ZA918805B - Inhibitors and substrates of thrombin - Google Patents
Inhibitors and substrates of thrombinInfo
- 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
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)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (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)
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 (xx) |
EP (3) | EP0509080B1 (xx) |
JP (2) | JP3173786B2 (xx) |
AT (1) | ATE195531T1 (xx) |
AU (1) | AU636521B2 (xx) |
DE (2) | DE69132369T4 (xx) |
DK (1) | DK0509080T3 (xx) |
ES (1) | ES2149158T3 (xx) |
GB (1) | GB9024129D0 (xx) |
GR (1) | GR3034839T3 (xx) |
IE (2) | IE913871A1 (xx) |
NZ (2) | NZ240477A (xx) |
WO (1) | WO1992007869A1 (xx) |
ZA (1) | ZA918805B (xx) |
Families Citing this family (58)
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 |
US6387881B1 (en) * | 1992-09-19 | 2002-05-14 | Trigen Ltd | Inhibitors and substrates of thrombin |
DE69419141D1 (de) * | 1993-02-12 | 1999-07-22 | Corvas Int Inc | Inhibitoren gegen 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 |
EP0699074B1 (en) * | 1993-04-30 | 2002-11-13 | Merck & Co. Inc. | Thrombin inhibitors |
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 |
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 |
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 |
WO1995009859A1 (en) * | 1993-10-07 | 1995-04-13 | The Du Pont Merck Pharmaceutical Company | Boropeptide inhibitors of thrombin which contain a substituted pyrrolidine ring |
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 |
SK104697A3 (en) * | 1995-02-17 | 1998-11-04 | Basf Ag | Novel dipeptide amidines as thrombin inhibitors |
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 |
HUP0100082A3 (en) | 1998-01-26 | 2001-12-28 | Abbott Gmbh & Co Kg | Thrombin inhibitor, peptide derivatives, pharmaceutical compositions comprising thereof and their use |
JP2003504301A (ja) | 1998-04-01 | 2003-02-04 | ブリストル−マイヤーズ スクイブ ファーマ カンパニー | インテグリンアンタゴニスト |
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 |
EP1207897A2 (en) * | 1999-08-09 | 2002-05-29 | Tripep Ab | Pharmaceutical compositions containing tripeptides |
US6258932B1 (en) * | 1999-08-09 | 2001-07-10 | Tripep Ab | Peptides that block viral infectivity and methods of use thereof |
US6528503B2 (en) | 2000-12-18 | 2003-03-04 | Merck & Co., Inc. | Thrombin inhibitors |
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 |
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 |
MXPA05002661A (es) | 2002-09-09 | 2005-08-19 | Trigen Ltd | Sales de acido boronico y su uso en el tratamiento de trombosis. |
US7112572B2 (en) | 2002-09-09 | 2006-09-26 | Trigen Limited | Multivalent metal salts of boronic acids |
US20050096319A1 (en) * | 2003-02-21 | 2005-05-05 | Balzarini Jan M.R. | Identification of compounds that inhibit replication of human immunodeficiency virus |
WO2004073703A1 (en) * | 2003-02-21 | 2004-09-02 | Tripep Ab | Glycinamide derivative for inhibiting hiv replication |
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 |
CA2678717A1 (en) * | 2007-02-28 | 2008-09-04 | Sanofi-Aventis | Imaging probes |
EP4079316A1 (en) | 2012-06-08 | 2022-10-26 | Bioverativ Therapeutics Inc. | Procoagulant compounds |
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 |
EP4257191A3 (en) | 2016-06-21 | 2023-11-22 | Orion Ophthalmology LLC | Heterocyclic prolinamide derivatives |
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 |
DE102016009766A1 (de) | 2016-08-11 | 2018-02-15 | Julius-Maximilians-Universität Würzburg | Herstellung von Bitterstoffderivaten |
WO2023283256A1 (en) | 2021-07-09 | 2023-01-12 | Aligos Therapeutics, Inc. | Anti-viral compounds |
WO2023043816A1 (en) | 2021-09-17 | 2023-03-23 | Aligos Therapeutics, Inc. | Anti-viral compounds for treating coronavirus, picornavirus, and norovirus infections |
Family Cites Families (8)
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 |
-
1990
- 1990-11-06 GB GB909024129A patent/GB9024129D0/en active Pending
-
1991
- 1991-11-05 NZ NZ240477A patent/NZ240477A/en not_active IP Right Cessation
- 1991-11-05 NZ NZ264128A patent/NZ264128A/en not_active IP Right Cessation
- 1991-11-06 IE IE387191A patent/IE913871A1/en not_active IP Right Cessation
- 1991-11-06 AU AU89007/91A patent/AU636521B2/en not_active Ceased
- 1991-11-06 DE DE69132369T patent/DE69132369T4/de not_active Expired - Lifetime
- 1991-11-06 IE IE20000539A patent/IE20000539A1/en not_active IP Right Cessation
- 1991-11-06 DE DE69132369A patent/DE69132369D1/de not_active Expired - Fee Related
- 1991-11-06 EP EP91919539A patent/EP0509080B1/en not_active Expired - Lifetime
- 1991-11-06 WO PCT/GB1991/001946 patent/WO1992007869A1/en active IP Right Grant
- 1991-11-06 ZA ZA918805A patent/ZA918805B/xx unknown
- 1991-11-06 ES ES91919539T patent/ES2149158T3/es not_active Expired - Lifetime
- 1991-11-06 JP JP51818591A patent/JP3173786B2/ja not_active Expired - Fee Related
- 1991-11-06 EP EP99200841A patent/EP0955309A1/en not_active Withdrawn
- 1991-11-06 EP EP97201436A patent/EP0807638A1/en not_active Withdrawn
- 1991-11-06 AT AT91919539T patent/ATE195531T1/de not_active IP Right Cessation
- 1991-11-06 DK DK91919539T patent/DK0509080T3/da active
-
1995
- 1995-06-02 US US08/459,394 patent/US5858979A/en not_active Expired - Fee Related
-
2000
- 2000-11-13 GR GR20000402527T patent/GR3034839T3/el not_active IP Right Cessation
- 2000-12-27 JP JP2000398079A patent/JP3453357B2/ja not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
EP0509080A1 (en) | 1992-10-21 |
EP0955309A1 (en) | 1999-11-10 |
IE20000539A1 (en) | 2002-03-20 |
DE69132369D1 (en) | 2000-09-21 |
DK0509080T3 (da) | 2000-09-18 |
ATE195531T1 (de) | 2000-09-15 |
NZ240477A (en) | 1994-10-26 |
AU8900791A (en) | 1992-05-26 |
JPH05504775A (ja) | 1993-07-22 |
IE913871A1 (en) | 1992-05-22 |
US5858979A (en) | 1999-01-12 |
EP0807638A1 (en) | 1997-11-19 |
GR3034839T3 (en) | 2001-02-28 |
WO1992007869A1 (en) | 1992-05-14 |
JP3173786B2 (ja) | 2001-06-04 |
AU636521B2 (en) | 1993-04-29 |
JP3453357B2 (ja) | 2003-10-06 |
DE69132369T2 (de) | 2001-02-22 |
NZ264128A (en) | 1996-11-26 |
GB9024129D0 (en) | 1990-12-19 |
JP2001226397A (ja) | 2001-08-21 |
DE69132369T4 (de) | 2001-09-13 |
EP0509080B1 (en) | 2000-08-16 |
ES2149158T3 (es) | 2000-11-01 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
GR3034839T3 (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 | |
GR3000524T3 (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. | |
EP0314239A3 (en) | Tripeptide renin inhibitors with n-terminal ureido or sulfamido groups | |
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 | |
KR870001226A (ko) | 바이사이클 화합물의 제조방법 | |
JPS5738769A (en) | Azetidinone derivative and its preparation |