JP2015063536A5 - - Google Patents
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- Publication number
- JP2015063536A5 JP2015063536A5 JP2014231987A JP2014231987A JP2015063536A5 JP 2015063536 A5 JP2015063536 A5 JP 2015063536A5 JP 2014231987 A JP2014231987 A JP 2014231987A JP 2014231987 A JP2014231987 A JP 2014231987A JP 2015063536 A5 JP2015063536 A5 JP 2015063536A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- solution
- water
- process according
- formula
- 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.)
- Granted
Links
- 238000000034 method Methods 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 13
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 7
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical group CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 6
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 4
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 3
- 239000003960 organic solvent Substances 0.000 claims 3
- 239000002904 solvent Substances 0.000 claims 3
- 238000004821 distillation Methods 0.000 claims 2
- 238000001914 filtration Methods 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 238000003756 stirring Methods 0.000 claims 2
- IXXFZUPTQVDPPK-ZAWHAJPISA-N (1r,2r,4r,6r,7r,8r,10s,13r,14s)-17-[4-[4-(3-aminophenyl)triazol-1-yl]butyl]-7-[(2s,3r,4s,6r)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-13-ethyl-10-fluoro-6-methoxy-2,4,6,8,10,14-hexamethyl-12,15-dioxa-17-azabicyclo[12.3.0]heptadecane-3,9,11,16-tet Chemical compound O([C@@H]1[C@@H](C)C(=O)[C@](C)(F)C(=O)O[C@@H]([C@]2(OC(=O)N(CCCCN3N=NC(=C3)C=3C=C(N)C=CC=3)[C@@H]2[C@@H](C)C(=O)[C@H](C)C[C@@]1(C)OC)C)CC)[C@@H]1O[C@H](C)C[C@H](N(C)C)[C@H]1O IXXFZUPTQVDPPK-ZAWHAJPISA-N 0.000 claims 1
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 claims 1
- 238000010438 heat treatment Methods 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31606310P | 2010-03-22 | 2010-03-22 | |
| US61/316,063 | 2010-03-22 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013501396A Division JP5711352B2 (ja) | 2010-03-22 | 2011-03-22 | マクロライドの結晶形、およびその使用 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016244733A Division JP2017081953A (ja) | 2010-03-22 | 2016-12-16 | マクロライドの結晶形、およびその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015063536A JP2015063536A (ja) | 2015-04-09 |
| JP2015063536A5 true JP2015063536A5 (enExample) | 2015-08-06 |
| JP6121387B2 JP6121387B2 (ja) | 2017-04-26 |
Family
ID=44673574
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013501396A Active JP5711352B2 (ja) | 2010-03-22 | 2011-03-22 | マクロライドの結晶形、およびその使用 |
| JP2014231987A Active JP6121387B2 (ja) | 2010-03-22 | 2014-11-14 | マクロライドの結晶形、およびその使用 |
| JP2016244733A Pending JP2017081953A (ja) | 2010-03-22 | 2016-12-16 | マクロライドの結晶形、およびその使用 |
| JP2019163614A Pending JP2020002168A (ja) | 2010-03-22 | 2019-09-09 | マクロライドの結晶形、およびその使用 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013501396A Active JP5711352B2 (ja) | 2010-03-22 | 2011-03-22 | マクロライドの結晶形、およびその使用 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016244733A Pending JP2017081953A (ja) | 2010-03-22 | 2016-12-16 | マクロライドの結晶形、およびその使用 |
| JP2019163614A Pending JP2020002168A (ja) | 2010-03-22 | 2019-09-09 | マクロライドの結晶形、およびその使用 |
Country Status (19)
| Country | Link |
|---|---|
| US (4) | US8975386B2 (enExample) |
| EP (2) | EP3009442B1 (enExample) |
| JP (4) | JP5711352B2 (enExample) |
| KR (2) | KR20180101643A (enExample) |
| CN (2) | CN103080122A (enExample) |
| AU (2) | AU2011232627B2 (enExample) |
| BR (1) | BR112012023950A2 (enExample) |
| CA (1) | CA2793884C (enExample) |
| DK (1) | DK2550286T3 (enExample) |
| ES (1) | ES2564097T3 (enExample) |
| HR (1) | HRP20160168T1 (enExample) |
| IL (1) | IL222018B (enExample) |
| MX (1) | MX361413B (enExample) |
| MY (1) | MY162411A (enExample) |
| NZ (1) | NZ602544A (enExample) |
| PL (1) | PL2550286T3 (enExample) |
| RU (1) | RU2650883C2 (enExample) |
| SI (1) | SI2550286T1 (enExample) |
| WO (1) | WO2011119604A1 (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2529817C (en) | 2003-03-10 | 2013-02-12 | Optimer Pharmaceuticals, Inc. | Novel antibacterial agents |
| AU2008316830B2 (en) | 2007-10-25 | 2016-03-17 | Cempra Pharmaceuticals, Inc. | Process for the preparation of macrolide antibacterial agents |
| WO2010048600A1 (en) | 2008-10-24 | 2010-04-29 | Cempra Pharmaceuticals, Inc. | Methods for treating resistant diseases 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 |
| HRP20160168T1 (hr) | 2010-03-22 | 2016-03-25 | Cempra Pharmaceuticals Inc | Kristalne forme makrolida i njihova uporaba |
| EP2571506B1 (en) | 2010-05-20 | 2017-05-10 | Cempra Pharmaceuticals, Inc. | Processes for preparing macrolides and ketolides and intermediates therefor |
| KR20130120458A (ko) | 2010-09-10 | 2013-11-04 | 셈프라 파마슈티컬스, 인크. | 질환을 치료하기 위한 수소결합 형성 플루오로 케토라이드 |
| WO2013148891A1 (en) | 2012-03-27 | 2013-10-03 | Cempra Pharmaceuticals, Inc. | Parenteral formulations for administering macrolide antibiotics |
| EP2968801B1 (en) | 2013-03-14 | 2018-09-26 | Cempra Pharmaceuticals, Inc. | Methods for treating respiratory diseases and formulations therefor |
| MX356772B (es) | 2013-03-15 | 2018-06-13 | Cempra Pharmaceuticals Inc | Procesos convergentes para la preparacion de agentes antibacterianos macrolidos. |
| CN105246334A (zh) | 2013-04-04 | 2016-01-13 | 哈佛大学的校长及成员们 | 大环内酯及其制备和使用方法 |
| CN106604729A (zh) * | 2014-08-05 | 2017-04-26 | 森普拉制药公司 | 抗菌剂的粉末口服混悬制剂 |
| 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 |
| 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 |
| 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 |
| AU2020395150A1 (en) * | 2019-12-02 | 2022-06-23 | AliquantumRx, Inc. | Salts and polymorphs of cethromycin for the treatment of disease salts and polymorphs of cethromycin |
Family Cites Families (66)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US5527780A (en) | 1992-11-05 | 1996-06-18 | Roussel Uclaf | Erythromycin derivatives |
| FR2697524B1 (fr) | 1992-11-05 | 1994-12-23 | Roussel Uclaf | Nouveaux dérivés de l'érythromycine, leur procédé de préparation et leur application comme médicaments. |
| 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. |
| US5834428A (en) | 1995-04-14 | 1998-11-10 | 1149336 Ontario Inc. | Glucagon-like peptide-2 and its therapeutic use |
| FR2739620B1 (fr) | 1995-10-09 | 1997-12-19 | Roussel Uclaf | Nouveaux derives de la 5-0-desosaminyl 6-o-methyl erythronolide a, leur procede de preparation et leur application a la preparation de produits biologiquement actifs |
| US6274715B1 (en) | 1995-11-08 | 2001-08-14 | Abbott Laboratories | Tricyclic erythromycin derivatives |
| FR2742757B1 (fr) | 1995-12-22 | 1998-01-30 | Roussel Uclaf | Nouveaux derives de l'erythromycine, leur procede de preparation et leur application comme medicaments |
| FR2745290B1 (fr) | 1996-02-28 | 1998-04-03 | Roussel Uclaf | Nouveaux derives de l'erythromycine, leur procede de preparation et leur application comme medicaments |
| EP1291351B1 (en) | 1996-09-04 | 2005-07-13 | Abbott Laboratories | 6-0 substituted ketolides having antibacterial activity |
| US6407074B1 (en) | 1997-06-11 | 2002-06-18 | Pfizer Inc | C-4″-substituted macrolide derivatives |
| HN1998000086A (es) | 1997-06-11 | 1999-03-08 | Pfizer Prod Inc | Derivados de 9 - desofo - 9 aza - 9a - homoeritromicina a - c - 4 sustituidos. |
| PL337606A1 (en) | 1997-06-11 | 2000-08-28 | Pfizer Prod Inc | Derivatives of erythromycin 9-oxime |
| HN1998000159A (es) | 1997-10-29 | 1999-02-09 | Monsanto Co | Derivados de 9- amino - 3 ceto eritromicina |
| IL135792A0 (en) | 1997-12-01 | 2001-05-20 | Abbott Lab | 6-o-alkyl derivatives of erythronolide b |
| 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 |
| US6387885B1 (en) | 1998-08-26 | 2002-05-14 | Abbott Laboratories | 3′,3′-N-bis-desmethyl-3′-N-cycloalkyl erythromycin derivatives as LHRH antagonists |
| 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 |
| 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 |
| KR100317907B1 (ko) | 1998-11-24 | 2001-12-24 | 김 완 주 | 신규한 중간체, 이를 이용한 마크로라이드계 항생제의제조방법 |
| AU6484199A (en) | 1998-12-10 | 2000-06-26 | Pfizer Products Inc. | Carbamate and carbazate ketolide antibiotics |
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| CN1373767A (zh) | 1999-04-16 | 2002-10-09 | 奥索-麦克尼尔药品公司 | 酮式大环内酯抗菌剂 |
| US6420535B1 (en) | 1999-06-07 | 2002-07-16 | Abbott Laboratories | 6-O-carbamate ketolide derivatives |
| US6437106B1 (en) | 1999-06-24 | 2002-08-20 | Abbott Laboratories | Process for preparing 6-o-substituted erythromycin derivatives |
| WO2001010878A1 (fr) | 1999-08-06 | 2001-02-15 | Taisho Pharmaceutical Co., Ltd. | Derives d'erythromycine a |
| KR100336447B1 (ko) | 1999-11-24 | 2002-05-15 | 민경윤 | 클라리스로마이신의 개선된 제조방법 |
| JP2001261694A (ja) | 2000-03-06 | 2001-09-26 | Pfizer Prod Inc | ケトライド抗生物質 |
| DE60122791T2 (de) | 2000-03-15 | 2007-10-04 | Hanmi Pharm. Co., Ltd. | Verfahren zur Herstellung von Clarythromycin mit nicht pharmazeutischer Qualität |
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| GB0031312D0 (en) | 2000-12-21 | 2001-02-07 | Glaxo Group Ltd | Macrolides |
| PT1320355E (pt) | 2001-05-18 | 2006-08-31 | Chiron Corp | Sistema para administracao de uma formulacao de tobramicina |
| CA2451391A1 (en) | 2001-07-03 | 2003-01-16 | Chiron Corporation | C12 modified erythromycin macrolides and ketolides having antibacterial activity |
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| AU2003218059A1 (en) | 2002-02-22 | 2003-09-09 | Pharmacia Corporation | Ophthalmic antibiotic drug formulations containing a cyclodextrin compound and cetyl pyridinium chloride |
| ATE469135T1 (de) | 2002-05-30 | 2010-06-15 | Scripps Research Inst | Kupferkatalysierte ligierung von aziden und acetylenen |
| AR043050A1 (es) | 2002-09-26 | 2005-07-13 | Rib X Pharmaceuticals Inc | Compuestos heterociclicos bifuncionales y metodos para preparar y usar los mismos |
| ITMI20022292A1 (it) | 2002-10-29 | 2004-04-30 | Zambon Spa | 9a-azalidi ad attivita' antiinfiammatoria. |
| CA2529817C (en) | 2003-03-10 | 2013-02-12 | Optimer Pharmaceuticals, Inc. | Novel antibacterial agents |
| JP2006524706A (ja) | 2003-04-25 | 2006-11-02 | カイロン コーポレイション | 新規なケトライド誘導体 |
| US20050014706A1 (en) | 2003-07-14 | 2005-01-20 | Kanakeshwari Falzari | Method of treating tuberculosis |
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| CA2591746A1 (en) * | 2004-12-21 | 2006-06-29 | Pfizer Products Inc. | Macrolides |
| US20080113926A1 (en) | 2005-01-14 | 2008-05-15 | Zrinka Ivezic | 9A-Carbamoyl-Y-Aminopropyl- And 9A-Thiocabamoyl-Y-Aminopropyl-Azalides With Antimalarial Activity |
| WO2007039914A2 (en) | 2005-10-06 | 2007-04-12 | Alembic Limited | Novel polymorphs of telithromycin |
| US20070167382A1 (en) * | 2005-11-15 | 2007-07-19 | Nina Finkelstein | Crystalline and amorphous forms of telithromycin |
| WO2007060627A2 (en) | 2005-11-23 | 2007-05-31 | Ranbaxy Laboratories Limited | Use of macrolide derivatives for treating acne |
| DOP2006000268A (es) | 2005-12-22 | 2007-07-31 | Pfizer Prod Inc | Agentes antibacterianos |
| CN101129383B (zh) | 2006-08-25 | 2014-04-02 | 天津和美生物技术有限公司 | 含氨基糖苷类抗生素的抗生素复方 |
| US7742562B2 (en) * | 2007-06-27 | 2010-06-22 | Accuray Incorporated | Lower-torso assembly of a treatment couch useable in an X-ray environment |
| AU2008316830B2 (en) | 2007-10-25 | 2016-03-17 | Cempra Pharmaceuticals, Inc. | Process for the preparation of macrolide antibacterial agents |
| WO2009053259A1 (en) * | 2007-10-25 | 2009-04-30 | Sandoz Ag | Process for the production of telithromycin |
| WO2010048600A1 (en) * | 2008-10-24 | 2010-04-29 | Cempra Pharmaceuticals, Inc. | Methods for treating resistant diseases using triazole containing macrolides |
| PL2544537T3 (pl) | 2010-03-10 | 2017-10-31 | Cempra Pharmaceuticals Inc | Pozajelitowe preparaty antybiotyków makrolidowych |
| HRP20160168T1 (hr) * | 2010-03-22 | 2016-03-25 | Cempra Pharmaceuticals Inc | Kristalne forme makrolida i njihova uporaba |
-
2011
- 2011-03-22 HR HRP20160168T patent/HRP20160168T1/hr unknown
- 2011-03-22 DK DK11760068.4T patent/DK2550286T3/en active
- 2011-03-22 NZ NZ602544A patent/NZ602544A/en not_active IP Right Cessation
- 2011-03-22 BR BR112012023950A patent/BR112012023950A2/pt not_active Application Discontinuation
- 2011-03-22 US US13/636,510 patent/US8975386B2/en not_active Expired - Fee Related
- 2011-03-22 CN CN2011800174629A patent/CN103080122A/zh active Pending
- 2011-03-22 EP EP15194057.4A patent/EP3009442B1/en active Active
- 2011-03-22 RU RU2012144614A patent/RU2650883C2/ru not_active IP Right Cessation
- 2011-03-22 PL PL11760068T patent/PL2550286T3/pl unknown
- 2011-03-22 WO PCT/US2011/029424 patent/WO2011119604A1/en not_active Ceased
- 2011-03-22 MY MYPI2012004183A patent/MY162411A/en unknown
- 2011-03-22 SI SI201130745T patent/SI2550286T1/sl unknown
- 2011-03-22 MX MX2012010895A patent/MX361413B/es active IP Right Grant
- 2011-03-22 ES ES11760068.4T patent/ES2564097T3/es active Active
- 2011-03-22 EP EP11760068.4A patent/EP2550286B1/en not_active Revoked
- 2011-03-22 CN CN201810569806.0A patent/CN108570083A/zh active Pending
- 2011-03-22 AU AU2011232627A patent/AU2011232627B2/en not_active Ceased
- 2011-03-22 KR KR1020187025895A patent/KR20180101643A/ko not_active Ceased
- 2011-03-22 CA CA2793884A patent/CA2793884C/en not_active Expired - Fee Related
- 2011-03-22 KR KR1020127027222A patent/KR102006200B1/ko not_active Expired - Fee Related
- 2011-03-22 JP JP2013501396A patent/JP5711352B2/ja active Active
-
2012
- 2012-09-20 IL IL222018A patent/IL222018B/en not_active IP Right Cessation
-
2013
- 2013-05-22 US US13/900,147 patent/US8759500B2/en not_active Expired - Fee Related
-
2014
- 2014-11-14 JP JP2014231987A patent/JP6121387B2/ja active Active
-
2015
- 2015-09-21 US US14/859,736 patent/US20160244472A1/en not_active Abandoned
-
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
-
2019
- 2019-09-09 JP JP2019163614A patent/JP2020002168A/ja active Pending
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