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KR840005710A - GnRH 길항질 II - Google Patents

GnRH 길항질 II Download PDF

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Publication number
KR840005710A
KR840005710A KR1019830003427A KR830003427A KR840005710A KR 840005710 A KR840005710 A KR 840005710A KR 1019830003427 A KR1019830003427 A KR 1019830003427A KR 830003427 A KR830003427 A KR 830003427A KR 840005710 A KR840005710 A KR 840005710A
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KR
South Korea
Prior art keywords
phe
arg
hydrogen
gly
tyr
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KR1019830003427A
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KR900003096B1 (ko
Inventor
에드워어드 프레드릭 리비어 지인
에드워어드 프레드릭 리비어 지인 (외 1)
워어커 베일 쥬니어 윌리
Original Assignee
더 솔크 인스티튜트 훠 바이올로지칼 스터디 이즈
델버어트 어어니스트 그란즈
더 솔크 인스티튜트 훠 바이올로지칼 스터디이즈
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Application filed by 더 솔크 인스티튜트 훠 바이올로지칼 스터디 이즈, 델버어트 어어니스트 그란즈, 더 솔크 인스티튜트 훠 바이올로지칼 스터디이즈 filed Critical 더 솔크 인스티튜트 훠 바이올로지칼 스터디 이즈
Publication of KR840005710A publication Critical patent/KR840005710A/ko
Application granted granted Critical
Publication of KR900003096B1 publication Critical patent/KR900003096B1/ko
Expired legal-status Critical Current

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    • 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
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • 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
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08—Peptides having 5 to 11 amino acids
    • A61K38/09—Luteinising hormone-releasing hormone [LHRH], i.e. Gonadotropin-releasing hormone [GnRH]; 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)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Endocrinology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Reproductive Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

내용 없음

Description

GnRH 길항질 II
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (14)

  1. (a) 다음 구조식을 갖는 중간체의 제조하는 것과 X1-β-D-2NAL-R2-D-Trp-Ser(X2)-R5(X3)-R6(X4)-R7-Arg(X4)-Pro-X5(여기서 X1는 수소 또는 α-아미노보호기; X2는 수소 또는 Ser의 알콜성 히드록시기에 대한 보호기; X3는 수소 또는 Tyr의 페놀성 히드록시기에 대한 보호기; X4는 수소 또는 Arg의 질소원자에 대한 보호기; X5는 Gly-O-CH2-(지지수지), O-CH2-(지지수지), D-Ala-O-CH2-(지지수지), Gly-NH2, NHCH2CH3및 Gly 또는 D-Ala의 에스테르, 아미드 및 히드라지드에서 선택된 기).
  2. (b) 하나 이상의 X1내지 X4기의 분해 및/또는 X5에 포함된 어떤 지지수지의 제거 및 소망에 따라 이 펩티드를 비독성염으로 전환하는 것으로 구성된 다음 구조를 갖는 펩티드 또는 이들의 비독성 염기염의 제조방법.
  3. X-β-D-2NAL-R2-D-Trp-Ser-R5-R6-R7-Arg-Pro-R10
  4. 여기서 X는 수소 또는 C7이하의 아실기이고; R2는 Cl-D-Phe, F-D-Phe, No2-D-Phe, Cl2-D-Phe, 또는 Br-D-Phe이며; R5는 Tyr 또는 2-Cl-Phe이며; R6는4-NH2-D-Phe 또는 D-Arg이며; R7은 Leu 또는 Nα-Me-Leu이며; R10은 Gly-NH2, NHCH2CH3또는 D-Ala-NH2이다.
  5. 제 1 항에 있어서, R2가 4-Cl-D-Phe 또는 4-F-D-Phe인 방법.
  6. 제 2 항에 있어서, R7이 Leu인 방법.
  7. 제 3 항에 있어서, R6가 D-Arg인 방법.
  8. 제 4 항에 있어서, R5가 Tyr인 방법.
  9. 제 5 항에 있어서, X가 Ac인 방법.
  10. 제 5 항에 있어서, X가 Acr인 방법.
  11. 제 1 항에 있어서, X가 Ac이고, R4가 D-Agr인 방법.
  12. 제 8 항에 있어서, R2가 4-Cl-D-Phe인 방법.
  13. 제 8 항에 있어서, R2가 4-F-D-Phe인 방법.
  14. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019830003427A 1982-07-26 1983-07-25 G_nRH 길항질 II Expired KR900003096B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US402117 1982-07-26
US402,117 1982-07-26
US06/402,117 US4444759A (en) 1982-07-26 1982-07-26 GnRH Antagonists II

Publications (2)

Publication Number Publication Date
KR840005710A true KR840005710A (ko) 1984-11-15
KR900003096B1 KR900003096B1 (ko) 1990-05-07

Family

ID=23590595

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019830003427A Expired KR900003096B1 (ko) 1982-07-26 1983-07-25 G_nRH 길항질 II

Country Status (21)

Country Link
US (1) US4444759A (ko)
EP (1) EP0100218B1 (ko)
JP (1) JPS5946253A (ko)
KR (1) KR900003096B1 (ko)
AT (1) ATE33252T1 (ko)
AU (1) AU558402B2 (ko)
CA (1) CA1263500A (ko)
DD (1) DD216923A5 (ko)
DE (1) DE3376115D1 (ko)
DK (1) DK328183A (ko)
ES (1) ES8505335A1 (ko)
GR (1) GR78886B (ko)
HU (1) HU191865B (ko)
IE (1) IE55580B1 (ko)
IL (1) IL69098A (ko)
MX (1) MX7312E (ko)
NO (1) NO832671L (ko)
NZ (1) NZ204692A (ko)
PH (1) PH18967A (ko)
PT (1) PT77067B (ko)
ZA (1) ZA834645B (ko)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL70888A0 (en) * 1983-03-10 1984-05-31 Salk Inst For Biological Studi Gn rh antagonist peptides and pharmaceutical compositions containing them
US4619914A (en) * 1983-03-10 1986-10-28 The Salk Institute For Biological Studies GNRH antagonists IIIB
ZA846154B (en) * 1983-08-16 1985-03-27 Akzo Nv Lh-rh antagonists
EP0145032B1 (en) * 1983-08-16 1987-11-04 Akzo N.V. Lh- rh antagonists
US4547370A (en) * 1983-11-29 1985-10-15 The Salk Institute For Biological Studies GnRH Antagonists
US4569927A (en) * 1984-02-23 1986-02-11 The Salk Institute For Biological Studies GnRH Antagonists IV
IL74827A (en) * 1984-05-21 1989-06-30 Salk Inst For Biological Studi Peptides active as gnrh antagonists and pharmaceutical compositions containing them
US4652550A (en) * 1984-05-21 1987-03-24 The Salk Institute For Biological Studies GnRH antagonists VII
US4647653A (en) * 1984-08-23 1987-03-03 Tulane Educational Fund Therapeutic peptides
US4565804A (en) * 1984-09-07 1986-01-21 The Salk Institute For Biological Studies GnRH Antagonists VI
US4866160A (en) * 1985-04-09 1989-09-12 The Administrators Of The Tulane Educational Fund Therapeutic decapeptides
ZA862570B (en) * 1985-04-09 1986-12-30 Univ Tulane Therapeutic decapeptides
US4705778A (en) * 1985-10-22 1987-11-10 Sri International Orally active LHRH analogs
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
US4935491A (en) * 1987-08-24 1990-06-19 Board Of Regents, The University Of Texas System Effective antagonists of the luteinizing hormone releasing hormone which release negligible histamine
US5110904A (en) * 1989-08-07 1992-05-05 Abbott Laboratories Lhrh analogs
EP0400065B1 (en) * 1988-02-10 1997-08-27 TAP Pharmaceuticals Inc. Lhrh analog
US5300492A (en) * 1988-02-10 1994-04-05 Tap Pharmaceuticals LHRH analogs
WO1990009799A1 (en) * 1989-02-23 1990-09-07 Colorado State University Research Foundation GnRH ANALOGS FOR DESTROYING GONADOTROPHS
US6326467B1 (en) 1989-02-23 2001-12-04 Colorado State University Research Foundation Hormone-recombinant toxin compounds and methods for using same
US5786457A (en) * 1989-02-23 1998-07-28 Colorado State University Research Foundation Hormone-nuclease compounds and method for regulating hormone related diseases
US5084443A (en) * 1989-12-04 1992-01-28 Biomeasure, Inc. Promoting expression of acetylcholine receptors with lhrh antagonist
US5965695A (en) * 1990-05-15 1999-10-12 Chiron Corporation Modified peptide and peptide libraries with protease resistance, derivatives thereof and methods of producing and screening such
IE66205B1 (en) * 1990-06-14 1995-12-13 Paul A Bartlett Polypeptide analogs
US5656727A (en) * 1992-09-15 1997-08-12 The Administrators Of The Tulane Educational Fund Antagonists of LHRH
US5480969A (en) * 1992-09-15 1996-01-02 The Administrators Of The Tulane Educational Fund Antagonists of LHRH
US20050277582A1 (en) * 1993-07-20 2005-12-15 Nett Torrance M Method for inactivating gonadotrophs
US5502035A (en) * 1993-08-06 1996-03-26 Tap Holdings Inc. N-terminus modified analogs of LHRH
US5506207A (en) * 1994-03-18 1996-04-09 The Salk Institute For Biological Studies GNRH antagonists XIII
US5843901A (en) 1995-06-07 1998-12-01 Advanced Research & Technology Institute LHRH antagonist peptides
US6455499B1 (en) 1999-02-23 2002-09-24 Indiana University Foundation Methods for treating disorders associated with LHRH activity
US6598784B2 (en) * 2000-12-20 2003-07-29 Meadwestvaco Packaging Syatens, Llc Beverage carton with strap type carrying handle
JP2017517484A (ja) 2014-03-31 2017-06-29 イオテック インターナショナル， インコーポレイテッド 非錯体化ヨウ素の安定な組成物及び使用方法

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4261887A (en) * 1973-11-06 1981-04-14 The Salk Institute For Biological Studies Peptide compositions
US4072668A (en) * 1973-11-06 1978-02-07 The Salk Institute For Biological Studies LH-RH Analogs
DE2617646C2 (de) * 1976-04-22 1986-07-31 Hoechst Ag, 6230 Frankfurt Nonapeptid-amide und Decapeptid-amide mit Gonadoliberin-Wirkung, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende pharmazeutische Präparate
US4215038A (en) * 1978-10-16 1980-07-29 The Salk Institute For Biological Studies Peptides which inhibit gonadal function
US4307083A (en) * 1978-10-16 1981-12-22 The Salk Institute For Biological Studies LRF Antagonists
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
US4292313A (en) * 1980-04-15 1981-09-29 The Salk Institute For Biological Studies LRF Antagonists
DE3165535D1 (en) * 1980-06-02 1984-09-20 Andrew Victor Schally Lh-rh antagonists
US4341767A (en) * 1980-10-06 1982-07-27 Syntex Inc. Nonapeptide and decapeptide analogs of LHRH, useful as LHRH antagonists
AU9102582A (en) * 1981-12-10 1983-06-16 David Howard Coy Lh-rh antagonists

Also Published As

Publication number Publication date
ZA834645B (en) 1984-03-28
PT77067A (en) 1983-08-01
DE3376115D1 (en) 1988-05-05
DK328183A (da) 1984-01-27
DK328183D0 (da) 1983-07-15
IE831582L (en) 1984-01-26
PH18967A (en) 1985-11-26
CA1263500A (en) 1989-11-28
ATE33252T1 (de) 1988-04-15
HU191865B (en) 1987-04-28
IE55580B1 (en) 1990-11-07
IL69098A (en) 1986-09-30
EP0100218B1 (en) 1988-03-30
DD216923A5 (de) 1985-01-02
ES524370A0 (es) 1985-05-16
KR900003096B1 (ko) 1990-05-07
GR78886B (ko) 1984-10-02
AU558402B2 (en) 1987-01-29
NO832671L (no) 1984-01-27
IL69098A0 (en) 1983-10-31
NZ204692A (en) 1986-03-14
EP0100218A2 (en) 1984-02-08
PT77067B (en) 1986-01-27
MX7312E (es) 1988-05-11
JPS5946253A (ja) 1984-03-15
AU1637183A (en) 1984-02-02
ES8505335A1 (es) 1985-05-16
US4444759A (en) 1984-04-24
EP0100218A3 (en) 1984-08-15

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