US2005250701A1PendingUtilityA1

Method of treating the syndrome of coronary heart disease risk factors in humans

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Assignee: CPD LLCPriority: Aug 15, 2000Filed: Jul 15, 2005Published: Nov 10, 2005
Est. expiryAug 15, 2020(expired)· nominal 20-yr term from priority
Inventors:Anton H. Clemens
A61K 31/135A61K 31/4468A61K 38/22A61K 31/4184A61K 31/445A61K 31/27A61K 31/485A61K 31/44A61K 31/5375A61K 38/2278A61K 31/137A61K 38/26A61P 9/00A61K 31/451A61K 45/06A61K 31/64A61K 31/00
62
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Claims

Abstract

The invention provides an improved method of treating a human suffering from one or more conditions included within the Coronary Heart Disease Risk Factor (CHDRF) syndrome. The method includes administering, by a pharmaceutically effective mode, a drug composition having an opioidergic agent including an opiate antagonist, opiate having μ-agonist activity or combination thereof, and an insulin secretagogue.

Claims

exact text as granted — not AI-modified
1 . A method of treating a human suffering from one or more conditions included within Coronary Heart Disease Risk Factor (CHDRF) syndrome, the method comprising administering, by a pharmaceutically effective mode, a drug composition comprising: 
 an opioidergic agent; and    an insulin secretagogue.    
   
   
       2 . The method of  claim 1 , wherein the opioidergic agent is an opiate antagonist, an opiate having μ-agonist activity or a combination thereof.  
   
   
       3 . The method of  claim 2 , wherein the opiate antagonist comprises a single molecular entity.  
   
   
       4 . The method of  claim 2 , wherein the opiate antagonist comprises a combination of molecular entities.  
   
   
       5 . The method of  claim 2 , wherein the opiate having μ-agonist activity comprises a single molecular entity.  
   
   
       6 . The method of  claim 2 , wherein the opiate having μ-agonist activity comprises a combination of molecular entities.  
   
   
       7 . The method of  claim 2 , wherein the drug composition comprises a peripherally acting μ-agonist.  
   
   
       8 . The method of  claim 7 , wherein the drug composition comprises loperamide.  
   
   
       9 . The method of  claim 2 , wherein the drug composition comprises a centrally acting μ-agonist.  
   
   
       10 . The method of  claim 2 , wherein the drug composition further comprises an opiate having mixed μ-agonist and κ antagonist activity.  
   
   
       11 . The method of  claim 10 , wherein the opiate having mixed μ-agonist and κ antagonist activity is buprenorphine.  
   
   
       12 . The method of  claim 2  wherein the opioidergic agent includes at least one of the following: 
 i) dihydromorphine;    ii) morphine;    iii) hydromorphone;    iv) methadone;    v) fentanyl;    vi) sufentanyl;    vii) buprenorphine;    viii) demorphine;    ix) codeine;    x) ethylmorphine;    xi) etonitazene;    xii) hydrocodone;    xiii) levorphanol;    xiv) norcodeine;    xv) normophine;    xvi) (D-Ala 2 -N-Me-Phe 4 -Gly 3 -ol)-Enkephalin (DAMGO); and    xvii) oxycodone.    
   
   
       13 . The method of  claim 2 , wherein the opioidergic agent includes at least one of the following: 
 i) nalmefene;    ii) naltrexone;    iii) nor-binaltorphimine;    iv) (−)-(1R,5R,9R)-5,9-diethyl-2-(3-furylmethyl)-2-hydroxy-6,7-benzomorphan (MR 2266);    v) a triethylenedioxy derivative of B-naltrexamine (TENA); and    vi) guanidylated naltrindole (GNTI).    
   
   
       14 . The method of  claim 2 , wherein the condition included within the CHDRF Syndrome is Insulin Resistance (IR).  
   
   
       15 . The method of  claim 2 , wherein the condition included within the CHDRF Syndrome is Beta-Cell Dysfunction.  
   
   
       16 . The method of  claim 2 , wherein the condition included within the CHDRF Syndrome is Impaired Glucose Tolerance (IGT).  
   
   
       17 . The method of  claim 2 , wherein the condition included within the CHDRF Syndrome is Type 2 Diabetes.  
   
   
       18 . The method of  claim 2 , wherein the condition included within the CHDRF syndrome is overweight.  
   
   
       19 . The method of  claim 2 , wherein the condition included within the CHDRF syndrome is obesity.  
   
   
       20 . The method of  claim 2 , wherein the condition included within the CHDRF syndrome is dyslipidemia.  
   
   
       21 . The method of  claim 1 , wherein the insulin secretagogue includes at least one of the following: 
 i. sulphonylureas;    ii. tolbutamide;    iii. chlorpropamide;    iv. glimepiride;    v. glipizide;    vi. glyburide;    vii. meglitinides;    viii. repaglinide;    ix. pramlintide;    x. morphilinoguanide;    xi. acetylcholine;    xii. muscarinic agonists;    xiii. carbachol;    xiv. bethanechol;    xv. beta-L-glucose pentaacetate;    xvi. chiro-inositol;    xvii. myo-inositol;    xviii. GIP;    xix. GLP-1; and    xx. Extendin-4.    
   
   
       22 . The method of  claim 1 , wherein the insulin secretagogue is a non-glucose dependent insulin secretagogue, the method producing insulin release patterns capable of attaining glucose dependent, bi-phasic release characteristics with reduced likelihood of producing hypoglycemia.  
   
   
       23 . The method of  claim 22 , wherein the insulin secretagogue is sulphonylurea.  
   
   
       24 . A method of treating a human suffering from one or more conditions included within Coronary Heart Disease Risk Factor (CHDRF) syndrome, the method comprising administering, by a pharmaceutically effective mode, a drug composition comprising: 
 an opiate antagonist; and    an insulin secretagogue.    
   
   
       25 . The method of  claim 24 , wherein the opiate antagonist comprises a single molecular entity.  
   
   
       26 . The method of  claim 24 , wherein the opiate antagonist comprises a combination of molecular entities.  
   
   
       27 . The method of  claim 24 , wherein the opiate antagonist includes at least one of the following: 
 i) nalmefene    ii) naltrexone;    iii) nor-binaltorphimine;    iv) (−)-(1R,5R,9R)-5,9-diethyl-2-(3-furylmethyl)-2-hydroxy-6,7-benzomorphan (MR 2266);    v) a triethylenedioxy derivative of B-naltrexamine (TENA); and    vi) guanidylated naltrindole (GNTI).    
   
   
       28 . The method of  claim 24 , wherein the condition included within the CHDRF Syndrome is Insulin Resistance.  
   
   
       29 . The method of  claim 24 , wherein the condition included within the CHDRF Syndrome is Beta-Cell Dysfunction.  
   
   
       30 . The method of  claim 24 , wherein the condition included within the CHDRF syndrome is Impaired Glucose Tolerance (IGT).  
   
   
       31 . The method of  claim 24 , wherein the condition included within the CHDRF syndrome is Type 2 Diabetes.  
   
   
       32 . The method of  claim 24 , wherein the condition included within the CHDRF syndrome is overweight.  
   
   
       33 . The method of  claim 24 , wherein the condition included within the CHDRF syndrome is obesity.  
   
   
       34 . The method of  claim 24 , wherein the condition included within the CHDRF syndrome is dyslipidemia.  
   
   
       35 . The method of  claim 24  wherein the opiate antagonist has IC 50  levels for the μ, δ, and κ opiate receptors, the IC 50  levels being {(IC 50 κ/IC 50 μ)<3} and {(IC 50 κ/IC 50 δ)<3}.  
   
   
       36 . The method of  claim 24 , wherein the insulin secretagogue includes at least one of the following: 
 i. sulphonylureas;    ii. tolbutamide;    iii. chlorpropamide;    iv. glimepiride;    v. glipizide;    vi. glyburide;    vii. meglitinides;    viii. repaglinide;    ix. pramlintide;    x. morphilinoguanide;    xi. acetylcholine;    xii. muscarinic agonists;    xiii. carbachol;    xiv. bethanechol;    xv. beta-L-glucose pentaacetate;    xvi. chiro-inositol;    xvii. myo-inositol;    xviii. GIP;    xix. GLP-1; and    xx. Extendin-4.    
   
   
       37 . The method of  claim 24 , wherein the insulin secretagogue is a non-glucose dependent insulin secretagogue, the method producing insulin release patterns capable of attaining glucose dependent, bi-phasic release characteristics with reduced likelihood of producing hypoglycemia.  
   
   
       38 . The method of  claim 37 , wherein the insulin secretagogue is sulphonylurea.  
   
   
       39 . A method of treating a human suffering from one or more conditions included within the Coronary Heart Disease Risk Factor (CHDRF) syndrome, the method comprising administering, by a pharmaceutically effective mode, a drug composition comprising: 
 an opiate agonist; and    an insulin secretagogue.    
   
   
       40 . The method of  claim 39 , wherein the opiate agonist comprises a single molecular entity.  
   
   
       41 . The method of  claim 39 , wherein the opiate agonist comprises a combination of molecular entities.  
   
   
       42 . The method of  claim 39 , wherein the opiate agonist is a peripherally acting μ-agonist.  
   
   
       43 . The method of  claim 42 , wherein the opiate agonist is loperamide.  
   
   
       44 . The method of  claim 39 , wherein the opiate agonist is a centrally acting μ agonist.  
   
   
       45 . The method of  claim 39 , wherein the opiate agonist includes at least one of the following: 
 i) dihydromorphine;    ii) morphine;    iii) hydromorphone;    iv) methadone;    v) fentanyl;    vi) sufentanyl;    vii) demorphine;    viii) codeine;    ix) ethylmorphine;    x) etonitazene;    xi) hydrocodone;    xii) levorphanol;    xiii) norcodeine;    xiv) normophine;    xv) (D-Ala 2 -N-Me-Phe 4 -Gly 3 -ol)-Enkephalin (DAMGO); and    xvi) oxycodone.    
   
   
       46 . The method of  claim 39 , wherein the condition included within the CHDRF Syndrome is Insulin Resistance.  
   
   
       47 . The method of  claim 39 , wherein the condition included within the CHDRF Syndrome is Beta-Cell Dysfunction.  
   
   
       48 . The method of  claim 39 , wherein the condition included within the CHDRF syndrome is Impaired Glucose Tolerance (IGT).  
   
   
       49 . The method of  claim 39 , wherein the condition included within the CHDRF syndrome is Type 2 Diabetes.  
   
   
       50 . The method of  claim 39 , wherein the condition included within the CHDRF syndrome is overweight.  
   
   
       51 . The method of  claim 39 , wherein the condition included within the CHDRF syndrome is obesity.  
   
   
       52 . The method of  claim 39 , wherein the condition included within the CHDRF syndrome is dyslipidemia.  
   
   
       53 . The method of  claim 39 , wherein the insulin secretagogue includes at least one of the following: 
 i. sulphonylureas;    ii. tolbutamide;    iii. chlorpropamide;    iv. glimepiride;    v. glipizide;    vi. glyburide;    vii. meglitinides;    viii. repaglinide;    ix. pramlintide;    x. morphilinoguanide;    xi. acetylcholine;    xii. muscarinic agonists;    xiii. carbachol;    xiv. bethanechol;    xv. beta-L-glucose pentaacetate;    xvi. chiro-inositol;    xvii. myo-inositol;    xviii. GIP;    xix. GLP-1; and    xx. Extendin-4.    
   
   
       54 . The method of  claim 39 , wherein the insulin secretagogue is a non-glucose dependent insulin secretagogue, the method producing insulin release patterns capable of attaining glucose dependent, bi-phasic release characteristics with reduced likelihood of producing hypoglycemia.  
   
   
       55 . The method of  claim 39 , wherein the insulin secretagogue is sulphonylurea.

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