JP2014515364A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2014515364A5 JP2014515364A5 JP2014511862A JP2014511862A JP2014515364A5 JP 2014515364 A5 JP2014515364 A5 JP 2014515364A5 JP 2014511862 A JP2014511862 A JP 2014511862A JP 2014511862 A JP2014511862 A JP 2014511862A JP 2014515364 A5 JP2014515364 A5 JP 2014515364A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- cycloalkyl
- phenyl
- alkoxy
- substituted
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 claims 173
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 43
- 125000003545 alkoxy group Chemical group 0.000 claims 27
- 239000003112 inhibitor Substances 0.000 claims 27
- 125000004452 carbocyclyl group Chemical group 0.000 claims 25
- 229910052736 halogen Inorganic materials 0.000 claims 23
- 150000002367 halogens Chemical class 0.000 claims 23
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 22
- 150000001875 compounds Chemical class 0.000 claims 22
- 125000000753 cycloalkyl group Chemical group 0.000 claims 22
- 125000001072 heteroaryl group Chemical group 0.000 claims 21
- 125000000623 heterocyclic group Chemical group 0.000 claims 19
- -1 cyano, hydroxyl Chemical group 0.000 claims 13
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 12
- 125000003118 aryl group Chemical group 0.000 claims 12
- 238000001514 detection method Methods 0.000 claims 12
- 238000000034 method Methods 0.000 claims 12
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 10
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 10
- 125000003302 alkenyloxy group Chemical group 0.000 claims 10
- 125000005133 alkynyloxy group Chemical group 0.000 claims 10
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 10
- 125000004001 thioalkyl group Chemical group 0.000 claims 10
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 9
- 208000012902 Nervous system disease Diseases 0.000 claims 8
- 208000025966 Neurological disease Diseases 0.000 claims 7
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims 6
- 125000004043 oxo group Chemical group O=* 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 208000024827 Alzheimer disease Diseases 0.000 claims 4
- 208000037259 Amyloid Plaque Diseases 0.000 claims 4
- 125000002877 alkyl aryl group Chemical group 0.000 claims 4
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 125000002950 monocyclic group Chemical group 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000012453 solvate Substances 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 210000005013 brain tissue Anatomy 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 239000012216 imaging agent Substances 0.000 claims 3
- 238000003384 imaging method Methods 0.000 claims 3
- 210000002682 neurofibrillary tangle Anatomy 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 102000013498 tau Proteins Human genes 0.000 claims 3
- 108010026424 tau Proteins Proteins 0.000 claims 3
- 210000001519 tissue Anatomy 0.000 claims 3
- 208000023697 ABri amyloidosis Diseases 0.000 claims 2
- 208000017227 ADan amyloidosis Diseases 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 201000010374 Down Syndrome Diseases 0.000 claims 2
- 208000023105 Huntington disease Diseases 0.000 claims 2
- 201000000162 ITM2B-related cerebral amyloid angiopathy 1 Diseases 0.000 claims 2
- 201000000194 ITM2B-related cerebral amyloid angiopathy 2 Diseases 0.000 claims 2
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 claims 2
- 208000010877 cognitive disease Diseases 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 238000000338 in vitro Methods 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 208000027061 mild cognitive impairment Diseases 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- RGICCULPCWNRAB-UHFFFAOYSA-N 2-[2-(2-hexoxyethoxy)ethoxy]ethanol Chemical compound CCCCCCOCCOCCOCCO RGICCULPCWNRAB-UHFFFAOYSA-N 0.000 claims 1
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 1
- YZCKVEUIGOORGS-NJFSPNSNSA-N Tritium Chemical compound [3H] YZCKVEUIGOORGS-NJFSPNSNSA-N 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 125000000319 biphenyl-4-yl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 229910052805 deuterium Inorganic materials 0.000 claims 1
- 238000001506 fluorescence spectroscopy Methods 0.000 claims 1
- 102000003642 glutaminyl-peptide cyclotransferase Human genes 0.000 claims 1
- 108010081484 glutaminyl-peptide cyclotransferase Proteins 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 238000002595 magnetic resonance imaging Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 1
- 108090000765 processed proteins & peptides Proteins 0.000 claims 1
- 230000002285 radioactive effect Effects 0.000 claims 1
- 238000002603 single-photon emission computed tomography Methods 0.000 claims 1
- 238000004611 spectroscopical analysis Methods 0.000 claims 1
- 229910052722 tritium Inorganic materials 0.000 claims 1
- XHIKZWOEFZENIX-GOSISDBHSA-N CCCOc1ccc([C@@H](CNC2=O)N2c(cc2)cc3c2[nH]cn3)cc1 Chemical compound CCCOc1ccc([C@@H](CNC2=O)N2c(cc2)cc3c2[nH]cn3)cc1 XHIKZWOEFZENIX-GOSISDBHSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161490654P | 2011-05-27 | 2011-05-27 | |
| US61/490,654 | 2011-05-27 | ||
| PCT/EP2012/059649 WO2012163773A1 (en) | 2011-05-27 | 2012-05-24 | Radiolabelled glutaminyl cyclase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014515364A JP2014515364A (ja) | 2014-06-30 |
| JP2014515364A5 true JP2014515364A5 (enExample) | 2015-06-25 |
Family
ID=46149465
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014511862A Pending JP2014515364A (ja) | 2011-05-27 | 2012-05-24 | 放射能標識グルタミニルシクラーゼ阻害剤 |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US8945510B2 (enExample) |
| EP (1) | EP2714098A1 (enExample) |
| JP (1) | JP2014515364A (enExample) |
| KR (1) | KR20140028076A (enExample) |
| CN (1) | CN103561776B (enExample) |
| AU (1) | AU2012264951A1 (enExample) |
| BR (1) | BR112013030341A2 (enExample) |
| CA (1) | CA2835014A1 (enExample) |
| EA (1) | EA028533B1 (enExample) |
| IL (1) | IL229187A (enExample) |
| MX (1) | MX2013013946A (enExample) |
| SG (2) | SG194770A1 (enExample) |
| WO (1) | WO2012163773A1 (enExample) |
| ZA (1) | ZA201308329B (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014140279A1 (en) | 2013-03-15 | 2014-09-18 | Probiodrug Ag | Novel inhibitors |
| CN104230778B (zh) * | 2014-07-14 | 2017-01-04 | 大连大学 | β-烃氧酰基-γ-烃基-N-烃基-γ-丁内酰胺的合成方法 |
| SG11201700777VA (en) | 2014-08-04 | 2017-02-27 | Nuevolution As | Optionally fused heterocyclyl-substituted derivatives of pyrimidine useful for the treatment of inflammatory, metabolic, oncologic and autoimmune diseases |
| US10513515B2 (en) | 2017-08-25 | 2019-12-24 | Biotheryx, Inc. | Ether compounds and uses thereof |
| EP3830093A1 (en) | 2018-07-27 | 2021-06-09 | Biotheryx, Inc. | Bifunctional compounds as cdk modulators |
| KR102230832B1 (ko) * | 2019-06-17 | 2021-03-24 | (주) 메디프론디비티 | N-치환된 티오우레아 또는 우레아 유도체 및 이를 유효성분으로 함유하는 글루타미닐 사이클레이즈 활성 관련 질환의 예방 또는 치료용 약학적 조성물 |
| EP4076657A1 (en) | 2019-12-20 | 2022-10-26 | Nuevolution A/S | Compounds active towards nuclear receptors |
| EP4076661A1 (en) | 2019-12-20 | 2022-10-26 | Nuevolution A/S | Compounds active towards nuclear receptors |
| WO2021198955A1 (en) | 2020-03-31 | 2021-10-07 | Nuevolution A/S | Compounds active towards nuclear receptors |
| EP4126875A1 (en) | 2020-03-31 | 2023-02-08 | Nuevolution A/S | Compounds active towards nuclear receptors |
| US11897930B2 (en) | 2020-04-28 | 2024-02-13 | Anwita Biosciences, Inc. | Interleukin-2 polypeptides and fusion proteins thereof, and their pharmaceutical compositions and therapeutic applications |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT712759A (enExample) | 1963-01-09 | |||
| US5304367A (en) * | 1990-11-16 | 1994-04-19 | New York University | In vivo brain imaging agent and method for diagnosis of psychiatric disorders |
| US7732162B2 (en) * | 2003-05-05 | 2010-06-08 | Probiodrug Ag | Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases |
| KR101099206B1 (ko) * | 2004-02-05 | 2011-12-27 | 프로비오드룩 아게 | 신규한 글루타미닐 시클라제 저해제 |
| US8703096B2 (en) | 2006-04-21 | 2014-04-22 | The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services | Beta-amyloid PET imaging agents |
| WO2008055945A1 (en) * | 2006-11-09 | 2008-05-15 | Probiodrug Ag | 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases |
| NZ590658A (en) * | 2008-07-31 | 2012-07-27 | Probiodrug Ag | Glutaminyl cyclase as a diagnostic / prognostic indicator for neurodegenerative diseases |
| EP2344157B1 (en) | 2008-09-04 | 2016-05-25 | Probiodrug AG | Novel inhibitors |
| EP2411057B1 (en) | 2009-03-23 | 2020-05-06 | Eli Lilly and Company | Imaging agents for detecting neurological disorders |
| ES2548913T3 (es) * | 2009-09-11 | 2015-10-21 | Probiodrug Ag | Derivados heterocíclicos como inhibidores de glutaminil ciclasa |
| CA2789440C (en) | 2010-03-10 | 2020-03-24 | Probiodrug Ag | Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5) |
-
2012
- 2012-05-24 SG SG2013081567A patent/SG194770A1/en unknown
- 2012-05-24 AU AU2012264951A patent/AU2012264951A1/en not_active Abandoned
- 2012-05-24 SG SG10201604304RA patent/SG10201604304RA/en unknown
- 2012-05-24 CN CN201280025603.6A patent/CN103561776B/zh not_active Expired - Fee Related
- 2012-05-24 MX MX2013013946A patent/MX2013013946A/es unknown
- 2012-05-24 US US13/479,826 patent/US8945510B2/en not_active Expired - Fee Related
- 2012-05-24 BR BR112013030341A patent/BR112013030341A2/pt not_active IP Right Cessation
- 2012-05-24 EA EA201301334A patent/EA028533B1/ru not_active IP Right Cessation
- 2012-05-24 EP EP12723476.3A patent/EP2714098A1/en not_active Withdrawn
- 2012-05-24 WO PCT/EP2012/059649 patent/WO2012163773A1/en not_active Ceased
- 2012-05-24 KR KR20137033449A patent/KR20140028076A/ko not_active Withdrawn
- 2012-05-24 JP JP2014511862A patent/JP2014515364A/ja active Pending
- 2012-05-24 CA CA 2835014 patent/CA2835014A1/en not_active Abandoned
-
2013
- 2013-10-31 IL IL229187A patent/IL229187A/en not_active IP Right Cessation
- 2013-11-06 ZA ZA2013/08329A patent/ZA201308329B/en unknown
-
2014
- 2014-12-15 US US14/570,350 patent/US9610368B2/en not_active Expired - Fee Related
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2014515364A5 (enExample) | ||
| JP6681498B2 (ja) | 重水素化ヘテロ環式化合物及びイメージング剤としてのその使用 | |
| JP2009528271A5 (enExample) | ||
| ES2584653T3 (es) | Sonda para la obtención de imágenes de Tau | |
| BRPI0617151B8 (pt) | composto, multímero, composto vetorizado, complexo do referido composto, bem como composições farmacêutica, farmacêutica lipídica e de diagnóstico para imagiologia por ressonância magnética e processo para a preparação de um complexo metálico | |
| MY165906A (en) | Phenothiazine diaminium salts and their use | |
| ES2675301T3 (es) | Heteroarilamidas como inhibidores de la agregación de proteínas | |
| BR112016028345A2 (pt) | composto, composição farmacêutica, métodos para inibir agregação de tau em um mamífero e para avaliar depósitos de tau em um paciente, e, uso de um composto. | |
| JP2019500352A5 (enExample) | ||
| WO2008118122A8 (en) | Compounds and amyloid probes thereof for therapeutic and imaging uses | |
| CA2496633A1 (en) | Diagnostic probes and remedies for diseases with accumulation of prion protein, and stains for prion protein | |
| US20060018825A1 (en) | Probe for diseases with amyloid accumulation, amyloid-staining agent, remedy and preventive for diseases with amyloid accumulation and diagnostic probe and staining agent for neurofibrillary change | |
| JP2018524403A5 (enExample) | ||
| JP2012514007A5 (enExample) | ||
| JP2021508318A5 (enExample) | ||
| JP2013521325A5 (enExample) | ||
| RU2013125326A (ru) | Гетероциклические соединения в качестве зондов для визуализации tau-патологии | |
| JP2014515364A (ja) | 放射能標識グルタミニルシクラーゼ阻害剤 | |
| CA2680157A1 (en) | Novel 2-heteroaryl substituted benzothiophenes and benzofuranes 709 | |
| JP2010520276A5 (enExample) | ||
| AU2004265174A1 (en) | Probe for diseases in which amyloid accumulates, agents for staining amyloid, drugs for treatment and prophylaxis of diseases with accumulated amyloid, and probes for diagnosis of neurofibrillary tangles and agents for staining neurofibrillary tangles. | |
| RU2016112547A (ru) | Имидазо[1,2-а]пиридин-7-амины в качестве средств визуализации | |
| WO2023285661A1 (en) | Novel compounds for the diagnosis of tdp-43 proteinopathies | |
| JP2018520124A5 (enExample) | ||
| Levigoureux et al. | Binding of the PET radiotracer [18F] BF227 does not reflect the presence of alpha-synuclein aggregates in transgenic mice |