KR960701088A - 포스포노메틸디펩타이드(Phosphonomethyldipeptides) - Google Patents

포스포노메틸디펩타이드(Phosphonomethyldipeptides) Download PDF

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KR960701088A
KR960701088A KR1019950704199A KR19950704199A KR960701088A KR 960701088 A KR960701088 A KR 960701088A KR 1019950704199 A KR1019950704199 A KR 1019950704199A KR 19950704199 A KR19950704199 A KR 19950704199A KR 960701088 A KR960701088 A KR 960701088A
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compound
alkyl
aryl
hydrogen
disease
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KR1019950704199A
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KR100311852B1 (ko
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도르시몽 위그
비고 마르끄
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게리 디. 스트리트
메렐 다우 파마슈티칼즈 인코포레이티드
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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
    • 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
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/55—Protease inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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
    • 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
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
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  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Peptides Or Proteins (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

본 발명은 엔도첼린 전환 효소를 억제함으로써 이에 반응하는 상태를 치료하는데 유용한 포스포노메틸 잔기가 부착되어 있는 디펩타이드 및 이의 동족체에 관한 것이다.

Description

포스포노메틸디펩타이드(Phosphonomethyldipeptides)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 일반식(Ⅰ)의 화합물, 이의 입체이성체, 이의 수화물,이의 내부염 또는 약제학적으로 허용되는 이의염.
    (Ⅰ)
    상기 식에서, R1또는 R2는 각각 독립적으로 수소 C1-6알킬, (CH2)m-아릴, R4-C(O)O-CH(R5)-를 나타내거나 내부염이 형성되는 경우 존재하지 않으며, 단 R1또는 R2중 하나가 수소, C1-6알킬 또는 (CH2)m-아릴을 나타내는 경우, 다른 하나는 수소이거나 내부염이 형성되는 경우 존재하지 않고;R3는 수소, C1-6알킬, (CH2)m-사이클로알킬 또는 (CH2)m-아릴이며; R4는 C1-10알킬, (CH2)m-사이클로알킬 또는 (CH2)m-아릴이고; R5는 C1-6알킬, (CH2)m-사이클로알킬 또는 수소이며; R6은 H이거나 R1또는 R2중하나가 존재하지 않아 내부염을 형성하는 경우 H2이고; R7은 CH3또는 H이며; R8은 H, Br, CH3또는 OCH3이고, 단 R7또는 R8중 하나는 H이며; Z는 (CH2)m-아릴 또는 C1-12알킬이고; X는 수소 또는 C1-6알킬이며; m은 각각 독립적으로 0, 1, 2 또는 3이고; n은 1, 2 또는 3이다.
  2. 제1항에 있어서, R1이 H인 화합물.
  3. 제1항에 있어서, R2가 존재하지 않고 R6가 H2인 화합물.
  4. 제1항에 있어서, R3가 H 또는 (CH2)-아릴인 화합물.
  5. 제1항에 있어서, Z가 이소- 부틸인 화합물.
  6. 제1항에 있어서, X가 H인 화합물.
  7. 제1항에 있어서, N-(N-포스포노메틸-L-류실)-L-트립토판, N-(N-벤질옥시하이드록시포스피닐메틸-L-류실)-L-트립토판, 벤질 에스테르, N-(N-벤질옥시하이드록시포스피닐메틸-L-류실)-L-트립토판, N-(N-포스포노메틸-L-류실)-DL-호모트립토판, N-〔N-(디-(피발로일옥시메틸)-포스포닐)-류실〕-L-트립토판, 에틸 에스테르 및 N-(N-피발로일옥시메틸옥시하이드록시포스피닐-L-류실)-L-트립토판, 에틸 에스테르로 이루어진 그룹으로부터 선택된 화합물.
  8. 제1항에 있어서, 약제학적 활성 화합물로서 사용하기위한 화합물.
  9. 약제학적으로 허용되는 담체와임의로 배합된 제1항에 따른 화합물을 포함하는 약제학적 조성물.
  10. 제1항에 있어서, 내피억제에 반응하는 상태인, 심장 혈관질환, 기관지협착, 뉴론성 작용질환, 혈관질환 및 신장질환의 치료시 사용하기 위한 화합물.
    내피 억제에 방응하는 상태인, 심장 혈관질환, 기관지협착, 뉴론성 작용질환, 혈관질환 및 신장질환치료용의 약제학적 조성물을 제조하기 위한, 약제학적으로 허용되는 담체와 임의로 배합된 제1항에 따른 화합믈의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019950704199A 1993-03-30 1994-02-22 포스포노메틸디펩타이드,이의제조방법및이를포함하는약제학적조성물 KR100311852B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP93400824A EP0618224A1 (en) 1993-03-30 1993-03-30 Phosphonomethyldipeptides
EP93400824.4 1993-03-30
PCT/US1994/001716 WO1994022908A1 (en) 1993-03-30 1994-02-22 Phosphonomethyldipeptides

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KR960701088A true KR960701088A (ko) 1996-02-24
KR100311852B1 KR100311852B1 (ko) 2002-02-28

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KR1019950704199A KR100311852B1 (ko) 1993-03-30 1994-02-22 포스포노메틸디펩타이드,이의제조방법및이를포함하는약제학적조성물

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EP (2) EP0618224A1 (ko)
JP (1) JP3541230B2 (ko)
KR (1) KR100311852B1 (ko)
CN (1) CN1120844A (ko)
AT (1) ATE192456T1 (ko)
AU (1) AU670866B2 (ko)
CA (1) CA2156742C (ko)
DE (1) DE69424281T2 (ko)
DK (1) DK0691985T3 (ko)
ES (1) ES2148322T3 (ko)
FI (1) FI954656A (ko)
GR (1) GR3034015T3 (ko)
HU (1) HU217836B (ko)
IL (1) IL109128A (ko)
NO (1) NO953877L (ko)
NZ (1) NZ262996A (ko)
PT (1) PT691985E (ko)
TW (1) TW290550B (ko)
WO (1) WO1994022908A1 (ko)
ZA (1) ZA942091B (ko)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5583123A (en) * 1994-12-22 1996-12-10 Ciba-Geigy Corporation Certain tetrazole derivatives
US5550119A (en) * 1995-03-02 1996-08-27 Ciba-Geigy Corporation Phosphono substituted tetrazole derivatives as ECE inhibitors

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8726714D0 (en) * 1987-11-14 1987-12-16 Beecham Group Plc Compounds
JP2811608B2 (ja) * 1991-04-26 1998-10-15 日本ケミファ株式会社 ホスホン酸アミド誘導体およびエンドセリン変換酵素阻害剤
JPH05105698A (ja) * 1991-06-13 1993-04-27 Takeda Chem Ind Ltd ホスホン酸誘導体、その製造法および用途

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HU217836B (hu) 2000-04-28
NO953877D0 (no) 1995-09-29
CA2156742C (en) 2001-04-17
ZA942091B (en) 1994-10-24
JPH08508480A (ja) 1996-09-10
FI954656A0 (fi) 1995-09-29
EP0618224A1 (en) 1994-10-05
HUT72465A (en) 1996-04-29
TW290550B (ko) 1996-11-11
CN1120844A (zh) 1996-04-17
ES2148322T3 (es) 2000-10-16
HU9502852D0 (en) 1995-11-28
DE69424281T2 (de) 2000-09-21
EP0691985A1 (en) 1996-01-17
DK0691985T3 (da) 2000-08-07
CA2156742A1 (en) 1994-10-13
GR3034015T3 (en) 2000-11-30
NO953877L (no) 1995-11-30
KR100311852B1 (ko) 2002-02-28
AU670866B2 (en) 1996-08-01
JP3541230B2 (ja) 2004-07-07
NZ262996A (en) 1996-06-25
PT691985E (pt) 2000-08-31
WO1994022908A1 (en) 1994-10-13
EP0691985B1 (en) 2000-05-03
IL109128A (en) 1999-09-22
DE69424281D1 (en) 2000-06-08
ATE192456T1 (de) 2000-05-15
AU6298994A (en) 1994-10-24
FI954656A (fi) 1995-09-29
IL109128A0 (en) 1994-06-24

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