patentnim zahtjevom 2; i
farmaceutski prihvatljivi nosač.
5. Spoj ili pripravak u skladu s patentnim zahtjevom 2 ili 4 namijenjeni upotrebi u postupku dijagnosticiranja Alzheimerove bolesti ili sklonosti prema navedenoj bolesti kod sisavca, naznačeni time što se postupak sastoji u:
a. primjeni na sisavcu dijagnostički djelotvorne količine radioaktivno obilježenog spoja ili pripravka u skladu s patentnim zahtjevom 2 ili 4, gdje spoj prolazi krvno-moždanu barijeru i preferencijalno se veže na topljive oligomere, polimere i vlakna AD u moždanom tkivu;
b. omogućavanju raspodjeljivanja spoja u moždanom tkivu; i
c. vizualizaciji moždanog tkiva, gdje pojačano vezanje spoja na moždano tkivo u usporedbi s normalnom kontrolnom razinom vezanja ukazuje da sisavac boluje od ili je u opasnosti od razvoja Alzheimerove bolesti.
6. Spoj ili pripravak u skladu s patentnim zahtjevom 2 ili 4 namijenjeni upotrebi u skladu s patentnim zahtjevom 5, naznačeni time što se spoj preferencijalno veže na vlakna.
7. Spoj ili pripravak u skladu s patentnim zahtjevom 2 ili 4 namijenjeni upotrebi u skladu s patentnim zahtjevom 5, naznačeni time što moždano tkivo sadrži frontotemporalno područje ili hipokampalno područje.
8. Spoj ili pripravak u skladu s patentnim zahtjevom 2 ili 4 namijenjeni upotrebi u skladu s patentnim zahtjevom 5, naznačeni time što je pojačano vezanje najmanje 10% veće od navedene normalne kontrolne vrijednosti.
9. Spoj ili pripravak u skladu s patentnim zahtjevom 2 ili 4 namijenjeni upotrebi u skladu s bilo kojim od patentnih zahtjeva 5 do 8, naznačeni time što se spoj primijenjuje intravenskom injekcijom.
10. Spoj u skladu s patentnim zahtjevom 2 namijenjen upotrebi u postupku dijagnosticiranja Alzheimerove bolesti ili sklonosti prema navedenoj bolesti kod sisavca, naznačen time što se postupak sastoji u:
a. primjeni na sisavcu dijagnostički djelotvorne količine spoja u skladu s patentnim zahtjevom 2, gdje spoj prolazi krvno-moždanu barijeru i preferencijalno se veže na topljive ili netopljive oligomere, polimere, vlakna AD, hiperfosforilirane tau, neurofibrilarna klupka, sparene spiralne filamente i/ili neurotoksične topljive oligomere u mozgu;
b. upotrebi tehnike nuklearne vizualizacije koju se bira iz skupine koju čine pozitronska emisijska tomografija (PET) i jednofotonska emisijska računalna tomografija (SPECT) u praćenju ili visualizaciji raspodjele radioaktivno obilježenog spoja u mozgu ili u njegovom dijelu.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US6610108P | 2008-02-14 | 2008-02-14 | |
| PCT/US2009/000961 WO2009102498A1 (en) | 2008-02-14 | 2009-02-17 | Novel imaging agents for detecting neurological dysfunction |
| EP09711194.2A EP2247558B2 (en) | 2008-02-14 | 2009-02-17 | Novel imaging agents for detecting neurological dysfunction |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HRP20220401T3 HRP20220401T3 (hr) | 2022-05-27 |
| HRP20220401T4 true HRP20220401T4 (hr) | 2024-09-27 |
Family
ID=40627498
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20220401TT HRP20220401T4 (hr) | 2008-02-14 | 2009-02-17 | Nova vizualizacijska sredstva za detektiranje neurološke disfunkcije |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US8318132B2 (hr) |
| EP (2) | EP2247558B2 (hr) |
| JP (1) | JP2011512354A (hr) |
| KR (1) | KR20100135235A (hr) |
| CA (1) | CA2715390A1 (hr) |
| CY (1) | CY1125258T1 (hr) |
| DK (1) | DK2247558T4 (hr) |
| ES (1) | ES2907992T5 (hr) |
| FI (1) | FI2247558T4 (hr) |
| HR (1) | HRP20220401T4 (hr) |
| HU (1) | HUE058352T2 (hr) |
| LT (1) | LT2247558T (hr) |
| PL (1) | PL2247558T5 (hr) |
| PT (1) | PT2247558T (hr) |
| SI (1) | SI2247558T2 (hr) |
| WO (1) | WO2009102498A1 (hr) |
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| PT2247558T (pt) | 2022-03-21 |
| FI2247558T4 (fi) | 2024-09-19 |
| ES2907992T5 (en) | 2025-03-19 |
| KR20100135235A (ko) | 2010-12-24 |
| US20110046378A1 (en) | 2011-02-24 |
| US20110091382A1 (en) | 2011-04-21 |
| PL2247558T5 (pl) | 2024-10-14 |
| EP2247558B1 (en) | 2022-02-02 |
| HUE058352T2 (hu) | 2022-07-28 |
| LT2247558T (lt) | 2022-04-11 |
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| CY1125258T1 (el) | 2024-02-16 |
| DK2247558T3 (da) | 2022-02-21 |
| CA2715390A1 (en) | 2009-08-20 |
| SI2247558T1 (sl) | 2022-07-29 |
| ES2907992T3 (es) | 2022-04-27 |
| EP2599763A1 (en) | 2013-06-05 |
| EP2247558A1 (en) | 2010-11-10 |
| HRP20220401T3 (hr) | 2022-05-27 |
| JP2011512354A (ja) | 2011-04-21 |
| EP2247558B2 (en) | 2024-07-03 |
| DK2247558T4 (da) | 2024-07-29 |
| US8318132B2 (en) | 2012-11-27 |
| PL2247558T3 (pl) | 2022-05-02 |
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