JP2017510570A5 - - Google Patents
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- JP2017510570A5 JP2017510570A5 JP2016556784A JP2016556784A JP2017510570A5 JP 2017510570 A5 JP2017510570 A5 JP 2017510570A5 JP 2016556784 A JP2016556784 A JP 2016556784A JP 2016556784 A JP2016556784 A JP 2016556784A JP 2017510570 A5 JP2017510570 A5 JP 2017510570A5
- Authority
- JP
- Japan
- Prior art keywords
- nitrogen
- group
- ring
- carbon
- 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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- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 32
- 229910052757 nitrogen Inorganic materials 0.000 claims 22
- 229910052799 carbon Inorganic materials 0.000 claims 17
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 16
- 125000000217 alkyl group Chemical group 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 14
- 125000000623 heterocyclic group Chemical group 0.000 claims 11
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 6
- 125000002947 alkylene group Chemical group 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 5
- 125000004429 atom Chemical group 0.000 claims 5
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 5
- 125000002950 monocyclic group Chemical group 0.000 claims 5
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- PECYZEOJVXMISF-UHFFFAOYSA-N 3-aminoalanine Chemical compound [NH3+]CC(N)C([O-])=O PECYZEOJVXMISF-UHFFFAOYSA-N 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 4
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 3
- OGNSCSPNOLGXSM-UHFFFAOYSA-N 2,4-diaminobutyric acid Chemical compound NCCC(N)C(O)=O OGNSCSPNOLGXSM-UHFFFAOYSA-N 0.000 claims 3
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
- 125000002619 bicyclic group Chemical group 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 125000001909 leucine group Chemical group [H]N(*)C(C(*)=O)C([H])([H])C(C([H])([H])[H])C([H])([H])[H] 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000006413 ring segment Chemical group 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 2
- 241000894006 Bacteria Species 0.000 claims 2
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims 2
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 claims 2
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 claims 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 2
- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 claims 2
- 239000004473 Threonine Substances 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 150000001721 carbon Chemical group 0.000 claims 2
- 125000004474 heteroalkylene group Chemical group 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 150000004677 hydrates Chemical class 0.000 claims 2
- 125000005647 linker group Chemical group 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 125000000341 threoninyl group Chemical group [H]OC([H])(C([H])([H])[H])C([H])(N([H])[H])C(*)=O 0.000 claims 2
- 125000006586 (C3-C10) cycloalkylene group Chemical group 0.000 claims 1
- XTFIVUDBNACUBN-UHFFFAOYSA-N 1,3,5-trinitro-1,3,5-triazinane Chemical compound [O-][N+](=O)N1CN([N+]([O-])=O)CN([N+]([O-])=O)C1 XTFIVUDBNACUBN-UHFFFAOYSA-N 0.000 claims 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 1
- 241000589291 Acinetobacter Species 0.000 claims 1
- 241001135756 Alphaproteobacteria Species 0.000 claims 1
- 241000588923 Citrobacter Species 0.000 claims 1
- 241000588914 Enterobacter Species 0.000 claims 1
- 241000588921 Enterobacteriaceae Species 0.000 claims 1
- 241000588722 Escherichia Species 0.000 claims 1
- 241000589989 Helicobacter Species 0.000 claims 1
- 241000588748 Klebsiella Species 0.000 claims 1
- SNDPXSYFESPGGJ-BYPYZUCNSA-N L-2-aminopentanoic acid Chemical group CCC[C@H](N)C(O)=O SNDPXSYFESPGGJ-BYPYZUCNSA-N 0.000 claims 1
- AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 claims 1
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 claims 1
- 241000589248 Legionella Species 0.000 claims 1
- 208000007764 Legionnaires' Disease Diseases 0.000 claims 1
- 241000588621 Moraxella Species 0.000 claims 1
- 241000588772 Morganella morganii Species 0.000 claims 1
- 241000589516 Pseudomonas Species 0.000 claims 1
- 241000607142 Salmonella Species 0.000 claims 1
- 241000607768 Shigella Species 0.000 claims 1
- 241000122971 Stenotrophomonas Species 0.000 claims 1
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Natural products CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 claims 1
- 241000607477 Yersinia pseudotuberculosis Species 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 125000002527 bicyclic carbocyclic group Chemical group 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 125000002993 cycloalkylene group Chemical group 0.000 claims 1
- 208000027096 gram-negative bacterial infections Diseases 0.000 claims 1
- ZRALSGWEFCBTJO-UHFFFAOYSA-N guanidine group Chemical group NC(=N)N ZRALSGWEFCBTJO-UHFFFAOYSA-N 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- AGPKZVBTJJNPAG-UHFFFAOYSA-N isoleucine Natural products CCC(C)C(N)C(O)=O AGPKZVBTJJNPAG-UHFFFAOYSA-N 0.000 claims 1
- 229960000310 isoleucine Drugs 0.000 claims 1
- 235000014705 isoleucine Nutrition 0.000 claims 1
- 125000003588 lysine group Chemical group [H]N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 claims 1
- 230000000813 microbial effect Effects 0.000 claims 1
- 229940076266 morganella morganii Drugs 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- AHLPHDHHMVZTML-BYPYZUCNSA-N ornithyl group Chemical group N[C@@H](CCCN)C(=O)O AHLPHDHHMVZTML-BYPYZUCNSA-N 0.000 claims 1
- GJVFBWCTGUSGDD-UHFFFAOYSA-L pentamethonium bromide Chemical compound [Br-].[Br-].C[N+](C)(C)CCCCC[N+](C)(C)C GJVFBWCTGUSGDD-UHFFFAOYSA-L 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000003607 serino group Chemical group [H]N([H])[C@]([H])(C(=O)[*])C(O[H])([H])[H] 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 239000011593 sulfur Substances 0.000 claims 1
- 239000004474 valine Substances 0.000 claims 1
- 125000002987 valine group Chemical group [H]N([H])C([H])(C(*)=O)C([H])(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB201404301A GB201404301D0 (en) | 2014-03-11 | 2014-03-11 | Compounds and combinations |
| GB1404301.2 | 2014-03-11 | ||
| GB1421019.9 | 2014-11-26 | ||
| GB201421019A GB201421019D0 (en) | 2014-11-26 | 2014-11-26 | Compounds |
| PCT/EP2015/055046 WO2015135976A1 (en) | 2014-03-11 | 2015-03-11 | Polymyxin derivatives and their use in combination therapy together with different antibiotics |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017510570A JP2017510570A (ja) | 2017-04-13 |
| JP2017510570A5 true JP2017510570A5 (enExample) | 2018-06-07 |
| JP6785659B2 JP6785659B2 (ja) | 2020-11-18 |
Family
ID=52823596
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016556784A Active JP6785659B2 (ja) | 2014-03-11 | 2015-03-11 | 異なった抗生物質と一緒の組合せ療法におけるポリミキシン誘導体及びその使用 |
Country Status (21)
| Country | Link |
|---|---|
| US (3) | US20170073373A1 (enExample) |
| EP (1) | EP3116897B1 (enExample) |
| JP (1) | JP6785659B2 (enExample) |
| KR (2) | KR20160135739A (enExample) |
| CN (1) | CN106232617B (enExample) |
| AU (1) | AU2015228898B2 (enExample) |
| CA (1) | CA2940455C (enExample) |
| CY (1) | CY1125175T1 (enExample) |
| DK (1) | DK3116897T3 (enExample) |
| ES (1) | ES2910072T3 (enExample) |
| HR (1) | HRP20220387T1 (enExample) |
| IL (1) | IL247243B (enExample) |
| LT (1) | LT3116897T (enExample) |
| MX (1) | MX359104B (enExample) |
| PL (1) | PL3116897T3 (enExample) |
| PT (1) | PT3116897T (enExample) |
| RS (1) | RS63138B1 (enExample) |
| RU (1) | RU2740190C2 (enExample) |
| SI (1) | SI3116897T1 (enExample) |
| TW (1) | TWI709575B (enExample) |
| WO (1) | WO2015135976A1 (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX355217B (es) * | 2011-11-18 | 2018-04-10 | New Pharma Licence Holdings Ltd | Derivados de polimixina. |
| US10047126B2 (en) | 2014-04-01 | 2018-08-14 | Monash University | Polymyxin derivatives as antimicrobial compounds |
| CN107108699A (zh) | 2014-11-26 | 2017-08-29 | 新药物许可控股有限公司 | 化合物 |
| EP3233889B1 (en) | 2014-12-16 | 2022-07-06 | Shanghai MicuRx Pharmaceutical Co., Ltd. | Antimicrobial polymyxins for treatment of bacterial infections |
| CN105030744B (zh) * | 2015-07-09 | 2019-04-19 | 广州英赛特生物技术有限公司 | 取代苯胍衍生物作为多粘菌素类抗生素增效剂的应用 |
| JP7367950B2 (ja) * | 2015-09-29 | 2023-10-24 | モナッシュ ユニバーシティ | 抗菌性ポリミキシン誘導体化合物 |
| JP6744622B2 (ja) * | 2016-06-16 | 2020-08-19 | 学校法人上智学院 | ピペリジン化合物の製造方法 |
| WO2019084628A1 (en) | 2017-11-02 | 2019-05-09 | The University Of Queensland | Peptide antibiotics |
| DK3810633T3 (da) | 2018-06-25 | 2024-01-15 | Spero Therapeutics Inc | Forbindelser |
| CN111690040A (zh) * | 2019-03-12 | 2020-09-22 | 上海来益生物药物研究开发中心有限责任公司 | 多粘菌素衍生物、其制备方法和应用 |
| WO2021150792A1 (en) | 2020-01-21 | 2021-07-29 | Micurx Pharmaceuticals, Inc. | Novel compounds and composition for targeted therapy of kidney-associated cancers |
| TW202233649A (zh) | 2020-11-06 | 2022-09-01 | 美商斯佩羅治療學股份有限公司 | 化合物 |
| CN116847735B (zh) * | 2021-02-02 | 2026-02-03 | 韩国生命工学研究院 | 含有联苯基衍生物化合物作为有效成分的抗菌佐剂及其用途 |
| CN120574287B (zh) * | 2025-06-10 | 2026-07-03 | 中国药科大学 | 一种抗菌肽、组合物及应用 |
| CN120699105B (zh) * | 2025-08-19 | 2025-11-21 | 中国药科大学 | 一种氘代抗菌肽及其组合物和应用 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060004185A1 (en) * | 2004-07-01 | 2006-01-05 | Leese Richard A | Peptide antibiotics and peptide intermediates for their prepartion |
| BRPI0715095B8 (pt) * | 2006-08-11 | 2021-05-25 | Northern Antibiotics Oy | derivado de polimixina da fórmula geral (i); produto de combinação; composição farmacêutica; método para se sensibilizar bactérias gram-negativas a um agente antibacteriano; método para o desenvolvimento de antibióticos; método para a redução da toxicidade de polimixinas, octapeptinas naturais e seus derivados durante a aplicação das mesmas no tratamento de infecções em um indivíduo; método para melhorar as propriedades farmacocinéticas, de polimixinas, octapeptinas naturais e seus derivados; método para a sensibilização de bactérias gram-negativas clinicamente importantes a um complemento de mecanismo de defesa presente no soro; uso de um derivado; e processo para a preparação de um derivado de polimixina da fórmula (i). |
| WO2010075416A1 (en) * | 2008-12-23 | 2010-07-01 | Biosource Pharm, Inc. | Antibiotic compositions for the treatment of gram negative infections |
| CN101851270A (zh) * | 2009-04-03 | 2010-10-06 | 梁浩 | 一种多粘菌素衍生物及其制备方法 |
| US8415307B1 (en) * | 2010-06-23 | 2013-04-09 | Biosource Pharm, Inc. | Antibiotic compositions for the treatment of gram negative infections |
| WO2012168820A1 (en) * | 2011-06-08 | 2012-12-13 | Pfizer Inc. | Polymyxin derivatives useful as antibacterial agents |
| MX355217B (es) * | 2011-11-18 | 2018-04-10 | New Pharma Licence Holdings Ltd | Derivados de polimixina. |
| HUE059544T2 (hu) * | 2013-05-22 | 2022-11-28 | Spero Therapeutics Inc | Polimixin-származékok és ezek alkalmazása kombinációs terápiában különbözõ antibiotikumokkal |
-
2015
- 2015-03-11 KR KR1020167027152A patent/KR20160135739A/ko not_active Ceased
- 2015-03-11 RU RU2016139978A patent/RU2740190C2/ru active
- 2015-03-11 CA CA2940455A patent/CA2940455C/en active Active
- 2015-03-11 WO PCT/EP2015/055046 patent/WO2015135976A1/en not_active Ceased
- 2015-03-11 DK DK15715172.1T patent/DK3116897T3/da active
- 2015-03-11 AU AU2015228898A patent/AU2015228898B2/en active Active
- 2015-03-11 CN CN201580011858.0A patent/CN106232617B/zh active Active
- 2015-03-11 HR HRP20220387TT patent/HRP20220387T1/hr unknown
- 2015-03-11 LT LTEPPCT/EP2015/055046T patent/LT3116897T/lt unknown
- 2015-03-11 PL PL15715172T patent/PL3116897T3/pl unknown
- 2015-03-11 JP JP2016556784A patent/JP6785659B2/ja active Active
- 2015-03-11 US US15/125,415 patent/US20170073373A1/en not_active Abandoned
- 2015-03-11 MX MX2016011682A patent/MX359104B/es active IP Right Grant
- 2015-03-11 ES ES15715172T patent/ES2910072T3/es active Active
- 2015-03-11 TW TW104107773A patent/TWI709575B/zh active
- 2015-03-11 SI SI201531832T patent/SI3116897T1/sl unknown
- 2015-03-11 RS RS20220387A patent/RS63138B1/sr unknown
- 2015-03-11 EP EP15715172.1A patent/EP3116897B1/en active Active
- 2015-03-11 PT PT157151721T patent/PT3116897T/pt unknown
- 2015-03-11 KR KR1020237036093A patent/KR20230152779A/ko active Pending
-
2016
- 2016-08-11 IL IL247243A patent/IL247243B/en active IP Right Grant
-
2021
- 2021-01-25 US US17/157,393 patent/US20210221848A1/en not_active Abandoned
-
2022
- 2022-04-20 CY CY20221100299T patent/CY1125175T1/el unknown
-
2023
- 2023-03-24 US US18/126,270 patent/US20230322858A1/en active Pending
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