KR830010052A - 펩티드의 제조방법 - Google Patents

펩티드의 제조방법 Download PDF

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Publication number
KR830010052A
KR830010052A KR1019820001743A KR820001743A KR830010052A KR 830010052 A KR830010052 A KR 830010052A KR 1019820001743 A KR1019820001743 A KR 1019820001743A KR 820001743 A KR820001743 A KR 820001743A KR 830010052 A KR830010052 A KR 830010052A
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KR
South Korea
Prior art keywords
phe
nal
gly
group
resin carrier
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KR1019820001743A
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English (en)
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에드워어드 프레드릭 리비어 지인
워어커 베일 쥬니어 윌리
Original Assignee
델버어트 어어니스트 그란쯔
더솔크 인스티튜르훠 바이올로지칼 스터디이즈
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Application filed by 델버어트 어어니스트 그란쯔, 더솔크 인스티튜르훠 바이올로지칼 스터디이즈 filed Critical 델버어트 어어니스트 그란쯔
Publication of KR830010052A publication Critical patent/KR830010052A/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
    • C07K1/04—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length on carriers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/16—Oxytocins; Vasopressins; Related peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/23—Luteinising hormone-releasing hormone [LHRH]; Related peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • 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
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S930/00—Peptide or protein sequence
    • Y10S930/01—Peptide or protein sequence
    • Y10S930/13—Luteinizing hormone-releasing hormone; related peptides

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

Abstract

내용 없음

Description

펩티드의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 펩티드의 제조함에 있어서, 하기 일반식(ⅱ)로 표시되는 펍티드 중간체를 생성시키고(a), 일반식(ⅱ)에 있어서 X1내지 X4기돌중 1개 이상을 분할시키거나 또는 일반식(ⅱ)에 있어서 X5기중에 포함되어 있는 수지담체를 분리시켜 펩티드를 생성시킨 다음(b), 필요에 따라서는 생성 펩티드를 약학적으로 무해한 이의 염으로 전환시킴을 특징으로 하여 하기 일반식(ⅰ)로 표시되는 폅티드의 제조방법.
    X-R1-R2-R3-Ser-Tyr-R4-R5-Arg-Pro-R6(ⅰ)
    상기 식에서, X는 수소원자, 또는 탄소 원자 7이하의 아실기이고, R1은 데히드로 Pro, 또는 데히드로 D-Pro이며, R2는 D-phe, Cl-D-phe, 디클로로 D-phe, CF3-D-phe, F-D-phe, 디플루오로-D-phe, ACNH-D-phe, NO2-D-phe, 디니트로-D-phe, Br-D-phe, 디브모로 -D-phe, CH3-S-D-phe, OCH3-D-phe 또는 CH3-D-phe이며, R3는 D-Trp, 또는 B-D-NAL이며, R4는 B-D-NAL, 또는 D-이성체 방향족 아미노산이며, R5는 Leu, 또는 NaMe-Leu이며, R6는 Gly-NHz, 또는 NHCH2CH3이다.
    (단, R3또는 R4중 하나는 B-D-NAL임)
    X′-R1-R2-R3-ser(X2)-Tyr(X3)-R4-R5-Arg(X4) (ⅱ)
    상기 식에서, X1은 α-아미노 보호기이고, X2는 ser중 알코올형 히드록시기의 보호기이며, X3는 Tyr 중 페놀형 히드록시기의 보호기이며, X4는 Arg중 질소원자의 보호기이며, X5는 Gly-O-CH2(수지 담체), O-CH2-(수지 담체), Gly-NH-(수지 담체), Gly-NH2또는 NHCH2CH3기이다.
  2. 제1항에 있어서, R2가 4-Cl-D-phe, 디클로로-D-phe, 4-CF3-D-phe, 4-F-D-phe, 디플루오로-D-phe, 4-ACNH-D-phe, 4-NO2-D-phe, -D-phe, 디니트로-D-phe, 4-CH3S-D-phe, 4-OCH3-D-phe, 또는 4-CH3-D-phe임을 특징으로 하는 방법.
  3. 제2항에 있어서, R1이 데히드로-pro임을 특징으로 하는 방법.
  4. 제2항 또는 제3항에 있어서, R3가 B-D-NAL임을 특징으로 하는 방법.
  5. 제4항에 있어서, R3가 B-D-NAL임을 특징으로 하는 방법.
  6. 제2항 또는 제3항에 있어서, R4가 B-D-NAL임을 특징으로 하는 방법.
  7. 제6항에 있어서, R4가 B-D-NAL임을 특징으로 하는 방법.
  8. 제4항에 있어서, R4가 B-D-NAL임을 특징으로 하는 방법.
  9. 제5항에 있어서, R4가 B-D-NAL임을 특징으로 하는 방법.
  10. 제3항에 있어서, X5가 Gly-NH-(수지 담체)임을 특징으로 하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019820001743A 1981-04-21 1982-04-20 펩티드의 제조방법 KR830010052A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US256063 1981-04-21
US06/256,063 US4409208A (en) 1980-04-15 1981-04-21 GnRH antagonists

Publications (1)

Publication Number Publication Date
KR830010052A true KR830010052A (ko) 1983-12-24

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ID=22970967

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019820001743A KR830010052A (ko) 1981-04-21 1982-04-20 펩티드의 제조방법

Country Status (20)

Country Link
US (1) US4409208A (ko)
EP (1) EP0063423B1 (ko)
JP (1) JPS57181047A (ko)
KR (1) KR830010052A (ko)
AT (1) ATE14886T1 (ko)
AU (1) AU551892B2 (ko)
CA (1) CA1241950A (ko)
CS (1) CS228924B2 (ko)
DD (1) DD202694A5 (ko)
DE (1) DE3265349D1 (ko)
DK (1) DK151033C (ko)
ES (1) ES511525A0 (ko)
GR (1) GR75542B (ko)
HU (1) HU186007B (ko)
IE (1) IE52442B1 (ko)
IL (1) IL65371A (ko)
NO (1) NO821274L (ko)
NZ (1) NZ200125A (ko)
PH (1) PH18965A (ko)
ZA (1) ZA822053B (ko)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS58162562A (ja) * 1982-03-05 1983-09-27 シンテツクス・（ユ−・エス・エイ）・インコ−ポレ−テツド Ｌｈｒｈのノナペプチド及びデカペプチドアナロ−グ
IL70888A0 (en) * 1983-03-10 1984-05-31 Salk Inst For Biological Studi Gn rh antagonist peptides and pharmaceutical compositions containing them
US4547370A (en) * 1983-11-29 1985-10-15 The Salk Institute For Biological Studies GnRH Antagonists
IL74827A (en) * 1984-05-21 1989-06-30 Salk Inst For Biological Studi Peptides active as gnrh antagonists and pharmaceutical compositions containing them
DE3634435A1 (de) * 1986-10-09 1988-04-14 Hoechst Ag Analoga von gonadoliberin mit verbesserter loeslichkeit, verfahren zu deren herstellung, diese enthaltende mittel und ihre verwendung
WO1988007056A1 (en) * 1987-03-10 1988-09-22 Eastern Virginia Medical Authority METHOD AND KIT FOR CONTRACEPTION WITH GnRH-ANTAGONIST AND PROGESTIN
US5068221A (en) * 1989-05-09 1991-11-26 Mathias John R Treatment of motility disorders with a gnrh analog
US5434136A (en) * 1990-12-14 1995-07-18 Mathias; John R. Treatment of motility disorders with a GNRH analog
US5502035A (en) * 1993-08-06 1996-03-26 Tap Holdings Inc. N-terminus modified analogs of LHRH
US5843901A (en) * 1995-06-07 1998-12-01 Advanced Research & Technology Institute LHRH antagonist peptides
MY150763A (en) 2006-10-24 2014-02-28 Repros Therapeutics Inc Compositions and methods for suppressing endometrial proliferation
US20220257695A1 (en) 2017-03-31 2022-08-18 Institut National De La Sante Et De La Recherche Medicale (Inserm) A gnrh antagonist for use in the treatment of a women affected with polycystic ovary syndrome

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PH11571A (en) * 1973-10-03 1978-03-31 American Home Prod P-gui-d-phe-trp-ser-tyr-d-ala-leu-arg-pro-gly-nh2,its non-toxic salts and method of use thereof
US3933782A (en) * 1974-11-14 1976-01-20 American Home Products Corporation (N-Acetyl)-Pro-D-Phe-Trp-Ser-Tyr-D-Ala-Leu-Arg-Pro-NHEt and intermediates
NZ188987A (en) * 1977-11-30 1982-02-23 Salk Inst For Biological Studi Peptide analogues of luteinizing hormone releasing factor
US4234571A (en) * 1979-06-11 1980-11-18 Syntex (U.S.A.) Inc. Nonapeptide and decapeptide derivatives of luteinizing hormone releasing hormone
GB2053229B (en) * 1979-06-13 1983-03-02 Schally Andrew Victor Lh-rh antagonists
US4253997A (en) * 1979-12-17 1981-03-03 American Home Products Corporation Anti-ovulatory decapeptides
NZ196558A (en) * 1980-04-15 1984-10-19 Salk Inst For Biological Studi Lrf antagonists and pharmaceutical compositions

Also Published As

Publication number Publication date
ATE14886T1 (de) 1985-08-15
ES8307720A1 (es) 1983-07-16
AU551892B2 (en) 1986-05-15
IE820819L (en) 1982-10-21
IE52442B1 (en) 1987-10-28
HU186007B (en) 1985-05-28
NO821274L (no) 1982-10-22
IL65371A0 (en) 1982-05-31
AU8283882A (en) 1982-10-28
NZ200125A (en) 1984-10-19
DK173082A (da) 1982-10-22
DK151033C (da) 1988-03-14
DD202694A5 (de) 1983-09-28
US4409208A (en) 1983-10-11
GR75542B (ko) 1984-07-27
PH18965A (en) 1985-11-26
DE3265349D1 (en) 1985-09-19
CA1241950A (en) 1988-09-13
ES511525A0 (es) 1983-07-16
CS228924B2 (en) 1984-05-14
JPS57181047A (en) 1982-11-08
EP0063423A1 (en) 1982-10-27
DK151033B (da) 1987-10-12
EP0063423B1 (en) 1985-08-14
ZA822053B (en) 1983-02-23
IL65371A (en) 1985-12-31

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