KR960701088A - 포스포노메틸디펩타이드(Phosphonomethyldipeptides) - Google Patents
포스포노메틸디펩타이드(Phosphonomethyldipeptides) Download PDFInfo
- Publication number
- 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
- Authority
- KR
- South Korea
- Prior art keywords
- compound
- alkyl
- aryl
- hydrogen
- disease
- Prior art date
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Classifications
-
- 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)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- 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)
- Pulmonology (AREA)
- Endocrinology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Reproductive Health (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- 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
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (10)
- 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.
- 제1항에 있어서, R1이 H인 화합물.
- 제1항에 있어서, R2가 존재하지 않고 R6가 H2인 화합물.
- 제1항에 있어서, R3가 H 또는 (CH2)-아릴인 화합물.
- 제1항에 있어서, Z가 이소- 부틸인 화합물.
- 제1항에 있어서, X가 H인 화합물.
- 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.
- 제1항에 있어서, 약제학적 활성 화합물로서 사용하기위한 화합물.
- 약제학적으로 허용되는 담체와임의로 배합된 제1항에 따른 화합물을 포함하는 약제학적 조성물.
- 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.
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 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR960701088A true KR960701088A (ko) | 1996-02-24 |
KR100311852B1 KR100311852B1 (ko) | 2002-02-28 |
Family
ID=8214693
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019950704199A KR100311852B1 (ko) | 1993-03-30 | 1994-02-22 | 포스포노메틸디펩타이드,이의제조방법및이를포함하는약제학적조성물 |
Country Status (20)
Country | Link |
---|---|
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)
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)
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 |
-
1993
- 1993-03-30 EP EP93400824A patent/EP0618224A1/en not_active Withdrawn
-
1994
- 1994-02-22 NZ NZ262996A patent/NZ262996A/en unknown
- 1994-02-22 EP EP94910701A patent/EP0691985B1/en not_active Expired - Lifetime
- 1994-02-22 HU HU9502852A patent/HU217836B/hu not_active IP Right Cessation
- 1994-02-22 AT AT94910701T patent/ATE192456T1/de not_active IP Right Cessation
- 1994-02-22 KR KR1019950704199A patent/KR100311852B1/ko not_active IP Right Cessation
- 1994-02-22 JP JP52205194A patent/JP3541230B2/ja not_active Expired - Fee Related
- 1994-02-22 DK DK94910701T patent/DK0691985T3/da active
- 1994-02-22 ES ES94910701T patent/ES2148322T3/es not_active Expired - Lifetime
- 1994-02-22 CA CA002156742A patent/CA2156742C/en not_active Expired - Fee Related
- 1994-02-22 WO PCT/US1994/001716 patent/WO1994022908A1/en active IP Right Grant
- 1994-02-22 AU AU62989/94A patent/AU670866B2/en not_active Ceased
- 1994-02-22 DE DE69424281T patent/DE69424281T2/de not_active Expired - Fee Related
- 1994-02-22 CN CN94191635A patent/CN1120844A/zh active Pending
- 1994-02-22 PT PT94910701T patent/PT691985E/pt unknown
- 1994-03-24 ZA ZA942091A patent/ZA942091B/xx unknown
- 1994-03-25 TW TW083102628A patent/TW290550B/zh active
- 1994-03-25 IL IL10912894A patent/IL109128A/en not_active IP Right Cessation
-
1995
- 1995-09-29 NO NO953877A patent/NO953877L/no unknown
- 1995-09-29 FI FI954656A patent/FI954656A/fi not_active IP Right Cessation
-
2000
- 2000-07-26 GR GR20000401701T patent/GR3034015T3/el not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
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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