KR20230121780A - Sars-cov-2 mpro 억제제 화합물 - Google Patents
Sars-cov-2 mpro 억제제 화합물 Download PDFInfo
- Publication number
- KR20230121780A KR20230121780A KR1020237022567A KR20237022567A KR20230121780A KR 20230121780 A KR20230121780 A KR 20230121780A KR 1020237022567 A KR1020237022567 A KR 1020237022567A KR 20237022567 A KR20237022567 A KR 20237022567A KR 20230121780 A KR20230121780 A KR 20230121780A
- Authority
- KR
- South Korea
- Prior art keywords
- oxopyrrolidin
- dioxo
- butan
- cyclopropylamino
- dimethylpentanamide
- 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 title claims abstract description 201
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- 101500025527 Severe acute respiratory syndrome coronavirus 2 3C-like proteinase nsp5 Proteins 0.000 title claims description 19
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- 101800000535 3C-like proteinase Proteins 0.000 claims abstract description 19
- 101800002396 3C-like proteinase nsp5 Proteins 0.000 claims abstract description 19
- 125000001153 fluoro group Chemical group F* 0.000 claims description 157
- 125000000217 alkyl group Chemical group 0.000 claims description 85
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/24—Oxygen or sulfur atoms
- C07D207/26—2-Pyrrolidones
- C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
- C07D207/267—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to the ring nitrogen atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4015—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
- C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/572—Five-membered rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
- C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
- C07C2601/16—Systems containing only non-condensed rings with a six-membered ring the ring being unsaturated
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Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB2020190.1 | 2020-12-18 | ||
| GBGB2020190.1A GB202020190D0 (en) | 2020-12-18 | 2020-12-18 | Sars-Cov-2 MPRO inhibitor compounds |
| GBGB2107385.3A GB202107385D0 (en) | 2021-05-24 | 2021-05-24 | Sars-cov-2 mpro inhibitor compounds |
| GB2107385.3 | 2021-05-24 | ||
| PCT/GB2021/053374 WO2022129953A1 (en) | 2020-12-18 | 2021-12-20 | Sars-cov-2 mpro inhibitor compounds |
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| KR20230121780A true KR20230121780A (ko) | 2023-08-21 |
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| KR1020237022567A Pending KR20230121780A (ko) | 2020-12-18 | 2021-12-20 | Sars-cov-2 mpro 억제제 화합물 |
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| IL (1) | IL303757A (cg-RX-API-DMAC7.html) |
| WO (1) | WO2022129953A1 (cg-RX-API-DMAC7.html) |
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| EP4545075A1 (en) * | 2022-06-23 | 2025-04-30 | Goryo Chemical, Inc. | Calpain inhibitor |
| CN115073347B (zh) * | 2022-07-14 | 2024-07-30 | 浙江江北药业有限公司 | 一种内酰胺环类医药中间体的制备方法 |
| WO2024102455A1 (en) * | 2022-11-09 | 2024-05-16 | Emory University | Non-covalent inhibitors of coronavirus main protease |
| CN116535460A (zh) * | 2023-04-28 | 2023-08-04 | 中国人民解放军军事科学院军事医学研究院 | 一类含硫拟肽类化合物及其制备方法和用途 |
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| US5763576A (en) * | 1995-10-06 | 1998-06-09 | Georgia Tech Research Corp. | Tetrapeptide α-ketoamides |
| SK6572000A3 (en) * | 1997-11-05 | 2000-10-09 | Novartis Ag | Dipeptide nitriles, process for the preparation thereof, their use as medicaments and pharmaceutical composition comprising them |
| WO2004093860A1 (en) * | 2003-04-21 | 2004-11-04 | Pfizer Inc. | Inhibitors of sars related coronavirus proteinase |
| WO2005113580A1 (en) * | 2004-05-21 | 2005-12-01 | Pfizer Inc. | Anticoronviral compounds and compositions, their pharmaceutical uses and materials for their synthesis |
| CN100363346C (zh) * | 2004-10-22 | 2008-01-23 | 清华大学 | 冠状病毒主蛋白酶的小分子抑制剂、制备方法及其应用 |
| WO2006061714A2 (en) * | 2004-12-09 | 2006-06-15 | Pfizer Inc. | Anticoronaviral compounds and compositions, their pharmaceutical uses and materials for their synthesis |
| 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 |
| CN103145608B (zh) * | 2011-12-07 | 2015-09-02 | 南开大学 | 抗肠病毒71(ev71)己内酰胺类化合物及其制备方法和用途 |
| TW201817714A (zh) * | 2016-08-30 | 2018-05-16 | 英商葛蘭素史密斯克藍智慧財產權有限公司 | 抑制3c及3cl蛋白酶之化合物及其使用方法 |
| 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 |
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2021
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- 2021-12-20 JP JP2023537316A patent/JP2024500136A/ja active Pending
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- 2021-12-20 CA CA3204314A patent/CA3204314A1/en active Pending
- 2021-12-20 AU AU2021402179A patent/AU2021402179A1/en not_active Abandoned
- 2021-12-20 IL IL303757A patent/IL303757A/en unknown
- 2021-12-20 WO PCT/GB2021/053374 patent/WO2022129953A1/en not_active Ceased
- 2021-12-20 EP EP21839626.5A patent/EP4263502B1/en active Active
Also Published As
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|---|---|
| EP4263502C0 (en) | 2024-12-25 |
| US20240083845A1 (en) | 2024-03-14 |
| IL303757A (en) | 2023-08-01 |
| EP4263502A1 (en) | 2023-10-25 |
| WO2022129953A1 (en) | 2022-06-23 |
| CA3204314A1 (en) | 2022-06-23 |
| JP2024500136A (ja) | 2024-01-04 |
| AU2021402179A9 (en) | 2024-09-26 |
| AU2021402179A1 (en) | 2023-07-06 |
| EP4263502B1 (en) | 2024-12-25 |
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