KR850002834A - 염기성 헵타 펩타이드 바조프레신 길항근의 제조방법 - Google Patents
염기성 헵타 펩타이드 바조프레신 길항근의 제조방법 Download PDFInfo
- Publication number
- KR850002834A KR850002834A KR1019840005806A KR840005806A KR850002834A KR 850002834 A KR850002834 A KR 850002834A KR 1019840005806 A KR1019840005806 A KR 1019840005806A KR 840005806 A KR840005806 A KR 840005806A KR 850002834 A KR850002834 A KR 850002834A
- Authority
- KR
- South Korea
- Prior art keywords
- tyr
- phe
- pro
- alk
- val
- Prior art date
Links
- 238000000034 method Methods 0.000 title claims 13
- 239000005557 antagonist Substances 0.000 title 1
- 108090000765 processed proteins & peptides Proteins 0.000 title 1
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims 5
- 150000001875 compounds Chemical class 0.000 claims 5
- -1 D- Chg Chemical compound 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- OUYCCCASQSFEME-MRVPVSSYSA-N D-tyrosine Chemical compound OC(=O)[C@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-MRVPVSSYSA-N 0.000 claims 2
- 125000002849 D-tyrosine group Chemical group [H]N([H])[C@@]([H])(C(=O)[*])C([H])([H])C1=C([H])C([H])=C(O[H])C([H])=C1[H] 0.000 claims 2
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 150000001718 carbodiimides Chemical class 0.000 claims 2
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims 2
- 239000007800 oxidant agent Substances 0.000 claims 2
- 125000006239 protecting group Chemical group 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims 1
- SNDPXSYFESPGGJ-SCSAIBSYSA-N D-2-aminopentanoic acid Chemical compound CCC[C@@H](N)C(O)=O SNDPXSYFESPGGJ-SCSAIBSYSA-N 0.000 claims 1
- AGPKZVBTJJNPAG-RFZPGFLSSA-N D-Isoleucine Chemical compound CC[C@@H](C)[C@@H](N)C(O)=O AGPKZVBTJJNPAG-RFZPGFLSSA-N 0.000 claims 1
- ONIBWKKTOPOVIA-SCSAIBSYSA-N D-Proline Chemical compound OC(=O)[C@H]1CCCN1 ONIBWKKTOPOVIA-SCSAIBSYSA-N 0.000 claims 1
- ROHFNLRQFUQHCH-RXMQYKEDSA-N D-leucine Chemical compound CC(C)C[C@@H](N)C(O)=O ROHFNLRQFUQHCH-RXMQYKEDSA-N 0.000 claims 1
- FFEARJCKVFRZRR-SCSAIBSYSA-N D-methionine Chemical compound CSCC[C@@H](N)C(O)=O FFEARJCKVFRZRR-SCSAIBSYSA-N 0.000 claims 1
- COLNVLDHVKWLRT-MRVPVSSYSA-N D-phenylalanine Chemical group OC(=O)[C@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-MRVPVSSYSA-N 0.000 claims 1
- 125000001711 D-phenylalanine group Chemical group [H]N([H])[C@@]([H])(C(=O)[*])C([H])([H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- KZSNJWFQEVHDMF-SCSAIBSYSA-N D-valine Chemical compound CC(C)[C@@H](N)C(O)=O KZSNJWFQEVHDMF-SCSAIBSYSA-N 0.000 claims 1
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 claims 1
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 150000004985 diamines Chemical class 0.000 claims 1
- YAGKRVSRTSUGEY-UHFFFAOYSA-N ferricyanide Chemical compound [Fe+3].N#[C-].N#[C-].N#[C-].N#[C-].N#[C-].N#[C-] YAGKRVSRTSUGEY-UHFFFAOYSA-N 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 229910052740 iodine Inorganic materials 0.000 claims 1
- 239000011630 iodine Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000003647 oxidation Effects 0.000 claims 1
- 238000007254 oxidation reaction Methods 0.000 claims 1
- 235000019260 propionic acid Nutrition 0.000 claims 1
- 238000007363 ring formation reaction Methods 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
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/16—Oxytocins; Vasopressins; Related peptides
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/10—Antioedematous agents; Diuretics
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Biophysics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Pharmacology & Pharmacy (AREA)
- Diabetes (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Genetics & Genomics (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Optical Communication System (AREA)
- Thin Film Transistor (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (13)
- A가 -NR-(CH2)n-NR2이거나 -NR-(CH2)n-NH--NR2이고; Z가 Phe,Phe(4´-Alk) 혹은 Tyr(Alk)이고; X는 D-Phe, D-Phe(4´-Alk), D-Val, D-Nva, D-Leu, D-Ile, D-Pba, D-Cha, D-Abu, D-Met, D-Chg, D-Tyr, L-Tyr, D-Tyr(Alk) 혹은 L-Tyr(Alk)이고; P는 D-Pro, L-Pro, △3-Pro, L-Ala, L-N-MeAla, L-Gly, L-Sar 혹은 단일 결합이며; Y는 Val, Ile, Abu, Ala, Chg, Gln, Lys, Cha, Nle, Phe, Leu 혹은 Gly이고; R은 각 경우에 수소이거나 C1-5-알킬이고; n은 2-8의 정수이고; m은 0-2의 정수인 일반식 I의 화합물을 제조하는 방법.또는 X,Z,Y과 P가 위에서 정의된 바와 같고; Q1과 Q2가 각각 수소이거나 치환될 수 없는 그룹이고; A가 OH이거나 상기 정의한 바와 같고; Cap이 β-위치에 붙은 S-Q1를 가진 β,β-싸이클로 알킬렌 프로피온산인 일반식(Ⅱ)의 임의로 보호된 화합물을 환식화하는 것과 싸이클로 알킬렌 사슬에 5-7유니트를 가지는 것 및 그후 임의의 어떤 순서로 (a) 어떤 보호그룹을 제거하는 것 (b) 언제나 존재하는 상기 Cys(OH)6혹은 P(OH)7화합물을 보호된 형태에서 임의로 디아민, H-A로 반응시키는 것. (c) 이들의 약제상 허용 가능한 염을 형성하는 것으로 구성되는 약제상 허용 가능한 상기 화합물의 산부가염을 제조하는 방법.
- Q1과 Q2가 둘다 수소인 청구범위 제1항에 따른 방법.
- Q1과 Q2가 둘다 아세트 아미도메틸인 청구범위 제1항에 따른 방법.
- 산화에 의한 환식화로 구성되는 청구범위 제1항-제3항에 따른 방법.
- 산화제인 요오드를 사용하여 실시되는 청구범위 제4항에 따른 방법.
- 산화제로서 페리시아나이드를 사용하여 실시되는 청구범위 제4항에 따른 방법.
- 일반식 Ⅰ의 Cys(OH)6화합물을 카보디이미드의 존재하에 H-A와 반응시키고 뒤이어 임의로 어떤 보호그룹을 제거하는 청구범위 제1항에 따른 방법.
- 일반식 Ⅰ의 Pro(OH)7화합물을 카보디이미드의 존재하에 H-H와 반응시키고 뒤이어 임의로 어떤 보회그룹을 제거하는 청구범위 제1항에 따른 방법.
- A가 -NHC5H10NH2이고; Z가 Phe이고; X가 D-Tyr(Et)이고; Y가 Val이고; P가 Pro이고; m이 1인 청구범위 제8항의 방법.
- A가 -NHC2H10NH2이고; Z가 Phe이고; X가 D-Tyr(Et)이고; Y가 Val이고; P가 단일결합이며; m이 1인 청구범위 제7항의 방법.
- X가 D-이거나 L-Tvr 혹은 D-이거나 L-Tyr(Alk)이고; Z가 Phe이고; Y가 Val이고; P가 Pro이거나 △3-Pro이고 A가 청구범위 제1항에서 정의된 바와 같은 청구범위 제1항의 방법.
- A가 OH인 청구범위 제1-6항이나 11항의 방법.
- X가 L-Tyr이고 Y가 Gln인 청구범위 제1항의 방법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US53500083A | 1983-09-22 | 1983-09-22 | |
| US535000 | 1983-09-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR850002834A true KR850002834A (ko) | 1985-05-20 |
Family
ID=24132435
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019840005806A KR850002834A (ko) | 1983-09-22 | 1984-09-21 | 염기성 헵타 펩타이드 바조프레신 길항근의 제조방법 |
Country Status (21)
| Country | Link |
|---|---|
| EP (1) | EP0135379B1 (ko) |
| JP (1) | JPS6094997A (ko) |
| KR (1) | KR850002834A (ko) |
| AT (1) | ATE33659T1 (ko) |
| AU (1) | AU576519B2 (ko) |
| CA (1) | CA1238314A (ko) |
| DE (1) | DE3470544D1 (ko) |
| DK (1) | DK408284A (ko) |
| EG (1) | EG16586A (ko) |
| ES (1) | ES536117A0 (ko) |
| FI (1) | FI843723L (ko) |
| GR (1) | GR80427B (ko) |
| HU (1) | HU199881B (ko) |
| IL (1) | IL72789A (ko) |
| JO (1) | JO1335B1 (ko) |
| NO (1) | NO843816L (ko) |
| NZ (1) | NZ209207A (ko) |
| PH (1) | PH20384A (ko) |
| PT (1) | PT79236B (ko) |
| ZA (1) | ZA846450B (ko) |
| ZW (1) | ZW13284A1 (ko) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4599324A (en) * | 1984-11-21 | 1986-07-08 | Smithkline Beckman Corporation | V1-vasopressin antagonists |
| US4604378A (en) * | 1984-11-21 | 1986-08-05 | Smithkline Beckman Corporation | Basic V1 -vasopressin antagonists |
| US4772586A (en) * | 1985-01-23 | 1988-09-20 | Medical College Of Ohio | Novel derivatives of arginine vasopressin antagonists |
| PT83455B (en) * | 1985-10-02 | 1988-10-20 | Smithkline Beckman Corp | Vasopressin compounds |
| US4742154A (en) * | 1985-10-23 | 1988-05-03 | Smithkline Beckman Corporation | GLN- or ASN-vasopressin compounds |
| US4687758A (en) * | 1985-11-19 | 1987-08-18 | Smithkline Beckman Corporation | Des-proline-N-methylarginine vasopressins |
| EP3877439A4 (en) * | 2018-11-07 | 2022-08-10 | Regents of the University of Minnesota | ANALGESIC AND ANTI-ADDICTION COMPOSITIONS FOR THE TREATMENT OF CHRONIC PAIN AND OPIOID DEPENDENCE |
| CN116003518B (zh) * | 2023-01-10 | 2023-09-29 | 深圳市维琪科技股份有限公司 | 经设计的肽及其组合物和用途 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4399125A (en) * | 1981-03-24 | 1983-08-16 | Maurice Manning | Novel antagonists of the antidiuretic action of arginine vasopressin |
| US4491577A (en) * | 1981-11-16 | 1985-01-01 | The Medical College Of Ohio | Antagonists of the antidiuretic action of arginine vasopressin |
| US4643520A (en) * | 1983-03-10 | 1987-02-17 | Allied Corporation | Method of terminating fiber optic connector without polishing optical fiber |
| IE58407B1 (en) * | 1984-04-13 | 1993-09-22 | Akzo Nv | Peptides |
| GB8427651D0 (en) * | 1984-11-01 | 1984-12-05 | Beecham Group Plc | Compounds |
-
1984
- 1984-08-13 CA CA000460840A patent/CA1238314A/en not_active Expired
- 1984-08-14 NZ NZ209207A patent/NZ209207A/xx unknown
- 1984-08-15 ZW ZW132/84A patent/ZW13284A1/xx unknown
- 1984-08-20 ZA ZA846450A patent/ZA846450B/xx unknown
- 1984-08-23 AT AT84305764T patent/ATE33659T1/de not_active IP Right Cessation
- 1984-08-23 EP EP84305764A patent/EP0135379B1/en not_active Expired
- 1984-08-23 DE DE8484305764T patent/DE3470544D1/de not_active Expired
- 1984-08-27 DK DK408284A patent/DK408284A/da not_active Application Discontinuation
- 1984-08-28 IL IL72789A patent/IL72789A/xx unknown
- 1984-08-28 PH PH31152A patent/PH20384A/en unknown
- 1984-09-14 AU AU33037/84A patent/AU576519B2/en not_active Ceased
- 1984-09-18 EG EG576/84A patent/EG16586A/xx active
- 1984-09-19 PT PT79236A patent/PT79236B/pt unknown
- 1984-09-20 GR GR80427A patent/GR80427B/el unknown
- 1984-09-21 JP JP59199326A patent/JPS6094997A/ja active Pending
- 1984-09-21 HU HU843584A patent/HU199881B/hu not_active IP Right Cessation
- 1984-09-21 ES ES536117A patent/ES536117A0/es active Granted
- 1984-09-21 KR KR1019840005806A patent/KR850002834A/ko not_active Application Discontinuation
- 1984-09-21 FI FI843723A patent/FI843723L/fi not_active Application Discontinuation
- 1984-09-21 NO NO843816A patent/NO843816L/no unknown
- 1984-09-29 JO JO19841335A patent/JO1335B1/en active
Also Published As
| Publication number | Publication date |
|---|---|
| NO843816L (no) | 1985-03-25 |
| ZA846450B (en) | 1985-05-29 |
| DE3470544D1 (en) | 1988-05-26 |
| ES8506599A1 (es) | 1985-08-01 |
| AU3303784A (en) | 1985-03-28 |
| HU199881B (en) | 1990-03-28 |
| EP0135379A3 (en) | 1986-03-12 |
| ES536117A0 (es) | 1985-08-01 |
| HUT36142A (en) | 1985-08-28 |
| PT79236B (en) | 1986-11-24 |
| JPS6094997A (ja) | 1985-05-28 |
| DK408284D0 (da) | 1984-08-27 |
| IL72789A (en) | 1988-10-31 |
| CA1238314A (en) | 1988-06-21 |
| AU576519B2 (en) | 1988-09-01 |
| EP0135379A2 (en) | 1985-03-27 |
| JO1335B1 (en) | 1986-11-30 |
| EP0135379B1 (en) | 1988-04-20 |
| FI843723A0 (fi) | 1984-09-21 |
| FI843723L (fi) | 1985-03-23 |
| GR80427B (en) | 1985-01-18 |
| ATE33659T1 (de) | 1988-05-15 |
| EG16586A (en) | 1987-10-30 |
| DK408284A (da) | 1985-03-23 |
| PH20384A (en) | 1986-12-08 |
| PT79236A (en) | 1984-10-01 |
| IL72789A0 (en) | 1984-11-30 |
| NZ209207A (en) | 1988-10-28 |
| ZW13284A1 (en) | 1984-11-07 |
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| Date | Code | Title | Description |
|---|---|---|---|
| A201 | Request for examination | ||
| E902 | Notification of reason for refusal | ||
| E601 | Decision to refuse application |