KR840005709A - 치환펩티드 화합물의 제조방법 - Google Patents

치환펩티드 화합물의 제조방법 Download PDF

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KR840005709A
KR840005709A KR1019830003289A KR830003289A KR840005709A KR 840005709 A KR840005709 A KR 840005709A KR 1019830003289 A KR1019830003289 A KR 1019830003289A KR 830003289 A KR830003289 A KR 830003289A KR 840005709 A KR840005709 A KR 840005709A
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group
lower alkyl
hydrogen
alkyl group
general formula
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KR1019830003289A
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아이어 나타라잔 세샤 (외 1)
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조오지 제이.코에서
이이, 아아트. 스퀴부 앤드 산즈 인코오포레이티드
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Publication of KR840005709A publication Critical patent/KR840005709A/ko

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    • 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
    • C07K5/06—Dipeptides
    • C07K5/06086—Dipeptides with the first amino acid being basic
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • 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
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • 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
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • 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
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • C07K5/06—Dipeptides
    • C07K5/06086—Dipeptides with the first amino acid being basic
    • C07K5/06095—Arg-amino acid
    • 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
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • 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
    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyrrole Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Furan Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

내용 없음

Description

치환펩티드 화합물의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (20)

  1. a) 다음 일반식(Ⅱ)의 산 할로겐화합물과 다음 일반식(Ⅲ)의 옥사졸론과 반응시키고 보호기 B40을 제거한 후, -COOR6를 -COOH로 임의로 전환시켜서 R가 수소인 일반식(Ⅰ)의 생성물을 제조하거나, b)할로기가 CI또는 Br인 다음 일반식(V)의 케톤을 X기의 -COOR6은 다음에 정의한 바와 같은 일반식(Ⅵ)의 화합물과 반응시킨 다음 위의 (a)에서와 같이 기능적으로 전환시키거나, c) 다음 일반식(Ⅸ)의 아미노케톤을 다음 일반식(Ⅹ)의 화합물과 반응시키는 것을 특징으로 하는 다음 일반식(Ⅰ)의 화합물 또는 약리학적으로 허용가능한 이들의 염을 제조하는 방법.
  3. 위의 실시예 (Ⅰ)에서, X는
  5. 또는이고 R은 수소, 저급알킬기, 시클로알킬기,, -(CH2)2- NH2, -(CH2)3- NH2, -(CH|2)4-NH2, -(CH2)2-OH, -(CH2)3-OH, -(CH2)4-OH, -(CH2)2-SH, -(CH2)3-SH, 또는 -(CH2)4-SH이며, R1은 수소, 저급알킬기, 할로겐으로 치환된 저급알킬기,
  7. -(CH2)r- OH,, -(CH2)r-NH2, -(CH2)r-SH, -(CH2)r-OH, -(CH2)r
  8. -NH2, -(CH2)r-SH, -(CH2)r-S-저급알킬,또는이고 (단, R1은 R가 수소가 아닌 경우에만 수소이다),
  11. 할로겐으로 치환된 저급알킬기 - (CH2)m-시클토알킬,
  13. -(CH2)r-NH2, -(CH2)r-SH, -(CH2)r-S-저급 알킬,또는 -(CH2)r-이고, R4는 수소, 저급 알킬기,-(CH2)m-시클로알킬-(CH2)r-
  17. -(CH2)r-OH2, -(CH2)r-NH2, -(CH2)r-SH, -(CH2)r- S-저급 알킬,또는이고, r는 1-4의 정수이며, R7은 수소, 저급알킬기, 할로켄, 케토기, 히드록시기,저급알킬기, 이지도기, 이미노기, 일반식의 1 또는 2 -나프틸기, -(CH2)m-시클로알킬기,-O-저급알킬,의 1 또는 2-나프틸옥시기, -S-저급알킬기,또는 일반식의 1 또는 2-나프틸티오기이고, R8는 케토기, 할로겐,-O-저급알킬기,
  18. 일반식의 1 또는 2-나프틸옥시기, -S-저급알킬기,
  19. 의 1 또는 2-나프틸티오기이며, R9는 케토기, 또는이고, R10은 할로겐 또는 -Y-R16이며, R11,R12,R13,및R"12는 수소 및 저급 알킬기에서 독립적으로 선발되거나 Ru',R12및|R12'는 수소이고, R11이이고, R13은 수소, C1-4의 저급 알킬기, C1-4의 저급 알콕시기, C1-4의 저급알킬티오기, Cl, Br, F, 트리플루오로메틸기, -OH, 페닐기, 펜옥시기, 페닐티오기, 또는 페닐메틸기이며, R14는 수소, C1-4의 저급 알킬기, C1-4의 저급 알콕시기, C1-4의 저급 알킬티오기, Cl, Br, F, 트리플루오로메틸기, 또는 -OH이고, m은 0, 1, 2, 3, 또는 4이며, p는 1, 2, 또는 3이며(단, p는R23또는 R14가 수소, 메틸기, 메톡시기, CI 또는 F일 경우에만 1이다),R15는 수소, C1-4의 저급 알킬기이고, Y는 산소 또는 황이며, R16은 C1-4의 저급 알킬기,또는 R6기가 연결되어 불포화 5 또는 6원링을 형성하거나 이들 링의 1개 이상의 탄소가 C1-4의 저급 알킬기 또는 이치환체(C1-4의 저급 알킬기의)를 가질 수 있고, R19는 저급 알킬기, 벤질기 또는 펜에틸기이며, R20은 수소, 저급알킬기, 벤질기 또는 펜에틸기이고, R6은 수소, 저급 알킬기, 벤질기. 벤즈히드릴,또는이며, R17은 수소, 저급 알킬기, 시클로알킬기 또는 페닐기이고, R18은 수소, 저급 알킬기, 저급 알콕시기, 페닐기이거나, 또는 R17과 R18이 함께 취하여 -(CH2)2- , -(CH2)3- , -CH=CH 또는이고, R24는 수소, 저급알킬기, 이며 R21및 R22는 수소와 저급 알킬기로 구성된 군에서 독립적으로 선택된 기이고, R23은 저급 알킬기이며, 위의 일반식에서 할로기의 CI도는 Br이고, X기의 -COOR6은 -COOH 이외의 것이며, R4는 아미노 보호기임.
  20. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019830003289A 1982-07-19 1983-07-18 치환펩티드 화합물의 제조방법 KR840005709A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US39965082A 1982-07-19 1982-07-19
US399650 1982-07-19

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JP (3) JPS5951246A (ko)
KR (1) KR840005709A (ko)
AU (1) AU1643283A (ko)
BE (1) BE897327A (ko)
CA (1) CA1244006A (ko)
CH (1) CH659475A5 (ko)
DE (1) DE3325850A1 (ko)
DK (1) DK330683A (ko)
ES (4) ES524200A0 (ko)
FI (1) FI832620A (ko)
FR (3) FR2530238B1 (ko)
GB (1) GB2123834B (ko)
GR (1) GR79602B (ko)
HU (1) HU187090B (ko)
IE (1) IE55818B1 (ko)
IL (1) IL69136A0 (ko)
IT (1) IT1163800B (ko)
NL (1) NL8302562A (ko)
PT (1) PT77045B (ko)
SE (1) SE8304031L (ko)
ZA (1) ZA834980B (ko)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS55159749A (en) * 1979-05-31 1980-12-12 Takeda Chem Ind Ltd Preparation of dried fish flesh
US4500518A (en) * 1984-04-19 1985-02-19 E. R. Squibb & Sons, Inc. Amino thiol dipeptides
DE3588094T2 (de) * 1984-09-12 1996-08-22 Rhone Poulenc Rorer Pharma Antihypertensive Derivate
US4629724A (en) * 1984-12-03 1986-12-16 E. R. Squibb & Sons, Inc. Amino acid ester and amide renin inhibitors
FR2578544A1 (en) * 1985-03-11 1986-09-12 Usv Pharma Corp Antihypertension spirocyclic compounds
FI89058C (fi) * 1987-02-27 1993-08-10 Yamanouchi Pharma Co Ltd Foerfarande foer framstaellning av som remin-inhibitorer anvaenda 2-(l-alanyl-l-histidylamino)-butanol-derivat
EP1264707A3 (en) 2001-05-14 2004-05-19 Oji Paper Co., Ltd. Thermosensitive recording material and novel color developer compounds
DE202018107306U1 (de) 2017-01-10 2019-01-28 Mitsubishi Hitec Paper Europe Gmbh Neuartiger Farbentwickler für ein wärmeempfindliches Aufzeichnungsmedium und ein wärmeempfindliches Aufzeichnungsmaterial auf der Basis PLA

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US3751239A (en) * 1969-05-29 1973-08-07 Rohm & Haas Herbicidal compositions containing n-(1,1-dialkyl-3-chloroacetonyl) benzamides
JPS5430167A (en) * 1977-08-11 1979-03-06 Mitsubishi Chem Ind Ltd 4-aminomethyl-2-phenyloxazoles and their pharmaceutically acceptable acid salts
IL58849A (en) * 1978-12-11 1983-03-31 Merck & Co Inc Carboxyalkyl dipeptides and derivatives thereof,their preparation and pharmaceutical compositions containing them
FR2480747A1 (fr) * 1980-04-17 1981-10-23 Roques Bernard Derives d'acides amines et leur application therapeutique
IE51409B1 (en) * 1980-07-24 1986-12-24 Ici Ltd Amide derivatives
EP0048159A3 (en) * 1980-09-17 1982-05-12 University Of Miami Novel carboxyalkyl peptides and thioethers and ethers of peptides as antihypertensive agents
DE3174844D1 (en) * 1980-10-23 1986-07-24 Schering Corp Carboxyalkyl dipeptides, processes for their production and pharmaceutical compositions containing them
US4462943A (en) * 1980-11-24 1984-07-31 E. R. Squibb & Sons, Inc. Carboxyalkyl amino acid derivatives of various substituted prolines
EP0054862B1 (en) * 1980-12-18 1985-11-27 Schering Corporation Substituted dipeptides, processes for their preparation and pharmaceutical compositions containing them and their use in the inhibition of enkephalinase
US4514391A (en) * 1983-07-21 1985-04-30 E. R. Squibb & Sons, Inc. Hydroxy substituted peptide compounds

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ES8504675A1 (es) 1985-04-16
AU1643283A (en) 1984-01-26
BE897327A (fr) 1984-01-19
HUT34040A (en) 1985-01-28
SE8304031D0 (sv) 1983-07-18
GB8318492D0 (en) 1983-08-10
JPH0645582B2 (ja) 1994-06-15
IE831655L (en) 1984-01-19
FI832620A (fi) 1984-01-20
PT77045A (en) 1983-08-01
JPH0517420A (ja) 1993-01-26
IT1163800B (it) 1987-04-08
GB2123834B (en) 1986-10-22
SE8304031L (sv) 1984-03-30
JPH0532601A (ja) 1993-02-09
FR2540867A1 (fr) 1984-08-17
DK330683D0 (da) 1983-07-18
IL69136A0 (en) 1983-10-31
ES539083A0 (es) 1986-04-01
ES524200A0 (es) 1985-04-16
FR2530238B1 (ko) 1989-06-30
JPS5951246A (ja) 1984-03-24
PT77045B (en) 1986-02-12
ES8707549A1 (es) 1986-04-01
IT8322114A0 (it) 1983-07-18
ES8707548A1 (es) 1986-05-16
ZA834980B (en) 1984-03-28
JPH0526775B2 (ko) 1993-04-19
JPH0653713B2 (ja) 1994-07-20
FI832620A0 (fi) 1983-07-19
DE3325850A1 (de) 1984-01-19
CH659475A5 (fr) 1987-01-30
ES8707550A1 (es) 1986-04-01
ES539084A0 (es) 1986-04-01
NL8302562A (nl) 1984-02-16
FR2540867B1 (fr) 1987-07-31
DK330683A (da) 1984-01-20
IE55818B1 (en) 1991-01-30
FR2540866A1 (fr) 1984-08-17
ES539082A0 (es) 1986-05-16
HU187090B (en) 1985-11-28
GB2123834A (en) 1984-02-08
GR79602B (ko) 1984-10-31
FR2530238A1 (ko) 1984-01-20
CA1244006A (en) 1988-11-01

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