[go: up one dir, main page]

DK0509080T3 - Thrombininhibitorer og -substrater - Google Patents

Thrombininhibitorer og -substrater

Info

Publication number
DK0509080T3
DK0509080T3 DK91919539T DK91919539T DK0509080T3 DK 0509080 T3 DK0509080 T3 DK 0509080T3 DK 91919539 T DK91919539 T DK 91919539T DK 91919539 T DK91919539 T DK 91919539T DK 0509080 T3 DK0509080 T3 DK 0509080T3
Authority
DK
Denmark
Prior art keywords
sub
substrates
pro
thrombin inhibitors
certain
Prior art date
Application number
DK91919539T
Other languages
Danish (da)
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
Trigen Ltd
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 Trigen Ltd filed Critical Trigen Ltd
Application granted granted Critical
Publication of DK0509080T3 publication Critical patent/DK0509080T3/da

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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (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)
DK91919539T 1990-11-06 1991-11-06 Thrombininhibitorer og -substrater DK0509080T3 (da)

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 (fr) 1990-11-06 1991-11-06 Inhibiteurs et substrats de thrombine

Publications (1)

Publication Number Publication Date
DK0509080T3 true DK0509080T3 (da) 2000-09-18

Family

ID=10684957

Family Applications (1)

Application Number Title Priority Date Filing Date
DK91919539T DK0509080T3 (da) 1990-11-06 1991-11-06 Thrombininhibitorer og -substrater

Country Status (14)

Country Link
US (1) US5858979A (fr)
EP (3) EP0807638A1 (fr)
JP (2) JP3173786B2 (fr)
AT (1) ATE195531T1 (fr)
AU (1) AU636521B2 (fr)
DE (2) DE69132369D1 (fr)
DK (1) DK0509080T3 (fr)
ES (1) ES2149158T3 (fr)
GB (1) GB9024129D0 (fr)
GR (1) GR3034839T3 (fr)
IE (2) IE913871A1 (fr)
NZ (2) NZ240477A (fr)
WO (1) WO1992007869A1 (fr)
ZA (1) ZA918805B (fr)

Families Citing this family (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1993009134A1 (fr) * 1991-11-06 1993-05-13 The Scripps Research Institute Pseudopeptides contenant des esters de phosphonamidate
SE9103612D0 (sv) * 1991-12-04 1991-12-04 Astra Ab New peptide derivatives
US6387881B1 (en) * 1992-09-19 2002-05-14 Trigen Ltd Inhibitors and substrates of thrombin
CA2155931C (fr) * 1993-02-12 2002-11-19 George Phillip Vlasuk Inhibiteurs de la thrombose
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
DE69431718T2 (de) * 1993-04-30 2003-07-10 Merck & Co., Inc. Thrombin-inhibitoren
US6984627B1 (en) 1993-06-03 2006-01-10 Astrazeneca Ab Peptide derivatives
US5780631A (en) * 1993-06-03 1998-07-14 Astra Aktiebolag Starting materials in the synthesis of thrombin and kininogenase inhibitors
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
US5462964A (en) * 1993-10-20 1995-10-31 The Du Pont Merck Pharmaceutical Company Dipeptide boronic acid inhibitors of trypsin-like enzymes
WO1995009859A1 (fr) * 1993-10-07 1995-04-13 The Du Pont Merck Pharmaceutical Company Inhibiteurs boropeptidiques de la thrombine contenant un noyau de pyrrolidine substitue
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 (fr) * 1995-02-17 1996-08-22 Basf Aktiengesellschaft Nouvelles amidines dipeptidiques utilisees comme inhibiteurs de thrombine
US5629324A (en) * 1995-04-10 1997-05-13 Merck & Co., Inc. Thrombin inhibitors
TW541316B (en) 1995-12-21 2003-07-11 Astrazeneca Ab Prodrugs of thrombin inhibitors
EP1890483A3 (fr) 1996-07-23 2011-07-06 Canon Kabushiki Kaisha Dispositif et méthode de commande de caméra
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
AU751111B2 (en) 1998-01-26 2002-08-08 Basf Aktiengesellschaft Thrombin inhibitors
AU3213799A (en) 1998-04-01 1999-10-18 Du Pont Pharmaceuticals Company Integrin antagonists
AU3127900A (en) 1998-12-23 2000-07-31 Du Pont Pharmaceuticals Company Thrombin or factor xa inhibitors
KR20020004971A (ko) * 1999-03-16 2002-01-16 이경하 치환 프로린 유도체 및 이들을 함유하고 있는 의약 조성물
WO2001010457A2 (fr) * 1999-08-09 2001-02-15 Tripep Ab Inhibiteurs de polymerisation de proteines et leur procede d'utilisation
US6258932B1 (en) * 1999-08-09 2001-07-10 Tripep Ab Peptides that block viral infectivity and methods of use thereof
WO2002050056A1 (fr) 2000-12-18 2002-06-27 Merck & Co., Inc. Derives de benzylamine et leur utilisation comme inhibiteurs de thrombine
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
WO2003024995A1 (fr) * 2001-09-19 2003-03-27 Tripep Ab Molecules bloquant l'infectivite virale et methodes d'utilisation associees
US7084134B2 (en) 2002-05-02 2006-08-01 Merk & Co., Inc. Thrombin inhibitors
US7371729B2 (en) 2002-09-09 2008-05-13 Trigen Limited Boronic acid salts useful in parenteral formulations
ATE376551T1 (de) 2002-09-09 2007-11-15 Trigen Ltd Peptidborsäuren und deren verwendung in der herstellung von salzen derselben
US20050096319A1 (en) * 2003-02-21 2005-05-05 Balzarini Jan M.R. Identification of compounds that inhibit replication of human immunodeficiency virus
US20040180893A1 (en) * 2003-02-21 2004-09-16 Balzarini Jan Maria Rene Identification of compounds that inhibit replication of human immunodeficiency virus
GB0405267D0 (en) * 2004-03-09 2004-04-21 Trigen Ltd Compounds
EP1724253A3 (fr) * 2005-05-10 2009-11-04 Ajinomoto Co., Inc. Procédé de production de diphénylalanines optiquement actives
AU2008221036B2 (en) 2007-02-28 2014-03-20 Sanofi Imaging probes
EP2858659B1 (fr) 2012-06-08 2019-12-25 Bioverativ Therapeutics Inc. Composés pro-coagulants
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
PT3472149T (pt) 2016-06-21 2023-11-23 Orion Opthalmology Llc Derivados de prolinamida heterocíclicos
WO2017222914A1 (fr) 2016-06-21 2017-12-28 Inception 4, Inc. Dérivés de prolinamide carbocycliques
DE102016009766A1 (de) 2016-08-11 2018-02-15 Julius-Maximilians-Universität Würzburg Herstellung von Bitterstoffderivaten
CA3224494A1 (fr) 2021-07-09 2023-01-12 Koen Vandyck Composes anti-viraux
WO2023043816A1 (fr) 2021-09-17 2023-03-23 Aligos Therapeutics, Inc. Composés antiviraux pour le traitement d'infections à coronavirus, picornavirus et norovirus

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
EP0509080B1 (fr) 2000-08-16
EP0807638A1 (fr) 1997-11-19
AU636521B2 (en) 1993-04-29
GR3034839T3 (en) 2001-02-28
EP0509080A1 (fr) 1992-10-21
JP3173786B2 (ja) 2001-06-04
US5858979A (en) 1999-01-12
JP3453357B2 (ja) 2003-10-06
GB9024129D0 (en) 1990-12-19
NZ240477A (en) 1994-10-26
NZ264128A (en) 1996-11-26
JPH05504775A (ja) 1993-07-22
ZA918805B (en) 1993-04-28
IE913871A1 (en) 1992-05-22
DE69132369T4 (de) 2001-09-13
ES2149158T3 (es) 2000-11-01
ATE195531T1 (de) 2000-09-15
DE69132369D1 (en) 2000-09-21
IE20000539A1 (en) 2002-03-20
EP0955309A1 (fr) 1999-11-10
JP2001226397A (ja) 2001-08-21
DE69132369T2 (de) 2001-02-22
WO1992007869A1 (fr) 1992-05-14
AU8900791A (en) 1992-05-26

Similar Documents

Publication Publication Date Title
DK0509080T3 (da) Thrombininhibitorer og -substrater
BR9104181A (pt) Composto
ES2065880T3 (es) Proteina quimicamente modificada y obtencion de la misma.
CA2136622A1 (fr) Composes biologiquement actifs de type phosphotriesters
EP0181110A3 (fr) Dérivés d'histidine comme inhibiteurs de la rénine
ATE90107T1 (de) Peptide mit collagenase hemmender wirkung.
IT1241674B (it) Acidi gem-difosfonici, un processo per la loro preparazione e composizioni farmaceutiche che li contengono.
KR840005733A (ko) 무라밀 펩타이드의 제조방법
BG92842A (bg) Метод за получаване на бета-карбонил-карбоксиамиди на 1,3-тиазолидини
Shiozaki et al. SYNTHESIS OF 3-HYDROXYETHYL-4-OXOAZETIDIN-2-YLPHOSPHONATE DERIVATIVES
DK2887A (da) Phosphonyl-hydroxyacyl-proliner
ES467259A1 (es) Procedimiento para la obtencion de arilhexafuranosidos.
ES480969A1 (es) Procedimiento para la aclaracion optica de materiales organicos, en especial de tipo textil.
FI941635A0 (fi) Androst-4-eno(4,5-b)pyrrolijohdannaiset ja menetelmä niiden valmistamiseksi
EP0107907A3 (fr) Agents d'immunomodulation
MY111431A (en) Tripeptide antithrombotic agents
JPS5785349A (en) Tripeptide alkylamide derivative