KR870009989A - 스퍼구알린 (Spergualin) 관련 유도체의 제조방법 - Google Patents

스퍼구알린 (Spergualin) 관련 유도체의 제조방법 Download PDF

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KR870009989A
KR870009989A KR870003206A KR870003206A KR870009989A KR 870009989 A KR870009989 A KR 870009989A KR 870003206 A KR870003206 A KR 870003206A KR 870003206 A KR870003206 A KR 870003206A KR 870009989 A KR870009989 A KR 870009989A
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protected
guanidinophenyl
seryl
butanoyl
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KR870003206A
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KR940006768B1 (ko
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하마오 우메자와
도미오 다께우찌
데쓰시 사이노
마사오 요시다
가쓰도시 다까하시
데루야 나까무라
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이찌가와 도꾸지
자이단호오진 비세이부쓰 가가꾸 겡뀨우가이
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/04—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
    • C07C279/14—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by carboxyl groups
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/18—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to carbon atoms of six-membered aromatic rings
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Diaphragms For Electromechanical Transducers (AREA)
  • Pyrrole Compounds (AREA)
  • Train Traffic Observation, Control, And Security (AREA)
  • Electric Propulsion And Braking For Vehicles (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Medicines Containing Plant Substances (AREA)

Abstract

내용 없음

Description

스퍼구알린(Spergualin)관련 유도체의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (11)

  1. 일반식(Ⅱ)의 보호기 함유화합물로 부터 보호기를 분리하여 일반식(Ⅰ)의 스퍼구알린 관련화합물 또는 약제학적으로 허용되는 염을 제조하는 방법.
    위의 일반식에서,
    X능 -(CH2)3-5-또는이고,
    R은 -H또는 -CH2OH이고,
    R1-H,또는
    이고,
    R2는 아미노산 또는 펩타이드로 부터 카르복실기중의 하이드록실기를 제거한 잔기이며, R1이 -H 이외의 기일경우 R2는 R1과 같고,
    R3은 -H 또는 -CH2O-Y인데, Y는 -H이거나 또는-OH기의 보호기이고,
    R4는 -H, 아미노기가 보호된 페닐글리실기 또는 아미노기가 보호된 로이실기이고,
    R5는 보호된 아미노기를 가진 펩타이드 또는 아미노산으로 부터 카르복실기중의 하이드록실기를 제거한 잔기(잔기의 측쇄는 보호될 수 있음)인데, R4가 아미노기 보호된 로이실기 또는 페닐글리실기일 경우 R5는 아미노기 보호된 로이실기 또는 페닐글리실기이다.
  2. 제1항에 있어서, 일반식(Ⅰ)의 R2가
    일반식(Ⅱ)의 R5가 아미노기 보호된 R2에 상응하는 기인 방법.
    위의 일반식의 기에서, n은 0 또는 1; X1은 -H 또는 -OH; X2는 -H 또는 -CH2OH; m은 0또는 1 내지 4의 정수; X3은 -H, -COOH, -OH, -NH2또는 -CONH|2; X4는 -H 또는 -NH2; X3및 X4중 적어도 하나는 -NH2; y는 1 또는 2 ; A는또는;그리고 Y가 2인 경우 2개의 A는 펩타이드결합을 형성한다.
  3. 제1항에 있어서, 일반식(Ⅰ) 및 (Ⅱ)의 X가 -(CH2)3- 또는인 방법.
  4. 제1항에 있어서, X가, R이 -CH2OH, R1이 -H 또는
    (L), (L), 또는, R3이-CH2-O-Y이고 Y는 -H, 또는 -H의 보호기, R4는 -H, 아미노기 보호된 페닐글리실기이거나, 아미노기 보호된 로이실기, R5는 아미노기 보호된 R2에 상응하는 기인 방법.
  5. 제4항에 있어서, R2가 (L또는D),(L)-(CH3)2CHCH2CH-CO-, 또는인 방법.
  6. 10-{N-[4-(4-구아니디노페닐) 부타노일]-L-세릴}1-L-N-보호된-L-또는 D-페닐글리실-1,5,10-트리아자데칸 또는 그 염의 보호기를 제거하여, 10-{N-[4-(4-구아니디노페닐) 부타노일]-L-세릴}-1-L- 또는 D-페닐그리실-1,5,10-트리아자데칸 또는 약제학적으로 허용되는 그 염을 제조하는 방법.
  7. 10-{N-4-(4-구아니디노페닐) 부타노일]-L-세릴}-1-N-보호된-L-로이실-1,5,10-트리아자데칸 또는 그 염의 보호기를 제거하여, 10-{N-[4-(4-구아니디노페닐) 부타노일]-L-세릴}-1-L-로이실-1,5,10-트리아자데칸 또는 약제학적으로 허용되는 그 염을 제조하는 방법.
  8. 10-{N-4-(4-구아니디노페닐) 부타노일]-L-세릴}-1-N-보호된-L-로이실-L-로이실-1,5,10-트리아자데칸 또는 그 염의 보호기를 제거하여, 10-{N-[4-(4-구아니디노페닐) 부타노일]-L-세릴}-1-L-로이실-L-로이실-1,5,10-트리아자데칸 또는 약제학적으로 허용되는 그 염을 제조하는 방법.
  9. 10-{N-4-(4-구아니디노페닐) 부타노일]-O-벤질-L-세릴}-1,5-(디-N-보호된-L-페닐글리실)-1,5,10--트리아자데칸 또는 그 염의 보호기를 제거하여, 10-{N-[4-(4-구아니디노페닐) 부타노일]-L-세릴}-1,5-디-L-페닐글리실-1,5,10-트리아자데칸 또는 약제학적으로 허용되는 그 염을 제조하는 방법.
  10. 제1항에 있어서, 보호기 제거반응을 불활성 용매중에서 -60℃내지 용매의 비접의 온도에서 실시하는 방법.
  11. 제10항에 있어서, 보호기 제거반응을 환원, 산분해 또는 가수분해에 의하여 실시하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019870003206A 1986-04-04 1987-04-04 스퍼구알린(Spergualin)관련 유도체의 제조방법 KR940006768B1 (ko)

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JP86-77747 1986-04-04
JP7774786 1986-04-04
JP77747 1986-04-04

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KR870009989A true KR870009989A (ko) 1987-11-30
KR940006768B1 KR940006768B1 (ko) 1994-07-27

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KR1019870003206A KR940006768B1 (ko) 1986-04-04 1987-04-04 스퍼구알린(Spergualin)관련 유도체의 제조방법
KR1019870006966A KR940007743B1 (ko) 1986-04-04 1987-07-01 스퍼구알린(Spergualin) 관련 유도체

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US (1) US4956504A (ko)
EP (1) EP0241797B1 (ko)
JP (1) JPH0745460B2 (ko)
KR (2) KR940006768B1 (ko)
CN (1) CN1016341B (ko)
AT (1) ATE64378T1 (ko)
AU (1) AU599092B2 (ko)
CA (1) CA1305827C (ko)
DE (1) DE3770680D1 (ko)
DK (2) DK171487A (ko)
ES (1) ES2039213T3 (ko)
FI (1) FI86546C (ko)
GR (1) GR3002660T3 (ko)
HU (1) HU204069B (ko)
IE (1) IE60077B1 (ko)
PT (1) PT84620B (ko)
ZA (1) ZA872440B (ko)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0794424B2 (ja) * 1987-09-30 1995-10-11 財団法人微生物化学研究会 新スパガリン関連化合物およびその製造法
US5770625A (en) * 1988-02-08 1998-06-23 The Trustees Of Columbia University In The City Of New York Butyryl-tyrosinyl spermine, analogs thereof and methods of preparing and using same
US4990536A (en) * 1989-04-03 1991-02-05 Nippon Kayaku Kabushiki Kaisha Immunopotentiator and spergualin-related compound therefor
YU48230B (sh) * 1989-05-29 1997-08-22 Takara Shuzo Co.Ltd. Kristalni deoksispergvalin i postupak za njegovo pripremanje
US5086069A (en) * 1990-02-05 1992-02-04 Rorer Pharmaceutical Corporation Anti-thrombotic peptide and pseudopeptide derivatives
EP0467280B1 (en) * 1990-07-20 1994-09-28 Nippon Kayaku Kabushiki Kaisha Novel spergualin-related compound and use thereof
WO1992018117A1 (en) * 1991-04-11 1992-10-29 Rhone-Poulenc Rorer International (Holdings), Inc. Anti-thrombotic peptide and pseudopeptide derivatives
WO1994004140A1 (en) * 1992-08-19 1994-03-03 Nippon Kayaku Kabushiki Kaisha Antiprotozoan drug
FR2698628B1 (fr) * 1992-12-02 1995-02-17 Fournier Ind & Sante Analogues de 15-déoxyspergualine, leur procédé de préparation et leur utilisation en thérapeutique.
GB9726569D0 (en) * 1997-12-16 1998-02-11 Univ Southampton Neuroprotective agents
US20020142000A1 (en) * 1999-01-15 2002-10-03 Digan Mary Ellen Anti-CD3 immunotoxins and therapeutic uses therefor
KR100604206B1 (ko) * 2005-12-01 2006-07-24 박현미 배선용 단자

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5748957A (en) * 1980-09-08 1982-03-20 Microbial Chem Res Found Novel antibiotic bmg 162-af2, its preparation and carcinostatic agent comprising it as active ingredient
JPS57185254A (en) * 1981-05-11 1982-11-15 Microbial Chem Res Found Novel carcinostatic substances and their preparation
JPS5862152A (ja) * 1981-10-08 1983-04-13 Microbial Chem Res Found Ｎ−〔４−（３−アミノプロピル）アミノブチル〕−２−（ω−グアニジノ脂肪酸アミド）−２−ヒドロキシエタンアミドおよびその誘導体ならびにその製造法
JPS5942356A (ja) * 1982-09-02 1984-03-08 Microbial Chem Res Found スパガリン関連化合物およびその製造法
US4525299A (en) * 1983-05-10 1985-06-25 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai (-)-15-Deoxyspergualin, process for the preparation thereof, and intermediate of the same
JPS60104099A (ja) * 1983-11-09 1985-06-08 Nippon Kayaku Co Ltd スパガリン関連化合物の新規製造法
JPS60181056A (ja) * 1984-02-29 1985-09-14 Takara Shuzo Co Ltd Ν−〔４−（３−アミノプロピル）アミノブチル〕−２，２−ジヒドロキシエタンアミドの製造法
JPS60185758A (ja) * 1984-03-02 1985-09-21 Microbial Chem Res Found フエニレン基を有するスパガリン関連化合物およびその製造法
JPS61165322A (ja) * 1985-01-14 1986-07-26 Microbial Chem Res Found スパガリン類の注射用凍結乾燥製剤
EP0298135A1 (en) * 1987-03-30 1989-01-11 Shosuke Okamoto Phenylalanine derivative and proteinase inhibitor

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Publication number Publication date
KR940007743B1 (ko) 1994-08-24
FI86546C (fi) 1992-09-10
DK171487A (da) 1987-10-05
DK102792D0 (da) 1992-08-18
AU7107587A (en) 1987-10-08
JPH0745460B2 (ja) 1995-05-17
HUT44577A (en) 1988-03-28
KR890001965A (ko) 1989-04-06
CA1305827C (en) 1992-07-28
FI871445A (fi) 1987-10-05
EP0241797A3 (en) 1988-07-20
KR940006768B1 (ko) 1994-07-27
ATE64378T1 (de) 1991-06-15
ZA872440B (en) 1987-12-30
DK171487D0 (da) 1987-04-03
US4956504A (en) 1990-09-11
EP0241797B1 (en) 1991-06-12
ES2039213T3 (es) 1993-09-16
IE60077B1 (en) 1994-06-01
GR3002660T3 (en) 1993-01-25
CN87102538A (zh) 1987-11-18
IE870864L (en) 1987-10-04
EP0241797A2 (en) 1987-10-21
FI871445A0 (fi) 1987-04-02
JPS6345247A (ja) 1988-02-26
DK102792A (da) 1992-08-18
PT84620B (pt) 1989-11-30
AU599092B2 (en) 1990-07-12
PT84620A (en) 1987-05-01
HU204069B (en) 1991-11-28
FI86546B (fi) 1992-05-29
CN1016341B (zh) 1992-04-22
DE3770680D1 (de) 1991-07-18

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