KR850001230A - 옥타펩티드 바조프레신 길항물질의 제조방법 - Google Patents

옥타펩티드 바조프레신 길항물질의 제조방법 Download PDF

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KR850001230A
KR850001230A KR1019840000736A KR840000736A KR850001230A KR 850001230 A KR850001230 A KR 850001230A KR 1019840000736 A KR1019840000736 A KR 1019840000736A KR 840000736 A KR840000736 A KR 840000736A KR 850001230 A KR850001230 A KR 850001230A
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South Korea
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pro
phe
tyr
arg
formula
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KR1019840000736A
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English (en)
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프란시스 허프맨 윌리암 (외 1)
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리챠드 도미니크포기오
스미스 클라인 베크만 코퍼레이션
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Publication of KR850001230A publication Critical patent/KR850001230A/ko

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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
    • C07K7/16—Oxytocins; Vasopressins; Related peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • 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
    • Y10S930/15—Oxytocin or vasopressin; related peptides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Emergency Protection Circuit Devices (AREA)
  • Measuring Pulse, Heart Rate, Blood Pressure Or Blood Flow (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

내용 없음

Description

옥타펩티드 바조프레신 길항물질의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (14)

  1. 식(I)의 화합물을 제조하는 방법 :
    여기에서, P는 Phe 또는 Phe(4-Alk)이고, X는 D-Phe, D-Val, D-Leu, D-Ile, D-Nva, D-Pba, D-alIe, D-Nle, D-Cha, D-Abu, D-Met, D-Chg, D-Tyr, L-Tyr, D-Tyr(Et) 또는 L-Try(alK)이고, Y는 NH2, NHAlK, NHBzl 또는 OH이고, W는 D-Pro, L-Pro, 디하이드로-Pro 또는 Y 및 Z가 없을 경우에는 CH일 수 있고, A는 Val, Ile,Abu,Ala,Gly, Lys, Cha, Nle, Phe, Leu, Chg 또는 Nva이고, Z는 D-Arg, L-Arg, D-Lys, L-Lys 또는 Y가 OH인 경우에 단일 결합일 수 있고, n는 0,1 또는 2이거나, 약학적으로 허용되는 대용약제 또는 그 염이고, 선택적으로 보호된 식(II)의 화합물을 환식화하는 것을 포함함;
    여기에서, X,P,A,W,Z 및 Y는 상기에서 정의된 바와같고, Q1및 Q2는 각각 수소 또는 치환가능한 그룹이고, Cap는 β-위치에 부착된 S-Q1을 가지는 β,β-씨클로알킬렌 프로피온산이고, 씨클로알킬렌고리에서 5-7단위체를 가지고 있으며, 필요하면 그 후에 어떤 순서로든지, (a) 어떤 보호하는 그룹을 제거하고, (b) 이른바 Cys(CH)6또는 Pro(OH)7화합물이 존재하면, 산으로 보호된 형태나 아미드 형태로 각각 디펩티드, W-Z-Y 또는 아미노산, Z-Y와 반응시키거나 또는 (c) 약학적으로 허용되는 염이나 대용약제를 형성시킴.
  2. 청구범위 제1항에서, Q1및 Q2가 둘다 수소인 경우의 방법.
  3. 청구범위 제1항에서, Q1및 Q2가 둘다 아세트아미도메틸인 경우의 방법.
  4. 청구범위 제1항 내지 제3항에서, 산화하는 환식화를 포함하는 방법.
  5. 청구범위 제4항에서, 요오드 존재시에 실시되는 방법.
  6. 청구범위 제4항에서, 훼리시아나이드 존재시에 실시되는 방법.
  7. 청구범위 제1항에서, 선택적으로 어떤 보호그룹을 제거시킨후에 식 I의 Cys(OH)6화합물을 카보디이미드 존재하에 (NH2)-W-Z-Y로써 반응시키는 방법.
  8. 청구범위 제1항에서, 선택적으로 어떤 보호하는 그룹을 제거시킨후에, 식 I의 Pro(OH)7화합물을 카보디이미드 존재하에 (NH)2-Z-Y로써 반응시키는 방법.
  9. 청구범위 제8항에서, Pro(OH)7을 Arg(NH2)나 그 염으로써 반응시키는 방법.
  10. 청구범위 제1항에서, n가 1, X가 D-Tyr(Et), P가 Phe, A가 Val, W가 Pro, Z가 Arg 및 Y가 NH2인 경우의 방법.
  11. 청구범위 제4항에서, n가 1, X가 D-Tyr(Et), P가 Phe 또는 Phe(4'-Et), A가 Val 또는 Abu, W가 L-Pro 또는 D-Pro, Z가 Arg 그리고 Y가 NH2인 경우의 방법.
  12. 식 II의 화합물을 제조하는 방법;
    여기에서, P는 Phe 또는 Phe(4'-Alk)이고, X가 D-Phe, D-Val, D-Leu, D-Ile, D-Nva, D-Pba, D-Alle, D-Nle, D-Cha, D-Abu, D-Met, D-Chg, D 또는 L-Tyr 또는 D 또는 L-Tyr(alK)이고, Y가 NH2, NHAlK, NHBzl 또는 OH이고, W는 D-Pro, L-Pro 디하이드로-Pro 또는, Y 및 Z가 없는 경우에 OH이고, A는 Val, Ile, Abu, Ala, Gly, LyS, Cha, Nle, Phe, Leu, Chg 또는 Nva이고, Z가 D-Arg, L-Arg, D-Lys, L-Lys 또는 Y가 OH인 경우에 단일 결합이거나 약학적으로 허용되는 그 염이고, 이것이 식 II의 화합물의 보호된 유도체를 보호 해제하는 것을 포함함.
  13. 청구범위 제12항에서, 식 II의 펩티드가 또는 지지하는 수지로 부터 분리된 경우의 방법.
  14. 청구범위 제12항 또는 제13항에서, 보호해제 시약이 불화수소인 경우의 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019840000736A 1983-02-16 1984-02-16 옥타펩티드 바조프레신 길항물질의 제조방법 KR850001230A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US467117 1983-02-16
US06/467,117 US4469679A (en) 1983-02-16 1983-02-16 Octapeptide vasopressin antagonists

Publications (1)

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KR850001230A true KR850001230A (ko) 1985-03-16

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KR1019840000736A KR850001230A (ko) 1983-02-16 1984-02-16 옥타펩티드 바조프레신 길항물질의 제조방법

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US (2) US4469679A (ko)
EP (1) EP0119705B1 (ko)
JP (1) JPS59155348A (ko)
KR (1) KR850001230A (ko)
AT (1) ATE46174T1 (ko)
AU (1) AU577778B2 (ko)
DE (1) DE3479664D1 (ko)
DK (1) DK65284A (ko)
ES (2) ES8606408A1 (ko)
FI (1) FI840577A (ko)
GR (1) GR81786B (ko)
HU (1) HU196227B (ko)
IE (1) IE56859B1 (ko)
IL (1) IL70944A (ko)
NO (1) NO840563L (ko)
NZ (1) NZ207106A (ko)
PH (1) PH20076A (ko)
PT (1) PT78094B (ko)
ZA (1) ZA841104B (ko)
ZW (1) ZW1884A1 (ko)

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US4649130A (en) * 1984-01-26 1987-03-10 Medical College Of Ohio Novel derivatives of arginine vasopressin antagonists
US4714696A (en) * 1984-01-26 1987-12-22 Medical College Of Ohio Novel derivatives of arginine vasopressin antagonists
US4599324A (en) * 1984-11-21 1986-07-08 Smithkline Beckman Corporation V1-vasopressin antagonists
US4684716A (en) * 1984-12-14 1987-08-04 Smithkline Beckman Corporation Polypeptide intermediates
US4624943A (en) * 1985-03-20 1986-11-25 Smithkline Beckman Corporation Aromatic basic-tailed vasopressin antagonists
US4656248A (en) * 1985-04-23 1987-04-07 Smithkline Beckman Corporation Cupric oxidation of 1,6-dimercapto-containing peptides
US4711877A (en) * 1985-09-18 1987-12-08 Smithkline Beckman Corporation 6-pen-vasopressin compounds
US4742154A (en) * 1985-10-23 1988-05-03 Smithkline Beckman Corporation GLN- or ASN-vasopressin compounds
US4687758A (en) * 1985-11-19 1987-08-18 Smithkline Beckman Corporation Des-proline-N-methylarginine vasopressins
US4760052A (en) * 1986-01-16 1988-07-26 Smithkline Beckman Corporation 1,6-dicarba-vasopressin compounds
US4876243A (en) * 1986-02-25 1989-10-24 Smithkline Beckman Corporation Vasopressin compounds
US4717715A (en) * 1986-06-23 1988-01-05 Smithkline Beckman Corporation ARG7 -ARG8 -vasopressin antagonists
US4724229A (en) * 1986-09-30 1988-02-09 Smithkline Beckman Corporation Arg-arg-arg-vasopressin antagonists
US4766108A (en) * 1986-12-04 1988-08-23 Smith Kline Beckman Corporation Tyr-Arg-vasopressin antagonists
US4826813A (en) * 1987-05-21 1989-05-02 Smithkline Beckman Corporation 4'-Methyl-β-mercapto-β,β-cyclopentamethylenepropionic acid vasopressin antagonists
US5055448A (en) * 1987-06-25 1991-10-08 Medical College Of Ohio Linear derivatives of arginine vasopressin antagonists
JP2542241B2 (ja) * 1988-08-12 1996-10-09 富士レビオ株式会社 ペプチド
US5051400A (en) * 1990-06-28 1991-09-24 Smithkline Beecham Corporation Method of treating nausea and emesis related to motion sickness with vasopressin antagonists
US6759384B1 (en) 1994-04-26 2004-07-06 Aventis Pharmaceuticals Inc. Factor Xa inhibitors
US5849510A (en) * 1994-04-26 1998-12-15 Selectide Corporation Factor Xa inhibitors
CA2186497C (en) * 1994-04-26 2008-06-17 Fahad Al-Obeidi Factor xa inhibitors
US6001809A (en) * 1994-07-11 1999-12-14 Elan Pharmaceuticals, Inc. Inhibitors of leukocyte adhesion
IL138214A0 (en) * 1998-03-09 2001-10-31 Zealand Pharmaceuticals As Pharmacolgically active peptide conjugates having a reduced tendency towards enzymatic hydrolysis
US9744239B2 (en) 2015-01-30 2017-08-29 Par Pharmaceutical, Inc. Vasopressin formulations for use in treatment of hypotension
US9925233B2 (en) 2015-01-30 2018-03-27 Par Pharmaceutical, Inc. Vasopressin formulations for use in treatment of hypotension
US9687526B2 (en) 2015-01-30 2017-06-27 Par Pharmaceutical, Inc. Vasopressin formulations for use in treatment of hypotension
US9750785B2 (en) 2015-01-30 2017-09-05 Par Pharmaceutical, Inc. Vasopressin formulations for use in treatment of hypotension
US9937223B2 (en) 2015-01-30 2018-04-10 Par Pharmaceutical, Inc. Vasopressin formulations for use in treatment of hypotension
US9744209B2 (en) 2015-01-30 2017-08-29 Par Pharmaceutical, Inc. Vasopressin formulations for use in treatment of hypotension

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CA1246055A (en) * 1980-03-24 1988-12-06 Joseph H. Cort N-.omega.-substituted hormonogens of vasopressin and its synthetic analogs
US4399125A (en) * 1981-03-24 1983-08-16 Maurice Manning Novel antagonists of the antidiuretic action of arginine vasopressin
US4367225A (en) * 1981-03-24 1983-01-04 The Medical College Of Ohio Novel antagonists of the antidiuretic and/or vasopressor action of arginine vasopressin
US4643520A (en) * 1983-03-10 1987-02-17 Allied Corporation Method of terminating fiber optic connector without polishing optical fiber

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Publication number Publication date
US4542124A (en) 1985-09-17
NO840563L (no) 1984-08-17
NZ207106A (en) 1990-12-21
HU196227B (en) 1988-10-28
IE56859B1 (en) 1992-01-01
JPS59155348A (ja) 1984-09-04
ES529738A0 (es) 1986-04-01
FI840577A (fi) 1984-08-17
DE3479664D1 (en) 1989-10-12
ES535842A0 (es) 1985-10-01
US4469679A (en) 1984-09-04
IE840352L (en) 1984-08-16
ATE46174T1 (de) 1989-09-15
FI840577A0 (fi) 1984-02-14
IL70944A (en) 1990-11-29
IL70944A0 (en) 1984-05-31
ZA841104B (en) 1985-04-24
DK65284A (da) 1984-08-17
DK65284D0 (da) 1984-02-14
ES8600216A1 (es) 1985-10-01
ES8606408A1 (es) 1986-04-01
ZW1884A1 (en) 1984-05-30
PT78094B (en) 1986-05-20
GR81786B (ko) 1984-12-12
EP0119705A2 (en) 1984-09-26
PT78094A (en) 1984-03-01
EP0119705A3 (en) 1987-04-22
AU577778B2 (en) 1988-10-06
PH20076A (en) 1986-09-18
HUT34042A (en) 1985-01-28
EP0119705B1 (en) 1989-09-06
AU2453484A (en) 1984-08-23

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