JP2000159790A - 新規のエリスロマイシン誘導体、それらの製造方法及びそれらの薬剤としての使用 - Google Patents
新規のエリスロマイシン誘導体、それらの製造方法及びそれらの薬剤としての使用Info
- Publication number
- JP2000159790A JP2000159790A JP11331141A JP33114199A JP2000159790A JP 2000159790 A JP2000159790 A JP 2000159790A JP 11331141 A JP11331141 A JP 11331141A JP 33114199 A JP33114199 A JP 33114199A JP 2000159790 A JP2000159790 A JP 2000159790A
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- Prior art keywords
- formula
- compound
- methyl
- acid addition
- group
- 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
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- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 2
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- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000002568 propynyl group Chemical group [*]C#CC([H])([H])[H] 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 125000002098 pyridazinyl group Chemical group 0.000 description 1
- 125000000714 pyrimidinyl group Chemical group 0.000 description 1
- 125000000168 pyrrolyl group Chemical group 0.000 description 1
- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 description 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 description 1
- 238000010992 reflux Methods 0.000 description 1
- 201000009890 sinusitis Diseases 0.000 description 1
- 235000019980 sodium acid phosphate Nutrition 0.000 description 1
- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 description 1
- 229910000104 sodium hydride Inorganic materials 0.000 description 1
- 239000012312 sodium hydride Substances 0.000 description 1
- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 238000010561 standard procedure Methods 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 125000004434 sulfur atom Chemical group 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- 239000013077 target material Substances 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 229960001367 tartaric acid Drugs 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- 125000001113 thiadiazolyl group Chemical group 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
- C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
- C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Oncology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Communicable Diseases (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR9814782 | 1998-11-24 | ||
| FR9814782A FR2786188B1 (fr) | 1998-11-24 | 1998-11-24 | Nouveaux derives de l'erythromycine, leur procede de preparation et leur applicaion comme medicaments |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2000159790A true JP2000159790A (ja) | 2000-06-13 |
| JP2000159790A5 JP2000159790A5 (enExample) | 2006-12-07 |
Family
ID=9533122
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP11331141A Pending JP2000159790A (ja) | 1998-11-24 | 1999-11-22 | 新規のエリスロマイシン誘導体、それらの製造方法及びそれらの薬剤としての使用 |
Country Status (24)
| Country | Link |
|---|---|
| US (2) | US6440941B1 (enExample) |
| EP (1) | EP1004592B1 (enExample) |
| JP (1) | JP2000159790A (enExample) |
| KR (1) | KR100587445B1 (enExample) |
| CN (1) | CN1165546C (enExample) |
| AR (1) | AR021388A1 (enExample) |
| AT (1) | ATE245160T1 (enExample) |
| AU (1) | AU772171B2 (enExample) |
| BR (1) | BR9905735A (enExample) |
| CA (1) | CA2290136C (enExample) |
| DE (1) | DE69909577T2 (enExample) |
| DK (1) | DK1004592T3 (enExample) |
| ES (1) | ES2198867T3 (enExample) |
| FR (1) | FR2786188B1 (enExample) |
| HU (1) | HUP9904392A3 (enExample) |
| IL (1) | IL133101A (enExample) |
| MX (1) | MXPA99010813A (enExample) |
| NO (1) | NO314729B1 (enExample) |
| PL (1) | PL336736A1 (enExample) |
| PT (1) | PT1004592E (enExample) |
| RU (1) | RU2237672C2 (enExample) |
| TR (1) | TR199902888A3 (enExample) |
| TW (1) | TWI247747B (enExample) |
| ZA (1) | ZA997176B (enExample) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2008508322A (ja) * | 2004-07-28 | 2008-03-21 | ランバクシー ラボラトリーズ リミテッド | 抗菌剤としてのケトライド誘導体 |
| JP4833078B2 (ja) * | 2003-11-25 | 2011-12-07 | アバンテイス・フアルマ・エス・アー | 急性または慢性神経退行を治療する薬剤の形態のピラゾリル誘導体 |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| OA11753A (en) * | 1999-01-27 | 2005-07-19 | Pfizer Prod Inc | Ketolide antibiotics. |
| KR20020016799A (ko) | 1999-05-24 | 2002-03-06 | 데이비드 존 우드 | 13-메틸-에리트로마이신 유도체 |
| EP1167376B1 (en) | 2000-06-30 | 2004-07-14 | Pfizer Products Inc. | Macrolide antibiotics |
| 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 |
| US8552162B2 (en) | 2008-05-09 | 2013-10-08 | Enanta Pharmaceuticals, Inc. | Processes for the preparation of 2 fluoro 6-11 bicyclic erythromycin derivatives |
| 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 |
| JP5953308B2 (ja) | 2010-10-22 | 2016-07-20 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ | 殺害虫剤としての新規ヘテロ環式化合物 |
| 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. |
| CN106432383A (zh) * | 2016-09-14 | 2017-02-22 | 重庆两江药物研发中心有限公司 | 索利霉素及其中间体的制备方法 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5377059A (en) * | 1976-12-20 | 1978-07-08 | Sterling Drug Inc | 11aminooloweralkyll3*44diphenyll 1hhpyrazol salt thereof and process for preparing same |
| JPH06220082A (ja) * | 1992-11-05 | 1994-08-09 | Roussel Uclaf | エリスロマイシンの新誘導体、それらの製造法及びそれらの薬剤としての用途 |
| JPH0853489A (ja) * | 1994-05-03 | 1996-02-27 | Roussel Uclaf | 新規なエリスロマイシン誘導体、それらの製造法及び薬剤としての使用 |
| JPH09176182A (ja) * | 1995-12-22 | 1997-07-08 | Roussel Uclaf | 新規なエリスロマイシン、それらの製造法及び薬剤としての用途 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4182895A (en) * | 1976-12-20 | 1980-01-08 | Sterling Drug Inc. | 1-Amino-lower-alkyl-3,4-diphenyl-1H-pyrazoles |
| JPH04234891A (ja) * | 1990-03-05 | 1992-08-24 | Fujisawa Pharmaceut Co Ltd | 新規セフェム化合物およびその塩 |
| 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. |
| FR2727969B1 (fr) * | 1994-12-09 | 1997-01-17 | Roussel Uclaf | Nouveaux derives de l'erythromycine, leur procede de preparation et leur application comme medicaments |
| PL337606A1 (en) * | 1997-06-11 | 2000-08-28 | Pfizer Prod Inc | Derivatives of erythromycin 9-oxime |
| 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 |
-
1998
- 1998-11-24 FR FR9814782A patent/FR2786188B1/fr not_active Expired - Fee Related
-
1999
- 1999-11-16 TW TW088119939A patent/TWI247747B/zh not_active IP Right Cessation
- 1999-11-17 AU AU59522/99A patent/AU772171B2/en not_active Expired
- 1999-11-18 ZA ZA9907176A patent/ZA997176B/xx unknown
- 1999-11-18 CA CA2290136A patent/CA2290136C/fr not_active Expired - Lifetime
- 1999-11-18 US US09/442,681 patent/US6440941B1/en not_active Expired - Lifetime
- 1999-11-22 JP JP11331141A patent/JP2000159790A/ja active Pending
- 1999-11-23 HU HU9904392A patent/HUP9904392A3/hu unknown
- 1999-11-23 ES ES99402907T patent/ES2198867T3/es not_active Expired - Lifetime
- 1999-11-23 EP EP99402907A patent/EP1004592B1/fr not_active Expired - Lifetime
- 1999-11-23 DE DE69909577T patent/DE69909577T2/de not_active Expired - Lifetime
- 1999-11-23 DK DK99402907T patent/DK1004592T3/da active
- 1999-11-23 CN CNB99127394XA patent/CN1165546C/zh not_active Expired - Lifetime
- 1999-11-23 PT PT99402907T patent/PT1004592E/pt unknown
- 1999-11-23 KR KR1019990052014A patent/KR100587445B1/ko not_active Expired - Lifetime
- 1999-11-23 RU RU99125547A patent/RU2237672C2/ru not_active IP Right Cessation
- 1999-11-23 MX MXPA99010813A patent/MXPA99010813A/es active IP Right Grant
- 1999-11-23 AT AT99402907T patent/ATE245160T1/de active
- 1999-11-23 IL IL133101A patent/IL133101A/en not_active IP Right Cessation
- 1999-11-23 NO NO19995745A patent/NO314729B1/no unknown
- 1999-11-24 PL PL99336736A patent/PL336736A1/xx not_active Application Discontinuation
- 1999-11-24 BR BR9905735-2A patent/BR9905735A/pt active Search and Examination
- 1999-11-24 TR TR1999/02888A patent/TR199902888A3/tr unknown
- 1999-11-24 AR ARP990105985A patent/AR021388A1/es not_active Application Discontinuation
-
2002
- 2002-07-02 US US10/188,394 patent/US6664398B2/en not_active Expired - Lifetime
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5377059A (en) * | 1976-12-20 | 1978-07-08 | Sterling Drug Inc | 11aminooloweralkyll3*44diphenyll 1hhpyrazol salt thereof and process for preparing same |
| JPH06220082A (ja) * | 1992-11-05 | 1994-08-09 | Roussel Uclaf | エリスロマイシンの新誘導体、それらの製造法及びそれらの薬剤としての用途 |
| JPH0853489A (ja) * | 1994-05-03 | 1996-02-27 | Roussel Uclaf | 新規なエリスロマイシン誘導体、それらの製造法及び薬剤としての使用 |
| JPH09176182A (ja) * | 1995-12-22 | 1997-07-08 | Roussel Uclaf | 新規なエリスロマイシン、それらの製造法及び薬剤としての用途 |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4833078B2 (ja) * | 2003-11-25 | 2011-12-07 | アバンテイス・フアルマ・エス・アー | 急性または慢性神経退行を治療する薬剤の形態のピラゾリル誘導体 |
| JP2008508322A (ja) * | 2004-07-28 | 2008-03-21 | ランバクシー ラボラトリーズ リミテッド | 抗菌剤としてのケトライド誘導体 |
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