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HUP0100082A2 - Trombininhibitor hatású peptidszármazékok, ezeket hatóanyagként tartalmazó gyógyszerkészítmények és alkalmazásuk - Google Patents

Trombininhibitor hatású peptidszármazékok, ezeket hatóanyagként tartalmazó gyógyszerkészítmények és alkalmazásuk

Info

Publication number
HUP0100082A2
HUP0100082A2 HU0100082A HUP0100082A HUP0100082A2 HU P0100082 A2 HUP0100082 A2 HU P0100082A2 HU 0100082 A HU0100082 A HU 0100082A HU P0100082 A HUP0100082 A HU P0100082A HU P0100082 A2 HUP0100082 A2 HU P0100082A2
Authority
HU
Hungary
Prior art keywords
group
general formula
pharmaceutical compositions
peptide derivatives
thrombin inhibitor
Prior art date
Application number
HU0100082A
Other languages
English (en)
Inventor
Dorit Baucke
Wilfried Hornberger
Hans Wolfgang Höffken
Udo Lange
Helmut Mack
Werner Seitz
Original Assignee
Basf Ag
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 Basf Ag filed Critical Basf Ag
Publication of HUP0100082A2 publication Critical patent/HUP0100082A2/hu
Publication of HUP0100082A3 publication Critical patent/HUP0100082A3/hu

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
    • C07K5/04—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
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)

Abstract

A találmány tárgya (I) általános képletű - ahol A (a) általánosképletű csoport; B (b) általános képletű csoport; tetrahidro-azetichint, pirrolidinil-, piperidinil-, perhidro-tiazolil-,pirazonil-, indolil- vagy tetrehidropiridazonil-karbinil-csoport Eadott esetben szubsztituált amino-metil-5 tagú heteroaril-csoport F(f1) vagy (f2 ) képletű csoport - új, öt építőelemből állóheterociklusos amidinek. A találmány tárgya továbbá az új vegyületekethatóanyagokként tartalmazó gyógyszerkészítmények, amelyektrombininhitorokként, antikoagulánsokként és gyulladásgátlókkéntalkalmazhatók. Ó
HU0100082A 1998-01-26 1999-01-23 Thrombin inhibitor, peptide derivatives, pharmaceutical compositions comprising thereof and their use HUP0100082A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19802793 1998-01-26
PCT/EP1999/000434 WO1999037668A1 (de) 1998-01-26 1999-01-23 Thrombininhibitoren

Publications (2)

Publication Number Publication Date
HUP0100082A2 true HUP0100082A2 (hu) 2001-06-28
HUP0100082A3 HUP0100082A3 (en) 2001-12-28

Family

ID=7855658

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0100082A HUP0100082A3 (en) 1998-01-26 1999-01-23 Thrombin inhibitor, peptide derivatives, pharmaceutical compositions comprising thereof and their use

Country Status (12)

Country Link
US (1) US6740647B1 (hu)
EP (1) EP1051431A1 (hu)
JP (1) JP2002501081A (hu)
KR (1) KR100689923B1 (hu)
CN (1) CN1289341A (hu)
AU (1) AU751111B2 (hu)
BR (1) BR9907112A (hu)
CA (1) CA2317761A1 (hu)
HU (1) HUP0100082A3 (hu)
IL (1) IL136139A0 (hu)
NO (1) NO20003814L (hu)
WO (1) WO1999037668A1 (hu)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1054886B1 (en) * 1998-02-09 2002-09-04 3-Dimensional Pharmaceuticals, Inc. Heteroaryl amidines, methylamidines and guanidines as protease inhibitors, in particular as urokinase inhibitors
KR20000047461A (ko) * 1998-12-29 2000-07-25 성재갑 트롬빈 억제제
PL351767A1 (en) * 1999-02-09 2003-06-16 Dimensional Pharmaceuticals 3 Heteroaryl amidines, methylamidines and guanidines as protease inhibitors
AU4111700A (en) * 1999-04-09 2000-11-14 Basf Aktiengesellschaft Low-molecular inhibitors of complement proteases
CN1355810A (zh) * 1999-04-09 2002-06-26 巴斯福股份公司 凝血酶抑制剂的前体药物
AR023510A1 (es) 1999-04-21 2002-09-04 Astrazeneca Ab Un equipo de partes, formulacion farmaceutica y uso de un inhibidor de trombina.
ATE454469T1 (de) 2002-01-28 2010-01-15 Ambion Inc Für den nachweis von nukleinsäuren kompetente biologische rohderivate
WO2007081530A2 (en) * 2006-01-03 2007-07-19 Med Institute, Inc. Endoluminal medical device for local delivery of cathepsin inhibitors
US7727978B2 (en) * 2006-08-24 2010-06-01 Bristol-Myers Squibb Company Cyclic 11-beta hydroxysteroid dehydrogenase type I inhibitors
US7964350B1 (en) 2007-05-18 2011-06-21 Applied Biosystems, Llc Sample preparation for in situ nucleic acid analysis
US8119658B2 (en) 2007-10-01 2012-02-21 Bristol-Myers Squibb Company Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors
AU2009263076B2 (en) * 2008-06-23 2012-07-26 Astrazeneca Ab New heterocyclic carboxamides for use as thrombin inhibitors
EP2367954B1 (en) * 2008-12-19 2015-02-18 Life Technologies Corporation Proteinase k inhibitors, methods and compositions therefor
CN102464701B (zh) * 2010-11-08 2015-10-21 上海医药工业研究院 一类新型化合物、其制备方法及用途
KR102256242B1 (ko) 2014-02-07 2021-05-26 엑시테라 파마슈티컬스 인코퍼레이티드 치료 화합물 및 조성물
WO2019156929A1 (en) 2018-02-07 2019-08-15 eXIthera Pharmaceuticals Inc. Therapeutic compounds and compositions

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU178398B (en) 1979-06-12 1982-04-28 Gyogyszerkutato Intezet Process for producing new agmatine derivatives of activity against haemagglutination
GB8305985D0 (en) 1983-03-04 1983-04-07 Szelke M Enzyme inhibition
HU192646B (en) 1984-12-21 1987-06-29 Gyogyszerkutato Intezet Process for preparing new n-alkyl-peptide aldehydes
AU600226B2 (en) 1985-02-04 1990-08-09 Merrell Pharmaceuticals Inc. Novel peptidase inhibitors
US5187157A (en) 1987-06-05 1993-02-16 Du Pont Merck Pharmaceutical Company Peptide boronic acid inhibitors of trypsin-like proteases
EP0362002B1 (en) 1988-09-01 1995-07-26 Merrell Dow Pharmaceuticals Inc. HIV protease inhibitors
ZA897515B (en) 1988-10-07 1990-06-27 Merrell Dow Pharma Novel peptidase inhibitors
CA2021660A1 (en) 1989-07-26 1991-01-27 Philippe Bey Peptidase inhibitors
GB9017694D0 (en) 1990-08-13 1990-09-26 Sandoz Ltd Improvements in or relating to organic chemistry
IL99527A (en) 1990-09-28 1997-08-14 Lilly Co Eli Tripeptide antithrombotic agents
GB9024129D0 (en) 1990-11-06 1990-12-19 Thrombosis Research Trust Inhibitors and substrates of thrombin
EP0503203A1 (en) 1991-03-15 1992-09-16 Merrell Dow Pharmaceuticals Inc. Novel thrombin inhibitors
CA2075154A1 (en) 1991-08-06 1993-02-07 Neelakantan Balasubramanian Peptide aldehydes as antithrombotic agents
SE9102462D0 (sv) 1991-08-28 1991-08-28 Astra Ab New isosteric peptides
ZA928581B (en) 1991-11-12 1994-05-06 Lilly Co Eli Antithrombotic agents
SE9103612D0 (sv) 1991-12-04 1991-12-04 Astra Ab New peptide derivatives
WO1993015756A1 (en) 1992-02-14 1993-08-19 Corvas International, Inc. Inhibitors of thrombosis
EP0629212B1 (en) 1992-03-04 1997-10-08 Gyogyszerkutato Intezet Kft. New anticoagulant peptide derivatives and pharmaceutical compositions containing the same as well as a process for the preparation thereof
FR2695562B1 (fr) 1992-09-11 1994-10-14 Synthelabo Utilisation d'un inhibiteur direct de la thrombine pour la fabrication d'un médicament à activité thrombolytique.
US5371072A (en) 1992-10-16 1994-12-06 Corvas International, Inc. Asp-Pro-Arg α-keto-amide enzyme inhibitors
AU675981B2 (en) 1992-12-02 1997-02-27 Bristol-Myers Squibb Company Guanidinyl-substituted heterocyclic thrombin inhibitors
SE9301916D0 (sv) 1993-06-03 1993-06-03 Ab Astra New peptides derivatives
ZA951617B (en) * 1994-03-04 1997-02-27 Lilly Co Eli Antithrombotic agents.
US5705487A (en) * 1994-03-04 1998-01-06 Eli Lilly And Company Antithrombotic agents
DE4421052A1 (de) * 1994-06-17 1995-12-21 Basf Ag Neue Thrombininhibitoren, ihre Herstellung und Verwendung
DE19504504A1 (de) * 1995-02-10 1996-08-14 Basf Ag Heterocyclische Thrombininhibitoren
US6069232A (en) 1995-10-02 2000-05-30 Hoechst Marion Roussel, Inc. Polyfluoroalkyl tryptophan tripeptide thrombin inhibitors
DE19632773A1 (de) * 1996-08-14 1998-02-19 Basf Ag Neue Thrombininhibitoren

Also Published As

Publication number Publication date
EP1051431A1 (de) 2000-11-15
NO20003814D0 (no) 2000-07-25
KR20010034360A (ko) 2001-04-25
IL136139A0 (en) 2001-05-20
WO1999037668A1 (de) 1999-07-29
CA2317761A1 (en) 1999-07-29
AU2829799A (en) 1999-08-09
AU751111B2 (en) 2002-08-08
NO20003814L (no) 2000-07-25
KR100689923B1 (ko) 2007-03-09
US6740647B1 (en) 2004-05-25
HUP0100082A3 (en) 2001-12-28
JP2002501081A (ja) 2002-01-15
CN1289341A (zh) 2001-03-28
BR9907112A (pt) 2000-10-24

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