JP2014515364A5 - - Google Patents
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- 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) | SG10201604304RA (enExample) |
| WO (1) | WO2012163773A1 (enExample) |
| ZA (1) | ZA201308329B (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6454651B2 (ja) | 2013-03-15 | 2019-01-23 | プロビオドルグ エージー | 新規阻害剤 |
| 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 |
| SG10202006053UA (en) | 2014-08-04 | 2020-07-29 | 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 |
| WO2021124277A1 (en) | 2019-12-20 | 2021-06-24 | Nuevolution A/S | Compounds active towards nuclear receptors |
| CN114728170B (zh) | 2019-12-20 | 2024-03-01 | 纽韦卢森公司 | 对核受体具有活性的化合物 |
| JP7713954B2 (ja) | 2020-03-31 | 2025-07-28 | ヌエヴォリューション・アクティーゼルスカブ | 核内受容体に対して活性な化合物 |
| CA3174252A1 (en) | 2020-03-31 | 2021-10-07 | Nuevolution A/S | Compounds active towards nuclear receptors |
| WO2021222150A2 (en) | 2020-04-28 | 2021-11-04 | 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 |
| AU2005210004B2 (en) * | 2004-02-05 | 2010-10-28 | Probiodrug Ag | Novel inhibitors of glutaminyl cyclase |
| WO2007124345A2 (en) | 2006-04-21 | 2007-11-01 | The Government Of The United States, As Represented By The Secretary Of Health And Human Services | Beta-amyloid pet imaging agents |
| JP5379692B2 (ja) * | 2006-11-09 | 2013-12-25 | プロビオドルグ エージー | 潰瘍、癌及び他の疾患の治療のためのグルタミニルシクラーゼの阻害薬としての３−ヒドロキシ−１，５−ジヒドロ−ピロール−２−オン誘導体 |
| NZ590658A (en) * | 2008-07-31 | 2012-07-27 | Probiodrug Ag | Glutaminyl cyclase as a diagnostic / prognostic indicator for neurodegenerative diseases |
| CN102186475B (zh) | 2008-09-04 | 2016-08-03 | 前体生物药物股份公司 | 新抑制剂 |
| CN102438660A (zh) | 2009-03-23 | 2012-05-02 | 美国西门子医疗解决公司 | 用于检测神经障碍的显像剂 |
| ES2548913T3 (es) * | 2009-09-11 | 2015-10-21 | Probiodrug Ag | Derivados heterocíclicos como inhibidores de glutaminil ciclasa |
| EP2545047B9 (en) | 2010-03-10 | 2015-06-10 | Probiodrug AG | Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5) |
-
2012
- 2012-05-24 KR KR20137033449A patent/KR20140028076A/ko not_active Withdrawn
- 2012-05-24 SG SG10201604304RA patent/SG10201604304RA/en unknown
- 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 US US13/479,826 patent/US8945510B2/en not_active Expired - Fee Related
- 2012-05-24 EP EP12723476.3A patent/EP2714098A1/en not_active Withdrawn
- 2012-05-24 CA CA 2835014 patent/CA2835014A1/en not_active Abandoned
- 2012-05-24 SG SG2013081567A patent/SG194770A1/en unknown
- 2012-05-24 JP JP2014511862A patent/JP2014515364A/ja active Pending
- 2012-05-24 WO PCT/EP2012/059649 patent/WO2012163773A1/en not_active Ceased
- 2012-05-24 CN CN201280025603.6A patent/CN103561776B/zh not_active Expired - Fee Related
- 2012-05-24 AU AU2012264951A patent/AU2012264951A1/en not_active Abandoned
- 2012-05-24 MX MX2013013946A patent/MX2013013946A/es unknown
-
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
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