CA2835014A1 - Radiolabelled glutaminyl cyclase inhibitors - Google Patents
Radiolabelled glutaminyl cyclase inhibitors Download PDFInfo
- Publication number
- CA2835014A1 CA2835014A1 CA 2835014 CA2835014A CA2835014A1 CA 2835014 A1 CA2835014 A1 CA 2835014A1 CA 2835014 CA2835014 CA 2835014 CA 2835014 A CA2835014 A CA 2835014A CA 2835014 A1 CA2835014 A1 CA 2835014A1
- Authority
- CA
- Canada
- Prior art keywords
- 4alkyl
- substituted
- 6alkyl
- phenyl
- inhibitor
- 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.)
- Abandoned
Links
- 239000003112 inhibitor Substances 0.000 title claims abstract description 57
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- 238000000034 method Methods 0.000 claims abstract description 49
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- 150000001875 compounds Chemical class 0.000 claims description 149
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 101
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 71
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 52
- 229910052736 halogen Inorganic materials 0.000 claims description 46
- 150000002367 halogens Chemical class 0.000 claims description 46
- 125000001072 heteroaryl group Chemical group 0.000 claims description 42
- 125000000623 heterocyclic group Chemical group 0.000 claims description 40
- -1 cyano, hydroxyl Chemical group 0.000 claims description 36
- 125000003118 aryl group Chemical group 0.000 claims description 24
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 21
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims description 20
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 20
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- 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
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- 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
- A61K51/0453—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A—HUMAN NECESSITIES
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- A61K49/00—Preparations for testing in vivo
- A61K49/06—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
- A61K49/08—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier
- A61K49/10—Organic compounds
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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
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- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
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| PCT/EP2012/059649 WO2012163773A1 (en) | 2011-05-27 | 2012-05-24 | Radiolabelled glutaminyl cyclase inhibitors |
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| 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 |
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| 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 |
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| 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) |
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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
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2013
- 2013-10-31 IL IL229187A patent/IL229187A/en not_active IP Right Cessation
- 2013-11-06 ZA ZA2013/08329A patent/ZA201308329B/en unknown
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2014
- 2014-12-15 US US14/570,350 patent/US9610368B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| JP2014515364A (ja) | 2014-06-30 |
| BR112013030341A2 (pt) | 2016-11-29 |
| CN103561776A (zh) | 2014-02-05 |
| US9610368B2 (en) | 2017-04-04 |
| US8945510B2 (en) | 2015-02-03 |
| EA201301334A1 (ru) | 2014-05-30 |
| SG10201604304RA (en) | 2016-07-28 |
| MX2013013946A (es) | 2014-01-31 |
| IL229187A0 (en) | 2013-12-31 |
| ZA201308329B (en) | 2015-02-25 |
| SG194770A1 (en) | 2013-12-30 |
| KR20140028076A (ko) | 2014-03-07 |
| IL229187A (en) | 2017-04-30 |
| US20120301398A1 (en) | 2012-11-29 |
| WO2012163773A1 (en) | 2012-12-06 |
| EA028533B1 (ru) | 2017-11-30 |
| CN103561776B (zh) | 2016-08-31 |
| NZ617581A (en) | 2016-03-31 |
| US20150104389A1 (en) | 2015-04-16 |
| EP2714098A1 (en) | 2014-04-09 |
| AU2012264951A1 (en) | 2013-12-12 |
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