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Acyloxyalkyl carbamate prodrugs of sulfinic acids, methods of synthesis, and useAcyloxyalkyl carbamate prodrugs of sulfinic acids, methods of synthesis, and use description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20080242723, Acyloxyalkyl carbamate prodrugs of sulfinic acids, methods of synthesis, and use. Brief Patent Description - Full Patent Description - Patent Application Claims
This application claims the benefit under 35 U.S.C. § 119(e) from U.S. Provisional Application Ser. No. 60/625,050 filed Nov. 3, 2004, which is incorporated herein by reference in its entirety. The disclosure relates to acyloxyalkyl carbamate prodrugs of 3-aminopropylsulfinic acid and analogs thereof, pharmaceutical compositions comprising 3-aminopropylsulfinic acid and analogs thereof, methods of making prodrugs of 3-aminopropylsulfinic acid and analogs thereof, and methods of using prodrugs of 3-aminopropylsulfinic acid and analogs thereof, and pharmaceutical compositions thereof to treat various diseases or disorders. The disclosure also relates to prodrugs of 3-aminopropylsulfinic acid and analogs thereof suitable for oral administration, and for oral administration using sustained release dosage forms. (±)-4-Amino-3-(4-chlorophenyl)butanoic acid (baclofen), (1),
is an analog of gamma-aminobutyric acid (GABA) that selectively activates GABAB receptors resulting in neuronal hyperpolarization. GABAB receptors are located in laminae I-IV of the spinal cord, where primary sensory fibers end. These G-protein coupled receptors activate conductance by K+-selective ion channels and can reduce currents mediated by Ca2+ channels in certain neurons. Baclofen has a presynaptic inhibitory effect on the release of excitatory neurotransmitters and also acts postsynaptically to decrease motor neuron firing (see Bowery, Trends Pharmacol. Sci. 1989, 10, 401-407; Misgeld et al., Prog. Neurobiol. 1995, 46, 423-462, each of which is incorporated herein by reference in its entirety). Many examples of compounds having agonistic or partially agonistic affinity to GABAB receptors exist and include certain amino acids, aminophosphonic acids, aminophosphinic acids, aminophosphonous acids, and aminosulfinic acids. Examples of 4-aminobutanoic acid GABAB receptor ligands include:
4-amino-3-(2-chlorophenyl)butanoic acid;
4-amino-3-(4-fluorophenyl)butanoic acid;
4-amino-3-hydroxybutanoic acid;
4-amino-3-(4-chlorophenyl)-3-hydroxyphenylbutanoic acid;
4-amino-3-(thien-2-yl)butanoic acid;
4-amino-3-(5-chlorothien-2-yl)butanoic acid;
4-amino-3-(5-bromothien-2-yl)butanoic acid;
4-amino-3-(5-methylthien-2-yl)butanoic acid;
4-amino-3-(2-imidazolyl)butanoic acid; and
4-guanidino-3-(4-chlorophenyl)butanoic acid.
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