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
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- 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) | KR102006200B1 (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 |
|---|---|---|---|---|
| EP1638549A4 (en) | 2003-03-10 | 2011-06-15 | Optimer Pharmaceuticals Inc | NEW ANTIBACTERIAL AGENTS |
| CA2703475A1 (en) | 2007-10-25 | 2009-04-30 | Cempra Pharmaceuticals, Inc. | Process for the preparation of macrolide antibacterial agents |
| US8796232B2 (en) | 2008-10-24 | 2014-08-05 | 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 |
| 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 |
| 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 |
| WO2011146829A1 (en) | 2010-05-20 | 2011-11-24 | Cempra Pharmaceuticals, Inc. | Processes for preparing macrolides and ketolides and intermediates therefor |
| 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 |
| 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 |
| BR112017002335A2 (pt) * | 2014-08-05 | 2018-01-16 | Cempra Pharmaceuticals, Inc. | formulações de suspensão oral em pó de agentes antibacterianos |
| 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 |
| EP3273969A4 (en) | 2015-03-25 | 2018-11-21 | President and Fellows of Harvard College | Macrolides with modified desosamine sugars and uses thereof |
| WO2017061431A1 (ja) * | 2015-10-05 | 2017-04-13 | 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 |
| TW201811811A (zh) * | 2016-09-02 | 2018-04-01 | 森普拉製藥公司 | 製備氟酮內酯之方法 |
| 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 |
Family Cites Families (66)
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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 |
| IL99995A (en) | 1990-11-21 | 1997-11-20 | Roussel Uclaf | Erythromycin derivatives, their preparation and pharmaceutical compositions containing them |
| 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. |
| 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 |
| SK285534B6 (sk) | 1996-09-04 | 2007-03-01 | Abbott Laboratories | 6-O-substituované ketolidy s antibakteriálnou aktivitou, farmaceutická kompozícia s ich obsahom, ich použitie a spôsob ich prípravy |
| HN1998000086A (es) | 1997-06-11 | 1999-03-08 | Pfizer Prod Inc | Derivados de 9 - desofo - 9 aza - 9a - homoeritromicina a - c - 4 sustituidos. |
| US6407074B1 (en) | 1997-06-11 | 2002-06-18 | Pfizer Inc | C-4″-substituted macrolide derivatives |
| CN1259135A (zh) | 1997-06-11 | 2000-07-05 | 辉瑞产品公司 | 9－肟红霉素衍生物 |
| HN1998000159A (es) | 1997-10-29 | 1999-02-09 | Monsanto Co | Derivados de 9- amino - 3 ceto eritromicina |
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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 |
| US6387885B1 (en) | 1998-08-26 | 2002-05-14 | Abbott Laboratories | 3′,3′-N-bis-desmethyl-3′-N-cycloalkyl erythromycin derivatives as LHRH antagonists |
| US6020521A (en) | 1998-08-26 | 2000-02-01 | Abbott Laboratories | Macrolide 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 |
| 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 |
| ES2273964T3 (es) | 1998-12-10 | 2007-05-16 | Pfizer Products Inc. | Antibioticos de carbamato y carbazato cetolida. |
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| WO2003101972A1 (en) | 2002-05-30 | 2003-12-11 | The Scripps Research Institute | Copper-catalysed ligation of azides and acetylenes |
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| EP1618120A2 (en) | 2003-04-25 | 2006-01-25 | Chiron Corporation | Novel ketolide derivatives |
| WO2005007143A2 (en) | 2003-07-14 | 2005-01-27 | The Board Of Trustees Of The University Of Illinois | Use of makrolides and ketolides for the treatment of tuberculosis |
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| US8796232B2 (en) * | 2008-10-24 | 2014-08-05 | Cempra Pharmaceuticals, Inc. | Methods for treating resistant diseases using triazole containing macrolides |
| 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 |
-
2011
- 2011-03-22 CN CN2011800174629A patent/CN103080122A/zh active Pending
- 2011-03-22 KR KR1020127027222A patent/KR102006200B1/ko not_active Expired - Fee Related
- 2011-03-22 CN CN201810569806.0A patent/CN108570083A/zh active Pending
- 2011-03-22 US US13/636,510 patent/US8975386B2/en not_active Expired - Fee Related
- 2011-03-22 JP JP2013501396A patent/JP5711352B2/ja active Active
- 2011-03-22 PL PL11760068T patent/PL2550286T3/pl unknown
- 2011-03-22 AU AU2011232627A patent/AU2011232627B2/en not_active Ceased
- 2011-03-22 SI SI201130745T patent/SI2550286T1/sl unknown
- 2011-03-22 NZ NZ602544A patent/NZ602544A/en not_active IP Right Cessation
- 2011-03-22 CA CA2793884A patent/CA2793884C/en not_active Expired - Fee Related
- 2011-03-22 BR BR112012023950A patent/BR112012023950A2/pt not_active Application Discontinuation
- 2011-03-22 DK DK11760068.4T patent/DK2550286T3/en active
- 2011-03-22 WO PCT/US2011/029424 patent/WO2011119604A1/en not_active Ceased
- 2011-03-22 EP EP15194057.4A patent/EP3009442B1/en active Active
- 2011-03-22 KR KR1020187025895A patent/KR20180101643A/ko not_active Ceased
- 2011-03-22 ES ES11760068.4T patent/ES2564097T3/es active Active
- 2011-03-22 HR HRP20160168T patent/HRP20160168T1/hr unknown
- 2011-03-22 MX MX2012010895A patent/MX361413B/es active IP Right Grant
- 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 MY MYPI2012004183A patent/MY162411A/en unknown
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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
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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