WO2002030940A3 - Niedermolekulare inhibitoren von serinproteasen mit polyhydroxyalkyl- und polyhydroxycycloakylresten - Google Patents

Niedermolekulare inhibitoren von serinproteasen mit polyhydroxyalkyl- und polyhydroxycycloakylresten Download PDF

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Publication number
WO2002030940A3
WO2002030940A3 PCT/EP2001/011207 EP0111207W WO0230940A3 WO 2002030940 A3 WO2002030940 A3 WO 2002030940A3 EP 0111207 W EP0111207 W EP 0111207W WO 0230940 A3 WO0230940 A3 WO 0230940A3
Authority
WO
WIPO (PCT)
Prior art keywords
polyhydroxy
serine protease
sugar
inhibitors
compounds
Prior art date
Application number
PCT/EP2001/011207
Other languages
English (en)
French (fr)
Other versions
WO2002030940A2 (de
Inventor
Dieter Herr
Helmut Mack
Werner Seitz
Wilfried Hornberger
Original Assignee
Abbott Gmbh & Co Kg
Dieter Herr
Helmut Mack
Werner Seitz
Wilfried Hornberger
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 Abbott Gmbh & Co Kg, Dieter Herr, Helmut Mack, Werner Seitz, Wilfried Hornberger filed Critical Abbott Gmbh & Co Kg
Priority to CA002424926A priority Critical patent/CA2424926A1/en
Priority to US10/398,269 priority patent/US20040048815A1/en
Priority to MXPA03002923A priority patent/MXPA03002923A/es
Priority to AU2001289932A priority patent/AU2001289932A1/en
Priority to EP01969785A priority patent/EP1370573A2/de
Priority to JP2002534325A priority patent/JP2004511489A/ja
Publication of WO2002030940A2 publication Critical patent/WO2002030940A2/de
Publication of WO2002030940A3 publication Critical patent/WO2002030940A3/de
Priority to US12/850,545 priority patent/US20110071285A1/en
Priority to US13/277,829 priority patent/US20120190832A1/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • 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
    • 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
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H7/00—Compounds containing non-saccharide radicals linked to saccharide radicals by a carbon-to-carbon bond

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Die vorliegende Erfindung betrifft neue Amidine und Guanidine, ihre Herstellung und ihre Verwendung als kompetitive Inhibitoren von Trypsin-ähnlichen Serinproteasen, besonders Thrombin und der Komplementproteasen Cls und Clr. Die Erfindung bezieht sich auch auf pharmazeutische Zusammensetzugen, die die Verbindungen als aktive Bestandteile enthalten, sowie die Verwendung der Verbindungen als Thrombininhibitoren, Antikoagulantien, Komplementinhibitoren und als antiinflammatorische Agenzien. Charakteristisch für die neuen Verbindungen ist die Verknüpfung eines Serinproteaseinhibitors, mit Amidin- oder Guanidinfunktion, mit einem Alkyrest mit zwei oder mehreren Hydroxylfunktionen, wobei sich dieser Alkylrest von Zuckerderivaten ableitet. Dabei können auch mehrere Zuckerba usteine oder von Zuckern abgeleitete Bausteine miteinander verknüpft sein. Dieses Prinzip der Kupplung mit Zuckerderivaten führt zu oral aktiven Verbindungen.
PCT/EP2001/011207 2000-10-06 2001-09-27 Niedermolekulare inhibitoren von serinproteasen mit polyhydroxyalkyl- und polyhydroxycycloakylresten WO2002030940A2 (de)

Priority Applications (8)

Application Number Priority Date Filing Date Title
CA002424926A CA2424926A1 (en) 2000-10-06 2001-09-27 Low molecular serine protease inhibitors comprising polyhydroxy-alkyl and polyhydroxy-cycloalkyl radicals
US10/398,269 US20040048815A1 (en) 2000-10-06 2001-09-27 Low-molecular serine proteases inhibitors comprising polyhydroxy-alkyl and polyhydroxy-cycloalkyl radicals
MXPA03002923A MXPA03002923A (es) 2000-10-06 2001-09-27 Inhibidores de proteasas serina de peso molecular inferior que poseen radicales polihidroxialquilo y polihidroxicicloalquilo.
AU2001289932A AU2001289932A1 (en) 2000-10-06 2001-09-27 Low molecular serine protease inhibitors comprising polyhydroxy-alkyl and polyhydroxy-cycloalkyl radicals
EP01969785A EP1370573A2 (de) 2000-10-06 2001-09-27 Niedermolekulare inhibitoren von serinproteasen mit polyhydroxyalkyl- und polyhydroxycycloakylresten
JP2002534325A JP2004511489A (ja) 2000-10-06 2001-09-27 ポリヒドロキシアルキル基およびポリヒドロキシシクロアルキル基を有するセリンプロでアーゼの低分子インヒビター
US12/850,545 US20110071285A1 (en) 2000-10-06 2010-08-04 Low-molecular serine proteases inhibitors comprising polyhydroxy-alkyl and polyhydroxy-cycloalkyl radicals
US13/277,829 US20120190832A1 (en) 2000-10-06 2011-10-20 Low-molecular serine proteases inhibitors comprising polyhydroxy-alkyl and polyhydroxy-cycloalkyl radicals

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10049937.6 2000-10-06
DE10049937A DE10049937A1 (de) 2000-10-06 2000-10-06 Niedermolekulare Inhibitoren von Serinproteasen mit Polyhydroxyalkyl- und Polyhydroxycycloalkylresten

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US12/850,545 Continuation US20110071285A1 (en) 2000-10-06 2010-08-04 Low-molecular serine proteases inhibitors comprising polyhydroxy-alkyl and polyhydroxy-cycloalkyl radicals

Publications (2)

Publication Number Publication Date
WO2002030940A2 WO2002030940A2 (de) 2002-04-18
WO2002030940A3 true WO2002030940A3 (de) 2003-10-02

Family

ID=7659136

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2001/011207 WO2002030940A2 (de) 2000-10-06 2001-09-27 Niedermolekulare inhibitoren von serinproteasen mit polyhydroxyalkyl- und polyhydroxycycloakylresten

Country Status (9)

Country Link
US (3) US20040048815A1 (de)
EP (1) EP1370573A2 (de)
JP (1) JP2004511489A (de)
AR (1) AR036326A1 (de)
AU (1) AU2001289932A1 (de)
CA (1) CA2424926A1 (de)
DE (1) DE10049937A1 (de)
MX (1) MXPA03002923A (de)
WO (1) WO2002030940A2 (de)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10259382A1 (de) * 2002-12-18 2004-07-01 Abbott Gmbh & Co. Kg 3-Substituierte 3,4-Dihydro-thieno[2,3-d]pyrimidin-4-on-Derivate, ihre Herstellung und Verwendung
WO2020061067A2 (en) * 2018-09-17 2020-03-26 Board Of Regents, The University Of Texas System Texas System Compositions and methods for treating bone injury

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0513543A1 (de) * 1991-05-11 1992-11-19 BEHRINGWERKE Aktiengesellschaft Amidinophenylalaninderivate, Verfahren zu deren Herstellung, deren Verwendung und diese enthaltende Mittel als Antikoagulantien
EP0558961A2 (de) * 1992-03-05 1993-09-08 BEHRINGWERKE Aktiengesellschaft Glycopeptid-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende pharmazeutische Mittel
WO1999065934A1 (en) * 1998-06-17 1999-12-23 Akzo Nobel N.V. Antithrombotic compounds
WO2000039124A1 (en) * 1998-12-29 2000-07-06 Lg Ci Ltd. Thrombin inhibitors

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE9301916D0 (sv) * 1993-06-03 1993-06-03 Ab Astra New peptides derivatives
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
DE4443390A1 (de) * 1994-12-06 1996-06-13 Basf Ag Neue dipeptidische p-Amidinobenzylamide mit N-terminalen Sulfonyl- bzw. Aminosulfonylresten
CN1173872A (zh) * 1995-02-10 1998-02-18 巴斯福股份公司 凝血酶抑制剂
PL321759A1 (en) * 1995-02-17 1997-12-22 Basf Ag Novel thrombosin inhibitors
EP0846682B9 (de) * 1995-07-26 2003-05-14 Mitsubishi Chemical Corporation Penizillaminamid-derivate
DE19632772A1 (de) * 1996-08-14 1998-02-19 Basf Ag Neue Benzamidine
DE19632773A1 (de) * 1996-08-14 1998-02-19 Basf Ag Neue Thrombininhibitoren

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0513543A1 (de) * 1991-05-11 1992-11-19 BEHRINGWERKE Aktiengesellschaft Amidinophenylalaninderivate, Verfahren zu deren Herstellung, deren Verwendung und diese enthaltende Mittel als Antikoagulantien
EP0558961A2 (de) * 1992-03-05 1993-09-08 BEHRINGWERKE Aktiengesellschaft Glycopeptid-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende pharmazeutische Mittel
WO1999065934A1 (en) * 1998-06-17 1999-12-23 Akzo Nobel N.V. Antithrombotic compounds
WO2000039124A1 (en) * 1998-12-29 2000-07-06 Lg Ci Ltd. Thrombin inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
BUIJSMAN E.A.: "Design and synthesis of a novel synthetic NAPAP-penta-saccharide conjugate displaying a dual antithrombotic action", BIOORG.MED.CHEM.ETT., vol. 9, 1999, pages 2013 - 2018, XP004171628 *

Also Published As

Publication number Publication date
AR036326A1 (es) 2004-09-01
CA2424926A1 (en) 2003-04-04
DE10049937A1 (de) 2002-04-11
EP1370573A2 (de) 2003-12-17
US20040048815A1 (en) 2004-03-11
US20110071285A1 (en) 2011-03-24
US20120190832A1 (en) 2012-07-26
MXPA03002923A (es) 2003-08-07
AU2001289932A1 (en) 2002-04-22
JP2004511489A (ja) 2004-04-15
WO2002030940A2 (de) 2002-04-18

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