JP2017506248A5 - - Google Patents
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- JP2017506248A5 JP2017506248A5 JP2016552984A JP2016552984A JP2017506248A5 JP 2017506248 A5 JP2017506248 A5 JP 2017506248A5 JP 2016552984 A JP2016552984 A JP 2016552984A JP 2016552984 A JP2016552984 A JP 2016552984A JP 2017506248 A5 JP2017506248 A5 JP 2017506248A5
- Authority
- JP
- Japan
- Prior art keywords
- lower alkyl
- cor
- halo
- membered heteroaryl
- optionally substituted
- 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.)
- Granted
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- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims 61
- 125000000217 alkyl group Chemical group 0.000 claims 37
- 150000001875 compounds Chemical class 0.000 claims 28
- 125000001188 haloalkyl group Chemical group 0.000 claims 27
- 125000005843 halogen group Chemical group 0.000 claims 23
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 17
- 125000004093 cyano group Chemical group *C#N 0.000 claims 16
- 239000008194 pharmaceutical composition Substances 0.000 claims 13
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 12
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 6
- 210000004027 cell Anatomy 0.000 claims 6
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 5
- 125000004429 atom Chemical group 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 208000035475 disorder Diseases 0.000 claims 5
- 201000009030 Carcinoma Diseases 0.000 claims 4
- 206010009944 Colon cancer Diseases 0.000 claims 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 4
- 206010033128 Ovarian cancer Diseases 0.000 claims 4
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 4
- 206010017758 gastric cancer Diseases 0.000 claims 4
- 201000001441 melanoma Diseases 0.000 claims 4
- 208000037819 metastatic cancer Diseases 0.000 claims 4
- 208000011575 metastatic malignant neoplasm Diseases 0.000 claims 4
- LWBFIOPAFDTCND-UHFFFAOYSA-N n-[1-[[4-(trifluoromethyl)phenyl]methyl]indazol-3-yl]furan-2-carboxamide Chemical compound C1=CC(C(F)(F)F)=CC=C1CN1C2=CC=CC=C2C(NC(=O)C=2OC=CC=2)=N1 LWBFIOPAFDTCND-UHFFFAOYSA-N 0.000 claims 4
- 241001465754 Metazoa Species 0.000 claims 3
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 3
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 3
- 230000000694 effects Effects 0.000 claims 3
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 3
- CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical compound C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 claims 3
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical compound C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 claims 3
- VQKFNUFAXTZWDK-UHFFFAOYSA-N 2-Methylfuran Chemical compound CC1=CC=CO1 VQKFNUFAXTZWDK-UHFFFAOYSA-N 0.000 claims 2
- 206010003571 Astrocytoma Diseases 0.000 claims 2
- 208000035143 Bacterial infection Diseases 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 208000017897 Carcinoma of esophagus Diseases 0.000 claims 2
- 102000004204 Fascin Human genes 0.000 claims 2
- 108090000786 Fascin Proteins 0.000 claims 2
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 2
- 208000017604 Hodgkin disease Diseases 0.000 claims 2
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 2
- 206010051808 Lymphoid tissue hyperplasia Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 206010027406 Mesothelioma Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims 2
- 206010038389 Renal cancer Diseases 0.000 claims 2
- 206010039491 Sarcoma Diseases 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 2
- 208000036142 Viral infection Diseases 0.000 claims 2
- 208000022362 bacterial infectious disease Diseases 0.000 claims 2
- 201000001531 bladder carcinoma Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 201000007455 central nervous system cancer Diseases 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 201000005619 esophageal carcinoma Diseases 0.000 claims 2
- 208000021045 exocrine pancreatic carcinoma Diseases 0.000 claims 2
- 208000010749 gastric carcinoma Diseases 0.000 claims 2
- 230000004968 inflammatory condition Effects 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 208000028867 ischemia Diseases 0.000 claims 2
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 201000005296 lung carcinoma Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 210000002569 neuron Anatomy 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 201000000498 stomach carcinoma Diseases 0.000 claims 2
- 229930192474 thiophene Natural products 0.000 claims 2
- 230000000451 tissue damage Effects 0.000 claims 2
- 231100000827 tissue damage Toxicity 0.000 claims 2
- 208000010570 urinary bladder carcinoma Diseases 0.000 claims 2
- 230000009385 viral infection Effects 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- 229940082729 Fascin inhibitor Drugs 0.000 claims 1
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 claims 1
- RFRXIWQYSOIBDI-UHFFFAOYSA-N benzarone Chemical compound CCC=1OC2=CC=CC=C2C=1C(=O)C1=CC=C(O)C=C1 RFRXIWQYSOIBDI-UHFFFAOYSA-N 0.000 claims 1
- 108010085672 beta-lactamase PSE-2 Proteins 0.000 claims 1
- 125000000068 chlorophenyl group Chemical group 0.000 claims 1
- -1 cyano, methyl Chemical group 0.000 claims 1
- 230000007850 degeneration Effects 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- JKFAIQOWCVVSKC-UHFFFAOYSA-N furazan Chemical group C=1C=NON=1 JKFAIQOWCVVSKC-UHFFFAOYSA-N 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- ZLTPDFXIESTBQG-UHFFFAOYSA-N isothiazole Chemical compound C=1C=NSC=1 ZLTPDFXIESTBQG-UHFFFAOYSA-N 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 230000003961 neuronal insult Effects 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 1
- 0 CCCC(*)c1ccn[o]1 Chemical compound CCCC(*)c1ccn[o]1 0.000 description 9
- XJJVJKLSFMUBAR-UHFFFAOYSA-N CCc1n[s]cc1 Chemical compound CCc1n[s]cc1 XJJVJKLSFMUBAR-UHFFFAOYSA-N 0.000 description 1
- PEXOZHFJFQGDBR-UHFFFAOYSA-N Cc1c([N]2(C)CC2)[s]cn1 Chemical compound Cc1c([N]2(C)CC2)[s]cn1 PEXOZHFJFQGDBR-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461942554P | 2014-02-20 | 2014-02-20 | |
| US61/942,554 | 2014-02-20 | ||
| PCT/US2015/016686 WO2015127125A1 (en) | 2014-02-20 | 2015-02-19 | Compounds and methods for inhibiting fascin |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017506248A JP2017506248A (ja) | 2017-03-02 |
| JP2017506248A5 true JP2017506248A5 (cg-RX-API-DMAC7.html) | 2018-03-29 |
| JP6691869B2 JP6691869B2 (ja) | 2020-05-13 |
Family
ID=53878980
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016552984A Active JP6691869B2 (ja) | 2014-02-20 | 2015-02-19 | ファシンを阻害するための化合物及び方法 |
Country Status (8)
| Country | Link |
|---|---|
| US (7) | US9573946B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP3107902B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP6691869B2 (cg-RX-API-DMAC7.html) |
| CN (2) | CN111349087B (cg-RX-API-DMAC7.html) |
| CA (2) | CA2940144C (cg-RX-API-DMAC7.html) |
| DK (1) | DK3107902T3 (cg-RX-API-DMAC7.html) |
| ES (1) | ES2868882T3 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2015127125A1 (cg-RX-API-DMAC7.html) |
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| EP4643881A2 (en) * | 2016-01-05 | 2025-11-05 | The Regents of the University of California | Benzothiazole amphiphiles |
| CN108727340B (zh) | 2017-04-11 | 2020-12-29 | 广东东阳光药业有限公司 | 氟取代的吲唑类化合物及其用途 |
| AU2018312558B2 (en) | 2017-08-02 | 2022-09-29 | Spinogenix, Inc. | Benzothiazole and related compounds |
| CN111655259A (zh) * | 2017-11-22 | 2020-09-11 | 康奈尔大学 | 包括转移抑制剂的共疗法 |
| CN112912141A (zh) * | 2018-08-27 | 2021-06-04 | 斯皮诺吉尼克斯公司 | 用于树突棘生成的肌成束蛋白结合化合物 |
| EP3628330A1 (en) | 2018-09-28 | 2020-04-01 | Fundacion Universitaria San Antonio | Imipramine for use as inhibitor of fascin1 overexpression |
| TW202043198A (zh) * | 2019-01-17 | 2020-12-01 | 美商Ｉｆｍ Ｄｕｅ有限公司 | 用於治療與sting活性相關之病況的化合物及組合物 |
| HUE072464T2 (hu) | 2019-01-31 | 2025-11-28 | Spinogenix Inc | Spinogenézis egy promoterének szilárd formái |
| WO2025001864A1 (en) * | 2023-06-30 | 2025-01-02 | Beijing Double-Crane Runchuang Technology Co., Ltd. | Fascin inhibitors |
| WO2024109642A1 (zh) * | 2023-07-28 | 2024-05-30 | 常州大学 | 一种苯并氮杂环类化合物作为β2-肾上腺素受体别构调节剂的应用 |
| WO2025111414A1 (en) * | 2023-11-21 | 2025-05-30 | Katholieke Universiteit Leuven | Trpm3-modulating benzofuran derivatives |
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-
2015
- 2015-02-19 US US14/626,791 patent/US9573946B2/en active Active
- 2015-02-19 DK DK15752063.6T patent/DK3107902T3/da active
- 2015-02-19 WO PCT/US2015/016686 patent/WO2015127125A1/en not_active Ceased
- 2015-02-19 CA CA2940144A patent/CA2940144C/en active Active
- 2015-02-19 CN CN202010244131.XA patent/CN111349087B/zh active Active
- 2015-02-19 EP EP15752063.6A patent/EP3107902B1/en active Active
- 2015-02-19 CN CN201580009687.8A patent/CN106232583B/zh active Active
- 2015-02-19 CA CA3195815A patent/CA3195815A1/en active Pending
- 2015-02-19 JP JP2016552984A patent/JP6691869B2/ja active Active
- 2015-02-19 ES ES15752063T patent/ES2868882T3/es active Active
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2017
- 2017-02-20 US US15/437,229 patent/US9850243B2/en active Active
- 2017-12-21 US US15/851,141 patent/US10227345B2/en active Active
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2019
- 2019-03-11 US US16/298,632 patent/US10941141B2/en active Active
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2021
- 2021-02-16 US US17/176,855 patent/US11858929B2/en active Active
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2023
- 2023-12-21 US US18/393,515 patent/US12168658B2/en active Active
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2024
- 2024-12-17 US US18/984,475 patent/US20250333411A1/en active Pending