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  Compounds, methods and formulations for the oral delivery of a glucagon-like peptide (glp)-1 compound or a melanocortin-4 receptor (mc4) agonist peptideUSPTO Application #: 20070293423Title: Compounds, methods and formulations for the oral delivery of a glucagon-like peptide (glp)-1 compound or a melanocortin-4 receptor (mc4) agonist peptide Abstract: The present invention relates to novel compounds, methods, and formulations useful for the oral delivery of a GLP-1 compound or an MC4 agonist peptide. (end of abstract) Agent: Eli Lilly & Company - Indianapolis, IN, US Inventors: Louis Nickolaus Jungheim, John McNeill McGill, III, Kenneth Jeff Thrasher, Robert Jason Herr, Muralikrishna Valluri USPTO Applicaton #: 20070293423 - Class: 514012000 (USPTO) Related Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Peptide Containing (e.g., Protein, Peptones, Fibrinogen, Etc.) Doai, Cyclopeptides, 25 Or More Peptide Repeating Units In Known Peptide Chain Structure The Patent Description & Claims data below is from USPTO Patent Application 20070293423. Brief Patent Description - Full Patent Description - Patent Application Claims
BACKGROUND OF THE INVENTION [0001] Conventional means for delivering active agents are often severely limited by biological, chemical, and physical barriers. Typically, these barriers are imposed by the environment through which delivery occurs, the environment of the target for delivery, or the target itself. Biologically or chemically active agents are particularly vulnerable to such barriers. In the delivery to animals of biologically active or chemically active pharmacological and therapeutic agents, physical and chemical barriers are imposed by the body. Examples of physical barriers are the skin and various organ membranes that must be traversed before reaching a target, and examples of chemical barriers include, but are not limited to, variations in pH, lipid bilayers, and degrading enzymes. [0002] These barriers are of particular significance in the design of oral delivery systems. Oral delivery of many biologically or chemically active agents would be the route of choice for administration to animals if not for biological, chemical, and physical barriers such as varying pH in the gastrointestinal (GI) tract, powerful digestive enzymes, and active agent impermeable gastrointestinal membranes. Among the numerous agents which are not typically amenable to oral administration are biologically or chemically active peptides, such as calcitonin and insulin; polysaccharides, and in particular mucopolysaccharides including, but not limited to, heparin; heparinoids; antibiotics; and other organic substances. These agents are rapidly rendered ineffective or are destroyed in the gastrointestinal tract by acid hydrolysis, enzymes, or the like. [0003] Earlier methods for orally administering vulnerable pharmacological agents have relied on the co-administration of excipients or enhancers (e.g., resorcinols and non-ionic surfactants such as polyoxyethylene oleyl ether and n-hexadecylpolyethylene ether) to increase artificially the permeability of the intestinal walls, as well as the co-administration of enzyme inhibitors (e.g., pancreatic trypsin inhibitors, diisopropylfluorophosphate) to inhibit enzymatic degradation. [0004] Liposomes have also been described as drug delivery systems for insulin and heparin. See, for example, U.S. Pat. No. 4,239,754; Patel et al (1976), FEBS Letters, Vol 62, pg. 60, and Hashimoto et al. (1970), Endocrinology Japan, Vol, 26, pg. 337. [0005] However, broad spectrum use of such drug delivery systems is precluded because: (1) the systems require toxic amounts of excipients, enhancers or inhibitors; (2) suitable low molecular weight cargos, i.e. active agents, are not available; (3) they exhibit poor stability and inadequate shelf life; (4) the systems are difficult to manufacture; (5) the systems fail to protect the active agent (cargo); (6) the systems adversely alter the active agent; or (7) the systems fail to allow or promote absorption of the active agent. [0006] More recently, microspheres of artificial polymers of mixed amino acids (proteinoids) have been used to deliver pharmaceuticals. For example, U.S. Pat. No. 4,925,673 describes drug-containing proteinoid microsphere carriers as well as methods for their preparation and use. These proteinoid microspheres are useful for the delivery of a number of active agents. [0007] Delivery agent molecules have also been disclosed in U.S. Pat. Nos. 5,541,155; 5,693,338; 5,976,569; 5,643,957; 5,955,503; 6,100,298; 5,650,386; 5,866,536; 5,965,121; 5,989,539; 6,001,347; 6,071,510; 5,820,881; and 6,242,495; see also WO 02/02509; WO 01/51454; WO 01/44199; WO 01/32130; WO 00/59863; WO 00/50386; WO 00/47188; and WO 00/40203. BRIEF SUMMARY OF THE INVENTION [0008] The present invention relates to a compound of formula I: wherein: [0009] R.sup.1 and R.sup.2 are each independently H, OH, cyano, C.sub.1-C.sub.6 alkyl, C.sub.1-C.sub.6 alkoxy, CF.sub.3, halo or NR.sup.4R.sup.4; [0010] R.sup.3 is H, C.sub.1-C.sub.6 alkyl; [0011] X is a 5 membered aromatic heterocycle that is optionally substituted with C.sub.1-C.sub.4 alkyl; wherein said heterocycle contains at least two or three heteroatoms selected from N, S and O wherein at least one heteroatom must be N; [0012] Y is S, CR.sup.5.dbd.N or N.dbd.CR.sup.5; [0013] n is 2, 3, 4, 5, 6 or 7; [0014] R.sup.4 is H, COR.sup.6, SO.sub.2R.sup.7, or C.sub.1-C.sub.6 alkyl; [0015] R.sup.4 is H or C.sub.1-C.sub.6 alkyl; [0016] R.sup.5 is H or forms a bond with X; [0017] R.sup.6 is H or C.sub.1-C.sub.6 alkyl; and [0018] R.sup.7 is H or C.sub.1-C.sub.6 alkyl; or a pharmaceutical salt thereof. [0019] The present invention further relates to a compound of formula I wherein R.sup.3 is H. This compound is hereafter referred to as a compound of formula II. [0020] The present invention also relates to a pharmaceutical composition containing a compound of formula II, or a pharmaceutical salt thereof, and a pharmaceutical carrier. [0021] The present invention also relates to a pharmaceutical composition containing a compound of formula II, or a pharmaceutical salt thereof, and a GLP-1 compound. [0022] The present invention also relates to a pharmaceutical composition containing a compound of formula II, or a pharmaceutical salt thereof, and a MC4 agonist peptide. Continue reading... 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