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 (enExample) | 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 (enExample) |
| EP (1) | EP3658567A1 (enExample) |
| JP (1) | JP2020529472A (enExample) |
| WO (1) | WO2019023634A1 (enExample) |
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 |
| CN120309693B (zh) * | 2025-06-12 | 2025-09-16 | 杭州湃肽生化科技有限公司 | 一类环肽化合物及其制备方法和应用 |
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 |
| GB2369823B (en) | 1999-11-30 | 2003-06-04 | Cyclacel Ltd | Assays for cyclin-interacting compounds |
| GB9928323D0 (en) | 1999-11-30 | 2000-01-26 | Cyclacel Ltd | Peptides |
| US20050153894A1 (en) | 1999-11-30 | 2005-07-14 | Cyclacel Limited | p21 peptides |
| CN1592752A (zh) | 2000-12-20 | 2005-03-09 | 诺瓦提斯公司 | 用于治疗癌症的e2f－1/细胞周期蛋白相互作用的抑制剂 |
| US20040053849A1 (en) | 2000-12-20 | 2004-03-18 | Bair Kenneth Walter | Inhibitors of the E2F-1/cyclin interaction for cancer therapy |
| US20040077549A1 (en) | 2000-12-20 | 2004-04-22 | 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 |
| US20100184684A1 (en) | 2009-01-06 | 2010-07-22 | C3 Jian, Inc. | Antibacterial and antifungal peptides |
| 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 |
| 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 |
| EP3349777B1 (en) | 2015-09-17 | 2025-05-07 | Histide AG | Pharmaceutical association comprising a growth factor receptor agonist conjugated to a bioactive carrierfor converting a neoplastic cell into a non-neoplastic cell and uses thereof |
| EP3349782A2 (en) | 2015-09-17 | 2018-07-25 | Histide AG | Pharmaceutical association comprising a growth factor receptor agonist conjugated to a bioactive carrier for converting a neoplastic cell into a non-neoplastic cell and uses thereof |
| KR20180052726A (ko) | 2015-09-17 | 2018-05-18 | 히스티드 아게 | 신생물성 세포를 비-신생물성 세포로 전환시키기 위한 약제학적 회합물 및 이것의 용도 |
| IL299622A (en) | 2015-09-17 | 2023-03-01 | Histide Ag | A pharmaceutical composition containing a growth receptor agonist and an adhesion protein inhibitor for converting a neoplastic cell into a non-neoplastic cell and its uses |
| 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. |
-
2018
- 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
- 2018-07-27 EP EP18759006.2A patent/EP3658567A1/en not_active Withdrawn
- 2018-07-27 JP JP2020527859A patent/JP2020529472A/ja active Pending
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