KR890009930A - (1r,5s,6s)-2-치환 티오-6-[(r)-1- 히드록시에틸]-1- 메틸-카르바페넴-3-카르복실산 유도체 - Google Patents

(1r,5s,6s)-2-치환 티오-6-[(r)-1- 히드록시에틸]-1- 메틸-카르바페넴-3-카르복실산 유도체 Download PDF

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KR890009930A
KR890009930A KR1019880009645A KR880009645A KR890009930A KR 890009930 A KR890009930 A KR 890009930A KR 1019880009645 A KR1019880009645 A KR 1019880009645A KR 880009645 A KR880009645 A KR 880009645A KR 890009930 A KR890009930 A KR 890009930A
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South Korea
Prior art keywords
methyl
hydroxyethyl
thio
carbapenem
carboxylate
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KR1019880009645A
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English (en)
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사까에 아오야기
시게아끼 고바야시
Original Assignee
고니시 시뵤에, 히사나가 쇼오이찌로오
니혼레다리가부시끼가이샤
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Application filed by 고니시 시뵤에, 히사나가 쇼오이찌로오, 니혼레다리가부시끼가이샤 filed Critical 고니시 시뵤에, 히사나가 쇼오이찌로오
Publication of KR890009930A publication Critical patent/KR890009930A/ko

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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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

내용 없음

Description

(1R,5S,6S)-2-치환 티오-6-[(R)-1- 히드록시 에틸]-1- 메틸-카르바페넴-3-카르복실산 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (17)

  1. 하기 식(Ⅰ)로 나타내어지는 결정성(1R,5S,6S)-2-[(메틸 치환-1,2,3-티아디아졸륨-4-일)메틸]티오-6-[(R)-1-히드록시에틸]-1-메틸-카르바페넴-3-카르복실레이트.
  2. 하기 식(Ⅰ-1)로 나타내어지는 결정성(1R,5S,6S)-2-[(2-메틸-1,2,3-티아디아졸륨-4-일)메틸]티오-6-[(R)-1-히드록시에틸]-1-메틸-카르바페넴-3-카르복실레이트.
  3. 제2항에 있어서, 분말 X-선 회절 패턴중 펴면간격(d) 6.9,5.3,4.6, 4.2, 3.9, 3.3, 3.0, 2.5 및 2.4Å에서 특성 피이크들을 지니는 화합물.
  4. 제1항 내지 제3항중 어느 한 항에 있어서, 항균제인 화합물.
  5. 항균제인 결정성(1R,5S,6S)-2-[(2-메틸-1,2,3-티아디아졸륨-4-일)메틸]티오-6-[(R)-1-히드록시에틸]-1-메틸-카르바페넴-3-카르복실레이트.
  6. 무정형(1R,5S,6S)-2-[(2-메틸-1,2,3-티아디아졸륨-4-일)메틸]티오-6-[(R)-1-히드록시에틸]-1-메틸-카르바페냄-3-카르복실레이트를 물중에 약 65%의 농도로 용해시켜서 수용액으로부터 결정물을 침전시킴을 특징으로 하는 하기 식(Ⅰ)로 나타내어지는 결정성(1R,5S,6S)-2-[(메틸 치환-1,2,3-티아디아졸륨-4-일)메틸]티오-6-[(R)-1-히드록시에틸]-1-메틸-카르바페넴-3-카르복실레이트의 제조방법.
  7. 제6항에 있어서, 하기 식(Ⅰ-1)로 나타내어지는 결정성(1R,5S,6S)-2-[(2-메틸-1,2,3-티아디아졸륨-4-일)메틸]티오-6-[(R)-1-히드록시에틸]-1-메틸-카르바페넴-3-카르복실레이트의 제조방법.
  8. 제1항에서 청구된 식(Ⅰ)의 결정성(1R,5S,6S)-2-[(메틸 치환-1,2,3-티아디아졸륨-4-일)메틸]티오-6-[(R)-1-히드록시에틸]-1-메틸-카르바페넴-3-카르복실레이트를 함유하는 약물.
  9. 제2항에서 청구된 식(Ⅰ-1)의 결정성(1R,5S,6S)-2-[(2-메틸-1,2,3-티아디아졸륨-4-일)메틸]티오-6-[(R)-1-히드록시에틸]-1-메틸-카르바페넴-3-카르복실레이트를 함유하는 약물.
  10. 제1항에서 청구된 식(Ⅰ)의 결정성(1R,5S,6S)-2-[(메틸 치환-1,2,3-티아디아졸륨-4-일)메틸]티오-6-[(R)-1-히드록시에틸]-1-메틸-카르바페넴-3-카르복실레이트를 함유하는 항균제.
  11. 제2항에서 청구한 식(Ⅰ-1)의 결정성(1R,5S,6S)-2-[(2-메틸-1,2,3-티아디아졸륨-4-일)메틸]티오-6-[(R)-1-히드록시에틸]-1-메틸-카르바페넴-3-카르복실레이트를 함유하는 항균제.
  12. 항균 효용량의 제1항에서 청구된 식(Ⅰ)의 결정성(1R,5S,6S)-2-[(메틸 치환-1,2,3-티아디아졸륨-4-일)메틸]티오-6-[(R)-1-히드록시에틸]-1-메틸-카르바페넴-3-카르복실레이트, 및 약학적으로 허용 가능한 담체 또는 희석제를 함유하는 약학적 조성물.
  13. 제1항에서 청구된 식(Ⅰ)의 결정성(1R,5S,6S)-2-[(메틸 치환-1,2,3-티아디아졸륨-4-일)메틸]티오-6-[(R)-1-히드록시에틸]-1-메틸-카르바페넴-3-카르복실레이트의 세균 감염의 억제 또는 예방을 위한 용도.
  14. 제2항에서 청구된 식(Ⅰ)의 결정성(1R,5S,6S)-2-[(2-메틸-1,2,3-티아디아졸륨-4-일)메틸]티오-6-[(R)-1-히드록시에틸]-1-메틸-카르바페넴-3-카르복실레이트의 용도.
  15. 항균 효용량의 제1항에서 청구된 식(Ⅰ)의 결정성(1R,5S,6S)-2-[(메틸 치환-1,2,3-티아디아졸륨-4-일)메틸]티오-6-[(R)-1-히드록시에틸]-1-메틸-카르바페넴-3-카르복실레이트를 포유 동물에게 투여함을 특징으로 하는 포유동물의 세균 감염의 치료 또는 예방법.
  16. 주사 바늘에 의하여 침투 가능한 막에 의해서 오염으로부터 각기 밀봉된, 투여 단위의 결정성(1R,5S,6S)-2-[(2-메틸-1,2,3-티아디아졸륨-4-일)메틸]티오-6-[(R)-1-히드록시에틸]-1-메틸-카르바페넴-3-카르복실레이트를 함유하는 제1 바아알 ; 및 주사 바늘에 의하여 취입되어 상기 제1바아알로 주입시켜 단일투여 단위의 (1R,5S,6S)-2-[(2-메틸-1,2,3-티아디아졸륨-4-일)메틸]티오-6-[(R)-1-히드록시에틸]-1-메틸-카르바페냄-3-카르복실레이트를 이루기 위한 주사용 염수를 함유하는 제2바아알을 포함하는 (1R,5S,6S)-2-[(2-메틸-1,2,3-티아디아졸륨-4-일)메틸]티오-6-[(R)-1-히드록시에틸]-1-메틸-카르바페넴-3-카르복실레이트의 투여 단위의 준비용 키트.
  17. 주사 바늘에 의하여 침투 가능한 막을 포함하여 오염으로부터 밀봉된, 결정성(1R,5S,6S)-2-[(2-메틸-1,2,3-티아디아졸륨-4-일)메틸]티오-6-[(R)-1-히드록시에틸]-1-메틸-카르바페넴-3-카르복실레이트를 함유하는 멸균 바이알.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019880009645A 1987-12-07 1988-07-29 (1r,5s,6s)-2-치환 티오-6-[(r)-1- 히드록시에틸]-1- 메틸-카르바페넴-3-카르복실산 유도체 KR890009930A (ko)

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US12955587A 1987-12-07 1987-12-07
US129,555 1987-12-07

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KR890009930A true KR890009930A (ko) 1989-08-04

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EP (1) EP0326640B1 (ko)
KR (1) KR890009930A (ko)
AT (1) ATE88706T1 (ko)
AU (1) AU604949B2 (ko)
DE (1) DE3880660T2 (ko)
DK (1) DK168047B1 (ko)
ES (1) ES2053638T3 (ko)
FI (1) FI883505A (ko)
IL (1) IL87226A (ko)
NO (1) NO883297L (ko)
ZA (1) ZA885481B (ko)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW264475B (ko) * 1991-09-20 1995-12-01 Takeda Pharm Industry Co Ltd
AU2009277936B2 (en) * 2008-07-30 2014-11-27 Sun Pharmaceutical Industries Limited Process for the preparation of carbapenem compounds

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK153486C (da) * 1978-07-03 1988-11-28 Merck & Co Inc Analogifremgangsmaade til fremstilling af krystallinsk n-formimidoyl-thienamycin-monohydrat
US4644061A (en) * 1982-09-28 1987-02-17 Bristol-Myers Company Carbapenem antibiotics
CA1269978A (en) * 1982-09-28 1990-06-05 Choung U. Kim Carbapenem antibiotics
US4713451A (en) * 1984-04-09 1987-12-15 Merck & Co., Inc. Crystalline dimethyliminothienamycin
CA1273012A (en) * 1984-07-02 1990-08-21 Burton G. Christensen 1-methylcarbapenems having an externally alkylated mono- of bicyclic 2-quarternary heteroarylalkylthio substituent

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FI883505A0 (fi) 1988-07-25
EP0326640B1 (en) 1993-04-28
AU604949B2 (en) 1991-01-03
EP0326640A1 (en) 1989-08-09
AU2025788A (en) 1989-06-08
ATE88706T1 (de) 1993-05-15
NO883297D0 (no) 1988-07-25
ZA885481B (en) 1989-04-26
DE3880660T2 (de) 1993-09-23
ES2053638T3 (es) 1994-08-01
IL87226A0 (en) 1988-12-30
DK168047B1 (da) 1994-01-24
IL87226A (en) 1993-04-04
DK411488A (da) 1989-06-08
DE3880660D1 (en) 1993-06-03
DK411488D0 (da) 1988-07-22
NO883297L (no) 1989-06-08
FI883505A (fi) 1989-06-08

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