JPWO2021071802A5 - - Google Patents
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- JPWO2021071802A5 JPWO2021071802A5 JP2022546587A JP2022546587A JPWO2021071802A5 JP WO2021071802 A5 JPWO2021071802 A5 JP WO2021071802A5 JP 2022546587 A JP2022546587 A JP 2022546587A JP 2022546587 A JP2022546587 A JP 2022546587A JP WO2021071802 A5 JPWO2021071802 A5 JP WO2021071802A5
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- JP
- Japan
- Prior art keywords
- alkyl
- optionally substituted
- compound
- occurrence
- formula
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims description 97
- 125000000217 alkyl group Chemical group 0.000 claims description 61
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 33
- 125000000623 heterocyclic group Chemical group 0.000 claims description 30
- 229910052757 nitrogen Inorganic materials 0.000 claims description 26
- 125000001072 heteroaryl group Chemical group 0.000 claims description 22
- 229910052736 halogen Inorganic materials 0.000 claims description 17
- 150000002367 halogens Chemical class 0.000 claims description 17
- 150000003839 salts Chemical class 0.000 claims description 17
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 12
- 125000003118 aryl group Chemical group 0.000 claims description 11
- 229910052739 hydrogen Inorganic materials 0.000 claims description 11
- 125000003107 substituted aryl group Chemical group 0.000 claims description 10
- 241000894007 species Species 0.000 claims description 9
- 208000020832 chronic kidney disease Diseases 0.000 claims description 8
- 125000005842 heteroatom Chemical group 0.000 claims description 8
- 230000002757 inflammatory effect Effects 0.000 claims description 8
- 229910052760 oxygen Inorganic materials 0.000 claims description 8
- 229910052717 sulfur Inorganic materials 0.000 claims description 8
- 229910052799 carbon Inorganic materials 0.000 claims description 7
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 5
- 208000035475 disorder Diseases 0.000 claims description 5
- 208000024827 Alzheimer disease Diseases 0.000 claims description 4
- 208000023275 Autoimmune disease Diseases 0.000 claims description 4
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 4
- 208000032382 Ischaemic stroke Diseases 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- 208000008589 Obesity Diseases 0.000 claims description 4
- 201000004681 Psoriasis Diseases 0.000 claims description 4
- 201000002661 Spondylitis Diseases 0.000 claims description 4
- 206010052779 Transplant rejections Diseases 0.000 claims description 4
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 125000004432 carbon atom Chemical group C* 0.000 claims description 4
- 208000015114 central nervous system disease Diseases 0.000 claims description 4
- 208000022831 chronic renal failure syndrome Diseases 0.000 claims description 4
- 208000026278 immune system disease Diseases 0.000 claims description 4
- 208000027866 inflammatory disease Diseases 0.000 claims description 4
- 208000017169 kidney disease Diseases 0.000 claims description 4
- 208000030159 metabolic disease Diseases 0.000 claims description 4
- 201000006417 multiple sclerosis Diseases 0.000 claims description 4
- 201000001119 neuropathy Diseases 0.000 claims description 4
- 230000007823 neuropathy Effects 0.000 claims description 4
- 235000020824 obesity Nutrition 0.000 claims description 4
- 201000001245 periodontitis Diseases 0.000 claims description 4
- 208000033808 peripheral neuropathy Diseases 0.000 claims description 4
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 4
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims description 4
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 4
- 208000012902 Nervous system disease Diseases 0.000 claims description 3
- 206010009900 Colitis ulcerative Diseases 0.000 claims description 2
- 208000011231 Crohn disease Diseases 0.000 claims description 2
- 206010018367 Glomerulonephritis chronic Diseases 0.000 claims description 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims description 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims description 2
- 125000003342 alkenyl group Chemical group 0.000 claims description 2
- 206010003246 arthritis Diseases 0.000 claims description 2
- 125000004122 cyclic group Chemical group 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 201000008383 nephritis Diseases 0.000 claims description 2
- 125000006413 ring segment Chemical group 0.000 claims description 2
- -1 2-(2-ethoxy-1-naphthalenyl)tetrahydro-2-furancarboxylic acid Chemical compound 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 description 9
- 229910052794 bromium Inorganic materials 0.000 description 3
- 229910052731 fluorine Inorganic materials 0.000 description 3
- 108010027296 Kv1.3 Potassium Channel Proteins 0.000 description 1
- 102000018706 Kv1.3 Potassium Channel Human genes 0.000 description 1
- 230000000903 blocking effect Effects 0.000 description 1
- 125000004093 cyano group Chemical group *C#N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962911670P | 2019-10-07 | 2019-10-07 | |
| US62/911,670 | 2019-10-07 | ||
| PCT/US2020/054347 WO2021071802A1 (en) | 2019-10-07 | 2020-10-06 | Aryl heterocyclic compounds as kv1.3 potassium shaker channel blockers |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2025136895A Division JP2025186255A (ja) | 2019-10-07 | 2025-08-20 | Ｋｖ１．３カリウムシェーカーチャネル遮断薬としてのアリール複素環式化合物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2022550640A JP2022550640A (ja) | 2022-12-02 |
| JPWO2021071802A5 true JPWO2021071802A5 (enExample) | 2024-09-10 |
Family
ID=75438323
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022546587A Pending JP2022550640A (ja) | 2019-10-07 | 2020-10-06 | Ｋｖ１．３カリウムシェーカーチャネル遮断薬としてのアリール複素環式化合物 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20230026611A1 (enExample) |
| EP (1) | EP4041407A4 (enExample) |
| JP (1) | JP2022550640A (enExample) |
| KR (1) | KR20220079882A (enExample) |
| CN (1) | CN114746151A (enExample) |
| AU (1) | AU2020362108A1 (enExample) |
| BR (1) | BR112022006202A2 (enExample) |
| CA (1) | CA3156980A1 (enExample) |
| IL (1) | IL291868A (enExample) |
| MX (1) | MX2022004127A (enExample) |
| WO (1) | WO2021071802A1 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112023005387A2 (pt) * | 2020-10-06 | 2023-04-25 | De Shaw Res Llc | Compostos lactam como bloqueadores de canais agitadores de potássio kv1.3 |
| TW202304875A (zh) * | 2021-03-30 | 2023-02-01 | 美商Ｄ Ｅ 蕭爾研究有限公司 | 做為Kv1.3鉀SHAKER通道阻斷劑之芳基雜環化合物 |
| US20240391926A1 (en) * | 2021-05-28 | 2024-11-28 | D.E. Shaw Research, Llc | SPIROINDOLINONE COMPOUNDS AS Kv1.3 POTASSIUM SHAKER CHANNEL BLOCKERS |
| CN113637002B (zh) * | 2021-08-02 | 2022-09-30 | 天津太平洋化学制药有限公司 | 一种尼拉帕尼的制备方法 |
| CN113603573A (zh) * | 2021-08-09 | 2021-11-05 | 苏州求索生物科技有限公司 | 一种3,5-二氯-2-碘苯甲醚的制备工艺 |
| CN114213315A (zh) * | 2021-12-31 | 2022-03-22 | 上海陶术生物科技有限公司 | 含氮杂环类化合物及其中间体的合成方法 |
| CN114524800A (zh) * | 2022-01-20 | 2022-05-24 | 上海陶术生物科技有限公司 | 尼拉帕尼中间体的合成方法 |
| AU2023370498A1 (en) * | 2022-10-28 | 2025-05-15 | Shanghai Shenshi Wise Technology Co., Ltd. | Aryl heterocyclic kv1.3 inhibitor, preparation method therefor, and use thereof |
| WO2025021167A1 (zh) * | 2023-07-26 | 2025-01-30 | 上海汇伦医药股份有限公司 | 芳基含氮杂环化合物、药物组合物和应用 |
| TW202521512A (zh) | 2023-07-31 | 2025-06-01 | 美商美國禮來大藥廠 | Kv1.3鉀shaker通道阻斷劑之固體形式及其使用方法 |
| WO2025077671A1 (zh) * | 2023-10-09 | 2025-04-17 | 浙江海正药业股份有限公司 | 多取代芳基类衍生物及其制备方法和用途 |
| CN120383599A (zh) * | 2024-01-29 | 2025-07-29 | 上海深势唯思科技有限责任公司 | 芳基杂环类Kv1.3抑制剂及其制备方法和用途 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2950479A1 (de) * | 1979-12-14 | 1981-06-19 | A. Nattermann & Cie GmbH, 5000 Köln | N-(3-alkylamino-2-hydroxypropoxy-phenyl)-lactame, deren herstellungsverfahren und arzneimitttel auf deren basis |
| JPH07309837A (ja) * | 1993-04-28 | 1995-11-28 | Takeda Chem Ind Ltd | ピリジン誘導体、その製造法および剤 |
| JPH09278757A (ja) * | 1996-04-15 | 1997-10-28 | Takeda Chem Ind Ltd | ヒドラゾン誘導体および剤 |
| TW467902B (en) * | 1996-07-31 | 2001-12-11 | Bristol Myers Squibb Co | Diphenyl heterocycles as potassium channel modulators |
| US5948802A (en) * | 1998-01-29 | 1999-09-07 | Bristol-Myers Squibb Company | Benzoate derivatives of diaryl 1,3,4-oxadiazolone |
| US20040147557A1 (en) * | 2001-01-15 | 2004-07-29 | Anne Bouillot | Aryl piperidine derivatives as inducers of ldl-receptor expression |
| US7223788B2 (en) * | 2003-02-14 | 2007-05-29 | Sanofi-Aventis Deutschland Gmbh | Substituted N-aryl heterocycles, process for their preparation and their use as medicaments |
| US7384930B2 (en) * | 2004-11-03 | 2008-06-10 | Bristol-Myers Squibb Company | Constrained compounds as CGRP-receptor antagonists |
| NZ584480A (en) * | 2007-10-04 | 2011-08-26 | Bionomics Ltd | Novel aryl potassium channel blockers and uses thereof |
| GB0815784D0 (en) * | 2008-08-29 | 2008-10-08 | Xention Ltd | Novel potassium channel blockers |
| GB0909672D0 (en) * | 2009-06-04 | 2009-07-22 | Xention Discovery Ltd | Compounds |
| WO2011073269A1 (en) * | 2009-12-16 | 2011-06-23 | Evotec Ag | Piperidine aryl sulfonamide derivatives as kv1.3 modulators |
| WO2017058716A1 (en) * | 2015-09-28 | 2017-04-06 | Vivace Therapeutics, Inc. | Tricyclic compounds |
| GB201610055D0 (en) * | 2016-06-09 | 2016-07-27 | Galapagos Nv And Laboratoires Servier Les | Novel compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders and osteoarthritis |
| GB201610056D0 (en) * | 2016-06-09 | 2016-07-27 | Galapagos Nv And Laboratoires Servier Les | Novel compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders and osteoarthritis |
| CN109705033B (zh) * | 2019-01-22 | 2021-03-30 | 杭州壹瑞医药科技有限公司 | N-杂芳基磺酰胺类衍生物及制备和应用 |
-
2020
- 2020-10-06 BR BR112022006202A patent/BR112022006202A2/pt not_active IP Right Cessation
- 2020-10-06 JP JP2022546587A patent/JP2022550640A/ja active Pending
- 2020-10-06 EP EP20874180.1A patent/EP4041407A4/en active Pending
- 2020-10-06 CN CN202080084663.XA patent/CN114746151A/zh active Pending
- 2020-10-06 AU AU2020362108A patent/AU2020362108A1/en not_active Abandoned
- 2020-10-06 US US17/766,832 patent/US20230026611A1/en active Pending
- 2020-10-06 WO PCT/US2020/054347 patent/WO2021071802A1/en not_active Ceased
- 2020-10-06 KR KR1020227013513A patent/KR20220079882A/ko not_active Withdrawn
- 2020-10-06 IL IL291868A patent/IL291868A/en unknown
- 2020-10-06 CA CA3156980A patent/CA3156980A1/en active Pending
- 2020-10-06 MX MX2022004127A patent/MX2022004127A/es unknown