Novel compounds for use in weight loss and appetite suppression in humans

Abstract

Phenolic compounds with a phenolic molecule to which are covalently linked an oxygen-containing group, a nitrogen or another oxygen containing group, and a C 1 -C 4 alkoxy group, obtainable from monocotyledonous plants, or by chemical synthesis, have been found to act as weight loss agents, appetite suppressants, mood enhancers and adjunctive therapy for arthritis, sleep apnea, fibromyalgia, diabetes and hyperglycemia. Additional chemical compounds of the present invention may include benzoxazinoids-cyclic hydroxyamic acids, lactams, and corresponding glucosides, which may serve as precursors to phenolic compounds. The phenolic compounds and precursors of phenolic compounds of the present invention, at concentrations suitable for human therapeutic use, may be obtained from monocotyledonous plants such as corn in their early growth states which are timely harvested for optimum yield.

What is claimed and desired to be secured by United States Letters Patent is:  
     
         1 . A process for promoting weight loss in mammals by the administration of a therapeutically effective amount of one or more chemical compositions defined as:  
       
         
           
           
               
               
           
         
         Wherein “R” represents C 1 -C 4  alkoxy, with the provision the R is in the 4 or 5 ring position;  
         Wherein “n” represents one of the integers 0, 1 or 2;  
         Wherein “B” represents H and “A” represents —OH, —NH 2  or NHCR′, where R′ denotes C 1 -C 4  alkyl; and “B A” represents  
         
           
             
             
                 
                 
             
           
         
         or pharmaceutically acceptable salts thereof.  
       
     
     
         2 . A process as defined in  claim 1 , further comprising the administration of a therapeutically effective amount of one or more chemical compositions defined as:  
       
         
           
           
               
               
           
         
         Wherein “R 1 ” is selected from the group consisting of H and OCH 3 ;  
         Wherein “R 2 ” is selected from the group consisting of H and Glucose (as a glucoside)  
         Wherein “R 3 ” is selected from the group consisting of H, OH, and OCH 3 ; or  
         pharmaceutically acceptable salts thereof.  
       
     
     
         3 . A process as defined in  claim 1 , wherein said administered chemical composition comprises a daily dosage of between about 5 mcg and about 60 mg.  
     
     
         4 . A process as defined in  claim 1 , wherein the administered chemical composition comprises a daily dosage of 15 mg.  
     
     
         5 . A process as defined in  claim 1 , wherein at least one of said chemical compositions is obtained from one or more monocotyledonous plants selected from the group consisting of corn, wheat, barley, rye, oats, rice, sorghum, millet, bamboo, Job's Tears, barley-like grasses, and wild grasses, by growing the plant to an immature life history stage and harvesting the plant.  
     
     
         6 . A process as defined in  claim 5 , wherein said harvested plant is dried.  
     
     
         7 . A process as defined in  claim 6 , wherein said harvested plant is dried at a temperature in the range of between about 40° C. and about 45° C.  
     
     
         8 . A process as defined in  claim 6 , wherein said dried harvested plant contains phenols in total amounts greater than 17.0 mg/gm (dry weight).  
     
     
         9 . A process as defined in  claim 6 , wherein said dried harvested plant contains combined amounts of 4-hydroxycinnamic acid and 4-hydroxy-3-methoxycinnamic acid totaling no more than 1.5 mg/gm (dry weight).  
     
     
         10 . A process as defined in  claim 5 , wherein said harvested plant is immature corn,  Zea mays.    
     
     
         11 . A process as defined in  claim 10 , wherein said immature corn has been grown to a height between about 45 centimeters and about 122 centimeters.  
     
     
         12 . A process as defined in  claim 10 , wherein said immature corn has been grown to a height that does not exceed between about 30 centimeters and about 45 centimeters.  
     
     
         13 . A process as defined in  claim 10 , wherein said immature corn has been grown for less than ten weeks after planting.  
     
     
         14 . A process as defined in  claim 1 , wherein said chemical composition is administered in a manner selected from the group consisting of: (1) orally, in the form of tablets, capsules, suspensions, solutions and other means suitable for ingestion, including sublingual dosage forms; (2) intranasal administration; (3) transmucosal administration; (4) parenteral injection, in the form of subcutaneous, intramuscular, intravenous; (5) implant for sustained release; and (6) transdermal patch.  
     
     
         15 . A process as defined in  claim 1 , wherein therapeutically effective amounts of said chemical composition further comprise adjunctive therapy for a condition selected from the group consisting of arthritis, sleep apnea, fibromyalgia, diabetes, and hyperglycemia.  
     
     
         16 . A process for promoting weight loss in mammals by the administration of a therapeutically effective amount of one or more chemical compositions defined as:  
       
         
           
           
               
               
           
         
         Wherein “R” represents C 1 -C 4  alkoxy, with stipulation that R is in the 4 or 5 ring position;  
         Wherein “n” represents one of the integers 0, 1 or 2;  
         or pharmaceutically acceptable salts thereof.  
       
     
     
         17 . A process as defined in  claim 16 , wherein one of said chemical compositions comprise 6-methoxy-2,3-benzoxazolinone defined as:  
       
         
           
           
               
               
           
         
       
       or pharmaceutically acceptable salts thereof.  
     
     
         18 . A process as defined in  claim 16 , wherein one of said chemical compositions comprise 5-methoxy-2,3-benzoxazolinone defined as:  
       
         
           
           
               
               
           
         
       
       or pharmaceutically acceptable salts thereof.  
     
     
         19 . A process as defined in  claim 18 , wherein said administered chemical composition comprises a daily dosage of between about 5 mcg and about 60 mg.  
     
     
         20 . A process as defined in  claim 17 , wherein the administered chemical composition comprises a daily dosage of 15 mg.  
     
     
         21 . A process as defined in  claim 16 , wherein at least one of said chemical compositions is obtained from one or more monocotyledonous plants selected from the group consisting of corn, wheat, barley, rye, oats, rice, sorghum, millet, bamboo, Job's Tears, barley-like grasses, and wild grasses, by growing the plant to an immature life history stage and harvesting the plant.  
     
     
         22 . A process as defined in  claim 21 , wherein said harvested plant is dried.  
     
     
         23 . A process as defined in  claim 22 , wherein said harvested plant is dried at a temperature in the range of between about 40° C. and about 45° C.  
     
     
         24 . A process as defined in  claim 22 , wherein said dried harvested plant contains phenols in total amounts greater than 17.0 mg/gm (dry weight).  
     
     
         25 . A process as defined in  claim 22 , wherein said dried harvested plant contains combined amounts of 4-hydroxycinnamic acid and 4-hydroxy-3-methoxycinnamic acid totaling no more than 1.5 mg/gm (dry weight).  
     
     
         26 . A process as defined in  claim 21 , wherein said harvested plant is immature corn,  Zea mays.    
     
     
         27 . A process as defined in  claim 26 , wherein said immature corn has been grown to a height between about 45 centimeters and about 122 centimeters.  
     
     
         28 . A process as defined in  claim 26 , wherein said immature corn has been grown to a height that does not exceed between about 30 centimeters and about 45 centimeters.  
     
     
         29 . A process as defined in  claim 26 , wherein said immature corn has been grown for less than ten weeks after planting.  
     
     
         30 . A process as defined in  claim 16 , wherein said chemical composition is administered in a manner selected from the group consisting of: (1) orally, in the form of tablets, capsules, suspensions, solutions and other means suitable for ingestion, including sublingual dosage forms; (2) intranasal administration; (3) transmucosal administration; (4) parenteral injection, in the form of subcutaneous, intramuscular, intravenous; (5) implant for sustained release; and (6) transdermal patch.  
     
     
         31 . A process as defined in  claim 16 , wherein therapeutically effective amounts of said chemical composition further comprise adjunctive therapy for a condition selected from the group consisting of arthritis, sleep apnea, fibromyalgia, diabetes, and hyperglycemia.  
     
     
         32 . A process for suppressing appetite in mammals by the administration of a therapeutically effective amount of one or more chemical compositions defined as:  
       
         
           
           
               
               
           
         
         Wherein “R” represents C 1 -C 4  alkoxy, with the provision the R is in the 4 or 5 ring position;  
         Wherein “n” represents one of the integers 0, 1 or 2;  
         Wherein “B” represents H and “A” represents —OH, —NH 2  or NHCR′, where R′ denotes C 1 -C 4  alkyl; and “B A” represents  
         
           
             
             
                 
                 
             
           
         
         or pharmaceutically acceptable salts thereof.  
       
     
     
         33 . A process as defined in  claim 32 , further comprising the administration of a therapeutically effective amount of one or more chemical compositions defined as:  
       
         
           
           
               
               
           
         
         Wherein “R 1 ” is selected from the group consisting of H and OCH 3 ;  
         Wherein “R 2 ” is selected from the group consisting of H and Glucose (as a glucoside)  
         Wherein “R 3 ” is selected from the group consisting of H, OH, and OCH 3 ; or  
         pharmaceutically acceptable salts thereof.  
       
     
     
         34 . A process as defined in  claim 32 , wherein said administered chemical composition comprises a daily dosage of between about 5 mcg and about 60 mg.  
     
     
         35 . A process as defined in  claim 32 , wherein the administered chemical composition comprises a daily dosage of 15 mg.  
     
     
         36 . A process as defined in  claim 32 , wherein at least one of said chemical compositions is obtained from one or more monocotyledonous plants selected from the group consisting of corn, wheat, barley, rye, oats, rice, sorghum, millet, bamboo, Job's Tears, barley-like grasses, and wild grasses, by growing the plant to an immature life history stage and harvesting the plant.  
     
     
         37 . A process as defined in  claim 36 , wherein said harvested plant is dried.  
     
     
         38 . A process as defined in  claim 37 , wherein said harvested plant is dried at a temperature in the range of between about 40° C. and about 45° C.  
     
     
         39 . A process as defined in  claim 37 , wherein said dried harvested plant contains phenols in total amounts greater than 17.0 mg/gm (dry weight).  
     
     
         40 . A process as defined in  claim 37 , wherein said dried harvested plant contains combined amounts of 4-hydroxycinnamic acid and 4-hydroxy-3-methoxycinnamic acid totaling no more than 1.5 mg/gm (dry weight).  
     
     
         41 . A process as defined in  claim 36 , wherein said harvested plant is immature corn,  Zea mays.    
     
     
         42 . A process as defined in  claim 41 , wherein said immature corn has been grown to a height between about 45 centimeters and about 122 centimeters.  
     
     
         43 . A process as defined in  claim 41 , wherein said immature corn has been grown to a height that does not exceed between about 30 centimeters and about 45 centimeters.  
     
     
         44 . A process as defined in  claim 41 , wherein said immature corn has been grown for less than ten weeks after planting.  
     
     
         45 . A process as defined in  claim 32 , wherein said chemical composition is administered in a manner selected from the group consisting of: (1) orally, in the form of tablets, capsules, suspensions, solutions and other means suitable for ingestion, including sublingual dosage forms; (2) intranasal administration; (3) transmucosal administration; (4) parenteral injection, in the form of subcutaneous, intramuscular, intravenous; (5) implant for sustained release; and (6) transdermal patch.  
     
     
         46 . A process as defined in  claim 32 , wherein therapeutically effective amounts of said chemical composition further comprise adjunctive therapy for a condition selected from the group consisting of arthritis, sleep apnea, fibromyalgia, diabetes, and hyperglycemia.  
     
     
         47 . A process for suppressing appetite in mammals by the administration of a therapeutically effective amount of one or more chemical compositions defined as:  
       
         
           
           
               
               
           
         
         Wherein “R” represents C 1 -C 4  alkoxy, with stipulation that R is in the 4 or 5 ring position;  
         Wherein “n” represents one of the integers 0, 1 or 2;  
         or pharmaceutically acceptable salts thereof.  
       
     
     
         48 . A process as defined in  claim 47 , wherein one of said chemical compositions comprise 6-methoxy-2,3-benzoxazolinone defined as:  
       
         
           
           
               
               
           
         
       
       or pharmaceutically acceptable salts thereof.  
     
     
         49 . A process as defined in  claim 47 , wherein one of said chemical compositions comprise 5-methoxy-2,3-benzoxazolinone defined as:  
       
         
           
           
               
               
           
         
       
       or pharmaceutically acceptable salts thereof.  
     
     
         50 . A process as defined in  claim 47 , wherein said administered chemical composition comprises a daily dosage of between about 5 mcg and about 60 mg.  
     
     
         51 . A process as defined in  claim 47 , wherein the administered chemical composition comprises a daily dosage of 15 mg.  
     
     
         52 . A process as defined in  claim 47 , wherein at least one of said chemical compositions is obtained from one or more monocotyledonous plants selected from the group consisting of corn, wheat, barley, rye, oats, rice, sorghum, millet, bamboo, Job's Tears, barley-like grasses, and wild grasses, by growing the plant to an immature life history stage and harvesting the plant.  
     
     
         53 . A process as defined in  claim 52 , wherein said harvested plant is dried.  
     
     
         54 . A process as defined in  claim 53 , wherein said harvested plant is dried at a temperature in the range of between about 40° C. and about 45° C.  
     
     
         55 . A process as defined in  claim 53 , wherein said dried harvested plant contains phenols in total amounts greater than 17.0 mg/gm (dry weight).  
     
     
         56 . A process as defined in  claim 53 , wherein said dried harvested plant contains combined amounts of 4-hydroxycinnamic acid and 4-hydroxy-3-methoxycinnamic acid totaling no more than 1.5 mg/gm (dry weight).  
     
     
         57 . A process as defined in  claim 52 , wherein said harvested plant is immature corn,  Zea mays.    
     
     
         58 . A process as defined in  claim 57 , wherein said immature corn has been grown to a height between about 45 centimeters and about 122 centimeters.  
     
     
         59 . A process as defined in  claim 57 , wherein said immature corn has been grown to a height that does not exceed between about 30 centimeters and about 45 centimeters.  
     
     
         60 . A process as defined in  claim 67 , wherein said immature corn has been grown for less than ten weeks after planting.  
     
     
         61 . A process as defined in  claim 47 , wherein said chemical composition is administered in a manner selected from the group consisting of: (1) orally, in the form of tablets, capsules, suspensions, solutions and other means suitable for ingestion, including sublingual dosage forms; (2) intranasal administration; (3) transmucosal administration; (4) parenteral injection, in the form of subcutaneous, intramuscular, intravenous; (5) implant for sustained release; and (6) transdermal patch.  
     
     
         62 . A process as defined in  claim 47 , wherein therapeutically effective amounts of said chemical composition further comprise adjunctive therapy for a condition selected from the group consisting of arthritis, sleep apnea, fibromyalgia, diabetes, and hyperglycemia.  
     
     
         63 . A process for promoting weight loss in a mammal by the administration of a therapeutically effective amount of one or more chemical compositions defined as:  
       
         
           
           
               
               
           
         
         Wherein “R 1 ” is selected from the group consisting of H and OCH 3 ;  
         Wherein “R 2 ” is selected from the group consisting of H and Glucose (as a glucoside)  
         Wherein “R 3 ” is selected from the group consisting of H, OH, and OCH 3 ; or  
         pharmaceutically acceptable salts thereof.  
       
     
     
         64 . A process as defined in  claim 63 , wherein said administered chemical composition comprises a daily dosage of between about 5 mcg and about 60 mg.  
     
     
         65 . A process as defined in  claim 63 , wherein the administered chemical composition comprises a daily dosage of 15 mg.  
     
     
         66 . A process as defined in  claim 63 , wherein at least one of said chemical compositions is obtained from one or more monocotyledonous plants selected from the group consisting of corn, wheat, barley, rye, oats, rice, sorghum, millet, bamboo, Job's Tears, barley-like grasses, and wild grasses, by growing the plant to an immature life history stage and harvesting the plant.  
     
     
         67 . A process as defined in  claim 66 , wherein said harvested plant is dried.  
     
     
         68 . A process as defined in  claim 67 , wherein said harvested plant is dried at a temperature in the range of between about 40° C. and about 45° C.  
     
     
         69 . A process as defined in  claim 67 , wherein said dried harvested plant contains phenols in total amounts greater than 17.0 mg/gm (dry weight).  
     
     
         70 . A process as defined in  claim 67 , wherein said dried harvested plant contains combined amounts of 4-hydroxycinnamic acid and 4-hydroxy-3-methoxycinnamic acid totaling no more than 1.5 mg/gm (dry weight).  
     
     
         71 . A process as defined in  claim 66 , wherein said harvested plant is immature corn,  Zea mays.    
     
     
         72 . A process as defined in  claim 71 , wherein said immature corn has been grown to a height between about 45 centimeters and about 122 centimeters.  
     
     
         73 . A process as defined in  claim 71 , wherein said immature corn has been grown to a height that does not exceed between about 30 centimeters and about 45 centimeters.  
     
     
         74 . A process as defined in  claim 71 , wherein said immature corn has been grown for less than ten weeks after planting.  
     
     
         75 . A process as defined in  claim 63 , wherein said chemical composition is administered in a manner selected from the group consisting of: (1) orally, in the form of tablets, capsules, suspensions, solutions and other means suitable for ingestion, including sublingual dosage forms; (2) intranasal administration; (3) transmucosal administration; (4) parenteral injection, in the form of subcutaneous, intramuscular, intravenous; (5) implant for sustained release; and (6) transdermal patch.  
     
     
         76 . A process as defined in  claim 63 , wherein therapeutically effective amounts of said chemical composition further comprise adjunctive therapy for a condition selected from the group consisting of arthritis, sleep apnea, fibromyalgia, diabetes, and hyperglycemia.  
     
     
         77 . A process for suppressing appetite in mammals by the administration of a therapeutically effective amount of one or more chemical compositions defined as:  
       
         
           
           
               
               
           
         
         Wherein “R 1 ” is selected from the group consisting of H and OCH 3 ;  
         Wherein “R 2 ” is selected from the group consisting of H and Glucose (as a glucoside)  
         Wherein “R 3 ” is selected from the group consisting of H, OH, and OCH 3 ; or  
         pharmaceutically acceptable salts thereof.  
       
     
     
         78 . A process as defined in  claim 77 , wherein said administered chemical composition comprises a daily dosage of between about 5 mcg and about 60 mg.  
     
     
         79 . A process as defined in  claim 77 , wherein the administered chemical composition comprises a daily dosage of 15 mg.  
     
     
         80 . A process as defined in  claim 77 , wherein at least one of said chemical compositions is obtained from one or more monocotyledonous plants selected from the group consisting of corn, wheat, barley, rye, oats, rice, sorghum, millet, bamboo, Job's Tears, barley-like grasses, and wild grasses, by growing the plant to an immature life history stage and harvesting the plant.  
     
     
         81 . A process as defined in  claim 80 , wherein said harvested plant is dried.  
     
     
         82 . A process as defined in  claim 81 , wherein said harvested plant is dried at a temperature in the range of between about 40° C. and about 45° C.  
     
     
         83 . A process as defined in  claim 81 , wherein said dried harvested plant contains phenols in total amounts greater than 17.0 mg/gm (dry weight).  
     
     
         84 . A process as defined in  claim 81 , wherein said dried harvested plant contains combined amounts of 4-hydroxycinnamic acid and 4-hydroxy-3-methoxycinnamic acid totaling no more than 1.5 mg/gm (dry weight).  
     
     
         85 . A process as defined in  claim 80 , wherein said harvested plant is immature corn,  Zea mays.    
     
     
         86 . A process as defined in  claim 85 , wherein said immature corn has been grown to a height between about 45 centimeters and about 122 centimeters.  
     
     
         87 . A process as defined in  claim 85 , wherein said immature corn has been grown to a height that does not exceed between about 30 centimeters and about 45 centimeters.  
     
     
         88 . A process as defined in  claim 85 , wherein said immature corn has been grown for less than ten weeks after planting.  
     
     
         89 . A process as defined in  claim 77 , wherein said chemical composition is administered in a manner selected from the group consisting of: (1) orally, in the form of tablets, capsules, suspensions, solutions and other means suitable for ingestion, including sublingual dosage forms; (2) intranasal administration; (3) transmucosal administration; (4) parenteral injection, in the form of subcutaneous, intramuscular, intravenous; (5) implant for sustained release; and (6) transdermal patch.  
     
     
         90 . A process as defined in  claim 77 , wherein therapeutically effective amounts of said chemical composition further comprise adjunctive therapy for a condition selected from the group consisting of arthritis, sleep apnea, fibromyalgia, diabetes, and hyperglycemia.