JP2020529472A5 - - Google Patents
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- JP2020529472A5 JP2020529472A5 JP2020527859A JP2020527859A JP2020529472A5 JP 2020529472 A5 JP2020529472 A5 JP 2020529472A5 JP 2020527859 A JP2020527859 A JP 2020527859A JP 2020527859 A JP2020527859 A JP 2020527859A JP 2020529472 A5 JP2020529472 A5 JP 2020529472A5
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- JP
- Japan
- Prior art keywords
- group
- formula
- compound
- alkyl
- cycloalkyl
- 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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- 238000000034 method Methods 0.000 claims 33
- 150000001875 compounds Chemical class 0.000 claims 29
- 125000000217 alkyl group Chemical group 0.000 claims 23
- 229910052739 hydrogen Inorganic materials 0.000 claims 18
- 229910052799 carbon Inorganic materials 0.000 claims 17
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 12
- 108090000765 processed proteins & peptides Proteins 0.000 claims 12
- 239000011541 reaction mixture Substances 0.000 claims 9
- 229910052717 sulfur Inorganic materials 0.000 claims 9
- 125000005842 heteroatom Chemical group 0.000 claims 8
- 229910052760 oxygen Inorganic materials 0.000 claims 8
- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical compound CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 claims 7
- 239000003054 catalyst Substances 0.000 claims 6
- 230000000269 nucleophilic effect Effects 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 125000001424 substituent group Chemical group 0.000 claims 5
- 125000006648 (C1-C8) haloalkyl group Chemical group 0.000 claims 4
- DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 125000006588 heterocycloalkylene group Chemical group 0.000 claims 4
- 229910052751 metal Inorganic materials 0.000 claims 4
- 239000002184 metal Substances 0.000 claims 4
- 238000006462 rearrangement reaction Methods 0.000 claims 4
- FPGGTKZVZWFYPV-UHFFFAOYSA-M tetrabutylammonium fluoride Chemical compound [F-].CCCC[N+](CCCC)(CCCC)CCCC FPGGTKZVZWFYPV-UHFFFAOYSA-M 0.000 claims 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 3
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 claims 3
- 239000002253 acid Substances 0.000 claims 3
- 150000001412 amines Chemical class 0.000 claims 3
- 125000004429 atom Chemical group 0.000 claims 3
- 125000002993 cycloalkylene group Chemical group 0.000 claims 3
- 125000005549 heteroarylene group Chemical group 0.000 claims 3
- 125000005647 linker group Chemical group 0.000 claims 3
- 238000007363 ring formation reaction Methods 0.000 claims 3
- 229910052709 silver Inorganic materials 0.000 claims 3
- 239000004332 silver Substances 0.000 claims 3
- 239000007790 solid phase Substances 0.000 claims 3
- 125000006582 (C5-C6) heterocycloalkyl group Chemical group 0.000 claims 2
- 125000006585 (C6-C10) arylene group Chemical group 0.000 claims 2
- PXHVJJICTQNCMI-UHFFFAOYSA-N Nickel Chemical compound [Ni] PXHVJJICTQNCMI-UHFFFAOYSA-N 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000006242 amine protecting group Chemical group 0.000 claims 2
- 238000005859 coupling reaction Methods 0.000 claims 2
- 238000010511 deprotection reaction Methods 0.000 claims 2
- 150000007970 thio esters Chemical group 0.000 claims 2
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 2
- 125000000025 triisopropylsilyl group Chemical group C(C)(C)[Si](C(C)C)(C(C)C)* 0.000 claims 2
- GETQZCLCWQTVFV-UHFFFAOYSA-N trimethylamine Chemical compound CN(C)C GETQZCLCWQTVFV-UHFFFAOYSA-N 0.000 claims 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 1
- UWKQJZCTQGMHKD-UHFFFAOYSA-N 2,6-di-tert-butylpyridine Chemical compound CC(C)(C)C1=CC=CC(C(C)(C)C)=N1 UWKQJZCTQGMHKD-UHFFFAOYSA-N 0.000 claims 1
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 1
- RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 claims 1
- 238000006751 Mitsunobu reaction Methods 0.000 claims 1
- KJTLSVCANCCWHF-UHFFFAOYSA-N Ruthenium Chemical compound [Ru] KJTLSVCANCCWHF-UHFFFAOYSA-N 0.000 claims 1
- BQCADISMDOOEFD-UHFFFAOYSA-N Silver Chemical compound [Ag] BQCADISMDOOEFD-UHFFFAOYSA-N 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 150000001413 amino acids Chemical class 0.000 claims 1
- 238000003776 cleavage reaction Methods 0.000 claims 1
- 229910052802 copper Inorganic materials 0.000 claims 1
- 239000010949 copper Substances 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- DNJIEGIFACGWOD-UHFFFAOYSA-N ethyl mercaptane Natural products CCS DNJIEGIFACGWOD-UHFFFAOYSA-N 0.000 claims 1
- QSHDDOUJBYECFT-UHFFFAOYSA-N mercury Chemical compound [Hg] QSHDDOUJBYECFT-UHFFFAOYSA-N 0.000 claims 1
- 229910052753 mercury Inorganic materials 0.000 claims 1
- 229910052759 nickel Inorganic materials 0.000 claims 1
- 229910052762 osmium Inorganic materials 0.000 claims 1
- SYQBFIAQOQZEGI-UHFFFAOYSA-N osmium atom Chemical compound [Os] SYQBFIAQOQZEGI-UHFFFAOYSA-N 0.000 claims 1
- SBYHFKPVCBCYGV-UHFFFAOYSA-N quinuclidine Chemical compound C1CC2CCN1CC2 SBYHFKPVCBCYGV-UHFFFAOYSA-N 0.000 claims 1
- 229910052707 ruthenium Inorganic materials 0.000 claims 1
- 230000007017 scission Effects 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 229910052712 strontium Inorganic materials 0.000 claims 1
- CIOAGBVUUVVLOB-UHFFFAOYSA-N strontium atom Chemical compound [Sr] CIOAGBVUUVVLOB-UHFFFAOYSA-N 0.000 claims 1
- 125000000565 sulfonamide group Chemical group 0.000 claims 1
- DGVVWUTYPXICAM-UHFFFAOYSA-N β‐Mercaptoethanol Chemical compound OCCS DGVVWUTYPXICAM-UHFFFAOYSA-N 0.000 claims 1
- 0 C*CC1OC1N(*)C(C)* Chemical compound C*CC1OC1N(*)C(C)* 0.000 description 6
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762538477P | 2017-07-28 | 2017-07-28 | |
| US62/538,477 | 2017-07-28 | ||
| PCT/US2018/044182 WO2019023634A1 (en) | 2017-07-28 | 2018-07-27 | CYCLATIVE RELEASE OF PEPTIDE COMPOUNDS |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020529472A JP2020529472A (ja) | 2020-10-08 |
| JP2020529472A5 true JP2020529472A5 (cg-RX-API-DMAC7.html) | 2021-09-09 |
Family
ID=63312461
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020527859A Pending JP2020529472A (ja) | 2017-07-28 | 2018-07-27 | ペプチド化合物の環化放出関連する出願の相互参照 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US11299513B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP3658567A1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP2020529472A (cg-RX-API-DMAC7.html) |
| WO (1) | WO2019023634A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112592382B (zh) * | 2020-11-27 | 2022-10-04 | 安徽大学 | 一种树脂及其制备方法以及其在制备头尾环肽中的应用 |
| CN121248729A (zh) * | 2025-06-12 | 2026-01-02 | 杭州湃肽生化科技有限公司 | 一种全保护环肽及其制备方法 |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AUPP616598A0 (en) * | 1998-09-25 | 1998-10-15 | University Of Queensland, The | Auxiliary for amide bond formation |
| GB9928323D0 (en) | 1999-11-30 | 2000-01-26 | Cyclacel Ltd | Peptides |
| GB2369823B (en) | 1999-11-30 | 2003-06-04 | Cyclacel Ltd | Assays for cyclin-interacting compounds |
| US20050153894A1 (en) | 1999-11-30 | 2005-07-14 | Cyclacel Limited | p21 peptides |
| US20040077549A1 (en) | 2000-12-20 | 2004-04-22 | Bair Kenneth Walter | Inhibitors of the E2F-1/cyclin interaction for cancer therapy |
| AU2002234591A1 (en) | 2000-12-20 | 2002-07-01 | Novartis Ag | Inhibitors of the e2f-1/cyclin interaction for cancer therapy |
| US20040053849A1 (en) | 2000-12-20 | 2004-03-18 | Bair Kenneth Walter | Inhibitors of the E2F-1/cyclin interaction for cancer therapy |
| JP2004269357A (ja) | 2002-01-25 | 2004-09-30 | Marine Biotechnol Inst Co Ltd | 鉄と高い結合能を有する化合物およびその製造方法 |
| WO2006105386A1 (en) | 2005-03-30 | 2006-10-05 | Genentech, Inc. | Cdk2 inhibitors |
| WO2008000870A1 (es) | 2006-06-19 | 2008-01-03 | Fundación De La Comunidad Valenciana, Centro De Investigación Principe Felipe | Compuestos orgánicos que inhiben la actividad catalítica del complejo ciclina a/kinasa 2 dependiente de ciclina mediante su unión a un nuevo sitio farmacofórico en la molécula de ciclina |
| AU2010203698B2 (en) | 2009-01-06 | 2016-07-21 | C3 Jian, Inc. | Targeted antimicrobial moieties |
| US9376465B2 (en) | 2012-03-27 | 2016-06-28 | University Of South Carolina | Cyclin based inhibitors of CDK2 and CDK4 |
| US20140296484A1 (en) | 2013-03-27 | 2014-10-02 | University Of South Carolina | Cyclin Based Inhibitors of CDK2 and CDK4 |
| US10011635B2 (en) | 2013-09-27 | 2018-07-03 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Cyclic peptide conjugates and methods of use |
| JP6890836B2 (ja) | 2015-09-17 | 2021-06-18 | ヒスタイド アクツィエンゲゼルシャフト | 腫瘍細胞を非腫瘍細胞に変換するための医薬的連合体及びその使用 |
| CN109715191A (zh) | 2015-09-17 | 2019-05-03 | 伊斯迪德股份公司 | 将赘生性细胞转化成非赘生性细胞的药物缔合物及其用途 |
| WO2017046226A2 (en) | 2015-09-17 | 2017-03-23 | Histide Ag | Pharmaceutical association for converting a neoplastic cell into a non-neoplastic cell and uses thereof. |
| WO2017046229A1 (en) | 2015-09-17 | 2017-03-23 | Histide Ag | Pharmaceutical association of growth factor receptor agonist and adhesion protein inhibitor for converting a neoplastic cell into a non-neoplastic cell and uses thereof |
| KR20180052682A (ko) | 2015-09-17 | 2018-05-23 | 히스티드 아게 | 신생물성 세포를 비-신생물성 세포로 전환시키기 위한 약제학적 회합물 및 이것의 용도 |
| SG10201913366QA (en) | 2015-09-17 | 2020-02-27 | Histide Ag | Pharmaceutical association for converting a neoplastic cell into a non-neoplastic cell and uses thereof |
-
2018
- 2018-07-27 EP EP18759006.2A patent/EP3658567A1/en not_active Withdrawn
- 2018-07-27 JP JP2020527859A patent/JP2020529472A/ja active Pending
- 2018-07-27 US US16/633,969 patent/US11299513B2/en active Active
- 2018-07-27 WO PCT/US2018/044182 patent/WO2019023634A1/en not_active Ceased
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