KR840007713A - 고혈압 치료용 화합물의 제조방법 - Google Patents

고혈압 치료용 화합물의 제조방법 Download PDF

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Publication number
KR840007713A
KR840007713A KR1019840000106A KR840000106A KR840007713A KR 840007713 A KR840007713 A KR 840007713A KR 1019840000106 A KR1019840000106 A KR 1019840000106A KR 840000106 A KR840000106 A KR 840000106A KR 840007713 A KR840007713 A KR 840007713A
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South Korea
Prior art keywords
alanyl
ethoxycarbonyl
alkyl
phenylpropyl
fused
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KR1019840000106A
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English (en)
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후앙(외 3) 후-치
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원본미기재
유 에스 브이 파마슈티칼 코포레이숀
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Publication of KR840007713A publication Critical patent/KR840007713A/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
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/022—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2
    • 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
    • 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
    • Y10S530/00—Chemistry: natural resins or derivatives; peptides or proteins; lignins or reaction products thereof
    • Y10S530/80—Antihypertensive peptides

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Veterinary Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Cardiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Steroid Compounds (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Measurement And Recording Of Electrical Phenomena And Electrical Characteristics Of The Living Body (AREA)
  • Stereophonic System (AREA)
  • Indole Compounds (AREA)
  • Magnetic Resonance Imaging Apparatus (AREA)

Abstract

내용 없음.

Description

고혈압 치료용 화합물의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (4)

  1. 아미드-생성 조건하에서 일반식(2)의 아미노 화합물을 일반식(3)의 산의 아실화 유도체와 반응시키고, 임의로 상기 생성물에 여러 치환체를 도입시켜 치환 또는 전환 반응을 수행하고, 임의로 그의 염, 특히 산 및 염기와의 약학적으로 허용되는 염을 생성시킴을 특징으로 하여, 일반식(1)의 화합물 및 그의 염을 제조하는 방법.
    상기식에서, A 및 A′는 독립적으로 하드록시, 알콕시, 아릴옥시 또는 하이드록시아미노이며; R1, R2, R4및 R5는 독립적으로 수소, 알킬, 아릴, 아르알킬, 융합된 사이클로알킬아릴, 융합된 아릴사이클로알킬, 아릴옥시알킬 또는 아릴알킬옥시알킬이고; R3는 수소, 저급알킬, 저급알케닐, 저급알키닐, 아릴, 융합된 사이클로알킬아릴, 융합된 아릴 사이클로알킬, 융합된 사이클로알킬아릴알킬, 융합된 아릴사이클로알킬알킬, 아르알킬, 사이클로알킬 또는 헤테로 사이클이며; R6는 수소, 알킬, 알케닐, 알키닐, 아실사, 이클로알킬, 사이클로알킬알킬, 폴리사이클로알킬, 폴리사이클로알킬알킬, 아릴, 아르알킬, 폴리사이클릭아릴, 융합된 사이클로알킬아릴, 융합된 아릴사이클로 알킬, 융합된 아릴사이클로알킬알킬 또는 융합된 사이클로알킬아릴알킬이고; 여기에서 알길, 알콕시, 알켄옥시, 알커닐 및 알키닐그룹은 하이드록시, 아실옥시, 아릴, 알콕시, 아릴옥시, 아미노, 모노-또는 디알킬아미노, 아실아미노, 머캅토, 알킬 또는 알킬 티오로 치환될 수 있으며; 아릴 및 사이클로알킬 환을 하나 이상의 헤테로 원자를 함유할 수 있고, 카복실산, 시아노, 카보-저급알콕시, 알킬, 하이드록시, 알콕시, 하이드록시알킬, 할로, 할로알킬, 머캅토, 머캅토알킬, 알킬티오, 아미노, 알킬아미노, 아미노알킬, 니트로, 메틸렌디옥시 또는 설파밀 그룹으로 치환될 수 있으며; 사이클로알킬 그룹은 포화 또는 불포화 될 수 있다.
  2. 제 1항에 있어서, R1, R2, R3, R4및 R5중의 적어도 하나가 수소인 방법.
  3. 제 1항에 있어서, A 및 A′는 독립적으로 하이드록시 또는 알콕시이며; Rl, R2, R3,R4및 R5는 독립적으로 수소, 알킬, 아릴, 아르알킬, 아릴옥시알킬 또는 W-아미노알킬이고; R5는 수소, 알킬, 아릴, 아르알킬, 사이클로알킬, 알콕시알킬, 아미노알킬, 헤테로아릴, 헤테로아릴알킬 또는 융합된 아릴아릴인 방법.
  4. 제 1항 내지 3항 중의 어느 하나에 있어서, 생성물이 다음 화합물들 중의 하나인 방법; 0-벤질-N-[N-[(1S)-1-에톡시카보닐-3-페닐프로필]-L-알라닐]-α-[하이드록실-아미노]-아세트산, 0-벤질-N-[N-[(1S)-1-에톡시카보닐-3-페닐프로필]-L-알라닐]-α-[하이드록실-아미노]-아세트산 3급-부틸 에스테르, 0-메틸-N-[N-[(1S)-1-에톡시카보닐-3-페닐프로필]-L-알라닐]-α-[하이드록실-아미노]-아세트산, 0-메틸-N-[N-[(1S)-1-에톡시카보닐-3-페닐프로필]-L-알라닐]-α-[하이드록실-0-아미노]-아세트산 3급-부틸 에스테르, 0-벤질-N-[N-[(1S)-1-에톡시카보닐-3-페닐프로필]-L-리시닐]-α-[하이드록실-0-아미노]-아세트산, 0-벤질-N-[N-[(1S)-1-에톡시카보닐-에틸]-L-알라닐]-α-[하이드록실아미노]-아세트산, 0-(4-피리디메틸)-N-[N-[(1S)-1-에톡시-카보닐-3-페닐프로필]-L-알라닐]-α-[하이드록실-아미노]-아세트산, 0-(에톡시에틸)-N-[N-[(1S)-1-에톡시카보닐-3-페닐프로필]-L-알라닐]-α-[하이드록실아미노]-아세트산, 0-벤질-N-[N[(1S)-1-에톡시카보닐-3-펜옥시프로필]-L-알라닐]-α-[하이드록실아미노]-아세트산, 0-벤질-N-[N[(1S)-1-에톡시카보닐-3-페닐프로필]-L-알라닐]-α-[하이드록실-아미노]-프로피온산, 0-(1-나프틸메틸)-N-[N-[(1S)-1-에톡시카보닐-3-페닐프로필]-L-알라닐]-α-[하이드록실아미노]-아세트산, 및 0-[N-모르폴리노에틸]-N-[N-{(1S)-에톡시카보닐-3-페닐프로필]-L-알라닐]-α-[하이드록실아미노]-아세트산.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019840000106A 1983-01-12 1984-01-12 고혈압 치료용 화합물의 제조방법 KR840007713A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US06/457,611 US4496541A (en) 1983-01-12 1983-01-12 Compounds for treating hypertension
US457611 1983-01-12

Publications (1)

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KR840007713A true KR840007713A (ko) 1984-12-10

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Country Status (16)

Country Link
US (1) US4496541A (ko)
EP (1) EP0114067B1 (ko)
JP (1) JPS59130844A (ko)
KR (1) KR840007713A (ko)
AT (1) ATE26841T1 (ko)
AU (1) AU560330B2 (ko)
CA (1) CA1257749A (ko)
DE (1) DE3463385D1 (ko)
DK (1) DK13484A (ko)
ES (1) ES8504109A1 (ko)
FI (1) FI85012C (ko)
IE (1) IE56586B1 (ko)
IL (1) IL70676A (ko)
NO (1) NO840102L (ko)
NZ (1) NZ206826A (ko)
ZA (1) ZA84262B (ko)

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US4686295A (en) * 1982-03-10 1987-08-11 Usv Pharmaceutical Corporation N-carboxy anhydride intermediates
JPS6248696A (ja) * 1985-08-27 1987-03-03 Kanegafuchi Chem Ind Co Ltd Ｎ−〔１（ｓ）−エトキシカルボニル−３−フエニルプロピル〕−ｌ−アラニル−ｌ−プロリンの製造法
SI9200213A (en) * 1992-09-16 1994-03-31 Krka Process for preparing alkyl-l-alanil-l-proline derivates
US6262274B1 (en) * 2000-10-13 2001-07-17 Everlight Usa, Inc. Process for preparing N-[1-(S)-ethyoxycarbonyl-3-phenylpropyl]-L-ananine N-carboxyanhydride
FR2815962B1 (fr) * 2000-10-30 2003-03-07 Isochem Sa Procede de preparation des n-carboxyanhydrides
US7973173B2 (en) * 2005-07-05 2011-07-05 Cipla Limited Process for the synthesis of an ACE inhibitor
UA98767C2 (uk) 2006-05-12 2012-06-25 Егіш Дьйодьсердьяр Нільваношан Мюкьодо Ресвеньтаршашаг Фармацевтичні проміжні сполуки в синтезі інгібіторів ацетилхолінестерази (асе)
US7911232B2 (en) * 2008-04-30 2011-03-22 B & Plus K.K. Input/output signal controller
US8443112B2 (en) * 2009-03-24 2013-05-14 B & Plus K.K. Input/output signal controller and input/output signal control system employing the input/output controller

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR1904M (fr) * 1962-03-01 1963-07-08 Merck & Co Inc Médicament a base d'acide n-acyl-hydroxyamino-acétique pour le traitement des tumeurs.
AT296252B (de) * 1968-03-30 1972-02-10 Richter Gedeon Vegyeszet Verfahren zur Herstellung von neuen N-Acyl-hydroxylaminderivaten und deren Säureadditionssalzen
JPS4843726A (ko) * 1971-10-05 1973-06-23
US4098903A (en) * 1976-06-01 1978-07-04 Research Corporation Anti-hypertensive compounds
IL58849A (en) * 1978-12-11 1983-03-31 Merck & Co Inc Carboxyalkyl dipeptides and derivatives thereof,their preparation and pharmaceutical compositions containing them
US4820729A (en) * 1981-03-30 1989-04-11 Rorer Pharmaceutical Corporation N-substituted-amido-amino acids

Also Published As

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FI85012B (fi) 1991-11-15
IL70676A (en) 1988-09-30
ATE26841T1 (de) 1987-05-15
DK13484D0 (da) 1984-01-12
IE840054L (en) 1984-07-12
EP0114067A1 (en) 1984-07-25
IL70676A0 (en) 1984-04-30
CA1257749A (en) 1989-07-18
JPS59130844A (ja) 1984-07-27
AU2325484A (en) 1984-07-19
US4496541A (en) 1985-01-29
DE3463385D1 (en) 1987-06-04
IE56586B1 (en) 1991-10-09
FI85012C (fi) 1992-02-25
FI840109A0 (fi) 1984-01-12
ES528816A0 (es) 1985-05-01
FI840109A (fi) 1984-07-13
ES8504109A1 (es) 1985-05-01
DK13484A (da) 1984-07-13
NZ206826A (en) 1986-03-14
AU560330B2 (en) 1987-04-02
EP0114067B1 (en) 1987-04-29
ZA84262B (en) 1984-08-29
NO840102L (no) 1984-07-13

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