Compound and method of treating neurogenic conditions using...

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

Reexamination Certificate

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Reexamination Certificate

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07151084

ABSTRACT:
A complex is provided for the treatment of neurogenic conditions having the formula:where R1isM is a metal ion Ca(II), Mg(II), Cu(II) or Ni(II); n is an integer 1 or 2; R is BBB peptide, transferrin, membrane transporter peptide, TAT peptide, bradykinin, beta-endorphin, bombesin, calcitonin, cholecystokinin, an enkephalin, dynorphin, insulin, gastrin, substance P, neurotensin, glucagon, secretin, somatostatin, motilin, vasopressin, oxytocin, prolactin, thyrotropin, an angiotensin, galanin, neuropeptide Y, thyrotropin-releasing hormone, gonadotropnin-releasing hormone, growth hormone-releasing hormone, luteinizing hormone, vasoactive intestinal peptidegluconate, L-lactate, L-leucine, L-tryptophan, and L-glutamate; and R is coupled to M through a carboxylate moiety. Magnesium(II) represents the preferred metal ion as magnesium is known to have neuroprotective effects. The metal ion is in part chelated by a non-steroidal anti-inflammatory drug that does not inhibit platelet activity and includes salicylate and ibuprofenate. The complex also includes a ligand operative in transport across the blood brain barrier. A process for making an inventive complex includes the stoichiometric addition of ligands containing carboxylate groups to a solution of the metal ion. In instances where the metal ion is magnesium(II), a stoichiometric ratio of 1:1:1 is found between the non-steroidal anti-inflammatory ligand:magnesium(II):transporter ligand.

REFERENCES:
Mojumdar, et al., Chem. Papers, 1999, 53(4), 265-271.
Tamer Fouad, M.D. “New research published this week in The Lancet medical journal suggests that ibuprofen may counteract the antiplatelet activities of aspirin.” www.thedoctorslounge.net, Feb. 16, 2003.
S.C. Mojumdar et al. “Preparation and Properties of Magnesium(II) Compounds with Some Bioactive Ligands” Chem. Papers 53(4)265-271 (1999).
Michael Schmidt et al. “Magnesium Bis[D(-)-Mandelate] Dihydrate and Other Alkaline Earth, Alkali, and Zinc Salts of Mandelic Acid” Z. Naturforsch. 53 b, 1098-1102 (1998).

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