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ES2149170T3 - Inhibidores mejorados de trombina. - Google Patents

Inhibidores mejorados de trombina.

Info

Publication number
ES2149170T3
ES2149170T3 ES92905748T ES92905748T ES2149170T3 ES 2149170 T3 ES2149170 T3 ES 2149170T3 ES 92905748 T ES92905748 T ES 92905748T ES 92905748 T ES92905748 T ES 92905748T ES 2149170 T3 ES2149170 T3 ES 2149170T3
Authority
ES
Spain
Prior art keywords
atoms
link
group
chain consisting
amino
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES92905748T
Other languages
English (en)
Inventor
John M Maraganore
Jo-Ann M Jablonski
Paul R Bourdon
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Biogen Inc
Original Assignee
Biogen Inc
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 Biogen Inc filed Critical Biogen Inc
Application granted granted Critical
Publication of ES2149170T3 publication Critical patent/ES2149170T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

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
    • C07K7/02—Linear peptides containing at least one abnormal peptide link
    • 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
    • C07K14/81—Protease inhibitors
    • C07K14/815—Protease inhibitors from leeches, e.g. hirudin, eglin
    • 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
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1016—Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Materials For Medical Uses (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pyrane Compounds (AREA)
  • Lighting Device Outwards From Vehicle And Optical Signal (AREA)
  • Manipulator (AREA)

Abstract

LA INVENCION SE REFIERE A NUEVAS MOLECULAS BIOLOGICAMENTE ACTIVAS QUE SE UNEN E INHIBEN LA TROMBINA. ESTAS MOLECULAS COMPRENDEN UNA MITAD DIRIGIDA DE ZONA CATALITICA (CSDM) DE LA FORMULA (I), EN DONDE X ES HIDROGENO O SE CARACTERIZA DE UNA CADENA DE RESPALDO QUE CONSTA DE ENTRE 1 Y 100 ATOMOS, R1 SE SELECCIONA ENTRE EL GRUPO QUE CONSTA DE ESTRUCTURAS DE ANILLO SATURADAS MONO, DI O TRISUBSTITUIDAS O INSUBSTITUIDAS; R2 ES UN ENLACE O SE CARACTERIZA POR UNA CADENA DE RESPALDO QUE CONSTA DE ENTRE 1 Y 5 ATOMOS; R3 ES UN ENLACE O SE CARACTERIZA POR UNA CADENA DE RESPALDO QUE CONSTA DE ENTRE 1 Y 3 ATOMOS; R4 ES CUALQUIER ACIDO AMINO; R5 ES CUALQUIER ACIDO L-AMINO QUE COMPRENDA UN GRUPO DE CADENA LATERAL QUE CONTENGA GUANIDINIUM O AMINO; R6 ES UN ENLACE NO AMIDO; E Y SE CARACTERIZA POR UNA CADENA DE RESPALDO QUE CONSTA DE ENTRE 1 Y 9 ATOMOS; O LA FORMULA (II), EN LA QUE R1'' SE SELECCIONA ENTRE EL GRUPO QUE CONSTA DE ESTRUCTURAS DE ANILLO MONO, DI O TRISUBSTITUIDAS O INSUBSTITUIDAS; R4'' ES CUALQUIERACIDO AMINO QUE COMPRENDA UN GRUPO DE CADENA LATERAL QUE SE CARACTERIZA POR LA CAPACIDAD DE ACEPTAR UN ENLACE DE HIDROGENO A UN PH DE ENTRE 5.5 Y 9.5; Y X, R2, R3, R5, R6 E Y SON COMO SE DEFINIERON ANTERIORMENTE. LOS INHIBIDORES DE LA TROMBINA MAS ADECUADOS SE CARACTERIZAN ADEMAS POR UNA ZONA DE ENLACE ASOCIATIVO EXOGENA QUE SE UNE A UN ANION (ABEAM) Y UNA PARTE ENLAZADORA DE ENTRE 18A Y 42A DE LONGITUD QUE CONECTA LA Y CON EL ABEAM. ESTA INVENCION TAMBIEN SE REFIERE A COMPUESTOS, COMBINACIONES Y METODOS QUE EMPLEAN ESTAS MOLECULAS PARA PROPOSITOS TERAPEUTICOS, PROFILACTICOS Y DIAGNOSTICOS.
ES92905748T 1991-02-08 1992-02-03 Inhibidores mejorados de trombina. Expired - Lifetime ES2149170T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US07/652,929 US5240913A (en) 1989-08-18 1991-02-08 Inhibitors of thrombin

Publications (1)

Publication Number Publication Date
ES2149170T3 true ES2149170T3 (es) 2000-11-01

Family

ID=24618783

Family Applications (1)

Application Number Title Priority Date Filing Date
ES92905748T Expired - Lifetime ES2149170T3 (es) 1991-02-08 1992-02-03 Inhibidores mejorados de trombina.

Country Status (18)

Country Link
US (3) US5240913A (es)
EP (1) EP0529031B9 (es)
JP (1) JPH05506252A (es)
KR (1) KR100259759B1 (es)
AT (1) ATE193325T1 (es)
AU (1) AU659828B2 (es)
BG (1) BG61243B2 (es)
CA (1) CA2079778C (es)
DE (1) DE69231081T2 (es)
DK (1) DK0529031T3 (es)
ES (1) ES2149170T3 (es)
FI (2) FI120348B (es)
GR (1) GR3034257T3 (es)
HU (1) HU218831B (es)
NO (1) NO315710B1 (es)
NZ (1) NZ241557A (es)
TW (1) TW222642B (es)
WO (1) WO1992013952A1 (es)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5240913A (en) * 1989-08-18 1993-08-31 Biogen, Inc. Inhibitors of thrombin
US6060451A (en) * 1990-06-15 2000-05-09 The National Research Council Of Canada Thrombin inhibitors based on the amino acid sequence of hirudin
US5458568A (en) * 1991-05-24 1995-10-17 Cortrak Medical, Inc. Porous balloon for selective dilatation and drug delivery
US5811447A (en) * 1993-01-28 1998-09-22 Neorx Corporation Therapeutic inhibitor of vascular smooth muscle cells
US6515009B1 (en) 1991-09-27 2003-02-04 Neorx Corporation Therapeutic inhibitor of vascular smooth muscle cells
US5656600A (en) * 1993-03-25 1997-08-12 Corvas International, Inc. α-ketoamide derivatives as inhibitors of thrombosis
US5599307A (en) * 1993-07-26 1997-02-04 Loyola University Of Chicago Catheter and method for the prevention and/or treatment of stenotic processes of vessels and cavities
EP0738156A1 (en) * 1993-12-27 1996-10-23 Hamilton Civic Hospitals Research Development, Inc. Methods and compositions for inhibiting thrombogenesis
WO1995019359A1 (en) * 1994-01-12 1995-07-20 Massachusetts Institute Of Technology Process for making xanthene or cubane based compounds, and protease inhibitors
US5510330A (en) * 1994-03-25 1996-04-23 Boehringer Mannheim Gmbh Combinations of thrombolytically active proteins and non-heparin anticoagulants, and uses thereof.
US6759384B1 (en) 1994-04-26 2004-07-06 Aventis Pharmaceuticals Inc. Factor Xa inhibitors
US5849510A (en) * 1994-04-26 1998-12-15 Selectide Corporation Factor Xa inhibitors
DE4430204A1 (de) 1994-08-26 1996-02-29 Behringwerke Ag Arzneimittel, welches als Gegenmittel für Blut-Antikoagulanzien geeignet ist und seine Verwendung
DE4430205A1 (de) 1994-08-26 1996-02-29 Behringwerke Ag Zusammensetzungen, die als Gegenmittel für Blut-Antikoagulanzien geeignet sind und deren Verwendung
US5747453A (en) * 1995-06-06 1998-05-05 Alza Corporation Method for increasing the electrotransport flux of polypeptides
DE19549118C2 (de) * 1995-12-29 2000-07-13 Thomas W Stief Hämostaseaktivierungs-Inhibitor und Verfahren zum Hemmen der Hämostaseaktivierung in Blut oder anderen biologischen Flüssigkeiten
US6333189B1 (en) 1996-06-06 2001-12-25 Alza Corporation Method of making an electrotransport device
JPH1010784A (ja) * 1996-06-27 1998-01-16 Brother Ind Ltd 正帯電性一成分現像剤並びにその現像剤を用いた画像形成装置
GB9613719D0 (en) * 1996-06-29 1996-08-28 Thrombosis Res Inst Serine protease inhibitors
GB9613718D0 (en) * 1996-06-29 1996-08-28 Thrombosis Res Inst Thrombin inhibitors
US5840733A (en) * 1996-07-01 1998-11-24 Redcell, Canada, Inc. Methods and compositions for producing novel conjugates of thrombin inhibitors and endogenous carriers resulting in anti-thrombins with extended lifetimes
US5985833A (en) * 1996-09-17 1999-11-16 Wisconsin Alumni Research Foundation Thrombin inhibitor
US20030077310A1 (en) 2001-10-22 2003-04-24 Chandrashekhar Pathak Stent coatings containing HMG-CoA reductase inhibitors
DE10162521A1 (de) * 2001-12-19 2003-07-17 Goetz Nowak Verwendung von molekulargewichtserweiterten Substanzen in der Tumortherapie
WO2006045503A1 (en) 2004-10-19 2006-05-04 Lonza Ag Method for solid phase peptide synthesis
US7598343B1 (en) 2008-07-27 2009-10-06 The Medicines Company Pharmaceutical formulations of bivalirudin and processes of making the same
US7582727B1 (en) 2008-07-27 2009-09-01 The Medicinces Company Pharmaceutical formulations of bivalirudin and processes of making the same
EP2334314A4 (en) 2008-09-03 2012-03-21 Scinopharm Taiwan Ltd PROCESS FOR THE PREPARATION OF PRAMLINTIDE
US7803762B1 (en) 2009-08-20 2010-09-28 The Medicines Company Ready-to-use bivalirudin compositions
US7985733B1 (en) 2010-01-06 2011-07-26 The Medicines Company Buffer-based method for preparing bivalirudin drug product
GB201121513D0 (en) 2011-12-14 2012-01-25 Cambridge Entpr Ltd Thrombin-binding antibody molecules and uses thereof
US9518128B2 (en) 2011-12-14 2016-12-13 Janssen Pharmaceuticals, Inc. Thrombin-binding antibody molecules
PL3464336T3 (pl) 2016-06-01 2022-05-16 Athira Pharma, Inc. Związki
WO2019030706A1 (en) 2017-08-10 2019-02-14 Janssen Pharmaceutica Nv ANTI-THROMBIN ANTIBODY MOLECULES AND METHODS OF USE IN ORTHOPEDIC SURGERY
WO2019035055A1 (en) 2017-08-16 2019-02-21 Janssen Pharmaceutica Nv ANTI-THROMBIN ANTIBODY MOLECULES AND METHODS OF USE WITH PLATELET ANTI-AGGREGATE AGENTS
US11992514B2 (en) 2019-05-20 2024-05-28 MAIA Pharmaceuticals, Inc. Ready-to-use bivalirudin compositions

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1161431A (en) * 1979-05-11 1984-01-31 Lars G. Svendsen Tripeptide derivatives
GB8305985D0 (en) * 1983-03-04 1983-04-07 Szelke M Enzyme inhibition
DE3501107A1 (de) * 1985-01-15 1986-07-17 Josef 8358 Vilshofen Paul Nutzfahrzeug mit schieberahmenwechselaufbau
CA1341032C (en) * 1987-01-23 2000-06-20 John L. Krstenansky Anticoagulant peptides
ZA883444B (es) * 1987-05-21 1988-11-16
ZA883443B (en) * 1987-05-21 1988-11-16 Merrell Dow Pharmaceuticals Inc. Cyclic anticoagulant peptides
EP0333356A3 (en) * 1988-03-04 1990-12-19 Biogen, Inc. Hirudin peptides
NZ228995A (en) * 1988-05-10 1992-03-26 Merrell Dow Pharma Hirudin peptide derivatives and pharmaceutical compositions
US4971953A (en) * 1988-05-10 1990-11-20 Merrell Dow Pharmaceuticals Anticoagulant peptide alcohols
JPH04500802A (ja) * 1988-09-29 1992-02-13 バイオジェン インコーポレイテッド ヒルジンペプチド
US5196404B1 (en) * 1989-08-18 1996-09-10 Biogen Inc Inhibitors of thrombin
US5240913A (en) * 1989-08-18 1993-08-31 Biogen, Inc. Inhibitors of thrombin
AU654820B2 (en) * 1990-06-15 1994-11-24 Majesty (Her) In Right Of Canada As Represented By The National Research Council Of Canada Thrombin inhibitors based on the amino acid sequence of hirudin

Also Published As

Publication number Publication date
NO923889L (no) 1992-12-08
US5514409A (en) 1996-05-07
DE69231081T2 (de) 2001-02-01
TW222642B (es) 1994-04-21
JPH05506252A (ja) 1993-09-16
US5425936A (en) 1995-06-20
AU1362192A (en) 1992-09-07
KR100259759B1 (ko) 2000-06-15
FI20050027L (fi) 2005-01-11
CA2079778C (en) 2002-09-03
AU659828B2 (en) 1995-06-01
FI120348B (fi) 2009-09-30
NO315710B1 (no) 2003-10-13
FI924503A0 (fi) 1992-10-06
GR3034257T3 (en) 2000-12-29
DK0529031T3 (da) 2000-10-09
EP0529031B9 (en) 2007-11-21
HU218831B (hu) 2000-12-28
EP0529031B1 (en) 2000-05-24
BG61243B2 (bg) 1997-03-31
FI924503A7 (fi) 1992-10-06
DE69231081D1 (de) 2000-06-29
EP0529031A1 (en) 1993-03-03
NZ241557A (en) 1996-11-26
HUT65675A (en) 1994-07-28
ATE193325T1 (de) 2000-06-15
FI120690B (fi) 2010-01-29
US5240913A (en) 1993-08-31
NO923889D0 (no) 1992-10-07
WO1992013952A1 (en) 1992-08-20
CA2079778A1 (en) 1992-08-09
HK1005995A1 (en) 1999-02-05
HU9203500D0 (en) 1993-01-28

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