KR830007518A - 약리적 활성 펩티드의 제조방법 - Google Patents

약리적 활성 펩티드의 제조방법 Download PDF

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Publication number
KR830007518A
KR830007518A KR1019810003971A KR810003971A KR830007518A KR 830007518 A KR830007518 A KR 830007518A KR 1019810003971 A KR1019810003971 A KR 1019810003971A KR 810003971 A KR810003971 A KR 810003971A KR 830007518 A KR830007518 A KR 830007518A
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South Korea
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alanyl
methyl
tyrosyl
ethyl
glycyl
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KR1019810003971A
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English (en)
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데이빗 게젤첸 폴
데오도르 슈만 로버트
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아디 알·웨일
일라이 릴리 앤드 캄파니
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Publication of KR830007518A publication Critical patent/KR830007518A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/06—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using protecting groups or activating agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1027—Tetrapeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1016—Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Analytical Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

내용 없음

Description

약리적 활성 펩티드의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 탈차단제를 사용하여, 상응하게 보호된 다음, 일반식(Ⅰ)의 화합물로 부터 차단그룹을 제거함을 특징으로 하여 다음 일반식(Ⅰ)의 화합물 및 이의 약하적으로 무독한 비독성 산부가염을 제조하는 방법.
    상기 일반식에서
    R은 수소, 메틸, 에틸, 사이클로프로필메틸 또는 알릴이고,
    A는 Ala, Abu, Nva, Val, Nle, Leu, Ile, Gly(Al), Gly(Cp), Met, Cys(Me), Met(O), Cys(Me)(O), Ser, Thr 및 Hse 중의 그룹에서 선택된 D―아미노산 잔기이며,
    R1은 수소, C1―C31급알킬, 사이클로프로필메틸, 알릴, 에틸티오메틸, 2―플루오로메틸, 또는 프로파길이고,
    X는 브로모, 요도, 클로로, 메틸, 트리플루오로메틸 또는 메톡시이고,
    Z는 ―CH2OR2,또는이고,
    R2는 수소, 아세틸 도는 아세톡시 메틸이고,
    R3는 C1―C3알킬이다.
  2. 제1항에 있어서 Na―3급―부틸옥시카보닐― Na―메틸―L―티로실―D―알라닐―글리실―L―(Na―사이클로프로필메틸)――브로모페닐알라닐아미드를 트리플루오로아세트산과 반응시켜 L―(N―메틸)티로실―D―알라닐―글리실―L―(N―사이클로프로필메틸)――브로모페닐알라닌아미드를 제조하는 방법
  3. 제1항에 있어서 Na―3급―부틸옥시카보닐― Na―메틸―L―티로실―D―알라닐―글리실―L―(Na―에틸)――브로모페닐알라닐아미드를 트리플루오로아세트산과 반응시켜 L―(N―메틸)티로실―D―알라닐―글리실―L―(N―에틸)――브로모페닐아라닌 아미드를 제조하는 방법
  4. 제1항에 있어서 Na―3급―부틸옥시카보닐― L―티로실―D―알라닐―글리실―L―(Na―에틸)――브로모페닐알라닐아미드를 트리플루오로아세트산과 반응시켜 L―티로실―D―알라닐―글리실―L―(N―에틸)――브로모페닐 알라닌 아미드를 제조하는 방법
  5. 제1항에 있어서 Na―3급―부틸옥시카보닐― Na―메틸―L―티로실―D―알라닐―글리실―L―(Na―메틸)――메틸페닐알라닌아미드를 트리플루오로아세트산과 반응시켜 L―(N―메틸)―티로실―D―알라닐―글리실―L―(N―메틸)――메틸페닐알라닌아미드를 제조하는 방법
  6. 제1항에 있어서 Na―3급―부틸옥시카보닐―L―티로실―D―알라닐―글리실 ―L―(Na―에틸)――클로로페닐알라닌아미드를 트리플루오로아세트산과 반응시켜 L―티로실―D―알라닐―글리실―L―(N―에틸)――클로로페닐 알라닌 아미드를 제조하는 방법
  7. 제1항에 있어서 Na―3급―부틸옥시카보닐― Na―메틸―L―티로실―D―알라닐―글리실―L―(Na―에틸)――클로로페닐 알라닌 아미드를 트리플루오로아세트산과 반응시켜 L―(N―메틸)티로실―D―알라닐―글리실―L―(N―에틸)――클로로페닐 알라닌 아미드를 제조하는 방법
  8. 제1항에 있어서 Na―3급―부틸옥시카보닐―L―티로실―D―알라닐―글리실― L―(Na―에틸)――요도페닐알라닌아미드를 트리플루오로아세트산과 반응시켜 L―티로실―D―알라닐―글리실―L―(N―에틸)――요도페닐 알라닌 아미드를 제조하는 방법
  9. 제1항에 있어서 Na―3급―부틸옥시카보닐―L―티로실―D―알라닐―글리실― L―(Na―사이클로프로필메틸)――요도페닐알라닌을 트리플루오로아세트산과 반응시켜 L―티로실―D―알라닐―글리실―L―(N―사이클로프로필메틸)――요도페닐 알라닌 아미드를 제조하는 방법
  10. 제1항에 있어서 Na―3급―부틸옥시카보닐― Na―메틸―L―티로실―D―알라닐―글리실―L―(Na―사이클로프로필메틸)――요도페닐알라닌 아미드를 트리플루오로아세트산과 반응시켜 L―(N―메틸)티로실―D―알라닐―글리실―L―(N―사이클로프로필메틸)――요도페닐알라닌아미드를 제조하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019810003971A 1980-10-20 1981-10-20 약리적 활성 펩티드의 제조방법 KR830007518A (ko)

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Application Number Priority Date Filing Date Title
US06/198,900 US4322340A (en) 1980-10-20 1980-10-20 Pharmacologically active peptides
US198,900 1980-10-20

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US (1) US4322340A (ko)
EP (1) EP0050502B1 (ko)
JP (1) JPS57108052A (ko)
KR (1) KR830007518A (ko)
AR (1) AR230046A1 (ko)
AT (1) ATE6777T1 (ko)
AU (1) AU547221B2 (ko)
BG (1) BG36928A3 (ko)
CA (1) CA1187871A (ko)
DD (1) DD200798A5 (ko)
DE (1) DE3162823D1 (ko)
DK (1) DK461481A (ko)
ES (1) ES506316A0 (ko)
FI (1) FI813198L (ko)
GB (1) GB2085893B (ko)
GR (1) GR75342B (ko)
HU (1) HU185320B (ko)
IE (1) IE52186B1 (ko)
IL (1) IL64083A (ko)
NZ (1) NZ198628A (ko)
PH (1) PH17006A (ko)
PL (1) PL131155B1 (ko)
PT (1) PT73839B (ko)
RO (1) RO83301B (ko)
SU (1) SU1082319A3 (ko)
YU (1) YU249081A (ko)
ZA (1) ZA817063B (ko)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0076557B1 (en) * 1981-06-22 1985-11-13 Imperial Chemical Industries Plc Peptides and pseudopeptides in which the n terminus bears two substituents
US4448717A (en) * 1982-11-12 1984-05-15 Eli Lilly And Company Pharmacologically active peptides
US4510082A (en) * 1983-03-07 1985-04-09 Eli Lilly And Company Pharmacologically active peptides
US4473497A (en) * 1983-03-07 1984-09-25 Eli Lilly And Company Pharmacologically active peptides
DK134784A (da) * 1983-03-07 1984-09-08 Lilly Co Eli Farmakologisk virksomme tripeptid-derivater og fremgangsmaade til fremstilling deraf
US4495178A (en) * 1983-10-06 1985-01-22 G. D. Searle & Co. Enkephalin analogs
JPH0449298A (ja) * 1990-06-19 1992-02-18 Univ New York State 新規なエンケファリン誘導体および鎮痛剤
US5209930A (en) * 1990-12-10 1993-05-11 Rohm And Haas Company Preparation and use of n-iodopropargyl oxycarbonyl amino acid esters and derivatives as antimicrobial agents
US5965698A (en) * 1993-04-23 1999-10-12 Virginia Commonwealth University Polypeptides that include conformation-constraining groups which flank a protein--protein interaction site
AU6770794A (en) * 1993-04-23 1994-11-21 Herbert J. Evans Polypeptides that include conformation-constraining groups which flank a protein-protein interaction site
US5952465A (en) * 1993-04-23 1999-09-14 Virginia Commonwealth University Polypeptides that include conformation-constraining groups which flank a protein-protein interaction site
US5928896A (en) * 1993-04-23 1999-07-27 Virginia Commonwealth University Polypeptides that include conformation-constraining groups which flank a protein--protein interaction site
US6258550B1 (en) 1993-04-23 2001-07-10 Virginia Commonwealth University Polypeptides that include conformation-constraining groups which flank a protein-protein interaction site
US6084066A (en) * 1993-10-29 2000-07-04 Virginia Commonwealth University Polypetides that include conformation-constraining groups which flank a protein-protein interaction site

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1577115A (en) * 1976-07-27 1980-10-22 Reckitt & Colmann Prod Ltd Container closure units
CH619686A5 (en) * 1976-02-02 1980-10-15 Sandoz Ag Process for the preparation of novel peptides or peptide derivatives
DE2702711A1 (de) * 1976-02-02 1977-08-04 Sandoz Ag Neue organische verbindungen, ihre herstellung und verwendung
US4264491A (en) * 1977-10-03 1981-04-28 Eli Lilly And Company Analgesic compounds
US4265808A (en) * 1979-12-17 1981-05-05 Eli Lilly And Company Pharmacologically active peptides

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ZA817063B (en) 1983-05-25
HU185320B (en) 1985-01-28
PT73839A (en) 1981-11-01
PL233498A1 (ko) 1982-05-24
ES8306713A1 (es) 1983-06-01
AU547221B2 (en) 1985-10-10
IL64083A0 (en) 1982-01-31
CA1187871A (en) 1985-05-28
EP0050502A1 (en) 1982-04-28
DE3162823D1 (en) 1984-04-26
ES506316A0 (es) 1983-06-01
RO83301B (ro) 1984-02-28
FI813198L (fi) 1982-04-21
IE812442L (en) 1982-04-20
IE52186B1 (en) 1987-08-05
AU7657481A (en) 1982-04-29
NZ198628A (en) 1985-01-31
RO83301A (ro) 1984-02-21
GR75342B (ko) 1984-07-13
GB2085893A (en) 1982-05-06
PL131155B1 (en) 1984-10-31
SU1082319A3 (ru) 1984-03-23
BG36928A3 (en) 1985-02-15
US4322340A (en) 1982-03-30
PT73839B (en) 1983-01-17
EP0050502B1 (en) 1984-03-21
PH17006A (en) 1984-05-11
YU249081A (en) 1983-12-31
JPS57108052A (en) 1982-07-05
GB2085893B (en) 1984-03-21
DK461481A (da) 1982-04-21
AR230046A1 (es) 1984-02-29
IL64083A (en) 1985-03-31
ATE6777T1 (de) 1984-04-15
DD200798A5 (de) 1983-06-15

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