ZA918805B - Inhibitors and substrates of thrombin - Google Patents

Inhibitors and substrates of thrombin

Info

Publication number
ZA918805B
ZA918805B ZA918805A ZA918805A ZA918805B ZA 918805 B ZA918805 B ZA 918805B ZA 918805 A ZA918805 A ZA 918805A ZA 918805 A ZA918805 A ZA 918805A ZA 918805 B ZA918805 B ZA 918805B
Authority
ZA
South Africa
Prior art keywords
sub
thrombin
inhibitors
substrates
pro
Prior art date
Application number
ZA918805A
Other languages
English (en)
Inventor
Vijay Vir Kakkar
Vir Kakkar Vijay
John Joseph Deadman
Joseph Deadman John
Goran Karl Claeson
Karl Claeson Goran
Leifeng Cheng
Cheng Leifeng
Naoyashi Chino
Chino Naoyashi
Said Mohamed Anwar Elgendy
Mohamed Anwar Elgendy Said
Michael Finbarr Scully
Finbarr Scully Michael
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 ZA918805B publication Critical patent/ZA918805B/xx

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)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Diabetes (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)
ZA918805A 1990-11-06 1991-11-06 Inhibitors and substrates of thrombin ZA918805B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GB909024129A GB9024129D0 (en) 1990-11-06 1990-11-06 Inhibitors and substrates of thrombin

Publications (1)

Publication Number Publication Date
ZA918805B true ZA918805B (en) 1993-04-28

Family

ID=10684957

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA918805A ZA918805B (en) 1990-11-06 1991-11-06 Inhibitors and substrates of thrombin

Country Status (14)

Country Link
US (1) US5858979A (el)
EP (3) EP0509080B1 (el)
JP (2) JP3173786B2 (el)
AT (1) ATE195531T1 (el)
AU (1) AU636521B2 (el)
DE (2) DE69132369D1 (el)
DK (1) DK0509080T3 (el)
ES (1) ES2149158T3 (el)
GB (1) GB9024129D0 (el)
GR (1) GR3034839T3 (el)
IE (2) IE20000539A1 (el)
NZ (2) NZ240477A (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
AU3136693A (en) * 1991-11-06 1993-06-07 Scripps Research Institute, The Phosphonamidate ester-containing pseudopeptides
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 (en) * 1993-02-12 2002-11-19 George Phillip Vlasuk Inhibitors of thrombosis
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.
WO1994021650A1 (en) * 1993-03-24 1994-09-29 The Du Pont Merck Pharmaceutical Company 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
US5783563A (en) * 1993-06-03 1998-07-21 Astra Aktiebolag Method for treatment or prophylaxis of venous thrombosis
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
WO1995009859A1 (en) * 1993-10-07 1995-04-13 The Du Pont Merck Pharmaceutical Company Boropeptide inhibitors of thrombin which contain a substituted pyrrolidine ring
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
US5462964A (en) * 1993-10-20 1995-10-31 The Du Pont Merck Pharmaceutical Company Dipeptide boronic acid inhibitors of trypsin-like enzymes
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
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
JPH11500120A (ja) * 1995-02-17 1999-01-06 ビーエーエスエフ アクチェンゲゼルシャフト 新規なトロンビンインヒビター
US5629324A (en) * 1995-04-10 1997-05-13 Merck & Co., Inc. Thrombin inhibitors
TWI238827B (en) 1995-12-21 2005-09-01 Astrazeneca Ab Prodrugs of thrombin inhibitors
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
WO1999037668A1 (de) 1998-01-26 1999-07-29 Basf Aktiengesellschaft Thrombininhibitoren
CA2333927A1 (en) 1998-04-01 1999-10-07 Dupont Pharmaceuticals Company Pyrimidines and triazines as integrin antagonists
AU3127900A (en) 1998-12-23 2000-07-31 Du Pont Pharmaceuticals Company Thrombin or factor xa inhibitors
WO2000055188A1 (fr) * 1999-03-16 2000-09-21 C & C Research Laboratories Derives de proline substitues et compositions medicinales les contenant
AU5701300A (en) * 1999-08-09 2001-03-05 Tripep Ab Protein polymerization inhibitors and methods of use
US6258932B1 (en) * 1999-08-09 2001-07-10 Tripep Ab Peptides that block viral infectivity and methods of use thereof
JP2004516286A (ja) 2000-12-18 2004-06-03 メルク エンド カムパニー インコーポレーテッド ベンジルアミン誘導体およびそれのトロンビン阻害薬としての使用
US6528503B2 (en) 2000-12-18 2003-03-04 Merck & Co., Inc. Thrombin inhibitors
CA2436176A1 (en) 2001-02-09 2002-08-22 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
EP1466916B1 (en) 2002-09-09 2007-10-24 Trigen Limited Peptide boronic acids useful in making salts thereof
US7112572B2 (en) 2002-09-09 2006-09-26 Trigen Limited Multivalent metal salts of boronic acids
CA2515679A1 (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
BRPI0808046A2 (pt) 2007-02-28 2014-07-08 Sanofi Aventis Sondas de imageamento
WO2013185114A2 (en) 2012-06-08 2013-12-12 Biogen Idec Ma Inc. Chimeric clotting factors
EP4079316A1 (en) 2012-06-08 2022-10-26 Bioverativ Therapeutics Inc. Procoagulant compounds
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
CN114685453A (zh) 2016-06-21 2022-07-01 奥瑞恩眼科有限责任公司 杂环脯氨酰胺衍生物
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
AU8900791A (en) 1992-05-26
WO1992007869A1 (en) 1992-05-14
GB9024129D0 (en) 1990-12-19
JPH05504775A (ja) 1993-07-22
EP0807638A1 (en) 1997-11-19
EP0509080B1 (en) 2000-08-16
DE69132369T4 (de) 2001-09-13
DK0509080T3 (da) 2000-09-18
JP3173786B2 (ja) 2001-06-04
GR3034839T3 (en) 2001-02-28
NZ264128A (en) 1996-11-26
ATE195531T1 (de) 2000-09-15
AU636521B2 (en) 1993-04-29
DE69132369T2 (de) 2001-02-22
IE913871A1 (en) 1992-05-22
IE20000539A1 (en) 2002-03-20
NZ240477A (en) 1994-10-26
US5858979A (en) 1999-01-12
DE69132369D1 (en) 2000-09-21
JP2001226397A (ja) 2001-08-21
ES2149158T3 (es) 2000-11-01
JP3453357B2 (ja) 2003-10-06
EP0955309A1 (en) 1999-11-10
EP0509080A1 (en) 1992-10-21

Similar Documents

Publication Publication Date Title
ZA918805B (en) Inhibitors and substrates of thrombin
AU645347B2 (en) Tripeptide antithrombotic agents
CA2136622A1 (fr) Composes biologiquement actifs de type phosphotriesters
EP0181110A3 (en) Histidine derivatives as renin inhibitors
AU4799793A (en) Beta -aminoalkyl and beta -n-peptidylaminoalkyl boronic acids
ATE90107T1 (de) Peptide mit collagenase hemmender wirkung.
BG102691A (en) New erythromycin derivatives, method for their preparation and application as medicamentous form
HU9201215D0 (en) Process for the production of geminal diphosphonic acids and of medical preparations containing them
ATE130312T1 (de) Polypeptid mit sich wiederholenden zelladhäsiven hauptsequenzen.
IL119297A (en) 2,3-Dihydroxypropyl-2-(1-oxoalkyl) amino-2-deoxyglucopyranosides a process for their preparation and compositions containing them
EP0173510A3 (en) Tripeptide derivatives for use as anti-hypertensive agents
IE811601L (en) Pentapeptides
ES8505948A1 (es) Un derivado de amida.
ES467259A1 (es) Procedimiento para la obtencion de arilhexafuranosidos.
EP0292923A3 (en) Piperidine compounds and pharmaceutical uses thereof
ZA869058B (en) Orally active phosphonyl hydroxyacyl prolines and processes for preparing phosphonyl hydroxyacyl prolines
ES480969A1 (es) Procedimiento para la aclaracion optica de materiales organicos, en especial de tipo textil.
EP0107907A3 (en) Improvements in or relating to immunomodulating agents
FI941635A0 (fi) Androst-4-eno(4,5-b)pyrrolijohdannaiset ja menetelmä niiden valmistamiseksi
MY111431A (en) Tripeptide antithrombotic agents
JPS5785349A (en) Tripeptide alkylamide derivative
CA2019005A1 (en) Antiherpes pentapeptide derivatives having a cycloalkyl substituted aspartic acid side chain
ES445895A1 (es) Procedimiento para la produccion de nuevos peptidos.
KR870001226A (ko) 바이사이클 화합물의 제조방법
JPS56161397A (en) Substituted alanylaminoethylphosphonic acid