US 7,402,652 B2
Baclofen conjugate and a pharmaceutical composition for treatment of neuronal disorders
Landon C. G. Miller, 325 Queens City Ave., Tuscaloosa, Ala. 35401 (US)
Filed on Apr. 19, 2005, as Appl. No. 11/109,015.
Application 11/109015 is a continuation in part of application No. 11/023196, filed on Dec. 27, 2004, granted, now 7,074,775.
Claims priority of provisional application 60/609659, filed on Sep. 14, 2004.
Prior Publication US 2006/0058221 A1, Mar. 16, 2006
Int. Cl. C07K 2/00 (2006.01); A61K 38/00 (2006.01); A61K 38/02 (2006.01); C07K 1/00 (2006.01); C07K 1/107 (2006.01)
U.S. Cl. 530—300  [530/333; 530/345; 514/2] 4 Claims
 
1. A conjugate compound having the formula

OG Complex Work Unit Drawing
where R1 is p-chlorophenyl; R is a moiety capable of crossing the blood brain barrier; linker L is interposed between R and the remainder of the compound; and R as a free compound is: serotonin, dopamine, blood brain barrier (BBB) peptide, membrane translocating protein, TAT peptide, penetratin, transportan, 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 peptide, transferrin, glucosylamine, amino saccharin, lactylamine, leucine, tryptophan, glutamate or amino choline;
wherein said linker L has an alkyl backbone of less than eight carbon atoms; and
wherein said alkyl of said linker L backbone is linked to

OG Complex Work Unit Drawing
 of the compound through an ether bond.