KR940011463A - 결정성 카르바페넴 유도체 - Google Patents

결정성 카르바페넴 유도체 Download PDF

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KR940011463A
KR940011463A KR1019930024477A KR930024477A KR940011463A KR 940011463 A KR940011463 A KR 940011463A KR 1019930024477 A KR1019930024477 A KR 1019930024477A KR 930024477 A KR930024477 A KR 930024477A KR 940011463 A KR940011463 A KR 940011463A
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crystal
compound
formula
ray
copper
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KR1019930024477A
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KR100236845B1 (ko
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이사오 가와모또
마사오 미야우찌
로꾸로 엔도
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가와무라 요시부미
상꾜 가부시끼가이샤
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Oncology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)

Abstract

결정형으로 있는 (1R,5S,6S)-2-[(4R)-2-옥소-4-피롤리디닐티오]-6-[(1R)-1-히드록시에틸]-1-메틸-1-카르바펜-2-엠-3-카르복실산으로 공지된 카르바페넴 유도체의 피발로일옥시메틸 에스테르의 보관 안정형태.

Description

결정성 카르바페넴 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 구리 Kα-선, λ=1.54Å을 사용한 분말법에 의하여 본 발명의 결정에 대한 X-선 회절 패턴을 나타낸다.

Claims (10)

  1. 결정형으로 있는 하기식(I)의 피발로일옥시메틸(1R,5S,6S)-2-[(4R)-2-옥소-4-피롤리디닐티오]-6-[(1R)-1-히드록시에틸]-1-메틸-1-카르바펜-2-엠-3-카르복실레이트
  2. 제1항에 있어서, 189℃에서 용융되는 결정.
  3. 제1항에 있어서, 구리 Kα-선, λ=1.54Å을 사용한 분말법에 의하여 X선 회절로 측정된 18.41, 9.21, 6.24, 5.28, 5.04 및 4.72Å의 결정면간 거리에서 주요 피크를 갖는 결정.
  4. 제1항에서 정의된 바와같은 결정형으로 있는 식(I)의 화합물인 항생 물질과 혼합된 약제학적으로 허용가능한 담체 또는 희석제를 함유하는 약제학적 조성물.
  5. 제4항에 있어서, 식(I)의 화합물의 결정이 189℃의 융점을 갖는 조성물.
  6. 제4항에 있어서, 식(I)의 화합물의 결정이 구리 Kα-선, λ=1.54Å을 사용한 분말법에 의하여 X선 회절로 측정된 18.41, 9.21, 6.24, 5.28, 5.04 및 4.72Å의 결정면간 거리에서 주요 피크를 갖는 조성물.
  7. 제1항에서 정의한 바와 같은 결정형의 식(I)의 화합물인 항생물질의 유효량을 세균에 감염된 포유동물에게 투여하는 것을 특징으로 하는 세균에 감염된 포유동물의 예방 또는 치료방법.
  8. 제7항에 있어서, 식(I)의 화합물의 결정이 189℃의 융점을 갖는 방법.
  9. 제7항에 있어서, 식(I)의 화합물의 결정은 구리 Kα-선, λ=1.54Å을 사용한 분말법에 의하여 X선 회절로 측정된 18.41, 9.21, 6.24, 5.28, 5.04 및 4.72Å의 결정면간 거리에서 주요 피크를 갖는 방법.
  10. (1R,5S,6S)-2-[(4R)-2-옥소-4-피롤리디닐티오]-6-[(1R)-1-히드록시에틸]-1-메틸-1-카르바펜-2-엠-3-카르복산의 피발로일옥시메틸 에스테르에 용매를 가한 후 용매를 능동 또는 수동제거하고 수득한 결정을 세척, 건조 및 단리하는 것을 특징으로 하는 결정형으로 있는 하기식(I)의 화합물의 제조방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019930024477A 1992-11-17 1993-11-17 결정성 카르바페넴 유도체 KR100236845B1 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
JP30688492 1992-11-17
JP92-306884 1992-11-17
JP17026793 1993-07-09
JP93-170267 1993-07-09

Publications (2)

Publication Number Publication Date
KR940011463A true KR940011463A (ko) 1994-06-21
KR100236845B1 KR100236845B1 (ko) 2000-02-01

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Country Link
US (1) US5424306A (ko)
EP (1) EP0599512B1 (ko)
JP (1) JP2848552B2 (ko)
KR (1) KR100236845B1 (ko)
CN (1) CN1036714C (ko)
AT (1) ATE178066T1 (ko)
AU (1) AU677235B2 (ko)
CA (1) CA2103223C (ko)
CZ (1) CZ280507B6 (ko)
DE (1) DE69324106T2 (ko)
DK (1) DK0599512T3 (ko)
ES (1) ES2131560T3 (ko)
FI (1) FI103576B1 (ko)
GR (1) GR3029975T3 (ko)
HK (1) HK1011977A1 (ko)
HU (1) HU219582B (ko)
IL (1) IL107596A (ko)
NO (1) NO304431B1 (ko)
NZ (1) NZ250201A (ko)
PH (1) PH30464A (ko)
TW (1) TW360657B (ko)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2180972T3 (es) * 1996-05-09 2003-02-16 Sankyo Co Composicion contra el helicobacter pilori que contiene derivados de 1-metilcarbapenem como ingrediente activo.
TWI250160B (en) 1999-07-06 2006-03-01 Sankyo Co Crystalline 1-methylcarbapenem compound
US7041660B2 (en) * 1999-07-06 2006-05-09 Sankyo Company, Limited Crystalline 1-methylcarbapenem derivatives
WO2003079972A2 (en) 2002-02-22 2003-10-02 New River Parmaceuticals Inc. Active agent delivery systems and methods for protecting and administering active agents
KR100451672B1 (ko) * 2001-06-05 2004-10-08 한미약품 주식회사 결정성 세프디니르 산부가염, 이의 제조방법 및 이를이용한 세프디니르의 제조방법
ITMI20012364A1 (it) * 2001-11-09 2003-05-09 Antibioticos Spa Processo di sintesi della cefixima via alchil-o arilsolfonati
WO2004035539A1 (ja) * 2002-10-18 2004-04-29 Meiji Seika Kaisha, Ltd. カルバペネム類の製造方法およびその製造に用いられる中間体
JP2008501657A (ja) * 2004-06-02 2008-01-24 サンド・アクチエンゲゼルシヤフト 結晶形態のメロペネム中間体
JP2009143808A (ja) * 2006-03-28 2009-07-02 Kaneka Corp メロペネム中間体の単離方法
JP5715339B2 (ja) 2007-01-12 2015-05-07 ノバルティス アーゲー ５−ビフェニル−４−アミノ−２−メチルペンタン酸の製造方法

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US5242914A (en) * 1988-04-01 1993-09-07 Sankyo Company, Limited 2-(heterocyclylthio) carbapenem derivatives, their preparation and their use as antibiotics
ATE114654T1 (de) * 1988-04-01 1994-12-15 Sankyo Co 2-(heterocyclylthio)carbapenemderivate, deren herstellung und deren verwendung als antibiotika.
JPH0745499B2 (ja) * 1988-05-10 1995-05-17 三共株式会社 １―メチルカルバペネム誘導体
EP0462521A1 (en) * 1990-06-19 1991-12-27 Takeda Chemical Industries, Ltd. Crystalline penem, its production and use

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CZ280507B6 (cs) 1996-02-14
DE69324106D1 (de) 1999-04-29
AU5063193A (en) 1994-06-02
JPH07165759A (ja) 1995-06-27
ES2131560T3 (es) 1999-08-01
AU677235B2 (en) 1997-04-17
FI103576B (fi) 1999-07-30
TW360657B (en) 1999-06-11
NO304431B1 (no) 1998-12-14
GR3029975T3 (en) 1999-07-30
HK1011977A1 (en) 1999-07-23
IL107596A0 (en) 1994-02-27
FI103576B1 (fi) 1999-07-30
JP2848552B2 (ja) 1999-01-20
DK0599512T3 (da) 1999-10-11
HU219582B (hu) 2001-05-28
EP0599512B1 (en) 1999-03-24
PH30464A (en) 1997-05-28
EP0599512A1 (en) 1994-06-01
CN1093366A (zh) 1994-10-12
ATE178066T1 (de) 1999-04-15
KR100236845B1 (ko) 2000-02-01
CA2103223A1 (en) 1994-05-18
CA2103223C (en) 2002-09-24
CZ245493A3 (en) 1995-08-16
NZ250201A (en) 1995-04-27
US5424306A (en) 1995-06-13
NO934140L (no) 1994-05-18
CN1036714C (zh) 1997-12-17
DE69324106T2 (de) 1999-12-09
HUT66001A (en) 1994-08-29
FI935063A0 (fi) 1993-11-16
FI935063A (fi) 1994-05-18
NO934140D0 (no) 1993-11-16
IL107596A (en) 1998-02-08

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