KR920002608A - 라파마이신 유도체 - Google Patents

라파마이신 유도체 Download PDF

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Publication number
KR920002608A
KR920002608A KR1019910012015A KR910012015A KR920002608A KR 920002608 A KR920002608 A KR 920002608A KR 1019910012015 A KR1019910012015 A KR 1019910012015A KR 910012015 A KR910012015 A KR 910012015A KR 920002608 A KR920002608 A KR 920002608A
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KR
South Korea
Prior art keywords
carbon atoms
pharmaceutically acceptable
hydrogen
rapamycin
acceptable salt
Prior art date
Application number
KR1019910012015A
Other languages
English (en)
Inventor
유진 커필드 크레이그
아르투로 페일리 아메데오
죤 스테판 로버트
Original Assignee
에곤 이. 버그
아메리칸 홈 프로덕츠 코포레이션
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Priority claimed from US07/667,684 external-priority patent/US5120726A/en
Application filed by 에곤 이. 버그, 아메리칸 홈 프로덕츠 코포레이션 filed Critical 에곤 이. 버그
Publication of KR920002608A publication Critical patent/KR920002608A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

내용 없음

Description

라파마이신 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (15)

  1. 일반식(Ⅰ)의 화합물 및 이의 약학적으로 허용가능한 염.
    상기식에서, R은 NR1R2또는 -OR3이고, R1은 수소, 탄소수 1내지 6의 알킬 또는 탄소수 7내지 10의 아르알킬이며, R2는 수소, 탄소수 1내지 6의 알킬, 탄소수 3내지 10의 사이클로알킬,탄소수 7내지 10의 아르알킬, -COR4, -CO2R4, -SO2R4, -CONR5R6, -CSNR5R6, -COCONR5R6또는 Ar이고, R3는 수소, 탄소수 1내지 6의 알킬 또는 -CH2Ar이며, R4는 탄소수 1내지 6의 알킬, 탄소수 7내지 10의 아르알킬 또는 Ar이고, R5및 R6는 각각,독립적으로, 수소, 탄소수, 1내지 6의 알킬, 탄소수 3내지 10의 사이클로알킬, 알릴, 탄소수 7내지 10의 아르알킬 또는 Ar이며,
    R7,R8,R9는 각각 독립적으로, 수소, 탄소수 1내지 6의 알킬, 탄소수 1내지 6의 알콕시, 하이드록시, 시아노, 할로, 니트로, 탄소수 2내지 7의 카브알콕시, 트리플루오로메틸, 트리플루오로메톡시, 아미노 또는 카복실산이며, X는 CH 또는 N이고 Y는 NH, O 또는 S이다.
  2. 제1항에 있어서, R이 -NR1R2이고 R1이 수소인 화합물 및 이의 약학적으로 허용가능한 염.
  3. 제1항에 있어서, R이 -NR1R2이고 R1이 수소이며, R2가 -CONR5R6인 화합물 및 이의 약학적으로 허용가능한 염.
  4. 제1항에 있어서, R이 -NR1R2이고 R1이 수소이며, R2가 -CONR4인 화합물 및 이의 약학적으로 허용가능한 염.
  5. 제1항에 있어서, R이 -NR1R2이고 R1이 수소이며, R2가 Ar인 화합물 및 이의 약학적으로 허용가능한 염.
  6. 제1항에 있어서, R이 -OR3이고 R3가 탄소수 1내지 6의 알킬인 화합물 및 이의 약학적으로 허용가능한 염.
  7. 제1항에 있어서, R이 -OR3이고 R3가 -CH2Ar이며
    인 화합물 및 이의 약학적으로 허용가능한 염.
  8. 제1항에 있어서, 라파마이신 27-(메틸카보닐하이드라존) 및 이의 약학적으로 허용가능한 염.
  9. 제1항에 있어서, 라파마이신 27-(4-페닐세미카브아존) 및 이의 약학적으로 허용가능한 염.
  10. 제1항에 있어서, 라파마이신 27-(2-피리디닐하이드리존) 및 이의 약학적으로 허용가능한 염.
  11. 제1항에 있어서, 라파마이신 27-세미키보아존 및 이의 약학적으로 허용가능한 염.
  12. 제1항에 있어서, 라파마이신 27-하이드라존 및 이의 약학적으로 허용가능한 염.
  13. 제1항에 있어서, 라파마이신 27-옥심 및 이의 약학적으로 허용가능한 염.
  14. 제1항에 있어서, 라파마이신-O-벤질-27-옥심 및 이의 약학적으로 허용가능한 염.
  15. 제1항에 있어서, 라파마이신-O-메틸-27-옥심 및 이의 약학적으로 허용가능한 염.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019910012015A 1990-07-16 1991-07-15 라파마이신 유도체 KR920002608A (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US55272090A 1990-07-16 1990-07-16
US07/552,720 1990-07-16
US07/667,684 1991-03-08
US07/667,684 US5120726A (en) 1991-03-08 1991-03-08 Rapamycin hydrazones

Publications (1)

Publication Number Publication Date
KR920002608A true KR920002608A (ko) 1992-02-28

Family

ID=27070117

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019910012015A KR920002608A (ko) 1990-07-16 1991-07-15 라파마이신 유도체

Country Status (8)

Country Link
EP (1) EP0467606A1 (ko)
JP (1) JPH04230389A (ko)
KR (1) KR920002608A (ko)
AU (1) AU641785B2 (ko)
GB (1) GB2247017B (ko)
HU (1) HUT58745A (ko)
IE (1) IE912468A1 (ko)
PT (1) PT98303A (ko)

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Also Published As

Publication number Publication date
GB2247017A (en) 1992-02-19
JPH04230389A (ja) 1992-08-19
HU912356D0 (en) 1991-12-30
IE912468A1 (en) 1992-01-29
GB2247017B (en) 1994-04-20
EP0467606A1 (en) 1992-01-22
AU641785B2 (en) 1993-09-30
GB9115205D0 (en) 1991-08-28
AU8045091A (en) 1992-01-16
HUT58745A (en) 1992-03-30
PT98303A (pt) 1992-05-29

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