Peptide-based carrier devices for stellate cells

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

Reexamination Certificate

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C530S300000

Reexamination Certificate

active

06844319

ABSTRACT:
The present invention relates to a compound comprising a carrier molecule, said carrier molecule being linked to a further molecule, said further molecule being at least one cyclic peptide, said cyclic peptide comprising in the cyclic peptide portion thereof at least one sequence encoding a cell receptor recognising peptide (RRP) and with the proviso that the compound is not a naturally occuring receptor agonist or antagonist. Preferably, the RRP is of a receptor specific for Hepatic Stellate Cells (HSC) or a receptor that is upregulated on HSC during disease. In particular, the RRP may be of a receptor selected from the group of PDGF receptor, collagen type VI receptor, cytokine receptor(s) such as TGFβ, IFNα and interleukin 1β. Preferably, the cyclic portion of the cyclic peptide comprises at least the amino acid sequence RGD or KPT. The compounds can be used as an active targeting ingredient for manufacturing a pharmaceutical composition for therapy, prophylaxis or diagnosis of a disease selected from the group consisting of fibrotic disease, sclerotic disease and chronic or acute inflammatory processes such as glomerulosclerosis, interstitial fibrosis, lung fibrosis, atherosclerosis, rheumatoid arthritis, Crohns disease, colitis ulcerosa, glomerulonephritis and sepsis, in particular for targeting HSC. The invention also relates to pharmaceutial compositions comprising the above compound(s).

REFERENCES:
patent: 0 844 252 (1998-05-01), None
patent: WO 9746099 (1997-12-01), None
Beljaars, Leonie (1) et al : “The development of novel albumin carriers to hepatic stellate by application of cyclopeptide moieties recognizing collage type VI and platelet derived growth factor receptors, ” Hepatology, (Oct., 1998) vol.28, No. 4 Part 2, PP. 313A. Meeting Info.: Biennial Scientific Meeting Of The International Association For The Study Of The Liver And The 49TH Annual Meeting And Postgraduate Courses Of The American Association For The, XP002108150 See p. 313A, abstract 602.
Beljaars, Leonie et al : “Mannose 6-phosphate modified albumin accumulates in hepatic stellate cells: Potential application as an antifibroti drug carrier,” Hepatology, (Oct., 1998) vol. 28, No. 4 Part 2, PP. 233A. Meeting Info.: Biennial Scientific Meeting Of The International Association For The Study Of The Liver And The 49TH. Annual Meeting And Postgraduate Courses of the American Association For The, XP002108151 see p. 233A, abstract 282.
Database Chemabs Chemical Abstracts Service, Columbus, Ohio, US An=129:260816,Delforge, Dominque et al; “Designof a synthetic adhesion protein by grafting RGD tailed cyclic peptides on bovine serum albumin” XP002108152 see abstract &Lett. Pept. Sci. (1998), 5(2-3), 87-91 Coden: LPSCEM; issn; 0929-5666, 1998.
Goto, M., The Liver-Cell Specific Drug Delivary System, Nippon Rinsho (Aug. 1994), 52(8):2214-24.

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