GR3034839T3 - Inhibitors and substrates of thrombin. - Google Patents

Inhibitors and substrates of thrombin.

Info

Publication number
GR3034839T3
GR3034839T3 GR20000402527T GR20000402527T GR3034839T3 GR 3034839 T3 GR3034839 T3 GR 3034839T3 GR 20000402527 T GR20000402527 T GR 20000402527T GR 20000402527 T GR20000402527 T GR 20000402527T GR 3034839 T3 GR3034839 T3 GR 3034839T3
Authority
GR
Greece
Prior art keywords
sub
thrombin
inhibitors
substrates
pro
Prior art date
Application number
GR20000402527T
Other languages
English (en)
Inventor
Vijay Vir Kakkar
John Joseph Deadman
Goran Karl Claeson
Leifeng Cheng
Naoyashi Chino
Said Mohamed Anwar Elgendy
Michael Finbarr Scully
Original Assignee
Thrombosis Res Inst
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Thrombosis Res Inst filed Critical Thrombosis Res Inst
Publication of GR3034839T3 publication Critical patent/GR3034839T3/el

Links

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
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids
    • 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
    • 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
    • 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
    • C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-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
    • C07K5/04—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
    • 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
    • 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
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
GR20000402527T 1990-11-06 2000-11-13 Inhibitors and substrates of thrombin. GR3034839T3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB909024129A GB9024129D0 (en) 1990-11-06 1990-11-06 Inhibitors and substrates of thrombin
PCT/GB1991/001946 WO1992007869A1 (en) 1990-11-06 1991-11-06 Inhibitors and substrates of thrombin

Publications (1)

Publication Number Publication Date
GR3034839T3 true GR3034839T3 (en) 2001-02-28

Family

ID=10684957

Family Applications (1)

Application Number Title Priority Date Filing Date
GR20000402527T GR3034839T3 (en) 1990-11-06 2000-11-13 Inhibitors and substrates of thrombin.

Country Status (14)

Country Link
US (1) US5858979A (el)
EP (3) EP0807638A1 (el)
JP (2) JP3173786B2 (el)
AT (1) ATE195531T1 (el)
AU (1) AU636521B2 (el)
DE (2) DE69132369T4 (el)
DK (1) DK0509080T3 (el)
ES (1) ES2149158T3 (el)
GB (1) GB9024129D0 (el)
GR (1) GR3034839T3 (el)
IE (2) IE913871A1 (el)
NZ (2) NZ264128A (el)
WO (1) WO1992007869A1 (el)
ZA (1) ZA918805B (el)

Families Citing this family (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1993009134A1 (en) * 1991-11-06 1993-05-13 The Scripps Research Institute Phosphonamidate ester-containing pseudopeptides
SE9103612D0 (sv) * 1991-12-04 1991-12-04 Astra Ab New peptide derivatives
US5492895A (en) * 1992-02-14 1996-02-20 Corvas International, Inc. Inhibitors of thrombosis
US6387881B1 (en) * 1992-09-19 2002-05-14 Trigen Ltd Inhibitors and substrates of thrombin
FR2701951B1 (fr) * 1993-02-24 1995-06-09 Adir Nouveaux derives peptidiques de l'acide boronique, leur procede de preparation et les compositions pharmaceutiques qui les contiennent.
AU6448794A (en) * 1993-03-24 1994-10-11 Du Pont Merck Pharmaceutical Company, The Boronic acid and ester inhibitors of thrombin
IL109319A0 (en) * 1993-04-27 1994-07-31 Du Pont Merck Pharma Amidino and guanidino substituted boronic acid compounds
ES2184763T3 (es) * 1993-04-30 2003-04-16 Merck & Co Inc Inhibidores de trombina.
US5783563A (en) * 1993-06-03 1998-07-21 Astra Aktiebolag Method for treatment or prophylaxis of venous thrombosis
US6984627B1 (en) 1993-06-03 2006-01-10 Astrazeneca Ab Peptide derivatives
SE9301916D0 (sv) * 1993-06-03 1993-06-03 Ab Astra New peptides derivatives
GB9318637D0 (en) * 1993-09-08 1993-10-27 Ferring Res Ltd Enzyme inhibitors
IL111175A0 (en) * 1993-10-07 1994-12-29 Du Pont Merck Pharma Electrophilic peptide analogs as inhibitors of trypsin-like serine proteases and pharmaceutical compositions containing them
IL111176A0 (en) * 1993-10-07 1994-12-29 Du Pont Merck Pharma Dipeptide boronic acid inhibitors of trypsin-like enzymes and pharmaceutical compositions containing them
WO1995009859A1 (en) * 1993-10-07 1995-04-13 The Du Pont Merck Pharmaceutical Company Boropeptide inhibitors of thrombin which contain a substituted pyrrolidine ring
US5462964A (en) * 1993-10-20 1995-10-31 The Du Pont Merck Pharmaceutical Company Dipeptide boronic acid inhibitors of trypsin-like enzymes
US6060462A (en) * 1993-10-20 2000-05-09 Dupont Pharmaceuticals Company Electrophilic peptide analogs as inhibitors of trypsin-like enzymes
US5686419A (en) * 1994-01-21 1997-11-11 Georgia Tech Research Corp. Basic α-aminoalkylphosphonate derivatives
US5693617A (en) * 1994-03-15 1997-12-02 Proscript, Inc. Inhibitors of the 26s proteolytic complex and the 20s proteasome contained therein
US5561146A (en) * 1994-06-10 1996-10-01 Bristol-Myers Squibb Company Modified guanidino and amidino thrombin inhibitors
FR2721611B1 (fr) * 1994-06-22 1996-09-27 Adir Nouveaux dérivés peptidiques de l'acide boronique, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent .
US5510369A (en) * 1994-07-22 1996-04-23 Merck & Co., Inc. Pyrrolidine thrombin inhibitors
US6083903A (en) 1994-10-28 2000-07-04 Leukosite, Inc. Boronic ester and acid compounds, synthesis and uses
SE9404196D0 (sv) * 1994-12-02 1994-12-02 Astra Ab New antithrombotic formulation
GB9502985D0 (en) * 1995-02-16 1995-04-05 Thrombosis Res Inst Enzyme inhibitors
WO1996025426A1 (de) * 1995-02-17 1996-08-22 Basf Aktiengesellschaft Neue dipeptidische amidine als thrombin-inhibitoren
US5629324A (en) * 1995-04-10 1997-05-13 Merck & Co., Inc. Thrombin inhibitors
AR005245A1 (es) * 1995-12-21 1999-04-28 Astrazeneca Ab Prodrogas de inhibidores de trombina, una formulación farmaceutica que las comprende, el uso de dichas prodrogas para la manufactura de un medicamento y un procedimiento para su preparacion
DE69738619T2 (de) 1996-07-23 2009-05-20 Canon K.K. Verfahren und Vorrichtung zur Kamerakontrolle
US6004955A (en) * 1996-08-15 1999-12-21 Dupont Pharmaceuticals Company Cyclic carbamates and isoxazolidines as IIb/IIIa antagonists
US5798377A (en) * 1996-10-21 1998-08-25 Merck & Co., Inc. Thrombin inhibitors
CN1289341A (zh) 1998-01-26 2001-03-28 Basf公司 凝血酶抑制剂
AU3213799A (en) 1998-04-01 1999-10-18 Du Pont Pharmaceuticals Company Integrin antagonists
CA2320730A1 (en) 1998-12-23 2000-07-06 Renhua Li Thrombin or factor xa inhibitors
AU3192500A (en) * 1999-03-16 2000-10-04 C & C Research Laboratories Substituted proline derivatives and medicinal compositions containing the same
US6258932B1 (en) * 1999-08-09 2001-07-10 Tripep Ab Peptides that block viral infectivity and methods of use thereof
CA2378480A1 (en) * 1999-08-09 2001-02-15 Tripep Ab Pharmaceutical compositions containing tripeptides
CA2431588A1 (en) 2000-12-18 2002-06-27 Merck & Co., Inc. Benzylamine derivatives and their use as thrombin inhibitors
US6528503B2 (en) 2000-12-18 2003-03-04 Merck & Co., Inc. Thrombin inhibitors
US7144899B2 (en) 2001-02-09 2006-12-05 Merck & Co., Inc. Thrombin inhibitors
US6593455B2 (en) * 2001-08-24 2003-07-15 Tripep Ab Tripeptide amides that block viral infectivity and methods of use thereof
US6455670B1 (en) * 2001-09-06 2002-09-24 Tripep Ab Pentamer peptide amide, ALGPG-NH2, that inhibits viral infectivity and methods of use thereof
EP1436317A1 (en) * 2001-09-19 2004-07-14 Tripep Ab Molecules that block viral infectivity and methods of use thereof
US7084134B2 (en) 2002-05-02 2006-08-01 Merk & Co., Inc. Thrombin inhibitors
EP1396269A1 (en) * 2002-09-09 2004-03-10 Trigen Limited Boronic acid salts of multivalent metals used in the preparation of a medicament for treating thrombosis
US7112572B2 (en) 2002-09-09 2006-09-26 Trigen Limited Multivalent metal salts of boronic acids
WO2004073703A1 (en) * 2003-02-21 2004-09-02 Tripep Ab Glycinamide derivative for inhibiting hiv replication
US20050096319A1 (en) * 2003-02-21 2005-05-05 Balzarini Jan M.R. Identification of compounds that inhibit replication of human immunodeficiency virus
GB0405267D0 (en) * 2004-03-09 2004-04-21 Trigen Ltd Compounds
EP1724253A3 (en) * 2005-05-10 2009-11-04 Ajinomoto Co., Inc. Production method of optically active diphenylalanine compounds
EP2117605B1 (en) * 2007-02-28 2012-09-26 Sanofi Imaging probes
JP2015525222A (ja) 2012-06-08 2015-09-03 バイオジェン・エムエイ・インコーポレイテッドＢｉｏｇｅｎ ＭＡ Ｉｎｃ． キメラ性凝固因子
JP2015521589A (ja) 2012-06-08 2015-07-30 バイオジェン・エムエイ・インコーポレイテッドＢｉｏｇｅｎ ＭＡ Ｉｎｃ． プロコアグラント化合物
JP7164521B2 (ja) 2016-06-21 2022-11-01 オリオン・オフサルモロジー・エルエルシー 炭素環式プロリンアミド誘導体
DK3472149T3 (da) 2016-06-21 2023-11-27 Orion Ophthalmology LLC Heterocykliske prolinamidderivater
DE102016009766A1 (de) 2016-08-11 2018-02-15 Julius-Maximilians-Universität Würzburg Herstellung von Bitterstoffderivaten
IL309732A (en) 2021-07-09 2024-02-01 Aligos Therapeutics Inc Antiviral compounds

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4428874A (en) * 1981-03-25 1984-01-31 Pentapharm A.G. Tripeptide derivatives
JPS5856695A (ja) * 1981-09-28 1983-04-04 Nitto Boseki Co Ltd 新規なトロンビン測定用基質
US4499082A (en) * 1983-12-05 1985-02-12 E. I. Du Pont De Nemours And Company α-Aminoboronic acid peptides
DE3606480A1 (de) * 1986-02-28 1987-09-03 Behringwerke Ag Oligopeptidylnitrilderivate, diese enthaltende mittel, verfahren zu ihrer herstellung und ihre verwendung
US5187157A (en) * 1987-06-05 1993-02-16 Du Pont Merck Pharmaceutical Company Peptide boronic acid inhibitors of trypsin-like proteases
US4929602A (en) * 1987-11-25 1990-05-29 Scripps Clinic And Research Foundation Method of inhibiting platelet dependent arterial thrombosis
US5023236A (en) * 1988-04-07 1991-06-11 Corvas, Inc. Factor VII/VIIA active site inhibitors
US5288707A (en) * 1990-08-13 1994-02-22 Sandoz Ltd. Borolysine peptidomimetics

Also Published As

Publication number Publication date
ES2149158T3 (es) 2000-11-01
AU8900791A (en) 1992-05-26
NZ240477A (en) 1994-10-26
EP0509080A1 (en) 1992-10-21
WO1992007869A1 (en) 1992-05-14
DE69132369D1 (en) 2000-09-21
AU636521B2 (en) 1993-04-29
IE913871A1 (en) 1992-05-22
DE69132369T2 (de) 2001-02-22
EP0807638A1 (en) 1997-11-19
EP0955309A1 (en) 1999-11-10
DK0509080T3 (da) 2000-09-18
DE69132369T4 (de) 2001-09-13
NZ264128A (en) 1996-11-26
US5858979A (en) 1999-01-12
JPH05504775A (ja) 1993-07-22
ATE195531T1 (de) 2000-09-15
ZA918805B (en) 1993-04-28
GB9024129D0 (en) 1990-12-19
IE20000539A1 (en) 2002-03-20
JP3453357B2 (ja) 2003-10-06
JP3173786B2 (ja) 2001-06-04
JP2001226397A (ja) 2001-08-21
EP0509080B1 (en) 2000-08-16

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Legal Events

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