WO2001025264A3 - Substituted phosphinate based peptide derivatives - Google Patents

Substituted phosphinate based peptide derivatives Download PDF

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Publication number
WO2001025264A3
WO2001025264A3 PCT/EP2000/009173 EP0009173W WO0125264A3 WO 2001025264 A3 WO2001025264 A3 WO 2001025264A3 EP 0009173 W EP0009173 W EP 0009173W WO 0125264 A3 WO0125264 A3 WO 0125264A3
Authority
WO
WIPO (PCT)
Prior art keywords
peptide derivatives
based peptide
phosphinate based
substituted phosphinate
substituted
Prior art date
Application number
PCT/EP2000/009173
Other languages
French (fr)
Other versions
WO2001025264A9 (en
WO2001025264A2 (en
Inventor
Jens Buchardt
Niels Taekker Foged
Morten Meldal
Jean-Marie Delaisse
Michael Engsig
Mercedes Ferreras
Morten Karsdal
Maria Del Carmen Ovejero
Christine Bruun Schioedt
Bent Winding
Original Assignee
Osteopro As
Jens Buchardt
Niels Taekker Foged
Morten Meldal
Delaisse Jean Marie
Michael Engsig
Mercedes Ferreras
Morten Karsdal
Maria Del Carmen Ovejero
Christine Bruun Schioedt
Bent Winding
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 Osteopro As, Jens Buchardt, Niels Taekker Foged, Morten Meldal, Delaisse Jean Marie, Michael Engsig, Mercedes Ferreras, Morten Karsdal, Maria Del Carmen Ovejero, Christine Bruun Schioedt, Bent Winding filed Critical Osteopro As
Priority to AU77785/00A priority Critical patent/AU7778500A/en
Priority to EP00967712A priority patent/EP1220871A2/en
Publication of WO2001025264A2 publication Critical patent/WO2001025264A2/en
Publication of WO2001025264A3 publication Critical patent/WO2001025264A3/en
Publication of WO2001025264A9 publication Critical patent/WO2001025264A9/en

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
    • C07K7/04—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
    • 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
    • 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
    • C07K5/1027—Tetrapeptides containing heteroatoms different from O, S, or N
    • 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

Abstract

Compounds of Formula (I): wherein the substituents are as defined in the description and their use in the treatment of metabolic bone diseases such as osteoporosis and bone metastasis.
PCT/EP2000/009173 1999-09-23 2000-09-19 Substituted phosphinate based peptide derivatives WO2001025264A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU77785/00A AU7778500A (en) 1999-09-23 2000-09-19 Substituted phosphinate based peptide derivatives
EP00967712A EP1220871A2 (en) 1999-09-23 2000-09-19 Substituted phosphinate based peptide derivatives

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9922577.3A GB9922577D0 (en) 1999-09-23 1999-09-23 Substituted phosphinate based peptide derivatives
GB9922577.3 1999-09-23

Publications (3)

Publication Number Publication Date
WO2001025264A2 WO2001025264A2 (en) 2001-04-12
WO2001025264A3 true WO2001025264A3 (en) 2001-10-18
WO2001025264A9 WO2001025264A9 (en) 2002-09-19

Family

ID=10861504

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2000/009173 WO2001025264A2 (en) 1999-09-23 2000-09-19 Substituted phosphinate based peptide derivatives

Country Status (4)

Country Link
EP (1) EP1220871A2 (en)
AU (1) AU7778500A (en)
GB (1) GB9922577D0 (en)
WO (1) WO2001025264A2 (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2996003B1 (en) 2012-09-25 2014-10-17 Commissariat Energie Atomique METHOD FOR SPECIFICALLY DETECTION IN SAMPLE MATRIX METALLOPROTEASE (MMP) OF INTEREST ONLY IN ACTIVE FORM

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0276436A1 (en) * 1986-12-15 1988-08-03 F. Hoffmann-La Roche Ag Phosphinic acid derivatives
WO1999003878A2 (en) * 1997-07-17 1999-01-28 Polifarma S.P.A. Inhibitors of metalloproteinases, their therapeutic use, and process for the production of the starting compound in their synthesis
WO2000043404A1 (en) * 1999-01-19 2000-07-27 Commissariat A L'energie Atomique Phosphinic pseudopeptides inhibitors of matrix metalloproteases

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0276436A1 (en) * 1986-12-15 1988-08-03 F. Hoffmann-La Roche Ag Phosphinic acid derivatives
WO1999003878A2 (en) * 1997-07-17 1999-01-28 Polifarma S.P.A. Inhibitors of metalloproteinases, their therapeutic use, and process for the production of the starting compound in their synthesis
WO2000043404A1 (en) * 1999-01-19 2000-07-27 Commissariat A L'energie Atomique Phosphinic pseudopeptides inhibitors of matrix metalloproteases

Non-Patent Citations (8)

* Cited by examiner, † Cited by third party
Title
BLAVIER L ET AL: "Matrix metalloproteinases are obligatory for the migration of preosteoclasts to the developing marrow cavity of primitive long bones.", JOURNAL OF CELL SCIENCE, (1995 DEC) 108 ( PT 12) 3649-59., XP002165431 *
BUCHARDT E.A.: "Phosphinic peptide matrix metalloproteinase-9 inhibitors by solid-phase synthesis using a building block approach", CHEM.EUR.J, vol. 5, no. 10, 24 September 1999 (1999-09-24), pages 2877 - 2884, XP002165432 *
BUCHARDT E.A.: "Solid phase combinatorial library of phosphinic peptides for discovery of matrix metalloproteinase inhibitors", J.COMB.CHEM, vol. 2, 13 September 2000 (2000-09-13), pages 624 - 638, XP002165433 *
NAGASE H ET AL: "DESIGN AND CHARACTERIZATION OF A FLUOROGENIC SUBSTRATE SELECTIVELY HYDROLYZED BY STROMELYSIN 1 (MATRIX METALLOPROTEINASE-3)", JOURNAL OF BIOLOGICAL CHEMISTRY,US,AMERICAN SOCIETY OF BIOLOGICAL CHEMISTS, BALTIMORE, MD, vol. 269, no. 33, 19 August 1994 (1994-08-19), pages 20952 - 20957, XP000566937, ISSN: 0021-9258 *
SATO T ET AL: "The migration of purified osteoclasts through collagen is inhibited by matrix metalloproteinase inhibitors.", JOURNAL OF BONE AND MINERAL RESEARCH, (1998 JAN) 13 (1) 59-66., XP000992863 *
VASSILIOU S ET AL: "Phosphinic pseudo-tripeptides as potent inhibitors of matrix metalloproteinases: a structure-activity study.", JOURNAL OF MEDICINAL CHEMISTRY, (1999 JUL 15) 42 (14) 2610-20., XP002165434 *
YIALLOUROS I ET AL: "Phosphinic peptides, the first potent inhibitors of astacin, behave as extremely slow-binding inhibitors.", BIOCHEMICAL JOURNAL, (1998 APR 15) 331 ( PT 2) 375-9., XP002165429 *
YIOTAKIS, ATHANASIOS ET AL: "Protection of the Hydroxyphosphinyl Function of Phosphinic Dipeptides by Adamantyl. Application to the Solid-Phase Synthesis of Phosphinic Peptides", J. ORG. CHEM. (1996), 61(19), 6601-6605, XP002165430 *

Also Published As

Publication number Publication date
WO2001025264A9 (en) 2002-09-19
EP1220871A2 (en) 2002-07-10
WO2001025264A2 (en) 2001-04-12
GB9922577D0 (en) 1999-11-24
AU7778500A (en) 2001-05-10

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