CN101031572A - (r/s)利福霉素衍生物,它们的制备和药物组合物 - Google Patents
(r/s)利福霉素衍生物,它们的制备和药物组合物 Download PDFInfo
- Publication number
- CN101031572A CN101031572A CNA2005800308596A CN200580030859A CN101031572A CN 101031572 A CN101031572 A CN 101031572A CN A2005800308596 A CNA2005800308596 A CN A2005800308596A CN 200580030859 A CN200580030859 A CN 200580030859A CN 101031572 A CN101031572 A CN 101031572A
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- Prior art keywords
- compound
- cyclopropyl
- solvent
- formula
- methyl
- Prior art date
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D455/00—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
- C07D455/02—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing not further condensed quinolizine ring systems
Abstract
Description
生物 | 利福平 | 环丙沙星 | 实施例1 | 实施例2 | |
金黄色葡萄球菌ATCC29213 | RifS | 0.008 | 0.25 | 0.06 | 0.24 |
金黄色葡萄球菌ATCC29213 rpoBD417V | RifR | >256 | 0.25 | 0.5 | 8 |
金黄色葡萄球菌MT1222a gyrAA116EgrlBS80F | CipR | 0.004 | 8 | 0.06 | 0.24 |
表皮葡萄球菌ATCC1228 | RifR | 0.03 | 0.125 | 0.06 | 0.12 |
肺炎链球菌ATCC6303 | RifS | 0.061 | 1 | 0.015 | 0.015 |
化脓性链球菌ATCC19615 | RifS | 0.013 | 0.5 | 0.015 | 0.03 |
流感杆菌ATCC10211 | RifS | 0.24 | 0.008 | 0.5 | 0.5 |
Claims (15)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US59019004P | 2004-07-22 | 2004-07-22 | |
US60/590,190 | 2004-07-22 | ||
PCT/US2005/025924 WO2006012443A1 (en) | 2004-07-22 | 2005-07-21 | (r/s) rifamycin derivatives, their preparation and pharmaceutical compositions |
Publications (2)
Publication Number | Publication Date |
---|---|
CN101031572A true CN101031572A (zh) | 2007-09-05 |
CN101031572B CN101031572B (zh) | 2010-12-08 |
Family
ID=35355764
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN2005800308596A Active CN101031572B (zh) | 2004-07-22 | 2005-07-21 | (r/s)利福霉素衍生物,它们的制备和药物组合物 |
CNA2005800316554A Pending CN101065385A (zh) | 2004-07-22 | 2005-07-21 | 治疗微生物感染的利福霉素衍生物 |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CNA2005800316554A Pending CN101065385A (zh) | 2004-07-22 | 2005-07-21 | 治疗微生物感染的利福霉素衍生物 |
Country Status (11)
Country | Link |
---|---|
US (2) | US7226931B2 (zh) |
EP (2) | EP1781670A1 (zh) |
JP (2) | JP5153329B2 (zh) |
CN (2) | CN101031572B (zh) |
AT (1) | ATE427311T1 (zh) |
AU (1) | AU2005267054B2 (zh) |
CA (2) | CA2574307A1 (zh) |
DE (1) | DE602005013671D1 (zh) |
HK (1) | HK1102808A1 (zh) |
NZ (1) | NZ565002A (zh) |
WO (2) | WO2006012470A1 (zh) |
Cited By (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102834398A (zh) * | 2010-02-19 | 2012-12-19 | 萨利克斯药品有限公司 | 利福昔明的晶型及其用途 |
CN103709177A (zh) * | 2013-12-20 | 2014-04-09 | 武汉工程大学 | 利福霉素类沃尼妙林杂合抗生素及其制备方法 |
CN104628745A (zh) * | 2015-03-06 | 2015-05-20 | 丹诺医药(苏州)有限公司 | 一种利福霉素-喹嗪酮双靶标分子的富马酸盐及其制备方法 |
CN104710439A (zh) * | 2015-03-06 | 2015-06-17 | 丹诺医药(苏州)有限公司 | 一种利福霉素-喹嗪酮双靶标分子的晶型i及其制备方法 |
US9181274B2 (en) | 2008-02-25 | 2015-11-10 | Karen S. Gushurst | Forms of rifaximin and uses thereof |
CN105879009A (zh) * | 2016-04-18 | 2016-08-24 | 丹诺医药(苏州)有限公司 | 一种用于治疗革兰氏阴性菌感染的抗菌药物组合物 |
CN106822125A (zh) * | 2017-02-28 | 2017-06-13 | 丹诺医药(苏州)有限公司 | 一种利福霉素‑喹嗪酮双靶标分子的新用途 |
CN106902116A (zh) * | 2017-02-28 | 2017-06-30 | 丹诺医药(苏州)有限公司 | 一种利福霉素‑喹嗪酮双靶标分子的新应用 |
CN108310393A (zh) * | 2018-02-12 | 2018-07-24 | 丹诺医药(苏州)有限公司 | 一种利福霉素-喹嗪酮偶联分子的应用 |
CN109464673A (zh) * | 2019-01-08 | 2019-03-15 | 丹诺医药(苏州)有限公司 | 利福霉素-喹嗪酮偶联分子及其盐的应用和制剂 |
CN109529045A (zh) * | 2019-01-08 | 2019-03-29 | 丹诺医药(苏州)有限公司 | 利福霉素-喹嗪酮偶联分子及其药学上可接受的盐的应用 |
CN115501230A (zh) * | 2022-08-05 | 2022-12-23 | 丹诺医药(苏州)有限公司 | 利福霉素-喹嗪酮偶联分子软膏剂及其制备方法 |
Families Citing this family (34)
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US6544555B2 (en) | 2000-02-24 | 2003-04-08 | Advancis Pharmaceutical Corp. | Antibiotic product, use and formulation thereof |
US6541014B2 (en) * | 2000-10-13 | 2003-04-01 | Advancis Pharmaceutical Corp. | Antiviral product, use and formulation thereof |
US20020068078A1 (en) * | 2000-10-13 | 2002-06-06 | Rudnic Edward M. | Antifungal product, use and formulation thereof |
US20020197314A1 (en) * | 2001-02-23 | 2002-12-26 | Rudnic Edward M. | Anti-fungal composition |
JP2006528185A (ja) * | 2003-07-21 | 2006-12-14 | アドバンシス ファーマスーティカル コーポレイション | 抗生物質製剤、その使用法及び作成方法 |
US8313776B2 (en) * | 2003-07-21 | 2012-11-20 | Shionogi Inc. | Antibiotic product, use and formulation thereof |
US8313775B2 (en) * | 2003-07-21 | 2012-11-20 | Shionogi Inc. | Antibiotic product, use and formulation thereof |
WO2005016311A1 (en) | 2003-08-11 | 2005-02-24 | Advancis Pharmaceutical Corporation | Robust pellet |
JP2007502294A (ja) * | 2003-08-12 | 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 | 抗生物質製剤、その使用法及び作成方法 |
EP1658034A4 (en) * | 2003-08-29 | 2011-06-22 | Middlebrook Pharmaceuticals Inc | ANTIBIOTIC PRODUCT, ITS USE AND FORMULATION |
JP2007513869A (ja) * | 2003-09-15 | 2007-05-31 | アドバンシス ファーマスーティカル コーポレイション | 抗生物質製剤、その使用法及び作成方法 |
US7569599B2 (en) | 2003-12-12 | 2009-08-04 | Daiichi Pharmaceutical Co., Ltd. | Intermediates for the production of optically active cyclopropylamine derivatives and process for the production of the intermediates |
JP2008505124A (ja) * | 2004-07-02 | 2008-02-21 | アドバンシス ファーマスーティカル コーポレイション | パルス送達用錠剤 |
GB0505909D0 (en) * | 2005-03-23 | 2005-04-27 | Univ Leeds | Formulations |
CN101282981B (zh) | 2005-08-11 | 2012-09-26 | 塔甘塔治疗公司 | 膦酸化利福霉素及其在预防和治疗骨和关节感染中的用途 |
US7892826B2 (en) | 2005-08-15 | 2011-02-22 | Janssen Pharmaceutica N.V. | Human cell clones having an endogeneous urotensin II receptor |
US8778924B2 (en) * | 2006-12-04 | 2014-07-15 | Shionogi Inc. | Modified release amoxicillin products |
US8357394B2 (en) | 2005-12-08 | 2013-01-22 | Shionogi Inc. | Compositions and methods for improved efficacy of penicillin-type antibiotics |
US8299052B2 (en) * | 2006-05-05 | 2012-10-30 | Shionogi Inc. | Pharmaceutical compositions and methods for improved bacterial eradication |
TWI454262B (zh) | 2006-11-02 | 2014-10-01 | Targacept Inc | 菸鹼乙醯膽鹼受體亞型選擇性之二氮雜雙環烷類醯胺 |
WO2009064792A1 (en) * | 2007-11-16 | 2009-05-22 | Cumbre Pharmaceuticals Inc. | Quinolone carboxylic acid-substituted rifamycin derivatives |
RU2010140613A (ru) * | 2008-03-05 | 2012-04-10 | Таргасепт, Инк. (Us) | Амиды диазабициклоалканов, селективные в отношении подтипа никотиновых ацетилхолиновых рецепторов |
US8278313B2 (en) * | 2008-03-11 | 2012-10-02 | Abbott Laboratories | Macrocyclic spiro pyrimidine derivatives |
WO2010019511A2 (en) | 2008-08-13 | 2010-02-18 | Targanta Therapeutics Corp. | Phosphonated rifamycins and uses thereof for the prevention and treatment of bone and joint infections |
CN101875658B (zh) * | 2009-04-28 | 2013-01-09 | 上海药明康德新药开发有限公司 | 3-羰基-2,8-二氮杂螺[4.5] 癸烷-8-羧酸叔丁酯的制备方法 |
JP5759470B2 (ja) | 2009-10-23 | 2015-08-05 | ヤンセン ファーマシューティカ エヌ.ベー. | オレキシン受容体調節因子としての二置換オクタヒドロピロロ[3,4−c]ピロール |
AU2011261375B2 (en) | 2010-06-04 | 2016-09-22 | Albany Molecular Research, Inc. | Glycine transporter-1 inhibitors, methods of making them, and uses thereof |
UA120030C2 (uk) * | 2012-08-13 | 2019-09-25 | Адіфарм Еад | Фармацевтичні склади, які містять 3-(4-цинаміл-1-піперазиніл)амінопохідні 3-формілрифаміцину s та їх застосування |
WO2014043320A1 (en) * | 2012-09-12 | 2014-03-20 | Salix Pharmaceuticals, Inc. | Methods of administering rifaximin without producing antibiotic resistance |
HRP20220642T1 (hr) | 2016-03-10 | 2022-06-24 | Janssen Pharmaceutica Nv | Postupci za liječenje depresije uporabom antagonista receptora oreksina 2 |
CN109563034A (zh) * | 2016-06-08 | 2019-04-02 | 葛兰素史密斯克莱知识产权发展有限公司 | 化学化合物 |
CN109251258B (zh) * | 2017-07-13 | 2021-06-01 | 中国石油天然气股份有限公司 | 宽分布聚丙烯催化组分、组分制备方法及其催化剂 |
CN110944999A (zh) | 2017-08-01 | 2020-03-31 | 勃林格殷格翰国际有限公司 | 中间体化合物和方法 |
CN109942474B (zh) * | 2019-03-04 | 2020-09-18 | 华中科技大学 | 一种邻叠氮-肼类化合物及其制备方法 |
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DE68924722T2 (de) * | 1988-03-18 | 1996-04-18 | Kanegafuchi Chemical Ind | Substituiertes Benzoxazinorifamycinderivat, Verfahren zur Herstellung und dieses Derivat enthaltende Bakterizidmittel. |
DK0700399T3 (da) * | 1993-05-24 | 2001-11-26 | Lepetit Spa | Derivater i 36-stilling af rifamyciner og anvendelse af sådanne som antimikrobemidler |
EP1453837A4 (en) * | 2001-11-21 | 2007-11-07 | Activbiotics Inc | TARGETED THERAPEUTIC AGENTS AND USES THEREOF |
US7247634B2 (en) * | 2004-01-13 | 2007-07-24 | Cumbre Pharmaceuticals Inc. | Rifamycin derivatives effective against drug-resistant microbes |
WO2005070941A1 (en) | 2004-01-13 | 2005-08-04 | Cumbre Pharmaceuticals Inc. | Rifamycin imino derivatives effective against drug-resistant microbes |
-
2005
- 2005-07-21 WO PCT/US2005/025969 patent/WO2006012470A1/en active Application Filing
- 2005-07-21 CN CN2005800308596A patent/CN101031572B/zh active Active
- 2005-07-21 CA CA002574307A patent/CA2574307A1/en not_active Abandoned
- 2005-07-21 US US11/186,425 patent/US7226931B2/en active Active
- 2005-07-21 AU AU2005267054A patent/AU2005267054B2/en active Active
- 2005-07-21 US US11/186,187 patent/US7229996B2/en active Active
- 2005-07-21 DE DE602005013671T patent/DE602005013671D1/de active Active
- 2005-07-21 JP JP2007522765A patent/JP5153329B2/ja active Active
- 2005-07-21 EP EP05773711A patent/EP1781670A1/en not_active Withdrawn
- 2005-07-21 AT AT05791212T patent/ATE427311T1/de not_active IP Right Cessation
- 2005-07-21 CA CA2574301A patent/CA2574301C/en active Active
- 2005-07-21 JP JP2007522780A patent/JP5236944B2/ja active Active
- 2005-07-21 CN CNA2005800316554A patent/CN101065385A/zh active Pending
- 2005-07-21 NZ NZ565002A patent/NZ565002A/en active Application Filing
- 2005-07-21 EP EP05791212A patent/EP1768987B1/en active Active
- 2005-07-21 WO PCT/US2005/025924 patent/WO2006012443A1/en active Application Filing
-
2007
- 2007-10-04 HK HK07110800.2A patent/HK1102808A1/xx unknown
Cited By (23)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US9700545B2 (en) | 2008-02-25 | 2017-07-11 | Salix Pharmaceuticals, Ltd | Forms of rifaximin and uses thereof |
US9034892B2 (en) | 2008-02-25 | 2015-05-19 | Salix Pharmaceuticals, Inc. | Forms of rifaximin and uses thereof |
US9181274B2 (en) | 2008-02-25 | 2015-11-10 | Karen S. Gushurst | Forms of rifaximin and uses thereof |
US9359357B2 (en) | 2008-02-25 | 2016-06-07 | Salix Pharmaceuticals, Ltd. | Forms of rifaximin and uses thereof |
US9546183B2 (en) | 2008-02-25 | 2017-01-17 | Salix Pharmaceuticals, Ltd | Forms of rifaximin and uses thereof |
CN102834398A (zh) * | 2010-02-19 | 2012-12-19 | 萨利克斯药品有限公司 | 利福昔明的晶型及其用途 |
CN103709177A (zh) * | 2013-12-20 | 2014-04-09 | 武汉工程大学 | 利福霉素类沃尼妙林杂合抗生素及其制备方法 |
CN104628745A (zh) * | 2015-03-06 | 2015-05-20 | 丹诺医药(苏州)有限公司 | 一种利福霉素-喹嗪酮双靶标分子的富马酸盐及其制备方法 |
CN104710439A (zh) * | 2015-03-06 | 2015-06-17 | 丹诺医药(苏州)有限公司 | 一种利福霉素-喹嗪酮双靶标分子的晶型i及其制备方法 |
CN104628745B (zh) * | 2015-03-06 | 2017-03-08 | 丹诺医药(苏州)有限公司 | 一种利福霉素‑喹嗪酮双靶标分子的富马酸盐及其制备方法 |
CN105879009A (zh) * | 2016-04-18 | 2016-08-24 | 丹诺医药(苏州)有限公司 | 一种用于治疗革兰氏阴性菌感染的抗菌药物组合物 |
WO2017181831A1 (zh) * | 2016-04-18 | 2017-10-26 | 丹诺医药(苏州)有限公司 | 一种用于治疗革兰氏阴性菌感染的抗菌药物组合物 |
CN106822125A (zh) * | 2017-02-28 | 2017-06-13 | 丹诺医药(苏州)有限公司 | 一种利福霉素‑喹嗪酮双靶标分子的新用途 |
CN106902116A (zh) * | 2017-02-28 | 2017-06-30 | 丹诺医药(苏州)有限公司 | 一种利福霉素‑喹嗪酮双靶标分子的新应用 |
WO2018157749A1 (zh) * | 2017-02-28 | 2018-09-07 | 丹诺医药(苏州)有限公司 | 一种利福霉素-喹嗪酮双靶标分子的新用途 |
CN108310393A (zh) * | 2018-02-12 | 2018-07-24 | 丹诺医药(苏州)有限公司 | 一种利福霉素-喹嗪酮偶联分子的应用 |
CN109464673A (zh) * | 2019-01-08 | 2019-03-15 | 丹诺医药(苏州)有限公司 | 利福霉素-喹嗪酮偶联分子及其盐的应用和制剂 |
CN109529045A (zh) * | 2019-01-08 | 2019-03-29 | 丹诺医药(苏州)有限公司 | 利福霉素-喹嗪酮偶联分子及其药学上可接受的盐的应用 |
WO2020143535A1 (zh) * | 2019-01-08 | 2020-07-16 | 丹诺医药(苏州)有限公司 | 利福霉素-喹嗪酮偶联分子及其盐的应用和制剂 |
WO2020143534A1 (zh) * | 2019-01-08 | 2020-07-16 | 丹诺医药(苏州)有限公司 | 利福霉素-喹嗪酮偶联分子及其药学上可接受的盐的应用 |
CN115501230A (zh) * | 2022-08-05 | 2022-12-23 | 丹诺医药(苏州)有限公司 | 利福霉素-喹嗪酮偶联分子软膏剂及其制备方法 |
CN115501230B (zh) * | 2022-08-05 | 2023-11-21 | 丹诺医药(苏州)有限公司 | 利福霉素-喹嗪酮偶联分子软膏剂及其制备方法 |
WO2024027816A1 (zh) * | 2022-08-05 | 2024-02-08 | 丹诺医药(苏州)有限公司 | 利福霉素-喹嗪酮偶联分子软膏剂及其制备方法 |
Also Published As
Publication number | Publication date |
---|---|
WO2006012443A1 (en) | 2006-02-02 |
EP1781670A1 (en) | 2007-05-09 |
WO2006012470A1 (en) | 2006-02-02 |
EP1768987B1 (en) | 2009-04-01 |
JP2008507549A (ja) | 2008-03-13 |
CN101031572B (zh) | 2010-12-08 |
HK1102808A1 (en) | 2007-12-07 |
AU2005267054B2 (en) | 2011-06-23 |
US20060019986A1 (en) | 2006-01-26 |
CA2574307A1 (en) | 2006-02-02 |
US7229996B2 (en) | 2007-06-12 |
CA2574301A1 (en) | 2006-02-02 |
NZ565002A (en) | 2009-08-28 |
DE602005013671D1 (de) | 2009-05-14 |
CA2574301C (en) | 2013-09-10 |
US20060019985A1 (en) | 2006-01-26 |
JP5236944B2 (ja) | 2013-07-17 |
JP5153329B2 (ja) | 2013-02-27 |
CN101065385A (zh) | 2007-10-31 |
ATE427311T1 (de) | 2009-04-15 |
EP1768987A1 (en) | 2007-04-04 |
AU2005267054A1 (en) | 2006-02-02 |
US7226931B2 (en) | 2007-06-05 |
JP2008507548A (ja) | 2008-03-13 |
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