JPWO2022093552A5 - - Google Patents
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- Publication number
- JPWO2022093552A5 JPWO2022093552A5 JP2023548533A JP2023548533A JPWO2022093552A5 JP WO2022093552 A5 JPWO2022093552 A5 JP WO2022093552A5 JP 2023548533 A JP2023548533 A JP 2023548533A JP 2023548533 A JP2023548533 A JP 2023548533A JP WO2022093552 A5 JPWO2022093552 A5 JP WO2022093552A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- ring
- independently selected
- cycloalkyl
- 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
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- 125000000217 alkyl group Chemical group 0.000 claims description 141
- 229910052739 hydrogen Inorganic materials 0.000 claims description 139
- 150000001875 compounds Chemical class 0.000 claims description 134
- 229910052799 carbon Inorganic materials 0.000 claims description 99
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 92
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 90
- 125000001424 substituent group Chemical group 0.000 claims description 80
- 125000004432 carbon atom Chemical group C* 0.000 claims description 78
- 125000004122 cyclic group Chemical group 0.000 claims description 72
- 229910052736 halogen Inorganic materials 0.000 claims description 69
- 150000002367 halogens Chemical class 0.000 claims description 69
- 125000003545 alkoxy group Chemical group 0.000 claims description 67
- 125000001188 haloalkyl group Chemical group 0.000 claims description 50
- 125000000623 heterocyclic group Chemical group 0.000 claims description 49
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 47
- 125000005842 heteroatom Chemical group 0.000 claims description 43
- 239000001257 hydrogen Substances 0.000 claims description 42
- 150000003839 salts Chemical class 0.000 claims description 40
- 229920006395 saturated elastomer Polymers 0.000 claims description 40
- 150000002431 hydrogen Chemical class 0.000 claims description 37
- 125000003118 aryl group Chemical group 0.000 claims description 35
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 34
- 125000001072 heteroaryl group Chemical group 0.000 claims description 31
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 31
- 125000001624 naphthyl group Chemical group 0.000 claims description 30
- 125000005843 halogen group Chemical group 0.000 claims description 28
- 229910052760 oxygen Inorganic materials 0.000 claims description 28
- 125000003282 alkyl amino group Chemical group 0.000 claims description 27
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 27
- 125000004663 dialkyl amino group Chemical group 0.000 claims description 27
- -1 hydroxy, sulfonyl Chemical group 0.000 claims description 27
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 26
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 22
- 239000012453 solvate Substances 0.000 claims description 20
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 18
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 18
- 229910052717 sulfur Inorganic materials 0.000 claims description 18
- 125000001691 aryl alkyl amino group Chemical group 0.000 claims description 16
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 14
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 12
- 239000008194 pharmaceutical composition Substances 0.000 claims description 10
- 201000010099 disease Diseases 0.000 claims description 9
- 208000035475 disorder Diseases 0.000 claims description 9
- 125000000732 arylene group Chemical group 0.000 claims description 8
- 208000019901 Anxiety disease Diseases 0.000 claims description 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 4
- 208000029578 Muscle disease Diseases 0.000 claims description 4
- 208000021642 Muscular disease Diseases 0.000 claims description 4
- 208000012902 Nervous system disease Diseases 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 3
- 125000003107 substituted aryl group Chemical group 0.000 claims description 3
- 229940124597 therapeutic agent Drugs 0.000 claims description 3
- 208000023275 Autoimmune disease Diseases 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- 208000036110 Neuroinflammatory disease Diseases 0.000 claims description 2
- 208000008589 Obesity Diseases 0.000 claims description 2
- 206010040047 Sepsis Diseases 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 230000036506 anxiety Effects 0.000 claims description 2
- 230000005784 autoimmunity Effects 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 208000037976 chronic inflammation Diseases 0.000 claims description 2
- 230000006020 chronic inflammation Effects 0.000 claims description 2
- 208000010877 cognitive disease Diseases 0.000 claims description 2
- 208000019622 heart disease Diseases 0.000 claims description 2
- 201000006938 muscular dystrophy Diseases 0.000 claims description 2
- 230000003959 neuroinflammation Effects 0.000 claims description 2
- 235000020824 obesity Nutrition 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 208000001076 sarcopenia Diseases 0.000 claims description 2
- 208000019116 sleep disease Diseases 0.000 claims description 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 2
- 125000003368 amide group Chemical group 0.000 claims 5
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 238000000034 method Methods 0.000 description 25
- 108020005497 Nuclear hormone receptor Proteins 0.000 description 22
- 102000007399 Nuclear hormone receptor Human genes 0.000 description 18
- 150000001408 amides Chemical class 0.000 description 10
- 239000000203 mixture Substances 0.000 description 5
- 102000006255 nuclear receptors Human genes 0.000 description 4
- 108020004017 nuclear receptors Proteins 0.000 description 4
- 125000005415 substituted alkoxy group Chemical group 0.000 description 4
- 125000005466 alkylenyl group Chemical group 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 238000001802 infusion Methods 0.000 description 2
- 238000007912 intraperitoneal administration Methods 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 229910052757 nitrogen Inorganic materials 0.000 description 2
- 125000005346 substituted cycloalkyl group Chemical group 0.000 description 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 description 1
- 208000025966 Neurological disease Diseases 0.000 description 1
- 125000001246 bromo group Chemical group Br* 0.000 description 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 125000001153 fluoro group Chemical group F* 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000001361 intraarterial administration Methods 0.000 description 1
- 238000007917 intracranial administration Methods 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 238000007913 intrathecal administration Methods 0.000 description 1
- 230000002601 intratumoral effect Effects 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 230000010412 perfusion Effects 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063092893P | 2020-10-16 | 2020-10-16 | |
| US63/092,893 | 2020-10-16 | ||
| PCT/US2021/055165 WO2022093552A2 (en) | 2020-10-16 | 2021-10-15 | Rev-erb agonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023552490A JP2023552490A (ja) | 2023-12-15 |
| JPWO2022093552A5 true JPWO2022093552A5 (https=) | 2024-10-21 |
| JP2023552490A5 JP2023552490A5 (https=) | 2024-10-21 |
Family
ID=81384462
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023548533A Pending JP2023552490A (ja) | 2020-10-16 | 2021-10-15 | Ｒｅｖ－ｅｒｂアゴニスト |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20240002380A1 (https=) |
| EP (1) | EP4228632A4 (https=) |
| JP (1) | JP2023552490A (https=) |
| CN (1) | CN116635029A (https=) |
| AU (1) | AU2021372389A1 (https=) |
| CA (1) | CA3195127A1 (https=) |
| WO (1) | WO2022093552A2 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114432302B (zh) * | 2020-11-05 | 2024-08-27 | 中国科学院上海营养与健康研究所 | 小分子sr9009在抗衰老以及减轻衰老引起的慢性炎症中的用途 |
| CN114907333B (zh) * | 2022-05-11 | 2023-07-04 | 中国人民解放军军事科学院军事医学研究院 | 环丙甲酰胺衍生物及其制备方法和用途 |
| WO2025024550A1 (en) * | 2023-07-25 | 2025-01-30 | University Of Florida Research Foundation, Incorporated | Rev-erb antagonists |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4472193A (en) * | 1982-07-06 | 1984-09-18 | The Dow Chemical Company | Naphthyridinyloxy(or thio)phenoxy propanoic acids, derivatives thereof and methods of herbicidal use |
| ES2200617B1 (es) * | 2001-01-19 | 2005-05-01 | Almirall Prodesfarma, S.A. | Derivados de urea como antagonistas de integrinas alfa 4. |
| BRPI0718161A2 (pt) * | 2006-10-27 | 2013-11-26 | Merck & Co Inc | Composto, composição farmacêutica, e, uso do composto. |
| WO2008144268A1 (en) * | 2007-05-15 | 2008-11-27 | Boehringer Ingelheim International Gmbh | Urotensin ii receptor antagonists |
| UY31984A (es) * | 2008-07-16 | 2010-02-26 | Boehringer Ingelheim Int | DERIVADOS DE 1-(3,4-difluorobencil)-6-oxo-1,6-dihidropirimidin-5-carboxamidas N-sustituidas y de 2-(3,4-difluorobencil)-3-oxo-2,3-dihidro-1H-pirazol-4-carboxamidas N-sustituidas. |
| TW201026667A (en) * | 2008-09-30 | 2010-07-16 | Merz Pharma Gmbh & Co Kgaa | Glycine b antagonists |
| EP2417133A1 (en) * | 2009-04-06 | 2012-02-15 | PTC Therapeutics, Inc. | Compounds and methods for antiviral treatment |
| AU2011253058A1 (en) * | 2010-05-13 | 2012-12-06 | Amgen Inc. | Heteroaryloxycarbocyclyl compounds as PDE10 inhibitors |
| WO2013033310A1 (en) * | 2011-08-31 | 2013-03-07 | Theodore Mark Kamenecka | Modulators of rev-erb |
| US9586963B2 (en) * | 2011-09-27 | 2017-03-07 | Genfit | Derivatives of 6-substituted triazolopyridazines as Rev-Erb agonists |
| US9266876B2 (en) * | 2012-02-02 | 2016-02-23 | Actelion Pharmaceuticals Ltd. | 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives |
| TW201348231A (zh) * | 2012-02-29 | 2013-12-01 | Amgen Inc | 雜雙環化合物 |
| ES2618004T3 (es) * | 2012-08-07 | 2017-06-20 | Merck Patent Gmbh | Derivados de piridopirimidina como inhibidores de proteínas quinasas |
| JP2016505000A (ja) * | 2012-12-21 | 2016-02-18 | エピザイム，インコーポレイティド | Ｐｒｍｔ５阻害剤およびその使用 |
| WO2015103527A1 (en) * | 2014-01-06 | 2015-07-09 | The Scripps Research Institute | Modulators of rev-erb |
| ES2735087T3 (es) * | 2014-12-24 | 2019-12-16 | Gilead Sciences Inc | Compuestos de pirimidina fusionados para el tratamiento de VIH |
| US11066396B2 (en) * | 2016-06-23 | 2021-07-20 | Merck Sharp & Dohme Corp. | 3-aryl- heteroaryl substituted 5-trifluoromethyl oxadiazoles as histonedeacetylase 6 (HDAC6) inhibitors |
| CN109776335B (zh) * | 2017-11-15 | 2022-03-18 | 武汉尚赛光电科技有限公司 | 芘的胺类衍生物及其制备方法、应用和器件 |
| GB201810486D0 (en) * | 2018-06-26 | 2018-08-08 | Imperial Innovations Ltd | Natural killer cells |
-
2021
- 2021-10-15 EP EP21887190.3A patent/EP4228632A4/en not_active Withdrawn
- 2021-10-15 CA CA3195127A patent/CA3195127A1/en active Pending
- 2021-10-15 JP JP2023548533A patent/JP2023552490A/ja active Pending
- 2021-10-15 CN CN202180076854.6A patent/CN116635029A/zh active Pending
- 2021-10-15 WO PCT/US2021/055165 patent/WO2022093552A2/en not_active Ceased
- 2021-10-15 AU AU2021372389A patent/AU2021372389A1/en not_active Abandoned
-
2023
- 2023-04-13 US US18/134,055 patent/US20240002380A1/en active Pending
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