JP2017531663A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2017531663A5 JP2017531663A5 JP2017519264A JP2017519264A JP2017531663A5 JP 2017531663 A5 JP2017531663 A5 JP 2017531663A5 JP 2017519264 A JP2017519264 A JP 2017519264A JP 2017519264 A JP2017519264 A JP 2017519264A JP 2017531663 A5 JP2017531663 A5 JP 2017531663A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- alkyl
- hydrogen
- alkenyl
- carbocyclyl
- 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.)
- Pending
Links
- 229910052739 hydrogen Inorganic materials 0.000 claims 63
- 239000001257 hydrogen Substances 0.000 claims 63
- 125000000547 substituted alkyl group Chemical group 0.000 claims 59
- 125000000623 heterocyclic group Chemical group 0.000 claims 55
- 125000001072 heteroaryl group Chemical group 0.000 claims 50
- 150000002431 hydrogen Chemical group 0.000 claims 49
- 125000004452 carbocyclyl group Chemical group 0.000 claims 47
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 47
- 125000003107 substituted aryl group Chemical group 0.000 claims 46
- 150000001875 compounds Chemical class 0.000 claims 44
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 44
- 150000003839 salts Chemical class 0.000 claims 21
- 229910052736 halogen Inorganic materials 0.000 claims 17
- 150000002367 halogens Chemical group 0.000 claims 17
- 150000003573 thiols Chemical class 0.000 claims 17
- 125000001181 organosilyl group Chemical group [SiH3]* 0.000 claims 16
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 14
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 14
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 12
- 238000000034 method Methods 0.000 claims 11
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 8
- -1 amino, substituted amino Chemical class 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- 125000003710 aryl alkyl group Chemical group 0.000 claims 6
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 5
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 5
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 5
- 239000001301 oxygen Substances 0.000 claims 5
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 3
- 125000004122 cyclic group Chemical group 0.000 claims 3
- 229910052731 fluorine Inorganic materials 0.000 claims 3
- 239000011737 fluorine Substances 0.000 claims 3
- 239000003120 macrolide antibiotic agent Substances 0.000 claims 3
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 230000008878 coupling Effects 0.000 claims 2
- 238000010168 coupling process Methods 0.000 claims 2
- 238000005859 coupling reaction Methods 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 2
- 229920002554 vinyl polymer Polymers 0.000 claims 2
- 125000006706 (C3-C6) carbocyclyl group Chemical group 0.000 claims 1
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 208000035473 Communicable disease Diseases 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000004450 alkenylene group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000004419 alkynylene group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 150000001720 carbohydrates Chemical class 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 150000005676 cyclic carbonates Chemical class 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 125000004474 heteroalkylene group Chemical group 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 230000004968 inflammatory condition Effects 0.000 claims 1
- 125000005647 linker group Chemical group 0.000 claims 1
- 229940041033 macrolides Drugs 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000012038 nucleophile Substances 0.000 claims 1
- 125000000466 oxiranyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462061571P | 2014-10-08 | 2014-10-08 | |
| US62/061,571 | 2014-10-08 | ||
| PCT/US2015/054700 WO2016057798A1 (en) | 2014-10-08 | 2015-10-08 | 14-membered ketolides and methods of their preparation and use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017531663A JP2017531663A (ja) | 2017-10-26 |
| JP2017531663A5 true JP2017531663A5 (enExample) | 2018-11-15 |
Family
ID=55653777
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017519264A Pending JP2017531663A (ja) | 2014-10-08 | 2015-10-08 | 14員ケトライドならびにそれらの調製および使用の方法 |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US10633407B2 (enExample) |
| EP (1) | EP3211997A4 (enExample) |
| JP (1) | JP2017531663A (enExample) |
| CN (1) | CN106998685A (enExample) |
| CA (1) | CA2963815A1 (enExample) |
| HK (1) | HK1242920A1 (enExample) |
| WO (1) | WO2016057798A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX377459B (es) | 2013-04-04 | 2025-03-10 | Harvard College | Macrolidos y metodos para su preparacion y uso. |
| WO2016057798A1 (en) | 2014-10-08 | 2016-04-14 | President And Fellows Of Harvard College | 14-membered ketolides and methods of their preparation and use |
| CN107530365A (zh) | 2015-03-25 | 2018-01-02 | 哈佛大学的校长及成员们 | 具有修饰的脱氧糖胺糖的大环内酯及其用途 |
| WO2018201076A2 (en) | 2017-04-28 | 2018-11-01 | Macrolide Pharmaceuticals Inc. | Macrolides with modified desosamine sugars and uses thereof |
| IL283194B2 (en) | 2018-11-19 | 2025-03-01 | Zikani Therapeutics Inc | C10-alkylene substituted 13-membered macrolides and uses thereof |
| US20220177508A1 (en) * | 2018-11-19 | 2022-06-09 | Zikani Therapeutics, Inc. | C10-Cyclic Substituted 13-Membered Macrolides and Uses Thereof |
| IL303173A (en) * | 2023-05-23 | 2024-12-01 | Yeda Res & Dev | Active macrolide antibiotic compounds against pathogens |
| WO2025228440A1 (zh) * | 2024-04-30 | 2025-11-06 | 苏州信诺维医药科技股份有限公司 | 大环内酯类化合物、其制备方法及其用途 |
Family Cites Families (65)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ZA859575B (en) | 1984-12-21 | 1986-08-27 | Hoffmann La Roche | Oxetanones |
| FR2718450B1 (fr) * | 1994-04-08 | 1997-01-10 | Roussel Uclaf | Nouveaux dérivés de l'érythromycine, leur procédé de préparation et leur application comme médicaments. |
| JP3652394B2 (ja) | 1995-01-27 | 2005-05-25 | 高砂香料工業株式会社 | N−置換−7−アミノ−5−ヒドロキシ−3−オキソヘプタン酸誘導体およびその製造法 |
| HN1998000074A (es) | 1997-06-11 | 1999-01-08 | Pfizer Prod Inc | Derivados de macrolidos c-4 sustituidos |
| WO1999000125A1 (en) | 1997-06-27 | 1999-01-07 | Merck & Co., Inc. | 9a-aza-3-ketolides, compositions containing such compounds and methods of treatment |
| HN1998000159A (es) | 1997-10-29 | 1999-02-09 | Monsanto Co | Derivados de 9- amino - 3 ceto eritromicina |
| GB9814006D0 (en) | 1998-06-29 | 1998-08-26 | Biotica Tech Ltd | Polyketides and their synthesis |
| FR2785612A1 (fr) | 1998-11-10 | 2000-05-12 | Hoechst Marion Roussel Inc | Nouveaux derives de l'erythromycine, leur procede de preparation et leur application comme medicaments |
| US6262030B1 (en) | 1998-11-03 | 2001-07-17 | Pfizer Inc. | Erythromycin derivatives |
| US6399582B1 (en) * | 1999-04-16 | 2002-06-04 | Ortho-Mcneil Pharmaceutical, Inc. | Ketolide antibacterials |
| US6939861B2 (en) * | 1999-04-16 | 2005-09-06 | Kosan Biosciences, Inc. | Amido macrolides |
| US6590083B1 (en) | 1999-04-16 | 2003-07-08 | Ortho-Mcneil Pharmaceutical, Inc. | Ketolide antibacterials |
| HRP990116B1 (en) | 1999-04-20 | 2007-10-31 | GlaxoSmithKline istra�iva�ki centar Zagreb d.o.o. | NOVEL 8a AND 9a- 15-MEMBERED LACTAMES |
| IL145739A0 (en) * | 1999-05-24 | 2002-07-25 | Pfizer Prod Inc | 13-methyl-erythromycin derivatives |
| AU6316400A (en) * | 1999-08-06 | 2001-03-05 | Taisho Pharmaceutical Co., Ltd. | Erythromycin a derivatives |
| DE60025370T2 (de) | 1999-08-24 | 2006-09-21 | Abbott Laboratories, Abbott Park | 9a-azalide mit antibakterieller wirkung |
| WO2001055158A1 (en) | 2000-01-27 | 2001-08-02 | Pfizer Products Inc. | Azalide antibiotic compositions |
| JP4596591B2 (ja) | 2000-03-09 | 2010-12-08 | 塩野義製薬株式会社 | 8a−オキサホモエリスロマイシン誘導体、製造方法、合成中間体および医薬組成物 |
| US6440942B1 (en) * | 2000-12-22 | 2002-08-27 | Enanta Pharmaceuticals, Inc. | 14-membered macrolides derived from leucomycins |
| WO2003050132A1 (en) * | 2001-12-05 | 2003-06-19 | Ortho-Mcneil Pharmaceutical, Inc. | 6-o-acyl ketolide derivatives of erythromycine useful as antibacterials |
| US8063021B2 (en) * | 2002-01-17 | 2011-11-22 | Kosan Biosciences Incorporated | Ketolide anti-infective compounds |
| CA2507641A1 (en) * | 2002-11-29 | 2004-06-17 | Mercian Corporation | Method of producing macrolide compound |
| WO2004065346A1 (ja) | 2003-01-21 | 2004-08-05 | Sumitomo Chemical Company, Limited | (-)-テトラヒドロリプスタチンおよびその中間体の製造方法 |
| EP3738591A3 (en) | 2003-03-10 | 2021-03-24 | Merck Sharp & Dohme Corp. | Novel antibacterial agents |
| HRP20030381B1 (en) | 2003-05-14 | 2007-05-31 | GlaxoSmithKline istra�iva�ki centar Zagreb d.o.o. | 3-DECLADINOZYL 9a-N-CARBAMOYL AND 9a-N-THIOCARBAMOYL DERIVATIVES 9-DEOXO-9-DIHYDRO-9a-AZA-9a-HOMOERYTHROMICYNE A |
| US7276487B2 (en) | 2003-09-23 | 2007-10-02 | Enanta Pharmaceuticals, Inc. | 9a, 11-3C-bicyclic 9a-azalide derivatives |
| JP2008508322A (ja) * | 2004-07-28 | 2008-03-21 | ランバクシー ラボラトリーズ リミテッド | 抗菌剤としてのケトライド誘導体 |
| US7767797B1 (en) | 2004-09-30 | 2010-08-03 | Synovo Gmbh | Macrocyclic compounds and methods of use thereof |
| US20090170790A1 (en) * | 2004-10-25 | 2009-07-02 | Biswajit Das | Ketolide derivatives as antibacterial agents |
| US20060096158A1 (en) | 2004-11-08 | 2006-05-11 | Robinson J M | Lactones as new oxygenate fuel additives, fuels based thereon and methods for using same |
| CN101103039A (zh) * | 2005-01-12 | 2008-01-09 | 阿尔法马股份公司 | 作为抗菌剂的红霉素衍生物 |
| AU2006205828A1 (en) * | 2005-01-12 | 2006-07-20 | Alpharma Aps | Erythromycin derivatives as antibacterial agents |
| US8080529B2 (en) * | 2005-01-13 | 2011-12-20 | Glaxo Group Limited | Macrolides with anti-inflammatory activity |
| JP2008540503A (ja) | 2005-05-10 | 2008-11-20 | グラクソスミスクライン・イストラジヴァッキ・センタル・ザグレブ・ドルズバ・ゼー・オメイェノ・オドゴヴォルノスティオ | 細菌感染症の処置に有用なエーテル結合マクロライド |
| JP2009502838A (ja) | 2005-07-26 | 2009-01-29 | メルクレ,ゲーエムベーハー | ピロリジンおよびインドリジン化合物のマクロライド接合体 |
| JPWO2007043621A1 (ja) | 2005-10-13 | 2009-04-16 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | プラジエノライドb及びプラジエノライドdの全合成方法 |
| EP1985620A4 (en) | 2006-02-07 | 2012-08-15 | Taisho Pharmaceutical Co Ltd | COMPOUND 10a-AZALIDE |
| KR20090042971A (ko) * | 2006-08-24 | 2009-05-04 | 욱크하르트 리서치 센터 | 항미생물 활성을 갖는 신규한 마크로라이드 및 케토라이드 |
| KR20090110381A (ko) | 2007-03-13 | 2009-10-21 | 화이자 프로덕츠 인크. | 에리트로마이신계 마크로라이드 |
| AU2008316830B2 (en) | 2007-10-25 | 2016-03-17 | Cempra Pharmaceuticals, Inc. | Process for the preparation of macrolide antibacterial agents |
| US20090209547A1 (en) | 2008-02-15 | 2009-08-20 | In Jong Kim | C-8 halogenated macrolides |
| KR100980379B1 (ko) | 2008-04-02 | 2010-09-06 | 주식회사 파마코스텍 | 광학활성을 갖는 5-히드록시-3-옥소헵타노에이트 유도체의제조방법 |
| WO2010015703A2 (en) | 2008-08-07 | 2010-02-11 | Glaxosmithkline Istrazivacki Centar Zagreb D.O.O. | Novel 6-o-substituted 15-membered 8a- and 9a-lactams |
| US9072759B2 (en) | 2008-10-24 | 2015-07-07 | Cempra Pharmaceuticals, Inc. | Biodefenses using triazole-containing macrolides |
| WO2011018510A1 (en) * | 2009-08-13 | 2011-02-17 | Basilea Pharmaceutica Ag | New macrolides and their use |
| ES2608285T3 (es) | 2009-09-10 | 2017-04-07 | Cempra Pharmaceuticals, Inc. | Procedimientos para el tratamiento de paludismo, tuberculosis y enfermedades por MAC |
| PL2544537T3 (pl) | 2010-03-10 | 2017-10-31 | Cempra Pharmaceuticals Inc | Pozajelitowe preparaty antybiotyków makrolidowych |
| ES2564097T3 (es) | 2010-03-22 | 2016-03-17 | Cempra Pharmaceuticals, Inc. | Formas cristalinas de un macrólido, y usos de las mismas |
| WO2011131749A1 (en) * | 2010-04-23 | 2011-10-27 | Glaxo Group Limited | New 14 and 15 membered macrolides for the treatment of neutrophil dominated inflammatory diseases |
| ES2636948T3 (es) * | 2010-05-20 | 2017-10-10 | Cempra Pharmaceuticals, Inc. | Procesos para preparar macrólidos y cetólidos e intermediarios para los mismos |
| EP4324524A2 (en) | 2010-07-01 | 2024-02-21 | Elanco Tiergesundheit AG | Antibiotic compositions |
| US8975232B2 (en) * | 2010-07-29 | 2015-03-10 | President And Fellows Of Harvard College | Macrocyclic kinase inhibitors and uses thereof |
| US8796474B1 (en) * | 2010-08-23 | 2014-08-05 | Rutgers, The State University Of New Jersey | Macrolide compounds and methods and intermediates useful for their preparation |
| WO2012034058A1 (en) | 2010-09-10 | 2012-03-15 | Cempra Pharmaceuticals, Inc. | Hydrogen bond forming fluoro ketolides for treating diseases |
| WO2012051126A2 (en) | 2010-10-10 | 2012-04-19 | Synovo Gmbh | Anti-inflammatory macrolides |
| CN102690297A (zh) | 2011-03-22 | 2012-09-26 | 连云港海康生物科技有限公司 | 一种壳寡糖季铵盐及其合成方法 |
| WO2012127351A1 (en) * | 2011-03-22 | 2012-09-27 | Wockhardt Limited | Process for preparation of ketolide compounds |
| JP6023192B2 (ja) | 2011-07-01 | 2016-11-09 | プレジデント アンド フェローズ オブ ハーバード カレッジ | 大環状インスリン分解酵素(ide)阻害剤およびその使用 |
| IN2014DN08939A (enExample) | 2012-03-27 | 2015-05-22 | Cempra Pharmaceuticals Inc | |
| CN105163785A (zh) | 2013-03-14 | 2015-12-16 | 森普拉制药公司 | 用于治疗呼吸道疾病的方法及其制剂 |
| RU2015138797A (ru) | 2013-03-15 | 2017-04-24 | Семпра Фармасьютикалс, Инк. | Конвергентные способы получения макролидных антибактериальных агентов |
| MX377459B (es) | 2013-04-04 | 2025-03-10 | Harvard College | Macrolidos y metodos para su preparacion y uso. |
| WO2016057798A1 (en) | 2014-10-08 | 2016-04-14 | President And Fellows Of Harvard College | 14-membered ketolides and methods of their preparation and use |
| CN107530365A (zh) | 2015-03-25 | 2018-01-02 | 哈佛大学的校长及成员们 | 具有修饰的脱氧糖胺糖的大环内酯及其用途 |
| CN107531737A (zh) | 2015-03-25 | 2018-01-02 | 哈佛大学的校长及成员们 | 脱氧糖胺的合成 |
-
2015
- 2015-10-08 WO PCT/US2015/054700 patent/WO2016057798A1/en not_active Ceased
- 2015-10-08 JP JP2017519264A patent/JP2017531663A/ja active Pending
- 2015-10-08 US US15/517,843 patent/US10633407B2/en active Active
- 2015-10-08 HK HK18102636.6A patent/HK1242920A1/zh unknown
- 2015-10-08 CA CA2963815A patent/CA2963815A1/en not_active Abandoned
- 2015-10-08 CN CN201580066344.5A patent/CN106998685A/zh active Pending
- 2015-10-08 EP EP15848340.4A patent/EP3211997A4/en active Pending
-
2020
- 2020-04-08 US US16/843,259 patent/US11466046B2/en active Active
-
2022
- 2022-07-25 US US17/872,769 patent/US20230109357A1/en not_active Abandoned