KR950701645A - 신규펩티드와 그것을 사용한 혈소판응집억제제, 체외순환용혈액 응고억제제, 세포접착저지제, 암전이저지제, 수혈용 혈소판제제보호제 및 수혈용혈소판제제팩 - Google Patents
신규펩티드와 그것을 사용한 혈소판응집억제제, 체외순환용혈액 응고억제제, 세포접착저지제, 암전이저지제, 수혈용 혈소판제제보호제 및 수혈용혈소판제제팩Info
- Publication number
- KR950701645A KR950701645A KR1019940701533A KR19940701533A KR950701645A KR 950701645 A KR950701645 A KR 950701645A KR 1019940701533 A KR1019940701533 A KR 1019940701533A KR 19940701533 A KR19940701533 A KR 19940701533A KR 950701645 A KR950701645 A KR 950701645A
- Authority
- KR
- South Korea
- Prior art keywords
- peptide
- inhibitors
- platelet
- transfusion
- derivative
- Prior art date
Links
- 108090000765 processed proteins & peptides Proteins 0.000 title claims abstract description 28
- 230000023555 blood coagulation Effects 0.000 title claims abstract description 5
- 238000002360 preparation method Methods 0.000 title claims abstract 7
- 230000021164 cell adhesion Effects 0.000 title claims abstract 4
- 206010028980 Neoplasm Diseases 0.000 title claims abstract 3
- 239000003130 blood coagulation factor inhibitor Substances 0.000 title claims abstract 3
- 201000011510 cancer Diseases 0.000 title claims abstract 3
- 229940127218 antiplatelet drug Drugs 0.000 title claims 2
- 239000000106 platelet aggregation inhibitor Substances 0.000 title claims 2
- 102000004196 processed proteins & peptides Human genes 0.000 title claims 2
- 239000002257 antimetastatic agent Substances 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 239000004480 active ingredient Substances 0.000 claims abstract 6
- 150000003839 salts Chemical class 0.000 claims 10
- 150000001413 amino acids Chemical class 0.000 claims 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 5
- 239000011782 vitamin Substances 0.000 claims 5
- 229940088594 vitamin Drugs 0.000 claims 5
- 229930003231 vitamin Natural products 0.000 claims 5
- 235000013343 vitamin Nutrition 0.000 claims 5
- 239000000556 agonist Substances 0.000 claims 4
- 150000003862 amino acid derivatives Chemical class 0.000 claims 4
- 150000003722 vitamin derivatives Chemical class 0.000 claims 3
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical group NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 2
- QIVBCDIJIAJPQS-VIFPVBQESA-N L-tryptophane Chemical compound C1=CC=C2C(C[C@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-VIFPVBQESA-N 0.000 claims 2
- QIVBCDIJIAJPQS-UHFFFAOYSA-N Tryptophan Natural products C1=CC=C2C(CC(N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-UHFFFAOYSA-N 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000003277 amino group Chemical group 0.000 claims 2
- UCMIRNVEIXFBKS-UHFFFAOYSA-N beta-alanine Chemical compound NCCC(O)=O UCMIRNVEIXFBKS-UHFFFAOYSA-N 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 150000007523 nucleic acids Chemical class 0.000 claims 2
- 102000039446 nucleic acids Human genes 0.000 claims 2
- 108020004707 nucleic acids Proteins 0.000 claims 2
- BMLMGCPTLHPWPY-UHFFFAOYSA-N 2-oxo-1,3-thiazolidine-4-carboxylic acid Chemical compound OC(=O)C1CSC(=O)N1 BMLMGCPTLHPWPY-UHFFFAOYSA-N 0.000 claims 1
- ODHCTXKNWHHXJC-VKHMYHEASA-N 5-oxo-L-proline Chemical compound OC(=O)[C@@H]1CCC(=O)N1 ODHCTXKNWHHXJC-VKHMYHEASA-N 0.000 claims 1
- 101000783577 Dendroaspis angusticeps Thrombostatin Proteins 0.000 claims 1
- 101000783578 Dendroaspis jamesoni kaimosae Dendroaspin Proteins 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 239000004471 Glycine Chemical group 0.000 claims 1
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims 1
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 claims 1
- 206010027476 Metastases Diseases 0.000 claims 1
- ODHCTXKNWHHXJC-GSVOUGTGSA-N Pyroglutamic acid Natural products OC(=O)[C@H]1CCC(=O)N1 ODHCTXKNWHHXJC-GSVOUGTGSA-N 0.000 claims 1
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims 1
- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 claims 1
- 239000004473 Threonine Substances 0.000 claims 1
- LIXQSGRMEVDRBL-UHFFFAOYSA-N acetic acid;imidazolidine-2,4-dione Chemical compound CC(O)=O.O=C1CNC(=O)N1 LIXQSGRMEVDRBL-UHFFFAOYSA-N 0.000 claims 1
- ODHCTXKNWHHXJC-UHFFFAOYSA-N acide pyroglutamique Natural products OC(=O)C1CCC(=O)N1 ODHCTXKNWHHXJC-UHFFFAOYSA-N 0.000 claims 1
- 125000000266 alpha-aminoacyl group Chemical group 0.000 claims 1
- 229940000635 beta-alanine Drugs 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 125000000524 functional group Chemical group 0.000 claims 1
- 230000002209 hydrophobic effect Effects 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 230000009401 metastasis Effects 0.000 claims 1
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 claims 1
- 239000011814 protection agent Substances 0.000 claims 1
- 239000003223 protective agent Substances 0.000 claims 1
- 125000003607 serino group Chemical group [H]N([H])[C@]([H])(C(=O)[*])C(O[H])([H])[H] 0.000 claims 1
- -1 vitamins Chemical class 0.000 claims 1
- 230000000694 effects Effects 0.000 abstract description 2
- 208000010110 spontaneous platelet aggregation Diseases 0.000 abstract description 2
- 208000007536 Thrombosis Diseases 0.000 abstract 2
- 208000005189 Embolism Diseases 0.000 abstract 1
- 208000001435 Thromboembolism Diseases 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 208000010125 myocardial infarction Diseases 0.000 abstract 1
- 230000001732 thrombotic effect Effects 0.000 abstract 1
- 238000010586 diagram Methods 0.000 description 6
- 241000282472 Canis lupus familiaris Species 0.000 description 3
- 238000000502 dialysis Methods 0.000 description 3
- 230000002401 inhibitory effect Effects 0.000 description 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
- C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/78—Connective tissue peptides, e.g. collagen, elastin, laminin, fibronectin, vitronectin or cold insoluble globulin [CIG]
-
- 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
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/745—Blood coagulation or fibrinolysis factors
-
- 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
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Gastroenterology & Hepatology (AREA)
- Zoology (AREA)
- Toxicology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
RGD를 기본골격으로서 갖는 혈소판응집저지작용, 혈액응고저지작용 및 세포접착저지작용을 갖는 신규펩티드유도체를 발견했다.
그리고, 당해 펩티드유도체의 상기의 효과에 착안하여, 당해 펩티드유도체를 유효성분으로서 포함하는, 혈전붕괴치료중의 치료후의 혈소판혈전증, 혈전폐색증에 대하여 유효한, 또는 재폐색이나 심근경색의 예방도 가능한 혈소판응집억제제; 체회순환시의 혈전형성의 주원인인 혈액응고를 억제할 수 있는 체외순환용혈액응고억제제, 세포접착저지제, 암전이저지제 및 수혈용혈소판제제보호제를 창제하였다.
또, 팩중에 수혈용혈소판제제중에 당해펩티드유도체를 포함하게 것을 특징으로 하는 수혈용혈소판제제팩도 본발명이 기도한 것이다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 인간혈장중에서 합성펩티드의 안정성을 나타낸 도면(1)이고,
제2도는 인간혈장중에서 합성펩티드의 안정성을 나타낸 도면(2)이고,
제3도는 마우스체내에서의 합성펩티드의 안정성을 나타낸 도면이고,
제4도는 비글견을 사용한 혈소판응집억제활성 및 프로트론빈시간의 검토도이고,
제5도는 비글견을 사용한 인공 투석모델 투석회로의 모식도이고,
제6도는 비글견을 사용한 인공 투석모델에 있어서의 혈액응고 효과를 나타낸 도면이다.
Claims (11)
- 일반식A-B-Arg-Gly-Asp-C-D(식중, A는 아미노산, 아미노산유도체, 비타민, 비타민유도체, 비타민과 같은 작용물질, 비타민과 같은 작용물질의 유도체, 핵산의 염기, 핵산의 염기의 유도체 및 히단토인 초산으로 된 군에서 선택된 화합물; B는 아미노산; C는 소수성관능기를 갖는 아미노산; D는 수산기 또는 아미노기를 나타냄)로 표시되는, 펩티드, 펩티드유도체 또는 그들의 염.
- 제1항에 있어서, A의 아미노산 또는 아미노산유도체가, 플로린, 티오플로린, 하이드록시플로린, 데히드로플로린, 2-옥소 4-티아조리딘카본산, 4-알킬글리신 또는 다음 일반식[식중, R1은, 수소원자, 일반식 -(CH2)PCH3, 일반식 -CO-(CH2)PCH3(식중, p는 0~5의 정수임), m은 2~5의 정수, n은 0~2의 정수임]로 표시되는 아미노산유도체, 트리프토판 또는 다음 일반식(식중의 R2는 수소원자 또는 알킬기, R3는 수소원자 또는 0-알킬기, R4는 수소원자 또는 알킬기, R5는 수소원자, 아미노기 또는 아미노아실기, q는 0~3의 정수임)로 표시되는 트리프토판유도체, 피로글루타민산 또는 2-아제티디논-4-카본산인 펩티드, 펩티드유도체 또는 그들의 염.
- 제1항에 있어서, 비타민과 같은작용물질 또는 비타민과 같은 작용물질의 유도체, 오로틴산 또는 하이드로오로틴산인 펩티드, 펩티드유도체 또는 들의 염.
- 제1항 내지 제3항 중의 어느 한항에 있어서, B가 세린,글리신, 바린, 아라신, 스레오닌 또는 β-아라닌인 펩티드, 펩티드 유도체 또는 그들의 염.
- 제1항 내지 제4항중 어느 한항에 있어서, C가 트리프토판 또는 페닐아라닌인, 펩티드 또는 펩티드유도체 또는 그들의 염.
- 제1항 내지 제5항 중 어느 한항에 기재한 펩티드, 펩티드 유도체 또는 그들 염을 유효성분으로서 포함하는, 혈소판응집억제제.
- 제1항 내지 제5항 중 어느 한항에 기재한 펩티드, 펩티드 유도체 또는 그들 염을 유효성분으로서 포함하는, 체외순환용혈액응고억제제.
- 제1항 내지 제5항 중 어느 한항에 기재한 펩티드, 펩티드 유도체 또는 그들 염을 유효성분으로서 포함하는, 세포접착지지제.
- 제1항 내지 제5항 중 어느 한항에 기재한 펩티드, 펩티드 유도체 또는 그들 염을 유효성분으로서 포함하는, 암전이저지제.
- 제1항 내지 제5항 중 어느 한항에 기재한 펩티드, 펩티드 유도체 또는 그들 염을 유효성분으로서 포함하는, 수혈용혈소판제제보호제.
- 제10항 기재한, 수혈용혈소판보호제를 팩 중의 수혈용혈소판제제중에 포함된 것을 특징으로 하는, 수혈용혈소판제제팩.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP92-238624 | 1992-09-07 | ||
| JP23862492 | 1992-09-07 | ||
| JP5203962A JPH06192291A (ja) | 1992-09-07 | 1993-08-18 | 新規ペプチドとそれを用いた血小板凝集抑制剤及び血液凝固抑制剤 |
| JP93-203962 | 1993-08-18 | ||
| PCT/JP1993/001262 WO1994005696A1 (en) | 1992-09-07 | 1993-09-07 | Novel peptide, and antithrombotic agent, anticoagulant for extracorporeal circulation, cell fusion inhibitor, cancer metastasis inhibitor, protective for platelet preparation for transfusion and pack of platelet preparation for transfusion |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR950701645A true KR950701645A (ko) | 1995-04-28 |
Family
ID=26514200
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019940701533A KR950701645A (ko) | 1992-09-07 | 1993-09-07 | 신규펩티드와 그것을 사용한 혈소판응집억제제, 체외순환용혈액 응고억제제, 세포접착저지제, 암전이저지제, 수혈용 혈소판제제보호제 및 수혈용혈소판제제팩 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US5498601A (ko) |
| EP (1) | EP0628571A4 (ko) |
| JP (1) | JPH06192291A (ko) |
| KR (1) | KR950701645A (ko) |
| CA (1) | CA2122912A1 (ko) |
| WO (1) | WO1994005696A1 (ko) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU673466B2 (en) * | 1993-09-30 | 1996-11-07 | Nippon Steel Corporation | Novel peptide, active as inhibitors of platelet aggregation |
| US6231834B1 (en) | 1995-06-07 | 2001-05-15 | Imarx Pharmaceutical Corp. | Methods for ultrasound imaging involving the use of a contrast agent and multiple images and processing of same |
| US6139819A (en) | 1995-06-07 | 2000-10-31 | Imarx Pharmaceutical Corp. | Targeted contrast agents for diagnostic and therapeutic use |
| US6521211B1 (en) | 1995-06-07 | 2003-02-18 | Bristol-Myers Squibb Medical Imaging, Inc. | Methods of imaging and treatment with targeted compositions |
| US5839443A (en) * | 1996-05-16 | 1998-11-24 | The Trustees Of Columbia University In The City Of New York | Method for inhibiting thrombosis in a patient whose blood is subjected to extracorporeal circulation |
| CA2266847A1 (en) * | 1996-09-24 | 1998-04-02 | Rapigene, Inc. | Compositions and methods for enhancing hybridization specificity |
| US6361940B1 (en) | 1996-09-24 | 2002-03-26 | Qiagen Genomics, Inc. | Compositions and methods for enhancing hybridization and priming specificity |
| EP0952228A3 (en) * | 1996-09-24 | 1999-12-15 | Rapigene, Inc. | Compositions and methods for enhancing hybridization specificity |
| US6120751A (en) | 1997-03-21 | 2000-09-19 | Imarx Pharmaceutical Corp. | Charged lipids and uses for the same |
| US6548047B1 (en) | 1997-09-15 | 2003-04-15 | Bristol-Myers Squibb Medical Imaging, Inc. | Thermal preactivation of gaseous precursor filled compositions |
| US6123923A (en) | 1997-12-18 | 2000-09-26 | Imarx Pharmaceutical Corp. | Optoacoustic contrast agents and methods for their use |
| US20050250688A1 (en) * | 1999-04-01 | 2005-11-10 | The Trustees Of Columbia University In The City Of New York | Methods for treating an ischemic disorder and improving stroke outcome |
| AU2003241531A1 (en) * | 2002-05-21 | 2003-12-12 | Emory University | Multivalent polymers with chain-terminating binding groups |
| EP1608681B1 (en) | 2003-03-28 | 2008-06-04 | FUJIFILM Manufacturing Europe B.V. | Rgd-enriched gelatine-like proteins with enhanced cell binding |
| EP2845601B1 (en) * | 2010-11-01 | 2018-04-25 | Industry-Academic Cooperation Foundation, Yonsei University | Composition for use for dissolving thrombi |
| WO2012075407A2 (en) | 2010-12-02 | 2012-06-07 | Becton, Dickinson And Company | Blood collection devices containing blood stabilization agent |
| CN103113456B (zh) * | 2013-03-05 | 2014-07-16 | 中国药科大学 | 具有抗血小板聚集活性的僵蚕多肽及其制备方法和应用 |
| WO2016201374A1 (en) * | 2015-06-11 | 2016-12-15 | University Of Florida Research Foundation, Incorporated | Sulfanide adenosine derivatives and uses thereof |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0275748B1 (fr) * | 1986-12-15 | 1992-08-19 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Nouveaux dérivés peptidiques et leur application notamment en thérapeutique |
| US5061693A (en) * | 1989-07-28 | 1991-10-29 | Merck & Co., Inc. | Fibrinogen receptor antagonists |
-
1993
- 1993-08-18 JP JP5203962A patent/JPH06192291A/ja active Pending
- 1993-09-07 US US08/232,261 patent/US5498601A/en not_active Expired - Fee Related
- 1993-09-07 KR KR1019940701533A patent/KR950701645A/ko not_active Application Discontinuation
- 1993-09-07 WO PCT/JP1993/001262 patent/WO1994005696A1/ja not_active Application Discontinuation
- 1993-09-07 CA CA002122912A patent/CA2122912A1/en not_active Abandoned
- 1993-09-07 EP EP93919619A patent/EP0628571A4/en not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| CA2122912A1 (en) | 1994-03-17 |
| EP0628571A1 (en) | 1994-12-14 |
| WO1994005696A1 (en) | 1994-03-17 |
| US5498601A (en) | 1996-03-12 |
| JPH06192291A (ja) | 1994-07-12 |
| EP0628571A4 (en) | 1998-03-11 |
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