JPWO2022234853A5 - - Google Patents
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- Publication number
- JPWO2022234853A5 JPWO2022234853A5 JP2023518700A JP2023518700A JPWO2022234853A5 JP WO2022234853 A5 JPWO2022234853 A5 JP WO2022234853A5 JP 2023518700 A JP2023518700 A JP 2023518700A JP 2023518700 A JP2023518700 A JP 2023518700A JP WO2022234853 A5 JPWO2022234853 A5 JP WO2022234853A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- hydrogen
- membered
- group
- alkylene
- 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
Links
- 229910052739 hydrogen Inorganic materials 0.000 claims 83
- 239000001257 hydrogen Substances 0.000 claims 83
- 125000000623 heterocyclic group Chemical group 0.000 claims 61
- 229910052736 halogen Inorganic materials 0.000 claims 54
- 150000002367 halogens Chemical class 0.000 claims 53
- 125000004432 carbon atom Chemical group C* 0.000 claims 49
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 48
- 229910052799 carbon Inorganic materials 0.000 claims 44
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 39
- 150000002431 hydrogen Chemical class 0.000 claims 31
- 125000002723 alicyclic group Chemical group 0.000 claims 29
- -1 C 1 -C 6 alkoxy Chemical group 0.000 claims 27
- 229910052757 nitrogen Inorganic materials 0.000 claims 25
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 22
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 22
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 20
- 125000003710 aryl alkyl group Chemical group 0.000 claims 20
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 19
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 19
- 150000003839 salts Chemical class 0.000 claims 18
- 239000012453 solvate Substances 0.000 claims 18
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 15
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 15
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 14
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 13
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 11
- 150000001923 cyclic compounds Chemical class 0.000 claims 10
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 9
- 108010038807 Oligopeptides Proteins 0.000 claims 9
- 102000015636 Oligopeptides Human genes 0.000 claims 9
- 150000001875 compounds Chemical class 0.000 claims 9
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 8
- 125000004450 alkenylene group Chemical group 0.000 claims 7
- 125000000539 amino acid group Chemical group 0.000 claims 7
- 125000000732 arylene group Chemical group 0.000 claims 7
- 125000004093 cyano group Chemical group *C#N 0.000 claims 7
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 7
- 108090000765 processed proteins & peptides Proteins 0.000 claims 7
- 125000006832 (C1-C10) alkylene group Chemical group 0.000 claims 6
- 125000003320 C2-C6 alkenyloxy group Chemical group 0.000 claims 6
- 125000004406 C3-C8 cycloalkylene group Chemical group 0.000 claims 6
- 125000004419 alkynylene group Chemical group 0.000 claims 6
- 125000005842 heteroatom Chemical group 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 5
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 5
- 125000002947 alkylene group Chemical group 0.000 claims 5
- 239000011347 resin Substances 0.000 claims 5
- 229920005989 resin Polymers 0.000 claims 5
- 238000010532 solid phase synthesis reaction Methods 0.000 claims 5
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 4
- 230000002401 inhibitory effect Effects 0.000 claims 4
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 4
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 125000004104 aryloxy group Chemical group 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000005089 alkenylaminocarbonyl group Chemical group 0.000 claims 2
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 2
- 125000004438 haloalkoxy group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000006239 protecting group Chemical group 0.000 claims 2
- 125000006727 (C1-C6) alkenyl group Chemical group 0.000 claims 1
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 1
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 1
- 125000003088 (fluoren-9-ylmethoxy)carbonyl group Chemical group 0.000 claims 1
- 125000000453 2,2,2-trichloroethyl group Chemical group [H]C([H])(*)C(Cl)(Cl)Cl 0.000 claims 1
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 1
- 102100029974 GTPase HRas Human genes 0.000 claims 1
- 102100039788 GTPase NRas Human genes 0.000 claims 1
- 101000584633 Homo sapiens GTPase HRas Proteins 0.000 claims 1
- 101000744505 Homo sapiens GTPase NRas Proteins 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000004103 aminoalkyl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 125000000612 phthaloyl group Chemical group C(C=1C(C(=O)*)=CC=CC1)(=O)* 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 125000002088 tosyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1C([H])([H])[H])S(*)(=O)=O 0.000 claims 1
- 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 claims 1
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021079012 | 2021-05-07 | ||
| PCT/JP2022/019544 WO2022234853A1 (ja) | 2021-05-07 | 2022-05-06 | Ｈｒａｓおよびｎｒａｓに対して選択的なｋｒａｓ阻害作用を有する環状化合物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPWO2022234853A1 JPWO2022234853A1 (https=) | 2022-11-10 |
| JPWO2022234853A5 true JPWO2022234853A5 (https=) | 2025-04-24 |
Family
ID=83932768
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023518700A Pending JPWO2022234853A1 (https=) | 2021-05-07 | 2022-05-06 |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US20240158446A1 (https=) |
| EP (1) | EP4309741A4 (https=) |
| JP (1) | JPWO2022234853A1 (https=) |
| KR (1) | KR20240005777A (https=) |
| CN (1) | CN117279933A (https=) |
| AR (1) | AR125796A1 (https=) |
| AU (1) | AU2022268781A1 (https=) |
| BR (1) | BR112023022755A2 (https=) |
| CA (1) | CA3218182A1 (https=) |
| CL (1) | CL2023003137A1 (https=) |
| CO (1) | CO2023014807A2 (https=) |
| CR (1) | CR20230572A (https=) |
| IL (1) | IL307605A (https=) |
| MX (1) | MX2023013139A (https=) |
| PE (1) | PE20250071A1 (https=) |
| TW (1) | TW202309063A (https=) |
| WO (1) | WO2022234853A1 (https=) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW202446781A (zh) | 2011-12-28 | 2024-12-01 | 日商中外製藥股份有限公司 | 胜肽化合物之製造方法 |
| EP4166664A1 (en) | 2015-03-13 | 2023-04-19 | Chugai Seiyaku Kabushiki Kaisha | Modified aminoacyl-trna synthetase and use thereof |
| JP7187323B2 (ja) | 2017-01-31 | 2022-12-12 | 中外製薬株式会社 | 無細胞翻訳系におけるペプチドの合成方法 |
| KR20250007021A (ko) | 2017-06-09 | 2025-01-13 | 추가이 세이야쿠 가부시키가이샤 | N-치환 아미노산을 포함하는 펩타이드의 합성 방법 |
| EP3878836B1 (en) | 2018-11-07 | 2025-07-23 | Chugai Seiyaku Kabushiki Kaisha | O-substituted serine derivative production method |
| EP4056580A4 (en) | 2019-11-07 | 2023-12-06 | Chugai Seiyaku Kabushiki Kaisha | METHOD FOR PRODUCING A PEPTIDE COMPOUND COMPRISING A STERICALLY HINDERED AMINO ACID |
| BR112022007535A2 (pt) | 2019-11-07 | 2022-07-12 | Chugai Pharmaceutical Co Ltd | Composto peptídico cíclico tendo ação inibitória de kras |
| US12312379B2 (en) | 2021-05-07 | 2025-05-27 | Chugai Seiyaku Kabushiki Kaisha | Methods for producing cyclic compounds comprising N-substituted amino acid residues |
| JP7823181B2 (ja) * | 2022-05-06 | 2026-03-03 | 中外製薬株式会社 | Ｈｒａｓおよびｎｒａｓに対して選択的なｋｒａｓ阻害作用を有する環状化合物 |
| CN115385867A (zh) * | 2022-09-19 | 2022-11-25 | 安徽普利药业有限公司 | 一种氨基酸及其类似物的成环反应与开环方法 |
| TW202430537A (zh) * | 2022-10-20 | 2024-08-01 | 日商中外製藥股份有限公司 | 環狀胜肽的結晶的製造方法 |
| EP4603105A1 (en) * | 2022-11-09 | 2025-08-20 | Chugai Seiyaku Kabushiki Kaisha | Pharmaceutical composition containing cyclic compound having selective kras inhibitory effect against hras and nras |
| CN120659773A (zh) * | 2022-11-09 | 2025-09-16 | 锐新医药公司 | 化合物、复合物以及其制备方法和用途 |
| WO2024101386A1 (ja) * | 2022-11-09 | 2024-05-16 | 中外製薬株式会社 | Ｈｒａｓおよびｎｒａｓに対して選択的なｋｒａｓ阻害作用を有する環状化合物 |
| WO2024195801A1 (ja) | 2023-03-20 | 2024-09-26 | 中外製薬株式会社 | 環状ペプチドの共結晶の製造方法 |
| TW202506168A (zh) | 2023-04-19 | 2025-02-16 | 日商中外製藥股份有限公司 | 包含環狀胜肽化合物及界面活性劑之組合物 |
| CN120936619A (zh) | 2023-04-20 | 2025-11-11 | 中外制药株式会社 | 用于生产环肽化合物的方法 |
| CN116655766B (zh) * | 2023-04-23 | 2023-12-12 | 山东第一医科大学(山东省医学科学院) | 一种订书肽及其制备方法和应用 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| WO2025162428A1 (en) * | 2024-01-29 | 2025-08-07 | Syneron Technology Co. Ltd. | Cyclic peptide compounds and compositions as ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| CN118324664B (zh) * | 2024-03-14 | 2026-04-07 | 四川鸿日医药科技有限公司 | 一种丝氨酸衍生物的制备方法 |
| TW202547461A (zh) | 2024-05-17 | 2025-12-16 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026004834A1 (ja) * | 2024-06-25 | 2026-01-02 | 中外製薬株式会社 | 固体分散体、及びそれを含む組成物 |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026009920A1 (ja) * | 2024-07-03 | 2026-01-08 | 中外製薬株式会社 | 環状ペプチドの精製法及び製造法 |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2586411T3 (es) | 2011-03-04 | 2016-10-14 | New York University | Macrociclos sustitutos de enlace de hidrógeno como moduladores de Ras |
| TW202446781A (zh) | 2011-12-28 | 2024-12-01 | 日商中外製藥股份有限公司 | 胜肽化合物之製造方法 |
| WO2015179438A1 (en) * | 2014-05-20 | 2015-11-26 | Ohio State Innovation Foundation | Small molecule rac or rho inhibitors |
| US10954287B2 (en) * | 2016-04-15 | 2021-03-23 | Ra Pharmaceuticals, Inc. | Ras binding peptides and methods of use |
| CN110869544B (zh) | 2017-06-09 | 2024-03-08 | 中外制药株式会社 | 膜透过性高的环状肽化合物及包含其的文库 |
| KR20250007021A (ko) * | 2017-06-09 | 2025-01-13 | 추가이 세이야쿠 가부시키가이샤 | N-치환 아미노산을 포함하는 펩타이드의 합성 방법 |
| WO2020122182A1 (ja) * | 2018-12-12 | 2020-06-18 | 中外製薬株式会社 | 分子内水素結合可能な官能基を有するアミノ酸とそれらのアミノ酸を含むペプチド化合物、およびそれらの製造方法 |
| BR112022007535A2 (pt) * | 2019-11-07 | 2022-07-12 | Chugai Pharmaceutical Co Ltd | Composto peptídico cíclico tendo ação inibitória de kras |
-
2022
- 2022-05-06 KR KR1020237040757A patent/KR20240005777A/ko active Pending
- 2022-05-06 IL IL307605A patent/IL307605A/en unknown
- 2022-05-06 TW TW111117092A patent/TW202309063A/zh unknown
- 2022-05-06 AU AU2022268781A patent/AU2022268781A1/en active Pending
- 2022-05-06 CN CN202280032929.5A patent/CN117279933A/zh active Pending
- 2022-05-06 JP JP2023518700A patent/JPWO2022234853A1/ja active Pending
- 2022-05-06 MX MX2023013139A patent/MX2023013139A/es unknown
- 2022-05-06 EP EP22798957.1A patent/EP4309741A4/en active Pending
- 2022-05-06 CR CR20230572A patent/CR20230572A/es unknown
- 2022-05-06 BR BR112023022755A patent/BR112023022755A2/pt unknown
- 2022-05-06 US US18/289,592 patent/US20240158446A1/en active Pending
- 2022-05-06 WO PCT/JP2022/019544 patent/WO2022234853A1/ja not_active Ceased
- 2022-05-06 AR ARP220101203A patent/AR125796A1/es unknown
- 2022-05-06 CA CA3218182A patent/CA3218182A1/en active Pending
- 2022-05-06 PE PE2023002874A patent/PE20250071A1/es unknown
-
2023
- 2023-10-20 CL CL2023003137A patent/CL2023003137A1/es unknown
- 2023-10-31 CO CONC2023/0014807A patent/CO2023014807A2/es unknown
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