HRP20202032T1 - Probe za snimanje huntingtonovog proteina - Google Patents
Probe za snimanje huntingtonovog proteina Download PDFInfo
- Publication number
- HRP20202032T1 HRP20202032T1 HRP20202032TT HRP20202032T HRP20202032T1 HR P20202032 T1 HRP20202032 T1 HR P20202032T1 HR P20202032T T HRP20202032T T HR P20202032TT HR P20202032 T HRP20202032 T HR P20202032T HR P20202032 T1 HRP20202032 T1 HR P20202032T1
- Authority
- HR
- Croatia
- Prior art keywords
- dihydro
- isoindol
- pyridin
- optionally substituted
- methoxy
- Prior art date
Links
- 102000004169 proteins and genes Human genes 0.000 title claims 4
- 108090000623 proteins and genes Proteins 0.000 title claims 4
- 238000003384 imaging method Methods 0.000 title claims 2
- 239000000523 sample Substances 0.000 title 1
- -1 cyano, methyl Chemical group 0.000 claims 19
- 239000003795 chemical substances by application Substances 0.000 claims 10
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 9
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 5
- 150000001875 compounds Chemical class 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical group 0.000 claims 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 5
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 4
- 125000003277 amino group Chemical group 0.000 claims 4
- 239000012216 imaging agent Substances 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 3
- 208000023105 Huntington disease Diseases 0.000 claims 3
- 238000012879 PET imaging Methods 0.000 claims 3
- 230000004770 neurodegeneration Effects 0.000 claims 3
- 208000015122 neurodegenerative disease Diseases 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 238000002600 positron emission tomography Methods 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 2
- HUGKALXNRWBIQE-UHFFFAOYSA-N COC=1C=CC(=NC=1)COC=1C=C2CN(C(C2=CC=1)=O)C1=CC=NC=C1 Chemical compound COC=1C=CC(=NC=1)COC=1C=C2CN(C(C2=CC=1)=O)C1=CC=NC=C1 HUGKALXNRWBIQE-UHFFFAOYSA-N 0.000 claims 2
- REHYONXLVUWYNH-UHFFFAOYSA-N COC=1C=CC(=NC=1)COC=1C=C2CN(CC2=CC=1)C1=C(C=NC=C1)C#N Chemical compound COC=1C=CC(=NC=1)COC=1C=C2CN(CC2=CC=1)C1=C(C=NC=C1)C#N REHYONXLVUWYNH-UHFFFAOYSA-N 0.000 claims 2
- BEDGSVZKCWBILF-UHFFFAOYSA-N COC=1C=CC(=NC=1)COC=1C=C2CN(CC2=CC=1)C1=NC=CC=C1C#N Chemical compound COC=1C=CC(=NC=1)COC=1C=C2CN(CC2=CC=1)C1=NC=CC=C1C#N BEDGSVZKCWBILF-UHFFFAOYSA-N 0.000 claims 2
- KQORCPPKKYMCPM-UHFFFAOYSA-N COC=1C=CC(=NC=1)COC=1C=C2CN(CC2=CC=1)C1=NC=NC=C1C#N Chemical compound COC=1C=CC(=NC=1)COC=1C=C2CN(CC2=CC=1)C1=NC=NC=C1C#N KQORCPPKKYMCPM-UHFFFAOYSA-N 0.000 claims 2
- AMAXXQKKZCHDNG-UHFFFAOYSA-N COC=1C=CC(=NC=1)COC=1C=C2CN(CC2=CC=1)C=1C=CC(N(N=1)C)=O Chemical compound COC=1C=CC(=NC=1)COC=1C=C2CN(CC2=CC=1)C=1C=CC(N(N=1)C)=O AMAXXQKKZCHDNG-UHFFFAOYSA-N 0.000 claims 2
- QRTPOXXFPDZCES-UHFFFAOYSA-N COC=1N=CC(=NC=1)COC=1C=C2CN(CC2=CC=1)C1=CC=NC=C1 Chemical compound COC=1N=CC(=NC=1)COC=1C=C2CN(CC2=CC=1)C1=CC=NC=C1 QRTPOXXFPDZCES-UHFFFAOYSA-N 0.000 claims 2
- VNSRTBKAWDJHOP-UHFFFAOYSA-N N1=CN=CC(=C1)COC=1C=C2CN(CC2=CC=1)C1=C(C=NC=C1)C#N Chemical compound N1=CN=CC(=C1)COC=1C=C2CN(CC2=CC=1)C1=C(C=NC=C1)C#N VNSRTBKAWDJHOP-UHFFFAOYSA-N 0.000 claims 2
- NVXYCFAAMKMACA-UHFFFAOYSA-N N1=CN=CC(=C1)COC=1C=C2CN(CC2=CC=1)C1=NC=CC=C1C#N Chemical compound N1=CN=CC(=C1)COC=1C=C2CN(CC2=CC=1)C1=NC=CC=C1C#N NVXYCFAAMKMACA-UHFFFAOYSA-N 0.000 claims 2
- JWFNVWRPBFZRLQ-UHFFFAOYSA-N OC=1C=CC(=NC=1)COC=1C=C2CN(CC2=CC=1)C1=NC=NC=C1C#N Chemical compound OC=1C=CC(=NC=1)COC=1C=C2CN(CC2=CC=1)C1=NC=NC=C1C#N JWFNVWRPBFZRLQ-UHFFFAOYSA-N 0.000 claims 2
- 208000037273 Pathologic Processes Diseases 0.000 claims 2
- 210000004556 brain Anatomy 0.000 claims 2
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims 2
- 238000002595 magnetic resonance imaging Methods 0.000 claims 2
- 239000000178 monomer Substances 0.000 claims 2
- 230000009054 pathological process Effects 0.000 claims 2
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 2
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- RWEYYSNPCVRJSQ-UHFFFAOYSA-N C(C1=CC=CC=C1)OC=1C=C2CN(CC2=CC=1)C1=NC=NC=C1C#N Chemical compound C(C1=CC=CC=C1)OC=1C=C2CN(CC2=CC=1)C1=NC=NC=C1C#N RWEYYSNPCVRJSQ-UHFFFAOYSA-N 0.000 claims 1
- DCRUQOOGKROGBZ-UHFFFAOYSA-N OC=1C=CC(=NC=1)COC=1C=C2CN(CC2=CC=1)C1=C(C=NC=C1)C#N Chemical compound OC=1C=CC(=NC=1)COC=1C=C2CN(CC2=CC=1)C1=C(C=NC=C1)C#N DCRUQOOGKROGBZ-UHFFFAOYSA-N 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000024777 Prion disease Diseases 0.000 claims 1
- 208000009415 Spinocerebellar Ataxias Diseases 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 210000004227 basal ganglia Anatomy 0.000 claims 1
- 238000002591 computed tomography Methods 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
Classifications
-
- 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
- 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
- A61K51/0446—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- 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
- A61K51/0455—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
- C07D513/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Optics & Photonics (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- Physics & Mathematics (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Investigating Or Analysing Biological Materials (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Magnetic Resonance Imaging Apparatus (AREA)
Claims (15)
1. Sredstvo za snimanje koje sadrži spoj formule I ili njegovu farmaceutski prihvatljivu sol,
[image]
naznačen time da su Z1, Z2, Z3 i Z4 svaki CH;
R1 je odabran iz arila, heteroarila i heterocikloalkenila, od kojih je svaki po izboru supstituiran s jednom ili dvije skupine neovisno odabrane između alkinil, heteroaril, cijano, po izboru supstituiranog amino, halogen, C1-6 alkil i C1-6 alkil supstituiranog s po izboru supstituiranim amino;
L1 je O;
L2 je (CH2)m, gdje je m 0, 1 ili 2;i
R2 je odabran iz arila, arila supstituiranog s hidroksilom ili C1-6 alkoksi, heteroarilom i heteroarilom supstituiranim s hidroksilom ili C1-6 alkoksilom,
R5 je odabran između C1-6 alkila, C1-6 alkoksi, halo i okso (kao supstituent na heterocikloalkilnom prstenu); i
n je 0 ili 1;
pri čemu je spoj formule I, ili njegova farmaceutska prihvatljiva sol obilježen s jednim ili više radionuklida koji emitiraju pozitron.
2. Sredstvo za snimanje prema zahtjevu 1, naznačeno time da je R1 fenil, po izboru supstituiran jednom ili dvije skupine, neovisno odabrane između cijano, po izboru supstituirani amino, halogeni, C1-6 -alkili i po izboru supstituirani amino-supstituirani C1-6 -alkili, gdje je R1, na primjer, fenil izborno supstituiran s jednom ili dvije skupine neovisno odabrane između cijano, metila i metila supstituiranih s amino, (alkil) amino ili (dialkil) amino, gdje je R1, na primjer, 2-cijanofenil.
3. Sredstvo za snimanje u skladu s patentnim zahtjevom 1, naznačeno time da je R1 heteroaril, po izboru supstituiran s jednom ili dvije skupine, neovisno odabrane između alkinil, cijano, izborno supstituirani amino, halogen, C1-6 -alkil i izborno supstituirane amino-supstituirane C1-6 -alkilne skupine,
na primjer, gdje je R1 odabran između piridin-4-il, piridin-2-il, piridin-3-il, pirimidin-4-il, 1,2-dihidropiridin-2-on-3-il, 1H-indazol- 4-il i 1H-indazol-7-il, od kojih je svaki izborno supstituiran s jednom ili dvije skupine, neovisno odabrane između alkinil, cijano, izborno supstituiranih amino, halogena, C1-6 -alkila i skupina odabranih izborno supstituiranih amino-supstituiranih C1-6 -alkila,
gdje je R1 na primjer sastavljen od piridin-4-il, piridin-2-il, piridin-3-il i pirimidin-4-il, svaki izborno supstituiran s jednim ili dva neovisno od alkinil, cijano, po želji supstituirani amino, halogen, C1-6 -alkil i skupine odabrane izbornog supstituiranim amino-supstituiranim C1-6 -alkilom ili gdje je R1 odabran od, na primjer, 5-cijanopirimidin-4-il, piridin-4-il, 5-bromo-1,2-dihidropiridina -2-na-3-il, 3-acet-amidopiridin-4-il, 2-acetamidopiridin-6-il, 3-cijanopiridin-4-il, 3-cijanopiridin-6-il, 3-bromopiridin-4-il , 3-bromo-piridin-2-il, 3-cijanopiridin-2-il, 3-fluoropiridin-4-il, 2-cijanopiridin-4-il, 4-cijanopiridin-3-il i 3-etinilpiridin-4-il je odabrano,
gdje je R1, na primjer, piridin-4-il, 5-cijanopirimidin-4-il ili 3-cijanopiridin-4-il.
4. Sredstvo za snimanje prema zahtjevu 1, naznačeno time da je R1 heterocikloalkenil, izborno supstituiran sa C1-6 alkilom, na primjer, gdje je R1 2,3-dihidropiridazin-6-il izborno supstituiran sa C1-6 alkilom.
5. Sredstvo za snimanje prema bilo kojem od zahtjeva 1 do 4, naznačeno time da m je 1.
6. Sredstvo za snimanje prema zahtjevu 5, naznačeno time da je R2 odabran između arila, arila supstituiranog s hidroksilnom ili C1-6 alkoksi, heteroarilom i heteroarilom supstituiran s hidroksilnom ili C1-6 alkoksi, na primjer, gdje se R2 bira između fenila, piridin-2 -il, pirimidin-5-il, pirazin-2-il i pirimidin-5-il, od kojih je svaki izborno supstituiran s hidroksil ili C1-6 alkoksi.
7. Sredstvo za snimanje prema zahtjevu 1, naznačeno time da je spoj formule I odabran iz
2-{5-[(5-metoksipindin-2-il)metoksi]-2,3-dihidro-1H-izoindol-2-il}piridin-3-karbonitril;
2-[5-(pirimidin-5-ilmetoksi)-2,3-dihidro-lH-izoindol-2-il]piridin-3-karbonitril;
4-{5-[(5-metoksipiridin-2-il)metoksi]-2,3-dihidro-1H-izoindol-2-il}piridin-3-karbonitril;
4-{5-[(5-metoksipiridin-2-il)metoksi]-2,3-dihidro-1H-izoindol-2-il}pirimidin-5-karbonitril;
4-{5-[(5-hidroksipiridin-2-il)metoksi]-2,3-dihidro-1H-izoindol-2-il}piridin-3-karbonitril;
4-[5-(pirimidin-5-ilmetoksi)-2,3-dihidro-lH-izoindol-2-il]piridin-3-karbonitril;
5-[(5-metoksipirazin-2-il)metoksi]-2-(piridin-4-il)-2,3-dihidro-1H-izoindol;
4-[5-(benziloksi)-2,3-dihidro-1H-izoindol-2-il]pirimidin-5-karbonitril;
4-{5-[(5-hidroksipiridin-2-il)metoksi]-2,3-dihidro-1H-izoindol-2-il}pirimidin-5-karbonitril;
6-{5-[(5-metoksipiridin-2-il)metoksi]-2,3-dihidro-1H-izoindol-2-il}-2-metil-2,3-dihidropiridazin-3-on i
5-[(5-metoksipiridin-2-il)metoksi]-2-(piridin-4-il)-2,3-dihidro-1H-izoindol-I-on.
8. Spoj formule I, ili njegova farmaceutski prihvatljiva sol, naznačen time da je odabran iz
2-{5-[(5-metoksipiridin-2-il)metoksi]-2,3-dihidro-1H-izoindol-2-il}piridin-3-karbonitril;
2-[5-(pirimidin-5-ilmetoksi)-2,3-dihidro-1H-izoindol-2-il]piridin-3-karbonitril;
4-{5-[(5-metoksipiridin-2-il)metoksi]-2,3-dihidro-1H-izoindol-2 -il}piridin-3-karbonitril;
4-{5-[(5-metoksipiridin-2-il)metoksi]-2,3-dihidro-1H-izoindol-2-il}pirimidin-5-karbonitril;
4-{5-[(5-hidroksipindin-2-il)metoksi]-2,3-dihidro-1H-izoindol-2-il}piridin-3-karbonitril;
4-[5-(pirimidin-5-ilmetoksi)-2,3-dihidro-1H-izoindol-2-il]piridin-3-karbonitril;
5-[(5-metoksipirazin-2-il)metoksi]-2-(piridin-4-il)-2,3-dihidro-1H-izoindol;
4-[5-(benziloksi)-2,3-dihidro-1H-izoindol-2-il]pirimidin-5-karbonitnle;
4-{5-[(5-hidroksipiridin-2-il)metoksi]-2,3-dihidro-1H-izoindol-2-il}pirimidin-5-karbonitril;
6-{5-[(5-metoksipiridin-2-il)metoksi]-2,3-dihidro-1H-izoindol-2-il}-2-metil-2,3-dihidropiridazin-3-on; i
5-[(5-metoksipiridin-2-il)metoksi]-2-(piridin-4-il)-2,3-dihidro-1H-izoindol-1-on.
9. Sredstvo za snimanje prema bilo kojem od zahtjeva 1 do 7, naznačeno time da spomenuti spoj sadrži jedan ili više radionuklida koji emitiraju pozitrone odabrane iz: 11C, 13N, 15O i 18F.
10. Postupak prikazivanja dijagnostičkih slika kod pojedinca, naznačen time da obuhvaća davanje pojedincu učinkovite količine agensa za slikanje prema bilo kojem od zahtjeva 1 do 7 ili 9 i prikazivanje slike barem dijela pojedinca.
11. Sredstvo za snimanje prema bilo kojem od zahtjeva 1 do 7 ili 9, naznačeno time da se koristi u postupku za prikazivanje dijagnostičkih slika kod pojedinca, koji obuhvaća davanje pojedincu efektivne količine sredstva za obradu slike prema bilo kojem od zahtjeva 1 do 7 ili 9 i najmanje jedne slike dijela pojedinca, pri čemu prikaz slike barem dijela pojedinca predstavlja prikaz slike za otkrivanje prisutnosti ili odsutnosti monomera ili agregata HDT proteina (HTT protein) u mozgu pojedinca i otkrivanje prisutnosti ili Uključuje odsutnost patološkog procesa.
12. Sredstvo za snimanje za uporabu prema zahtjevu 11, naznačeno time da su spomenuti monomeri ili agregati proteina HTT prisutni u bazalnim ganglijima spomenutog mozga spomenutog pojedinca.
13. Sredstvo za snimanje za uporabu prema zahtjevu 11, naznačeno time da je patološki proces neurodegenerativna bolest, na primjer, gdje se neurodegenerativna bolest bira između Alzheimerove bolesti, amiotrofične lateralne skleroze, Huntingtonove bolesti, Parkinsonove bolesti, Prionove bolesti i spinocerebelarnih ataksija, na primjer, gdje je neurodegenerativna bolest Huntingtonova bolest (HD).
14. Postupak prema zahtjevu 10 ili sredstvo za obradu slike za uporabu u skladu s bilo kojim od zahtjeva 11 do 13, naznačeno time da spomenuta učinkovita količina spomenutog sredstva za obradu sadrži od 0,1 do 20 mCi, na primjer, gdje navedena učinkovita količina spomenutog sredstva za obradu sadrži 10 mCi.
15. Postupak prema zahtjevu 10 ili 14, ili sredstvo za obradu slike za uporabu prema bilo kojem od zahtjeva 11 do 14, naznačeno time da navedeno generiranje slike obuhvaća slikanje pozitronske emisijske tomografije (PET) Primjerice, PET snimanje s istodobnom računalnom tomografijom (PET/CT), PET snimanje s istodobnom magnetskom rezonancom (PET/MRI) ili njihova kombinacija, pri čemu navedena generacija slike sadrži PET snimanje.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462043644P | 2014-08-29 | 2014-08-29 | |
| EP15836970.2A EP3186241B1 (en) | 2014-08-29 | 2015-08-28 | Probes for imaging huntington protein |
| PCT/US2015/047396 WO2016033436A1 (en) | 2014-08-29 | 2015-08-28 | Probes for imaging huntingtin protein |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20202032T1 true HRP20202032T1 (hr) | 2021-02-19 |
Family
ID=55400644
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20202032TT HRP20202032T1 (hr) | 2014-08-29 | 2020-12-18 | Probe za snimanje huntingtonovog proteina |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US11071793B2 (hr) |
| EP (1) | EP3186241B1 (hr) |
| JP (3) | JP2017527559A (hr) |
| KR (1) | KR102410760B1 (hr) |
| CN (2) | CN107074817B (hr) |
| AU (1) | AU2015308765B2 (hr) |
| BR (1) | BR112017004136B1 (hr) |
| CA (1) | CA2959531C (hr) |
| DK (1) | DK3186241T3 (hr) |
| EA (1) | EA037275B1 (hr) |
| ES (1) | ES2841746T3 (hr) |
| HR (1) | HRP20202032T1 (hr) |
| HU (1) | HUE052892T2 (hr) |
| IL (1) | IL250805B (hr) |
| MX (2) | MX2017002704A (hr) |
| PL (1) | PL3186241T3 (hr) |
| PT (1) | PT3186241T (hr) |
| SG (1) | SG11201701578YA (hr) |
| SI (1) | SI3186241T1 (hr) |
| WO (1) | WO2016033436A1 (hr) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112017004140B1 (pt) | 2014-08-29 | 2023-01-10 | Chdi Foundation, Inc. | Agente de imagemamento, seu uso e compostos |
| MX2017002705A (es) | 2014-08-29 | 2017-12-20 | Chdi Foundation Inc | Sondas para la proyección de imagen de la proteína huntingtina. |
| AU2015308774B2 (en) | 2014-08-29 | 2020-03-19 | Chdi Foundation, Inc. | Probes for imaging huntingtin protein |
| RU2721419C2 (ru) | 2015-08-28 | 2020-05-19 | СиЭйчДиАй ФАУНДЕЙШН, ИНК. | Зонды визуализации белка гентингтина |
| CA3041038A1 (en) | 2016-09-12 | 2018-03-15 | Numerate, Inc. | Bicyclic compounds useful as gpr120 modulators |
| WO2018049324A1 (en) | 2016-09-12 | 2018-03-15 | Numerate, Inc. | Monocyclic compounds useful as gpr120 modulators |
| US11389438B2 (en) | 2019-02-25 | 2022-07-19 | Chdi Foundation, Inc. | Compounds for targeting mutant huntingtin protein and uses thereof |
| JP2023507185A (ja) * | 2019-12-18 | 2023-02-21 | シーエイチディーアイ ファウンデーション，インコーポレーテッド | ハンチンチンタンパク質をイメージングするための化合物及びプローブ |
| JP2024513913A (ja) * | 2021-04-08 | 2024-03-27 | シーエイチディーアイ ファウンデーション，インコーポレーテッド | ハンチンチンタンパク質をイメージングするためのイソインドリノン化合物及びイメージング剤 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5726197A (en) * | 1992-11-02 | 1998-03-10 | Syntex (U.S.A.) Inc. | Isoindolinyl derivatives |
| PT1192131E (pt) * | 1999-06-10 | 2004-11-30 | Warner Lambert Co | Metodo para inibicao da agergacao de proteinas amiloides e para visualizar depositos amiloides utilizando derivados de isoindolina |
| CA2477903C (en) * | 2002-03-01 | 2010-10-12 | Takeda Chemical Industries, Ltd. | Substituted benzofurans useful as protein kinase b activators |
| US7968569B2 (en) | 2002-05-17 | 2011-06-28 | Celgene Corporation | Methods for treatment of multiple myeloma using 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione |
| US7320992B2 (en) * | 2003-08-25 | 2008-01-22 | Amgen Inc. | Substituted 2,3-dihydro-1h-isoindol-1-one derivatives and methods of use |
| US8110681B2 (en) | 2006-03-17 | 2012-02-07 | The United States Of America As Represented By The Secretary, Department Of Health And Human Services | Compounds for the treatment of spinal muscular atrophy and other uses |
| WO2009042907A1 (en) | 2007-09-27 | 2009-04-02 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Isoindoline compounds for the treatment of spinal muscular atrophy and other uses |
| JP5632612B2 (ja) * | 2007-12-05 | 2014-11-26 | あすか製薬株式会社 | ラクタム化合物又はその塩及びｐｐａｒ活性化剤 |
| WO2010104324A2 (ko) * | 2009-03-10 | 2010-09-16 | 한국과학기술연구원 | 베타-아밀로이드 집적체 및 피브릴에 우수한 결합 친화도를 가지는 할로겐화 이소인돌론 화합물, 및 이의 제조 방법 및 용도 |
| EP2841435B1 (en) | 2012-04-25 | 2017-09-06 | RaQualia Pharma Inc. | Pyrrolopyridinone derivatives as ttx-s blockers |
| CN104903312B (zh) * | 2013-10-07 | 2019-01-29 | 卡德门企业有限公司 | Rho激酶抑制剂 |
| AU2015308774B2 (en) | 2014-08-29 | 2020-03-19 | Chdi Foundation, Inc. | Probes for imaging huntingtin protein |
| MX2017002705A (es) | 2014-08-29 | 2017-12-20 | Chdi Foundation Inc | Sondas para la proyección de imagen de la proteína huntingtina. |
| BR112017004140B1 (pt) | 2014-08-29 | 2023-01-10 | Chdi Foundation, Inc. | Agente de imagemamento, seu uso e compostos |
| RU2721419C2 (ru) | 2015-08-28 | 2020-05-19 | СиЭйчДиАй ФАУНДЕЙШН, ИНК. | Зонды визуализации белка гентингтина |
-
2015
- 2015-08-28 AU AU2015308765A patent/AU2015308765B2/en active Active
- 2015-08-28 PT PT158369702T patent/PT3186241T/pt unknown
- 2015-08-28 MX MX2017002704A patent/MX2017002704A/es unknown
- 2015-08-28 JP JP2017511927A patent/JP2017527559A/ja not_active Ceased
- 2015-08-28 KR KR1020177008418A patent/KR102410760B1/ko active IP Right Grant
- 2015-08-28 EP EP15836970.2A patent/EP3186241B1/en active Active
- 2015-08-28 US US15/507,214 patent/US11071793B2/en active Active
- 2015-08-28 CN CN201580058254.1A patent/CN107074817B/zh active Active
- 2015-08-28 DK DK15836970.2T patent/DK3186241T3/da active
- 2015-08-28 BR BR112017004136-7A patent/BR112017004136B1/pt active IP Right Grant
- 2015-08-28 SG SG11201701578YA patent/SG11201701578YA/en unknown
- 2015-08-28 HU HUE15836970A patent/HUE052892T2/hu unknown
- 2015-08-28 CA CA2959531A patent/CA2959531C/en active Active
- 2015-08-28 WO PCT/US2015/047396 patent/WO2016033436A1/en active Application Filing
- 2015-08-28 ES ES15836970T patent/ES2841746T3/es active Active
- 2015-08-28 CN CN202311625463.2A patent/CN118005611A/zh active Pending
- 2015-08-28 SI SI201531461T patent/SI3186241T1/sl unknown
- 2015-08-28 PL PL15836970T patent/PL3186241T3/pl unknown
- 2015-08-28 EA EA201790432A patent/EA037275B1/ru unknown
-
2017
- 2017-02-27 IL IL250805A patent/IL250805B/en active IP Right Grant
- 2017-02-28 MX MX2021005891A patent/MX2021005891A/es unknown
-
2020
- 2020-02-04 JP JP2020016705A patent/JP6843282B2/ja active Active
- 2020-12-18 HR HRP20202032TT patent/HRP20202032T1/hr unknown
-
2021
- 2021-02-22 JP JP2021026146A patent/JP7042940B2/ja active Active
- 2021-06-21 US US17/353,611 patent/US20210379211A1/en active Pending
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| HRP20202032T1 (hr) | Probe za snimanje huntingtonovog proteina | |
| JP2017527559A5 (hr) | ||
| HRP20211778T1 (hr) | Kontrastna sredstva za slikovnu dijagnostiku huntingtin proteina | |
| HRP20180916T1 (hr) | Inhibitori demetilaze od lsd1 na bazi arilciklopropilamina i njihova medicinska uporaba | |
| JP2017529340A5 (hr) | ||
| HRP20171961T1 (hr) | Kemijski spojevi | |
| HRP20211156T1 (hr) | Kontrastna sredstva za slikovnu dijagnostiku huntingtin proteina | |
| MX2016014615A (es) | Compuestos heterociclicos deuterados y su uso como agentes formadores de imagenes. | |
| JP2016506958A5 (hr) | ||
| JP2016520131A5 (hr) | ||
| JP2018531897A5 (hr) | ||
| HRP20170453T1 (hr) | Sinteza stirilpiridina radioaktivno obilježenih s 18f iz tosilatnih preteča i njihovi stabilni farmaceutski pripravci | |
| HRP20170857T1 (hr) | Derivati stirilpiridina i njihova uporaba za vezanje i snimanje amiloidnih naslaga | |
| BR112016028345A8 (pt) | composto, composição farmacêutica, sal farmaceuticamente aceitável de um composto, e, métodos para inibir agregação de tau em um mamífero e para avaliar depósitos de tau em um paciente | |
| HRP20160447T1 (hr) | Spojevi benzensulfonamid-tiazola i benzensulfonamid-oksazola | |
| MA50918A (fr) | Nouveaux composés de chélate de gadolinium pour une utilisation dans l'imagerie par résonance magnétique | |
| GEP20237479B (en) | Labeled inhibitors of prostate specific membrane antigen (psma), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer | |
| JP2017520540A5 (hr) | ||
| JP2014513694A5 (hr) | ||
| AR042052A1 (es) | Diaminotriazoles utiles como inhibidores de proteinquinasas | |
| RU2016112547A (ru) | Имидазо[1,2-а]пиридин-7-амины в качестве средств визуализации | |
| JP2014510147A5 (hr) | ||
| AR115384A1 (es) | Compuestos de triazolopirimidina y su uso en el tratamiento del cáncer | |
| AR102743A1 (es) | Medios de contraste ir para imágenes por fluorescencia | |
| MX2019004967A (es) | Sales de derivado de indazol y cristales de las mismas. |