Method for targeting cells involved in sclerotic and/or...

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

Reexamination Certificate

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C514S776000

Reexamination Certificate

active

11012056

ABSTRACT:
A compound includes a carrier molecule wherein the carrier molecule is linked to a further molecule, wherein the further molecule is at least one cyclic peptide in which the cyclic peptide portion thereof contains at least one sequence encoding a cell receptor recognizing peptide (RRP) and with the proviso that the compound is not a naturally occurring receptor agonist or antagonist. Preferably, the RRP is a receptor specific for Hepatic Stellate Cells (HSC) or a receptor that is up-regulated on HSC during disease. The RFP may be chosen from among a PDGF receptor, a collagen type VI receptor, cytokine receptor(s) such as TGBβ, INFα and interleukinβ. The cyclic portion of the peptide can contain at least one 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 chosen from fibrotic disease, sclerotic disease, and chronic or acute inflammatory processes including glomeruloscherosis, interstitial fibrosis, lung fibrosis, atherosclerosis, rheumatoid arthritis, Crohns disease, colitis ulcerosa, glomerulonephritis and sepsis, and particularly for targeting HSC. Pharmaceutical compositions contain the above-compound(s).

REFERENCES:
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Beljaars et al., The Development of novel albumin carriers to hepatic stellate by application ofcyclopeptide moieties recognizing collage type VI and platelet derived growth factor receptors, HEPATOLOGY, (Oct. 1998) vol. 28, No. 4 Part 2, PP. 313A (Abstract 602) Meeting Info: Biennial Scientific Meeting of the International Association for the Study of the Liver and the 49thAnnual Meeting and Postgraduate Courses of the American Association for the . . . .
Beljaars 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 (Abstract 282) Meeting Info: Biennial Scientific Meeting of the International Association for the Study of the Liver and the 49thAnnual Meeting and Postgraduate Courses of the American Association for the . . . .
Delforge et al., Design of a synthetic adhesion protein by grafting RGD tailed cyclic peptides on bovine serum albumin, Lett. Pept. Sci. (1998) 5(2-3) 87-91 (Chem. Abs. 126:260818).

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