KR890006669A - 아미노산 유도체 - Google Patents
아미노산 유도체 Download PDFInfo
- Publication number
- KR890006669A KR890006669A KR1019880012511A KR880012511A KR890006669A KR 890006669 A KR890006669 A KR 890006669A KR 1019880012511 A KR1019880012511 A KR 1019880012511A KR 880012511 A KR880012511 A KR 880012511A KR 890006669 A KR890006669 A KR 890006669A
- Authority
- KR
- South Korea
- Prior art keywords
- formula
- carbon atoms
- compound
- chr
- amino
- Prior art date
Links
- 150000003862 amino acid derivatives Chemical class 0.000 title claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 6
- -1 Pyr Chemical compound 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 125000004103 aminoalkyl group Chemical group 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 239000007788 liquid Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 1
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 claims 1
- QNAYBMKLOCPYGJ-UHFFFAOYSA-N D-alpha-Ala Natural products CC([NH3+])C([O-])=O QNAYBMKLOCPYGJ-UHFFFAOYSA-N 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 102100028255 Renin Human genes 0.000 claims 1
- 108090000783 Renin Proteins 0.000 claims 1
- UCKMPCXJQFINFW-UHFFFAOYSA-N Sulphide Chemical compound [S-2] UCKMPCXJQFINFW-UHFFFAOYSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 238000005576 amination reaction Methods 0.000 claims 1
- 150000001450 anions Chemical class 0.000 claims 1
- UCMIRNVEIXFBKS-UHFFFAOYSA-N beta-alanine Chemical compound NCCC(O)=O UCMIRNVEIXFBKS-UHFFFAOYSA-N 0.000 claims 1
- 150000001602 bicycloalkyls Chemical group 0.000 claims 1
- 150000001735 carboxylic acids Chemical class 0.000 claims 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 238000007327 hydrogenolysis reaction Methods 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000000468 ketone group Chemical group 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 239000007800 oxidant agent Substances 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 102000004196 processed proteins & peptides Human genes 0.000 claims 1
- 108090000765 processed proteins & peptides Proteins 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 238000003797 solvolysis reaction Methods 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
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
- C07K7/02—Linear peptides 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
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/10—Tetrapeptides
- C07K5/1024—Tetrapeptides with the first amino acid being heterocyclic
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
-
- 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
- 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
- C07K5/06043—Leu-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
- C07K5/06008—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
- C07K5/06139—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
- C07K5/06139—Dipeptides with the first amino acid being heterocyclic
- C07K5/06156—Dipeptides with the first amino acid being heterocyclic and Trp-amino acid; Derivatives thereof
-
- 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
- C07K5/08—Tripeptides
- C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
- C07K5/0823—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp and Pro-amino acid; 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
Landscapes
- 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)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Peptides Or Proteins (AREA)
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (7)
- 다음 일반식(I)의 아미노산 유도체 및 이의 염.X-Z-NR3-CHR4-CR5(CHR6)n-E (I)상기식에서 X는 H, R1-O-CmH2m-CO-, R1-CmH2m-O-CO-,R1-CmH2m-CO-, R1-SO2-, (R1-CmH2M)-L (R2-CpH2p)-CrH2r-CO-, R1-(NHCH2CH2)m-NH-CH2CO-, 9-플루오르에닐-CmH2m-O-CO-, [R1-CmH2m-(T)X-, V-CtH2t]-L(R2-CpH2p)-CrH2r-CO- 또는 A3N-CmH2m-CO-An이고, Z는 서로 펩티드 형태로 결합한 1 내지 4의 아미노산 라디칼로서 Abu, Ada, Ala, β-Ala, Arg, Asn, Asp, Bia, Cal, Dab, Ftr, Gln, Glu, Gly, His, Hph, N(im)-A-His, Ile, Leu, 3급-Leu, Lys, Met, αNal, βNal, Nbg, Nle, Nva, Orn, Phe, Pro, Pyr, Ser, Thr, Tia, Tic, Trp, Tyr, O-A-Tyr 및 Val로 이루어진 그룹에서 선택하고, E는 S-R7, SO-R7, SO2,-R7, SO2-OR7, 또는 SO2-NR7R8이고, R1, R2, R4, R7및 R8는 각각 H, A, Ar, Ar-알킬, Het, Het-알킬 또는 탄소수 3 내지 7의 시클로알킬, 탄소수 4 내지 11의 시클로알킬알킬, 각기 탄소수 7 내지 14의 비시클로알킬 또는 트리시클로알킬 또는 트리시클로알킬 또는 각기 탄소수 8 내지 18의 비시클로알킬알킬 또는 트리시클로알킬알킬로서, 각 경우 A, AO 및/또는 Hal로 비치환 또는 일치환 또는 다치환되고,R3는 H 또는 A이고, R5는 각기 (H, OH), (H, NH2) 또는 =O이고, R6는 H, A또는 탄소수 2 내지 8의 알케닐이고, m, p, r 및 t는 각각 0, 1, 2, 3, 4 또는 5이고, n는 또는 2이고, X는 O 또는 I이고, L은 CH 또는 N이고, T는 O 또는 NH이고, V는 CO또는 SO2이고, An는 일가의 음이온이고, Ar은 A, AO, Hal, CF3, HO, 탄소수 1 내지 8의 아미노 알킬로 비치환 또는 일치한 또는 다치환된 페닐, 또는 비치환된 나프틸이고, Het는 1 내지 4의 N, O 및/또는 S원자를 갖는 포화 또는 불포화 5-원 또는 6-원 헤테로시 클릭라디칼로서 벤젠링과 응합할 수 있고/있거나, A, AO, Hal, CF3, HO, O2N, 카보닐산소, H2N, HAN, A2N, AcNH, AS, ASO, ASO2, AOOC, CN, H2NCO, H2NSO2, ASO2NH, Ar, Ar-알케닐, 각기 탄소수 1 내지 8의 히드록시알킬 및/또는 아미노알킬로 일치환 또는 다치환될 수 있고/있거나 이의 N 및/또는 S 헤테로원자는 또한 산화될 수도 있고, Hal은 F, Cl, Br 또는 I이고, AC는 A-CO-, Ar-CO- 또는 A-NH-CO-이고 A는 탄소수 1 내지 8의 알킬이며, 여기에서 하나 또는 그이상의 -NH-CO-그룹은 또한 하나 또는 그 이상의 -NA-CO- 그룹으로 대체될 수도 있다.
- a) 3S-히드록시 4S-BOC-Phe-His-아미노-6-메틸 헵탄설폰산 모르폴리드, b) 3S-히드록시 4S-[비스-(1-나프틸메틸)-아세틸-His]-아미노-6-메틸 헵탄-설폰산 모르폴리드, c) 1R-이소프로필-3S-히드록시 4S-BOC-Phe-His-아미노-5-시클로헥실-펙탄-설폰산 모르폴리드, d) IS-이소프로필-3S-히드록시 4S-BOC-Phe-His아미노-5-시클로헥실-펜탄-설폰산 모르폴리드.
- 일반식(I)의 아미노산 유도체 및 이의 염을 제조하는 방법에 있어서, 이의 작용성 유도체중 하나를 가용매 분해제 또는 가수소분해제로 처리하여 유리시키거나, 또는 일반식(II)의 카르복실산 또는 이의 반응성 유도체중, 하나를 일반식(II I)의 화합물 또는 이의 반응성 유도체중의 하나와반응시키고/시키거나, 적합하다면 E가 SO-R7또는 -SO2-R7인 일반식(I)의 화합물을 제조하기 위해서 E가 S-R7인 일반식(I)의 설피드를 산화제로 처리하고/하거나, 적합하다면, 일반식(I)의 화합물에 있어서 작용적으로 변형된 아미노 및/또는 히드록실 그룹을 가용매분해제 또는 가수소분해제로 처리하여 유리시키고/시키거나 케토 그룹을 CHOH 그룹으로 환원시키거나 또는 CH(NH2) 그룹으로 환원적으로 아민화시키고/시키거나 일반식(I)의 화합물을 산으로 처리하여 이의 염증의 하나로 전환시킴을 특징으로 하는 일반식(I)의 아미노산 유도체 및 이의 염을 제조하는 방법.X-G1-OH (Ⅱ)H-G2(Ⅲ)상기식에서 G1은(a)-Z1-또는 (b)-Z-이고, G2은(a)- Z2-NR3-CHR4-CR5-(CHR6)n-E 또는 (b)-NR3-CHR4-CR5-(CHR6)n-E이고, Z1+Z2는 함께 Z이고, R3, R4, R5, R6, n 및 E는 정의한 바와같다.
- 일반식(I)의 화합물 및/또는 이의 생리학적으로 허용되는 염을 적어도 하나의 고체, 액체 또는 반-액체 부형제 또는 보조제와 함께, 필요시, 하나 또는 그이상의 다른 활성 성분(들)과 함께 적절한 투여형으로 전환시킴을 특징으로 하는 약제학적 제형의 제조방법.
- 적어도 하나의 일반식(I)의 화합물 및/또는 이의 생리학적으로 허용되는 염증 하나를 함유하는 것을 특징으로 하는 약제학적 제형.
- 약물의 제조를 위한 일반식(I)의 화합물 또는 이의 생리학적으로 허용되는 염의 용도.
- 고혈압 또는 과알도스테론중에 관련된 레닌을 억제하는데 있어서 일반식(I)의 화합물 또는 이의 생리학적으로 허용되는 염의 용도.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19873733296 DE3733296A1 (de) | 1987-10-02 | 1987-10-02 | Aminosaeurederivate |
| DEP3733296.1 | 1987-10-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR890006669A true KR890006669A (ko) | 1989-06-15 |
Family
ID=6337447
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019880012511A KR890006669A (ko) | 1987-10-02 | 1988-09-28 | 아미노산 유도체 |
Country Status (7)
| Country | Link |
|---|---|
| EP (1) | EP0309841A3 (ko) |
| JP (1) | JPH01113360A (ko) |
| KR (1) | KR890006669A (ko) |
| AU (1) | AU615216B2 (ko) |
| DE (1) | DE3733296A1 (ko) |
| HU (1) | HU203770B (ko) |
| ZA (1) | ZA887373B (ko) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3721855A1 (de) * | 1987-03-12 | 1988-09-22 | Merck Patent Gmbh | Aminosaeurederivate |
| DE3814325A1 (de) * | 1988-04-28 | 1989-11-09 | Merck Patent Gmbh | Aminosaeurederivate |
| CA1340588C (en) * | 1988-06-13 | 1999-06-08 | Balraj Krishan Handa | Amino acid derivatives |
| GB8927913D0 (en) * | 1989-12-11 | 1990-02-14 | Hoffmann La Roche | Amino acid derivatives |
| AU7032391A (en) * | 1989-12-22 | 1991-07-24 | Astra Aktiebolag | New amides |
| TW209870B (ko) * | 1990-01-18 | 1993-07-21 | Pfizer | |
| DE4014421A1 (de) * | 1990-05-05 | 1991-11-07 | Merck Patent Gmbh | Aminosaeurederivate |
| TW198712B (ko) * | 1991-04-17 | 1993-01-21 | Hoffmann La Roche |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1987004349A1 (en) * | 1986-01-16 | 1987-07-30 | Joseph Dellaria | Peptide analogs |
| NL8800100A (nl) * | 1987-01-21 | 1988-08-16 | Sandoz Ag | Nieuwe peptidederivaten en werkwijzen voor het bereiden en toepassen van deze derivaten. |
-
1987
- 1987-10-02 DE DE19873733296 patent/DE3733296A1/de not_active Withdrawn
-
1988
- 1988-09-17 EP EP19880115274 patent/EP0309841A3/de not_active Withdrawn
- 1988-09-20 ZA ZA887373A patent/ZA887373B/xx unknown
- 1988-09-28 KR KR1019880012511A patent/KR890006669A/ko not_active Application Discontinuation
- 1988-09-29 AU AU22982/88A patent/AU615216B2/en not_active Ceased
- 1988-09-30 HU HU885097A patent/HU203770B/hu unknown
- 1988-09-30 JP JP63244664A patent/JPH01113360A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| ZA887373B (en) | 1989-06-28 |
| EP0309841A2 (de) | 1989-04-05 |
| JPH01113360A (ja) | 1989-05-02 |
| AU615216B2 (en) | 1991-09-26 |
| DE3733296A1 (de) | 1989-04-20 |
| AU2298288A (en) | 1989-06-08 |
| EP0309841A3 (de) | 1990-09-26 |
| HU203770B (en) | 1991-09-30 |
| HUT50485A (en) | 1990-02-28 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| KR880005148A (ko) | 아미노산 유도체 | |
| US5120831A (en) | Metal-peptide compositions | |
| TW487711B (en) | Conjugates of lipophilic moieties and peptides | |
| KR960701653A (ko) | 펩타이드 yy의 유사체 및 그의 용도 | |
| KR880011196A (ko) | 아미노산 유도체 | |
| KR970015598A (ko) | 환상 결합 억제제 | |
| HUT49891A (en) | Process for production of peptides with antiaggregation effect and medical compositions containing them | |
| TW343198B (en) | Cyclopeptides useful as adhesion inhibitors, process for the preparation thereof, and pharmaceutical composition containing them | |
| KR900002801A (ko) | 당뇨병 치료용 약학적제제 | |
| CA2027936A1 (en) | Cyclic anti-aggregatory peptides | |
| KR930007972A (ko) | 환상 혈관활성 펩티드 | |
| KR920009846A (ko) | 시클로펩티드 | |
| KR890006669A (ko) | 아미노산 유도체 | |
| KR880012641A (ko) | 아미노산 유도체 | |
| KR910000794A (ko) | Vip-유사체 ⅱ | |
| KR900003205A (ko) | 제약 화합물 | |
| KR910016739A (ko) | 글리콜 산 유도체 | |
| KR880000468A (ko) | 아미노산 유도체의 제조방법 | |
| KR880002784A (ko) | 아미노산 유도체 | |
| KR880013976A (ko) | 항응고제인 사이클릭 펩타이드 | |
| KR890014579A (ko) | 폴리펩티드 | |
| KR900001719A (ko) | 지질 및 폴리펩티드로 되는 합성 폐 계면활성제의 제조 방법 | |
| KR880013902A (ko) | 아미노산 유도체 | |
| KR910016768A (ko) | 아미노산 유도체 | |
| KR910009730A (ko) | 펩티드 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PA0109 | Patent application |
Patent event code: PA01091R01D Comment text: Patent Application Patent event date: 19880928 |
|
| PG1501 | Laying open of application | ||
| PC1203 | Withdrawal of no request for examination | ||
| WITN | Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid |