JPWO2021216195A5 - - Google Patents
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- JPWO2021216195A5 JPWO2021216195A5 JP2022564281A JP2022564281A JPWO2021216195A5 JP WO2021216195 A5 JPWO2021216195 A5 JP WO2021216195A5 JP 2022564281 A JP2022564281 A JP 2022564281A JP 2022564281 A JP2022564281 A JP 2022564281A JP WO2021216195 A5 JPWO2021216195 A5 JP WO2021216195A5
- Authority
- JP
- Japan
- Prior art keywords
- formula
- pharmaceutically acceptable
- acceptable salt
- alkyl
- compound
- 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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- 150000001875 compounds Chemical class 0.000 claims description 102
- 150000003839 salts Chemical class 0.000 claims description 97
- 125000000217 alkyl group Chemical group 0.000 claims description 54
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims description 15
- 125000003545 alkoxy group Chemical group 0.000 claims description 14
- IOJUPLGTWVMSFF-UHFFFAOYSA-N benzothiazole Chemical compound C1=CC=C2SC=NC2=C1 IOJUPLGTWVMSFF-UHFFFAOYSA-N 0.000 claims description 14
- 125000002252 acyl group Chemical group 0.000 claims description 8
- 150000001413 amino acids Chemical group 0.000 claims description 8
- 229910052757 nitrogen Inorganic materials 0.000 claims description 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 8
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims description 7
- 125000000335 thiazolyl group Chemical group 0.000 claims description 7
- 125000003118 aryl group Chemical group 0.000 claims description 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 6
- 125000000623 heterocyclic group Chemical group 0.000 claims description 6
- 229910052760 oxygen Inorganic materials 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- -1 -C(O)NR 2 ) Chemical class 0.000 claims description 5
- BCMCBBGGLRIHSE-UHFFFAOYSA-N 1,3-benzoxazole Chemical compound C1=CC=C2OC=NC2=C1 BCMCBBGGLRIHSE-UHFFFAOYSA-N 0.000 claims description 5
- 201000003176 Severe Acute Respiratory Syndrome Diseases 0.000 claims description 5
- 150000001408 amides Chemical class 0.000 claims description 5
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims description 4
- 230000002209 hydrophobic effect Effects 0.000 claims description 4
- 125000001041 indolyl group Chemical group 0.000 claims description 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 4
- 125000001424 substituent group Chemical group 0.000 claims description 4
- 229910052717 sulfur Inorganic materials 0.000 claims description 4
- 125000003368 amide group Chemical group 0.000 claims description 3
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 3
- BGSRFMFTXMPTSC-UHFFFAOYSA-N 6-fluoro-1,3-benzothiazole Chemical compound FC1=CC=C2N=CSC2=C1 BGSRFMFTXMPTSC-UHFFFAOYSA-N 0.000 claims description 2
- 208000025721 COVID-19 Diseases 0.000 claims description 2
- RDFMDVXONNIGBC-LURJTMIESA-N L-2-aminoheptanoic acid Chemical group CCCCC[C@H](N)C(O)=O RDFMDVXONNIGBC-LURJTMIESA-N 0.000 claims description 2
- SNDPXSYFESPGGJ-BYPYZUCNSA-N L-2-aminopentanoic acid Chemical compound CCC[C@H](N)C(O)=O SNDPXSYFESPGGJ-BYPYZUCNSA-N 0.000 claims description 2
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 claims description 2
- QWCKQJZIFLGMSD-VKHMYHEASA-N L-alpha-aminobutyric acid Chemical compound CC[C@H](N)C(O)=O QWCKQJZIFLGMSD-VKHMYHEASA-N 0.000 claims description 2
- AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 claims description 2
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims description 2
- SNDPXSYFESPGGJ-UHFFFAOYSA-N L-norVal-OH Natural products CCCC(N)C(O)=O SNDPXSYFESPGGJ-UHFFFAOYSA-N 0.000 claims description 2
- LRQKBLKVPFOOQJ-YFKPBYRVSA-N L-norleucine Chemical group CCCC[C@H]([NH3+])C([O-])=O LRQKBLKVPFOOQJ-YFKPBYRVSA-N 0.000 claims description 2
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims description 2
- QIVBCDIJIAJPQS-VIFPVBQESA-N L-tryptophane Chemical compound C1=CC=C2C(C[C@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-VIFPVBQESA-N 0.000 claims description 2
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims description 2
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 claims description 2
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 claims description 2
- QIVBCDIJIAJPQS-UHFFFAOYSA-N Tryptophan Natural products C1=CC=C2C(CC(N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-UHFFFAOYSA-N 0.000 claims description 2
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Natural products CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 claims description 2
- 235000004279 alanine Nutrition 0.000 claims description 2
- 125000003342 alkenyl group Chemical group 0.000 claims description 2
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims description 2
- 125000003282 alkyl amino group Chemical group 0.000 claims description 2
- 125000002877 alkyl aryl group Chemical group 0.000 claims description 2
- 125000004103 aminoalkyl group Chemical group 0.000 claims description 2
- 229910052799 carbon Inorganic materials 0.000 claims description 2
- 125000004432 carbon atom Chemical group C* 0.000 claims description 2
- 125000006310 cycloalkyl amino group Chemical group 0.000 claims description 2
- 125000005843 halogen group Chemical group 0.000 claims description 2
- 125000001072 heteroaryl group Chemical group 0.000 claims description 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 2
- 125000004476 heterocycloamino group Chemical group 0.000 claims description 2
- 229960000310 isoleucine Drugs 0.000 claims description 2
- AGPKZVBTJJNPAG-UHFFFAOYSA-N isoleucine Natural products CCC(C)C(N)C(O)=O AGPKZVBTJJNPAG-UHFFFAOYSA-N 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 claims description 2
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 claims description 2
- 239000004474 valine Substances 0.000 claims description 2
- 230000001154 acute effect Effects 0.000 description 1
- 230000000241 respiratory effect Effects 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2025104709A JP2025134881A (ja) | 2020-04-23 | 2025-06-20 | Ｓａｒｓの治療のための化合物 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063014501P | 2020-04-23 | 2020-04-23 | |
| US63/014,501 | 2020-04-23 | ||
| US202063120079P | 2020-12-01 | 2020-12-01 | |
| US63/120,079 | 2020-12-01 | ||
| PCT/US2021/019285 WO2021216195A1 (en) | 2020-04-23 | 2021-02-23 | Compounds for the treatment of sars |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2025104709A Division JP2025134881A (ja) | 2020-04-23 | 2025-06-20 | Ｓａｒｓの治療のための化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023522990A JP2023522990A (ja) | 2023-06-01 |
| JP2023522990A5 JP2023522990A5 (https=) | 2024-02-14 |
| JPWO2021216195A5 true JPWO2021216195A5 (https=) | 2024-02-14 |
Family
ID=78269813
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022564281A Pending JP2023522990A (ja) | 2020-04-23 | 2021-02-23 | Ｓａｒｓの治療のための化合物 |
| JP2025104709A Pending JP2025134881A (ja) | 2020-04-23 | 2025-06-20 | Ｓａｒｓの治療のための化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2025104709A Pending JP2025134881A (ja) | 2020-04-23 | 2025-06-20 | Ｓａｒｓの治療のための化合物 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20230159516A1 (https=) |
| EP (1) | EP4139280A4 (https=) |
| JP (2) | JP2023522990A (https=) |
| KR (1) | KR20230005240A (https=) |
| CN (1) | CN115667209A (https=) |
| AU (1) | AU2021259145A1 (https=) |
| BR (1) | BR112022021381A2 (https=) |
| CA (1) | CA3176370A1 (https=) |
| MX (1) | MX2022013081A (https=) |
| WO (1) | WO2021216195A1 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11124497B1 (en) | 2020-04-17 | 2021-09-21 | Pardes Biosciences, Inc. | Inhibitors of cysteine proteases and methods of use thereof |
| US11174231B1 (en) | 2020-06-09 | 2021-11-16 | Pardes Biosciences, Inc. | Inhibitors of cysteine proteases and methods of use thereof |
| JP2024102382A (ja) * | 2021-05-18 | 2024-07-31 | 国立研究開発法人国立国際医療研究センター | 抗ウイルス活性等の生理活性を有する化合物 |
| JP2024522990A (ja) * | 2021-06-02 | 2024-06-25 | エイシア セラピューティクス， インコーポレイテッド | 抗ウイルス薬としてのプロテアーゼ阻害剤 |
| WO2022266363A1 (en) * | 2021-06-16 | 2022-12-22 | The Scripps Research Institute | Protease inhibitors for the treatment of coronavirus infections |
| CN114456211B (zh) * | 2021-09-03 | 2024-03-26 | 中国药科大学 | 一种拟肽类化合物及其制备方法和应用 |
| CN115806570B (zh) * | 2021-11-15 | 2023-09-12 | 南京知和医药科技有限公司 | 一种拟肽衍生物及其药物组合物和用途 |
| US20240228535A1 (en) * | 2022-11-22 | 2024-07-11 | Merck Sharp & Dohme Llc | Protease inhibitors for treating or preventing coronavirus infection |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU643141B2 (en) | 1991-03-15 | 1993-11-04 | Amgen, Inc. | Pulmonary administration of granulocyte colony stimulating factor |
| US5451569A (en) | 1994-04-19 | 1995-09-19 | Hong Kong University Of Science And Technology R & D Corporation Limited | Pulmonary drug delivery system |
| PE20020157A1 (es) * | 1999-12-03 | 2002-02-22 | Agouron Pharma | Compuestos derivados de piridona como inhibidores de proteasas de picornaviral 3c, composiciones, sus usos farmaceuticos y materiales para su sintesis |
| WO2004093860A1 (en) * | 2003-04-21 | 2004-11-04 | Pfizer Inc. | Inhibitors of sars related coronavirus proteinase |
| AU2004312547A1 (en) * | 2003-12-31 | 2005-07-21 | Taigen Biotechnology | Protease inhibitors |
| WO2006061714A2 (en) * | 2004-12-09 | 2006-06-15 | Pfizer Inc. | Anticoronaviral compounds and compositions, their pharmaceutical uses and materials for their synthesis |
| US20110269834A1 (en) * | 2008-08-21 | 2011-11-03 | The Board Of Trustees Of The University Of Illinois | Compounds and methods for treating respiratory diseases |
| CN107043334B (zh) * | 2011-06-08 | 2020-06-16 | 日东电工株式会社 | 用于定向药物输送和增强siRNA活性的化合物 |
| CN102838523A (zh) * | 2011-06-23 | 2012-12-26 | 南开大学 | 抗肠病毒71(ev71)戊内酰胺类化合物及其制备方法和用途 |
| CA2850003C (en) * | 2011-09-27 | 2020-01-07 | Kansas State University Research Foundation | Broad-spectrum antivirals against 3c or 3c-like proteases of picornavirus-like supercluster: picornaviruses, caliciviruses and coronaviruses |
| CN103130710B (zh) * | 2011-11-29 | 2015-12-16 | 南开大学 | 抗肠病毒71(ev71)己内酰胺醛类化合物及其制备方法和用途 |
| CN106928206B (zh) * | 2015-12-31 | 2022-02-18 | 中国科学院上海药物研究所 | 醛基类化合物及其制法和用途 |
| CN110818691A (zh) * | 2018-08-09 | 2020-02-21 | 中国科学院上海药物研究所 | 酮酰胺类化合物及其制备方法、药物组合物和用途 |
| GB2595975B (en) * | 2020-06-09 | 2022-12-07 | Pardes Biosciences Inc | Inhibitors of cysteine proteases and methods of use thereof |
-
2021
- 2021-02-23 MX MX2022013081A patent/MX2022013081A/es unknown
- 2021-02-23 WO PCT/US2021/019285 patent/WO2021216195A1/en not_active Ceased
- 2021-02-23 KR KR1020227040414A patent/KR20230005240A/ko active Pending
- 2021-02-23 US US17/996,898 patent/US20230159516A1/en active Pending
- 2021-02-23 BR BR112022021381A patent/BR112022021381A2/pt unknown
- 2021-02-23 EP EP21793587.3A patent/EP4139280A4/en active Pending
- 2021-02-23 CN CN202180029527.5A patent/CN115667209A/zh active Pending
- 2021-02-23 JP JP2022564281A patent/JP2023522990A/ja active Pending
- 2021-02-23 AU AU2021259145A patent/AU2021259145A1/en active Pending
- 2021-02-23 CA CA3176370A patent/CA3176370A1/en active Pending
-
2025
- 2025-06-20 JP JP2025104709A patent/JP2025134881A/ja active Pending
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