KR100472842B1 - 피롤리딜티오카르바페넴 유도체의 신형결정 - Google Patents
피롤리딜티오카르바페넴 유도체의 신형결정 Download PDFInfo
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- KR100472842B1 KR100472842B1 KR10-2002-7012979A KR20027012979A KR100472842B1 KR 100472842 B1 KR100472842 B1 KR 100472842B1 KR 20027012979 A KR20027012979 A KR 20027012979A KR 100472842 B1 KR100472842 B1 KR 100472842B1
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- 239000013078 crystal Substances 0.000 title claims abstract description 162
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- 238000000634 powder X-ray diffraction Methods 0.000 claims abstract description 13
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D477/00—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring
- C07D477/10—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2
- C07D477/12—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2 with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached in position 6
- C07D477/16—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2 with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached in position 6 with hetero atoms or carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 3
- C07D477/20—Sulfur 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
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Communicable Diseases (AREA)
- Pharmacology & Pharmacy (AREA)
- Oncology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Description
보존기간 | Ⅱ형 | Ⅳ형 |
초기 | 4.56 | 4.62 |
1주일 | 9.51 | 4.79 |
2주일 | 10.36 | 4.89 |
한달 | 10.31 | 4.99 |
보존기간 | Ⅱ형 | Ⅳ형 |
초기 | 983.2 | 993.3 |
1주일 | 956.2 | 990.8 |
2주일 | 923.0 | 992.4 |
한달 | 826.4 | 981.5 |
Claims (7)
- 분말 X선 회절의 회절 패턴이, 회절 각도(2θ)= 13.04, 14.98, 15.88, 16.62, 20.62, 21.06, 22.18, 23.90, 26.08, 28.22 및 28.98(도)에서 메인피크를 갖는, (+)-(4R, 5S, 6S)-6-[(lR)-1-히드록시에틸]-4-메틸-7-옥소-3 [ [(3S, 5S)-5-(술파모일아미노메틸)피롤리딘-3-일]티오]-1-아자비시클로[3. 2. 0]헵-2-틴-2-카르본산 또는 그 수화물의 결정.
- 제 l 항에 따른 결정을 함유하는 항균용 조성물.
- 제 2 항에 있어서,상기 조성물이 주사제인 것을 특징으로 하는 항균용 조성물.
- 제 2 항에 있어서,상기 조성물이 분말충전제제인 것을 특징으로 하는 항균용 조성물.
- 분말 X선 회절의 회절 패턴이 회절 각도(2θ)=6.78, 6.96, 15.74, 17.92, 21.16, 23.56 및 25.80(도)에서 메인피크를 갖는, (+)-(4R, 5S, 6S)-6-[(lR)-1-히드록시에틸]-4-메틸-7-옥소-3 [ [(3S, 5S)-5- (술파모일아미노메틸)피롤리딘-3-일]티오]-1-아자비시클로[3. 2. 0]헵-2-틴-2-카르본산 또는 그 수화물의 결정.
- (A) (+)-(4R, 5S, 6S)-6-[(lR)-1-히드록시에틸]-4-메틸-7-옥소-3 [ [(3S, 5S)-5- (술파모일아미노메틸)피롤리딘-3-일]티오]-1-아자비시클로[3. 2. 0]헵-2-틴-2-카르본산 또는 그 수화물을 수중에서 용해하는 단계와,(B) 청구항 제5항에 기재된 결정인 종결정의 존재하에, 공정 (A)에서 얻어진 수용액으로부터 결정을 석출시키는 단계를 포함하는 제 5 항에 따른 결정을 제조하는 방법.
- (A) (+)-(4R, 5S, 6S)-6-[(lR)-1-히드록시에틸]-4-메틸-7-옥소-3 [ [(3S, 5S)-5- (술파모일아미노메틸)피롤리딘-3-일]티오]-1-아자비시클로[3. 2. 0]헵-2-틴-2-카르본산 또는 그 수화물을 수중에서 용해하는 단계와,(B') 청구항 제5항에 기재된 결정인 종결정의 존재하에, 공정 (A)에서 얻어진 수용액으로부터 상기 석출한 결정의 분말 X선 회절의 회절패턴이 회절 각도(2θ)= 6.78, 6.96, 15.74, 17.92, 21.16, 23.56 및 25.80(도)에서 메인피크를 갖는 결정을 석출시키는 단계; 및(C) 공정 (B')에서 얻어진 결정을 건조하는 단계를 포함하는 제 1 항에 따른 결정을 제조하는 방법.
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WO2015167148A1 (ko) * | 2014-04-28 | 2015-11-05 | 제이더블유중외제약 주식회사 | 도리페넴의 신규한 결정 및 이의 제조방법 |
KR20160007679A (ko) | 2016-01-04 | 2016-01-20 | 제일약품주식회사 | 도리페넴의 신규한 결정형 |
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MXPA02009592A (es) * | 2000-03-31 | 2003-03-12 | Shionogi & Co | Nueva forma cristalina de derivado de pirrolidiltiocarbapenema. |
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CN1608066A (zh) * | 2001-11-16 | 2005-04-20 | 兰贝克赛实验室有限公司 | 结晶亚胺培南的制备方法 |
TWI353855B (en) | 2005-05-26 | 2011-12-11 | Shionogi & Co | Method for preparing an aqueous solution of doripe |
TW200815442A (en) * | 2006-04-28 | 2008-04-01 | Kaneka Corp | Improved method for the crystallization of intermediates of carbapenem antibiotics |
CN101466713A (zh) * | 2006-07-03 | 2009-06-24 | 成都地奥九泓制药厂 | 多尼培南的新结晶及其制备方法和用途 |
CN101191787B (zh) * | 2006-11-21 | 2011-07-27 | 上海医药工业研究院 | 高效液相色谱法测定多利培南含量的方法 |
PL2276762T3 (pl) * | 2008-03-24 | 2015-06-30 | Ranbaxy Laboratories Ltd | Sposób wytwarzania jałowego doripenemu |
WO2011150679A1 (zh) * | 2010-06-03 | 2011-12-08 | 山东轩竹医药科技有限公司 | 碳青霉烯类衍生物或其水合物的晶型及其制备方法与用途 |
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WO2013068910A1 (en) * | 2011-11-08 | 2013-05-16 | Ranbaxy Laboratories Limited | Process for the preparation of polymorphs of doripenem |
CN104072497B (zh) * | 2013-03-29 | 2017-10-03 | 石药集团中奇制药技术(石家庄)有限公司 | 一种多尼培南新结晶及其制备方法 |
CN103389347B (zh) * | 2013-07-26 | 2015-12-09 | 深圳市海滨制药有限公司 | 高效液相色谱法测定多尼培南的方法 |
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WO2015167148A1 (ko) * | 2014-04-28 | 2015-11-05 | 제이더블유중외제약 주식회사 | 도리페넴의 신규한 결정 및 이의 제조방법 |
US9840506B2 (en) | 2014-04-28 | 2017-12-12 | Jw Pharmaceutical Corporation | Crystal of doripenem, and preparation method therefor |
KR101910048B1 (ko) | 2014-04-28 | 2018-10-22 | 제이더블유중외제약 주식회사 | 도리페넴의 신규한 결정 및 이의 제조방법 |
KR20160007679A (ko) | 2016-01-04 | 2016-01-20 | 제일약품주식회사 | 도리페넴의 신규한 결정형 |
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