BR112015025159A2 - macrolídeos e métodos de sua preparação e uso - Google Patents
macrolídeos e métodos de sua preparação e usoInfo
- Publication number
- BR112015025159A2 BR112015025159A2 BR112015025159A BR112015025159A BR112015025159A2 BR 112015025159 A2 BR112015025159 A2 BR 112015025159A2 BR 112015025159 A BR112015025159 A BR 112015025159A BR 112015025159 A BR112015025159 A BR 112015025159A BR 112015025159 A2 BR112015025159 A2 BR 112015025159A2
- Authority
- BR
- Brazil
- Prior art keywords
- macrolides
- methods
- eastern
- western
- synthesis
- Prior art date
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
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/424—Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
-
- 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
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/7056—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
-
- 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
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
-
- 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
-
- 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
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C231/00—Preparation of carboxylic acid amides
- C07C231/12—Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D307/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
- C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
- C07D317/10—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
- C07D317/14—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D317/30—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic System
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
- C07F7/1872—Preparation; Treatments not provided for in C07F7/20
- C07F7/1892—Preparation; Treatments not provided for in C07F7/20 by reactions not provided for in C07F7/1876 - C07F7/1888
-
- 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
-
- 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
- C07D498/08—Bridged systems
Abstract
abstract provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. intermediates in the synthesis of macrolides including the eastern and western halves are also provided. pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. a general diastereoselective aldol methodology used in the synthesis of the western half is further provided. tradução do resumo resumo patente de invenção para "macrolídeos e métodos de sua preparação e uso" são fornecidos aqui métodos de preparer macrolídeos pelo acoplamento de uma metade oriental e ocidental, seguido por macrociclização, para fornecer macrolídeos, incluindo igualmente macrolídeos conhecidos e novos. intermediários na síntese de macrolídeos incluindo as metades orientais e ocidentais são da mesma forma fornecidos. composições farmacêuticas e métodos de tratar doenças infecciosas e condições inflamatórias usando os macrolídeos inventivos são da mesma forma fornecidos. uma metodologia de aldol diastereosseletiva geral usada na sintase das metades ocidentais é também fornecida. 1/1
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201361808441P | 2013-04-04 | 2013-04-04 | |
US201361832639P | 2013-06-07 | 2013-06-07 | |
US201461946604P | 2014-02-28 | 2014-02-28 | |
PCT/US2014/033025 WO2014165792A2 (en) | 2013-04-04 | 2014-04-04 | Macrolides and methods of their preparation and use |
Publications (1)
Publication Number | Publication Date |
---|---|
BR112015025159A2 true BR112015025159A2 (pt) | 2017-07-18 |
Family
ID=51659360
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112015025159A BR112015025159A2 (pt) | 2013-04-04 | 2014-04-04 | macrolídeos e métodos de sua preparação e uso |
Country Status (11)
Country | Link |
---|---|
US (3) | US9982005B2 (pt) |
EP (2) | EP4095146A1 (pt) |
JP (3) | JP6437523B2 (pt) |
KR (2) | KR102363621B1 (pt) |
CN (2) | CN105246334A (pt) |
AU (3) | AU2014248014B2 (pt) |
BR (1) | BR112015025159A2 (pt) |
CA (2) | CA3130061A1 (pt) |
IL (1) | IL241878B (pt) |
MX (2) | MX2015014026A (pt) |
WO (1) | WO2014165792A2 (pt) |
Families Citing this family (20)
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US9453042B2 (en) | 2007-10-25 | 2016-09-27 | Cempra Pharmaceuticals, Inc. | Process for the preparation of macrolide antibacterial agents |
AU2009308182B2 (en) | 2008-10-24 | 2016-05-19 | Cempra Pharmaceuticals, Inc. | Biodefenses using triazole-containing macrolides |
US9937194B1 (en) | 2009-06-12 | 2018-04-10 | Cempra Pharmaceuticals, Inc. | Compounds and methods for treating inflammatory diseases |
EP2475253B1 (en) | 2009-09-10 | 2016-10-26 | Cempra Pharmaceuticals, Inc. | Methods for treating malaria, tuberculosis and mac diseases |
KR20130120458A (ko) | 2010-09-10 | 2013-11-04 | 셈프라 파마슈티컬스, 인크. | 질환을 치료하기 위한 수소결합 형성 플루오로 케토라이드 |
US10188674B2 (en) | 2012-03-27 | 2019-01-29 | Cempra Pharmaceuticals, Inc. | Parenteral formulations for administering macrolide antibiotics |
CA2905975A1 (en) | 2013-03-14 | 2014-09-25 | Cempra Pharmaceuticals, Inc. | Methods for treating respiratory diseases and formulations therefor |
CN105188712A (zh) | 2013-03-15 | 2015-12-23 | 森普拉制药公司 | 用于制备大环内酯抗菌剂的收敛方法 |
MX2015014026A (es) | 2013-04-04 | 2016-08-03 | Harvard College | Macrolidos y metodos para su preparacion y uso. |
CA2931547A1 (en) | 2013-12-09 | 2015-06-18 | Durect Corporation | Pharmaceutically active agent complexes, polymer complexes, and compositions and methods involving the same |
CN106998685A (zh) * | 2014-10-08 | 2017-08-01 | 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 |
MX2017011454A (es) * | 2015-03-06 | 2018-01-23 | Cempra Pharmaceuticals Inc | Procesos para preparar fluorocetólidos. |
WO2016154591A1 (en) | 2015-03-25 | 2016-09-29 | President And Fellows Of Harvard College | Macrolides with modified desosamine sugars and uses thereof |
CA2978670A1 (en) * | 2015-03-25 | 2016-09-29 | President And Fellows Of Harvard College | Synthesis of desosamines |
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CA3091413A1 (en) * | 2017-02-17 | 2018-08-23 | Cempra Pharmaceuticals, Inc. | Triazole-containing macrolides and ophthalmic uses therefor |
US11673910B2 (en) | 2017-04-28 | 2023-06-13 | Zikani Therapeutics, Inc. | Macrolides with modified desosamine sugars and uses thereof |
AU2019385333A1 (en) | 2018-11-19 | 2021-07-01 | President And Fellows Of Harvard College | C10-alkylene substituted 13-membered macrolides and uses thereof |
KR20210123288A (ko) * | 2018-11-19 | 2021-10-13 | 지카니 테라퓨틱스, 인크. | C11-환식 치환된 13-원 마크롤라이드 및 이의 용도 |
CN114591286B (zh) * | 2021-04-12 | 2023-05-23 | 南京大学 | 新型大环内酯化合物acautalides A-C及其制备方法和应用 |
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