CA2963815A1 - 14-membered ketolides and methods of their preparation and use - Google Patents
14-membered ketolides and methods of their preparation and use Download PDFInfo
- Publication number
- CA2963815A1 CA2963815A1 CA2963815A CA2963815A CA2963815A1 CA 2963815 A1 CA2963815 A1 CA 2963815A1 CA 2963815 A CA2963815 A CA 2963815A CA 2963815 A CA2963815 A CA 2963815A CA 2963815 A1 CA2963815 A1 CA 2963815A1
- Authority
- CA
- Canada
- Prior art keywords
- optionally substituted
- compound
- alkyl
- formula
- hydrogen
- 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.)
- Abandoned
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
- C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
- C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Epidemiology (AREA)
- Communicable Diseases (AREA)
- Pulmonology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Tropical Medicine & Parasitology (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
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 (1)
| Publication Number | Publication Date |
|---|---|
| CA2963815A1 true CA2963815A1 (en) | 2016-04-14 |
Family
ID=55653777
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2963815A Abandoned CA2963815A1 (en) | 2014-10-08 | 2015-10-08 | 14-membered ketolides and methods of their preparation and use |
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 |
|---|---|---|---|---|
| JP6437523B2 (ja) | 2013-04-04 | 2018-12-12 | 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 | マクロライドならびにそれらの調製および使用の方法 |
| US10633407B2 (en) | 2014-10-08 | 2020-04-28 | President And Fellows Of Harvard College | 14-membered ketolides and methods of their preparation and use |
| EP3273969A4 (en) | 2015-03-25 | 2018-11-21 | President and Fellows of Harvard College | Macrolides with modified desosamine sugars and uses thereof |
| US11673910B2 (en) | 2017-04-28 | 2023-06-13 | Zikani Therapeutics, Inc. | Macrolides with modified desosamine sugars and uses thereof |
| SMT202600094T1 (it) | 2018-11-19 | 2026-03-09 | Harvard College | Macrolidi a 13 membri sostituiti con c10-alchilene e loro impiego |
| CA3120235A1 (en) * | 2018-11-19 | 2020-05-28 | 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 |
| IL145976A0 (en) * | 1999-04-16 | 2002-07-25 | Ortho Mcneil Pharm Inc | Ketolide antibacterials |
| 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 |
| 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 |
| WO2001010879A1 (fr) * | 1999-08-06 | 2001-02-15 | Taisho Pharmaceutical Co., Ltd. | Derives d'erythromycine a |
| ATE315042T1 (de) | 1999-08-24 | 2006-02-15 | Abbott Lab | 9a-azalide mit antibakterieller wirkung |
| 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 |
| AU2002346475A1 (en) | 2001-12-05 | 2003-06-23 | 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 |
| NZ540103A (en) | 2002-11-29 | 2007-05-31 | Mercian Corp | Process for 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 |
| EP1638549A4 (en) | 2003-03-10 | 2011-06-15 | Optimer Pharmaceuticals Inc | NEW 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 |
| WO2005030227A1 (en) | 2003-09-23 | 2005-04-07 | Enanta Pharmaceuticals, Inc. | 9a, 11-3C-BICYCLIC 9a-AZALIDE DERIVATIVES |
| RU2397987C2 (ru) * | 2004-07-28 | 2010-08-27 | Рэнбакси Лабораториз Лимитед | Кетолидные производные в качестве антибактериальных агентов |
| 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 |
| EP1841775A2 (en) * | 2005-01-12 | 2007-10-10 | Alpharma APS | Erythromycin derivatives as antibacterial agents |
| 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 |
| KR20070105993A (ko) | 2005-01-13 | 2007-10-31 | 글락소스미쓰클라인 이스트라지바치키 센타 자그레브 디.오.오. | 소염 활성을 갖는 마크로라이드 |
| 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 |
| CA2615581A1 (en) | 2005-07-26 | 2007-02-01 | Merckle Gmbh | Macrolide conjugates of pyrrolizine and indolizine compounds as inhibitors of 5-lipooxygenase and cyclooxygenase |
| WO2007043621A1 (ja) | 2005-10-13 | 2007-04-19 | Eisai R & D Management Co., Ltd. | 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 |
| JP5015016B2 (ja) | 2006-02-07 | 2012-08-29 | 大正製薬株式会社 | 10a−アザライド化合物 |
| EP2056844A4 (en) * | 2006-08-24 | 2010-11-24 | Wockhardt Research Center | NEW MACROLIDS AND KETOLIDS WITH ANTIMICROBIAL EFFECT |
| AU2008224633A1 (en) * | 2007-03-13 | 2008-09-18 | Pfizer Products Inc. | Erythromycin-based macrolides |
| CA2703475A1 (en) | 2007-10-25 | 2009-04-30 | 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 |
| US8796232B2 (en) | 2008-10-24 | 2014-08-05 | Cempra Pharmaceuticals, Inc. | Methods for treating resistant diseases using triazole containing macrolides |
| ES2582794T3 (es) * | 2009-08-13 | 2016-09-15 | Basilea Pharmaceutica Ag | Nuevos macrólidos y su uso |
| JP5914335B2 (ja) | 2009-09-10 | 2016-05-11 | 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 | マラリア、結核、及びmac病の治療方法 |
| US20130045937A1 (en) | 2010-03-10 | 2013-02-21 | Cempra Pharmaceuticals, Inc. | Parenteral formulations of macrolide antibiotics |
| CN103080122A (zh) | 2010-03-22 | 2013-05-01 | 森普拉制药公司 | 大环内脂的结晶形式及其用途 |
| 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 |
| WO2011146829A1 (en) | 2010-05-20 | 2011-11-24 | Cempra Pharmaceuticals, Inc. | Processes for preparing macrolides and ketolides and intermediates therefor |
| US20130102551A1 (en) | 2010-07-01 | 2013-04-25 | Andreas Hotte | 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 |
| JP6042334B2 (ja) * | 2010-09-10 | 2016-12-14 | 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 | 疾患治療のための水素結合形成フルオロケトライド |
| CA2814333A1 (en) | 2010-10-10 | 2012-04-19 | Synovo Gmbh | Anti-inflammatory macrolides |
| CN103619863B (zh) * | 2011-03-22 | 2016-03-16 | 沃克哈特有限公司 | 酮内酯化合物的制备方法 |
| 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 |
| AU2012279202A1 (en) * | 2011-07-01 | 2014-02-20 | President And Fellows Of Harvard College | Macrocyclic insulin-degrading enzyme (IDE) inhibitors and uses thereof |
| CN104470527B (zh) | 2012-03-27 | 2019-05-28 | 森普拉制药公司 | 用于施用大环内酯抗生素的肠胃外制剂 |
| RU2015138796A (ru) | 2013-03-14 | 2017-04-19 | Семпра Фармасьютикалс, Инк. | Способы и составы для лечения респираторных заболеваний |
| WO2014145210A1 (en) | 2013-03-15 | 2014-09-18 | Cempra Pharmaceuticals, Inc. | Convergent processes for preparing macrolide antibacterial agents |
| JP6437523B2 (ja) | 2013-04-04 | 2018-12-12 | 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 | マクロライドならびにそれらの調製および使用の方法 |
| US10633407B2 (en) | 2014-10-08 | 2020-04-28 | President And Fellows Of Harvard College | 14-membered ketolides and methods of their preparation and use |
| EP3273969A4 (en) | 2015-03-25 | 2018-11-21 | President and Fellows of Harvard College | Macrolides with modified desosamine sugars and uses thereof |
| 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 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 not_active Withdrawn
- 2015-10-08 WO PCT/US2015/054700 patent/WO2016057798A1/en not_active Ceased
- 2015-10-08 JP JP2017519264A patent/JP2017531663A/ja 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
Also Published As
| Publication number | Publication date |
|---|---|
| EP3211997A1 (en) | 2017-09-06 |
| EP3211997A4 (en) | 2018-10-24 |
| JP2017531663A (ja) | 2017-10-26 |
| CN106998685A (zh) | 2017-08-01 |
| US10633407B2 (en) | 2020-04-28 |
| US20230109357A1 (en) | 2023-04-06 |
| HK1242920A1 (zh) | 2018-07-06 |
| US20170305953A1 (en) | 2017-10-26 |
| US20200361980A1 (en) | 2020-11-19 |
| US11466046B2 (en) | 2022-10-11 |
| WO2016057798A1 (en) | 2016-04-14 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Discontinued |
Effective date: 20211229 |