JP2017505779A5 - - Google Patents
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- Publication number
- JP2017505779A5 JP2017505779A5 JP2016549488A JP2016549488A JP2017505779A5 JP 2017505779 A5 JP2017505779 A5 JP 2017505779A5 JP 2016549488 A JP2016549488 A JP 2016549488A JP 2016549488 A JP2016549488 A JP 2016549488A JP 2017505779 A5 JP2017505779 A5 JP 2017505779A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- compound
- alkyl
- compound according
- 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.)
- Granted
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- 150000001875 compounds Chemical class 0.000 claims description 40
- 150000003839 salts Chemical class 0.000 claims description 37
- 125000000217 alkyl group Chemical group 0.000 claims description 19
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 18
- 229910052757 nitrogen Inorganic materials 0.000 claims description 14
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 10
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 125000006578 monocyclic heterocycloalkyl group Chemical group 0.000 claims description 6
- 125000002947 alkylene group Chemical group 0.000 claims description 5
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 4
- 238000000034 method Methods 0.000 claims description 4
- 201000010099 disease Diseases 0.000 claims description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 3
- 230000004845 protein aggregation Effects 0.000 claims description 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 9
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 7
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 4
- 125000001153 fluoro group Chemical group F* 0.000 claims 4
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 3
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 3
- 210000004027 cell Anatomy 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 3
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 3
- 208000009829 Lewy Body Disease Diseases 0.000 claims 2
- 201000002832 Lewy body dementia Diseases 0.000 claims 2
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- -1 chloro, bromo, methyl Chemical group 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 108090000765 processed proteins & peptides Proteins 0.000 claims 2
- 102000004169 proteins and genes Human genes 0.000 claims 2
- 108090000623 proteins and genes Proteins 0.000 claims 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- VLLMWSRANPNYQX-UHFFFAOYSA-N thiadiazole Chemical compound C1=CSN=N1.C1=CSN=N1 VLLMWSRANPNYQX-UHFFFAOYSA-N 0.000 claims 2
- NDOVLWQBFFJETK-UHFFFAOYSA-N 1,4-thiazinane 1,1-dioxide Chemical compound O=S1(=O)CCNCC1 NDOVLWQBFFJETK-UHFFFAOYSA-N 0.000 claims 1
- PVOAHINGSUIXLS-UHFFFAOYSA-N 1-Methylpiperazine Chemical compound CN1CCNCC1 PVOAHINGSUIXLS-UHFFFAOYSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims 1
- 239000005977 Ethylene Substances 0.000 claims 1
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 208000001089 Multiple system atrophy Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 1
- 238000009825 accumulation Methods 0.000 claims 1
- 230000002776 aggregation Effects 0.000 claims 1
- 238000004220 aggregation Methods 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- XYOVOXDWRFGKEX-UHFFFAOYSA-N azepine Chemical compound N1C=CC=CC=C1 XYOVOXDWRFGKEX-UHFFFAOYSA-N 0.000 claims 1
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims 1
- 125000001246 bromo group Chemical group Br* 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000002452 interceptive effect Effects 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 150000002780 morpholines Chemical class 0.000 claims 1
- 210000003205 muscle Anatomy 0.000 claims 1
- 102000004196 processed proteins & peptides Human genes 0.000 claims 1
- BRNULMACUQOKMR-UHFFFAOYSA-N thiomorpholine Chemical compound C1CSCCN1 BRNULMACUQOKMR-UHFFFAOYSA-N 0.000 claims 1
- 150000003852 triazoles Chemical class 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 description 2
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461933246P | 2014-01-29 | 2014-01-29 | |
| US61/933,246 | 2014-01-29 | ||
| US201462078895P | 2014-11-12 | 2014-11-12 | |
| US62/078,895 | 2014-11-12 | ||
| PCT/US2015/013263 WO2015116663A1 (en) | 2014-01-29 | 2015-01-28 | Heteroarly amides as inhibitors of protein aggregation |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019104159A Division JP6783900B2 (ja) | 2014-01-29 | 2019-06-04 | タンパク質凝集の阻害剤としてのヘテロアリールアミド |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017505779A JP2017505779A (ja) | 2017-02-23 |
| JP2017505779A5 true JP2017505779A5 (cg-RX-API-DMAC7.html) | 2018-02-22 |
| JP6619741B2 JP6619741B2 (ja) | 2019-12-11 |
Family
ID=52484559
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016549488A Active JP6619741B2 (ja) | 2014-01-29 | 2015-01-28 | タンパク質凝集の阻害剤としてのヘテロアリールアミド |
| JP2019104159A Active JP6783900B2 (ja) | 2014-01-29 | 2019-06-04 | タンパク質凝集の阻害剤としてのヘテロアリールアミド |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019104159A Active JP6783900B2 (ja) | 2014-01-29 | 2019-06-04 | タンパク質凝集の阻害剤としてのヘテロアリールアミド |
Country Status (38)
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE050964T2 (hu) | 2014-01-29 | 2021-01-28 | UCB Biopharma SRL | Heteroaril amidok mint protein aggregáció inhibitorai |
| US10975066B2 (en) | 2015-07-29 | 2021-04-13 | UCB Biopharma SRL | Bis-heteroaryl derivatives as modulators of protein aggregation |
| CN106474121B (zh) * | 2016-11-25 | 2017-10-10 | 刘淑兰 | 一种治疗慢性盆腔炎的药物 |
| EP4467565A3 (en) | 2016-12-21 | 2025-03-12 | Amgen Inc. | Anti-tnf alpha antibody formulations |
| WO2018138088A1 (en) * | 2017-01-26 | 2018-08-02 | Ucb Biopharma Sprl | Bicyclic bis-heteroaryl derivatives as modulators of protein aggregation |
| RU2019126170A (ru) * | 2017-01-26 | 2021-02-26 | Юсб Байофарма Спрл | Бисгетероарильные производные в качестве модуляторов агрегации белков |
| BR112019011931A2 (pt) * | 2017-01-26 | 2019-10-29 | Ucb Biopharma Sprl | derivados de alcóxi bis-heteroarila como moduladores da agregação de proteína |
| CA3062749A1 (en) * | 2017-05-12 | 2018-11-15 | Max-Planck-Gesellschaft Zur Foerderung Der Wissenschaften E.V. | Compounds for use in the treatment or prevention of melanoma |
| CA3108484A1 (en) | 2017-08-04 | 2019-02-07 | Anthony Stewart Campbell | Inhibitors of microbially induced amyloid |
| US20200254068A1 (en) * | 2017-10-31 | 2020-08-13 | Loma Linda University | Methods for treating traumatic brain injury |
| EP3841100A1 (en) | 2018-08-20 | 2021-06-30 | Arvinas Operations, Inc. | Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases |
| US20250074902A1 (en) * | 2021-12-27 | 2025-03-06 | Shanghai Jingxin Biomedical Co., Ltd. | Fused bicyclic heteroaryl amide compound as protein aggregation inhibitor |
| GB202213796D0 (en) * | 2022-09-21 | 2022-11-02 | Wista Lab Ltd | Tau aggregation inhibitors |
| EP4611895A1 (en) * | 2022-11-02 | 2025-09-10 | AC Immune SA | Novel compounds for the diagnosis of tdp-43 proteinopathies |
| WO2024184180A1 (en) | 2023-03-06 | 2024-09-12 | UCB Biopharma SRL | Minzasolmin for use in the treatment of parkinson's disease |
| WO2024184179A1 (en) | 2023-03-06 | 2024-09-12 | UCB Biopharma SRL | Minzasolmin for use in the treatment of parkinson's disease |
| WO2025002040A1 (zh) * | 2023-06-25 | 2025-01-02 | 上海京新生物医药有限公司 | 双环杂芳基酰胺化合物的晶型及盐、制备方法和用途 |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
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| AU1463997A (en) * | 1995-12-22 | 1997-07-17 | Acea Pharmaceuticals, Inc. | Subtype-selective nmda receptor ligands and the use thereof |
| RS20050363A (sr) * | 2002-11-28 | 2007-11-15 | Schering Aktiengesellschaft, | Chk-,Pdk- I Akt-INHIBITORNI PIRIMIDINI, NJIHOVA PROIZVODNJA I UPOTREBA KAO FARMACEUTSKIH SREDSTAVA |
| CN100536837C (zh) * | 2003-02-27 | 2009-09-09 | 乔安妮·麦克劳林 | 鲨肌醇在制备诊断试剂中的用途 |
| TW200530246A (en) * | 2003-12-19 | 2005-09-16 | Bristol Myers Squibb Co | Azabicyclic heterocycles as cannabinoid receptor modulators |
| AU2004309368A1 (en) * | 2003-12-19 | 2005-07-14 | Bristol-Myers Squibb Company | Azabicyclic heterocycles as cannabinoid receptor modulators |
| KR20070018824A (ko) * | 2003-12-19 | 2007-02-14 | 브리스톨-마이어스 스큅 컴퍼니 | 카나비노이드 수용체 조절제인 아자비사이클릭헤테로사이클 |
| KR100859891B1 (ko) * | 2004-08-26 | 2008-09-23 | 화이자 인코포레이티드 | 단백질 키나제 억제제로서 거울상이성질체적으로 순수한아미노헤테로아릴 화합물 |
| EP1797084A1 (en) * | 2004-09-20 | 2007-06-20 | 4Sc Ag | NOVEL HETEROCYCLIC NF-kB INHIBITORS |
| SE0403119D0 (sv) * | 2004-12-21 | 2004-12-21 | Astrazeneca Ab | Therapeutic agents |
| JP2009505948A (ja) * | 2005-07-11 | 2009-02-12 | デブジェン エヌブイ | キナーゼ阻害剤としてのアミド誘導体 |
| WO2007016979A2 (en) * | 2005-07-29 | 2007-02-15 | 4Sc Ag | NOVEL HETEROCYCLIC NF-κB INHIBITORS |
| BRPI0709595A2 (pt) * | 2006-03-15 | 2011-07-19 | 4Sc Ag | inibidores de nf-kapab heterocìclicos |
| EP2081892A4 (en) * | 2006-11-17 | 2014-03-05 | Donald F Weaver | COMPOUNDS AND METHOD FOR THE TREATMENT OF PROTEIN DISAPPEARANCE |
| EP2155226A4 (en) * | 2007-06-14 | 2010-07-28 | Univ California | COMPOUNDS FOR INHIBITING THE PROTEIN AGGREGATION AND METHOD FOR THE PRODUCTION AND USE THEREOF |
| WO2010068452A1 (en) * | 2008-11-25 | 2010-06-17 | Janssen Pharmaceutica Nv | Heteroaryl-substituted urea modulators of fatty acid amide hydrolase |
| GB0910003D0 (en) * | 2009-06-11 | 2009-07-22 | Univ Leuven Kath | Novel compounds for the treatment of neurodegenerative diseases |
| WO2011048525A1 (en) * | 2009-10-20 | 2011-04-28 | Pfizer Inc. | Novel heteroaryl imidazoles and heteroaryl triazoles as gamma-secretase modulators |
| NZ600449A (en) * | 2009-12-16 | 2014-10-31 | Neuropore Therapies Inc | Compound suitable for the treatment of synucleopathies |
| GB201021103D0 (en) * | 2010-12-13 | 2011-01-26 | Univ Leuven Kath | New compounds for the treatment of neurodegenerative diseases |
| WO2013134371A1 (en) | 2012-03-06 | 2013-09-12 | Neuropore Therapies, Inc. | Methods and compounds to be used in the treatment of neurodegenerative diseases |
| RU2014143242A (ru) | 2012-03-28 | 2016-05-20 | Ньюропор Терапис, Инк. | Производные фенилмочевины и фенилкарбаматов в качестве ингибиторов агрегации белка |
| CN104703604A (zh) * | 2012-07-16 | 2015-06-10 | 神经孔疗法股份有限公司 | 作为蛋白质聚集抑制剂的二-和三-杂芳基衍生物 |
| HUE050964T2 (hu) | 2014-01-29 | 2021-01-28 | UCB Biopharma SRL | Heteroaril amidok mint protein aggregáció inhibitorai |
| US10975066B2 (en) | 2015-07-29 | 2021-04-13 | UCB Biopharma SRL | Bis-heteroaryl derivatives as modulators of protein aggregation |
| RU2019126170A (ru) | 2017-01-26 | 2021-02-26 | Юсб Байофарма Спрл | Бисгетероарильные производные в качестве модуляторов агрегации белков |
| WO2018138088A1 (en) | 2017-01-26 | 2018-08-02 | Ucb Biopharma Sprl | Bicyclic bis-heteroaryl derivatives as modulators of protein aggregation |
-
2015
- 2015-01-28 HU HUE18156929A patent/HUE050964T2/hu unknown
- 2015-01-28 CN CN201580017216.1A patent/CN106132960B/zh active Active
- 2015-01-28 EP EP18156929.4A patent/EP3348556B1/en active Active
- 2015-01-28 PE PE2016001285A patent/PE20161393A1/es unknown
- 2015-01-28 BR BR112016017344-9A patent/BR112016017344B1/pt active IP Right Grant
- 2015-01-28 SM SM20180318T patent/SMT201800318T1/it unknown
- 2015-01-28 TR TR2018/09440T patent/TR201809440T4/tr unknown
- 2015-01-28 EP EP15705417.2A patent/EP3099684B8/en active Active
- 2015-01-28 HK HK17105014.2A patent/HK1231470A1/zh unknown
- 2015-01-28 RS RS20200827A patent/RS60547B1/sr unknown
- 2015-01-28 KR KR1020167023810A patent/KR102383038B1/ko active Active
- 2015-01-28 SG SG11201606108RA patent/SG11201606108RA/en unknown
- 2015-01-28 HR HRP20180813TT patent/HRP20180813T1/hr unknown
- 2015-01-28 ES ES18156929T patent/ES2808978T3/es active Active
- 2015-01-28 SI SI201531297T patent/SI3348556T1/sl unknown
- 2015-01-28 MX MX2016009896A patent/MX2016009896A/es active IP Right Grant
- 2015-01-28 HU HUE15705417A patent/HUE040274T2/hu unknown
- 2015-01-28 ME MEP-2020-148A patent/ME03800B/me unknown
- 2015-01-28 BR BR122018001892-5A patent/BR122018001892B1/pt active IP Right Grant
- 2015-01-28 PT PT15705417T patent/PT3099684T/pt unknown
- 2015-01-28 PT PT181569294T patent/PT3348556T/pt unknown
- 2015-01-28 PL PL15705417T patent/PL3099684T3/pl unknown
- 2015-01-28 CA CA2937967A patent/CA2937967C/en active Active
- 2015-01-28 WO PCT/US2015/013263 patent/WO2015116663A1/en not_active Ceased
- 2015-01-28 PL PL18156929T patent/PL3348556T3/pl unknown
- 2015-01-28 EA EA201691529A patent/EA032374B1/ru unknown
- 2015-01-28 AP AP2016009347A patent/AP2016009347A0/en unknown
- 2015-01-28 UA UAA201609003A patent/UA118209C2/uk unknown
- 2015-01-28 LT LTEP15705417.2T patent/LT3099684T/lt unknown
- 2015-01-28 LT LTEP18156929.4T patent/LT3348556T/lt unknown
- 2015-01-28 NZ NZ722487A patent/NZ722487A/en unknown
- 2015-01-28 JP JP2016549488A patent/JP6619741B2/ja active Active
- 2015-01-28 MY MYPI2016001401A patent/MY187450A/en unknown
- 2015-01-28 CN CN201911278647.XA patent/CN111039939B/zh active Active
- 2015-01-28 AU AU2015211119A patent/AU2015211119B2/en active Active
- 2015-01-28 CR CR20160394A patent/CR20160394A/es unknown
- 2015-01-28 ES ES15705417.2T patent/ES2675301T3/es active Active
- 2015-01-28 DK DK15705417.2T patent/DK3099684T3/en active
- 2015-01-28 DK DK18156929.4T patent/DK3348556T3/da active
- 2015-01-28 SI SI201530252T patent/SI3099684T1/en unknown
- 2015-01-28 SM SM20200376T patent/SMT202000376T1/it unknown
- 2015-01-28 RS RS20180644A patent/RS57533B1/sr unknown
- 2015-12-29 US US14/983,243 patent/US9738635B2/en active Active
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2016
- 2016-07-27 IL IL246987A patent/IL246987B/en unknown
- 2016-07-28 SA SA516371579A patent/SA516371579B1/ar unknown
- 2016-07-28 PH PH12016501493A patent/PH12016501493A1/en unknown
- 2016-07-28 CL CL2016001918A patent/CL2016001918A1/es unknown
- 2016-07-28 ZA ZA2016/05246A patent/ZA201605246B/en unknown
- 2016-08-29 EC ECIEPI201670327A patent/ECSP16070327A/es unknown
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2017
- 2017-08-01 US US15/666,503 patent/US10358443B2/en active Active
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2018
- 2018-06-15 CY CY20181100630T patent/CY1120348T1/el unknown
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2019
- 2019-06-04 JP JP2019104159A patent/JP6783900B2/ja active Active
- 2019-06-11 US US16/438,348 patent/US11078196B2/en active Active
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2020
- 2020-07-14 HR HRP20201107TT patent/HRP20201107T8/hr unknown
- 2020-07-24 CY CY20201100682T patent/CY1123374T1/el unknown
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