JP2009524675A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2009524675A5 JP2009524675A5 JP2008552415A JP2008552415A JP2009524675A5 JP 2009524675 A5 JP2009524675 A5 JP 2009524675A5 JP 2008552415 A JP2008552415 A JP 2008552415A JP 2008552415 A JP2008552415 A JP 2008552415A JP 2009524675 A5 JP2009524675 A5 JP 2009524675A5
- Authority
- JP
- Japan
- Prior art keywords
- bioavailability
- tetracycline compound
- hydrogen
- use according
- enhancer
- 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
- 239000003623 enhancer Substances 0.000 claims 34
- 239000004098 Tetracycline Substances 0.000 claims 32
- 229960002180 tetracycline Drugs 0.000 claims 32
- 229930101283 tetracycline Natural products 0.000 claims 32
- 235000019364 tetracycline Nutrition 0.000 claims 32
- -1 tetracycline compound Chemical class 0.000 claims 32
- 239000001257 hydrogen Substances 0.000 claims 31
- 229910052739 hydrogen Inorganic materials 0.000 claims 31
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 28
- 239000003795 chemical substances by application Substances 0.000 claims 11
- 150000001875 compounds Chemical class 0.000 claims 10
- 230000002708 enhancing effect Effects 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 9
- 230000001965 increasing effect Effects 0.000 claims 8
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- 239000000651 prodrug Substances 0.000 claims 6
- 229940002612 prodrug Drugs 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 4
- 230000001050 lubricating effect Effects 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 239000001301 oxygen Substances 0.000 claims 4
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 3
- 125000002252 acyl group Chemical group 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000003282 alkyl amino group Chemical group 0.000 claims 3
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 3
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 3
- 125000004414 alkyl thio group Chemical group 0.000 claims 3
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 125000004103 aminoalkyl group Chemical group 0.000 claims 3
- 125000003710 aryl alkyl group Chemical group 0.000 claims 3
- 125000004663 dialkyl amino group Chemical group 0.000 claims 3
- 150000002148 esters Chemical class 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- KBPLFHHGFOOTCA-UHFFFAOYSA-N 1-Octanol Chemical compound CCCCCCCCO KBPLFHHGFOOTCA-UHFFFAOYSA-N 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- DWAQJAXMDSEUJJ-UHFFFAOYSA-M Sodium bisulfite Chemical compound [Na+].OS([O-])=O DWAQJAXMDSEUJJ-UHFFFAOYSA-M 0.000 claims 2
- 125000005197 alkyl carbonyloxy alkyl group Chemical group 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 235000010267 sodium hydrogen sulphite Nutrition 0.000 claims 2
- MJPPGVVIDGQOQT-UHFFFAOYSA-N 2-bromo-5-(2-bromo-2-nitroethenyl)furan Chemical compound [O-][N+](=O)C(Br)=CC1=CC=C(Br)O1 MJPPGVVIDGQOQT-UHFFFAOYSA-N 0.000 claims 1
- 229910002016 Aerosil® 200 Inorganic materials 0.000 claims 1
- UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 claims 1
- 230000003796 beauty Effects 0.000 claims 1
- 230000000903 blocking effect Effects 0.000 claims 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 239000001110 calcium chloride Substances 0.000 claims 1
- 229910001628 calcium chloride Inorganic materials 0.000 claims 1
- 125000002704 decyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 210000001198 duodenum Anatomy 0.000 claims 1
- 239000002702 enteric coating Substances 0.000 claims 1
- 238000009505 enteric coating Methods 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000003187 heptyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000005343 heterocyclic alkyl group Chemical group 0.000 claims 1
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000001400 nonyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000002347 octyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 239000003921 oil Substances 0.000 claims 1
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims 1
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims 1
- 229920000053 polysorbate 80 Polymers 0.000 claims 1
- 229940068968 polysorbate 80 Drugs 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 230000002829 reductive effect Effects 0.000 claims 1
- 230000003014 reinforcing effect Effects 0.000 claims 1
- 239000000377 silicon dioxide Substances 0.000 claims 1
- 235000012239 silicon dioxide Nutrition 0.000 claims 1
- 210000000813 small intestine Anatomy 0.000 claims 1
- 230000000087 stabilizing effect Effects 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US76181906P | 2006-01-24 | 2006-01-24 | |
| PCT/US2007/002081 WO2007087416A2 (en) | 2006-01-24 | 2007-01-24 | Methods of increasing oral bioavailability of tetracyclines |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010013625A Division JP2010106043A (ja) | 2006-01-24 | 2010-01-25 | テトラサイクリンの経口バイオアベイラビリティーを増加する方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2009524675A JP2009524675A (ja) | 2009-07-02 |
| JP2009524675A5 true JP2009524675A5 (enExample) | 2010-03-18 |
Family
ID=38181071
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008552415A Pending JP2009524675A (ja) | 2006-01-24 | 2007-01-24 | テトラサイクリンの経口バイオアベイラビリティーを増加する方法 |
| JP2010013625A Pending JP2010106043A (ja) | 2006-01-24 | 2010-01-25 | テトラサイクリンの経口バイオアベイラビリティーを増加する方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010013625A Pending JP2010106043A (ja) | 2006-01-24 | 2010-01-25 | テトラサイクリンの経口バイオアベイラビリティーを増加する方法 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US9078811B2 (enExample) |
| EP (2) | EP2298324A1 (enExample) |
| JP (2) | JP2009524675A (enExample) |
| AU (2) | AU2007208214B2 (enExample) |
| CA (1) | CA2639406A1 (enExample) |
| WO (1) | WO2007087416A2 (enExample) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6756365B2 (en) * | 1991-11-06 | 2004-06-29 | Trustees Of Tufts College | Reducing tetracycline resistance in living cells |
| US20040224927A1 (en) * | 2000-06-16 | 2004-11-11 | Trustees Of Tufts College | 7-N-substituted phenyl tetracycline compounds |
| US20020132798A1 (en) * | 2000-06-16 | 2002-09-19 | Nelson Mark L. | 7-phenyl-substituted tetracycline compounds |
| US7094806B2 (en) | 2000-07-07 | 2006-08-22 | Trustees Of Tufts College | 7, 8 and 9-substituted tetracycline compounds |
| US8088820B2 (en) * | 2001-04-24 | 2012-01-03 | Paratek Pharmaceuticals, Inc. | Substituted tetracycline compounds for the treatment of malaria |
| EP1648859B1 (en) | 2003-07-09 | 2013-02-27 | Paratek Pharmaceuticals, Inc. | Substituted tetracycline compounds |
| US20060287283A1 (en) * | 2003-07-09 | 2006-12-21 | Paratek Pharmaceuticals, Inc. | Prodrugs of 9-aminomethyl tetracycline compounds |
| CN1893956A (zh) | 2003-07-25 | 2007-01-10 | 沃纳奇尔科特公司 | 多西环素金属络合物固体剂型 |
| US8466132B2 (en) * | 2004-10-25 | 2013-06-18 | Paratek Pharmaceuticals, Inc. | Substituted tetracycline compounds |
| NZ556582A (en) * | 2005-01-21 | 2010-12-24 | Warner Chilcott Co Llc | A tetracycline metal complex in a solid dosage form |
| JP2008530023A (ja) | 2005-02-04 | 2008-08-07 | パラテック ファーマシューティカルズ インコーポレイテッド | テトラサイクリン化合物の１１ａ，１２−誘導体 |
| US20070093455A1 (en) * | 2005-07-21 | 2007-04-26 | Paul Abato | 10-substituted tetracyclines and methods of use thereof |
| EP2537934A3 (en) * | 2006-05-15 | 2013-04-10 | Paratek Pharmaceuticals, Inc. | Methods of regulating expression of genes or of gene products using substituted tetracycline compounds |
| SI2120963T1 (sl) | 2006-12-21 | 2019-02-28 | Paratek Pharmaceuticals, Inc. | Substituirane spojine tetraciklina za zdravljenje vnetnih kožnih motenj |
| JP5583411B2 (ja) * | 2006-12-21 | 2014-09-03 | パラテック ファーマシューティカルズ インコーポレイテッド | 細菌感染、ウイルス感染、および寄生虫感染の治療のためのテトラサイクリン誘導体 |
| EP2144614A1 (en) | 2007-04-12 | 2010-01-20 | Paratek Pharmaceuticals, Inc. | Methods for treating spinal muscular atrophy using tetracycline compounds |
| MX2010009693A (es) | 2008-03-05 | 2010-12-20 | Paratek Pharm Innc | Compuestos de monociclina y metodos de uso de la misma. |
| PT2271348T (pt) * | 2008-03-28 | 2018-04-16 | Paratek Pharm Innc | Formulação de comprimido oral de composto de tetraciclina |
| EP2276342A4 (en) * | 2008-04-14 | 2012-02-22 | Paratek Pharm Innc | SUBSTITUTED TETRACYCLIN COMPOUNDS |
| TW202436282A (zh) * | 2008-05-19 | 2024-09-16 | 美商Ｐｒｔｋ Ｓｐｖ２公司 | 四環素化合物之甲苯磺酸鹽及同素異形體 |
| US8906887B2 (en) | 2008-08-08 | 2014-12-09 | Tetraphase Pharmaceuticals, Inc. | C7-fluoro substituted tetracycline compounds |
| JP2012503017A (ja) * | 2008-09-19 | 2012-02-02 | パラテック ファーマシューティカルズ インコーポレイテッド | 関節リウマチの治療用のテトラサイクリン化合物および関連する治療方法 |
| CN107021887A (zh) | 2009-05-08 | 2017-08-08 | 四相制药公司 | 四环素类化合物 |
| PT2470500T (pt) | 2009-08-28 | 2018-01-09 | Tetraphase Pharmaceuticals Inc | Compostos de tetraciclina |
| US9119793B1 (en) | 2011-06-28 | 2015-09-01 | Medicis Pharmaceutical Corporation | Gastroretentive dosage forms for doxycycline |
| NZ722096A (en) * | 2011-12-15 | 2016-11-25 | Alkermes Pharma Ireland Ltd | Prodrugs of secondary amine compounds |
| PL2890673T3 (pl) | 2012-08-31 | 2019-06-28 | Tetraphase Pharmaceuticals, Inc. | Związki tetracyklinowe |
| US10842802B2 (en) | 2013-03-15 | 2020-11-24 | Medicis Pharmaceutical Corporation | Controlled release pharmaceutical dosage forms |
| EP3432891A4 (en) * | 2016-03-24 | 2019-10-30 | Paratek Pharmaceuticals, Inc. | METHOD FOR THE TREATMENT AND PREVENTION OF C. DIFFICILE |
| KR102660864B1 (ko) | 2016-10-19 | 2024-04-25 | 테트라페이즈 파마슈티컬스, 인코포레이티드 | 에라바사이클린의 결정질 형태 |
| US10383884B2 (en) | 2016-11-01 | 2019-08-20 | Paratek Pharmaceuticals, Inc. | 9-aminomethyl minocycline compounds and use thereof in treating community-acquired bacterial pneumonia (CABP) |
| PT117254B (pt) | 2021-05-26 | 2024-04-18 | Hovione Farm S A | Método de síntese de compostos 9-aminometil tetraciclinas |
| WO2023238143A1 (en) * | 2022-06-11 | 2023-12-14 | Gufic Biosciences Limited | A freeze dried parenteral composition of omadacycline tosylate with improved stability |
Family Cites Families (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2990331A (en) | 1956-11-23 | 1961-06-27 | Pfizer & Co C | Stable solutions of salts of tetracyclines for parenteral administration |
| US2980584A (en) | 1957-10-29 | 1961-04-18 | Pfizer & Co C | Parenteral magnesium oxytetracycline acetic or lactic acid carboxamide vehicle preparation |
| US3062717A (en) | 1958-12-11 | 1962-11-06 | Pfizer & Co C | Intramuscular calcium tetracycline acetic or lactic acid carboxamide vehicle preparation |
| US3165531A (en) | 1962-03-08 | 1965-01-12 | Pfizer & Co C | 13-substituted-6-deoxytetracyclines and process utilizing the same |
| US3454697A (en) | 1965-06-08 | 1969-07-08 | American Cyanamid Co | Tetracycline antibiotic compositions for oral use |
| NL6607516A (enExample) | 1966-05-31 | 1967-12-01 | ||
| DE1767891C3 (de) | 1968-06-28 | 1980-10-30 | Pfizer | Verfahren zur Herstellung von wäßrigen arzneilichen Lösungen für die parenterale, perorale und lokale Anwendung mit einem Gehalt an einem Tetracyclinderivat |
| US3957980A (en) | 1972-10-26 | 1976-05-18 | Pfizer Inc. | Doxycycline parenteral compositions |
| DE2442829A1 (de) | 1974-09-06 | 1976-03-18 | Merck Patent Gmbh | Tetracyclische verbindungen und verfahren zu ihrer herstellung |
| US4018889A (en) | 1976-01-02 | 1977-04-19 | Pfizer Inc. | Oxytetracycline compositions |
| US4126680A (en) | 1977-04-27 | 1978-11-21 | Pfizer Inc. | Tetracycline antibiotic compositions |
| DE3176215D1 (en) * | 1980-11-19 | 1987-07-02 | Procter & Gamble | Non-yellowing topical pharmaceutical composition |
| US5277916A (en) * | 1988-02-01 | 1994-01-11 | F. H. Faulding & Co., Ltd. | Tetracycline dosage form |
| IL95423A (en) * | 1989-09-21 | 1994-11-11 | American Cyanamid Co | Pulsatile once-a-day delivery systems for minocycline |
| US5188836A (en) * | 1990-07-27 | 1993-02-23 | Warner-Lambert Company | Sustained release formulations |
| JP3037393B2 (ja) * | 1990-10-22 | 2000-04-24 | 大正薬品工業株式会社 | 経口投与用固形薬剤の製造方法 |
| HUP0003364A3 (en) * | 1997-06-19 | 2002-03-28 | Sepracor Inc Marlborough | Quinoline-indole antimicrobial agents, uses and compositions related thereto |
| CA2383220C (en) * | 1999-09-02 | 2009-11-03 | Nostrum Pharmaceuticals, Inc. | Controlled release pellet formulation |
| US20030180352A1 (en) * | 1999-11-23 | 2003-09-25 | Patel Mahesh V. | Solid carriers for improved delivery of active ingredients in pharmaceutical compositions |
| US20030118547A1 (en) * | 2000-01-27 | 2003-06-26 | Vandenberg Grant William | Composition for intestinal delivery |
| KR101083571B1 (ko) | 2000-07-07 | 2011-11-14 | 파라테크 파마슈티컬스, 인크. | 7-치환 테트라사이클린 화합물 |
| ATE544745T1 (de) * | 2000-07-07 | 2012-02-15 | Tufts College | 9-substituierte minocyclinverbindungen |
| KR100863146B1 (ko) * | 2000-07-17 | 2008-10-14 | 아스텔라스세이야쿠 가부시키가이샤 | 경구 흡수 개선 의약 조성물 |
| ATE404528T1 (de) | 2001-03-13 | 2008-08-15 | Paratek Pharm Innc | 7,9 substituierte tetracyclinverbindungen |
| JP2005504722A (ja) * | 2001-03-14 | 2005-02-17 | パラテック ファーマシューティカルズ インコーポレイテッド | 相乗的抗真菌薬剤としての置換テトラサイクリン化合物 |
| ITMI20011756A1 (it) | 2001-08-09 | 2003-02-09 | Remedia S R L | Composizione farmaceutica comprendente una microemulsione doppia acqua/olio/acqua incorporata in un supporto solido |
| ES2551708T3 (es) | 2002-01-08 | 2015-11-23 | Paratek Pharmaceuticals, Inc. | Compuestos de 4-desdimetilamino tetraciclina |
| CN1653037A (zh) | 2002-03-21 | 2005-08-10 | 帕拉特克药品公司 | 取代的四环素化合物 |
| CA2503446C (en) * | 2002-10-24 | 2012-12-18 | Paratek Pharmaceuticals, Inc. | Methods of using substituted tetracycline compounds to modulate rna |
| US6841547B2 (en) * | 2003-02-28 | 2005-01-11 | Albert Einstein College Of Medicine Of Yeshevia University | Method for decreasing low density lipoprotein |
| WO2004091513A2 (en) | 2003-04-10 | 2004-10-28 | Paratek Pharmaceuticals, Inc. | 9-aminomethyl substituted minocycline compounds |
| US20050137174A1 (en) | 2003-07-09 | 2005-06-23 | Paratek Pharmaceuticals, Inc. | Prodrugs of 9-aminomethyl tetracycline compounds |
| EP1648859B1 (en) * | 2003-07-09 | 2013-02-27 | Paratek Pharmaceuticals, Inc. | Substituted tetracycline compounds |
| JP2007502296A (ja) | 2003-08-11 | 2007-02-08 | アドバンシス ファーマスーティカル コーポレイション | ロバストペレット |
| WO2005046651A1 (en) * | 2003-11-12 | 2005-05-26 | Ranbaxy Laboratories Limited | Liquid filled capsules of doxycycline |
| GB2414668B (en) * | 2004-06-03 | 2009-07-29 | Dexcel Ltd | Tetracycline modified release delivery system |
-
2007
- 2007-01-24 EP EP10192776A patent/EP2298324A1/en not_active Withdrawn
- 2007-01-24 EP EP07762567A patent/EP1991236A2/en not_active Withdrawn
- 2007-01-24 US US11/657,412 patent/US9078811B2/en active Active
- 2007-01-24 AU AU2007208214A patent/AU2007208214B2/en not_active Expired - Fee Related
- 2007-01-24 CA CA002639406A patent/CA2639406A1/en not_active Abandoned
- 2007-01-24 WO PCT/US2007/002081 patent/WO2007087416A2/en not_active Ceased
- 2007-01-24 JP JP2008552415A patent/JP2009524675A/ja active Pending
-
2010
- 2010-01-25 JP JP2010013625A patent/JP2010106043A/ja active Pending
- 2010-10-26 AU AU2010236028A patent/AU2010236028A1/en not_active Abandoned
-
2015
- 2015-07-01 US US14/789,506 patent/US20160030453A1/en not_active Abandoned