JPWO2021026520A5 - - Google Patents
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- Publication number
- JPWO2021026520A5 JPWO2021026520A5 JP2022506948A JP2022506948A JPWO2021026520A5 JP WO2021026520 A5 JPWO2021026520 A5 JP WO2021026520A5 JP 2022506948 A JP2022506948 A JP 2022506948A JP 2022506948 A JP2022506948 A JP 2022506948A JP WO2021026520 A5 JPWO2021026520 A5 JP WO2021026520A5
- Authority
- JP
- Japan
- Prior art keywords
- unsubstituted
- substituted
- alkyl
- membered heterocyclyl
- compound
- 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
Links
- 150000001875 compounds Chemical class 0.000 claims 30
- 239000001257 hydrogen Substances 0.000 claims 27
- 229910052739 hydrogen Inorganic materials 0.000 claims 27
- 125000000217 alkyl group Chemical group 0.000 claims 19
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 claims 15
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 14
- 125000004452 carbocyclyl group Chemical group 0.000 claims 12
- 150000002431 hydrogen Chemical class 0.000 claims 11
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 10
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 9
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 9
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 7
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 claims 6
- 238000000034 method Methods 0.000 claims 5
- -1 guanidinyl Chemical group 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 239000012026 peptide coupling reagents Substances 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 125000003088 (fluoren-9-ylmethoxy)carbonyl group Chemical group 0.000 claims 2
- LMDZBCPBFSXMTL-UHFFFAOYSA-N 1-Ethyl-3-(3-dimethylaminopropyl)carbodiimide Substances CCN=C=NCCCN(C)C LMDZBCPBFSXMTL-UHFFFAOYSA-N 0.000 claims 2
- FPQQSJJWHUJYPU-UHFFFAOYSA-N 3-(dimethylamino)propyliminomethylidene-ethylazanium;chloride Chemical compound Cl.CCN=C=NCCCN(C)C FPQQSJJWHUJYPU-UHFFFAOYSA-N 0.000 claims 2
- KXDHJXZQYSOELW-UHFFFAOYSA-N Carbamic acid Chemical group NC(O)=O KXDHJXZQYSOELW-UHFFFAOYSA-N 0.000 claims 2
- QOSSAOTZNIDXMA-UHFFFAOYSA-N Dicylcohexylcarbodiimide Chemical compound C1CCCCC1N=C=NC1CCCCC1 QOSSAOTZNIDXMA-UHFFFAOYSA-N 0.000 claims 2
- 239000007821 HATU Substances 0.000 claims 2
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 150000004657 carbamic acid derivatives Chemical class 0.000 claims 2
- 239000004202 carbamide Substances 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 125000005270 trialkylamine group Chemical group 0.000 claims 2
- 150000003672 ureas Chemical class 0.000 claims 2
- JERHCAZKZXMKMU-UHFFFAOYSA-N 4-[4,6-bis(3,5-dimethylpyrazol-1-yl)-1,3,5-triazin-2-yl]-n,n-diethylaniline Chemical compound C1=CC(N(CC)CC)=CC=C1C1=NC(N2C(=CC(C)=N2)C)=NC(N2C(=CC(C)=N2)C)=N1 JERHCAZKZXMKMU-UHFFFAOYSA-N 0.000 claims 1
- 206010017533 Fungal infection Diseases 0.000 claims 1
- 208000031888 Mycoses Diseases 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 125000006242 amine protecting group Chemical group 0.000 claims 1
- 229960003942 amphotericin b Drugs 0.000 claims 1
- AJDPNPAGZMZOMN-UHFFFAOYSA-N diethyl (4-oxo-1,2,3-benzotriazin-3-yl) phosphate Chemical compound C1=CC=C2C(=O)N(OP(=O)(OCC)OCC)N=NC2=C1 AJDPNPAGZMZOMN-UHFFFAOYSA-N 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 239000006207 intravenous dosage form Substances 0.000 claims 1
- 239000006186 oral dosage form Substances 0.000 claims 1
- 238000010647 peptide synthesis reaction Methods 0.000 claims 1
- 239000007790 solid phase Substances 0.000 claims 1
- 150000003512 tertiary amines Chemical class 0.000 claims 1
- 230000009466 transformation Effects 0.000 claims 1
- 238000000844 transformation Methods 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962884464P | 2019-08-08 | 2019-08-08 | |
| US62/884,464 | 2019-08-08 | ||
| US201962951753P | 2019-12-20 | 2019-12-20 | |
| US62/951,753 | 2019-12-20 | ||
| PCT/US2020/045566 WO2021026520A1 (en) | 2019-08-08 | 2020-08-10 | Hybrid amide derivatives of amphotericin b |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2022543420A JP2022543420A (ja) | 2022-10-12 |
| JP2022543420A5 JP2022543420A5 (https=) | 2023-08-14 |
| JPWO2021026520A5 true JPWO2021026520A5 (https=) | 2023-08-14 |
| JP7636004B2 JP7636004B2 (ja) | 2025-02-26 |
Family
ID=74503735
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022506948A Active JP7636004B2 (ja) | 2019-08-08 | 2020-08-10 | アムホテリシンｂのハイブリッドアミド誘導体 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20230016424A1 (https=) |
| EP (1) | EP4009985A4 (https=) |
| JP (1) | JP7636004B2 (https=) |
| KR (1) | KR20220071185A (https=) |
| CN (1) | CN114555094A (https=) |
| AU (1) | AU2020325163B2 (https=) |
| BR (1) | BR112022001866A2 (https=) |
| CA (1) | CA3149916A1 (https=) |
| CL (1) | CL2022000319A1 (https=) |
| IL (1) | IL290289B2 (https=) |
| MX (1) | MX2022001678A (https=) |
| WO (1) | WO2021026520A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PH12022551513A1 (en) | 2019-12-20 | 2023-04-24 | Mirati Therapeutics Inc | Sos1 inhibitors |
| US20230357303A1 (en) * | 2020-08-10 | 2023-11-09 | The Board Of Trustees Of The University Of Illinois | Hybrid amide derivatives of amphotericin b |
| CN115536716B (zh) * | 2021-06-29 | 2025-08-08 | 中国科学院上海药物研究所 | 两性霉素b半合成衍生物及其制备方法和用途 |
| TW202519239A (zh) * | 2023-07-19 | 2025-05-16 | 美國伊利諾大學理事會 | 利用遺失蛋白質（ｍｉｓｓｉｎｇ ｐｒｏｔｅｉｎｓ）之小分子模擬物恢復生理機能 |
| GB202406857D0 (en) * | 2024-05-15 | 2024-06-26 | Univ Manchester | Polyenes |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL122086B1 (en) * | 1979-04-09 | 1982-06-30 | Politechnika Gdanska | Process for preparing amides of antibiotics from the group of polyene macrolides and their derivativesvykh makrolidov i ikh proizvodnykh |
| FR2776927B1 (fr) * | 1998-04-07 | 2002-07-05 | Univ Paris Curie | Compositions pour la vectorisation de molecules |
| US6664241B2 (en) * | 2000-05-31 | 2003-12-16 | Micrologix Biotech Inc. | Water-soluble amide derivatives of polyene macrolides and preparation and uses thereof |
| MX365184B (es) * | 2010-12-21 | 2019-05-21 | Centro De Investig Y De Estudios Avanzados Del I P N | Nuevos compuestos analogos de la anfotericina y composiciones farmaceuticas que los contienen. |
| KR20150027217A (ko) * | 2012-06-15 | 2015-03-11 | 블러트 에스.에이. | 항진균성 항생 암포테리신 b의 n-치환된 제2 세대 유도체, 및 이의 제조 및 응용 방법 |
| WO2015164289A1 (en) | 2014-04-21 | 2015-10-29 | Cidara Therapeutics, Inc. | Compositions and methods for the treatment of fungal infections |
| JP6543272B2 (ja) * | 2014-05-16 | 2019-07-10 | ザ ボード オブ トラスティーズ オブ ザ ユニヴァーシティ オブ イリノイＴｈｅ Ｂｏａｒｄ Ｏｆ Ｔｒｕｓｔｅｅｓ Ｏｆ Ｔｈｅ Ｕｎｉｖｅｒｓｉｔｙ Ｏｆ Ｉｌｌｉｎｏｉｓ | 低減された毒性を有するアンホテリシンｂ誘導体 |
| TWI702223B (zh) | 2014-06-12 | 2020-08-21 | 日商塩野義製藥股份有限公司 | 多烯巨環內酯衍生物 |
| AU2016205187B2 (en) | 2015-01-08 | 2020-02-27 | The Board Of Trustees Of The University Of Illinois | Concise synthesis of urea derivatives of amphotericin B |
| CA3021061C (en) * | 2015-04-15 | 2023-10-24 | Martin D. Burke | Derivatives of amphotericin b |
| US10322187B2 (en) * | 2015-08-10 | 2019-06-18 | Lehigh University | Reduced toxicity molecular conjugates of anti-fungal agents |
| RU2688658C1 (ru) * | 2018-04-10 | 2019-05-22 | Федеральное государственное бюджетное научное учреждение "Научно-исследовательский институт по изысканию новых антибиотиков имени Г.Ф. Гаузе" | Противогрибковый полусинтетический полиеновый антибиотик, его водорастворимые соли и фармацевтические композиции на их основе |
-
2020
- 2020-08-10 EP EP20850514.9A patent/EP4009985A4/en active Pending
- 2020-08-10 WO PCT/US2020/045566 patent/WO2021026520A1/en not_active Ceased
- 2020-08-10 KR KR1020227007294A patent/KR20220071185A/ko active Pending
- 2020-08-10 MX MX2022001678A patent/MX2022001678A/es unknown
- 2020-08-10 CN CN202080070120.2A patent/CN114555094A/zh active Pending
- 2020-08-10 IL IL290289A patent/IL290289B2/en unknown
- 2020-08-10 JP JP2022506948A patent/JP7636004B2/ja active Active
- 2020-08-10 BR BR112022001866A patent/BR112022001866A2/pt unknown
- 2020-08-10 US US17/633,254 patent/US20230016424A1/en active Pending
- 2020-08-10 AU AU2020325163A patent/AU2020325163B2/en active Active
- 2020-08-10 CA CA3149916A patent/CA3149916A1/en active Pending
-
2022
- 2022-02-07 CL CL2022000319A patent/CL2022000319A1/es unknown
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