CN108570083A - 大环内脂的结晶形式及其用途 - Google Patents
大环内脂的结晶形式及其用途 Download PDFInfo
- Publication number
- CN108570083A CN108570083A CN201810569806.0A CN201810569806A CN108570083A CN 108570083 A CN108570083 A CN 108570083A CN 201810569806 A CN201810569806 A CN 201810569806A CN 108570083 A CN108570083 A CN 108570083A
- Authority
- CN
- China
- Prior art keywords
- cem
- another embodiment
- peaks
- water
- crystalline
- 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
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
-
- 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
- A61K31/04—Nitro compounds
-
- 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
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
-
- 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
- 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
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Communicable Diseases (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Cephalosporin Compounds (AREA)
- Medicinal Preparation (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31606310P | 2010-03-22 | 2010-03-22 | |
| US61/316,063 | 2010-03-22 | ||
| CN2011800174629A CN103080122A (zh) | 2010-03-22 | 2011-03-22 | 大环内脂的结晶形式及其用途 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2011800174629A Division CN103080122A (zh) | 2010-03-22 | 2011-03-22 | 大环内脂的结晶形式及其用途 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN108570083A true CN108570083A (zh) | 2018-09-25 |
Family
ID=44673574
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201810569806.0A Pending CN108570083A (zh) | 2010-03-22 | 2011-03-22 | 大环内脂的结晶形式及其用途 |
| CN2011800174629A Pending CN103080122A (zh) | 2010-03-22 | 2011-03-22 | 大环内脂的结晶形式及其用途 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2011800174629A Pending CN103080122A (zh) | 2010-03-22 | 2011-03-22 | 大环内脂的结晶形式及其用途 |
Country Status (19)
| Country | Link |
|---|---|
| US (4) | US8975386B2 (https=) |
| EP (2) | EP3009442B1 (https=) |
| JP (4) | JP5711352B2 (https=) |
| KR (2) | KR20180101643A (https=) |
| CN (2) | CN108570083A (https=) |
| AU (2) | AU2011232627B2 (https=) |
| BR (1) | BR112012023950A2 (https=) |
| CA (1) | CA2793884C (https=) |
| DK (1) | DK2550286T3 (https=) |
| ES (1) | ES2564097T3 (https=) |
| HR (1) | HRP20160168T1 (https=) |
| IL (1) | IL222018B (https=) |
| MX (1) | MX361413B (https=) |
| MY (1) | MY162411A (https=) |
| NZ (1) | NZ602544A (https=) |
| PL (1) | PL2550286T3 (https=) |
| RU (1) | RU2650883C2 (https=) |
| SI (1) | SI2550286T1 (https=) |
| WO (1) | WO2011119604A1 (https=) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2552682T3 (es) | 2003-03-10 | 2015-12-01 | Merck Sharp & Dohme Corp. | Agentes antibacterianos novedosos |
| CN105732745A (zh) | 2007-10-25 | 2016-07-06 | 森普拉制药公司 | 大环内酯类抗菌剂的制备方法 |
| 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 |
| US9480679B2 (en) | 2009-09-10 | 2016-11-01 | Cempra Pharmaceuticals, Inc. | Methods for treating malaria, tuberculosis and MAC diseases |
| DK2550286T3 (en) * | 2010-03-22 | 2016-02-29 | Cempra Pharmaceuticals Inc | CRYSTALLINE FORMS OF A MACROLID AND APPLICATIONS THEREOF |
| CN105198944B (zh) | 2010-05-20 | 2018-06-01 | 森普拉制药公司 | 制备大环内酯和酮内酯及其中间体的方法 |
| EP2613630A4 (en) | 2010-09-10 | 2014-01-15 | Cempra Pharmaceuticals Inc | HYDROGEN BOND FOR THE PREPARATION OF FLUOROCHETOLIDES FOR THE TREATMENT OF DISEASES |
| MX2014011537A (es) | 2012-03-27 | 2015-02-10 | Cempra Pharmaceuticals Inc | Formulaciones parenterales para la administracion de antibioticos macrolidos. |
| HK1217665A1 (zh) | 2013-03-14 | 2017-01-20 | 森普拉制药公司 | 用於治療呼吸道疾病的方法及其製劑 |
| RU2015138797A (ru) | 2013-03-15 | 2017-04-24 | Семпра Фармасьютикалс, Инк. | Конвергентные способы получения макролидных антибактериальных агентов |
| US9982005B2 (en) | 2013-04-04 | 2018-05-29 | President And Fellows Of Harvard College | Macrolides and methods of their preparation and use |
| KR20170039689A (ko) * | 2014-08-05 | 2017-04-11 | 셈프라 파마슈티컬스, 인크. | 항균제의 분말 경구 현탁제 제형 |
| CN104151382B (zh) * | 2014-08-08 | 2016-09-14 | 广东东阳光药业有限公司 | 一种固态大环内酯的晶型 |
| CN104311611B (zh) * | 2014-08-13 | 2017-01-18 | 广东东阳光药业有限公司 | 一种制备固态大环内酯的方法 |
| US10633407B2 (en) | 2014-10-08 | 2020-04-28 | President And Fellows Of Harvard College | 14-membered ketolides and methods of their preparation and use |
| JP2018509452A (ja) | 2015-03-25 | 2018-04-05 | 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 | 修飾デソサミン糖をもつマクロライドおよびその使用 |
| JP6112696B1 (ja) * | 2015-10-05 | 2017-04-12 | 富山化学工業株式会社 | ソリスロマイシンを含む錠剤 |
| EP3190122A1 (en) * | 2016-01-08 | 2017-07-12 | LEK Pharmaceuticals d.d. | A novel synthetic pathway towards solithromycin and purification thereof |
| WO2018045294A1 (en) * | 2016-09-02 | 2018-03-08 | Cempra Pharmaceuticals, Inc. | Processes for preparing fluoroketolides |
| CN115003309B (zh) | 2019-12-02 | 2024-05-24 | 阿里量子解决方法公司 | 一种具有结构式i的化合物的晶型 |
Citations (5)
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| EP1469008A1 (en) * | 2000-03-15 | 2004-10-20 | Hanmi Pharm. Co., Ltd. | Method of preparing a non-pharmaceutical grade clarithromycin |
| US20060100164A1 (en) * | 2003-03-10 | 2006-05-11 | Chang-Hsing Liang | Novel antibacterial agents |
| WO2007059307A2 (en) * | 2005-11-15 | 2007-05-24 | Teva Pharmaceutical Industries Ltd. | Crystalline and amorphous forms of telithromycin |
| WO2009053259A1 (en) * | 2007-10-25 | 2009-04-30 | Sandoz Ag | Process for the production of telithromycin |
| WO2009055557A1 (en) * | 2007-10-25 | 2009-04-30 | Cempra Pharmaceuticals, Inc. | Process for the preparation of macrolide antibacterial agents |
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| US4331803A (en) | 1980-06-04 | 1982-05-25 | Taisho Pharmaceutical Co., Ltd. | Novel erythromycin compounds |
| US4474768A (en) | 1982-07-19 | 1984-10-02 | Pfizer Inc. | N-Methyl 11-aza-10-deoxo-10-dihydro-erytromycin A, intermediates therefor |
| US4742049A (en) | 1986-06-04 | 1988-05-03 | Abbott Laboratories | Semisynthetic erythromycin antibiotics |
| IL114589A (en) | 1990-11-21 | 1999-12-22 | Roussel Uclaf | Intermediates for the preparation of erythromycin derivatives |
| US5985844A (en) | 1992-03-26 | 1999-11-16 | Merck & Co., Inc. | Homoerythromycin A derivatives modified at the 4"-and 8A-positions |
| FR2697524B1 (fr) | 1992-11-05 | 1994-12-23 | Roussel Uclaf | Nouveaux dérivés de l'érythromycine, leur procédé de préparation et leur application comme médicaments. |
| US5527780A (en) | 1992-11-05 | 1996-06-18 | Roussel Uclaf | Erythromycin derivatives |
| FR2718450B1 (fr) | 1994-04-08 | 1997-01-10 | Roussel Uclaf | Nouveaux dérivés de l'érythromycine, leur procédé de préparation et leur application comme médicaments. |
| FR2719587B1 (fr) | 1994-05-03 | 1996-07-12 | Roussel Uclaf | Nouveaux dérivés de l'érythromycine, leur procédé de préparation et leur application comme médicaments. |
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| FR2745290B1 (fr) | 1996-02-28 | 1998-04-03 | Roussel Uclaf | Nouveaux derives de l'erythromycine, leur procede de preparation et leur application comme medicaments |
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| FR2777282B1 (fr) | 1998-04-08 | 2001-04-20 | Hoechst Marion Roussel Inc | Nouveaux derives de la 2-fluoro 3-de((2,6-dideoxy 3-c-methyl 3-0-methyl-alpha-l-ribohexopyranosyl) oxyl) 6-o-methyl 3-oxo erythromycine, leur procede de preparation et leur application a la synthese de principes actifs de medicaments |
| US6020521A (en) | 1998-08-26 | 2000-02-01 | Abbott Laboratories | Macrolide LHRH antagonists |
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| 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 |
| KR100317907B1 (ko) * | 1998-11-24 | 2001-12-24 | 김 완 주 | 신규한 중간체, 이를 이용한 마크로라이드계 항생제의제조방법 |
| FR2786188B1 (fr) | 1998-11-24 | 2002-10-31 | Hoechst Marion Roussel Inc | Nouveaux derives de l'erythromycine, leur procede de preparation et leur applicaion comme medicaments |
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| JP2001261694A (ja) | 2000-03-06 | 2001-09-26 | Pfizer Prod Inc | ケトライド抗生物質 |
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| PT1320355E (pt) | 2001-05-18 | 2006-08-31 | Chiron Corp | Sistema para administracao de uma formulacao de tobramicina |
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| BR0307898A (pt) | 2002-02-22 | 2004-12-07 | Pharmacia Corp | Formulações de droga antibiótica oftálmica contendo um composto de ciclodextrina e cloreto de cetil piridìnio |
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| ITMI20022292A1 (it) | 2002-10-29 | 2004-04-30 | Zambon Spa | 9a-azalidi ad attivita' antiinfiammatoria. |
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| PL2544537T3 (pl) | 2010-03-10 | 2017-10-31 | Cempra Pharmaceuticals Inc | Pozajelitowe preparaty antybiotyków makrolidowych |
| DK2550286T3 (en) * | 2010-03-22 | 2016-02-29 | Cempra Pharmaceuticals Inc | CRYSTALLINE FORMS OF A MACROLID AND APPLICATIONS THEREOF |
-
2011
- 2011-03-22 DK DK11760068.4T patent/DK2550286T3/en active
- 2011-03-22 CN CN201810569806.0A patent/CN108570083A/zh active Pending
- 2011-03-22 KR KR1020187025895A patent/KR20180101643A/ko not_active Ceased
- 2011-03-22 MX MX2012010895A patent/MX361413B/es active IP Right Grant
- 2011-03-22 BR BR112012023950A patent/BR112012023950A2/pt not_active Application Discontinuation
- 2011-03-22 CN CN2011800174629A patent/CN103080122A/zh active Pending
- 2011-03-22 EP EP15194057.4A patent/EP3009442B1/en active Active
- 2011-03-22 WO PCT/US2011/029424 patent/WO2011119604A1/en not_active Ceased
- 2011-03-22 NZ NZ602544A patent/NZ602544A/en not_active IP Right Cessation
- 2011-03-22 ES ES11760068.4T patent/ES2564097T3/es active Active
- 2011-03-22 HR HRP20160168T patent/HRP20160168T1/hr unknown
- 2011-03-22 SI SI201130745T patent/SI2550286T1/sl unknown
- 2011-03-22 US US13/636,510 patent/US8975386B2/en not_active Expired - Fee Related
- 2011-03-22 MY MYPI2012004183A patent/MY162411A/en unknown
- 2011-03-22 JP JP2013501396A patent/JP5711352B2/ja active Active
- 2011-03-22 AU AU2011232627A patent/AU2011232627B2/en not_active Ceased
- 2011-03-22 PL PL11760068T patent/PL2550286T3/pl unknown
- 2011-03-22 RU RU2012144614A patent/RU2650883C2/ru not_active IP Right Cessation
- 2011-03-22 EP EP11760068.4A patent/EP2550286B1/en not_active Revoked
- 2011-03-22 KR KR1020127027222A patent/KR102006200B1/ko not_active Expired - Fee Related
- 2011-03-22 CA CA2793884A patent/CA2793884C/en not_active Expired - Fee Related
-
2012
- 2012-09-20 IL IL222018A patent/IL222018B/en not_active IP Right Cessation
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2013
- 2013-05-22 US US13/900,147 patent/US8759500B2/en not_active Expired - Fee Related
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2014
- 2014-11-14 JP JP2014231987A patent/JP6121387B2/ja active Active
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2015
- 2015-09-21 US US14/859,736 patent/US20160244472A1/en not_active Abandoned
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2016
- 2016-06-15 AU AU2016203986A patent/AU2016203986B2/en not_active Ceased
- 2016-12-16 JP JP2016244733A patent/JP2017081953A/ja active Pending
-
2018
- 2018-02-26 US US15/904,826 patent/US20190040096A1/en not_active Abandoned
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2019
- 2019-09-09 JP JP2019163614A patent/JP2020002168A/ja active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1469008A1 (en) * | 2000-03-15 | 2004-10-20 | Hanmi Pharm. Co., Ltd. | Method of preparing a non-pharmaceutical grade clarithromycin |
| US20060100164A1 (en) * | 2003-03-10 | 2006-05-11 | Chang-Hsing Liang | Novel antibacterial agents |
| WO2007059307A2 (en) * | 2005-11-15 | 2007-05-24 | Teva Pharmaceutical Industries Ltd. | Crystalline and amorphous forms of telithromycin |
| WO2009053259A1 (en) * | 2007-10-25 | 2009-04-30 | Sandoz Ag | Process for the production of telithromycin |
| WO2009055557A1 (en) * | 2007-10-25 | 2009-04-30 | Cempra Pharmaceuticals, Inc. | Process for the preparation of macrolide antibacterial agents |
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