AU2001282059A1 - Peptide and peptide mimetic conjugates with integrin-inhibitor properties - Google Patents

Peptide and peptide mimetic conjugates with integrin-inhibitor properties

Info

Publication number
AU2001282059A1
AU2001282059A1 AU2001282059A AU8205901A AU2001282059A1 AU 2001282059 A1 AU2001282059 A1 AU 2001282059A1 AU 2001282059 A AU2001282059 A AU 2001282059A AU 8205901 A AU8205901 A AU 8205901A AU 2001282059 A1 AU2001282059 A1 AU 2001282059A1
Authority
AU
Australia
Prior art keywords
lys
peptide
molecule
group
po3h2
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.)
Abandoned
Application number
AU2001282059A
Inventor
Michel Dard
Christoph Gibson
Ulrich Hersel
Gunter Holzemann
Martin Kantlehner
Horst Kessler
Jorg Meyer
Berthold Nies
Gabor Sulyok
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.)
Merck Patent GmbH
Original Assignee
Merck Patent GmbH
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 Merck Patent GmbH filed Critical Merck Patent GmbH
Publication of AU2001282059A1 publication Critical patent/AU2001282059A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A61K47/6435—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent the peptide or protein in the drug conjugate being a connective tissue peptide, e.g. collagen, fibronectin or gelatin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A61K47/6425—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent the peptide or protein in the drug conjugate being a receptor, e.g. CD4, a cell surface antigen, i.e. not a peptide ligand targeting the antigen, or a cell surface determinant, i.e. a part of the surface of a cell
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cell Biology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Hematology (AREA)
  • Peptides Or Proteins (AREA)
  • Cosmetics (AREA)

Abstract

The invention relates to compounds of formula (1) B-Q-X1, wherein B is bioactive cell adhesive mediating molecule. Q is absent or is an inorganic spacer molecule and X1 is an anchor molecule, selected from the group Lys-(CO-CH2-(CH2)n-PO3H2)2(I), -Lys-[-Lys-(CO-CH2-(CH2)a-PO3H2)2]2(ii) or -Lys-(Lys[-Lys-(CO-CH2-(CH2)n-PO3H2]2 (iii), and n independently represents 0, 1, 2 or 3, wherein a free amino group of group B is linked in peptide form to a free carboxyl group of the spacer molecule Q or of the anchor molecule X1, or a free amino group of the radical Q is linked in peptide form to a free carboxyl group of the radical X1. The invention also relates to the salts thereof. The inventive compounds can be used as integrin inhibitors for the treatment of illnesses, deficiencies, inflammations caused by implants and osteolytic illnesses such as osteoporosis, thrombosis, cardiac infarction and arteriosclerosis, in addition to the acceleration and strengthening of the integration process of implants or the biocompatible surface in tissue.
AU2001282059A 2000-08-17 2001-08-02 Peptide and peptide mimetic conjugates with integrin-inhibitor properties Abandoned AU2001282059A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE10040105A DE10040105A1 (en) 2000-08-17 2000-08-17 Peptide and peptide mimetic derivatives with integrin inhibitor properties
DE10040105 2000-08-17
PCT/EP2001/008932 WO2002013872A1 (en) 2000-08-17 2001-08-02 Peptide and peptide mimetic conjugates with integrin-inhibitor properties

Publications (1)

Publication Number Publication Date
AU2001282059A1 true AU2001282059A1 (en) 2002-02-25

Family

ID=7652668

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2001282059A Abandoned AU2001282059A1 (en) 2000-08-17 2001-08-02 Peptide and peptide mimetic conjugates with integrin-inhibitor properties

Country Status (19)

Country Link
US (1) US7655624B2 (en)
EP (1) EP1309355B9 (en)
JP (1) JP4902090B2 (en)
KR (1) KR20030062319A (en)
CN (1) CN1447699A (en)
AT (1) ATE395085T1 (en)
AU (1) AU2001282059A1 (en)
CA (1) CA2419423C (en)
CY (1) CY1108898T1 (en)
CZ (1) CZ2003692A3 (en)
DE (2) DE10040105A1 (en)
DK (1) DK1309355T3 (en)
ES (1) ES2306723T3 (en)
HU (1) HUP0301396A2 (en)
MX (1) MXPA03001428A (en)
PL (1) PL358809A1 (en)
PT (1) PT1309355E (en)
WO (1) WO2002013872A1 (en)
ZA (1) ZA200302049B (en)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10040105A1 (en) 2000-08-17 2002-02-28 Merck Patent Gmbh Peptide and peptide mimetic derivatives with integrin inhibitor properties
AU2001221607A1 (en) 2000-11-20 2002-05-27 Ecole Polytechnique Federale De Lausanne (Epfl) Endosseous implant
DE10325049A1 (en) * 2003-06-02 2004-12-23 Merck Patent Gmbh New peptide derivatives containing cell-adhesion molecule and phosphonate-containing anchor component, useful for treating disorders associated with implants, are inhibitors of integrins
EP1793875B9 (en) * 2004-06-16 2010-09-08 Affinergy, Inc. Ifbm's to promote attachment of target analytes
US20090053280A1 (en) * 2007-05-15 2009-02-26 Michael Joner Coating stents with cyclic rgd peptides or mimetics
KR102017026B1 (en) * 2013-01-10 2019-09-02 (주) 수파드엘릭사 Pharmaceutical composition for preventing or treating inflammation or allergy and cosmetic composition for improving inflammation or allergy
EP4252629A3 (en) 2016-12-07 2023-12-27 Biora Therapeutics, Inc. Gastrointestinal tract detection methods, devices and systems
CA3045931A1 (en) 2016-12-14 2018-06-21 Progenity, Inc. Treatment of a disease of the gastrointestinal tract with an integrin inhibitor
EP3810085A1 (en) 2018-06-20 2021-04-28 Progenity, Inc. Treatment of a disease of the gastrointestinal tract with an integrin inhibitor
KR20210095165A (en) 2018-11-19 2021-07-30 프로제너티, 인크. Methods and devices for treating diseases with biopharmaceuticals
CN115666704A (en) 2019-12-13 2023-01-31 比奥拉治疗股份有限公司 Ingestible device for delivery of therapeutic agents to the gastrointestinal tract

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4310643A1 (en) 1993-04-01 1994-10-06 Merck Patent Gmbh Cyclic adhesion inhibitors
DE19755801A1 (en) 1997-12-16 2000-06-21 Merck Patent Gmbh Implant with improved tissue integration
PL337019A1 (en) * 1997-05-22 2000-07-31 Merck Patent Gmbh Peptide-coated implants and method of obtaining them
DE19755800A1 (en) 1997-12-16 1999-06-17 Merck Patent Gmbh Cyclopeptide derivatives
DE19831710A1 (en) 1998-07-15 2000-01-20 Merck Patent Gmbh New diacyl-hydrazine derivatives, are integrin inhibitors useful for treating e.g. thrombosis, cardiac infarction, tumors, osteoporosis, inflammation or infection
DE19932796A1 (en) 1999-07-14 2001-01-18 Merck Patent Gmbh Diacylhydrazine derivatives
DE10040105A1 (en) 2000-08-17 2002-02-28 Merck Patent Gmbh Peptide and peptide mimetic derivatives with integrin inhibitor properties
CA2549202A1 (en) 2005-12-02 2007-06-02 Stoneadvise Products North America Inc.- Les Produits Stoneadvise D'amer Ique Du Nord Inc. Modular stone panel

Also Published As

Publication number Publication date
ES2306723T3 (en) 2008-11-16
CA2419423A1 (en) 2002-02-21
WO2002013872A1 (en) 2002-02-21
PT1309355E (en) 2008-08-26
DE10040105A1 (en) 2002-02-28
CA2419423C (en) 2011-01-04
JP4902090B2 (en) 2012-03-21
ATE395085T1 (en) 2008-05-15
US7655624B2 (en) 2010-02-02
HUP0301396A2 (en) 2003-09-29
EP1309355B9 (en) 2009-04-08
PL358809A1 (en) 2004-08-23
DK1309355T3 (en) 2008-08-25
CN1447699A (en) 2003-10-08
MXPA03001428A (en) 2003-06-06
JP2004506024A (en) 2004-02-26
US20040029782A1 (en) 2004-02-12
CY1108898T1 (en) 2014-07-02
CZ2003692A3 (en) 2003-06-18
KR20030062319A (en) 2003-07-23
EP1309355B1 (en) 2008-05-14
EP1309355A1 (en) 2003-05-14
ZA200302049B (en) 2004-08-27
DE50113975D1 (en) 2008-06-26

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