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 |
|---|---|---|---|---|
| BR112015025159A2 (pt) | 2013-04-04 | 2017-07-18 | Harvard College | macrolídeos e métodos de sua preparação e uso |
| HK1242920A1 (zh) | 2014-10-08 | 2018-07-06 | 哈佛大学的校长及成员们 | 14-元酮内酯及其制备和使用方法 |
| WO2016154591A1 (en) | 2015-03-25 | 2016-09-29 | President And Fellows Of Harvard College | Macrolides with modified desosamine sugars and uses thereof |
| WO2018201076A2 (en) | 2017-04-28 | 2018-11-01 | Macrolide Pharmaceuticals Inc. | Macrolides with modified desosamine sugars and uses thereof |
| SG11202105227QA (en) | 2018-11-19 | 2021-06-29 | Zikani Therapeutics Inc | C10-alkylene substituted 13-membered macrolides and uses thereof |
| WO2020106636A1 (en) * | 2018-11-19 | 2020-05-28 | Zikani Therapeutics, Inc. | C11-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 |
| US6590083B1 (en) | 1999-04-16 | 2003-07-08 | Ortho-Mcneil Pharmaceutical, Inc. | Ketolide antibacterials |
| US6939861B2 (en) * | 1999-04-16 | 2005-09-06 | Kosan Biosciences, Inc. | Amido macrolides |
| JP2002542197A (ja) * | 1999-04-16 | 2002-12-10 | オーソ−マクニール・フアーマシユーチカル・インコーポレーテツド | ケトライド抗菌剤 |
| HRP990116B1 (en) | 1999-04-20 | 2007-10-31 | GlaxoSmithKline istra�iva�ki centar Zagreb d.o.o. | NOVEL 8a AND 9a- 15-MEMBERED LACTAMES |
| TR200103395T2 (tr) * | 1999-05-24 | 2002-04-22 | Pfizer Products Inc. | 13-metil eritromisin türevleri. |
| WO2001010879A1 (fr) * | 1999-08-06 | 2001-02-15 | Taisho Pharmaceutical Co., Ltd. | Derives d'erythromycine a |
| CA2380455C (en) | 1999-08-24 | 2009-06-02 | Abbott Laboratories | 9a-azalides with antibacterial activity |
| BRPI0017013B1 (pt) | 2000-01-27 | 2015-07-14 | Zoetis P Llc | Composição de antibiótico azalídeo e método para sua obtenção |
| 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 |
| CA2469304A1 (en) * | 2001-12-05 | 2003-06-19 | Ortho-Mcneil Pharmaceutical, Inc. | 6-o acyl ketolide antibacterials |
| US8063021B2 (en) * | 2002-01-17 | 2011-11-22 | Kosan Biosciences Incorporated | Ketolide anti-infective compounds |
| KR20050086873A (ko) * | 2002-11-29 | 2005-08-30 | 메루샹가부시키가이샤 | 매크로라이드계 화합물의 제조 방법 |
| JPWO2004065346A1 (ja) | 2003-01-21 | 2006-05-18 | 住友化学株式会社 | （−）−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 |
| BRPI0513903A (pt) * | 2004-07-28 | 2008-05-20 | Ranbaxy Lab Ltd | derivados de cetolìdeos úteis como agentes antimicrobianos, seus processos de preparação e composições farmacêuticas compreendendo os mesmos |
| US7767797B1 (en) | 2004-09-30 | 2010-08-03 | Synovo Gmbh | Macrocyclic compounds and methods of use thereof |
| EP1807439A2 (en) * | 2004-10-25 | 2007-07-18 | Ranbaxy Laboratories Limited | 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 |
| US20100035832A1 (en) * | 2005-01-12 | 2010-02-11 | Alpharma Aps | Macrolides |
| RS51479B (sr) * | 2005-01-13 | 2011-04-30 | Glaxo Group Limited | Makrolidi sa anti-inflamatornim dejstvom |
| WO2006120541A1 (en) | 2005-05-10 | 2006-11-16 | Glaxosmithkline Istrazivacki Centar Zagreb D.O.O. | Ether linked macrolides useful for the treatment of microbial infections |
| WO2007012464A1 (en) | 2005-07-26 | 2007-02-01 | Merckle Gmbh | Macrolide conjugates of pyrrolizine and indolizine compounds as inhibitors of 5-lipooxygenase and cyclooxygenase |
| CN102010403A (zh) | 2005-10-13 | 2011-04-13 | 卫材R&D管理有限公司 | 普拉二烯内酯b和普拉二烯内酯d的全合成 |
| EP1985620A4 (en) | 2006-02-07 | 2012-08-15 | Taisho Pharmaceutical Co Ltd | 10a-azalide compound |
| KR20090042971A (ko) * | 2006-08-24 | 2009-05-04 | 욱크하르트 리서치 센터 | 항미생물 활성을 갖는 신규한 마크로라이드 및 케토라이드 |
| AU2008224633A1 (en) | 2007-03-13 | 2008-09-18 | Pfizer Products Inc. | Erythromycin-based macrolides |
| CN101917850B (zh) | 2007-10-25 | 2016-01-13 | 森普拉制药公司 | 大环内酯类抗菌剂的制备方法 |
| 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 |
| DK2358379T3 (en) * | 2008-10-24 | 2016-03-07 | Cempra Pharmaceuticals Inc | BIOFORSVAR USING TRIAZOLHOLDIGE macrolides |
| CA2769551A1 (en) * | 2009-08-13 | 2011-02-17 | Basilea Pharmaceutica Ag | New macrolides and their use |
| EP2475253B1 (en) | 2009-09-10 | 2016-10-26 | Cempra Pharmaceuticals, Inc. | Methods for treating malaria, tuberculosis and mac diseases |
| JP5890785B2 (ja) | 2010-03-10 | 2016-03-22 | センプラ ファーマシューティカルズ，インコーポレイテッド | マクロライド抗生物質の非経口製剤 |
| BR112012023950A2 (pt) | 2010-03-22 | 2016-07-05 | Cempra Pharmaceuticals Inc | formas cristalinas de um macrolídeo, e usos dos mesmos |
| 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 |
| PL2571506T3 (pl) | 2010-05-20 | 2017-10-31 | Cempra Pharmaceuticals Inc | Sposoby sporządzania makrolidów i ketolidów oraz ich produktów pośrednich |
| EP2588084B1 (en) | 2010-07-01 | 2023-11-22 | Elanco Tiergesundheit AG | Antibiotic compositions comprising tulathromycin |
| 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 |
| US9815863B2 (en) | 2010-09-10 | 2017-11-14 | Cempra Pharmaceuticals, Inc. | Hydrogen bond forming fluoro ketolides for treating diseases |
| US9145436B2 (en) | 2010-10-10 | 2015-09-29 | Michael W. Burnet | 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 |
| ES2603227T3 (es) * | 2011-03-22 | 2017-02-24 | Wockhardt Limited | Proceso para la preparación de compuestos cetólidos |
| CA2843853A1 (en) | 2011-07-01 | 2013-01-10 | President And Fellows Of Harvard College | Macrocyclic insulin-degrading enzyme (ide) inhibitors and uses thereof |
| MX2014011537A (es) | 2012-03-27 | 2015-02-10 | Cempra Pharmaceuticals Inc | Formulaciones parenterales para la administracion de antibioticos macrolidos. |
| WO2014152326A1 (en) | 2013-03-14 | 2014-09-25 | Cempra Pharmaceuticals, Inc. | Methods for treating respiratory diseases and formulations therefor |
| BR112015023670A2 (pt) | 2013-03-15 | 2017-07-18 | Cempra Pharmaceuticals Inc | processo para preparar um composto |
| BR112015025159A2 (pt) | 2013-04-04 | 2017-07-18 | Harvard College | macrolídeos e métodos de sua preparação e uso |
| HK1242920A1 (zh) | 2014-10-08 | 2018-07-06 | 哈佛大学的校长及成员们 | 14-元酮内酯及其制备和使用方法 |
| HK1250719A1 (zh) | 2015-03-25 | 2019-01-11 | President And Fellows Of Harvard College | 脱氧糖胺的合成 |
| WO2016154591A1 (en) | 2015-03-25 | 2016-09-29 | President And Fellows Of Harvard College | Macrolides with modified desosamine sugars and uses thereof |
-
2015
- 2015-10-08 HK HK18102636.6A patent/HK1242920A1/zh unknown
- 2015-10-08 CN CN201580066344.5A patent/CN106998685A/zh active Pending
- 2015-10-08 US US15/517,843 patent/US10633407B2/en active Active
- 2015-10-08 JP JP2017519264A patent/JP2017531663A/ja active Pending
- 2015-10-08 CA CA2963815A patent/CA2963815A1/en not_active Abandoned
- 2015-10-08 EP EP15848340.4A patent/EP3211997A4/en not_active Withdrawn
- 2015-10-08 WO PCT/US2015/054700 patent/WO2016057798A1/en not_active Ceased
-
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