JP2013522229A5 - - Google Patents
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- Publication number
- JP2013522229A5 JP2013522229A5 JP2012557258A JP2012557258A JP2013522229A5 JP 2013522229 A5 JP2013522229 A5 JP 2013522229A5 JP 2012557258 A JP2012557258 A JP 2012557258A JP 2012557258 A JP2012557258 A JP 2012557258A JP 2013522229 A5 JP2013522229 A5 JP 2013522229A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- acyl
- aryl
- hydrogen
- pharmaceutical composition
- 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
- 239000000203 mixture Substances 0.000 claims 21
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 125000002252 acyl group Chemical group 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 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 5
- 239000002535 acidifier Substances 0.000 claims 5
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 5
- 125000002877 alkyl aryl group Chemical group 0.000 claims 4
- 125000003710 aryl alkyl group Chemical group 0.000 claims 4
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 4
- 125000001951 carbamoylamino group Chemical group C(N)(=O)N* 0.000 claims 4
- 125000004404 heteroalkyl group Chemical group 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 4
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 3
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims 3
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 3
- 229930195725 Mannitol Natural products 0.000 claims 3
- 239000004067 bulking agent Substances 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims 3
- 238000010790 dilution Methods 0.000 claims 3
- 239000012895 dilution Substances 0.000 claims 3
- 239000000594 mannitol Substances 0.000 claims 3
- 235000010355 mannitol Nutrition 0.000 claims 3
- 238000007911 parenteral administration Methods 0.000 claims 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims 3
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims 2
- 208000035143 Bacterial infection Diseases 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 239000004471 Glycine Substances 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 206010037075 Protozoal infections Diseases 0.000 claims 2
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims 2
- 229930006000 Sucrose Natural products 0.000 claims 2
- 208000022362 bacterial infectious disease Diseases 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 239000005720 sucrose Substances 0.000 claims 2
- LJGHYPLBDBRCRZ-UHFFFAOYSA-N 3-(3-aminophenyl)sulfonylaniline Chemical group NC1=CC=CC(S(=O)(=O)C=2C=C(N)C=CC=2)=C1 LJGHYPLBDBRCRZ-UHFFFAOYSA-N 0.000 claims 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims 1
- 125000004423 acyloxy group Chemical group 0.000 claims 1
- 230000003113 alkalizing effect Effects 0.000 claims 1
- 125000004450 alkenylene group Chemical group 0.000 claims 1
- 125000005001 aminoaryl group Chemical group 0.000 claims 1
- 230000000844 anti-bacterial effect Effects 0.000 claims 1
- 239000003963 antioxidant agent Substances 0.000 claims 1
- 230000003078 antioxidant effect Effects 0.000 claims 1
- 235000006708 antioxidants Nutrition 0.000 claims 1
- 229960005070 ascorbic acid Drugs 0.000 claims 1
- 235000010323 ascorbic acid Nutrition 0.000 claims 1
- 239000011668 ascorbic acid Substances 0.000 claims 1
- 239000002738 chelating agent Substances 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 235000015165 citric acid Nutrition 0.000 claims 1
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- -1 dimethylaminoalkyl Chemical group 0.000 claims 1
- 150000002016 disaccharides Chemical class 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000003630 glycyl group Chemical group [H]N([H])C([H])([H])C(*)=O 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 150000002772 monosaccharides Chemical class 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 239000011975 tartaric acid Substances 0.000 claims 1
- 235000002906 tartaric acid Nutrition 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31241710P | 2010-03-10 | 2010-03-10 | |
| US61/312,417 | 2010-03-10 | ||
| PCT/US2011/027984 WO2011112864A1 (en) | 2010-03-10 | 2011-03-10 | Parenteral formulations of macrolide antibiotics |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013522229A JP2013522229A (ja) | 2013-06-13 |
| JP2013522229A5 true JP2013522229A5 (enExample) | 2014-04-03 |
| JP5890785B2 JP5890785B2 (ja) | 2016-03-22 |
Family
ID=44563855
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012557258A Active JP5890785B2 (ja) | 2010-03-10 | 2011-03-10 | マクロライド抗生物質の非経口製剤 |
Country Status (11)
| Country | Link |
|---|---|
| US (3) | US20130045937A1 (enExample) |
| EP (1) | EP2544537B1 (enExample) |
| JP (1) | JP5890785B2 (enExample) |
| CN (2) | CN109091489A (enExample) |
| AU (1) | AU2011224238B2 (enExample) |
| CA (1) | CA2792616A1 (enExample) |
| DK (1) | DK2544537T3 (enExample) |
| ES (1) | ES2637072T3 (enExample) |
| PL (1) | PL2544537T3 (enExample) |
| SI (1) | SI2544537T1 (enExample) |
| WO (1) | WO2011112864A1 (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2801100A1 (en) | 2003-03-10 | 2004-09-23 | Optimer Pharmaceuticals, Inc. | Macrolides and processes for their preparation |
| CN101917850B (zh) | 2007-10-25 | 2016-01-13 | 森普拉制药公司 | 大环内酯类抗菌剂的制备方法 |
| CN107854477A (zh) | 2008-10-24 | 2018-03-30 | 森普拉制药公司 | 使用含三唑的大环内酯治疗抗性疾病的方法 |
| US9937194B1 (en) | 2009-06-12 | 2018-04-10 | Cempra Pharmaceuticals, Inc. | Compounds and methods for treating inflammatory diseases |
| WO2011032052A1 (en) | 2009-09-10 | 2011-03-17 | Cempra Pharmaceuticals, Inc. | Methods for treating malaria, tuberculosis and mac diseases |
| JP5711352B2 (ja) | 2010-03-22 | 2015-04-30 | 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 | マクロライドの結晶形、およびその使用 |
| US9051346B2 (en) | 2010-05-20 | 2015-06-09 | Cempra Pharmaceuticals, Inc. | Process for preparing triazole-containing ketolide antibiotics |
| US9815863B2 (en) | 2010-09-10 | 2017-11-14 | Cempra Pharmaceuticals, Inc. | Hydrogen bond forming fluoro ketolides for treating diseases |
| WO2013053076A1 (en) | 2011-10-10 | 2013-04-18 | Zensun （Shanghai）Science & Technology Limited | Compositions and methods for treating heart failure |
| 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 |
| WO2014152326A1 (en) | 2013-03-14 | 2014-09-25 | Cempra Pharmaceuticals, Inc. | Methods for treating respiratory diseases and formulations therefor |
| HK1220394A1 (zh) | 2013-03-15 | 2017-05-05 | Cempra Pharmaceuticals, Inc. | 收敛了制备大环内酯类抗菌剂 |
| KR102528984B1 (ko) | 2013-04-04 | 2023-05-08 | 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 | 매크롤라이드 그리고 그의 제조방법 및 용도 |
| JP6568052B2 (ja) | 2013-05-22 | 2019-09-04 | ゼンサン （シャンハイ） サイエンス アンド テクノロジー，シーオー．，エルティーディー． | 心不全を治療するためのニューレグリンの徐放 |
| CN110946993A (zh) | 2014-01-03 | 2020-04-03 | 上海泽生科技开发股份有限公司 | 纽兰格林制剂的配方 |
| EP3185864A4 (en) * | 2014-08-05 | 2018-03-28 | Cempra Pharmaceuticals, Inc. | Powder oral suspension formulations of antibacterial agents |
| WO2016057798A1 (en) | 2014-10-08 | 2016-04-14 | President And Fellows Of Harvard College | 14-membered ketolides and methods of their preparation and use |
| CN111407882A (zh) | 2014-10-17 | 2020-07-14 | 上海泽生科技开发股份有限公司 | 神经调节蛋白用于预防、治疗或延迟射血分数保留的心力衰竭的方法和组合物 |
| US10640528B2 (en) | 2015-03-25 | 2020-05-05 | President And Fellows Of Havard College | Macrolides with modified desosamine sugars and uses thereof |
| CA3144443A1 (en) * | 2019-06-28 | 2020-12-30 | Moleculin Biotech, Inc. | Method of reconstituting liposomal annamycin |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6395300B1 (en) * | 1999-05-27 | 2002-05-28 | Acusphere, Inc. | Porous drug matrices and methods of manufacture thereof |
| NZ523693A (en) * | 2000-07-10 | 2004-08-27 | Chiron Corp | Macrolide formulations for inhalation and methods of treatment of endobronchial infections |
| MXPA04008173A (es) * | 2002-02-22 | 2004-11-26 | Pharmacia Corp | Formulaciones de farmaco antibiotico oftalmico que contienen un compuesto de ciclodextrina y cloruro de cetil piridinio. |
| CA2801100A1 (en) * | 2003-03-10 | 2004-09-23 | Optimer Pharmaceuticals, Inc. | Macrolides and processes for their preparation |
| US20060116336A1 (en) * | 2004-03-17 | 2006-06-01 | American Pharmaceutical Partners, Inc. | Lyophilized azithromycin formulation |
| US7468428B2 (en) * | 2004-03-17 | 2008-12-23 | App Pharmaceuticals, Llc | Lyophilized azithromycin formulation |
| CN101045063B (zh) * | 2006-03-28 | 2011-01-26 | 广州朗圣药业有限公司 | 注射用克拉霉素水溶性制剂 |
| 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 |
-
2011
- 2011-03-10 EP EP11754115.1A patent/EP2544537B1/en not_active Not-in-force
- 2011-03-10 CA CA2792616A patent/CA2792616A1/en not_active Abandoned
- 2011-03-10 CN CN201811127818.4A patent/CN109091489A/zh active Pending
- 2011-03-10 SI SI201131266T patent/SI2544537T1/sl unknown
- 2011-03-10 ES ES11754115.1T patent/ES2637072T3/es active Active
- 2011-03-10 DK DK11754115.1T patent/DK2544537T3/en active
- 2011-03-10 CN CN2011800150681A patent/CN102811616A/zh active Pending
- 2011-03-10 US US13/583,556 patent/US20130045937A1/en not_active Abandoned
- 2011-03-10 AU AU2011224238A patent/AU2011224238B2/en not_active Ceased
- 2011-03-10 PL PL11754115T patent/PL2544537T3/pl unknown
- 2011-03-10 JP JP2012557258A patent/JP5890785B2/ja active Active
- 2011-03-10 WO PCT/US2011/027984 patent/WO2011112864A1/en not_active Ceased
-
2018
- 2018-03-12 US US15/918,098 patent/US20190054059A1/en not_active Abandoned
-
2019
- 2019-12-02 US US16/700,384 patent/US20200276150A1/en not_active Abandoned
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