KR870002161A - 옥사-및 아자 호모사이클로 스타틴 폴리펩티드의 제조방법 - Google Patents
옥사-및 아자 호모사이클로 스타틴 폴리펩티드의 제조방법 Download PDFInfo
- Publication number
- KR870002161A KR870002161A KR1019860006442A KR860006442A KR870002161A KR 870002161 A KR870002161 A KR 870002161A KR 1019860006442 A KR1019860006442 A KR 1019860006442A KR 860006442 A KR860006442 A KR 860006442A KR 870002161 A KR870002161 A KR 870002161A
- Authority
- KR
- South Korea
- Prior art keywords
- omega
- lysphe
- aminohexylamino
- compound
- general formula
- Prior art date
Links
Classifications
-
- 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
- C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
-
- 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
- C07K5/0227—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the (partial) peptide sequence -Phe-His-NH-(X)2-C(=0)-, e.g. Renin-inhibitors with n = 2 - 6; for n > 6 see C07K5/06 - C07K5/10
-
- 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
-
- 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
- Y10S530/86—Renin inhibitors
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biophysics (AREA)
- General Health & Medical Sciences (AREA)
- Genetics & Genomics (AREA)
- Medicinal Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Biochemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (4)
- 하기 일반식(3)의 화합물을 하기 일반식(4)의 화합물과 탈수-커플링시킨 후 임의로 1)차단 그룹을 선택적으로 제거하고, 2) R2의 Lysphe 메틸 에스테르를 암모니아로 Lysphe 아미드로 전환시키고 3) R2의 오메가-시아노펜틸아미노를 촉매 수소화시켜 오멘가-아미노헥실아미노를 환원시키고 필요시 생성물의 약학적으로 허용되는 산 부가염을 제조함을 특징으로 하여 하기 일반식(1)의 화합물을 제조하는 방법.상기식에서, R1은 수소 또는 메틸이고, X는 산소, 아미노, 탄소수 1 내지 4의 알킬아미노, 사이클로헥실 메틸아미노, 벤질아미노, 오메가-아미노헥실아미노 또는 메톡시카보닐메틸아미노이며, R2는 Lysphe, Lysphe-메틸에스테르, Lysphe 아미드, Lyssta, 아미노 탄소수 1 내지 4의 알킬아미노, 탄소수 3 내지 4의 알킬, 4-이미다졸일 에틸아미노, 오메가-아미노헥실아미노 벤질옥시, 오메가-시아노펜닐아미노 또는 일반식의 환원된 Hephe (여기서, R3는 수소, 오메가-아미노헥실 또는 오메가-시아노펜틸이다)이고, 일반식(4)에서, 반응에 포함되지 않는 작용성 그룹은 차단된다.
- 제1항에 있어서, 커플링을 1-하이드록시벤조트리아졸 및 디사이클로헥실카보디이미드를 사용하여 수행하는 방법.
- 제2항에 있어서, 0-벤질 및 카보벤즈옥시 차단 그룹을 촉매 가수소분해시켜 제거하는 방법.
- 제2항에 있어서, 이미다졸 3급-부톡시카보닐 차단그룹을 메탄올중에서 무기염기로 제거하는 방법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US06/762,099 US4668769A (en) | 1985-08-02 | 1985-08-02 | Oxa- and azahomocyclostatine polypeptides |
US762099 | 1985-08-02 | ||
US780353 | 1985-09-26 | ||
US780553 | 1985-09-26 | ||
US06/780,353 US4599198A (en) | 1985-08-02 | 1985-09-26 | Intermediates in polypeptide synthesis |
Publications (2)
Publication Number | Publication Date |
---|---|
KR870002161A true KR870002161A (ko) | 1987-03-30 |
KR890003602B1 KR890003602B1 (ko) | 1989-09-27 |
Family
ID=27117072
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019860006442A KR890003602B1 (ko) | 1985-08-02 | 1986-08-02 | 옥사-및 아자호모사이클로스타틴 폴리펩티드의 제조방법 |
Country Status (14)
Country | Link |
---|---|
US (1) | US4599198A (ko) |
EP (1) | EP0211580A3 (ko) |
KR (1) | KR890003602B1 (ko) |
AU (3) | AU569821B2 (ko) |
CA (1) | CA1305175C (ko) |
DK (1) | DK366686A (ko) |
ES (1) | ES2001056A6 (ko) |
FI (1) | FI863153A (ko) |
GR (1) | GR862009B (ko) |
HU (1) | HU204284B (ko) |
IE (1) | IE862072L (ko) |
IL (1) | IL79570A0 (ko) |
NZ (2) | NZ217067A (ko) |
PT (1) | PT83123B (ko) |
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CA1108180A (en) * | 1976-07-21 | 1981-09-01 | Hamao Umezawa | Analogs of bestatin |
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CA1297631C (en) * | 1985-12-23 | 1992-03-17 | Sesha I. Natarajan | Ureido renin inhibitors |
-
1985
- 1985-09-26 US US06/780,353 patent/US4599198A/en not_active Expired - Fee Related
-
1986
- 1986-07-25 EP EP86305722A patent/EP0211580A3/en not_active Withdrawn
- 1986-07-29 GR GR862009A patent/GR862009B/el unknown
- 1986-07-30 IL IL79570A patent/IL79570A0/xx not_active IP Right Cessation
- 1986-07-31 ES ES8600783A patent/ES2001056A6/es not_active Expired
- 1986-08-01 HU HU863358A patent/HU204284B/hu not_active IP Right Cessation
- 1986-08-01 PT PT83123A patent/PT83123B/pt not_active IP Right Cessation
- 1986-08-01 FI FI863153A patent/FI863153A/fi not_active Application Discontinuation
- 1986-08-01 DK DK366686A patent/DK366686A/da not_active Application Discontinuation
- 1986-08-01 NZ NZ217067A patent/NZ217067A/xx unknown
- 1986-08-01 IE IE862072A patent/IE862072L/xx unknown
- 1986-08-01 NZ NZ228380A patent/NZ228380A/xx unknown
- 1986-08-01 AU AU60790/86A patent/AU569821B2/en not_active Ceased
- 1986-08-02 KR KR1019860006442A patent/KR890003602B1/ko not_active IP Right Cessation
-
1988
- 1988-02-29 AU AU12392/88A patent/AU598913B2/en not_active Ceased
-
1990
- 1990-10-05 AU AU63850/90A patent/AU633629B2/en not_active Ceased
-
1991
- 1991-01-04 CA CA000615970A patent/CA1305175C/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
AU569821B2 (en) | 1988-02-18 |
PT83123A (en) | 1986-09-01 |
FI863153A0 (fi) | 1986-08-01 |
AU6385090A (en) | 1991-01-10 |
NZ228380A (en) | 1990-08-28 |
DK366686D0 (da) | 1986-08-01 |
AU1239288A (en) | 1988-06-02 |
AU6079086A (en) | 1987-05-14 |
NZ217067A (en) | 1990-08-28 |
PT83123B (pt) | 1989-03-30 |
AU598913B2 (en) | 1990-07-05 |
KR890003602B1 (ko) | 1989-09-27 |
DK366686A (da) | 1987-03-20 |
EP0211580A2 (en) | 1987-02-25 |
FI863153A (fi) | 1987-02-03 |
ES2001056A6 (es) | 1988-04-16 |
US4599198A (en) | 1986-07-08 |
HUT41815A (en) | 1987-05-28 |
EP0211580A3 (en) | 1989-08-09 |
AU633629B2 (en) | 1993-02-04 |
HU204284B (en) | 1991-12-30 |
IE862072L (en) | 1987-02-02 |
CA1305175C (en) | 1992-07-14 |
GR862009B (en) | 1986-12-23 |
IL79570A0 (en) | 1986-10-31 |
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